Antipsychotic Medchem Flashcards

1
Q

What SEs would you expect from chlorpromazine?

A

antimuscarinic, sedative (H1), and hypotension (alpha 1)

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2
Q

a patient calls the pharmacy to report a painful rash on their arm. They stated they were outside for a couple hours yesterday, but it is worse than a normal sunburn you see in their medication list they are on chlorpromazine. what do you tell the patient?

A

chlorpromazine causes sun sensitivity, so you need to wear protective clothing when in sunlight

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3
Q

what chemical class is chlorpromazine?

A

phenothiazine

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4
Q

what are the structural requirements of phenothiazines?

A

-position 2 is best position for substitution
-3 carbon chain connecting nitrogens is required
-basic nitrogen substituents required: tertiary amines have optimal activity

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5
Q

T/F a tertiary amine phenothiazine is required for passage thru BBB

A

True

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6
Q

what classification is fluphenazine?

A

phenothiazine

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7
Q

what is fluphenazine decanoate?

A

an injectable prodrug of fluphenazine. it is slowly released into the active form over 3-4 wks

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8
Q

what classification is thioridazine?

A

phenothiazine

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9
Q

why is thioridazine not recommended for use in 2D6 poor metabolizers?

A

it has QT prolongation

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10
Q

what classification is clozapine?

A

dibenzazepine

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11
Q

how can you classify a drug as a dibenzazepine?

A

has a 7 membered ring

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12
Q

why does clozapine have a risk of granulocytosis?

A

it can be metabolized by 3A4 into a reactive nitrenium ion

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13
Q

what classification is olanzapine?

A

dibenzazepine

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14
Q

what is olanzapine pamoate used for?

A

IM injection

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15
Q

what classification is loxapine?

A

dibenzooxazepine

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16
Q

what classification is quetiapine?

A

dibenzothiazepine

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17
Q

what class is asenapine?

A

dibenzhydrooxepine

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18
Q

which antipsych is used as a transdermal patch?

A

asenapine

19
Q

what is the major metabolism of asenapine?

A

direct glucuronidation

20
Q

what is the minor metabolism of asenapine?

A

N-demethylation

21
Q

what class is haloperidol?

A

fluorobutyrophenone

22
Q

two major routes of metabolism of haloperidol?

A

n-dealkylation and reduction

23
Q

what is haldol decanoate?

A

prodrug of haloperidol for injection

24
Q

what is the minor route of metabolism of haloperidol?
what is it called?

A

3A4 oxidation
HPP+

25
Q

what class is lumateperone?

A

fluorobutyrophenone

26
Q

lumateperone should be avoided w/ strong _____ inhibitors/inducers

A

3A4

27
Q

what is the active metabolite of risperidone?

A

paliperidone

28
Q

what is paliperidone palmitate?

A

ester prodrug for injection

29
Q

Ziprasidone undergoes 1) aldehyde oxidase then 2) S-methylation into?

A

S-methyl metabolite

30
Q

what is aripiprazole lauroxil?

A

lipophilic prodrug for injection

31
Q

what is pimavanserin used for?

A

parkinson’s associated psychoses

32
Q

what is Tetrabenazine used for?

A

to treat tardive dyskinesia

33
Q

what drug class is Tetrabenazine?

A

VMAT 2 inhibitor

34
Q

Deutetrabenazine is used for?

A

to treat tardive dyskinesia

35
Q

what drug class is Deutetrabenazine?

A

VMAT 2 inhibitor

36
Q

what is Valbenazine used for?

A

to treat tardive dyskinesia

37
Q

what drug class is Valbenazine?

A

VMAT 2 inhibitor

38
Q

use caution with Valbenazine and _________ inhibitors

A

3A4 and 2D6

39
Q

name the drugs with 3A4 metabolism as only CYP pathway

A

Quetiapine
Haloperidol
Ziprasidone
Lurasidone
Pimavanserin

40
Q

name the drugs with 2D6 metabolism as only CYP pathway

A

Thioridazine
Risperidone

41
Q

name the drugs with both 3A4 and 2D6 metabolism

A

Chlorpromazine
Iloperidone
Aripiprazole
Brexpiprazole
Cariprazine

42
Q

name the drugs with 1A2 metabolism as only CYP pathway

A

olanzapine

43
Q

name the drugs with both 3A4 and 1A2 metabolism

A

Clozapine
Lumateperone

44
Q

which drugs have long acting injectable formulations?

A

fluphenazine
haloperidol
aripiprazole
risperidone
paliperidone
olanzapine