Basics Flashcards
(246 cards)
1
Q
How many half-lives does it take for a drug to reach steady state
A
- 1 half-life: 50%
- 2 half-lives: 75%
- 3 half-lives: 87.5%
- 4 half-lives: ~94%
- 5 half-lives: ~99%
*it takes a drug between 4 and 5 half lives to reach steady state! (IMPORTANT: this applies to first order kinetics with a drug infused at a constant rate)
2
Q
Define the volume of distribution (Vd)
A
The theoretical fluid volume that would be needed to contain the total amount of an administered drug in the body at the same concentration that is present in the plasma
3
Q
Half-life equation
A
t1/2 = (0.7xVd)/Cl
*this same equation can be used to calculate Vd
4
Q
What does it mean for a drug to have a high Vd
A
- It means that more of the drug was distributed to places other than plasma (including fat)
- Drugs that have this characteristic are small lipophilic molecules, especially if bound to tissue protein
5
Q
Equation for volume of distribution (Vd)
A
Vd = amount of drug in the body/plasma drug concentration
6
Q
What is potency
A
Amount of a drug needed for a given effect
- represented by EC50 (concentration of a drug that causes 50% of the maximal effect), therefore: left shifting reduces EC50, representing increased potency and less drug needed
7
Q
What is efficacy
A
It is the maximal effect a drug can produce
8
Q
General inducers of CYP450 isoenzyme system
A
“Chronic alcoholics STeal Phen-Phen and NEver Refuse GReasy CARBs”
- Antiepileptic (anticonvulsant) drugs
- EXCEPT valproate
- Phenytoin
- Phenobarbital
- Carbamazepine - Antibiotics (Rifampicine, Griseofulvin)
- CHRONIC alcohol
- Never give acetaminophen (increased toxic metabolites) - St. John’s wort
- Nevirapine
9
Q
General inhibitors of CYP450 isoenzyme system
A
- Antiulcer medications (Cimetidine, Omeprazole)
- Antibiotics (Macrolides, Ketoconazole, Isoniazid, Fluconazole, Chloramphenicol, Sulfonamides, Cipro, Metronidazole)
- Only macrolide that does not intercat is Azithromycin - ACUTE alcohol
- Grapefruit juice (more specific 3A4 inhibitor*)
- Sodium valproate
10
Q
Effects of etanol on the GABA-A receptor
A
Increases its affinity for GABA
*Explains their synergy and cross tolerance!
11
Q
Define Vmax
A
Speed at which the reaction occurs when the enzyme’s active sites are completely saturated with substrate
*Proportional to enzyme concentration
12
Q
Define the Michaelis constant
A
Substrate concentration required to reach half Vmax
13
Q
Characteristics of enzymatic competitive inhibitors
A
- Resemble subtrate, bind at active site
- Increasing substrate concentration can overcome inhibition
- Increase Km
- No effect on Vmax
- Decrease potency
14
Q
Characteristics of enzymatic noncompetitive inhibitors
A
- Typically bind at allosteric site, not near active site
- Cannot be overcome with increased substrate concentration
- Decrease Vmax
- No effect on Km
- Decrease efficacy
15
Q
Define clearance
A
The volumen of plasma cleared of drug per unit time
16
Q
Clearance (Cl) equation
A
Cl = rate of elimination of drug/plasma drug concentration
17
Q
Loading dose (Ld) equation
A
Ld = CpxVd/F
*Where F is bioavailability
18
Q
Dosing that needs to be adjusted in renal or liver disease
A
Maintenance dose
19
Q
Maintenance dose (Md) equiation
A
Md = CpxClxt/F
*Where F is bioavailability and t is the dosaje Interval (time between doses), if not administered continuously
20
Q
Define zero-order elimination kinetics
A
When a constant AMOUNT of drug is eliminated per unit time
- Regardless of plasma concentration
- Plasma concentration decreases linearly
21
Q
Examples of drugs that are eliminated through zero-order elimination kinetics
A
“a PEA is round (0)”
- Phenytoin
- Ethanol
- Aspirin
22
Q
Define first-order elimination kinetics
A
When a constant FRACTION of drug is eliminated per unit time
- Directly proportional to drug concentration
- Plasma concentration decreases exponentially
23
Q
Examples of weak acids
A
- Barbiturates
- Methotrexate
- Aspirin
24
Q
Treatment for overdose of molecules that are weak acids
A
Bicarbonate to alkalinize the urine
25
Examples of weak bases
* Amphetamines
| * TCAs
26
Treatment for overdose of molecules that are weak bases
Ammonium chloride to acidify the urine
27
Name the three mechanisms of metabolization of phase 1 of biotransformation
* Reduction
* Oxidation
* Hydrolysis
-Monoamine oxidase also belongs to phase 1
28
Phase of biotransformation that uses cytochrome P450 system
Phase 1
29
Phase 1 mechanisms of metabolization that are carried out by cytochrome P450 enzymes
Reduction and oxidation
30
Name the mechanisms of metabolization of phase 2 of biotransformation
* Methylation
* Glucuronidation
* Acetylation
* Sulfation
* Glutathion conjugation
31
Phase of biotransformation that remains more active in geriatric patients
Phase 2
32
Determinators of potency
Affinity and number of receptors
33
What is the effect of a competitive antagonist on potency and efficacy
* Shifts the curve to the right, DECREASING POTENCY
| * No change in efficacy
34
Example of a characteristic agonist-competitive antagonist interaction
Diazepam + Flumazenil on GABA receptor
35
What is the effect of a noncompetitive antagonist on potency and efficacy
* Shifts the curve down, DECREASING EFFICACY
| * No effect on potency
36
Example of a characteristic agonist-noncompetitive antagonist interaction
Norephinephrine + Phenoxybenzamine on alpha receptors
37
What is the effect of a partial agonist on potency and efficacy
* Acts at the same site as full agonist, but with lower maximal effect (lower efficacy)
* Potency is variabel
38
Example of a characteristic agonist-partial agonist difference
Morphine vs Buprenorphine at opioid miu receptors
39
What is the therapeutic index
It is a measurement of drug safety (the higher, the safer)
40
Equation of the therapeutic index
TI = TD50/ED50
*Where TD50 equals the median toxic does and ED50 equals the median effective dose
41
Examples of drugs with low therapeutic index that need monitoring
"Warning! These Drugs are Lethal"
* Warfarin
* Teophylline
* Digoxin
* Lithium
42
Nicotinic ACh receptors are which kind of receptor
Ligand-gated Na/K channels
43
Name the 2 subtypes of nicotinic ACh receptors and their location
* Nn (found in autonomic ganglia and adrenal medulla)
| * Nm (found in neuromuscular junction of skeletal muscle)
44
Muscarinic ACh receptors are which kind of receptor
G-protein coupled receptors
45
Location of muscarinic Ach receptors M1, 2, and 3
Autonomic nervous system
46
Location of muscarinic Ach receptors M4 and 5
CNS
47
Class and function of receptor alpha1
* Gq protein linked
* Vascular smooth muscle contraction
* Mydriasis
* Increased intestinal and bladder sphincter muscle
48
Class and function of receptor alpha2
* Gi protein linked
* Decreases sympathetic outflow
* Decrease insulin reléase
* Decrease lipolysis
* Decrease aqueous humor production
* Increase platelet aggregation
49
Class and function of receptor beta1
* Gs protein linked
* Increases heart rate
* Increases contractility
* Increases renin reléase
* Increases lipolysis
50
Class and function receptor beta2
* Gs protein linked
* Vasodilation
* Bronchodilation
* Increases lipolysis
* Increases insulin reléase
* Decreases uterine tone (tocolysis)
* Ciliary muscle relaxation
* Increases aqueous humor production
51
Class and function of receptor beta3
* Gs protein linked
* Increases lipolysis
* Increases thermogenesis in skeletal muscle
* Increases bladder relaxation
52
Class and function of receptor M1
* Gq protein linked
* Mediates higer cognitive functions
* Stimulates enteric nervous system
* Increases gastric secretions
53
Class and function of receptor M2
* Gi protein linked
| * Decreases heart rate and contractility of atria
54
Class and function of receptor M3
* Gq protein linked
* Increases exocrine gland secretions
* Increases gut peristalsis
* Increases bladder contraction
* Bronchoconstriction
* Miosis
* Ciliary muscle contraction (acommodation)
* Increases insulin release
* Increases pulmonary secretions
55
Class and function of receptor D1
* Gs protein linked
* Relaxes renal vascular smooth muscle
* Activates direct pathway of striatum
56
Class and function of receptor D2
* Gi protein linked
* Modulates transmitter release (brain)
* Inhibits indirect pathway of striatum
57
Class and function of receptor H1
* Gq protein linked
* Increases nasal and bronchial mucus production
* Increases vascular permeability
* Contraction of bronchioles
* Pruritus
* Pain
58
Class and function of receptor H2
* Gs protein linked
| * Increases gastric acid secretion
59
Class and function of receptor V1
* Gq protein linked
| * Increases smooth muscle contraction
60
Class and function of receptor V2
* Gs protein linked
| * Increases wáter permeability and reabsorption in collecting tubules of the kidney
61
Name the direct cholinomimetic agonists
* Bethanecol
* Carbachol
* Methacholine
* Pilocarpine
62
Name the direct colinomimetic agonists that are resistant to acetylcholine esterase (AChE)
* Bethanechol
* Carbachol
* Pilocarpine
63
Characteristics and uses of bethanecol
* Resistant to AChE
* No nicotinic activity
* Treatment of ileus and urinary retention
"Bethany, call (bethanecol) me to activate your bowels and bladder"
64
Characteristics and uses of carbachol
* Muscarinic/nicotinic agonist
* Resistant to AChE
* Constricts pupil
* Relief of open-angle glaucoma due to constriction of the ciliary muscle
65
Characteristics and uses of pilocarpine
* Resistant to AChE
* Potent stimulator of sweat, tears, and saliva
* Contracts ciliary muscle of eye and pupillary sphincter
* Can cross the blood brain barrier (tertiary amine)
* Used in open and closed-angle glaucoma and in xerostomia in Sjögren syndrome
66
Characteristics and uses of methacholine
* Causes bronchoconstriction when inhaled
| * Used as challenge test for diagnosis of asthma
67
Name the indirect cholinomimetics (anticholinesterases)
* Neostigmine
* Pyridostigmine
* Edrophonium
* Physostigmine
* Echothiophate
* Galantamine, donepezil, and rivastigmine
68
Anticholenesterase drugs used in Alzheimer disease
"Alzheimer patients gallantly swim down the river"
* Galantamine
* Donepezil
* Rivastigmine
69
Affected brain nucleus in Alzheimer disease that leads to a decrease in ACh neurons
Meynert's nucleus
70
Characteristics and uses of neostigmine
* No entry into the CNS (quaternary amine)
* Ileus, urinary retention, and myasthenia gravis
* Reversal of neuromuscular junction blockade (post-op)
71
Characteristics and uses of edrophonium
* Very short-acting
| * Historically used to diagnose myasthenia gravis
72
Characteristics and uses of physostigmine
* Can enter CNS (tertiary amine)
* Treatment of glaucoma
* Antidote for atropine toxicity
73
Characteristics and uses of echothiophate
*Treatment of glaucoma
74
Signs and symptoms of cholinesterase inhibitor poisoning
"DUMBBELSS"
* Diarrhea
* Urination
* Miosis
* Bronchospasm
* Bradycardia
* Excitation
* Lacrimation
* Sweating
* Salivation
75
Compounds used in insecticides that can cause cholinesterase inhibitor poisoning
Organophosphates (eg, parathion)
*Irreversible binding to AChE
76
Treatment for cholinesterase inhibitor poisoning
* Atropine (competitive inhibitor)
| * Pralidoxime (regenerates AChE if given early)
77
Clinical applications of the muscarinic antagonists benztropine and trihexyphenidyl
* Parkinson disease
| * Acute dystonia
78
Clinical applications of the mucarinic antagonists oxybutinin, solifenacin, and tolteridone
Reduce bladder spasms and urge urinary incontinence
79
Clinical applications of the muscarinic antagonist scopolamine
Motion sickness
80
Part of the cholinesterase inhibitor syndrome that atropnie cannot reverse
It cannot block excitation of skeletal muscle and CNS, because those are mediated by nicotinic receptors
81
Side effects of atropine
* Hot as a flare (hyperthermia)
* Dry as a bone
* Red as a beet
* Blind as a bat (cycloplegia)
* Mad as a hatter (disorientation)
* Full as a flask (urinary retention)
82
Causative agent of gardener's pupil
Jimson weed (Datura)
*Causes mydriasis due to plant alkaloids
83
Epinephrine acts on which sympathetic receptors
* Low dose: beta 1 and 2
* Medium dose: beta 1, beta 2, and alpha 1
* High dose: predominantly alpha 1
84
Norepinephrine acts on which sympathetic receptors
*Alpha 1 more than alpha 2 more than beta 1
85
Adverse effects of norepinephrine
* Splanchnic vasoconstriction and decreased renal perfusión
* Increased SBP and increased DBP
* Reflexive decrease in heart rate
86
Name the direct sympathomimetics
* Isoproterenol
* Dopamine
* Dobutamine
* Ritodrine
* Metaproterenol/albuterol/salmeterol/terbutaline
* Phenylephrine
87
Characteristics and uses of isoproterenol
* Beta 1 = beta 2 agonist
* Treatment of AV conduction block
* Decreased DBP (causing reflexive tachycardia)
88
Characteristics and uses of dopamine
* D1 = D2, more than beta, more than alpha agonist
* Treatment of shock, especially with heart failure
* Chronotropic and inotropic
89
Characteristics and uses of dobutamine
* Beta 1 more than beta 2 agonist
* Inotropic
* Treatment of heart failure
* Used in cardiac stress testing
90
Characteristics and uses of ritodrine
* Beta 2 agonist
| * Reduces premature uterine contractions
91
Characteristics and uses of metaproterenol/albuterol/salmeterol
* Beta 2 more than beta 1 agonists
* Used in the treatment of asthma
* Metaproterenol and albuterol: acute
* Salmeterol: long acting
92
Characteristics and uses of terbutaline
* Beta 2 more than beta 1 agonist
| * Tocolytic used in premature labor
93
Characteristis and uses of phenylephrine
* Alpha 1 more than alpha 2 agonist
| * Used in hypotension, ocular procedures (mydriatic), and rinitis (decongestant)
94
Name the indirect sympathomimetics
* Amphetamines
* Cocaine
* Ephedrine
* Tyramine
95
Characteristics and uses of amphetamines
* Reuptake inhibitor of NE, also releases stored catecholamines
* Used in narcolepsy, obesity and ADHD
96
Characteristics and uses of cocaine
* Reuptake inhibitor of NE
| * Causes vasoconstriction and local anesthesia (also decreases Na permeability)
97
Drugs that need to be avoided in a cocaine intoxication
Beta blockers
*They can lead to unopposed alpha 1 activation and extreme hypertension
98
Characteristics and uses of ephedrine
* Releases stored catecholamines
* Used as a nasal decongestant (pseudoephedrine)
* Used in urinary incontinence and hypotension
99
Characteristics of tyramine
* Similar mechanism to that of amphetamines
* Found in red wine and cheese
* Cleared by MAO
100
Name the sympatholytic drugs (alpha 2 agonists)
* Clonidine
* Guanfacine
* Alpha methyldopa
101
Uses of clonidine and ganfacine
* Hypertensive urgency
* ADHD
* Tourette syndrome
* Restless leg syndrome
102
Important alpha methyldopa adverse effects
* Direct Coombs + hemolysis
| * SLE-like syndrome
103
Name the nonselective alpha blockers
* Phenoxybenzamine
| * Phentolamine
104
Characteristics and uses of phenoxybenzamine
* Irreversible inhibitor (noncompetitive)
* Used pre-op for pheochromocytoma to prevent catecholamine crisis
* Raynaud syndrome
105
Characteristics and uses of phentolamine
* Reversible inhibitor (competitive)
* Given to patients on MAOI who eat tyramine-containing foods
* Raynaud syndrome
106
Adverse effects of nonselective alpha blockers
* Orthostatic hypotension
| * Reflex tachycardia
107
BP drop criteria for orthostatic hypotension
Drop in SBP more than 20 and/or drop in DBP more than 10
108
Name the alpha 1 selective alpha blockers
* Prazosin
* Terazosin
* Doxazosin (longest-acting)
* Tamsulosin
109
Clinical applications of alpha 1 selective alpha blockers
* Urinary symptoms of BPH
* PTSD (prazosin)
* Hypertension (except tamsulosin)
110
Adverse effects of alpha 1 selective alpha blockers
* 1st dose orthostatic hypotension
* Dizziness
* Headache
111
Name the alpha 2 selective alpha blocker
Mirtazapine
112
Adverse effects of mirtazapine
* Sedation
* Increased serum cholesterol
* Increased appetite
113
Name the mixed alpha and beta blockers
* Carvedilol
| * Labetalol
114
Name the partial beta agonists
* Acebutolol
| * Pindolol
115
Beta blocker that blocks beta 1 receptors and stimulates beta 3 receptors
Nebivolol
*Beta 3 activates nitric oxide synthase in vasculature and decreases SVR
116
Mechanism through which beta blockers alleviate angina pectoris
They decrease HR and inotropy, leading to decreased oxygen consumption
117
Mechanism through which beta blockers alleviate supraventricular tachycardias
They decrease AV conduction velocity (class 2 antiarrhythmics)
118
Mechanism through which beta blockers decrease hypertension
* Decrease CO
| * Decrease renin secretion from JG cells
119
Mechanism through which beta blockers decrease intraocular pressure (IOP) in glaucoma
They decrease production of aqueous humor
120
Mechanism through which beta blockers alleviate variceal bleeding
They decrease hepatic venous pressure gradient and portal hypertension
121
Side effects of beta blockers
* Erectile dysfunction (propranolol)
* Cardiovascular effects (bradicardia, AV block, HF)
* CNS adverse effects (seizures, sedation, sleep alterations)
* Dyslipidemia (metoprolol)
* Asthma/COPD exacerbations (better use beta 1 agonists in asthmatic patients)
* Decrease glucagon secretion
122
Antidote for salicilate toxicity
* Sodium bicarbonate to alkalinize urine
| * Dialysis
123
Antidote for beta blocker toxicity
* Atropine
| * Glucagon (positive inotropic and chronotropic due to increased cAMP)
124
Antidote for digitalis toxicity
* Anti-dig Fab fragments
| * Potassium levels must always be monitored and normalized (may need to replenish magnesium)
125
Antidote for lead toxicity
* Ca-EDTA
* Dimercaprol
* Succimer
* Penicillamine
126
Antidote for copper, arsenic, or gold toxicity
* Dimercaprol
| * Succimer
127
Antidote for cyanide toxicity
* Nitrite
* Thiosulfate
* Hydroxycobalamin
128
Antidote for methemoglobin formation
* Methylene blue
| * Vitamin C
129
Antidote for carbon monoxide toxicity
* 100% oxygen
| * Hyperbaric oxygen
130
Antidote for methanol or ethylene glycol toxicity
* Fomepizole
* Ethanol
* Dyalisis
131
Antidote for opioid intoxication
* Naloxone (competitive antagonist)
| * Naltrexone (receptor antagonist)
132
Antidote for benzodiazepine intoxication
*Flumazenil
133
Antidote for TCA intoxication
* Sodium bicarbonate
| * Adjunctively treat for seizures, hyperthermia and arrhythmia
134
Antidote for heparine overdose
*Protamine sulfate
135
Antidote for warfarin overdose
* Vitamin K (delayed effect)
| * Fresh frozen plasma (immediate effect)
136
Antidote for tPA or streptokinase overdose
*Aminocaproic acid (blocks the activation of plasminogen)
137
Antidote for teophylline toxicity
*Beta blockers
138
Drugs that can cause coronary vasospasm
* Amphetamines
* Cocaine
* Ergot alkaloids
* Sumatriptan
139
Mechanism of action of ergot alkaloids
Partial agonists at both alpha and 5HT2 receptors
*Vasoconstrictive actions lead to decrease pulsation in cerebral vessels
140
Drugs that can cause cutaneous flushing
"VANNCE"
* Vancomycin (red man syndrome)
* Adenosine
* Niacin
* Nitrates
* Calcium channel blockers
* Echinocandins
141
Drug used to prevent dilated cardiomyopathy with anthracycline treatment
Dexrazoxane
142
Drugs that can cause torsades de pointes
"ABCDE"
* AntiArrhythmics (class 3 -sotalol- and IA -quinidine-)
* AntiBiotics (eg, macrolides)
* Anti"C"ychotics (eg, haloperidol)
* AntiDepressants (eg, TCAs)
* AntiEmetics (eg, ondansetron)
143
Drugs that can cause agranulocytosis
"Can Cause Pretty Major Collapse of Granulocytes, Dear"
* Clozapine
* Carbamazepine
* Propylthiouracil
* Methimazole
* Colchicine
* Ganciclovir
* Dapsone
144
Drugs that can cause aplastic anemia
"Can't Make New Fucking Blood Cells Properly"
* Carbamazepine
* Methimazole
* NSAIDs
* Felbamate
* Benzene
* Chloramphenicol
* Propylthiouracil
145
Drugs that can cause direct Coombs + hemolytic anemia
* Alpha methyldopa
| * Penicillin
146
Drug that causes gray baby syndrome
*Chloramphenicol
147
Drugs that can cause hemolysis in G6PD deficiency
"Hemolysis IS D PAIN"
* Isoniazid
* Sulfonamides
* Dapsone
* Primaquine
* Aspirin
* Ibuprofen
* Nitrofurantoin
148
Drugs that can cause megaloblastic anemia with hypersegmented neutrophils
"You're having a mega blast with PMS"
* Hydroxyurea
* Phenytoin
* Methotrexate
* Sulfa drugs
149
Drugs with increased risk for thrombosis
Oral contraceptives
150
Drug that can cause immune thrombocytopenia
Heparin
151
Potentially fatal delayed hypersensitivity reaction with a latency period of 2 to 8 weeks, followed by fever, morbilliform skin rash, and multiorgan involvement
Drug reaction with eosinophilia and systemic symptoms (DRESS)
152
Treatment for drug reaction with eosinophilia and systemic symptoms (DRESS) syndrome
Withdrawal of the offending drug and corticosteroids
153
Drugs that can cause the drug reaction with eosinophilia and systemic symptoms (DRESS) syndrome
* Allopurinol
* Antibiotics
* Anticonvulsants
* Sulfa drugs
154
Drugs that can cause pulmonary fibrosis
"My Nose Cannot Breathe Bad Air"
* Methotrexate
* Nitrofurantoin
* Carmustine
* Bleomycin
* Busulfan
* Amiodarone
155
Drugs that can cause acute cholestatic hepatitis and jaundice
*Macrolides
156
Drugs that can cause hepatitis
"Hepatitis is caused by Reckless Intoxication with Sick Party Fuel"
* Isoniazid
* Rifampin
* Pyrazinamide
* Statins
* Fibrates
157
Drugs that can cause hepatic necrosis
Liver "HAVAc"
* Halothane
* Amanita phalloides (death cap mushroom)
* Valproic acid
* Acetaminophen
158
Drugs that can cause pancreatitis
"Drugs Causing A Violent Abdominal Distress"
* Didanosine
* Corticosteroids
* Alcohol
* Valproic acid
* Azathioptine
* Diuretics
159
Drugs that can cause adrenocortical insufficiency
* Glucocorticoid withdrawal
| * Etomidate
160
Drugs that can cause diabetes insipidus
* Lithium (nephrogenic)
| * Demeclocycline
161
Drugs that can cause hot flashes
* Tamoxifen
| * Clomiphene
162
Drugs that can cause hyperglycemia
"Taking Pills Necessitaes Having blood Checked"
* Tacrolimus
* Protease inhibitors
* Niacin
* HCTZ
* Corticosteroids
163
Drugs that can cause hypothyroidism
* Lithium
* Amiodarone
* Sulfonamides
164
Drugs that can cause SIADH
"Can't Concentrate Serum Sodium"
* Carbamazepine
* Cyclophosphamide
* SSRIs
165
Drugs that can cause gynecomastia
* Spironolactone
* Digitalis
* Cimetidine
* Alcohol
* Estrogens
* Ketoconazole
166
Drugs that can cause gingival hyperplasia
* Phenytoin
* Calcium channel blockers
* Cyclosporine
167
Drugs that can cause hyperuricemia (gout)
"Painful Tophi and Feet Need Care"
* Pyrazinamide
* Thiazides
* Furosemide
* Niacin
* Cyclosporine
168
Drugs that can cause osteoporosis
* Corticosteroids
| * Heparin
169
Drugs that cause photosensitivity
"SAT For Photo"
* Sulfonamides
* Amiodarone
* Tetracyclines
* 5-FU
170
Drugs that can cause Stevens-Johnson syndrome
"Steven Johnson has epileptic allergy to sulfa drugs and penicillin"
* Anti-epileptic drugs (lamotrigine, carbamazepine)
* Allopurinol
* Sulfa drugs
* Penicillin
171
Drugs that can cause SLE-like syndrome
"Having lupus is SHIPP-E"
* Sulfa drugs
* Hydralazine
* Isoniazid
* Procainamide
* Phenytoin
* Etanercept
172
Antibiotic group that can cause tendonitis, tendon rupture, and cartilage damage
Fluoroquinolones
173
Antibiotic group that causes teet discoloration
Tetracyclines
174
Drugs that can cause Fanconi syndrome
* Expired tetracyclines
* Cisplatin
* Ifosfamide
* Tenofovir
175
Drugs that can cause interstitial nephritis
* Methicillin
* Furosemide
* NSAIDs
* Proton pump inhibitors
* Sulfa drugs
176
Drugs that can cause Parkinson-like syndrome
"Cogwheeel rigidity of ARM"
* Antypsychotics
* Reserpine
* Metoclopramide
177
Drugs that can cause seizures
"With seizures, I BITE my tongue"
* Isoniazid (B6 deficiency)
* Bupropion
* Imipenem/cilastatin
* Tramadol
* Enflurane
178
Drugs that can cause a disulfiram-like reaction
"Sorry Pals, Can't Go Mingle"
* Sulfonylureas (1st generation)
* Procarbazine
* Cephalosporins (certain)
* Griseofulvin
* Metronidazole
179
Drugs that can cause nephrotoxicity/ototoxicity
* Aminoglycosides
* Vancomycin
* Loop diuretics
* Cisplatin
* Amphotericin B
180
Drug that can be administered in case of cisplatin nephrotoxiciti/ototoxicity
*Amifostine
181
Drugs that can cause nephrotoxicity/neurotoxicity
*Polymyxins
182
Drugs with antimuscarinic properties
* Atropine
* TCAs
* H1 blockers
* Antipsychotics
183
End-product of ethylene glycol metabolism
Calcium oxalate
184
Signs and symptoms of ethylene glycol intoxication
* CNS depression
* Severe metabolic acidosis
* Nephrotoxicity
185
End-product of methanol metabolism
Formic acid
186
Signs and symptoms of methanol metabolism
* Respiratory failure
* Severe anion gap metabolic acidosis
* Ocular damage
187
Drugs that contain a sulfonamide group
"Scary Sulfa Pharm FACTS"
* Sulfonamide antibiotics
* Sulfasalazine
* Probenecid
* Furosemide
* Acetazolamide
* Celecoxib
* Thiazides
* Sulfonylureas
188
Signs and symptoms of sulfa drug allergies
* Fever
* Stevens-Johnson syndrome
* UTI
* Hemolytic anemia
* Thrombocytopenia
* Agranulocytosis
* AIN
* Urticaria and pruritic rash
189
Drug that can be used in an overdose of Zolpidem
Flumazenil
190
Define the tachyphylactic drug response
Acute decrease in response to a drug after initial/repeated administration (eg, nitrates, aspirin, phenylephrine, LSD, MDMA)
191
Metabolic reaction of phase 2 of biotransformation that is subject to genetic polymorphisms
Acetylation
192
Slow acetylators are prone to develop what pathology when exposed to drugs such as hydralazine, procainamide, or isoniazide
Drug-induced SLE
193
Explain what happens when a partial agonist is added to a full agonist
The partial agonist displaces full agonist from active sites, acting as an antagonist
194
Cytochrome P450 isoenzyme that is increased by alcohol
CYP2E1 (accelerates its own metabolism)
195
Cytochrome P450 isoenzyme that is blocked by alcohol
CYP2B2 (metabolizes barbiturates)
*Alcohol + barbiturates = toxicity
196
Only macrolide that is not considered cytochrome P450 isoenzyme general inhibitor
Azithromycin
197
Clearance equation for protein-bound drugs
CL = (free fraction) x GFR
198
Local anesthetics and pseudocholinesterases pass through which phase of biotransformation
Phase 1
199
The postganglionic innervation of sweat glands and piloerector muscles is mediated by which neurotransmitter
Acetylcholine
200
Mechanism of action of vesamicol
Stops formation of acetylcholine via inhibition of choline-acetyl transferase
201
Mechanism of action of reserpine
Blocks the uptake of NE into vesicles
202
Antyarrhythmic that is useful in the setting of digitalis toxicity arrhythmias
Lidocaine
203
Important neurologic reaction in bulimic patients under treatment with bupropion
Seizures
204
Part of the nephron most susceptible tu injury from toxic agents
Proximal tubule
205
Toxic agents that can lead to acute tubular necrosis (ATN)
* Aminoglycosides
* Heavy metals (lead)
* Myoglobinuria
* Ethylene glycol (formation of oxalate crystals)
* Radiocontrast dye
* Urate (eg, tumor lysis syndrome)
206
Clinical triad of serotonin syndrome
1. Mental status changes
2. Autonomic hyperactivity
3. Neuromuscular abnormalities
207
Name the drugs that can precipitate serotonin syndrome that can increase serotonin release
* Cocaine
| * MDMA
208
Name the drugs that can precipitate serotonin syndrome that impair presynaptic serotonin reuptake
* SSRIs
* SNRIs
* TCAs
* Opiates (meperidine)
* Antiemetics (ondansetron)
* Antitussives (dextromethorphane)
209
Antidote for serotoninergic syndrome if agitation and vital signs fail to improve
* Cyproheptadine
| - Histamine 1 receptor antagonist with nonspecific 5HT1A and 5HT2A properties
210
Signs and symptoms of salicylate toxicity
Triad of:
* Hyperventilation
* Tinnitus
* Vomiting
211
Etiologies of anion gap metabolic acidosis
"MUDPILERS"
* Methanol (formic acid)
* Uremia
* Diabetic ketoacidosis
* Propylene glycol (paraldehyde)
* Iron tablets, INH
* Lactic acidosis
* Ethanol and ethyelene glycol (oxalic acid)
* Rhabdomyolysis
* Salicylates
212
Quantity of salicylate needed to increase urate levels by competing with uric acid for secretion by organic acid pump
Low doses
213
Effect of high doses of salicylates on uric acid metabolism
Promote urocosuria
214
Dose of acetaminophen that is hepatotoxic
7 grams
215
Type of patients with a higher risk of developing acetaminophen toxicity at lower doses
* Liver disease
* Chronic alcoholism
* Malnourishment
* Dehydration
216
Signs and symptoms of acetaminophen toxicity
* Initially nause, vomiting, and anorexia
* 24 to 72 hours later, acute liver failure (RUQ pain, jaundice, coagulopathies, encephalopathy)
* Fulminant hepatitis
217
Laboratory findings in acetaminophen toxicity
* AST and ALT more than 1000
* Prolonged PT
* Decreased glucose (impaired gluconeogenesis)
* Increased BUN and Cr
218
Toxic metabolite responsible for acetaminophen toxicity
*NAPQI
219
Compund that binds to NAPQI to form mercaptopuric conjugates that are non toxic in acetaminophen metabolism
*Glutathione
220
Enzymes that metabolize acetaminophen into NAPQI
*Cytochrome P450
221
Pathogenesis of liver damage by NAPQI
Forms covalent bonds with cysteinyl and sulfhydryl groups in proteins
222
Hepatic lobule zone that is damaged in acetaminophen toxicity
*Centrilobular zone (zone 3)
223
Mechanism of action of N-acetyl-cysteine
Provides sulfhydryl groups to NAPQI, preventing it from binding to proteins
224
How long do you have to administer activated charcoal after acetaminophen ingestion to prevent toxicity
1 hour
*More if acetaminophen is ingested with a drugs that delays gastric emptying
225
How long do you have to administer N-acetyl-cysteine after acetaminophen ingestion to prevent toxicity
8 hours
226
How long does it need to pass to be able to measure acetaminophen levels in posible acetaminophen toxicity
4 hours
227
Specific drugs used in the treatment of neuroleptic malignant syndrome (NMS)
* Dantrolene (direct skeletal muscle relaxant)
* Bromocriptine (D2 agonists)
* Amantadine (dopaminergic and anticholinergic drug)
228
Mechanism of action of dantrolene
Decrease skeletal muscle contractility by blocking calcium release from the sarcoplasmic reticulum through binding to ryanodine receptors
229
Signs and symptoms of neuroleptic malignant syndrome (NMS)
"Malignant FEVER"
* Myoglobinuria
* Fever
* Encephalopathy
* Vitals
* Enzymes (Ck more than a 1000)
* Rigidity
230
Pathogenesis of neuroleptic malignant syndrome (NMS)
* Blockade of nigrostriatal dopamine pathways may cause parkinsonian symptoms of rigidity and tremor
* Blockade of hypothalamus may cause hyperthermia and autonomic dysfunction
231
Treatment of serum sickness
Antihistamines and glucocorticoids
232
Mechanism of action of imatinib
Protein tyrosine kinase inhibitor that inhibits BCR-ABL tyrosine kinase and c-kit
233
Adverse effects of imatinib
*Fluid retention (pleural effusion, ascites, pulmonary edema, and rapid weight gain)
234
Mechanism of action of cyclophosphamide
Alkylating agent that attacks guanine N7
235
Mechanism of action of cisplatin
Alkylating agent that cross-links DNA strands
236
Mechanism of action of procarbazine
Alkylating agent
237
Mechanism of action of doxorubicin
* Intercalator
* Forms free radicals
* Inhibits topoisomerase
238
Mechanism of action of bleomycin
Complexes with iron and oxygen, leading to DNA strand scission
239
Most important side effect of vincristine
Neurotoxicity - peripheral neuropathy
240
Mechanism of action of all-trans retinoic acid (ATRA)
Differentiating agent, promotes differentiation of promyelocytes
241
Most important side effect of all-trans retinoic acid (ATRA)
"Differentiation syndrome"
* Respiratory distress
* Pleural and pericardial effusions
* CNS symptoms
242
Pyrimidine analog antimetabolite that interferes with DNA and RNA synthesis
5-FU (bioactivated to 5-FdUMP and F-UMP), affecting thymine synthesis
243
Mechanism of action of sirolimus
Inhibit T-cell activation and proliferation by binding mTOR
*Also inhibits antibody production
244
Most important side effects of sirolimus
* Peripheral edema
* Hypertension
* Hypercholesterolemia
* Hypertriglyceridemia
245
Mechanism of action of cyclosporine
Binds to cyclophilin in lymphocytes and inhibits calcineurin, thereby inhibiting production of IL-2
246
Main use of nicotinic receptor antagonists, like hexamethonium
Prevent vagal reflexes (eg, bradycardia caused by increased blood pressure due to increased norepinephrine)
