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Pharmacology > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What the body does to the drug is ….., and what the drug does to the body is ……

A

pharmacokinetics/ pharmacodynamics

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2
Q

Permeation, which is the movement of a drug through the body, depends on ….., ability to diffuse through lipid barriers, ……., diffusion down a concentration gradient, ….. and ……, important regard to absorption into systemic circulation

A

solubility/ concentration gradient/ surface area/ vascularity

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3
Q

Many drugs are weak acids, like ….., …… and ……, or weak bases, like ….., …… and …….., and can exist in nonionised or ionised forms in an equilibrium, depending on the ph of the environment and pka

A

aspirin/ loop diuretics/ thiazide/ local anesthetics/ amphetamines/ PCP (angel dust)

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4
Q

Only ….. form of drug crosses membrane, while ….. forms are better renally excreted because it’s water soluble

A

non-ionised/ ionised

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5
Q

Ionization …… renal clearance of Drugs, because only free, unbound drug is filtered, either ionise or nonionised drugs, however only …… undergo secretion and reabsorption. Thus, …… drugs are trapped in the filtrate. Acidification of urine increase ionisation of weak ….. and increase renal elimination. Alkalinization of urine increase ionisation of weak ….. and increase renal elimination.

A

increases/ nonionised/ ionised/ bases/ acids

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6
Q

The most rapid route of absorption is …….

A

inhalation

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7
Q

Warfarin and sulfonamide compete for the same protein binding, thus, when taken together it can increase ….. toxicity. Sulfonamides and unconjugated bilirubin also compete for the same protein site, thus when together, it can cause ….. and bilirubin …… in neonates

A

warfarin/ kernicterus/ encephalopathy

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8
Q

There are some special barriers to distribution: placental, in which most ….. molecules can cross, and the blood-brain barrier, which is permeable only for ….-soluble drugs or those transported by facilitated diffusion or active transport. For a drug to be safer during pregnancy it has to be …., …… and/or …..

A

small/ lipid/ large/ water-soluble/ protein-bound

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9
Q

Apparent volume of distribution (Vd) is calculated by= …../…… If the Vd is low, there’s a high amount of drug ……, If the Vd is high, there’s a high amount of drug …… Vd is needed to calculate …… dose in the clinical setting

A

dose/ plasma concentration of drug at 0 time/ bound to plasma proteins/ sequestered in tissues/ loading

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10
Q

There are 2 broad types of biotransformation, phase I and phase II. Phase I is modification of the drug molecule via ….. The microsomal metabolism is made by …… enzymes. The enzyme’s inducers are …., ….., ….., ……, ….. and ….., that increase gene expression and reduce drug availability. The enzyme’s inhibitors are …., ….., ….., ……, ….. and ….., that decrease gene expression and increase drug availability, thus toxicity

A

oxidation/ Cytochrome P450/ smoking/ drinking/ barbiturates/ carbamazepine/ rifampin/ phenytoin (SMOKING and DRINKING in BARB’S CAR RIFS her PHEN)/ Cimetidine/ Omeprazole/ Ketoconazole/ erythromycin/ grapefruit/ protease inhibitors (COKE + GRAPEFRUIT with PI)

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11
Q

There are 2 broad types of biotransformation, phase I and phase II. Phase II is modification of the drug molecule via ……. with endogenous compounds via activity of transferase. The glucuronidation requires the …… transferase, this enzyme can be induced by ….., and has reduced activity in neonates. The lack of this enzyme is responsible for gram baby syndrome due to …… toxicity. It’s deficient in …. or ….., resulting in increased bilirubin. In ….. type II, phenobarbital can be used to induce the enzyme.

A

conjugation/ glucuronosyl/ phenobarbitals/ chloramphenicol/ Gilbert/ Crigler-Najjar/ Crigler-Najjar

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12
Q

There are 2 broad types of biotransformation, phase I and phase II. Phase II is modification of the drug molecule via ……. with endogenous compounds via activity of transferase. The acetylation requires the …… transferase, enzyme that present genotypic variation with fast and slow metabolisers. The slow metabolisers can present with drug induced ….. when taking the drugs …., ….. or ….. The drug- and nondrug-induced lupus have butterfly malar rash and positive ANA, but only drug-induced have ….. antibodies and SLE goes away when drug is stoped

A

conjugation/ acetyl/ lupus/ hydralazine/ isoniazid/ procainamide (HIP)/ anti-histones

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13
Q

The elimination of a drug corresponds to it’s termination of action. A drug can be eliminated by biotransformation to inactive metabolites or excretion via the kidney. In the Zero-Order Elimination rate, the drug is at Vmax, and a constant …. of drug is eliminated per unit time. Thus the rate of elimination is …. of plasma concentration and there’s no fixed ….. The drugs with zero-order elimination are …, ….. and …..

A

AMOUNT/ independent/ half-life/ ethanol/ phenytoin/ aspirin (zero PEAs for me)

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14
Q

The elimination of a drug corresponds to it’s termination of action. A drug can be eliminated by biotransformation to inactive metabolites or excretion via the kidney. In the First-Order elimination rate a constant …. of drug is eliminated per unit time. Thus the rate of elimination is …. of plasma concentration and there’s fixed ….. Most of the drugs are eliminated with first-order elimination.

A

fraction/ dependent/ half-life

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15
Q

Time to reach steady state is dependent only on the …… of a drug. The clinical steady state is reached at ….. t1/2. Increasing the rate of infusion …… the amount of time to reach steady state, but …… the plasma level at steady state

A

elimination half-life/ 4-5/ doesn’t change/ increase

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16
Q

Plasma concentration is directly proportional too the ……, and indirectly proportional to the …..

A

dose/ clearance

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17
Q

It takes 4-5 t1/2 to achieve steady state, but in some situations, a higher dose (……. dose) may be needed to more rapidly achieve effective blood levels. The loading dose = ……

A

loading/ 2x maintenance dose

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18
Q

The ability of a drug two bind to receptor is the ……, shown by the proximity of the curve to the …… axis (if curves are parallel)

A

affinity/ y

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19
Q

The relative doses of 2 or more agonists to produce the same magnitude of effect is ……, shown by the proximity of the curve to the …… axis

A

potency/ y

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20
Q

The measurement of how well a drug produces a response is ……, shown as maximal …… reached by the curve

A

efficacy/ height

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21
Q

Most drugs have ……. antagonism. However, the drugs ….., …… and ….. have …… antagonism

A

competitive/ aspirin/ PPI/ phenoxybenzamine/ non-competitive

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22
Q

In pharmacologic antagonism: 2 agonists acting in ….. receptors.
In physiologic antagonism: 2 agonists acting in ….. receptors.
In chemical antagonism: 2 agonists acting in ….. receptors, they form a complex to reverse the action of the agonist.
In the other hand, the potentiation causes a parallel shift to the ….., due to increase in ….. of agonist

A

1 (same)/ 2/ 0/ left/ potency

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23
Q

Gs proteins increase ….., and such receptors include all …., and the oddballs: …., …., ….. and …..

A

cAMP/ Beta/ D1/ H2/ glucagon/ V2

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24
Q

Gs proteins decrease ….. production, and such receptors include ….., ….. and …..

A

cAMP/ alpha 2/ M2/ D2

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25
Q

Gq proteins are coupled via GTP, which activate ….. Activation of this enzyme release second messengers …. and ….. from membrane phospholipid. The …. induces Ca release, which together with the others activate protein kinase C. Such receptors include Most …. (…, …, …., …., and …..) and …..

A

phospholipase C/ IP3 (inositol triphosphate)/ DAG (diacylglycerol)/ IP3/ 1/ alpha 1/ M1/ V1 (vasopressin)/ AT1 (angiotensin II)/ H1/ M3

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26
Q

Nitric Oxide is synthesised in the endothelial cells and difuse to smooth muscle. It activates guanylyl cyclase, thus increasing …… The …… facilitates the dephosphorylation of the myosin light chains, preventing their interaction with actin thus causing ……. Endogenous compounds acting via NO are ….. and ……. Drugs that activate NO include ……

A

cGMP/ cGMP/ vasodilation/ bradykinin/ histamine/ nitrate

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27
Q

Clearance = …… x …….

A

GFR x Free fraction

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28
Q

Loading dose= ….. x …../ ……

A

Vd x Cp/ f

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29
Q

Maintenance dose = ….. x …..x …../ …..

A

Cl x Css x t/ f

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30
Q

Infusion rate = ….. x …….

A

Css x Cl

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31
Q

Blood pressure = …… x …… An increase in BP results in increase in ……. activity, leading to bradycardia, and decreased ……. activity, leading to decreased heart rate, force of contraction and vasoconstriction. Conversely, a decrease in BP increase …… activity, leading to increase in CO and TPR

A

CO/ TPR/ PANS/ SANS/ SANS

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32
Q

Choline uptake is inhibited by …… Ach is synthesised from ….. and …… via …….. transferase (ChAT)

A

hemicholinium/ choline/ acetyl-CoA/ choline acetyl

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33
Q

Presynaptic membrane depolarisation opens …… channels and the influx on this ion causes fusion of the synaptic vesicle, leading to exocytosis of Ach. ……. prevents this release of Ach

A

Ca/ Botulinum toxin

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34
Q

The muscarinic agonists are (…… drugs) acetylcholine, ……., used to treat ….. and …… retention, ……., used for diagnosis of ……. hyperreactivity, and …… and …….., used to treat ….. and …….

A

chol/ bethanechol (for bowels and bladder)/ ileus/ urinary retention/ bronchial/ pilocarpine/ cevimeline/ xerostomia/ glaucoma

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35
Q

Acetylcholinesterase inhibitors affects mainly PANS, because it is the dominant system. The drugs are: …….., a short-acting drug used for diagnosis of ….., …….., a lipid soluble drug used as an antidote of ……. overdose, …… and …….., a water-soluble drug used to treat …… and reverse the effect of ………., …….. and …… a lipid soluble drug used to treat Alzheimer disease because patients are loosing cholinergic neurons, and last …….., a lipid-soluble irriversible inhibitor used as insecticide

A

edrophonium/ myasthenia gravis/ physostigmine/ atropine/ neostigmine/ pyridostigmine/ myasthenia gravis/ nondepolarizing NM blockers/ donepezil/ rivastigmine/ organophosphate

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36
Q

Toxicity of AChE Inhibitors poisoning are ……..: 10 symptoms

A

DUMBBEELSS/ Diarrhea/ Urination/ Miosis/ Bradycardia/ Bronchoconstriction/ Emesis/ Excitation (CNS, muscle)/ Lacrimation/ Salivation/ Sweating

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37
Q

The treatment of AChE Inhibitors poisonings done with ……, used for everybody, and ……. (……) for the regeneration of AChE regeneration in patients with respiratory difficulty

A

Atropine/ pralidoxime/ 2-PAM

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38
Q

Treatment for acute atropine intoxication is symptomatic and ……

A

physostigmine

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39
Q

Common Muscharinic blockers are ….., the prototype of the class, …….., used for dilating pupil in eye exams, and ……, used in overactive bladder

A

atropine/ tropicamide/ oxybutynin

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40
Q

Ganglion blockers are nicotinic n receptor blockers. The drugs are …… and …….. They reduce the predominant autonomic tone and prevent baroreceptor reflex changes in HR

A

hexamethonium/ mecamylamine

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41
Q

The rate limiting enzyme in the NE synthesis is ……., that convert …… into …….

A

tyrosine hydroxylase/ tyrosine/ Dopa

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42
Q

Metabolism of NE is COMT in the synapse or ……… in the prejunctional nerve terminal

A

MAO A

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43
Q

Using Epi, ….. receptors are more sensitive than …. receptors, thus in low doses, the …. response is dominant and in high doses the ….. response is dominant

A

Beta/ alpha/ Beta/ alpha

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44
Q

Dopamine use in shock in low dose stimulate …. receptors, that increase ……. Increasing the dopamine dose it stimulates then the ….. receptors, increasing ……., And in high doses, it stimulate ….. receptors, causing …….

A

D1/ renal blood flow/ B1/ heart contractility/ alpha 1/ vasoconstriction

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45
Q

Whenever Pulse Pressure goes up, it’s due to …… activation

A

B1

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46
Q

Norepinephrine doesn’t have an effect on ….. receptors, because it’s not innervated, thus it increases BP, by acting in ….. receptors, and increase HR and PP, by acting in ….. receptors. It presents a reflex …….. that overcome the direct effect on receptors

A

B2/ alpha 1/ B1/ bradycardia

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47
Q

B2 specific effects, causes ….. of glucose and FA, and smooth muscle …… (blood vessels, bronchioles and uterus)

A

increase/ relaxation

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48
Q

In order to differentiate high-dose epinephrine from norepinephrine, we can use ……., in Epi the hypertension will be reversed to hypotension. In NE, the hypertension will be reversed to normotension

A

alpha 1-blocker

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49
Q

The indirect-acting adrenergic agonists are: RELEASERS, …, from red wine and cheese, …., for ex. methylphenidate, and ….., old decongestant; and REUPTAKE INHIBITORS, …. and …… These drugs only affect tissues innervated by SANS, and denervated tissues are non responsive

A

tyramine/ amphetamines/ ephedrine/ cocaine/ tricyclic antidepressant

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50
Q

Alpha Antagonists decrease BP and it’s used for …., ….. and ……. The non-selective blockers are ….. and ………, used in pheochromocytoma . The alpha 1 blockers are: …., …… and ……, used for high BP and BPH, and ….. used only for BPH. Selective alpha 2 blocker is …….., used as antidepressant

A

hypertension/ pheochromocytoma/ benign prostatic hyperplasia/ phenoxybenzamine/ phentolamine/ prazosin/ doxazosin/ terazosin/ tamsulosin/ mirtazapine

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51
Q

Chronic use of B blockers leads to receptor ……, thus withdrawal from use needs to tap the dose gradually

A

upregulation

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52
Q

….. can be used in B-blockers overdose, because it’s receptor is Gs and increase cAMP in the heart, having a positive inotropic and chronotropic effect

A

Glucagon

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53
Q

B 2 blockers can precipitate broncho….. and vast….., it decrease production of ……., used in glaucoma. It can also decrease blood ….. and increase blood ….. and ……

A

spasm/ spasm/ aqueous humor/ glucose/ LDL/ TG

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54
Q

The B1 blockers are ….., …… (with no sedation properties) and ……., while the non-selective blockers are …., …… and …… (with high sedation properties). The …… and …… are actually partial agonists, thus they cause minimal change in plasma lipid, less bradycardia

A

acebutolol/ atenolol/ metoprolol pindolol/ timolol/ propranolol/ acebutolol/ pindolol

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55
Q

The B blocker with K-channel blocking activity is ……, while the B blockers with alpha 1 blocker activity are ……. and …….

A

sotalol/ caverdiolol/ labetalol

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56
Q

The ……-angle glaucoma is a chronic condition with increase intraocular pressure due to decreased reabsorption of aqueous humour. It leads to progressive ….. visual loss and if left untreated, blindness. Strategies to treat include ……., to decrease the formation of fluid, ……. agonists and ……. (PG analog) to increase outflow

A

open/ painless/ beta-blockers/ muscarinic/ latanoprost

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57
Q

The ……-angle glaucoma is an acute (…..) condition with increase intraocular pressure due to blockage of the canal of Schlemm. It’s an emergency! Strategies to treat include ……. and ……… to decrease the formation of fluid

A

closed/ painful/ beta-blocker/ carbonic anhydrase inhibitors

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58
Q

The drugs used to treat glaucoma are: ……., a cholinomimetic that increase drainage of fluid, ……, a beta blocker that decrease production of aqueous humour, ……., a CA inhibitor that decrease production of aqueous humour, …….., an osmotic drug that increase fluid drainage, and ……., a PG2 that increase fluid outflow. The ……. drugs and …. agents are contraindicated, due to increase in IOP.

A

Pilocarpine/ Timolol/ acetazolamide/ mannitol/ latanoprost/ antimuscarinic/ alpha 1

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59
Q

Osmotic diuretics are contraindicated in ….. and …… because they draw water from the cells and increase the filling pressure of the heart

A

CHF/ pulmonary edema

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60
Q

The carbonic anhydrase inhibitor drugs are …… and …… They decrease the formation of ….. inside PCT cell, thus decreasing the ….. antiport, increasing ….. and …… in the lumen and therefore diuresis. Their side effects are ….naturia, metabolic ……., hypo…., hyper…., parestesis, renal ….. and sulfonamide hypersensitivity

A

acetazolamide/ dorzolamide/ H+/ Na-H/ Na/ HCO3/ bicarbonato/ acidosis/ calemia/ chloremia/ stones (calcium phosphate stones form in alcaline urine)/

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61
Q

The loop diuretics drugs are ……., …… and …… They block the …… transporter, resulting in decreased intracellular K and decreased reabsorption of …. and …… and increase in diuresis. Their side effects are hypo…. and metabolic ……., hypo…., hypo ….., hyper ……, ….toxicity and sulfonamide hypersensitivity (except ……)

A

furosemide/ torsemide/ ethacrynic acid/ Na-K-2Cl/ Ca/ Mg/ calemia/ alkalosis/ calcemia/ magnesia/ uricemia/ oto/ ethacrynic acid

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62
Q

Drugs that interact with loop diuretics are: ……, enhancing ototoxicity, ……, decreasing its clearance, and ……., due to electrolyte disturbance

A

aminoglycosides/ Lithium/ digoxin

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63
Q

The thiazide drugs are ……., …… and …… They block the …… transporter, resulting in increased ….. and …… excretion and thus increase in diuresis. Their side effects are hypo…. and metabolic ……., hyper…., hyper ….., hyper ……, and hyper ……., and sulfonamide hypersensitivity.

A

hydrochlorothiazide/ chlothalidone/ indapamide/ Na-Cl/ Na/ Cl/ calemia/ alcalosis/ calcemia/ uricemia/ glicemia/ lipemia

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64
Q

Drugs that interact with thiazides are: ……., due to electrolyte disturbance, and avoid in patients with ……

A

digoxin/ diabetes

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65
Q

The K sparing drugs are: Aldosterone-receptor antagonists: ……. and …… ; and Na channel blockers: …… and …… Their side effects are hyper…. and metabolic …….
The drug …… are also antiandorgenic.

A

spironolactone/ eplerenone/ amiloride/ triamterene/ calema/ acidosis/ spironolactone

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66
Q

The drug group used to treat glaucoma, acute mountain sickness and metabolic acidosis is …….. The drug group used to treat heart failure, acute pulmonary edema, hypertension, refractory edema and hypercalemia is …….. The drug group used to treat hypertension, CHF, nephrolithiasis and nephrogenic DI is …….. The drug used to treat hyperaldosterone states, CHF, adjunct to K-wasting diuretics and antiandrogenic use is …….. Last, the drug group used to lithium induced nephrogenic DI and adjunct K-wasting diuretics is ……..

A

CA inhibitor/ loop diuretic/ thiazide/ spironolactone/ Na channels blockers

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67
Q

The first line antihypertensive drug are ….., …… or …… and …….

A

Thiazides/ Angiotensin-Converting Enzyme inhibitors/ Angiotensin Receptor Blockers/ Ca-Channel blockers

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68
Q

The ACEIs drugs are “prils” They block the formation of ……, decreasing ….. and vaso…… They prevent bradykinin degradation. The ARBs block …… receptor, and has the same results as ACEI in BP, but doesn’t interfere in bradykinin degradation. Renin inhibitor is …… that block the formation of ……. and has the same results as ACEI on BP

A

Angiotensin II/ aldosterone/ dilating/ AT1/ aliskiren/ angiotensin I

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69
Q

The ACEIs and ARBs are used for hypertension, CHF and protective of ……. nephropathy. Their side effects are ….. (ACEI), hyper……, acute ……. in renal artery stenosis and …… It’s contraindicated in pregnancy

A

diabetic/ cough/ kalemia/ renal failure/ angioedema

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70
Q

Calcium-channel blockers block Ca channels in heart (…… and …….) and vessels (…….). It can be used to treat hypertension, angina and as antiarrhythmics (….. and ……). Side effects with the divines are …… and ……, and side effects with verapamil is …….

A

verapamil/ diltiazem/ dihydropyridine - dipines/ verapamil/ diltiazem/ tachycardia/ gengival hyperplasia/ constipation

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71
Q

Vasodilators may have specificity, arteriole specific vasodilators are: ……, …….. and …….; and venular specific vasodilator is: …… Orthostatic hypotension results from …… dilation, not …… dilation

A

Ca channel blockers/ K channel openers/ Hydralazine/ Nitrate/ venular/ arteriolar

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72
Q

Beta blockers are not first-line antihypertensives. But are used in hypertensive patients with selective comorbidities such as stable ….., …… and post-….

A

angina/ CHF/ MI

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73
Q

Alpha-1 blockers decrease …. and ….. resistance. It’s used to treat hypertension and BPH. One of its’s side effects is first-dose ….., due to potent vasodilation. An advantage of it’s use is the good effect on ….. profile.

A

arteriolar/ venous/ syncope/ lipid

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74
Q

The alpha-2 agonists drugs are ……. and ……. The cause decrease of …. outflow, thus decrease in …… and ….. It’s used to treat hypertension (drug of choice in pregnancy) and ….. withdrawal (clonidine). Their side effects are positive ….. test due to haemolytic anaemia associated with ….., CNS depression and edema.

A

methyldopa/ clonidine/ sympathetic/ TPR/ HR/ opioids/ Coombs/ methyldopa/

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75
Q

Direct-acting vasodilators drugs acting through Nitric Oxide are …… and ……. The ….. is arteriole specific and one of its most remarcable side effects is …..-like syndrome in slow acetylators. In the other hand, the …… dilates arterioles and venules, used for hypertensive emergency and can cause …. poisoning

A

hydralazine/ nitroprusside/ hydralazine/ lupus/ nitroprusside/ cyanide

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76
Q

Direct-acting vasodilators drugs acting through open K channels are …… and ……. It causes specific …… dilation. It’s used in insulinomas (…..), severe hypertension (…..) and baldness (….). Side effects are. hyper….., hyper……, edema and reflex ……

A

minoxidil/ diazoxide/ arteriolar/ diazoxide/ minoxidil/ minoxidil/ glycemia/ trichinosis/ tachycardia

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77
Q

Chronic (preexisting) hypertension in pregnancy is often treated with ….. and ……., while preeclampsia (new-onset hypertension in pregnancy) is treated with ….. and ……. The prevention and treatment of eclamptic seizures is made with ……..

A

methyldopa/ labetalol/ labetalol/ hydralazine/ magnesium sulfate

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78
Q

To treat cyanide poisoning, first ….. is given to form Methemoglobin, which binds to CN-, forming cyanomethemoglobin. This prevents the inhibitory action of CN- on complex IV of ETC. Cyanomethemoglobin is then converted to thiocyanate, a less toxic ion, by …… Lastly, MetHb is converted to oxyHb with ……

A

nitrite/ thiosulfate/ methylene blue

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79
Q

Indications for use of antihypertensive drugs in comorbid conditions are: angina (….. and ……), diabetes (…… and ……), CHF (……, …… and …..), post MI (…..), BPH (…..), dyslipdemia (….., ……, …… and ….), and Chronic Renal Disease (…… and ……)

A 
Beta blockers/ CCB.    
ACEIs/ ARBs.
ACEIs/ ARBs/ beta blockers.
 beta blockers.
alpha blockers.
ACEIs/ ARBs/ alpha blockers/ CCB.
ACEIs/ ARBs
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80
Q

Treatment of pulmonary hypertension is made using ……, an endothelin-A antagonist promoting vasodilation, …….., a prostacyclin agonist, and ……, that inhibits type V PDE, increases cGMP promoting pulmonary artery relaxation

A

Bosentan/ Epoprostenol/ Sildenafil

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81
Q

Heart failure is a defect in contractility causing decrease in ….. causing increased …… activity and ….. levels, which leads to loss of cardiac myocytes and fibrosis, denominated …… of the heart

A

CO/ SANS/ aldosterone/ remodelling

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82
Q

In the Cardiac Heart Failure, the pharmacotherapy aims to decrease preload: ….., …… and ……, decrease after load: ….., ….. and ……., increase contractility: ….., …… and ……, and decrease remodelling of cardiac muscle (improve survival): ……, ….., …… and ……

A

ARBs/ ACEIs/ venodilators/ ARBs/ ACEIs/ arteriodilators/ digoxin/ beta-agonist/ PDE III inhibitors/ ARBs/ ACEIs/ spironolactone/ B-blockers

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83
Q

…. and ….. are currently drugs of choice for the chronic management of CHF. ….. are more beneficial in management of acute CHF. For chronic therapy in patients who cannot tolerate ACEI or ARB we use ……, to decrease afterload, and ……., too decrease preload.

A

ARBs/ ACEIs/ ionotropes/ hydralazine/ isosorbide dinitrate

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84
Q

Digoxin is an inotropic drug that directly inhibits the cardiac ……… transporter, increase intracellular …., decreasing the activity of ……. exchange transporter, thus increasing intracellular …., increasing contractility. It also indirectly inhibit neural ……… transporter, resulting in increased ….. activity. It has a large Vd, hence it can be displaced by other drugs in the tissue, increasing it’s toxicity, like ….. and ……

A

NaKATPase/ Na/ NaCa/ Ca/ NaKATPase/ vagal/quinidine/ verapamil/

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85
Q

Digoxin is an inotropic drug that can be used to treat ……, …… tachycardias, except …… Early signs of side effects are nausea, anorexia and ECG changes. Later signs include …… and …… effects (blurry vision, yellow green color disturbance). In toxic doses it can cause any cardiac arrhythmias. Management of toxicity use Fab ….. toward digoxin and supportive therapy (electrolytes, antiarrythmics). It intracts with the drugs ……, that waist K, ….. and ……., that displace the drug in the tissue

A

CHF/ supraventricular/ Wolff-Parkinson White syndrome/ desorientation/ visual/ antibodies/ diuretics/ quinidine/ verapamil

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86
Q

The phosphodiesterase inhibitors drugs …… and …… is an inotropic drugs used only in …… CHF. The chronic use increase mortality. It increases cAMP in the heart muscle, increasing inotropy and increases cAMP in the blood vessels, decreasing …….

A

inamrinone/ milrinone/ acute/ TPR

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87
Q

The inotropic drugs that are sympathomimetics are …… and …… are used in ….. CHF only, because chronic use leads to tachyphylaxis

A

dopamine/ dobutamine/ acute

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88
Q

Diastolic dysfunction (CHF with preserved ejection fraction) is best treated with …… and ……

A

B-blockers/ diuretics

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89
Q

In Wolff-Parkinson-White Syndrome, there’s a conduction accessory pathway with fast muscle fibres, does you DO block accessory pathway with …. or ….. anti arrhythmic, and DO NOT slow AV node conduction (avoid ….., …., ….., and …..) that can increase activity of the reentry arrhythmia

A

IA/ III/ digoxin/ Beta-blocker/ CCB/ adenosine

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90
Q

Na channel blockers increase the duration of ventricular ……, thus it prolongs the …… interval.
K channel blockers increase the duration of ventricular ……, thus it prolongs the …… interval.

A

depolarization/ QRS/ repolarization/ QT

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91
Q

Effective Refractory Period (ERP) during the AP corresponds the time when no …… can elicit response. It last until late stage …. of the AP, because Na channels are effectively inactivated. Blockers of K channels prolong the …… Relative Refractory Period (RRP) during the AP corresponds the time when a …… stimulus can elicit response.

A

stimulus/ 3/ ERP/ strong

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92
Q

The rate of recovery of the Na channels is dependent on the resting potential. Recovery slows as membrane voltage ……. The rate of recovery is ….. in ischemic tissues because cells may be partially depolarised at rest.

A

increases/ slower

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93
Q

Class 1 antiarrhythmics block fast …. channels. The class 1A also blocks ….. channels, thus it …… repolarization, ….. AP duration and effective refractory period. One of the drugs is Quinidine, in addition to the above, this drugs also causes …… receptor blockage, which can increase HR and AV conduction, and vasodilation via …….. with possible reflex tachycardia.

A

Na/ K/ prolongs/ increase/ muscarinic/ alpha block/

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94
Q

Quinidine, a class 1A anti-arrhythmic, adverse effects are ……. (GI, ……, occular dysfunction and CNS excitation), hypotension, prolongation of ….. and ….. interval associated with associated with syncope (torsades). It can displace ….. from tissue binding sites, enhancing toxicity and ….. enhances the quinidine effects

A

cinchonism/ tinnitus/ QRS/ Q/ digoxin/ hyperK

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95
Q

Procainamide, a class 1A anti-arrhythmic, has less muscarinic receptor block effect than quinidine, it’s metabolised via N-acetyltransferase, thus, slow acetylators are prone to …….-like syndrome. It’s side effect also involves hematoxicity (….. and …….), besides CV effects (……)

A

lupus/ thrombocytopenia/ agranulocytosis/ torsades

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96
Q

Class 1 antiarrhythmics block fast …. channels. The class 1B block inactivated channels, preferentially the damage partially depolarised tissue. It ….. APD, and ….. diastole and time for recovery. The drugs from this class are: ……., that can’t be used prophylactic, even though it’s the least cardiotoxic of conventional anti-arrhythmics. It needs to be administered ….. and can cause ….. toxicity; a second drug is ……, which has an oral formula and is a back up for ventricular taquicardia

A

Na/ decrease/ increases/ lidocaine/ IV/ CNS/ mexiletine

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97
Q

Class 1 antiarrhythmics block fast …. channels. The class 1C block Na channels, specially Hiss-Purkinje tissue. It has ….. effect on APD and …. AND effects. The drug from this class is ……, limited because of its …… effects, increasing the risk of sudden death.

A

Na/ no/ no/ flecainide/ proarrhythmogenic

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98
Q

Class 2 antiarrhythmics block …. receptors, which would normally increase cAMP. It ….. SA and AV nodal activity, as it works as indirect Ca channel blockers. It can be used as prophylaxis of …… and in ……. tachyarrhythmias. ….. (IV) is used in acute SVTs, due to it’s short t1/2

A

BETA/ decrease/ post-MI/ supra ventricular/ Esmolol

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99
Q

Class 3 antiarrhythmics block …. channels, slowing phase 3 and increasing …. and ……, specially in purkinje and ventricular fibres. The drugs from this class are: ……., that can be used to treat ….. arrhythmia, it’s side effects are …… fibrosis, …… pigmentation of skin, …… dysfunction, …… necrosis and ….. deposits. The other drug is ……., that is also a non-selective ….. blocker, it’s used for life threatening …… arrhythmia, and it’s side effect is …..

A

K/ APD/ ERP/ amiodarone/ any/ pulmonary/ blue/ thyroid/ hepatic/ corneal/ sotalol/ Beta/ ventricular/ tornadoes

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100
Q

Class 4 antiarrhythmics block …. channels, ….. phase 0 and 4, thus ….. SA and AV nodal activity. The drugs of this class are ….. and ……. used for ….. tachycardias. It’s common side effects are …… (verapamil), dizziness, fusing hypotension (vasodilation effects). The can also have additive AV block effect with ….. and …… The drug …… displaces digoxin from tissue-binding sites.

A

Ca/ decreasing/ decreasing/ verapamil/ diltiazem/ SV/ Beta-blocker/ digoxin/ verapamil

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101
Q

Unckassified antiarrhythmics are ……., that activate ….. receptors, causing Gi coupled to decrease cAMP, increase efflux of K, hyperpolarize and cause a transient …… It …… SA and AV nodal activity. It’s the drug of choice for …… tachycardia and ….. nodal arrhythmia. Another unclassified drug is …., used for torsades

A

Adenosine/ adenosine/ assystole/ decrease/ SV/ AV/ magnesium

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102
Q

Antiarrhythmics used for SVT are class …, …., …. and ….. While antiarrhythmics used for VT are class …. and …..

A

II/ IV/ adenosine/ digoxin/ I/ III

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103
Q

Anginal pain occurs when ….. delivery to the heart is innadequate for myocardial requirement. Stable/classic angina is due to coronary …… occlusion. In the other hand, vasospastic or variant angina (Prinzmetal) is due to …… decrease in coronary blood flow

A

O2/ atherosclerotic/ reversible

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104
Q

Drug strategies in stable and vasospastic angina involve: decrease O2 requirement by ….. TPR, CO, or both (….., …… and ……) or increasing O2 delivery by decreasing vasospasm (….. and …..)

A

decreasing/ nitrates/ CCB/ beta blockers/ nitrate/ CCB

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105
Q

Nitrates are prodrugs of ……., it …… guanylyl cyclase, …… cGMP, causing relaxation, thus it acts as a venodilator. The drugs are …….., used sublingual (acute ttx), transdermal (prevention) and IV, the other drug is ……., used oral with extended release for chronic use. It’s side effects are related to the ventilation and drop in BP, like flushing, headache, orthostatic hypotension, reflex tachycardia and fluid retention. It can cause ……. with repeated use and has cardiovascular toxicity with ……

A

NO/ stimulates/ increase/ nitroglycerin/ isosorbide/ tachyphylaxis/ sildenafil

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106
Q

Sildenafil (viagra), ……. or …….. (36h) are drugs that inhibit the PDE 5, present in blood vessels of corpora cavernous. It increase cGMP and thus blood flow. If used with nitrates or others vasodilators, the excessive fall in BP may lead to death from cardiovascular causes. PDE6 in the eyes can cause blue and green ……

A

vardenafil/ tadalafil/ blindness

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107
Q

Beta blockers are used in angina of ….. and are contraindicated in ……… angina

A

effort/ vasospastic/ vasospastic

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108
Q

All calcium channel blockers can be used to treat angina, but …… is important for vasospastic angina.

A

nifedipine

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109
Q

Ranolazine is an antianginal drug that block …. channels, decreasing late inward of …. current in cardiac myocytes, thereby decreasing Ca accumulation. It increases the QT segment, thus it’s contraindicated in patients with long QT syndrome or taking drugs tanta increase QT.

A

Na/ Na

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110
Q

Drugs that decrease mortality in patients with stable angina are ….., …….. and ……. The drug …… is the preferred drug for acute management of both stable and vasospastic angina.

A

aspirin/ nitroglycerin/ beta blockers/ nitroglycerin

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111
Q

The lipid-lowering drugs HMG-CoA reductase inhibitors drugs are the -….. They inhibit the HMG-CoA reductase enzyme resulting in decreased liver ……, resulting in increased …..- receptor expression, thus decrease in plasma …… Plus decrease in VLDL synthesis results in decreased …… Side effects are ……. (check CPK), …… (rare) and …… (check liver function). When administered together, the drug …… can increase risk of rhabdomyolysis, and Cytochrome P450 inhibitors ….. toxicity

A

statins/ cholesterol/ LDL/ LDL/ triglyceridemia/ myalgia; myopathy/ rhabdomyolysis/ hepatotoxicity/ gemfibrozil/ enhance

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112
Q

The lipid-lowering drugs that are Bile Acid sequestrants are …… and ……. They make a complexation of bile acids in the gut, decreasing the …… recirculation of bile salts, increasing the synthesis of new bile salts in the liver, thus decreasing liver cholesterol and increasing LDL receptors to decrease LDL in blood. The side effects are …… disturbances, increase …. and ….. (due to increase bile salt synthesis) and malabsorption of lipid-soluble …… They interact with orally administered drugs due to change in absorption (thiazide, warfarin, digoxin ….) and are contraindicated in ……

A

cholestyramine/ colestipol/ enterohepatic/ gastrointestinal/ VLDL/ triglycerides/ vitamins/ hypertriglyceridemia

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113
Q

The lipid-lowering drug Nicotinic Acid (Niacin, Vitamin B3) inhibits the ….. synthesis, resulting in decreased plasma levels of …. and ….. and increased levels of ….. It’s side effects are flushing, pruritus and burning pain (mediated by …..) that can be treated with aspirin or ibuprofen, hepatotoxicity and hyperglycaemia.

A

VLDL/ VLDL/ LDL/ HDL/ PG

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114
Q

The lipid-lowering drugs Gemfibrozil (older) and Fenofibrate (less muscle effect) bind to bind to Peroxisome Proliferator Activated Receptor (PPAR) alpha increasing the expression of ……. (enzymes found in endothelial cells that breakdown TG). They decrease …. and increase ….. It’s used to treat ……. Their side effects are gallstones and myositis

A

lipoprotein/ VLDL/ HDL/ hypertriglyceridemia

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115
Q

The lipid-lowering drug Ezetimibe prevents intestinal absorption of ……, resulting in lower ….. It’s side effect is ….. distress

A

cholesterol/ LDL/ gastrointestinal

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116
Q

The lipid-lowering drug PCSK9 inhibitors …… and ….. inhibit the hepatic protease PCSK 9 that promotes destruction of ….. receptors. It can lower 50-60% above the achieved by statin therapy alone.

A

Alirocumab/ Evolocumab/ LDL

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117
Q

The drug Orlistat is used for ….. loss. It inhibits the …… lipase, decreasing …. breakdown in the intestine. It’s side effects are steatorrhea, diarrhea and decreased absorption of lipid-soluble ….

A

weight/ pancreatic/ TG/ vitamins

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118
Q

GABAa activation increase ….. influx, and GABAb activation increase ….. efflux. Both mechanisms result in membrane hyperpolarization - inhibitory.

A

Cl-/ K+

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119
Q

Benzodiazepines …… GABA activity (shift dose-response curve to the left), it increase ….. of Cl- channel opening. Have no GABA mimetic activity and act though BZ receptors (part of ….. complex). BZ1 mediate …… and BZ2 mediate …… and everything else.

A

potentiate/ frequency/ GABAa/ sedation/ anxiety/

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120
Q

Barbiturates …… GABA activity, it increase ….. of Cl- channel opening. Have GABA mimetic activity at high doses and have their own binding site on the ….. complex.

A

prolong/ duration/ GABAa/

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121
Q

….. is a non specific BZ receptor antagonists, used to reverse the CNS depression caused by BZ. It cannot reserve the CNS depression caused by ….. and …..

A

Flumazenil/ barbiturates/ alcohol

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122
Q

Important BZ to know are: ……., has an acute onset, used for anxiety, panic and phobias, ……. and ……., long lasting BZ, used for anxiety, sedation and withdrawal states, ……, used for anxiety and sedation and ………, a short lasting BZ used for anesthesia.

A

alprazolam/ diazepam/ clonazepam/ lorazepam/ midazolam

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123
Q

Most of the BZ are metabolised by the liver, however the exception are: …., ….. and ……., that are safer to use in elderly and patients with liver dysfunction

A

Oxazepam/ Temazepam/ Lorazepam (Outside The Liver)

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124
Q

The barbiturates, ……. drug for seizures, are metabolised by the liver and are inducers of ……., leading to a lot of drug interactions. Their used is contraindicated in ……, cause they induce production of porphyrin. Chronic use leads to tolerance and cross-tolerance between BZ, barbiturates and alcohol. Psychologic and physical dependence can occur. Withdrawal sings are rebound …., ….. and ….., that can be life threatening with alcohol (delirium tremens). The management of withdrawal is done using long-acting …..

A

phenobarbital/ cytochrome P450/ porphyrias/ insomnia/ anxiety/ seizures/ BZ

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125
Q

The Non-BZ drugs are ….. and ……., they are ….. receptor agonists. It’s used in sleep disorders and overdose can be reversed with …… It causes less tolerance and abuse liability.

A

zolpidem/ zaleplon/ BZ1/ flumazenil/

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126
Q

The drug Buspirone has no effect on ….. and is a …… partial agonist , used for generalised anxiety disorders, it’s non sedative (not CNS depressant), but takes 1-2 weeks for effect

A

GABA/ serotonin

127
Q

The alcohol ethylene glycol is metabolised by alcohol dehydrogenase into ……… (toxic to the ……), metabolised by aldehyde dehydrogenase into ….. and …….

A

glycoaldehyde/ kidney/ glycolic acid/ oxalic acid/

128
Q

The alcohol methanol is metabolised by alcohol dehydrogenase into ……… (toxic to the ……), metabolised by aldehyde dehydrogenase into …..

A

formaldehyde/ eyes/ formic acid

129
Q

The alcohol ethanol is metabolised by alcohol dehydrogenase into ……… (toxic to the ……), metabolised by aldehyde dehydrogenase into ….. The enzyme aldehyde dehydrogenase can be inhibit by …….. and the antibiotic ……., causing the accumulation of ……., which promotes nausea, vomiting and headache (hangover). Chronic alcoholism cause …..glycemia, …… liver, muscle ……. and ……. (lactates competes with irate for excretion)

A

acetaldehyde/ acetic acid/ disulfiram/ metronidazole/ acetaldehyde/ hypo/ fatty/ waisting/ gout

130
Q

Ethanol is the best substrate for the enzyme alcohol dehydrogenase, thus alcohol intoxications can be treated using …… or …….. (long lasting inhibitor of alcohol dehydrogenase)

A

ethanol/ fomepizole

131
Q

Alcohol withdrawal symptoms can be managed with …… and ….. plus ……. to prevent Wernicke Syndrome.

A

BZs/ thiamine/ folic acid

132
Q

Fetal alcohol syndrome is characterised by …… restriction, mid facial ….., ……cephaly and marked ….. dysfunction, including frequency occurrence of mental retardation.

A

growth/ hypoplasia/ micro/ CNS

133
Q

The Selective Serotonin Reuptake Inhibitors drugs are …., ….., ……, ….. and ……. Their advantages are: safety (high TI), no ANS effect and are non-sedating. They are used in major depression, Obsessive Compulsive Disorder, bulimia, anxiety, PreMenstrual Dysphoric Disorder and Post Traumatic Stress Disorder. Their main side effects are: anxiety, agitation, bruxism, …….dysfuntion and weight loss. It can interact with the drugs ….., ….. and ……., that can cause significant increase in 5HT, causing serotonin syndrome, characterised by sweating, ……, ……, ANS instability and seizures

A

paroxetine/ fluoxetine/ sertraline/ (es)citalopram/ fluvoxamine/ sexual (anorgasmya, reduced libido)/ MAOIs/ TCAs/ meperidine/ rigidity/ hyperthermia

134
Q

Most of the Selective Serotonin Reuptake Inhibitors drugs …… cytochrome P450 enzyme , in particular …… and …… Thus it increase levels of BZs in treatment of anxiety. The drug ….. is safer for this interaction.

A

inhibit/ fluoxetine/ fluvoxamine/ citalopram

135
Q

The Tricyclic Antidepressants drugs are ……, ….. and ……. Their mechanism are nonspecific blockage of …. and …… reuptake. It’s not used very used for depression anymore, nowadays it’s mainly used for ……… (diabetic, shingles) and …… (antimuscarinic). It’s side effects involves the …… blockade, ….. blockade and ….. blockade (sedation). It can cause hypertensive crises when administered with ……., and can cause serotonin syndrome when together with ….., ….. and ……

A

amitriptyline/ imipramine/ clomipramine/ 5-HT/ NE/ neuropathic pain/ enuresis/ Muscarinic/ alpha/ H1/ MAOI/ SSRI/ MAOI/ meperidine

136
Q

The cardio toxicity with TCAs are due to ……. block, …… block (reflex tachycardia), …….. inhibitor and ……. risk

A

muscarinic/ alpha/ NE reuptake/ torsades

137
Q

The Monoamine Oxidase (MAO) Inhibitors drugs are ….. and ……. Their mechanism are irreversible inhibition of MAOa and MAOb. They interact with …., ….. and ….., causing serotonin syndrome. They can also cause hypertensive syndrome (high BP, hyperthermia, excitation and arrhythmia) when together with ….., …… and …….

A

Phenelzine/ Tranylcypromine/ TCA/ SSRI/ meperidine/ tyramine/ alpha agonist/ TCA

138
Q

Other antidepressants are ……., associated with arrhythmias and priapism. ……., a nonselective reuptake blocker with devoid AND effects (differentiate from TCAs), …….., a dopamine and NE reuptake blocker with fewer sexual side effects and also used for smoking cessation, and last the ……, and alpha 2 antagonist, associated with weight gain.

A

Trazadone/ Venlafaxine/ Bupropion/ Mirtazapine

139
Q

Varenicline is a partial agonist of …… receptors and is used for …….

A

nicotinic/ smoking cessation

140
Q

The drug of choice for bipolar disorders is ….., even though antidepressants and antipsychotics are usually required. It works by preventing recycling of …… (decrease ….) by blocking …… monophosphatase. It has a narrow TI, requiring therapeutic monitoring. It’s side effects. involves tremor, hypo…… with …… and ……. (decrease ADH effect- usually treated with amiloride). It is teratogenic, causing ….. abnormality (malformed …… valve)

A

Lithium/ inositol/ PIP2/ inositol/ thyroidism/ goiter/ nephrogenic diabetes insipidus/ Ebstein’s/ tricuspid

141
Q

The drugs used for Attention Deficit Hyperactive Disorder are …….., an amphetamine-like drug, that can cause agitation, restlessness, insomnia and cardio toxicity, and ………, a selective NE reuptake inhibitor, used as a backup drug in the treatment for ADHD

A

Methylphenidate/ Atomoxetine

142
Q

Parkinson symptoms involves ….., muscle ….. and resting ….. The pathology involves the degeneration of nigrostriatal dopamine tracts with imbalance between ….. (decreased) and …… (increased). The pharmacological strategy for Parkinson disease is to restore normal ….. and decrease ….. activity in the striatum.

A

bradykinesia/ rigidity/ tremor/ dopamine/ Ach/ dopamine/ ach

143
Q

One of the drugs Increasing Dopamine Function is ……, a prodrug converted to dopamine by AAAD (dopa decarboxylase). It’s given with ……., that block the periphery conversion to dopamine. It’s side effects are dyskinesia, …… effects (akinesia x dyskinesia), psychosis, ……. (D1 in kidney), and vomiting

A

Levodopa/ carbidopa/ On-Off/ hypotension

144
Q

Two of the drugs Increasing Dopamine Function are …… and ……, drugs that inhibit COMT (periphery and CNS) to increase levels of levodopa. A big advantage is decreased …… effects, makes it makes more dopamine. The drug …… is hepatotoxic.

A

tolcapone/ entacapone/ on-off/ tolcapone

145
Q

One of the drugs Increasing Dopamine Function is ……, a MAOb selective inhibitor (no ….. interactions). It can be used as initial treatment or adjunct to levodopa. Side effects are: ….. (movement disorder when dopamine is excessive), …… (behaviour disorder when dopamine is excessive), ……. (metabolised to amphetamines)

A

Selegiline/ tyramine/ dyskinesia/ psychosis/ insomnia

146
Q

Dopamine-Receptor Agonist drugs are ……. and …… The can be used in restless leg syndrome

A

pramipexole/ ropinirole

147
Q

The drugs used to treat Parkinson that decrease Ach function can be muscarinic antagnoists: …… and ……., or drug that act as muscarinic antagonist and dopamine releaser: …….., that has atropine-like side-effects and …… reticular

A

Benztropine (Park your Bez)/ trihexyphenidyl/ amantadine/ livedo

148
Q

The antipsychotic drugs can block …… receptors (typical antipsychotics) or …….. receptors (atypical antipsychotics). They are used for schizophrenia, schizoaffective states, …… disorder, …… syndrome and …… disease, and for drug and radiation ……..

A

dopamine/ 5HT2/ bipolar/ Tourette/ Huntington/ emesis

149
Q

….. syndrome is a tic disorder with early onset (<21 yo), recurrent, involuntary rapid movements with 1 or more vocal tics.

A

Tourette

150
Q

The Typical Antipsychotic drugs block the …… receptor, the drugs are: ……., ……., ……. and …… These drugs also have M, H1 and alpha 1 blockage effects. The most potent drugs from this class are …… and ……. The most likely drug to cause neuroleptic malignant syndrome is ……., that can be treated with …..

A

D2/ haloperidol (and the zines) / chlorpromazine/ thioridazine/ fluphenazine/ Haloperidol/ Fluphenazine/ Haloperidol/ dantrolene

151
Q

The Atypical Antipsychotic drugs block the …… receptor, the drugs are: ….., ……., ……, ……., ……. and …… These drugs also have M, H1 and alpha 1 blockage effects. The drug ….. can cause ……, thus a weekly blood count is necessary. These drugs can cause hyperglycaemia, increased lipid and weigh gain, specially …….

A

5-HT2/ “apines” and “idones” Clozapine/ Olanzapine/ Risperidone/ Ziprasidone/ Aripiprazole/ Quetiapine/ Clozapine/ Agranulocytosis/ quetiapine

152
Q

Antipsychotic’s side. effects due to dopamine blockage are Acute Extra Piramidal Syndorme: pseudo……, dystonia and akathisia, that can be managed using ……. drugs and Chronic EPS, the …….. (TD - writhing, lip smacking, tongue darting). It can also caused temperature regulating problem, causing the …….. syndrome, treated with ……, increased protecting and eating disorders. Others side effects can be due to muscarinic blockage (tachycardia) and alpha blockage (hypotension).

A

Parkinsonism/ antimuscarinic/ tardive dyskineisa/ neuroleptic malignant/ dantrolene

153
Q

Seizures result from episodic electrical discharges in cerebral neutrons. The goal of drug management is restoration of normal patterns of electrical activity. The mechanisms of action are all CNS ……, by preventing ….. influx, increasing inhibitory tone using ……, decreased excitatory effects of ……. and decrease ….. influx through type T-channels.

A

depressing/ Na/ GABA/ glutamate/ Ca

154
Q

The anticonvulsant ethosuximide is used only in …… seizures (more common in kids)

A

absence

155
Q

Within the primary anticonvulsants, the Phenytoin block ….. channels. It’s used in seizure states. It is a P450 …… and works in ….-order kinetic of elimination. It’s side effects are …… hyperplasia (as Ca blockers), …….. and …….. (interferes with Vitamin D metabolism). It’s teratogenic causing ……

A

Na/ inducer/ zero/ gengival/ hirsutism/ osteomalacia/ cleft lip and palate

156
Q

Within the primary anticonvulsants, the Carbamazepine block ….. channels. It’s used in seizure states, ….. disorders and is the DOC for …… neuralgia. It is a P450 ……, including it’s own metabolism. One outstanding side effect is the increase in …… secretion, causing …… (dilution hyponatremia). It’s teratogenic causing …… and ……

A

Na/ bipolar/ trigeminal/ inducer/ ADH/ SIADH/ cleft lip and palate/ spina bifida

157
Q

Within the primary anticonvulsants, the Carbamazepine block ….. channels. It’s used in seizure states, ….. disorders and is the DOC for …… neuralgia. It is a P450 ……, including it’s own metabolism. One outstanding side effect is the increase in …… secretion, causing …… (dilution hyponatremia). It’s teratogenic causing …… and ……

A

Na/ bipolar/ trigeminal/ inducer/ ADH/ SIADH/ cleft lip and palate/ spina bifida

158
Q

Within the primary anticonvulsants, the Valproic acid block ….. channels, but it also inhibit GABA transaminase and block …. channels. It’s used in seizure states, ….. disorders and for …… prophylaxis. It is …..toxic, specially in young patients and can also cause …… It’s teratogenic causing ……

A

Na/ Ca/ bipolar/ migrane/ hepato/ pancreatitis/ spina bifida

159
Q

Within the primary anticonvulsants, the Ethosuximide block …. channels in thalamic neurons and is used in …… seizures

A

Ca/ absence

160
Q

Within the other anticonvulsants, the Lamotrigine block ….. channels and ….. receptors. It’s used in various seizures. It’s side effect is …… syndrome

A

Na/ glutamate/ Steven-Johnson

161
Q

Within the other anticonvulsants, the Topiramate block ….. channels, ….. receptors and enhance ….. activity. It’s used in seizures and …… prophylaxis. It’s side effect is …… loss

A

Na/ glutamate/ GABA/ migraine/ weight

162
Q

Within the other anticonvulsants, the Felbamate block ….. channels and ….. receptors. It’s used in seizures (usually as adjunct therapy). It’s side effect is ……

A

Na/ glutamate/ aplastic anemia

163
Q

Within the other anticonvulsants, the Gabapentin and Pregabalin block ….. channels and NT release. It’s used in various seizures and ……..

A

Ca/ neuropathic pain

164
Q

Anticonvulsants are addictive with other CNS depressants. Avoid abrupt withdrawal, which may precipitate seizures. It decrease efficacy of oral contraceptive via induction of P450 (…., ….. and …..)

A

phenytoin/ carbamazepine/ phenobarbital

165
Q

In inhaled anesthetic, MAC (minimal alveolar anaesthetic concentration) is a measure of …… The MAC values are additive and are lower in …. patients and in the presence of opiates and sedetaive-hypnotics. The blood-gas ratio determine the rate of ….. (high blood-gas ratio …. onset and …. recovery). The drugs used are ….. and the anes (…… and …….)

A

potency/ elderly/ onset/ slow/ slow/ nitrous oxide/ sevoflurane/ desflurane

166
Q

Midazolam is a benzodiazepine used as intravenous aesthetics for sedation, it causes anterograde ….. and the antidote is …….

A

amnesia/ flumazenil

167
Q

Propofol is used as intravenous aesthetics for induction and maintanance of anesthesia, it has ….. properties and is a ……. and …… depressant

A

antiemetic/ CNS/ cardiac

168
Q

Fentanyl is an opiate used as intravenous aesthetics for induction and maintanance of anesthesia, it can depress ….. function. The antidote is …….

A

respiratory/ naloxone

169
Q

Ketamine is a …..-receptor antagonist used as intravenous aesthetics, it’s a dissociative aesthetic. It’s used for anesthesia induction and cause cardiovascular stimulation and increase ……. pressure. It causes little effect on respiration and it’s used is okay in asthmatics and kids.

A

NMDA/ intracranial

170
Q

The local aesthetics block ….. entry. The drugs come in 2 types, the esters (one eyed), include ……, ….. and …….., which are metabolised by plasma …….; and the amides, include ….., …… and …….., which are metabolised by liver …… All of them are weak bases. One important side effect is ……. to esters via PABA formation.

A

Na/ cocaine/ procaine/ benzocaine/ esterase/ lidocaine/ bupivacaine/ mepivacaine/ amidase/ allergies

171
Q

The toxins …….. (puffer fish) and ……. (red tide) block ….. channels, decreasing ….. influx. The toxins …… (exotic fish) and ……. (frogs), bind to activated ….. channels, prolonging ….. influx

A

Tetrodotoxin/ Saxitoxin/ Na/ Na/ Ciguatoxin/ Batrachotoxin/ Na/ Na

172
Q

The nonionised form of the local anesthetics cross the axonal membrane and the ionised form blocks the inactivated …. channel, preventing propagation of AP. The nerves fibers most sensitive to blockage are of …… diameter and …… firing rates. Thus the order of sensitivity is: ……> touch> …..

A

Na/ small/ high/ pain/ motor

173
Q

The nondepolarizing (competitive) skeletal muscle relaxants are nicotinic ……. and its effect can be reversed using …….. It has no effect on CNS, cardiac and smooth muscle. The drugs are …… (don’t form laudosine, thus don’t cause ……), ……. and ……., that is safer in hepatic and renal impairment, because it spontaneously inactivate to laudosine (can cause …….)

A

antagonist/ AchE inhibitors/ cisatracurium/ seizures/ rocuronium/ atracurium/ seizures

174
Q

The Depolarizing (noncompetitive) skeletal muscle relaxants are nicotinic ……. and its effect can’t be reversed. The drugs is …… and it acts in 2 phases: phase I - ……. and phase 2 - …….. The drug is rapidly metabolised by ……. Cautions related to the drug are atypical …….. (can’t metabolise succinylcholine), …….. and ……

A

agonists/ succinylcholine/ depolarization/ desensitization/ pseudocholinesterase/ pseudocholinesterase/ hyperkalemia/ malignant hyperthermia

175
Q

The Malignant Hyperthermia is a life-threatening syndrome characterised by ……, ……, hypertension, acidosis and hypercalemia. It’s associated with use of Succinylcholine. Genotypic susceptibility may be related to mutations in the genes encoding ……. receptors in SR and/or protein component of ….. channel in skeletal muscle. The treatment is made with ….. that acts directly in the skeletal muscle decreasing contractility by blocking …… release from SR. It’s also used in …… malignant syndrome

A

muscle rigidity/ hyperthermia/ ryanodine/ Ca/ dantrolene/ Ca/ neuroleptic

176
Q

The centrally acting skeletal muscle relaxants are ……., through GABAa receptors and …….. through GABAb receptors. Used to treat spasticity due to acute muscle injury and CNS dysfunction, like MS, stroke and cerebral palsy.

A

benzodiazepines/ baclofen

177
Q

Opioides work presynaptic and postsynaptic through …. coupling to ….. receptor. The presynaptic receptors stimulation decrease ….. influx, decreasing the release of …… (stop pain transmission), while postsynaptic receptors increase …. efflux, hyperpolarizing the membrane decreasing the propagation of pain signal.

A

Gi/ Mu/ Ca/ substance P/ K

178
Q

Morphine is the prototype Mu-agonist that produce analgesia, sedation and CNS depression. It has minimal effects on CV, but ….. (increase histamine release). In smooth muscle it produces GI ….. peristalsis (…..), urinary ……., …… in biliary pressure and miosis. It also have an effect in ….. cough, independent of analgesia and respiratory depression. It can cause nausea and vomiting.

A

vasodilates/ decrease/ constipation/ retention/ increase/ suppress/

179
Q

It’s use is contraindicated in ….. injury (possible increase in intracranial pressure), …… dysfunction (except pulmonary edema), ……. and …… dysfunction (possible accumulation), ….. or ……. deficiencies (exaggerated response) and …… (possible neonatal depression or dependence).

A

head/ pulmonary/ liver/ renal/ adrenal/ thyroid/ pregnancy

180
Q

Opioides full agonists other than morphine are ……., that also have an antimuscarinic function, so it doesnt cause miosis, GI, GU and gallbladder spasms, but can cause tachycardia. It’s metabolised into ……., a SSRI that can cause serotonin syndrome and …..; another full agonist opiodide is ……., with long-lasting activity, it’s used in maintenance of opioid addict; other full agonist is ……., also used as a cough suppressant, often used in combination with NSAID.

A

meperidine/ normeperidine/ seizures/ methadone/ codeine

181
Q

An opioide partial agonist is ……. that can precipitate withdrawal. The new drug ……., uses the mixture of buprenorphine (active when taken orally) with naloxone (active when taken IV) to treat addiction.

A

buprenorphine/ Suboxone

182
Q

Mixed agonists and antagonists opioids are ……. and ……., they work as kappa agonism and mu antagonism. They have analgesic effects but can precipitate withdrawal in patients using full agonists.

A

nalbuphine/ pentazocine

183
Q

Opioides antagonists are ……., (short half life, used to reverse respiratory depression), ……. (used orally to reduce alcohol craving and in opiate addiction) and …… (used to treat opioid-induced constipation since it doesnt cross BBB)

A

naloxone/ naltrexone/ methylnaltrexone

184
Q

Acute toxicity with opioids is characterised by the classic triad: ……, …… and …… Management is made with ….. The abuse of opioids build tolerance, except for …. and ….. And the withdrawal effects are yawning, lacrimation, rhinorrhea, anxiety, sweating, muscle cramps, CNS-pain. It can be managed using …… (Long-lasting opioid) and …… (alpha 2 agonist to reduce sympathetic outflow).

A

pinpoint pupils/ respiratory depression/ coma/ Naloxone/ methadone/ clonidine

185
Q

The Penicillins bind to …….., inhibiting cross-linking (the final steps in cell wall synthesis). They have 3 mechanisms of resistance: ……., change in …… (eg. MRSA) and change in ……. (eg. Pseudomonas). Their activity can be enhanced by combination with beta-lactamase (….., ……). It has a synergic effect when associated with …… against pseudomonas and enterococos. They are weak acids and most are eliminated via active tubular secretion. The secretion can be blocked by ……. and dose reduction is required in major renal dysfunction. A common side effect is ….. and ……. reaction in Syphilis treatment (fever and muscle pain 1 hr after treatment.

A

Penicilin Binding Protein/ Beta-lactamase/ PBP/ porin/ clavulinic acid/ sulbactam/ ahminoglycosides/ probenacid/ hypersensitivity/ Jarisch-Herxheimer

186
Q

They are divided into 4 groups: the Very Narrow Spectrum (anti-…… pens): beta lactamase resistant, composed of the drugs ….., …… and …….., used for skin infections and endocarditis; the Narrow Spectrum, beta lactamase sensitive, composed of the drugs …… and …….., used for strep and treponema pallidum infections; the Broad spectrum, also known as …..penicilins, they are also beta lactamase sensitive, composed of the drugs …… (treat …..) and …….., (treat ……); last, the Very Broad (Extended) Spectrum, also called anti……, beta lactamase sensitive, composed of the drugs …… and ……..

A

staph/ nafcillin/ methicillin/ oxacillin/ Penicillin G/ Penicillin V/ amino/ amoxicillin/ otitis media/ ampicillin/ listeria/ pseudomonas/ piperacillin/ ticarcillin

187
Q

The Cephalosporins mechanisms of action and resistance are the same as penicillins. They are divided into 4 groups: First generation, drugs …… and …….., used for staph MSSA and strep (gram +), they dont enter the CNS; Second generation, drugs ….., …… and ……., with increased gram - coverage, including anaerobic, they dont enter the CNS, except ……; Third generation, drugs …… (IM/IV), …….. (IV) and ……. (VO), used to treat N. gonorrhoea and meningitis, they enter the CNS. Forth generation drug is ……, with very broad spectrum, beta-lactamase resistant. They are also weak acids and mostly eliminated via active tubular secretion. The secretion can be blocked by ……. and dose reduction is required in major renal dysfunction, except ceftriaxone that is largely and eliminated in the ……

A

cephalexin/ cefazolin/ cefaclor/ cefoxitin/ cefuroxime “Its a FACt, I don’t like FOXY, FURry man”/ cefuroxime/ ceftriaxone/ cefotaxime/ cefixime/ cefepime/ probenecid/ bile

188
Q

A side effect of cephalosporins is ……. If there’s a rash reaction to penicillin, the patient …. use cephalosporins, but If anaphylaxis to penicillin, the patient should use …… antibiotics.

A

hypersensitivity/ can/ non-betalactam

189
Q

The organisms not covered by cephalosporins are …. (treat with ….. +- ……), ….. (treat with ….. or ……), ….. (treat with …..)and ….. (treat with ….. +- ……)

A

LAME - Listeria/ Ampicilin/ Gentamycin/ Atypical (Mycoplasma, Chlamydia)/ Tets/ Macs/ MRSA/ vancomycin/ Enterococci/ Ampi/ Genta

190
Q

Third generation cephalosporins are usually the DOC to treat meningitis,, however in neonates, elderly and immunocompromised the drug …… should be added to the treatment in order to cover …….

A

ampicilin/ listeria meningitis

191
Q

Antibiotics that are not adjusted in renal failure are: ….. and ……

A

ceftriaxone/ doxycycline

192
Q

Imipenem and Meropenem have the same mechanism of action as penicillins, but they are …… resistants. They have very very broad spectrum, used in empiric treatment in severe life-threatening infection. Imipenenm is given with cilastatin, that inhibit metabolism of the drug to a …… metabolite. Both have renal elimination, and if imipenem is not adjusted to renal dysfunction, it accumulates and can cause …..

A

Beta-lactamase/ nephrotoxic/ seizures

193
Q

Aztreonam is a B-lactam, with same mechanism of action as penicillins, but they are …… resistants. They are mainly active against gram-…… and has no cross-allergenicity with penicillins and cephalosporins

A

Beta-lactamase/ negatives

194
Q

Vancomycin binds to ……. used to treat ….., ……. and …… (back-up). The resistant strains …… and …… are emerging. Their mechanism of resistance involves change in terminal D-ala to ……. It’s used mainly IV, because it’s nor absorbed orally, thus it’s used to treat …… It’s side effects are …… syndrome (histamine release - need slow infusion over 1 hour), ….. and …… (usually mild, but addictive with other drugs, like aminoglycosides)

A

D-ala terminus/ MRSA/ enterococci/ clostridium difficile/ vancomycin-resistant staphylococcal (VRS)/ enterococcal-resistant staphylococcal (ERS)/ D-lactate/ clostridium difficile/ red man/ ototoxicity/ nephrotoxicity

195
Q

Drugs that INHIBIT CELL WALL SYNTHESIS ARE …., ….., ….., …… and ……

A

penicillin/ cephalosporin/ imipenem, meropenem/ aztreonam/ vancomycin

196
Q

Aminoglycosides (bind to 30S subunit) work via O2 dependent uptake, so ….. are innately resistant to it. Their spectrum include GRAM …. and common drugs are: ……, ……. and ……, often used in combinations. It has an synergic action for infections caused by enterococci (with ……) and P. areuginosas (with extend spectrum …. or …..). The drug ….. is used for TB (back-up). It common side effects are ……, enhanced by vancomycin and amphotericin B, …….., enhanced by loop diuretics, and neuromuscular blockage with decreased release of …….

A

anaerobes/ negative/ Gentamicin/ Amikacin/ Tobramycin/ ampicillin/ penicillin/ 3G cephalosporin/ streptomycin/ nephrotoxicity/ ototoxicity/ Ach

197
Q

Tetracyclines (bind to 30S subunit) are broad-spectrum antibiotics with good action against …., ….. and……. (Rocky Mountain Spotted Fever), …… (Lyme disease) and …… (back up). The drugs are …., ….. and ……. Most of them are excreted by kidney, but …… is excreted by the liver. They can bind to divalent cations (Ca, Mg, Fe) which decrease their absorption. Their side effects are ….. discolouration and decrease …… in children, besides phytotoxicity.

A

Chlamydia/ Mycoplasm/ Rickettsia/ Borrelia/ Treponema/ doxycycline/ tigecycline/ minocycline/ doxycycline/ teeth/ bone growth

198
Q

Antibiotics that can’t be used in pregnancy are ….., ……, …….. and …….

A

aminoglycosides/ fluorquinolones/ sulfonamides/ tetracyclines

199
Q

Drugs with phototoxicity are ……, …… and …..

A

fluorquinolones/ sulfonamides/ tetracyclines

200
Q

Chloramphenicol blocks the enzyme ……. and is mainly a back up drug for …. in pregnancy. It’s use is limited because it is really toxic. It’s metabolised by hepatic glucuronidation, and dose reduction are needed in liver dysfunction and neonates. It’s side effects are dose-dependent …… suppression and ……. syndrome in neonates (low glucuronosyl transferase)

A

peptidil transferase/ Rickettsia/ bone marrow/ gray baby

201
Q

Macrolide drugs are ….., …… and …… They have a wide spectrum, mainly agains gram-……, atypicals (…… and …….), legionella and …… In patients with no comorbidity, the most common bacterias associated with community-acquired pneumonia are C. pneumonia, M. pneumonia and pneumococci (smokers). Thus macrolide is commonly used in treatment of CAP. They can inhibit P450 enzyme, except ….. They also stimulate motilin receptors (used in diabetic …… They increase QT interval, but it rarely cause torsades.

A

Azithromycin/ Erythromycin/ Clarithromycin/ positive/ Chlamydia/ Mycoplasma/ Mycobacterium avian-intracellulare (MAC)/ azithromycin/ gastroparesis/

202
Q

Macrolides are used to treat community-acquired pneumonia, due to it’s activity against gram-…. and ……, however in hospital-acquired pneumonia, the spectrum needs to amplified to cover gram-….., using anti pseudomonas ……. and …….

A

positive/ atypicals/ negative/ penicillins/ 3G cephalosporins

203
Q

Clindamycin has the same mechanism of action and resistance as ……, but it’s not a macrolide. It has a narrow spectrum covering gram-…… (including community acquired …..) and ……. (including B. fragilis). It’s side effect is ……. (most likely cause)

A

macrolide/ positive/ MRSA/ anaerobes/ pseudomembranous colitis

204
Q

Linezolid cover Gram-……., used in the treatment of …… and …… It’s side effect is ….. suppression

A

POSITIVE/ VRSA/ VRE/ bone marrow

205
Q

Quinupristin-Dalfopristin (also called …..) cover Gram-……., used in the treatment of …… and …… (for E. faecium, but not for E. faecalis)

A

streptogramins/ positive/ VRSA/

206
Q

Drugs that INHIBIT PROTEIN SYNTHESIS ARE ….., ……., …., ….., ….., …… and ……

A

Aminoglycosides/ Linezolid/ Tetracyclines/ Chloramphenicol/ Macrolides/ Clyndamycin/ Quinupristin-Dalfopristin

207
Q

The inhibitors of nucleic acid synthesis by inhibiting the folic acid synthesis are ….., ……. and …… Sulfonamides use alone is limited because of multiple resistance, thus it’s used in combination with dihydrofolate reductase inhibitors. Trimethoprim-sulfametoxaole (also called …….) is used to treat ……, …… (back up) and community acquired …. It’s also used to treat ……. infections (most common opportunistic infection in AIDS patients), and also …….. infections (sulfadiazine + pyrimethamine)

A

sulfonamide/ trimethoprim/ pyrimethamine/ cotrimoxazole/ UTI/ listeria/ MRSA/ pneumocystis jirovecii/ toxoplasma gondii

208
Q

Sulfasalazine is a prodrug used in …… and …….. because it is converted into 5-ASA and SulfaPyridine by colonic bacteria

A

ulcerative colitis/ rheumatoid arhtritis

209
Q

Sulfonamides have high protein binding, thus it has a lot of drug interactions and can cause ….. in neonates. It’s side effects are: hypersensitivity (rashes and ……. syndrome - more common in kids), …… in G6PD deficiency and …. In the other hand, trimethoprim and pyrimethamine can cause …… suppression.

A

kernicterus/ Steven-Johson/ hemolysis/ phototoxicity/ bone marrow

210
Q

Direct inhibitors of Nucleic Acid Synthesis are quinolones, ….., …… and others. They inhibit the enzyme ….. (…..) during cell division. It’s used to treat ……, when resistant to cotrimoxazole, STDs, mainly …… (not active against gonorrhea anymore), gram-……. organisms (like shigella, salmonella) and drug-resistant …… It’s absorption is also impaired by Fe and Ca (like ….). Their side effects are …… rupture, ……. (rashes) and is contraindicated in ….. and ….. (inhibition of chondrogenesis)

A

ciprofloxacin/ levofloxacin/ topoisomerase II/ DNA gyrase/ UTI/ chlamydia/ negative/ pneumococci/ tetracycline/ tendonitis, tendon/ phototoxicity/ pregnancy/ children

211
Q

Metronidazole in anaerobes is converted to free radicals that binds to DNA and kill bacteria. It has anti protozoa activity: …., ….. and ……; anti bacterial activity: ……, ….. and …… It’s side effects is ….. taste in mouth and …..-like effect

A

GET BaC to the metro G

Giardia/ Trichomonas/ Entamoeba/ Bacteroides/ Clostridium/ Gardnerella/ metalic/ disulfiram

212
Q

Antibiotics for H. pylori gastric ulcers are: …….., ….., ….. and …..

A

MCAT

Metronidazole/ Clarithromycin/ amoxicillin/ Tetracycline

213
Q

The drugs used to treat TB are …., ……, ……, …… and …..

A

Rifampin/ Isoniazid/ Pyrazinamide/ Ethambutol/ Streptomycin (RESPIre)

214
Q

Isoniazid inhibit ….. acid synthesis. It’s a prodrug requiring conversion by ……. There’s a high level of resistance related to deletions in ….. gene (encodes catalase needed for INH activation). Side effects are …… (age-dependent), peripheral ….. (used Vit B6), …… anaemia (used Vit B6), and ….. in slow acetylators.

A

mycolic/ catalase/ KatG/ hepatitis/ neuritis/ sideroblastic/ lupus-like

215
Q

Rifampin inhibits the DNA-dependent …….. It is a P450 …… and originate …… metabolites

A

RNA polymerase/ inducer/ red-orange

216
Q

Ethambutol cause reduction in ……. acuity and …… discrimination. Pyrazinamide can cause hyper…… and streptomycin can cause …. and ……

A

visual/ red-green/ uricemia/ deafness/ nephrotoxicity

217
Q

Amphotericin B and Nystatin bind to …… to form pores that disrupt fungal membrane permeability. Fungi resistant to these drugs have low …… content in their cell membranes. Amphotericin B has a very large spectrum and it’s used in severe infections. IV infusions has poor penetration into ….. and the side effects related are fever, chills, muscle rigidity and hypotension (….. release). It has a ….. clearance (t1/2 >2 weeks) and it is ….toxic. This side effect can be reduced by drug combination with …… and use of …… amp B. Nystatin is too toxic to be used systemically.

A

ergosterol/ ergosterol/ CNS/ histamine/ slow/ nephro/ flucytosine/ liposomal

218
Q

“Azoles” are antifungicidal and interfere with the synthesis of ergosterol by inhibiting the enzyme ……. The ….. is the DOC for oesophageal candidiasis, coccidiomycoses and cryptococcal meningitis. The …….. is used to treat aspergillosis, that branches in …. degree. The only Azole that penetrate the CNS and can be used to treat meningitis is …… Ketoconazole is an ….. of P450, thus it …. synthesis of steroids, including cortisol and testosterone, caution decrease libido, ginecomastia, mentrual irregularities. Thus it can be used to treat cushing and prostatic cancer

A

14-alpha-demethylase/ fluconazole/ voriconazole/ 45/ fluconazole/ inhibitor/ decrease

219
Q

Flucytosine is activated by fungal cytosine deaminase to ………, which can be incorporated to fungal RNA. 5-FU also forms 5-fluorodexyuridine monophosphate (5-Fd-UMP), which inhibits the conversion of dUMP into …… (decreased ……), decreasing DNA synthesis. It has synergic effect when associated with ……, resistance emerges rapidly If flucytosine is used alone.

A

5-fluorouracil (5-FU)/ dTMP/ thymine/ amp B

220
Q

Griseofulvin is rarely used because it has been replaced by ……., it works by disrupting microtubule structures and has a …..-like effect

A

Terbinafine/ dissulfiram

221
Q

Terbinafine is active only against ……. by inhibiting the enzyme ……, decreasing ergosterol. It’s superior to griseofulvin in treatment of ……

A

dermatophytes/ squalene epoxidase/ onychomycoses

222
Q

The echinocandins (caspofungin and other “fungins”) inhibit the synthesis of beta-1,2 gluten, a critical component of the fungal …… They are back-drug given IV for disseminated …… infection or invasive …..

A

cell wall/ Candida/ aspergillosis

223
Q

Acyclovir is a prodrug nucleoside that is monophosphorylated by viral ………, then bio activated by host-cell kinase to triphosphate. It is incorporated into DNA molecule and act as a chain terminator because it lacks the equivalent of ……. group. Resistance can be due to decreased activity of …… This drug is used to treat ….. virus and …… virus. Their common side effect are crystalluria and …..toxicity. It is not hematoxic.

A

thymidine kinase/ ribosyl 3’hydroxyl/ thymidine kinase/ herpes simplex/ varicella-zoster/ neuro

224
Q

Ganciclovir has a similar mechanism as acyclovir, it’s used to treat …., ….. and …… (retinitis in AIDs patients) viruses. It’s mostly used in prophylaxis and treatment of ….. infections. It’s most important side effect is dose-limiting ……

A

HSV/ VZV/ CMV/ CMV/ hematoxicity (leukopenia, thrombocytopenia)

225
Q

Foscarnet is already active and don’t need phosphorylation to work. It’s use is identical to ganciclovir, but it increases the activity against ……-resistant strains of HSV. It’s use is limited by the dose-limiting ……toxicity, with electrolyte electrolyte imbalance with …….

A

acyclovir/ nephro/ hypocalemia

226
Q

Nucleoside reverse transcriptase inhibitors (NRTIs) are component of drug combinations used in HIV infections. The prototype drug is ….. (…), it’s side effect is ….., which is the major dose limiting. Others NRTIs have the same mechanisms or action and resistance, but differ in their toxicity. As …… (DDI), it’s limiting side effect is ….. And the cytosine derivatives …… (3TC) and …….. (FTC), the least toxic of the NRTIs. There’s no complete cross-resistance between NRTIs.

A

zidovudin/ AZT/ hematotoxicity/ didanosine/ pancreatitis/ lamivudine/ emtricitabine

227
Q

The nonnucleoside reverse transcriptase inhibitors (NNRTIs) do not require metabolic activation. The drugs are ….. and …….. They are not myelosuppressant and have additive or synergistic effect in combination with NRTIs and/or PI

A

nevirapine/ efavirenz

228
Q

The drug …… is a NtRTI that has a single phosphate on its sugar and must be further phosphorylated to the triphosphate form

A

Tenofovir

229
Q

Aspartate protease (encoded by …. gene) is a HIV viral enzyme that forms the proteins of the mature virus core. This enzyme is inhibited by Protease Inhibitors. Resistance occurs via point mutations in the …… gene. And there’s no complete cross-resistance between different PIs. The drugs are …. and others -…. They are -450……, and thus work as boosts increasing level of the others PI. It causes syndrome of disorders lipid and CHO metabolism with central adiposity and insulin resistance.

A

pol/ pol/ Ritonavir/ avirs/ inhibitors/

230
Q

Integrase inhibitors prevents integration of viral genome in host cell DNA. Example of this drug is …..

A

Raltegravir

231
Q

Fusion inhibitors drugs block the entry of HIV virus into cells. For example: ….. and ……

A

Efuvirtine/ Maraviroc

232
Q

…. and ……. inhibit neuraminidase of …… and ….. (enzyme that prevent clumping of the viral so more particles are available for infecting host cells). It decreases the likelihood that the virus will penetrate uninfected cells. It’s used for prophylaxis mainly but may also decrease duration of flu symptoms.

A

Zanamivir/ Oseltamivir/ influenza A/ influenza B

233
Q

Ribavirin inhibit RNA polymerase and is used in adjunct to …… in hep C treatment and in management of severe cases of …… virus infection. It is …..toxic

A

alpha-interferon/ respiratory syncytial/ hemato

234
Q

Sofosbuvir is a nucleotide analog that inhibits …… used in the treatment of ……, in combination with ribavirin or alpha interferon.

A

RNA polymerase/ Hep C

235
Q

Treatment for toxoplasmose is made with ……. and …….

A

sulfadiazine/ pyrimethamine

236
Q

The Antimalarial treatment choice depends on the region. In chloroquine-sensitve regions, the prophylaxis is made using ….., and treatment for all types is made with ……, added with …… for P. vivax and ovale. In chloroquine-resistant regions, the prophylaxis is made using ….., and treatment is made with …… +/- ….. or ……. Side effects of primaquine and quinine is haemolytic anemia in ….., and ….. (quinine)

A

chloroquine/ chloroquine/ primaquine/ mefloquine/ quinine/ doxycycline/ clindamycin/ G6PD deficiency/ cinchonism (visual problems, tinnitus and GI symptoms)

237
Q

The P. falciparum is the most serious malaria infection. Thus, even in chloroquine-sensitive regions, their resistance to chloroquine is high, and ….. or ….. is added to treatment.

A

artesunate/ artemether

238
Q

Most nematodes (worms) are treated with ……. (decrease glucose uptake and microtubular structure) and …… pamoate (Nm agonist causing spastic paralysis). Most cetodes (tapeworms) and trematodes (flukes) are treated with ……. (increase Ca influx and vacuolisation)

A

albendazole/ pyrantel/ praziquantel

239
Q

Histamine is release from mast cells and basophils. The H1 activation is coupled to …. protein and increase capillary dilation, capillary permeability, bronchoconstriction and activation of peripheral nociceptive receptors. The H2 activation is coupled to …. protein and increase ….. secretion. All the H antagonists require ….. metabolism and most can cross the …….

A

Gq/ Gs/ gastric acid/ liver/ placenta

240
Q

The first generation antihistamines are ….., ….., …… and …… They all can block …… receptor, cross CNS to cause sedation and has anti….. properties. The second generation antihistamines are ….., …… and …… They are used to treat allergy reactions, motion sickness and vertigo (1st generation), nausea and vomiting in pregnancy. Their side effects are relative to M block and sedation.

A

diphenhydramine/ promethazine/ chlorpheniramine/ meclizine/ muscarinic/ motion/ cetirizine/ loratadine/ fexofenatidine

241
Q

Zollinger-Ellison syndrome is a tumor that hyper secrete ……, leading to increase in ….. release from ECL cells, thus increasing acid in stomach

A

gastrin/ histamine

242
Q

H2 antagonists drugs are ….., …… and …….. They suppress the secretory response by their ability to indirectly decrease activity of proton pump. It’s used in ….., ……. and …….. syndrome (PPI are better). Their side effects are related to cimetidine, a major P450 ……, leading to drug interactions, and decreasing of androgens, causing ginecomastia and decreased libido (like …..)

A

cimetidine/ ranitidine/ famotidine/ PUD/ GERD/ Zollinger-Ellison/ inhibitor/ ketoconazol

243
Q

Proton Pump inhibitors are ….. and the -prazoles. They are ….. (long lasting) direct inhibitors of PPI in the gastric parietal cells. They are more effective than ant H2 in the treatment of ….., ….. and ….. syndrome

A

omeprazole/ irreversible/ PUD/ GERD/ Zollinger-Ellison

244
Q

Misoprostol is a …… analog that increase ….. and ….. secretion and decrease …… secretion. It was previously used for NSAID-induced ulcers, but PPI are now used.

A

PGE1/ mucus/ bicarbonate/ HCl

245
Q

…… and ……. subsalicylate create a gel-like coating of ulcer beds. However …… require acid ph to work, thus antacids may interfere it’s activity. The ….. may be used combined with metronidazole and tetracycline to erradicate H. pylori.

A

Sucralfate/ Bismuth/Sucralfate/ Bismuth

246
Q

The antacids are …., ….. and ….. that neutralise protons in the gut. Their side effects are: …… (Al+++), …… (Mg++) and …….. They will ….. oral absorption of weak bases (ex. quinidine), ….. oral absorption of weak acids (ex. warfarin) and ….. oral absorption of tetracycline (via chelation)

A

Al(OH)3/ Mg(OH)2/ CaCO3/ constipation/ diarrhea/ rebound hyperacidity/ increase/ decrease/ increase

247
Q

Drugs for Nausea and vomiting are 5HT3 antagonists: ……. and ……., DA antagonist (like typicals antipsychotics): …….. and …….., H1 antagonists (enters CNS and block Musc receptors): ……, …… and ……, Muscarinic antagonist: …….., Cannabinoids agonist: ……., and NK1-receptor (substance P receptor) antagonist: …….

A

ondansetron/ granisetron/ prochlorperazine/ metoclopramide/ diphenhydramine/ meclizine/ promethazine/ scopolamine/ dronabinol/ aprepitant

248
Q

Opioides have duality action related to emesis, they decrease emesis by decreasing ….. transmission, but increase emesis by …… receptors in chemoreceptor trigger zone (CTZ)

A

pain/ stimulating

249
Q

Serotonin is synthesised and stored in ….. cells, ….. and …… It’s metabolised by MAO type A, it’s metabolite is ……, a marker of carcinoid.

A

GI/ neurons/ platelets/ 5HIAA

250
Q

The drug ….. is a partial agonist of the 5HT1a receptor, used to treat chronic anxiety. While the drug ….. and others …. are agonist of 5HT1d receptors in cerebral vessels, used to treat acute migraine.

A

buspirone/ sumatriptan/ triptans

251
Q

The drug ……. and other atypical antipsychotics are 5HT2a antagonists, used to decrease symptoms of psychosis. The drug ……is a 5HT2 antagonist, used in carcinoid and serotonin syndrome.

A

Olanzapine/ Cyproheptadine

252
Q

Sumatriptans and other triptans new agonist ….. used in acute migraine treatment. …… is a partial alpha and 5HT2 agonist used as a back up treatment of acute migraine, due to its vasoconstrictive properties, it possible side effect is due to prolonged vasoconstriction leading to ….. and gangrene, and abortion near term.

A

5HT1d/ ergotamine/ ischemia

253
Q

…… is a uterine smooth muscle contraction given IM after placenta delivery.

A

ergonovine

254
Q

Prostaglandins are protective in the ……, dilate ….. vasculature, contract uterus and maintain the …… Thromboxane causes platelet ……. GI PG and platelets TxA2 are synthesised by COX 1 (constitutive - always ON), COX 2 is induced by inflammation, and both enzymes synthesise …. PG

A

stomach/ renal/ ductus arteriosus/ aggregation/ renal

255
Q

Leukotrienes (LTs) are formed from action of lypoxygenase on arachidonic acid. The LT…. is an inflammatory mediator and LT….. plays an important role in asthma. Leukotrienes are target of the following drugs: ……… (decrease phospholipase A2 acivity), …….. (inhibits lipoxygenase) and …… and “-…..” (LT receptor antagonist)

A

B4/ D4/ glucocorticoids/ Zileuton/ Zafirlukast/ lukasts

256
Q

Protaglandins (PGs) are formed from action of cycloxygenase (COX) on arachidonic acid. PGE1 drugs are ……, previously used in ttx of NSAID-induced ulcer, and …….., maintains latency of ductus arteriosus and can be used in male impotence. They are contraindicated in pregnancy unless as an abortifacient. PGE2 drug is …… used as abortifacient.

A

misoprostol/ alprostadil/ dinoprostone

257
Q

PGF2alpha main drug is ……, used to treat glaucoma, because it helps to drain fluid more effectively. PGI2 (prostacyclin) drug is …… (oldest ttx for pulmonary hypertension). PGE2 and PGF2 are increase in primary …….

A

latanoprost/ epoprostenol/ dysmenorrhea

258
Q

Thromboxane (TXA2) is a platelet ……, thus the use of aspirin post MI is a protective role to inhibit this synthesis.

A

aggregator

259
Q

Acetylsalicylic Acid (ASA; aspirin) cause ….. inhibition of COX. At low dose, it has ……. property, at moderate dose, it has …. and ….. effect, and at high dose, it has …. effect. It can lead to hyper….., due to secretion in OAT of proximal tubule. At high therapeutic dose, it creates uncoupling with oxidative phosphorylation, …. respiration and …. CO2, causing respiratory ….. In toxic doses it inhibits the respiratory centre, causing respiratory ……, then metabolic ….. and hypo…..

A

irreversible/ antiplatelet aggregation/ analgesia/ antipyresis/ anti-inflammatory/ uricemia/ increasing/ decreasing/ alkalosis/ inhibition/ acidosis/ calemia

260
Q

Acetylsalicylic Acid (ASA; aspirin) side effects are:
1) gastritis and GI ……
2) ….. loss and tinnitus (often first sings of toxicity)
3) exacerbation of …… (bronchoconstriction)
4) ….. syndrome (kids with viral infection taking aspiring: ……, …… and …..)
5) …. bleeding Time (no effect on PT)
6) Chronic use is associated with ….. dysfunction
To treat overdose there’s no specific antidote. If recent intake, make a gastric lavage +/- charcoal. If a long time after intake, increase urine volume and …… of urine facilitate salicylate renal elimination.

A

bleeding/ hearing/ asthma/ Reye/ vomiting/ lethargy/ fever/ increase/ renal/ alkalinization

261
Q

NSAIDs other than aspirin are ……. inhibitors of COX 1 and 2. The drugs are …., ……. (longer t1/2), …… (closing PDA and gout), ……. (more potent) and …… (safer for kidneys). They produce ….. GI irritation than ASA, and has minimal acid-base effects. Allergy is common and chronic use can cause nephritis, except with ……. The drugs …. and ….. cause bone marrow suppression. The NSAIDs are associated with an increased risk of adverse cardiovascular thrombotic events.

A

reversible/ ibuprofen/ naproxen/ indomethacin/ ketorolac/ sulindac/ less/ sulindac/ indomethacin/ sulindac

262
Q

The selective COX2 inhibitor: ……. is equally effective to NSAIDs as anti-inflammatory agent. Gowever it has less …….. toxicity and ….. action. It may possibly exert prothrombotic effects (MI and strokes). It present cross-hypersensitivity with …..

A

GI/ antiplatelet/ sulfonamides

263
Q

Acetaminophen causes no inhibition of cox in ….. tissues and lacks anti-inflammatory effects. It has equivalent analgesic and antipyretic activity to ASA due to inhibition of COX in ….. It has no anti platelet effect, not implicated in …. syndrome, no effects on uric acid and cause no bronchospasm (safe in NSAID hypersensitivity and asthma).

A

peripheral/ CNS/ Reye

264
Q

Acetaminophen is metabolised mainly by liver glucuronyl transferase to form inactive conjugate. A minor pathway via …… results in formation of reactive metabolite (…..), which is inactivated by ….. (GSH). In overdose situations, the finite store of GSH is depleted causing liver failure. Chronic use of ethanol enhances liver toxicity due to induction of ….. Management of the hepatotoxicity is done with ……. (sulus -SH group), preferably within first 12 hours (liver damage is irreversible)

A

P450/ NAPQI/ glutathione/ P450/ N-acetylcysteine

265
Q

Reumathoid arthritis is marked by morning ….., ….. arthritis and positive …… The therapeutic goals of the treatment are: decrease pain and swelling with ….. and slow disease with ….. (slow onset). The DMARD first choice usually is ….., a side effect of this drug when used in high doses to treat cancer is ….toxicity, and ….toxicity when used chronically to treat RA.

A

stiffness/ symmetric/ Rheumatoid Factor/ NSAIDs/ DMARDs/ methotrexate/ hemato/ hepato/

266
Q

Drugs first choice to treat RA is ……, the drug ….. and …… can be used to treat mild disease. Both of them cause hemolysis in patients with ……, but only …… cause cinchonism (…., ….. and …..). The drugs used to treat severe disease are ….., …… and ……, they stop TNF and a common side effect is infection.

A

methotrexate/ hydroxychloroquine/ sulfasalazine/ G6PD deficiency/ hydroxychloroquine/ tinnitus/ visual dysfunction/ GI distress/ etanercept/ infliximab/ adalimumab

267
Q

The treatment of Gout involves …… for Acute Inflammatory Episodes, or ….. and intra-articular …. as alternatives. Colchicine is a back-up drug which decrease ……. polymerisation. Chronic Gout is used prophylactic and aims to reduce uric acid pool. The drugs used are …… or ……., that inhibit uric acid production by inhibiting xanthine oxidase (thus inhibit the metabolism of 6-mercaptopurine), which leads to increase of ……

A

NSAIDs/ colchicine/ steroids/ microtubular/ allopurinol/ febuxostat/ hypoxanthine

268
Q

Other drugs used to treat chronic gout are ……, an urate-oxidase enzyme that metabolises uric acid to allantoin, used in refractory gout; and ……., that inhibit proximal tubule reabsorption of rate, but it’s inner]fective if GFR < 50. Another drug that is also an irate-oxidase enzyme, used in the prevention of tutor lysis syndrome, but not to treat gout is …….

A

Pegloticase/ Probenecid/ Rasburicase

269
Q

Glucocorticoids inhibit Phospholipase A2, decreasing …. and ……, it also decrease expression of COX …, used as anti-inflammatory and immunosuppressive. It has a lot of side effects, like suppressing …… (malaise, myalgia, arthralgia, fever and shock with abrupt withdrawal); Iatrogenic …… syndrome (fat deposition, muscle weakness, bruising, acne), hyperglycaemia due to increased …….., osteoporosis, …… GI acid, electrolyte imbalance (Na/ water retention), …… cataracts and glaucoma, and ….. wound healing.

A

PGs/ LTs/ 2/ ACTH/ cushingoid/ gluconeogenesis/ increased/ increased/ decreased

270
Q

Drugs used to treat asthma are Beta Agonists: ……, meta….., …… and …… (longer-action); Muscarinic Blockers (specially in COPD patients) are ….. and ……., they are safer than B-agonists in patients with CV disease and is the drug of choice in bronchospasm caused by ……; Theophylline is the most dangerous drug, due to low ….. and many drug interactions, it bronchodilates via inhibition of ……. and by antagonism of ……

A

albuterol/ proterenol/ terbutaline/ salmeterol/ B-blockers/ TI/ PDE/ adenosine

271
Q

The drugs used to treat asthma called …… and ……. prevent degranulation of pulmonary mast cells and decrease release of histamine and LT from inflammatory cells.
…… is an IgE Ab that works like cromolyn, given SC for severe patients.

A

Cromolyn/ Nedocromil/ Omalizumab

272
Q

In asthma, glucocorticoids block mediator release, decreasing bronchial hyperreactivity and inflammation. There are some surface active drugs like …… and …… used via inhalation for acute attacks and prophylaxis. Low dosage may also prevent desensitisation of …. receptors that occur with overuse.

A

budesonide/ fluticasone/ Beta

273
Q

The antileukotrienes drugs used in asthma are …… and ….., antagonists at LTD4 receptors, with slow onset, used prophylactic, and ……., a selective inhibitor of lipoxygenase (LOX), decreasing the formation of all LT.

A

Zafirlukast/ Montelukast/ Zileuton

274
Q

Blood coagulates by transformation of soluble fibrinogen into insoluble ….. Anticoagulants are drugs which decrease formation of fibrin clots. Oral anticoagulants (eg. warfarin) inhibit the …… of clotting factors …, …., …. and …. Heparin inhibit activity of several activated clotting factors, specially factors …. and …., via activation of ……. The endogenous anticoagulants, protein C and S cause proteolysis of factors …. and …..

A

fibrin/ hepatic synthesis/ II/ VII/ IX/ X/ IIa/ Xa/ antithrombin III/ Va/ VIIIa

275
Q

Heparin is a …. molecule, …..-soluble, given ….., with …. half life and no placenta access. They catalyses the binding of …… (a protease inhibitor) to factors …., …., …, …. and …. It’s activity is monitored using ….. and it’s antagonist is ……. (chemical antagonism). It promotes rapid anticoagulation. It’s side effects are bleeding, heparin-induced …… and ……..

A

large/ water/ parenterally (IV/SC)/ short/ antithrombin III/ IIa/ IX a/ Xa/ XIa/ XIIa/ Partial Thromboplastin Time/ protamine sulfate/ thrombocytopenia (HIT)/ hypersensitivity

276
Q

Warfarin is a …. molecule, …..-soluble, given ….., with …. half life and placenta access. They inhibit hepatic synthesis of factors …., …., …. and …., by inhibiting gama-carboxylation by …… reductase. It’s activity is monitored using ….. and it’s antagonist is ……. (slow onset) or ……. (rapid onset). It promotes long-term anticoagulation. It’s side effects are bleeding, drug interactions and ……..

A

large/ lipid/ orally/ long (+30h)/ II/ VII/ IX/ X/ Vitamin K epoxide/ INR, Prothrombin Time/ Vitamin K/ Frozen fresh plasma/ teratogenesis

277
Q

Direct thrombin inhibitors directly inhibit thrombin (factor IIa) and do not require antithrombin III. The drugs are ……, used in HIT, and ……, oral anticoagulant that does not require monitoring of PT or INR

A

argatroban/ dabigatran

278
Q

Direct factor Xa inhibitors do not require monitoring of PT or INR. The drugs are ….. and other -….. They are used to prevent stroke and systemic embolism in non-valvular atrial fibrillation.

A

Rivaroxaban/ xabans

279
Q

Thrombolytics lyse thrombi by catalysing the formation of endogenous fibrinolytic …… These agents include tissue …… recombinant and …… (bacterial). The …… (tPA) is clot specific, acting mainly on fibrin-bound plasminogen; less allergy problems. The ….. acts on both bound and free plasminogen (not clot specific) and it’s antigenic. Antifibrinolysins …….. and ……. are possible antidotes in excessive bleeding.

A

plasminogen activator (tPA)/ streptokinase/ alteplase/ streptokinase/ aminocaproic/ tranexamic acid

280
Q

Thrombus formation involves platelet adhesion, activation of platelets by factors ….., ……, etc, and aggregation of platelets by cross-linking reaction due to fibrinogen binding to glycoprotein …… receptors. The drug ….. irreversibly inhibits COX in platelets, decreasing activation. The drugs ……., …….., ……. block ADP receptors on platelets, decreasing activation. Lastly, the drugs ……, eptifibatide and tirofiban, block fibrinogen receptors, decreasing agregation

A

TXA2/ ADP/ IIb/IIIa/ clopidogrel/ prasugrel/ ticagrelor/ abciximab.

281
Q

Sulfonylureas block …. channels, increasing ….. release and decreasing ….. release. The 2 generation drugs from this class are ….. and ….. Their side effects are … and ….. gain

A

K/ insulin/ glucagon/ glipizide/ glyburide/ hypoglycaemia/ weight

282
Q

Metformin increase tissue ….. to insulin and decrease hepatic ……., thus it doesn’t cause ….. gain and …… It can cause lytic acidosis and it’s use requires caution in renal dysfunction. It can also be used in Polycystic Ovarian Syndrome, …. insulin resistance and ….. ovulation.

A

sensitivity/ gluconeogenesis/ weight/ hypoglycemia/ decreasing/ increasing

283
Q

…… inhibit the enzyme alpha-glucosidase in brush borders of small intestine, ….. formation of absorbable carbohydrate, ….. postprandial glucose. A side effect is GI discomfort, flatulence and diarrheas.

A

acarbose/ decrease/ decreasing

284
Q

Thiazolidinediones drugs are ….. and ……, bind to nuclear peroxisome proliferator-activating receptors, increasing ….. receptor numbers (like exercise) and decreasing hepatic ….. It causes less …… than sulfonylureas, but still cause …… and edema. Caution in CHF.

A

Pioglitazone/ Rosiglitazone/ insulin/ gluconeogenesis/ hypoglycemia/ weight gain

285
Q

Repaglidine work just like ……, stimulating ….. release from pancreatic cells. They are used in adjunction therapy of DM type 2, administered just before meals due to ….. half-life.

A

Sulfonylureas/ insulin/ short

286
Q

Glucagon-like peptide-1 (GLP-1) are incretins released from the small intestine that increase the release of glucose-dependent insulin secretion. The drug …… act as a long-acting GLP-1 agonist. The drug ….. and other …… inhibits the dipeptidyl peptidase (DPP-4) thereby inhibiting the inactivation of …..

A

exenatide/ sitagliptin/ gliptins/ GLP-1

287
Q

Sodium-Glucose Cotransporter-2 (SGLT-2) Inhibitors block the SGLT-2 in the ……, increasing glucose excretion. The drugs are …… and other ……. Side effects are ….. and ….. infections

A

proximal tubule/ canaglifozin/ glifozins/ UTI/ candida

288
Q

Adrenal Steroids can be used for inflammatory disorders and as replacement therapy, the drug …… is frequently used as replacement and …… is good to replace aldosterone effect. The drug …… block aldosterone and androgen receptors, while …… just block aldosterone. The drug mifepristone block ……. and ……. receptors, used with PGs as abortifacient. An antifungial drug that inhibit synthesis of androgens and cortisol is …….

A

hydrocortisone/ fludrocortisone/ spironolactone/ eplerenone/ glucocorticoid/ progestin/ ketoconazole

289
Q

….. is the major natural estrogen. Chronic Hormonal Replacement Therapy (estrogens + prog) increase risk of ……, …….., …….. and ……., and decrease risk of …….

A

estradiol/ breast cancer/ stroke/ blood clot/ incontinence/ bone fracture

290
Q

Estrogen Antagonists are ……., that inhibit aromatase, decreasing oestrogen synthesis, used in estrogen-dependent post menopausal ……., and …… (fertility pill), a partial agonist that decrease feedback inhibition, increasing FSH and LH, thus increasing ovulation and pregnancy, a side effect is multiple births.

A

Anastrozole/ breast cancer/ clomiphene

291
Q

Selective Estrogen-Receptor Modulators (SERMs) are partial agonists and it’s actions depend on target tissue. The drug …….., work as an agonist in ……, antagonist in …… and partial agonist in ……. (increase risk of endometrium cancer), its used in oestrogen-dependent breast cancer. The drug …… is an agonist in ……, antagonist in …… and …… (no increased risk of cancer), it’s used in prophylaxis of postmenopausal osteoporosis and breast cancer.

A

Tamoxifen/ bone/ breast/ endometrium/ raloxifene/ bone/ breast/ uterus

292
Q

Androgens Antagonists are ……., androgen receptor blockers, used for androgen-receptor-positive prostate cancer, ………., a GnRH analog, given continuously cause desensitisation, used for androgen-receptor-positive prostate cancer, and ……., a 5-alpha-reductase inhibitor, preventing conversion of testosterone into DHT (cause hair loss and prostate enlargement), used for male baldness and BPH, caution due to teratogenicity.

A

Flutamide/ Leuprolide/ Finasteride

293
Q

For prostate cancer use …… and …….

A

Leuprolide/ Flutamide (Lue’s Flute)

294
Q

Drugs used to treat hyperthyroidism are …… and ……., used for uncomplicated hyperthyroidism. High-dose propylthiouracil inhibits …….. Both drugs can cause agranulocytosis and ….. can also cause liver failure. Both drugs can cross placenta, but …. is safer in pregnancy because its extensively protein bound. Other drugs used is ……. (Lugol’s solution), possibly used in thyrotoxicosis preoperatively to decrease gland size, and …….., most commonly used drug for hyperthyroidism.

A

propylthiouracil (PTU)/ methimazole/ 5’deiodinase/ PTU/ PTU/ Iodide/ I131

295
Q

Amiodarone can cause thyroid dysfunction, leading to ….. or …..thyroidism, while lithium cause ….thyroidism, …… TSH release and cause goiter.
Levothyroxine (T4) is used for ……..

A

hypo/ hyper/ hypo/ increase/ hypothyroidism

296
Q

GH hormone replacement is used in pituitary …… and ……, Somatostatin, long-lasting pharmacological form called ……, is used in ….., …… and secretory -GI tumours. ACTH is used in infantile spasms. GnRH is used in endometriosis and ….. carcinoma (repository form). FSH and LH is used in …… states. Dopamine (Prolactin-Inhibiting Hormone) is used by the name of ……. in hyperprolactinemia. Oxytocin is used in ….. induction. Last, vasopressin, named ……. (V2 seletive) is used in ……. diabetes insipidus, ……. (increase factor VIII from liver), …….. disease (increase vW factor from endothelium), and in primary nocturnal ……. (also use TCAs)

A

dwarfism/ osteoporosis/ octreotide/ carcinoid/ acromegaly/ prostate cancer/ hypogonadism/ cabergoline/ labor/ desmopressin/ neurogenic (pituitary)/ haemophilia A/ von Willebrand/ enuresis

297
Q

Octreotide is used in …… syndrome (liver metastasis, fusing and increased serotonin), …….. (use IGF-1 test to confirm) and bleeding ……. It may cause gall stones.

A

Carcinoid/ acromegaly/ varices

298
Q

Osteoporosis treatment can be done using the bisphosphonates: …… and others ……, they induce osteoblasts to secret inhibitors to osteoclasts, decreasing bone ……., thus decreasing progression of osteoporosis. It’s also beneficial in …. disease (bone pain, deformity and increased alkaline phosphate). It side effect is GI distress including …… ulcers (take a lot of water and stay upright).

A

Alendronate/ dronates/ reabsorption/ Paget/ oesophageal

299
Q

Osteoporosis treatment can be done using biphosphonates, or ………, a PTH analog that stimulates osteoblasts and bone formation, or even ……, a inhibitor of RANK Ligand, a protein that act as a primary signal for bone removal.

A

teriparatide/ denosumab

300
Q

Cyclophosphamide is an alkylating agent that binds to DNA (guanine N7) creating a dysfunction DNA. It causes BM suppression and hemorrhagic ……. due to production of a toxic metabolite …….., which the antidote is …… The drug Cisplatin is also an alkylating agent that binds to DNA. It has …….toxicity properties, and it’s antidote is ……..

A

cystitis/ acrolein/ mesna/ nephro/ aminofostine

301
Q

Doxorubicin forms free radicals that inhibit topoisomerase. The ….. is very sensitive to free radicals, thus a common side effect is delayed …… The antidote is ……., a iron chelating agent preventing free radicals formation.

A

heart/ CHF/ dexrazoxane

302
Q

Methotrexate inhibit …… reductase (S phase), it cause BMS, and a antidote is …… (folinic acid) that direct turn into tetrahydrofolate and rescue cells from BM). The drug 5-Fluorouracil inhibit …… synthetase (don’t make ….).

A

DHF/ leucovorin/ thymidylate/ thymine

303
Q

Bleomycin complex with Fe and O2 and break ….. strand. It doesn’t cause BMS, but has ….. toxicity.
The drugs vinblastin and vincristine block ……. polymerisation. Their side effects are: Vinblastin cause …… and Vincristine cause ……

A

DNA/ pulmonary/ microtubular/ BMS/ neurotoxicity

304
Q

The target cancer therapy drugs are ……., the first of the group, target BCR-ABL; ……., that target ErB1 in head and neck cancers, and ………, that target ErB2 (HER2) in breast cancer

A

Imatinib/ cetuximab/ transtuzumab

305
Q

The anticancer drugs that are LESS BMS are ….., …… and …… Each of the following toxicity is related to the drug: nephrotoxicity - ……., pulmonary toxicity - ………, cardiac toxicity - …….., neurologic toxicity- ……… and hemorrhagic cystitis - ………..

A

cisplatin/ bleomycin/ vincristine/ cisplatin/ bleomycin/ doxorubicin/ vincristine/ cyclophosphamide

306
Q

Anticancer drugs usually cause BMS, thus, colony-stimulating factors, erythropoietin and thrombopoietin can be used as supportive therapy. The drugs …… (G-CSF) and …… (GM-CSF) decrease neutropenia, ……. increase RBC and …… increase platelets.

A

Filgrastim/ Sargramostim/ erythropoietin/ thrombopoietin

307
Q

…… bind to cyclophilin and …… bind to FK-binding protein to decrease calcineurin, that decrease activation of T cell, decreasing IL-2, IL-3 and interferon gamma. The drug ….. is the DOC for organ transplantation and ….. is used as alternative in renal and liver transplants. Both drugs can cause …..toxicity, but only ….. cause gingival …… (like CCB and phenytoin)

A

Cyclosporine/ Tacrolimus/ Cyclosporine/ Tacrolimus/ nephro/ Cyclosporine/ hyperplasia

308
Q

The immunosuppressants ……., inhibitor of de novo synthesis of purines, and ……, converted to 6-mercaptorurine to inhibit DNA synthesis, can be used with cyclosporine to limit toxicity.

A

Mycophenolate/ Azathioprine

309
Q

Monoclonal antibodies are ……., used as antiplatelet (antagonist of …….. receptors), …… and ……. that binds to TNF, used to treat RA and Chron Disease, …….., antagonist of ERB-B2, used to treat breast cancer, ………., cause rapid reverse of dabigratand and Palivizumab used in ……. virus infection.

A

Abciximab/ IIb-IIIa/ Infliximab/ adalimumab/ Trastuzumab/ Idarucizumab/ Respiratory syncytial

310
Q

Cytokines Interferon can be used for several different purpose, ex. Interferon alpha plus ribavirin was used to treat ……., Interferon beta is used to treat …….., and interferon gamma is used treat …….. disease, by increasing TNF.

A

Hepatitis C/ Multiple Sclerosis/ chronic granulomatous

311
Q

Iron poisoning happens mainly in …… and is characterised by severe …… distress, with …… gastroenteritis with hematemesis and bloody diarrhea. The antidote is ……

A

children/ GI/ necrotizing/ deferoxamine

312
Q

Lead poisoning happens in the presence of leaded paint chips and is characterised by …… (decreased heme synthesis), …… (wrist drop) and …… (from pica). The antidote are …… or ……

A

anemia/ neuropathy/ mental retardation/ succimer/ dimercaprol

313
Q

Mercury poisoning can occur duet to large predatory fish consumption. It’s characterized by CNS effects with …. and …. loss. The antidote are …… or ……

A

auditory/ visual/ dimercaprol/ succimer

Pharmacology (1 decks)

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