Pharmacology Review
300 Multiple-Choice Questions with Answers and Rationales
1. Pharmacokinetics, Pharmacodynamics & General
Q1-50
Principles
2. Autonomic Pharmacology Q51-100
3. Cardiovascular, Renal & Hematologic Pharmacology Q101-150
4. CNS, Anesthesia & Pain Pharmacology Q151-200
5. Antimicrobial & Anticancer Pharmacology Q201-250
6. Endocrine, GI, Respiratory, Immunologic & Toxicology Q251-300
For educational review only. Always verify doses and clinical decisions against
current references and local guidelines.
,Pharmacokinetics, Pharmacodynamics & General
Principles
1. Which parameter describes the fraction of an administered dose that reaches the
systemic circulation unchanged?
A. Volume of distribution
B. Half-life
C. Bioavailability
D. Clearance
Answer: C - Bioavailability (F) is the fraction of the dose reaching systemic circulation in active form. By
definition it is 100% for IV administration.
2. A drug with extensive first-pass metabolism will have low bioavailability when given by
which route?
A. Intravenous
B. Transdermal
C. Oral
D. Sublingual
Answer: C - Oral drugs absorbed from the gut pass through the portal circulation and liver before
reaching systemic circulation. IV, sublingual and transdermal routes bypass first-pass metabolism.
3. A lipophilic drug that accumulates in adipose tissue is most likely to have:
A. A small volume of distribution
B. A very large volume of distribution
C. High renal clearance
D. Low oral absorption
Answer: B - Vd = dose / plasma concentration. Drugs sequestered in tissues leave little in plasma, giving
an apparent Vd that can exceed total body water.
4. Which equation correctly relates elimination half-life to other parameters?
A. t1/2 = CL x Vd
B. t1/2 = Vd / (0.693 x CL)
C. t1/2 = 0.693 x CL / Vd
D. t1/2 = 0.693 x Vd / CL
Answer: D - t1/2 = 0.693 x Vd / CL. Half-life increases with larger Vd and decreases with greater
clearance.
5. The loading dose of a drug depends primarily on which parameter?
A. Volume of distribution
B. Renal function
C. Half-life
D. Clearance
Answer: A - Loading dose = (target concentration x Vd) / F. It fills the volume of distribution quickly.
Pharmacology Review - 300 Questions | Page 2
,6. The maintenance dose rate of a drug depends primarily on which parameter?
A. Protein binding
B. Clearance
C. Volume of distribution
D. Lipophilicity
Answer: B - At steady state, dosing rate = CL x Css / F. Clearance determines how much drug must be
given to replace what is eliminated.
7. How many half-lives are needed to reach approximately 94-97% of steady state during
constant dosing?
A. 10
B. 2
C. 1
D. 4-5
Answer: D - Steady state is reached after about 4-5 half-lives, regardless of dose size.
8. Which drug exhibits zero-order (saturable) elimination at high therapeutic doses?
A. Penicillin
B. Amoxicillin
C. Phenytoin
D. Lisinopril
Answer: C - Phenytoin metabolism saturates within the therapeutic range, so small dose increases cause
disproportionate rises in plasma level. Ethanol and high-dose aspirin also show zero-order kinetics.
9. In first-order kinetics, which statement is true?
A. A constant fraction of drug is eliminated per unit time
B. A constant amount of drug is eliminated per unit time
C. Elimination is independent of concentration
D. Half-life increases as concentration rises
Answer: A - First-order elimination removes a constant fraction per unit time; the rate is proportional to
concentration, and half-life is constant.
10. Aspirin overdose is best treated with urinary:
A. No change in pH
B. Alkalinization with sodium bicarbonate
C. Acidification
D. Water restriction
Answer: B - Salicylic acid is a weak acid; alkalinizing the urine ionizes it and traps it in the tubule (ion
trapping), increasing excretion.
11. Which overdose is enhanced by urinary acidification?
A. Methotrexate
B. Phenobarbital
C. Aspirin
D. Amphetamine
Answer: D - Amphetamine is a weak base. In acidic urine it is ionized and trapped, so excretion increases.
Weak acids behave the opposite way.
Pharmacology Review - 300 Questions | Page 3
, 12. Which is a potent inducer of cytochrome P450 enzymes?
A. Ciprofloxacin
B. Rifampin
C. Ketoconazole
D. Cimetidine
Answer: B - Rifampin induces many CYPs (e.g., CYP3A4), lowering levels of warfarin, oral contraceptives
and others. Ketoconazole, cimetidine and ciprofloxacin are inhibitors.
13. Grapefruit juice increases the bioavailability of some oral drugs by inhibiting:
A. CYP3A4 in the intestinal wall
B. Acetylcholinesterase
C. Renal tubular secretion
D. Glucuronyl transferase
Answer: A - Furanocoumarins in grapefruit inhibit intestinal CYP3A4, reducing first-pass metabolism of
drugs such as simvastatin and felodipine.
14. Which of the following is a phase II (conjugation) reaction?
A. Hydrolysis
B. Glucuronidation
C. Reduction
D. Oxidation
Answer: B - Phase I reactions include oxidation, reduction and hydrolysis. Phase II reactions are
conjugations (glucuronidation, acetylation, sulfation).
15. Which benzodiazepines are preferred in elderly patients and liver disease because
they undergo only phase II metabolism?
A. Flurazepam, clonazepam
B. Alprazolam, triazolam
C. Lorazepam, oxazepam, temazepam
D. Diazepam, chlordiazepoxide
Answer: C - Lorazepam, oxazepam and temazepam ("LOT") are glucuronidated, have no active
metabolites, and are less affected by aging and hepatic impairment.
16. Slow acetylators of isoniazid are at increased risk of:
A. Treatment failure
B. Peripheral neuropathy
C. Hemolytic anemia
D. Malignant hyperthermia
Answer: B - Slow acetylators accumulate isoniazid and are more prone to neuropathy (prevented by
pyridoxine) and drug-induced lupus with hydralazine or procainamide.
17. A competitive antagonist causes which change in an agonist dose-response curve?
A. Rightward shift with unchanged Emax
B. Downward shift in Emax with unchanged EC50
C. Leftward shift
D. No change
Answer: A - A competitive antagonist can be overcome with more agonist, so potency (EC50) appears
decreased while Emax is unchanged.
Pharmacology Review - 300 Questions | Page 4
300 Multiple-Choice Questions with Answers and Rationales
1. Pharmacokinetics, Pharmacodynamics & General
Q1-50
Principles
2. Autonomic Pharmacology Q51-100
3. Cardiovascular, Renal & Hematologic Pharmacology Q101-150
4. CNS, Anesthesia & Pain Pharmacology Q151-200
5. Antimicrobial & Anticancer Pharmacology Q201-250
6. Endocrine, GI, Respiratory, Immunologic & Toxicology Q251-300
For educational review only. Always verify doses and clinical decisions against
current references and local guidelines.
,Pharmacokinetics, Pharmacodynamics & General
Principles
1. Which parameter describes the fraction of an administered dose that reaches the
systemic circulation unchanged?
A. Volume of distribution
B. Half-life
C. Bioavailability
D. Clearance
Answer: C - Bioavailability (F) is the fraction of the dose reaching systemic circulation in active form. By
definition it is 100% for IV administration.
2. A drug with extensive first-pass metabolism will have low bioavailability when given by
which route?
A. Intravenous
B. Transdermal
C. Oral
D. Sublingual
Answer: C - Oral drugs absorbed from the gut pass through the portal circulation and liver before
reaching systemic circulation. IV, sublingual and transdermal routes bypass first-pass metabolism.
3. A lipophilic drug that accumulates in adipose tissue is most likely to have:
A. A small volume of distribution
B. A very large volume of distribution
C. High renal clearance
D. Low oral absorption
Answer: B - Vd = dose / plasma concentration. Drugs sequestered in tissues leave little in plasma, giving
an apparent Vd that can exceed total body water.
4. Which equation correctly relates elimination half-life to other parameters?
A. t1/2 = CL x Vd
B. t1/2 = Vd / (0.693 x CL)
C. t1/2 = 0.693 x CL / Vd
D. t1/2 = 0.693 x Vd / CL
Answer: D - t1/2 = 0.693 x Vd / CL. Half-life increases with larger Vd and decreases with greater
clearance.
5. The loading dose of a drug depends primarily on which parameter?
A. Volume of distribution
B. Renal function
C. Half-life
D. Clearance
Answer: A - Loading dose = (target concentration x Vd) / F. It fills the volume of distribution quickly.
Pharmacology Review - 300 Questions | Page 2
,6. The maintenance dose rate of a drug depends primarily on which parameter?
A. Protein binding
B. Clearance
C. Volume of distribution
D. Lipophilicity
Answer: B - At steady state, dosing rate = CL x Css / F. Clearance determines how much drug must be
given to replace what is eliminated.
7. How many half-lives are needed to reach approximately 94-97% of steady state during
constant dosing?
A. 10
B. 2
C. 1
D. 4-5
Answer: D - Steady state is reached after about 4-5 half-lives, regardless of dose size.
8. Which drug exhibits zero-order (saturable) elimination at high therapeutic doses?
A. Penicillin
B. Amoxicillin
C. Phenytoin
D. Lisinopril
Answer: C - Phenytoin metabolism saturates within the therapeutic range, so small dose increases cause
disproportionate rises in plasma level. Ethanol and high-dose aspirin also show zero-order kinetics.
9. In first-order kinetics, which statement is true?
A. A constant fraction of drug is eliminated per unit time
B. A constant amount of drug is eliminated per unit time
C. Elimination is independent of concentration
D. Half-life increases as concentration rises
Answer: A - First-order elimination removes a constant fraction per unit time; the rate is proportional to
concentration, and half-life is constant.
10. Aspirin overdose is best treated with urinary:
A. No change in pH
B. Alkalinization with sodium bicarbonate
C. Acidification
D. Water restriction
Answer: B - Salicylic acid is a weak acid; alkalinizing the urine ionizes it and traps it in the tubule (ion
trapping), increasing excretion.
11. Which overdose is enhanced by urinary acidification?
A. Methotrexate
B. Phenobarbital
C. Aspirin
D. Amphetamine
Answer: D - Amphetamine is a weak base. In acidic urine it is ionized and trapped, so excretion increases.
Weak acids behave the opposite way.
Pharmacology Review - 300 Questions | Page 3
, 12. Which is a potent inducer of cytochrome P450 enzymes?
A. Ciprofloxacin
B. Rifampin
C. Ketoconazole
D. Cimetidine
Answer: B - Rifampin induces many CYPs (e.g., CYP3A4), lowering levels of warfarin, oral contraceptives
and others. Ketoconazole, cimetidine and ciprofloxacin are inhibitors.
13. Grapefruit juice increases the bioavailability of some oral drugs by inhibiting:
A. CYP3A4 in the intestinal wall
B. Acetylcholinesterase
C. Renal tubular secretion
D. Glucuronyl transferase
Answer: A - Furanocoumarins in grapefruit inhibit intestinal CYP3A4, reducing first-pass metabolism of
drugs such as simvastatin and felodipine.
14. Which of the following is a phase II (conjugation) reaction?
A. Hydrolysis
B. Glucuronidation
C. Reduction
D. Oxidation
Answer: B - Phase I reactions include oxidation, reduction and hydrolysis. Phase II reactions are
conjugations (glucuronidation, acetylation, sulfation).
15. Which benzodiazepines are preferred in elderly patients and liver disease because
they undergo only phase II metabolism?
A. Flurazepam, clonazepam
B. Alprazolam, triazolam
C. Lorazepam, oxazepam, temazepam
D. Diazepam, chlordiazepoxide
Answer: C - Lorazepam, oxazepam and temazepam ("LOT") are glucuronidated, have no active
metabolites, and are less affected by aging and hepatic impairment.
16. Slow acetylators of isoniazid are at increased risk of:
A. Treatment failure
B. Peripheral neuropathy
C. Hemolytic anemia
D. Malignant hyperthermia
Answer: B - Slow acetylators accumulate isoniazid and are more prone to neuropathy (prevented by
pyridoxine) and drug-induced lupus with hydralazine or procainamide.
17. A competitive antagonist causes which change in an agonist dose-response curve?
A. Rightward shift with unchanged Emax
B. Downward shift in Emax with unchanged EC50
C. Leftward shift
D. No change
Answer: A - A competitive antagonist can be overcome with more agonist, so potency (EC50) appears
decreased while Emax is unchanged.
Pharmacology Review - 300 Questions | Page 4
