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IDT Fall > Anxiolytics Medchem > Flashcards

Anxiolytics Medchem Flashcards

1
Q

what metabolizes buspirone?
what are the 2 metabolites?

A

3A4
1-PP and 6’-hydroxybuspirone

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2
Q

what is buspirones t1/2?

A

2-4 hours

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3
Q

what drug class is buspirone?

A

5HT1A agonist

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4
Q

what are the requirements of the structuring of benzos?

A
  1. a seven membered ring
  2. EWG at position 7
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5
Q

what does adding an EWG at position 2’ of benzos do?

A

increases potency

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6
Q

what is the name of the first benzo?

A

chlordiazepoxide

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7
Q

diazepam undergoes hydroxylation to become? active or inactive?

A

3-hydroxydiazepam (temazepam)
active

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8
Q

diazepam undergoes n-demethylation to become? active or inactive?

A

N-desmethyldiazepam (nordazepam)
active

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9
Q

both metabolites of diazepam are further metabolized into? active or inactive?

A

oxazepam
active

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10
Q

what metabolism inactivates oxazepam?

A

glucuronidation

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11
Q

what is unique about clorazepate?

A

its a prodrug

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12
Q

clorazepate undergoes decarboxylation into? active or inactive?

A

nordazepam
active

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13
Q

why is lorazepam more potent than oxazepam?

A

has a 2’ EWG making it more potent

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14
Q

what metabolism does lorazepam undergo?
active or inactive

A

glucuronidation
inactive

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15
Q

alprazolam undergoes cyp3A4 metabolism into what to metabolites?

A

4-hydroxyalprazolam
alpha-hydroxyalprazolam

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16
Q

clonazepam is reduced into? active or inactive?

A

7-aminoclonazepam
inactive

17
Q

midazolam undergoes what route of metabolism?

A

3A4

18
Q

what route of metabolism does triazolam undergo?

A

3A4

19
Q

what drug is used to reverse the effects of BZDs?

A

flumazenil

20
Q

all barbiturates are inducers of what metabolism?

A

Cyps

21
Q

which barbiturate is used to induce anesthesia?

A

methohexital

22
Q

what route of metabolism does zolpidem undergo?

A

3A4

23
Q

what is the minor route of metabolism of zaleplon?

A

3A4

24
Q

what is the major route of metabolism of zaleplon?

A

aldehyde oxidase

25
Q

what route of metabolism does eszopiclone undergo?

A

3A4

26
Q

what drug class is ramelteon?

A

melatonin receptor agonist

27
Q

what routes of metabolism does ramelteon undergo?

A

1A2 and 2C19

28
Q

ramelteon should not be used with fluvoxamine because?

A

fluvoxamine inhibits 1A2 and 2C19

29
Q

what routes of metabolism does tasimelteon undergo?

A

1A2 and 3A4

30
Q

what drug class is tasimelteon?

A

melatonin receptor agonist

31
Q

what are the three orexin receptor antagonists?

A

suvorexant
lemborexant
daridorexant

32
Q

all three orexin receptor antagonists are metabolized by?

A

3A4

IDT Fall (29 decks)

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