Board Review Flashcards by Denisse Tiangco

Buspirone, a drug with large first pass effect

Which of the following pharmacokinetic properties of the drug was most likely affected by this large first pass?

Oral bioavailability

Amount of concentration of the drug available at that particular time

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First pass effect affects

Absorption

Bioavailability

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Ability of drug to cross the placenta at fastest rate

Low molecular weight
Not bound to maternal plasma protein
Least ionized in maternal plasma

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Measure that most reliably reflects the total amount of drug reaching the target tissue

Area under the curve

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Factor that determines how long it will take for the drug to reach a steady-state concentration CSS in blood

Half-life

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Phase II reaction

a. Glucoronidation
b. Deamination
c. Hydrolysis
d. Reduction

Conjugation reaction
Transferase
Glucoronidation

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Elimination rate via metabolism catalyzed by alcohol dehydrogenase when the enzyme is saturated

Zero order kinetics

Ex. Phenytoin, Aspirin, Warfarin, Theophylline

Already saturated the enzyme
Plateau
Rate of elimination is not proportional to the concetration

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Related to zero order kinetics

Toxicity

Narrow therapeutic index

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Initial rates of drug distribution to different tissues depend primarily on which of the following parameter?

a. blood flow to the tissue
b. fat content of the tissue
c. degree of ionization of the drug un the tissue
d. active transport of the drug out of different cell type

INITIAL

blood flow

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The pro-drug increases the expression of CYP450 that converts the pro-drug to its active form.

With chronic, long-term administration of the prodrug, which of the following will be observed

a. potency will decrease
b. potency will increase

Potency will increase

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Antiseizure medication Phenobarbital

Diminished breathing
Low body temperature
Skin reddening

Barbiturate overdose

How does bicarbonate help overcome toxic effects of phenobarbital

Bicarbonate is a weak acid and there is overdose
We do not want it to recirculate
We want to trap weak acid (barbiturate) in the urine
It decreases distal tubular reabsorption

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protein binding

The more protein-bound, the lesser the binding to tissue

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What the drug can induce to body

Pharamcodynamics

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Loraradine binding to H1 receptor is

Affinity

Selective drug
Mass action
Total amount of drug that comes in, it will bind to a receptor

After the drug binds to receptor, receptor activation

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Full agonist

Maximal efficacy

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Two drugs act on the same tissue or organ via activarion of different receptors, resulting in effects that are qualitatively the opposite of one another

An example would be the direct effects of norepinephrine and acetylcholine on heart rate. This represents which of the following types of antagonism?

a. Chemical
b. Competitive
c. Pharmacologic
d. Physiologic

Physiologic - yin and yang of pharmacology
Insulin vs Cortisol
Sympa vs Para

Pharmacologic
•Chemical - Heparin vs Protamine sulfate
• Competitive - enzyme not saturable, concentration-dependent

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Dopamine, epinephrine and histamine interact with their cellular serpentine receptors

How do they mainly elicit their responses?

a. activating PLC
b. activating adenylate cyclase leading to inc cAMP
c. inducing or inhibiting synthesis of ligand-specific intracelualr proteins
d. opening or closing ligand-gated ion channels
e. regulating intracellular 2nd messengers through G protein-coupled receptors

Regulating intracellular 2nd messengers through G protein coupled recetors

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Range of doses that have a high probability of therapeutic success

a. Efficacy
b. Potency
c. Therapeutic index
d. Therapeutic window

Therapeutic window

LD50/ED50

TILED

Therapeutic index = Lethal dose/ED50

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If a drug has no intrinsic activity and bound reversible to B1 receptor, the drug is

a. Full agonist
b. Partial agonist
c. Competitive antagonist
d. Noncompetitive antagonist

Competitive antagonist

Non competitive antagonist = covalent, irreversible ex. aspirin (it will take you 7-10 days before aspirin will be eliminated)

Agonist = inherent power of 1
Antagonist = inherent power of 0

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TMP-SMZ

Both are bacteriostatic when given alone but bactericidal effect is obtained when the two drugs are given in combination

What do you call this drug interaction?

a. Additive effect
b. Potentiation
c. Synergysm
d. Tolerance

Synergism

Potentiation
- no relationship with each other but when given together, they are effective

Co-Amox (beta lactamase) when given together can eliminate beta lactam ring of clavulanic acid instead of amoxicillin (clavulanic is like suicide drug) -
potentiation

Synergysm - both agonist 1 + 1 = 3

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Drug with least amount that creates an effect (Potency) but it doesn’t mean that it is equally effective

At a dose of 2mg, it creates + 15 HR
Ar a dose of 10mg, it creates + 22
At a dose of 15mg, it creates + 30HR
At a dose of 20mg, it creates +55HR

Which is the most potent?

A dose of 2mg

Which is most effective?
A dose of 20mg

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A 51-year old man reported to his physician that in the morning he noticed his urine was cloudy and red.

The man had been taking on oral anticoagulant for 3 weeks to treat a deep venous thrombosis. If the patient’s symptoms were caused by the anticoagulant, which adverse drug reactions as most likely involved?

a. Overdose toxicity
b. Autoimmune reaction
c. Idiosyncratic reaction
d. Hypersensitivity
e. Immediate allergic reaction

Overdose

Augmented type of allergic reaction

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Non competitive antagonist

a. Alters the mechanism of action of an agonist
b. Alters the potency of an agonist
c. Shifts the dose-response curve of an agonist to the right
d. Decreases the maximum response to antagonist
e. Binds to the same site on the receptor as the agonist

Decreases the maximum response to antagonist

ED50 will not be affected by non competitive antagonist

ED 50 will be affected by competitive antagonist by increasing ED50

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Mild asthma b2 agonist

Which of the following was most likely the immediate consequence of activation of B2 receptors?

a. conformational change of a G protein
b. Increased synthesis of cAMP
c. Decreased synthesis of cAMP
d. Phosphorylation of a G protein

Conformational change of a G protein

Parasympthetic receptors -

M1 - Brain, (Gq) PLC 2nd: IP3 DAG always Ca

M2 - Heart (Gi)

M3 - Bladder and all of the body not supplied by the parasympathetic (Gq) oPLC 2nd: IP3 DAG always Ca

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Governs acid production

M1 (Gq)

Sympathetic

a 1 -Gq IP3 DAG, Ca, vasoconstrict, inc sphincter tone a 2 - Gi (autoreceptor) in presynapse release of NE from cleft, stimulates autoreceptor creating negative feedback -> inhibition of NE release Gs - beta receptors

Subfamily of CYP450 responsible for the highest fraction of clinically important drug interactions resulting from metabolism

CYP3A4 50% | CYP2D6 - prone to polymorphism

A japanese man had been receiving a standard dose of warfarin, which is an anticoagulant drug biotransformed by CYP2C9 Which is the most likely cause of the patient’s disorder? a. Increased protein binding of warfarin b. Decreased renal excretion of warfarin c. Inherent polymorphism of CYP2C9 d. Increased metabolism of CYP2C9

Inherent polymorphism of CYP2C9

African American with weakness, fatigue, yellowing of skin and sclera and slight fever He was given chloroquine as prophylaxis for malaria Lab findings confirmed hemolytic anemia likely due to chloroquine use Due to

G6PD deficiency

Patient has acute intermittent porphyria. If coma was caused by thiopental, which of the ff drug reactions is likely involved?

Idiosyncratic reaction

Which of the following drug may prevent absorption of Vit K? a. Lovastatin b. Cholestyramine c. Niacin d. Gemfibrozil

Cholestyramine Niacin converts cholesterol to VLDL Gemfibrozil stimulated PPAR-alpha gene transcription stimulating insulin and fat deposition

Succinylcholine was given and drug-induced paralysis lasted several hours Which enzyme polymorphism is responsible to cause this problem? a. acetylcholinesterase b. Glucose-6-phosphate dehydrogenase c. N-acetyltransferase

N-acetyltransferase Non-depolarizing drugs - curare (tobucurarine)

Severe allergic reaction to procaine an ester-type local anesthetic provokes allergic or anaphylactic reaction. Which will also provoke allergic or anaphylactic reaction? a. Bupivacaine - longest amide b. Lidocaine - intermediate c. Mepivacaine -intermediate d. Prilocaine -intermediate e. Tetracaine - long acting, lipid solubility amide

Tetracaine Esters - no “i” before caine Amide - procaine, tetracaine, cocaine (least)

A pregnant woman with low RBC and positive direct Coombs test during regular visit Woman had started treatment with methyldopa because of stage 1 Which most likely mediated the drug-induced reaction? a. Deficiency of NADH-methemoglobin reductase b. Product ion of autoantibodies against RBC c. Drug-induced deficiency of folic acid d. Drug-induced bone marrow supression e. Deficiency of G6PD

Product ion of autoantibodies against red blood cell Methyldopa is a good drug for pregnants because it is protein bound does not cross BBB

Peripheral neuropathy a known adverse effect of isoniazid, is caused by the patient’s symptoms and signs a. Rifampin-ibduced inhibition if isoniazid b. Deficiency of N-acetyltransferase

Deficiency of N-acetyltransferase

Palpitations, dry mouth, blurred visions and constipation Depression with use of antidepressant therapy a. a1 and a2 b. a1 and B1 c. M2 and M3 d. B1 and B2

M2 and M3 blockade

65 year old, open angle glaucoma underwent ocular surgery Before the operation, opthalmologist instilled few drops of carbachol in conjunctival sac Which of the following anatomical structures represents the primary site of action of this drug? a. Ganglionic neurons b. Ciliary muscle c. Lens d. Radial muscle of iris - dilate

Inc IOP, open angle glaucoma has too much aqueous production vs closed angle, there are ciliar muscles that impede canal of schlemm You need a drug to cause miosis to constrict Give Carbachol Contraction of ciliary muscle lead to drainage of aqueous humor to canal of schlemm Any drug that impede accomodation whether near or far (BOV) anticholinergic agents inhibits M3 receptor of ciliary muscle -> dilation with cyclopegia Beta blockers can cancel radial muscle but cannot paralyze ciliary muscle since it is controlled by M3

Urinary retention neurogenic atonic bladder Bethanechol was given Which of the following most likely mediated the therapeutic effectiveness of the drug?

Increased tone of the bladder detrusor muscle

Neostigmine for MG caused bradycardia Which molecular mechanism most likely mediated this adverse effect? a. Opening of ligand-gated K channels b. Opening of voltage-gated Na channels c. Increased synthesis of IP3 DAG

Opening of ligand gated K channel Ach slows the heart Slowing down of the heart rate is caused by opening of K channels

GA was induced with thiopental maintained with halothane and nitrous oxide Tubocurarine, a muscle relaxant Which is most likely given to reverse muscle paralysis a. Physostigmine b. Edrophonium c. Neostigmine d. Bethanicol e. Pralidoxime

Neostigmine Quarternay compound, polar, ionized and water soluble canNOT cross BBB something that will act on peripheral receptor Physostigmine can cross BBB because it is a tertiary compound physostigmine c

Atropine can control diarrhea because it acts on the a. histamine secretion by gastric cell b. inositol triphosphate/diacylglycerol (IP/DAG) c increase in cAMP

Inositol phosphate/DAG

Therapeutic effect of scopolamine is blockade of a. B1 adrenergic b. D2Dopaminergic c. M1 cholinergic

M1 cholinergic

Accidental spraying of ipratropium will most likely cause the following anticholinergic side effect? a. hallucination b. increase salivation c. AV block d. Difficulty in near vision

Difficulty in near vision

Mechanism of botulinum toxin a. Directly activated all muscarinic and nicotinic receptors b. Inhibits Ach release from all cholinergic nerves

Inhibits Ach release from all cholinergic nerves

Epinephrine-induced increase duration of lidocaine effect was most likely mediated by activation of the ff adrenoreceptor? a. B1 b. B2 c. a1 d. a2

alpha1

Molecular action of the therapeutic effect of dobutamine? a. Activation of PLA2 b. Increased synthesis of IP3DAG c. Increased cAMP

increased cAMP

Albuterol’s therapeutic efficacy is because of a. Increased microvascular permeability b. Decreased bronchial secretion c. Release of histamine from mast cell d. Increasef mucociliary clearance

Increasef mucociliary clearance

Acebutalol Type II antiarrythmic and Pindolol are classified as b blockers with intrinsic sympathomimetic activity (ISA) this means

They are partial agonist (mixed agonist/antagonist) submaximal effect

Therapeutic effect of phenoxybenzamine a. Decreases peripheral vascular resistance b. Increased cardiac output c. Decreased epinephrine release from adrenal medulla d. Increased heart rate

Decreased peripheral vascular resistance Phenoxybenzamine - irreversible covalent binding to alpha receptors So in a tumor, you need something that will bind permanently (covalently) despite release of tons of vasoconstrictors Phentolamine is kicked off because it does not bind irreversibly (non-covalent)

Weakness Drowsiness Palpitation Diagnosed with bladder obstruction due to BPH has been taling a drug for 2 weeks Which is the patient likely taking?

Tamsulosin Block of a1 on trigone sphincter loosens them

Prazosin will cause a. Mydriasis b. Impaired micturition c. Pale and cold skin d. Bronchoconstriction e. Postural hypotension

Postural hypotension First dose syncope Vasodilates capacitance vessels less blood going to brain

Timolol, open angle glaucoma for 3 months Treatment stopped progression of optic nerve damage Which of the following is the most likely site of action of timolol? a. Uvoscleral vessel b. Conjunctival vessel c. Ciliary EPITHELIUM NOT MUSCLE d. Retinal vessel

Ciliary epithelium

Parient has hyperthyroidism Which of the ff drugs is likely included in the therapeutic management of this patient? a. Albuterol b. Propranolol c. Labetalol d. Prazosin

Propranolol blocks 5’ deiodinade conversion of T4-T3 MSA membrane stabilizing effect highest MSA can cause sedation

Atenolol Verapamil Digoxin Which best explains the therapeutic effectiveness of all these drugs in treating atrial fibrillation? a. Decreased AV conduction b. Increased intra-atrial conduction c. Increased ventricular refractoriness d. Increased myocardial contractility d. Decreased cardiac preload

Decreased atrioventricular conduction Atenolol - both atria and ventricle Verapamil - on atria mostly Digoxin - on atria blocks Na-KATPase; blocks K arm of ATPase no sodium coming in, no depolarization

58 MI Ventricular tachycardia given IV Amiodarone The therapeutic effect of the drug was most likely mediated by an increase in which of the following electrophysiologic parameter a. Slope of phase 4 b. Slope of phase 0 c. Action potential duration d. Length of phase 2

Amiodarone is a class III antiarythmic affecting Phase III Block K channels Delay depolarization of heart Increase AP duration by blocking K channels

Dry disturbing cough from use of essential hypertension drug Which caused the sign and symptom? a. Captopril b. Clonidine c. Propranolol d. Minoxidil e. Nifedipine

Captopril

Safest drug to give on pregnant hypertensive patient a. Captopril b. Prazosin

Prazosin

Variant angina appropriate therapy a. Propranolol b. Furosemide c. Verapamil d. Captopril

Verapamil

Sublingual nitroglycerine oral isosorbide can cause a potential detrimental side effect of nitrate in prophylactic treatment of exertional angina? a. Decreased ejection time b. Increased heart rate

Increased heart rate

Prevents new stone production after operation? a. Acetazolamide b. Hydrochlorthiazide c. Furosemide d. Triamterine e. Spironolactone

HCTZ inhibits Na-Ca exchange Remove sodium reabsorption of Ca Loop diuretic will aggravate condition, loose calcium too much calcium in tube

CHF drug that caused serious allergic reaction to (furosemide) Which of the ff diuretics was most likely prescribed? a. Spironolactone b. Acetazolamide c. Triamterine d. Ethacrynic acid e. Indapamide

Ethacrynic acid Furosemide HCTZ sulfa-containing diuretics

Captopril for CHF delivers several benefits to CHF because a. High affinitt for angiotensin II receptors b. Promotes increased peripheral vascular resistance c. Decreases CO and increases afterload d. It causes venodilation and induces natriuresis e. It increases preload

It causes venodilation and natriuresis

Drug that acts by multiple mechanism including inhibition of phosphodiesterase in inflammatory cells a. Tiotropium b. Albuterol c. Theophylline

Theophylline inc cAMP (symp) parasympathetic cGMP, inc cGMP ensures bronchodilation Also acts on heart, inc cAMP goes to brain Effect on adenosine receptors on heart Gs Beta 1 Effect on inflammatory cells deacetylation