a
Which drug is a MOR/KOR agonist and DOR antagonist?
a) eluxadoline
b) oliceridine
c) tapentadol
d) tramadol
d
Which drug is metabolized via O-demethylation?
a) eluxadoline
b) oliceridine
c) tapentadol
d) tramadol
c
Which drug is a MOR agonist and NE reuptake inhibitor?
a) eluxadoline
b) oliceridine
c) tapentadol
d) tramadol
a
Which isomer is a weak MOR agonist?
a) tramadol (+)
b) tramadol (-)
b
Which isomer inhibits NE reuptake?
a) tramadol (+)
b) tramadol (-)
b
Which was designed to reduce respiratory depression?
a) eluxadoline
b) oliceridine
c) tapentadol
d) tramadol
5; 16
Morphine contains ______ stereogenic centers and ______ stereoisomers exist.
tertiary basic amine (N17), central carbon w/no hydrogens (C13), phenyl ring (C13), two carbons between C13 and N17
Which structures MUST be in Morphine (4)
methyl; alkyl
_______ are agonists and ______ groups are antagonist.
b
Codeine undergoes ________ to become Morphine.
a) n-demethylation
b) o-demethylation
a
Codeine undergoes ________ to become Norcodeine.
a) n-demethylation
b) o-demethylation
naltrexone, nalmefene
Which MOR antagonists are orally active? (2)
CYP3A4 N-demethylation
How is Meperidine metabolized?
no CNS; PGP substrate
Loperamide has _________ effects. This is due to the addition of a _______.
CYP3A4 N-dealkylation
Fentanyl & Fentanyl-derived drugs are metabolized via