Pharmaceutical Chemistry and Drug Design Flashcards
6 cards from real Pharm.D. Doctor of Pharmacy practice questions. Tap to flip, then mark Knew It or Still Learning — missed cards come back until you master them.
Read the first 6 Pharmaceutical Chemistry and Drug Design flashcards as text
Which phenomenon causes a drug to lose efficacy over time as the body reduces receptor expression or sensitivity?
Answer: Tachyphylaxis / receptor downregulation
Tachyphylaxis (acute tolerance) and receptor downregulation occur when prolonged drug exposure causes receptors to be internalized or decreased, reducing drug effect.
Which functional group undergoes Phase II glucuronidation conjugation during drug metabolism?
Answer: Hydroxyl, carboxyl, amino, or sulfhydryl groups
Phase II glucuronidation conjugates hydroxyl (–OH), carboxyl (–COOH), amino (–NH2), or sulfhydryl (–SH) groups with glucuronic acid to increase water solubility for excretion.
Isoteric replacement in medicinal chemistry refers to:
Answer: Substituting one atom or group with another of similar size and electronic properties to optimize activity
Isosteric replacement involves substituting atoms or groups with similar steric and electronic properties to optimize pharmacological activity, selectivity, or pharmacokinetics.
Which class of drugs acts as competitive inhibitors of HMG-CoA reductase in cholesterol biosynthesis?
Answer: Statins
Statins (e.g., atorvastatin, simvastatin) competitively inhibit HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis.
A pharmacophore is best defined as:
Answer: The three-dimensional arrangement of functional groups essential for a drug's biological activity
A pharmacophore is the ensemble of steric and electronic features necessary to ensure optimal interactions with a specific biological target and trigger or block its biological response.
Which type of formulation is used to extend drug release and reduce dosing frequency?
Answer: Extended-release (ER) formulations
Extended-release formulations use various technologies (matrix, reservoir, osmotic pump) to slowly release drug over an extended period, reducing dosing frequency and improving adherence.