Edition by Bertram G. Katzung,
structured for the updated 2026/2027
syllabus||newest version
Section 1: General Principles (Questions 1-15)
1. A drug that binds to a receptor and produces a maximal biological response
that is less than that of an endogenous agonist is best described as a:
a) Full agonist
b) Inverse agonist
c) Partial agonist
d) Competitive antagonist
e) Noncompetitive antagonist
ANSWER ✓ Partial agonist
2. Which of the following pharmacokinetic parameters is defined as the volume of
plasma from which a drug is completely removed per unit time?
a) Volume of distribution (Vd)
b) Elimination half-life (t½)
c) Clearance (Cl)
d) Bioavailability (F)
e) Area under the curve (AUC)
ANSWER ✓ Clearance (Cl)
3. A drug follows first-order kinetics. After administering a single intravenous
dose, how many half-lives are required for the drug to reach 97% elimination?
a) 2
,b) 3
c) 5
d) 7
e) 10
ANSWER ✓ 5
4. A drug with a very high volume of distribution (e.g., > 200 L in a 70 kg adult) is
most likely to be:
a) Highly bound to plasma albumin
b) Highly water-soluble
c) Accumulating in adipose or tissue binding sites
d) Confined to the vascular compartment
e) Excreted unchanged by the kidneys
ANSWER ✓ Accumulating in adipose or tissue binding sites
5. Which phase of drug metabolism (biotransformation) typically involves
conjugation reactions such as glucuronidation or acetylation?
a) Phase I
b) Phase II
c) Phase III
d) Absorption phase
e) Distribution phase
ANSWER ✓ Phase II
6. A patient with liver cirrhosis has reduced synthesis of albumin. How will this
most likely affect the pharmacokinetics of a drug that is normally 95% protein-
bound?
a) Decreased volume of distribution
b) Increased free drug concentration
c) Decreased elimination half-life
d) Decreased hepatic clearance
,e) Increased first-pass metabolism
ANSWER ✓ Increased free drug concentration
7. The therapeutic index (TI) of a drug is calculated as:
a) ED50 / TD50
b) TD50 / ED50
c) LD50 / ED50
d) ED50 / LD50
e) EC50 / IC50
ANSWER ✓ TD50 / ED50
8. Which route of administration is associated with 100% bioavailability, bypasses
absorption barriers, and is used for drugs that are poorly soluble or irritating?
a) Oral
b) Intramuscular
c) Subcutaneous
d) Intravenous
e) Transdermal
ANSWER ✓ Intravenous
9. The process by which a drug moves from the site of administration into the
systemic circulation is called:
a) Distribution
b) Metabolism
c) Excretion
d) Absorption
e) Bioavailability
ANSWER ✓ Absorption
10. Which of the following is a characteristic of zero-order elimination kinetics?
a) A constant fraction of the drug is eliminated per unit time
b) The half-life is constant regardless of dose
, c) A constant amount of the drug is eliminated per unit time
d) It is the typical kinetic process for most drugs at therapeutic doses
e) Clearance is directly proportional to drug concentration
ANSWER ✓ A constant amount of the drug is eliminated per unit time
11. An antagonist that binds to the same site on the receptor as the agonist but
does not activate it, and its effect can be overcome by increasing the
concentration of the agonist, is a:
a) Irreversible antagonist
b) Physiological antagonist
c) Chemical antagonist
d) Competitive antagonist
e) Noncompetitive antagonist
ANSWER ✓ Competitive antagonist
12. Which of the following is a Phase I metabolic reaction?
a) Glucuronidation
b) Acetylation
c) Oxidation via cytochrome P450
d) Sulfation
e) Methylation
ANSWER ✓ Oxidation via cytochrome P450
13. The steady-state concentration of a drug is achieved after approximately how
many half-lives of continuous dosing?
a) 1-2
b) 3-5
c) 6-8
d) 9-10
e) 12-15
ANSWER ✓ 3-5