FA General Pharmacology Flashcards

1
Q

Cholinomimetic Agents

A

Direct: Bethanecol, Carbachol, Pilocarpine, Methacholine
Indirect: Neostigmine, Pyridostigmine, Physostigmine, Donepezil, Rivastigmine, Galantamine, Edrophonium

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2
Q

Cholinomimetic Agent Toxicity

A

Watch for exacerbation of COPD, asthma, and peptic ulcers when given to susceptible patients

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3
Q

Bethanecol Use

A

Postoperative ileus, neurogenic ileus, and urinary retention

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4
Q

Bethanecol Mechanism

A

Activates bowel and bladder smooth muscle; resistant to AChE.

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5
Q

Carbachol Use

A

Glaucoma, pupillary constriction, and relief of intraocular pressure

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6
Q

Carbachol Mechanism

A

Carbon copy of acetylcholine

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7
Q

Pilocarpine Use

A

Potent stimulator of sweat, tears, and saliva. Open-angle and closed-angle glaucoma.

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8
Q

Pilocarpine Mechanism

A

Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE.

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9
Q

Methacholine Use

A

Challenge test for diagnosis of asthma

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10
Q

Methacholine Mechanism

A

Stimulates muscarinic receptors in airway when

inhaled

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11
Q

Neostigmine Use

A

Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative)

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12
Q

Neostigmine Mechanism

A

↑ endogenous ACh.

Neo CNS = No CNS penetration.

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13
Q

Pyridostigmine Use

A

Myasthenia gravis (long acting); does not penetrate CNS

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14
Q

Pyridostigmine Mechanism

A

↑ endogenous ACh; ↑ strength. Pyridostigmine

gets rid of myasthenia gravis.

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15
Q

Physostigmine Use

A
Anticholinergic toxicity (crosses blood-brain
barrier → CNS)
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16
Q

Physostigmine Mechanism

A

↑ endogenous ACh. Physostigmine “phyxes”

atropine overdose.

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17
Q

Donepezil, Rivastigmine, Galantamine Use

A

Alzheimer disease

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18
Q

Donepezil, Rivastigmine, Galantamine Mechanism

A

↑ endogenous ACh.

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19
Q

Edrophonium Use

A

Historically, diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab (antiacetylcholine receptor antibody) test.

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20
Q

Edrophonium Mechanism

A

↑ endogenous ACh.

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21
Q

Cholinesterase Inhibitor Poisoning

A

Often due to organophosphates, such as parathion, that irreversibly inhibit AChE.
Causes DUMBBELSS: Diarrhea, Urination, Miosis,
Bronchospasm, Bradycardia, Excitation
of skeletal muscle and CNS, Lacrimation,
Sweating, and Salivation.

Organophosphates are components of
insecticides; poisoning usually seen in farmers.
Antidote—atropine (competitive inhibitor) +
pralidoxime (regenerates AChE if given early).

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22
Q

Muscarinic Antagonists

A

Atropine, Homatropine, Tropicamide, Benztropine, Scopolamine, Ipratropium, Tiotropium, Oxybutynin, Darifenacin, Solifenacin, Glycopyrrolate

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23
Q

Eye Muscarinic Antagonists

A

Atropine, Homatropine, Tropicamide

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24
Q

CNS Muscarinic Antagonists

A

Benztropine, Scopolamine

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25
Q

Respiratory Muscarinic Antagonists

A

Ipratropium, Tiotropium

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26
Q

Genitourinary Muscarinic Antagonists

A

Oxybutynin, Darifenacin, Solifenacin

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27
Q

Gastrointestinal/Respiratory Muscarinic Antagonist

A

Glycopyrrolate

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28
Q

Atropine, Homatropine, Tropicamide Use

A

Produce mydriasis and cycloplegia

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29
Q

Benztropine Use

A

Parkinson disease

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30
Q

Scopolamine Use

A

Motion sickness

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31
Q

Ipratropium, Tiotropium Use

A

COPD, asthma

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32
Q

Oxybutynin, Darifenacin, Solifenacin Use

A

Reduce urgency in mild cystitis and reduce bladder spasms. Other agents: tolterodine, fesoterodine, trospium.

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33
Q

Glycopyrrolate Use

A

Parenteral: preoperative use to reduce airway secretions.
Oral: drooling, peptic ulcer.

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34
Q

Atropine Mechanism

A

Muscarinic antagonist.

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35
Q

Atropine Use

A

Used to treat bradycardia and for ophthalmic applications. ↑ pupil dilation, cycloplegia, ↓ airway secretions, ↓ stomach acid secretion, ↓ gut motility, ↓ urinary urgency in cystitis

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36
Q

Atropine Toxicity

A

↑ body temperature (due to ↓ sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants

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37
Q

Sympathomimetics

A

Direct: Epinephrine, Norepinephrine, Isoproterenol, Dopamine, Dobutamine, Phenylephrine, Albuterol, Salmeterol, Terbutaline
Indirect: Amphetamine, Ephedrine, Cocaine

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38
Q

Epinephrine Mechanism

A

β > α

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39
Q

Epinephrine Use

A

Anaphylaxis, open angle glaucoma, asthma, hypotension; α effects predominate at high doses

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40
Q

Norepinephrine Mechanism

A

α1 > α2 > β1
Causes ↑ in systolic and diastolic pressures as a result of α1-mediated vasoconstriction → ↑ mean arterial pressure → bradycardia.

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41
Q

Norepinephrine Use

A

Hypotension (but ↓ renal perfusion)

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42
Q

Isoproterenol Mechanism

A

β1 = β2
Isoproterenol (no longer commonly used) has little a effect but causes β2-mediated vasodilation, resulting in ↓ mean arterial pressure and ↑ heart rate through β1 and reflex activity.

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43
Q

Isoproterenol Use

A

Electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.

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44
Q

Dopamine Mechanism

A

D1 = D2 > β > α

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45
Q

Dopamine Use

A

Unstable bradycardia, heart failure, shock; inotropic and chronotropic α effects predominate at high doses

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46
Q

Dobutamine Mechanism

A

β1 > β2, α

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47
Q

Dobutamine Use

A

Heart failure (inotropic > chronotropic), cardiac stress testing

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48
Q

Phenylephrine Mechanism

A

α1 > α2

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49
Q

Phenylephrine Use

A

Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)

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50
Q

Albuterol, Salmeterol, Terbutaline Mechanism

A

β2 > β1

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51
Q

Albuterol, Salmeterol, Terbutaline Use

A

Albuterol for acute asthma; salmeterol for longterm asthma or COPD control; terbutaline to reduce premature uterine contractions

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52
Q

Amphetamine Mechanism

A

Indirect general agonist (sympathetic), reuptake inhibitor, also releases stored catecholamines

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53
Q

Amphetamine Use

A

Narcolepsy, obesity, attention deficit disorder

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54
Q

Ephedrine Mechanism

A

Indirect general agonist (sympathetics), releases stored catecholamines

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55
Q

Ephedrine Use

A

Nasal decongestion, urinary incontinence, hypotension

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56
Q

Cocaine Mechanism

A

Indirect general agonist (sympathetics), reuptake inhibitor

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57
Q

Cocaine Use

A

Causes vasoconstriction and local anesthesia;
never give β-blockers if cocaine intoxication is
suspected (can lead to unopposed α1 activation
and extreme hypertension)

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58
Q

Sympatholytics

A

Clonidine, α-methyldopa

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59
Q

Clonidine Use

A
Hypertensive urgency (limited situations); does not decrease renal blood flow.
ADHD, severe pain, and a variety of off-label indications (e.g. ethanol and opioid withdrawal)
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60
Q

Clonidine Toxicity

A

CNS depression, bradycardia, hypotension, respiratory depression, and small pupil size

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61
Q

α-methyldopa Use

A

Hypertension in pregnancy (safe in pregnancy)

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62
Q

α-methyldopa Toxicity

A

Direct Coombs positive hemolytic anemia, SLE-like syndrome

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63
Q

α-blockers

A

Non-selective: Phenoxybenzamine (irreversible), Phentolamine (reversible)
α1 selective: Prazosin, Terazosin, Doxazosin, Tamsulosin
α2 selective: Mirtazapine

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64
Q

Non-selective α-blockers

A

Phenoxybenzamine (irreversible), Phentolamine (reversible)

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65
Q

α1-blockers

A

Prazosin, Terazosin, Doxazosin, Tamsulosin

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66
Q

α2-blockers

A

Mirtazapine

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67
Q

Phenoxybenzamine Use

A

Pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis

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68
Q

Phenoxybenzamine Toxicity

A

Orthostatic hypotension, reflex tachycardia

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69
Q

Phentolamine Use

A

Give to patients on MAO inhibitors who eat tyramine-containing foods

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70
Q

α1-blocker Use

A

Urinary symptoms of BPH; PTSD (prazosin); hypertension (except tamsulosin)

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71
Q

α1-blocker Toxicity

A

1st-dose orthostatic hypotension, dizziness, headache

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72
Q

Mirtazapine Use

A

Depression

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73
Q

Mirtazapine Toxicity

A

Sedation, ↑ serum cholesterol, ↑ appetite

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74
Q

β-blockers

A

Metoprolol, acebutolol, betaxolol, carvedilol, esmolol, atenolol, nadolol, timolol, pindolol, labetalol

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75
Q

β-blocker Use

A

Angina Pectoris: ↓ heart rate and contractility, resulting in ↓ O2 consumption
MI: β-blockers (metoprolol, carvedilol, and bisoprolol) ↓ mortality
SVT (metoprolol, esmolol): ↓ AV conduction velocity (class II antiarrhythmic)
Hypertension: ↓ cardiac output, ↓ renin secretion (due to β1-receptor blockade on JGA cells)
CHF: Slows progression of chronic failure Glaucoma (timolol): ↓ secretion of aqueous humor

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76
Q

β-blocker Toxicity

A

Impotence, cardiovascular adverse effects (bradycardia, AV block, CHF), CNS adverse effects (seizures, sedation, sleep alterations), dyslipidemia (metoprolol), and asthmatics/ COPDers (may cause exacerbation).
Avoid in cocaine users due to risk of unopposed α-adrenergic receptor agonist activity.
Despite theoretical concern of masking hypoglycemia in diabetics, benefits likely outweigh risks; not contraindicated.

77
Q

β1-selective antagonists (β1 > β2)

A

acebutolol (partial agonist), atenolol, betaxolol, esmolol, metoprolol
Selective antagonists mostly go from A to M (β1 with 1st half of alphabet)

78
Q

Nonselective β-antagonists (β1 = β2)

A

nadolol, pindolol (partial agonist), propranolol, timolol

Nonselective antagonists mostly go from N to Z (β2 with 2nd half of alphabet)

79
Q

Nonselective α- and β-antagonists

A

carvedilol, labetalol

Nonselective α- and β-antagonists have modified suffixes (instead of “-olol”)

80
Q

Nebivolol Mechanism

A

Combines cardiac-selective
β1‑adrenergic blockade with stimulation
of β3‑receptors, which activate nitric oxide
synthase in the vasculature

81
Q

Acetaminophen Antidote

A

N-acetylcysteine (replenishes glutathione)

82
Q

AChE inhibitor, Organophosphate Antidote

A

Atropine followed by pralidoxime

83
Q

Amphetamine (basic) Antidote

A

NH4Cl (acidify urine)

84
Q

Antimuscarinic, Anticholinergic Antidote

A

Physostigmine salicylate, control hyperthermia

85
Q

Benzodiazepine Antidote

A

Flumazenil

86
Q

β-blocker Antidote

A

Glucagon

87
Q

Carbon Monoxide Antidote

A

100% O2, hyperbaric O2

88
Q

Copper, Arsenic, Gold Antidote

A

Penicillamine

89
Q

Cyanide Antidote

A

Nitrite + thiosulfate, hydroxocobalamin

90
Q

Digitalis Antidote

A

Anti-dig Fab fragments

91
Q

Heparin Antidote

A

Protamine sulfate

92
Q

Iron Antidote

A

Deferoxamine, deferasirox

93
Q

Lead Antidote

A

EDTA, dimercaprol, succimer, penicillamine

94
Q

Mercury, Arsenic, Gold Antidote

A

Dimercaprol (BAL), succimer

95
Q

Methanol, Ethylene Glycol (Antifreeze) Antidote

A

Fomepizole > ethanol, dialysis

96
Q

Methemoglobin Antidote

A

Methylene blue, vitamin C

97
Q

Opioid Antidote

A

Naloxone

98
Q

Salicylate Antidote

A

NaHCO3 (alkalinize urine), dialysis

99
Q

TCA Antidote

A

NaHCO3 (plasma alkalinization)

100
Q

tPA, streptokinase, urokinase Antidote

A

Aminocaproic acid

101
Q

Warfarin Antidote

A

Vitamin K, plasma (if active bleeding)

102
Q

Reaction Causes: Coronary Vasospasm

A

Cocain, Sumatriptan, Ergot Alkaloids

103
Q

Reaction Causes: Cutaneous Flushing Cause

A

Vancomycin, Adenosine, Niacin, Ca2+ channel blockers

104
Q

Reaction Causes: Dilated Cardiomyopathy Cause

A

Doxorubicin, Daunorubicin

105
Q

Reaction Causes: Torsades de Pointes Causes

A

Class III (e.g., sotalol) and class IA (e.g., quinidine) antiarrhythmics, macrolide antibiotics, antipsychotics, TCAs

106
Q

Reaction Causes: Adrenocortical Insufficiency

A

HPA suppression 2° to glucocorticoid withdrawal

107
Q

Reaction Causes: Hot Flashes

A

Tamoxifen, clomiphene

108
Q

Reaction Causes: Hyperglycemia

A

Tacrolimus, Protease inhibitors, Niacin, HCTZ, β-blockers, Corticosteroids

109
Q

Reaction Causes: Hypothyroidism

A

Lithium, amiodarone, sulfonamides

110
Q

Reaction Causes: Acute Cholestatic Hepatitis, Jaundice

A

Erythromycin

111
Q

Reaction Causes: Diarrhea

A

Metformin, Erythromycin, Colchicine, Orlistat,

Acarbose

112
Q

Reaction Causes: Focal to Massive Hepatic Necrosis

A

Halothane, Amanita phalloides (death cap mushroom), Valproic acid, Acetaminophen

113
Q

Reaction Causes: Hepatitis

A

INH

114
Q

Reaction Causes: Pancreatitis

A

Didanosine, Corticosteroids, Alcohol, Valproic acid, Azathioprine, Diuretics (furosemide, HCTZ)

115
Q

Reaction Causes: Pseudomembranous Colitis

A

Clindamycin, ampicillin, cephalosporins

Antibiotics predispose to superinfection by resistant C. difficile

116
Q

Reaction Causes: Agranulocytosis

A

Dapsone, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthiouracil

117
Q

Reaction Causes: Aplastic Anemia

A

Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil

118
Q

Reaction Causes: Direct Coombs-Positive Hemolytic Anemia

A

Methyldopa, penicillin

119
Q

Reaction Causes: Gray Baby Syndrome

A

Chloramphenicol

120
Q

Reaction Causes: Hemolysis in G6PD Deficiency

A

INH, Sulfonamides, Dapsone, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin

121
Q

Reaction Causes: Megaloblastic Anemia

A

Phenytoin, Methotrexate, Sulfa drugs

122
Q

Reaction Causes: Thrombocytopenia

A

Heparin, cimetidine

123
Q

Reaction Causes: Thrombotic Complications

A

OCPs (e.g., estrogens)

124
Q

Reaction Causes: Fat redistribution

A

Protease inhibitors, Glucocorticoids

125
Q

Reaction Causes: Gingival Hyperplasia

A

Phenytoin, verapamil, cyclosporine, nifedipine

126
Q

Reaction Causes: Hyperuricemia (Gout)

A

Pyrazinamide, Thiazides, Furosemide, Niacin, Cyclosporine

127
Q

Reaction Causes: Myopathy

A

Fibrates, niacin, colchicine, hydroxychloroquine, interferon-α, penicillamine, statins, glucocorticoids

128
Q

Reaction Causes: Osteoporosis

A

Corticosteroids, heparin

129
Q

Reaction Causes: Photosensitivity

A

Sulfonamides, Amiodarone, Tetracyclines, 5-FU

130
Q

Reaction Causes: Rash (Stevens-Johnson Syndrome)

A

Anti-epileptic drugs (ethosuximide, carbamazepine, lamotrigine, phenytoin, phenobarbital), Allopurinol, Sulfa drugs, Penicillin

131
Q

Reaction Causes: SLE-like Syndrome

A

Sulfa drugs, Hydralazine, INH, Procainamide, Phenytoin, Etanercept

132
Q

Reaction Causes: Teeth Discoloration

A

Tetracyclines

133
Q

Reaction Causes: Tendonitis, Tendon Rupture, and Cartilage Damage

A

Fluoroquinolones

134
Q

Reaction Causes: Cinchonism

A

Quinidine, quinine

135
Q

Reaction Causes: Parkinson-like Syndrome

A

Antipsychotics, Reserpine, Metoclopramide

136
Q

Reaction Causes: Seizures

A

INH (vitamin B6 deficiency), Bupropion, Imipenem/cilastatin, Tramadol, Enflurane, Metoclopramide

137
Q

Reaction Causes: Tardive Dyskinesia

A

Antipsychotics, metoclopramide

138
Q

Reaction Causes: Diabetes Insipidus

A

Lithium, demeclocycline

139
Q

Reaction Causes: Fanconi Syndrome

A

Expired tetracycline

140
Q

Reaction Causes: Hemorrhagic Cystitis

A

Cyclophosphamide, ifosfamide

Prevent by coadministering with mesna

141
Q

Reaction Causes: Interstitial Nephritis

A

Methicillin, NSAIDs, furosemide

142
Q

Reaction Causes: SIADH

A

Carbamazepine, Cyclophosphamide, SSRIs

143
Q

Reaction Causes: Dry Cough

A

ACE inhibitors

144
Q

Reaction Causes: Pulmonary Fibrosis

A

Bleomycin, Amiodarone, Busulfan, Methotrexate

145
Q

Reaction Causes: Antimuscarinic

A

Atropine, TCAs, H1-blockers, antipsychotics

146
Q

Reaction Causes: Disulfiram-like Reaction

A

Metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st-generation sulfonylureas

147
Q

Reaction Causes: Nephrotoxicity/Ototoxicity

A

Aminoglycosides, vancomycin, loop diuretics, cisplatin

148
Q

Cytochrome P-450 Inducers (+)

A

Chronic alcohol use, Modafinil, St. John’s wort, Phenytoin, Phenobarbital, Nevirapine, Rifampin, Griseofulvin, Carbamazepine

149
Q

Cytochrome P-450 Substrates

A

Anti-epileptics, Antidepressants, Antipsychotics, Anesthetics, Theophylline, Warfarin, Statins, OCPs

150
Q

Cytochrome P-450 Inhibitors (-)

A

Acute alcohol abuse, Gemfibrozil, Ciprofloxacin, Isoniazid, Grapefruit juice, Quinidine, Amiodarone, Ketoconazole, Macrolides, Sulfonamides, Cimetidine, Ritonavir

151
Q

Sulfa Drugs

A

Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine
Patients with sulfa allergies may develop fever, urinary tract infection, Stevens-Johnson syndrome, hemolytic anemia, thrombocytopenia, agranulocytosis, and urticaria (hives). Symptoms range from mild to life threatening.

152
Q

Drug Names: -azole

A

Ergosterol synthesis inhibitor

Ketoconazole

153
Q

Drug Names: -bendazole

A

Antiparasitic/antihelmintic

Mebendazole

154
Q

Drug Names: -cillin

A

Peptidoglycan synthesis inhibitor

Ampicillin

155
Q

Drug Names: -cycline

A

Protein synthesis inhibitor

Tetracycline

156
Q

Drug Names: -ivir

A

Neuraminidase inhibitor

Oseltamivir

157
Q

Drug Names: -navir

A

Protease inhibitor

Ritonavir

158
Q

Drug Names: -ovir

A

DNA polymerase inhibitor

Acyclovir

159
Q

Drug Names: -thromycin

A

Macrolide antibiotic

Azithromycin

160
Q

Drug Names: -ane

A

Inhalational general anesthetic

Halothane

161
Q

Drug Names: -azine

A

Typical antipsychotic

Thioridazine

162
Q

Drug Names: -barbital

A

Barbiturate

Phenobarbital

163
Q

Drug Names: -caine

A

Local anesthetic

Lidocaine

164
Q

Drug Names: -etine

A

SSRI

Fluoxetine

165
Q

Drug Names: -ipramine

A

TCA

Imipramine

166
Q

Drug Names: -triptan

A

5-HT1B/1D agonists

Sumatriptan

167
Q

Drug Names: -triptyline

A

TCA

Amitriptyline

168
Q

Drug Names: -zepam

A

Benzodiazepine

Diazepam

169
Q

Drug Names: -zolam

A

Benzodiazepine

Alprazolam

170
Q

Drug Names: -chol

A

Cholinergic agonist

Bethanechol/carbachol

171
Q

Drug Names: -curium or -curonium

A

Non-depolarizing paralytic

Atracurium or vecuronium

172
Q

Drug Names: -olol

A

β-blocker

Propranolol

173
Q

Drug Names: -stigmine

A

AChE inhibitor

Neostigmine

174
Q

Drug Names: -terol

A

β2-agonist

Albuterol

175
Q

Drug Names: -zosin

A

α1-antagonist

Prazosin

176
Q

Drug Names: -afil

A

PDE-5 inhibitor

Sildenafil

177
Q

Drug Names: -dipine

A

Dihydropyridine CCB

Amlodipine

178
Q

Drug Names: -pril

A

ACE inhibitor

Captopril

179
Q

Drug Names: -sartan

A

Angiotensin-II receptor blocker

Losartan

180
Q

Drug Names: -statin

A

HMG-CoA reductase inhibitor

Atorvastatin

181
Q

Drug Names: -dronate

A

Bisphosphonate

Alendronate

182
Q

Drug Names: -glitazone

A

PPAR-γ activator

Rosiglitazone

183
Q

Drug Names: -prazole

A

Proton pump inhibitor

Omeprazole

184
Q

Drug Names: -prost

A

Prostaglandin analog

Latanoprost

185
Q

Drug Names: -tidine

A

H2-antagonist

Cimetidine

186
Q

Drug Names: -tropin

A

Pituitary hormone

Somatotropin

187
Q

Drug Names: -ximab

A

Chimeric monoclonal Ab

Basiliximab

188
Q

Drug Names: -zumab

A

Humanized monoclonal Ab

Daclizumab