Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A pharmacologist is investigating a plant traditionally used for relieving
pain. Laboratory studies identify a purified compound from the plant
that produces a reproducible biological effect. Which feature best
explains why medicinal plants have historically been valuable starting
points for drug discovery?
,A. Plant-derived compounds are automatically safe for human use.
B. Traditional use can provide empirical clues about biologically active
chemical constituents.
C. Plant compounds generally require no chemical characterization.
D. Natural products usually have predictable pharmacokinetic profiles.
Correct Answer:
B. Traditional use can provide empirical clues about biologically active
chemical constituents.
Rationale:
Traditional medicinal use can serve as an empirical starting point for
identifying biologically active molecules, after which isolation,
characterization, and pharmacological testing can be performed.
Natural origin does not guarantee safety, predictable pharmacokinetics,
or absence of a need for characterization.
Question 2
During optimization of a promising chemical series, a medicinal chemist
changes a substituent on one region of the molecule and observes a
large increase in potency. Which concept is being investigated?
A. Bioavailability
B. Structure–activity relationship
C. Pharmacovigilance
D. Therapeutic equivalence
Correct Answer:
B. Structure–activity relationship
, Rationale:
A structure–activity relationship (SAR) describes how changes in
chemical structure affect biological activity. Comparing related
molecules allows investigators to identify structural features that
improve potency, selectivity, or other desirable properties.
Bioavailability concerns systemic exposure, whereas pharmacovigilance
concerns drug safety monitoring after exposure.
Question 3
A compound identified during screening binds a disease-relevant target
and produces a desirable biological effect, but it still requires chemical
modification before it can be considered a viable therapeutic candidate.
Which term best describes this compound?
A. Approved drug
B. Lead compound
C. Biologic license
D. Pharmacological antagonist
Correct Answer:
B. Lead compound
Rationale:
A lead compound is a promising starting molecule that demonstrates
useful biological activity but requires additional optimization before
development as a drug. Identification of a lead does not mean that
efficacy, pharmacokinetics, safety, or clinical utility have already been
established.