Antipsychotic Medchem

Question 1

What SEs would you expect from chlorpromazine?

Answer 1

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

Question 2

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?

Answer 2

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

Question 3

what chemical class is chlorpromazine?

Answer 3

phenothiazine

Question 4

what are the structural requirements of phenothiazines?

Answer 4

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

Question 5

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

Answer 5

True

Question 6

what classification is fluphenazine?

Answer 6

phenothiazine

Question 7

what is fluphenazine decanoate?

Answer 7

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

Question 8

what classification is thioridazine?

Answer 8

phenothiazine

Question 9

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

Answer 9

it has QT prolongation

Question 10

what classification is clozapine?

Answer 10

dibenzazepine

Question 11

how can you classify a drug as a dibenzazepine?

Answer 11

has a 7 membered ring

Question 12

why does clozapine have a risk of granulocytosis?

Answer 12

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

Question 13

what classification is olanzapine?

Answer 13

dibenzazepine

Question 14

what is olanzapine pamoate used for?

Answer 14

IM injection

Question 15

what classification is loxapine?

Answer 15

dibenzooxazepine

Question 16

what classification is quetiapine?

Answer 16

dibenzothiazepine

Question 17

what class is asenapine?

Answer 17

dibenzhydrooxepine

Question 18

which antipsych is used as a transdermal patch?

Answer 18

asenapine

Question 19

what is the major metabolism of asenapine?

Answer 19

direct glucuronidation

Question 20

what is the minor metabolism of asenapine?

Answer 20

N-demethylation

Question 21

what class is haloperidol?

Answer 21

fluorobutyrophenone

Question 22

two major routes of metabolism of haloperidol?

Answer 22

n-dealkylation and reduction

Question 23

what is haldol decanoate?

Answer 23

prodrug of haloperidol for injection

Question 24

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

Answer 24

3A4 oxidation
HPP+

Question 25

what class is lumateperone?

Answer 25

fluorobutyrophenone

Question 26

lumateperone should be avoided w/ strong _____ inhibitors/inducers

Answer 26

3A4

Question 27

what is the active metabolite of risperidone?

Answer 27

paliperidone

Question 28

what is paliperidone palmitate?

Answer 28

ester prodrug for injection

Question 29

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

Answer 29

S-methyl metabolite

Question 30

what is aripiprazole lauroxil?

Answer 30

lipophilic prodrug for injection

Question 31

what is pimavanserin used for?

Answer 31

parkinson's associated psychoses

Question 32

what is Tetrabenazine used for?

Answer 32

to treat tardive dyskinesia

Question 33

what drug class is Tetrabenazine?

Answer 33

VMAT 2 inhibitor

Question 34

Deutetrabenazine is used for?

Answer 34

to treat tardive dyskinesia

Question 35

what drug class is Deutetrabenazine?

Answer 35

VMAT 2 inhibitor

Question 36

what is Valbenazine used for?

Answer 36

to treat tardive dyskinesia

Question 37

what drug class is Valbenazine?

Answer 37

VMAT 2 inhibitor

Question 38

use caution with Valbenazine and _________ inhibitors

Answer 38

3A4 and 2D6

Question 39

name the drugs with 3A4 metabolism as only CYP pathway

Answer 39

Quetiapine Haloperidol Ziprasidone Lurasidone Pimavanserin

Question 40

name the drugs with 2D6 metabolism as only CYP pathway

Answer 40

Thioridazine Risperidone

Question 41

name the drugs with both 3A4 and 2D6 metabolism

Answer 41

Chlorpromazine Iloperidone Aripiprazole Brexpiprazole Cariprazine

Question 42

name the drugs with 1A2 metabolism as only CYP pathway

Answer 42

olanzapine

Question 43

name the drugs with both 3A4 and 1A2 metabolism

Answer 43

Clozapine Lumateperone

Question 44

which drugs have long acting injectable formulations?

Answer 44

fluphenazine haloperidol aripiprazole risperidone paliperidone olanzapine