TEST BANK
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A pharmacologist isolates a bioactive compound from a medicinal plant
and then modifies its chemical structure to improve potency and reduce
toxicity. What stage of drug discovery is most directly represented by
this process?
A. Clinical outcome assessment
B. Lead optimization
,C. Postmarketing surveillance
D. Therapeutic drug monitoring
Correct Answer:
B. Lead optimization
Rationale:
Lead optimization involves systematically modifying a promising
chemical compound to improve desirable properties such as potency,
selectivity, pharmacokinetics, and safety. A naturally occurring molecule
can serve as a starting lead, but further chemical refinement is usually
necessary before it becomes a viable drug candidate.
• A is incorrect because clinical outcome assessment occurs after a
candidate has advanced into clinical development.
• C is incorrect because postmarketing surveillance occurs after
regulatory approval and widespread clinical use.
• D is incorrect because therapeutic drug monitoring evaluates drug
concentrations during clinical treatment rather than optimizing a
lead molecule.
Question 2
Why have medicinal plants historically been important sources for drug
discovery?
A. Plant-derived compounds are automatically safe in humans
B. Plants produce chemically diverse molecules with biological activity
C. Plant compounds generally require no structural modification
D. Plant-derived drugs are exempt from pharmacological testing
, Correct Answer:
B. Plants produce chemically diverse molecules with biological activity
Rationale:
Plants synthesize diverse secondary metabolites, some of which interact
with biological targets and can provide useful starting points for
therapeutic discovery. Natural products have therefore served as
important sources of pharmacologically active molecules.
• A is incorrect because natural origin does not guarantee safety.
• C is incorrect because many natural products require modification
to improve their pharmacological properties.
• D is incorrect because natural products still require rigorous
pharmacological and toxicological evaluation.
Question 3
A newly isolated natural product produces a measurable biological
effect but has poor oral activity because it is extensively metabolized
before reaching systemic circulation. Which property is primarily
limiting its usefulness as an orally administered drug?
A. Receptor efficacy
B. Bioavailability
C. Therapeutic index
D. Receptor affinity
Correct Answer:
B. Bioavailability
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A pharmacologist isolates a bioactive compound from a medicinal plant
and then modifies its chemical structure to improve potency and reduce
toxicity. What stage of drug discovery is most directly represented by
this process?
A. Clinical outcome assessment
B. Lead optimization
,C. Postmarketing surveillance
D. Therapeutic drug monitoring
Correct Answer:
B. Lead optimization
Rationale:
Lead optimization involves systematically modifying a promising
chemical compound to improve desirable properties such as potency,
selectivity, pharmacokinetics, and safety. A naturally occurring molecule
can serve as a starting lead, but further chemical refinement is usually
necessary before it becomes a viable drug candidate.
• A is incorrect because clinical outcome assessment occurs after a
candidate has advanced into clinical development.
• C is incorrect because postmarketing surveillance occurs after
regulatory approval and widespread clinical use.
• D is incorrect because therapeutic drug monitoring evaluates drug
concentrations during clinical treatment rather than optimizing a
lead molecule.
Question 2
Why have medicinal plants historically been important sources for drug
discovery?
A. Plant-derived compounds are automatically safe in humans
B. Plants produce chemically diverse molecules with biological activity
C. Plant compounds generally require no structural modification
D. Plant-derived drugs are exempt from pharmacological testing
, Correct Answer:
B. Plants produce chemically diverse molecules with biological activity
Rationale:
Plants synthesize diverse secondary metabolites, some of which interact
with biological targets and can provide useful starting points for
therapeutic discovery. Natural products have therefore served as
important sources of pharmacologically active molecules.
• A is incorrect because natural origin does not guarantee safety.
• C is incorrect because many natural products require modification
to improve their pharmacological properties.
• D is incorrect because natural products still require rigorous
pharmacological and toxicological evaluation.
Question 3
A newly isolated natural product produces a measurable biological
effect but has poor oral activity because it is extensively metabolized
before reaching systemic circulation. Which property is primarily
limiting its usefulness as an orally administered drug?
A. Receptor efficacy
B. Bioavailability
C. Therapeutic index
D. Receptor affinity
Correct Answer:
B. Bioavailability
