These 87 USMLE Step 1 pharmacology practice questions cover the drug mechanisms, side effects and interactions that appear again and again on the exam. They are organized by organ system so you can study one topic at a time. Every question includes the correct answer and a short explanation.
Written by Dr. Ray Makar, MD, author of the Repeated USMLE Questions eBook series.
Prefer video? Watch daily USMLE case questions on MedFocus by Dr. Ray on YouTube.
How to use this page: read the question, pick your answer, then click Show Answer and Explanation. Read the explanation even when you are right — repeated question types are common on the real exam.
Jump to a topic
- Cardiovascular and Hematology Drugs (27 questions)
- Antimicrobials (18 questions)
- CNS, Psychiatry and Neuromuscular Drugs (15 questions)
- Endocrine and Renal Drugs (11 questions)
- Immunosuppressants, Chemotherapy and Gout Drugs (7 questions)
- Respiratory, GI, Autonomic and Toxicology (9 questions)
Cardiovascular and Hematology Drugs
Question 1. A patient with heart failure is prescribed a drug that inhibits the Na⁺/K⁺-ATPase pump, increasing intracellular calcium in cardiac myocytes. Which one of the following drugs is most likely responsible?
A- Amiodarone
B- Digoxin
C- Diltiazem
D- Verapamil
Question 2. A patient taking an ACE inhibitor has developed a persistent cough. Which one of the following mediators is most responsible for this complaint?
A- Bradykinin
B- Histamine
C- Leukotriene B4
D- Serotonin
Question 3. A patient treated for severe hypertension develops lupus-like syndrome, reflex tachycardia, and fluid retention. Which mechanism best describes his medication?
A- Alpha-1 receptor blockade
B- Calcium channel blockade
C- Direct arteriolar vasodilation
D- Muscarinic antagonism
Question 4. A patient with chronic angina is treated with ranolazine. What is the primary mechanism responsible for its antianginal effect?
A- Decreased heart rate via beta blockade
B- Inhibition of late sodium current in cardiac cells
C- Increased coronary artery dilation
D- Stimulation of nitric oxide release
Question 5. A patient with atrial fibrillation is treated with dofetilide. Which electrophysiologic effect explains the antiarrhythmic action of this drug?
A- Decreased phase 0 depolarization
B- Increased refractory period by potassium channel blockade
C- Inhibition of calcium influx in AV node
D- Sodium channel blockade during depolarization
Question 6. A patient treated with verapamil develops constipation and bradycardia. What class of drug does verapamil belong to?
A- Beta-blockers
B- Calcium channel blockers
C- Potassium channel blockers
D- Sodium channel blockers
Question 7. Thiazide diuretics increase digoxin toxicity primarily through which electrolyte disturbance?
A- Hypercalcemia
B- Hyponatremia
C- Hypomagnesemia
D- Hypokalemia
Question 8. A patient treated with a nonselective beta blocker develops hypoglycemia that is difficult to recognize. What explains the masking of hypoglycemia symptoms?
A- Alpha receptor blockade
B- Beta-1 receptor stimulation
C- Beta-2 receptor blockade
D- Muscarinic receptor blockade
Question 9. A patient with hypertension is treated with clonidine. What is the primary mechanism by which this drug lowers blood pressure?
A- Alpha-1 receptor blockade
B- Central alpha-2 receptor stimulation
C- Inhibition of angiotensin II receptors
D- Sodium channel blockade
Question 10. A patient who is taking a high dose of niacin for hyperlipidemia develops hyperglycemia. What explains this effect?
A- Decreased insulin secretion
B- Decreased peripheral glucose uptake
C- Increased hepatic gluconeogenesis
D- Increased pancreatic glucagon release
Question 11. A patient with heart failure is started on sacubitril/valsartan. What is the primary pharmacologic action of sacubitril?
A- Angiotensin II receptor blockade
B- Inhibition of neprilysin
C- Inhibition of renin release
D- Stimulation of natriuretic peptide receptors
Question 12. A patient with atrial fibrillation is prescribed sotalol. Which additional pharmacologic property does this drug possess?
A- Alpha-1 blockade
B- Beta-adrenergic blockade
C- Calcium channel blockade
D- Sodium channel blockade
Question 13. A patient taking warfarin is given vitamin K. What is the primary effect of vitamin K administration?
A- Decreases synthesis of clotting factors II, VII, IX, X
B- Increases synthesis of clotting factors II, VII, IX, X
C- Inhibits platelet aggregation
D- Prevents fibrin degradation
Question 14. A patient receiving heparin develops thrombocytopenia and thrombosis. What is the underlying mechanism?
A- Antibody formation against heparin–platelet factor 4 complex
B- Bone marrow suppression
C- Direct platelet destruction by heparin
D- Inhibition of platelet cyclooxygenase
Question 15. A patient with asthma is prescribed propranolol and develops worsening shortness of breath. What explains this effect?
A- Alpha-1 receptor blockade
B- Beta-1 receptor stimulation
C- Beta-2 receptor blockade
D- Muscarinic receptor activation
Question 16. Which medication reduces platelet aggregation by irreversibly inhibiting cyclooxygenase (COX)?
A- Aspirin
B- Clopidogrel
C- Dipyridamole
D- Warfarin
Question 17. A patient with heart failure is started on an ACE inhibitor. Which physiologic change contributes to its beneficial effect?
A- Decreased aldosterone secretion
B- Decreased heart rate
C- Increased preload
D- Increased sympathetic tone
Question 18. Which antiarrhythmic drug is classified as a Class III agent?
A- Amiodarone
B- Lidocaine
C- Propranolol
D- Verapamil
Question 19. A patient with hyperlipidemia is prescribed ezetimibe. What is the primary mechanism of action of this drug?
A- Decreased bile acid reabsorption
B- Increased lipoprotein lipase activity
C- Inhibition of cholesterol synthesis
D- Inhibition of intestinal cholesterol absorption
Question 20. A patient receiving heparin therapy develops a sudden drop in platelet count. What is the underlying mechanism?
A- Bone marrow suppression
B- Decreased platelet production
C- Direct platelet toxicity
D- Immune-mediated platelet activation
Question 21. A 60-year-old man with benign prostatic hyperplasia (BPH) and hypertension is prescribed terazosin. Which of the following adverse effects should he be warned about?
A- constipation
B- Orthostatic hypotension
C- Reflex bradycardia
D- Sedation
Question 22. A 26-year-old man presents with muscle pain and dark urine after starting simvastatin. Which enzyme system metabolizes this drug?
A- CYP1A2
B- CYP2C9
C- CYP2D6
D- CYP3A4
Question 23. A 55-year-old man with atrial fibrillation is taking warfarin. He is started on trimethoprim-sulfamethoxazole for a urinary tract infection. What is the most likely outcome of this drug interaction?
A- Decreased anticoagulant effect
B- Enhanced metabolism of warfarin
C- Increased risk of bleeding
D- No significant effect
Question 24. A 60-year-old man with atrial fibrillation is started on amiodarone. Which adverse effect is most commonly associated with this medication?
A- Hyperkalemia
B- Hypoglycemia
C- Nephrotoxicity
D- Pulmonary fibrosis
Question 25. A 28-year-old woman develops a dry cough after beginning treatment for hypertension. Which drug is most likely responsible?
A- Amlodipine
B- Lisinopril
C- Losartan
D- Propranolol
Question 26. A 60-year-old patient with chronic heart failure is started on digoxin. Which electrolyte imbalance increases the risk of digoxin toxicity?
A- Hyperkalemia
B- Hypocalcemia
C- Hypokalemia
D- Hyponatremia
Question 27. A patient with atrial fibrillation is prescribed warfarin. Which of the following factors will increase the anticoagulant effect of warfarin?
A- Vitamin K deficiency
B- Rifampin therapy
C- Liver disease
D- Chronic alcohol use
Antimicrobials
Question 28. A patient treated with amoxicillin develops a rash after taking the medication. What type of reaction is most likely?
A- Type I hypersensitivity
B- Type II hypersensitivity
C- Type III hypersensitivity
D- Type IV hypersensitivity
Question 29. A patient taking daptomycin for a resistant infection develops muscle pain and elevated creatine kinase levels. What is the mechanism of action of this drug?
A- Binds D-alanine in bacterial cell walls
B- Blocks bacterial DNA gyrase
C- Creates membrane pores causing depolarization
D- Inhibits bacterial ribosomal protein synthesis
Question 30. Isoniazid-induced peripheral neuropathy is caused by deficiency of which vitamin?
A- Vitamin B6
B- Vitamin B12
C- Vitamin B1
D- Folate
Question 31. A patient receiving trimethoprim-sulfamethoxazole develops megaloblastic anemia. Which mechanism explains this adverse effect?
A- Folate metabolism inhibition
B- Hemoglobin oxidation
C- Inhibition of erythropoietin synthesis
D- Vitamin B12 malabsorption
Question 32. A patient with tuberculosis treated with rifampin develops decreased effectiveness of multiple medications. What pharmacologic property of rifampin causes this effect?
A- CYP450 enzyme inhibition
B- CYP450 enzyme induction
C- Decreased intestinal absorption
D- Renal excretion competition
Question 33. A patient treated with vancomycin develops acute kidney injury. Which concurrent medication increases this risk most significantly?
A- Amoxicillin
B- Azithromycin
C- Gentamicin
D- Metronidazole
Question 34. A patient taking linezolid develops thrombocytopenia after prolonged therapy. What is the underlying mechanism?
A- Direct platelet destruction
B- Immune complex deposition
C- Mitochondrial protein synthesis inhibition
D- Vitamin K antagonism
Question 35. A patient treated with ciprofloxacin develops tendon pain and swelling. What is the most likely complication?
A- Achilles tendon rupture
B- Aplastic anemia
C- Cardiomyopathy
D- Hemolytic anemia
Question 36. Which medication is most likely to cause photosensitivity as a side effect?
A- Amoxicillin
B- Doxycycline
C- Erythromycin
D- Vancomycin
Question 37. A patient treated with gentamicin develops renal impairment. What is the primary mechanism of this adverse effect?
A- Accumulation in proximal tubule cells
B- Acute interstitial nephritis
C- Decreased renal blood flow
D- Immune-mediated glomerulonephritis
Question 38. Which of the following antifungal medications inhibits ergosterol synthesis by blocking fungal cytochrome P450 enzymes?
A- Amphotericin B
B- Fluconazole
C- Flucytosine
D- Terbinafine
Question 39. A patient treated with erythromycin develops QT prolongation on ECG. What is the main mechanism behind this effect?
A- Beta-adrenergic blockade
B- Calcium channel inhibition
C- Potassium channel blockade
D- Sodium channel blockade
Question 40. A patient treated for latent tuberculosis develops elevated liver enzymes. Which drug is most likely responsible?
A- Cycloserine
B- Ethambutol
C- Isoniazid
D- Streptomycin
Question 41. A 25-year-old woman is taking oral contraceptive pills (OCPs). Which antibiotic can decrease the effectiveness of her contraceptive therapy?
A- Amoxicillin
B- Azithromycin
C- Ciprofloxacin
D- Rifampin
Question 42. A 40-year-old man is treated with chloramphenicol for a severe infection. Later, he develops pancytopenia. What is the most likely mechanism of this adverse effect?
A- Immune-mediated hemolysis
B- Irreversible aplastic anemia
C- Megaloblastic anemia due to folate deficiency
Question 43. Which of the following drugs is most likely to cause ototoxicity and nephrotoxicity, especially when combined with loop diuretics?
A- Amoxicillin
B- Azithromycin
C- Ceftriaxone
D- Gentamicin
Question 44. Which of the following drugs inhibits bacterial folate synthesis by blocking dihydropteroate synthase?
A- Ciprofloxacin
B- Isoniazid
C- Trimethoprim
D- Sulfamethoxazole
Question 45. Which one of the following antibiotics is most associated with tendinitis and tendon rupture?
A- Ciprofloxacin
B- Azithromycin
C- Doxycycline
D- Amoxicillin
CNS, Psychiatry and Neuromuscular Drugs
Question 46. A patient with Parkinson’s disease is treated with selegiline. What is the primary mechanism of this drug?
A- Inhibition of catechol-O-methyltransferase
B- Inhibition of monoamine oxidase B
C- Stimulation of dopamine receptors
D- Stimulation of muscarinic receptors
Question 47. A patient with hyperlipidemia is treated with cholestyramine. What is the primary mechanism by which this drug lowers cholesterol?
A- Decreases hepatic cholesterol synthesis
B- Inhibits intestinal cholesterol absorption
C- Increases bile acid excretion in stool
D- Stimulates lipoprotein lipase
Question 48. A patient treated with morphine develops constipation. What is the primary mechanism responsible?
A- Decreased intestinal secretion
B- Decreased intestinal motility
C- Increased fluid absorption
D- Increased smooth muscle tone
Question 49. A patient with epilepsy is started on carbamazepine. Which laboratory abnormality should be monitored?
A- Hypercalcemia
B- Hyponatremia
C- Hypokalemia
D- Hypomagnesemia
Question 50. A patient taking phenelzine develops severe hypertension after eating aged cheese. What is the underlying cause of this reaction?
A- Excess dopamine release
B- Increased norepinephrine levels
C- Inhibition of acetylcholinesterase
D- Reduced serotonin reuptake
Question 51. A 29-year-old woman treated with lithium presents with tremor, polyuria, and confusion. Which laboratory finding is most likely present?
A- Hypercalcemia
B- Hypoglycemia
C- Hypokalemia
D- Hyponatremia
Question 52. A patient develops muscle weakness and respiratory failure after receiving a neuromuscular blocker during surgery. Which drug was most likely used?
A- Atracurium
B- Succinylcholine
C- Pancuronium
D- Rocuronium
Question 53. A patient taking metoclopramide develops restlessness and involuntary muscle movements. This adverse effect is due to blockade of which receptor?
A- Dopamine receptors
B- Histamine receptors
C- Muscarinic receptors
D- Serotonin receptors
Question 54. Which of the following is the mechanism of action of botulinum toxin at cholinergic nerve terminals?
A- Activates muscarinic receptors directly
B- Inhibits acetylcholine release by preventing SNARE protein function
C- Blocks acetylcholine reuptake
D- Blocks acetylcholine synthesis by inhibiting choline acetyltransferase
E- Stimulates excessive acetylcholine release at the neuromuscular junction
Question 55. A 32-year-old man presents with dry mouth, blurred vision, and urinary retention after taking an over-the-counter cold medication. Which component is most likely responsible for these symptoms?
A- Dextromethorphan
B- Diphenhydramine
C- Guaifenesin
D- Phenylephrine
Question 56. A 50-year-old man with Parkinson’s disease is started on levodopa–carbidopa. After several months, he develops involuntary movements of his limbs and face. What is this side effect called?
A- Akathisia
B- Chorea
C- Dystonia
D- Tardive dyskinesia
Question 57. A 25-year-old man develops muscle rigidity, hyperthermia, and autonomic instability after receiving haloperidol. Which drug can be used to treat this condition?
A- Atropine
B- Dantrolene
C- Physostigmine
D- Propranolol
Question 58. A patient taking haloperidol develops muscle rigidity, high fever, and confusion. What is the best initial management step?
A- Administer dantrolene
B- Give epinephrine
C- Start propranolol
D- Stop the antipsychotic
Question 59. A 35-year-old woman with generalized anxiety disorder is started on buspirone. Which of the following statements about this drug is correct?
A- It acts as a partial agonist at 5-HT₁A receptors
B- It causes dependence and withdrawal effects
C- It has sedative and muscle relaxant properties
D- It provides rapid relief of anxiety symptoms
Question 60. Which of the following drugs is a reversible cholinesterase inhibitor used in the management of myasthenia gravis?
A- Atropine
B- Neostigmine
C- Pralidoxime
D- Succinylcholine
Endocrine and Renal Drugs
Question 61. A patient taking metformin develops lactic acidosis. Which condition increases this risk?
A- Hypertension
B- Liver failure
C- Obesity
D- Smoking
Question 62. A patient treated with acetazolamide develops metabolic acidosis. What is the mechanism responsible for this effect?
A- Decreased ammonium excretion
B- Increased bicarbonate excretion
C- Increased hydrogen ion secretion
D- Inhibition of aldosterone release
Question 63. Furosemide-induced ototoxicity results from disrupted ion transport in which structure?
A- Organ of Corti hair cells
B- Vestibular apparatus
C- Stria vascularis of the cochlea
D- Auditory nerve
Question 64. Tamoxifen increases endometrial cancer risk because it acts as a partial estrogen agonist in which tissue?
A- Breast
B- Bone
C- Endometrium
D- Liver
Question 65. A patient receiving long-term glucocorticoid therapy develops osteoporosis. What is the main mechanism responsible for this effect?
A- Decreased calcium absorption and increased bone resorption
B- Decreased osteoclast activity
C- Increased vitamin D activation
D- Increased calcium reabsorption in bone
Question 66. A patient with metastatic prostate cancer is treated with leuprolide. Shortly after therapy begins, his bone pain temporarily worsens. What explains this phenomenon?
A- Direct androgen receptor activation
B- Initial surge in luteinizing hormone and testosterone
C- Inhibition of adrenal steroid synthesis
D- Increased prolactin secretion
Question 67. A patient taking spironolactone develops breast enlargement and sexual dysfunction. What is the mechanism behind this adverse effect?
A- Androgen receptor stimulation
B- Antiandrogen effect
C- Calcium channel blockade
D- Serotonin receptor activation-
Question 68. A patient with type 2 diabetes is started on acarbose. What is the mechanism of action of this drug?
A- Decreases hepatic gluconeogenesis
B- Delays intestinal carbohydrate absorption
C- Increases insulin secretion
D- Improves insulin sensitivity
Question 69. A 55-year-old woman with osteoporosis is prescribed a bisphosphonate. Which instruction is most important to prevent esophageal irritation?
A- Remain upright for 30 minutes after ingestion
B- Take at bedtime
C- Take with milk
D- Use with a proton pump inhibitor
Question 70. A 45-year-old woman treated with methimazole for hyperthyroidism develops fever and sore throat. What is the most appropriate next step?
A- Add propranolol
B- Administer prednisone
C- Continue the medication
D- Stop the drug and check WBC count
Question 71. A 70-year-old woman with hypertension and type 2 diabetes is started on a thiazide diuretic. Which electrolyte imbalance is most likely to occur?
A- Hyperkalemia
B- Hypernatremia
C- Hypocalcemia
D- Hypokalemia
Immunosuppressants, Chemotherapy and Gout Drugs
Question 72. A patient treated with tacrolimus after kidney transplantation develops nephrotoxicity. What is the primary molecular mechanism of tacrolimus?
A- Blocks IL-2 transcription by inhibiting calcineurin
B- Inhibits dihydrofolate reductase
C- Inhibits inosine monophosphate dehydrogenase
D- Stimulates T-cell apoptosis directly
Question 73. A patient treated with mycophenolate mofetil develops leukopenia. What is the primary molecular target of this drug?
A- Dihydrofolate reductase
B- Inosine monophosphate dehydrogenase
C- Thymidylate synthase
D- Xanthine oxidase
Question 74. A patient with acute gout is treated with colchicine. What is the primary mechanism of this drug?
A- Inhibition of uric acid synthesis
B- Inhibition of xanthine oxidase
C- Inhibition of neutrophil microtubule formation
D- Increased renal uric acid secretion
Question 75. Leucovorin rescues normal cells from methotrexate toxicity by bypassing inhibition of which enzyme?
A- Thymidylate synthase
B- Dihydrofolate reductase
C- Ribonucleotide reductase
D- DNA polymerase
Question 76. A patient taking allopurinol for gout should be closely monitored for which serious adverse effect?
A- Aplastic anemia
B- Hepatotoxicity
C- Severe hypersensitivity reaction
D- Thrombocytopenia
Question 77. A patient treated with cisplatin develops hearing loss. What is the mechanism of this adverse effect?
A- Accumulation in cochlear hair cells
B- Autoimmune inner ear inflammation
C- Decreased cerebral perfusion
D- Inhibition of prostaglandin synthesis
Question 78. A patient receiving chemotherapy develops neutropenia. Which drug is used to stimulate neutrophil production?
A- Aminocaproic acid
B- Epoetin alfa
C- Filgrastim
D- Romiplostim
Respiratory, GI, Autonomic and Toxicology
Question 79. A patient taking NSAIDs develops decreased kidney function. What is the mechanism of this effect?
A- Decreased prostaglandin synthesis
B- Increased aldosterone secretion
C- Increased renin release
D- Increased sodium reabsorption
Question 80. A patient with asthma is started on montelukast. What is the mechanism of action of this medication?
A- Blocks leukotriene receptors
B- Inhibits cyclooxygenase
C- Stimulates beta-2 receptors
D- Stimulates muscarinic receptors
Question 81. A patient on long-term NSAID therapy develops gastric ulcers. Which mechanism is responsible?
A- Decreased leukotriene production
B- Direct bacterial injury
C- Increased gastric acid secretion
D- Inhibition of prostaglandin synthesis
Question 82. A patient with chronic obstructive pulmonary disease (COPD) is prescribed tiotropium. What is the mechanism of action of this drug?
A- β₂-adrenergic agonism
B- Leukotriene receptor blocker
C- Muscarinic receptor antagonism
D- Phosphodiesterase inhibition
Question 83. Which drug is most appropriate for the acute management of anaphylaxis?
A- Albuterol
B- Diphenhydramine
C- Epinephrine
D- Hydrocortisone
Question 84. Which medication decreases gastric acid secretion by irreversibly inhibiting the H⁺/K⁺ ATPase pump?
A- Famotidine
B- Misoprostol
C- Omeprazole
D- Sucralfate
Question 85. A 25-year-old man presents with tremors, tachycardia, and anxiety after taking an excessive amount of caffeine. Which of the following drugs has a similar mechanism of action to caffeine?
A- Chlorpromazine
B- Diazepam
C- Metoprolol
D- Theophylline
Question 86. Which of the following drugs is used as an antidote for acetaminophen overdose?
A- Atropine
B- Flumazenil
C- N-acetylcysteine
D- Naloxone
Question 87. A patient with asthma develops tremor and tachycardia after using his inhaler. Which of the following drugs is most likely responsible?
A- Albuterol
B- Ipratropium
C- Beclomethasone
D- Montelukast
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