Anxiolytics Medchem Flashcards
what metabolizes buspirone?
what are the 2 metabolites?
3A4
1-PP and 6’-hydroxybuspirone
what is buspirones t1/2?
2-4 hours
what drug class is buspirone?
5HT1A agonist
what are the requirements of the structuring of benzos?
- a seven membered ring
- EWG at position 7
what does adding an EWG at position 2’ of benzos do?
increases potency
what is the name of the first benzo?
chlordiazepoxide
diazepam undergoes hydroxylation to become? active or inactive?
3-hydroxydiazepam (temazepam)
active
diazepam undergoes n-demethylation to become? active or inactive?
N-desmethyldiazepam (nordazepam)
active
both metabolites of diazepam are further metabolized into? active or inactive?
oxazepam
active
what metabolism inactivates oxazepam?
glucuronidation
what is unique about clorazepate?
its a prodrug
clorazepate undergoes decarboxylation into? active or inactive?
nordazepam
active
why is lorazepam more potent than oxazepam?
has a 2’ EWG making it more potent
what metabolism does lorazepam undergo?
active or inactive
glucuronidation
inactive
alprazolam undergoes cyp3A4 metabolism into what to metabolites?
4-hydroxyalprazolam
alpha-hydroxyalprazolam
clonazepam is reduced into? active or inactive?
7-aminoclonazepam
inactive
midazolam undergoes what route of metabolism?
3A4
what route of metabolism does triazolam undergo?
3A4
what drug is used to reverse the effects of BZDs?
flumazenil
all barbiturates are inducers of what metabolism?
Cyps
which barbiturate is used to induce anesthesia?
methohexital
what route of metabolism does zolpidem undergo?
3A4
what is the minor route of metabolism of zaleplon?
3A4
what is the major route of metabolism of zaleplon?
aldehyde oxidase
