Page 64 - Medicinal Chemistry Self Assessment
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1.15 Fluvoxamine 53
5. A number of fluvoxamine metabolites have been identified, all of which demonstrate little or no
pharmacological activity. Evaluate each of the metabolic products drawn below and identify which
metabolic transformation has occurred.
A B
C D
F
E
Name of Metabolic Transformation
A
B
C
D
E
F
6. Fluvoxamine is a strong inhibitor of CYP1A2, CYP3A4, and CYP2C19. These enzyme isoforms catalyze
a number of the phase I oxidative metabolic transformations. Several of the benzodiazepines (used
in the treatment of anxiety), including the very popular alprazolam, rely heavily on hepatic oxidation
for metabolic inactivation and elimination. Other benzodiazepines, including the equally popular
lorazepam, rely on glucuronide conjugation for metabolic inactivation and elimination. Which
combination of drugs, fluvoxamine + alprazolam or fluvoxamine + lorazepam, is the most likely to
generate an enhanced anxiolytic effect?
