Antipsychotic Medchem Flashcards
What SEs would you expect from chlorpromazine?
antimuscarinic, sedative (H1), and hypotension (alpha 1)
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?
chlorpromazine causes sun sensitivity, so you need to wear protective clothing when in sunlight
what chemical class is chlorpromazine?
phenothiazine
what are the structural requirements of phenothiazines?
-position 2 is best position for substitution
-3 carbon chain connecting nitrogens is required
-basic nitrogen substituents required: tertiary amines have optimal activity
T/F a tertiary amine phenothiazine is required for passage thru BBB
True
what classification is fluphenazine?
phenothiazine
what is fluphenazine decanoate?
an injectable prodrug of fluphenazine. it is slowly released into the active form over 3-4 wks
what classification is thioridazine?
phenothiazine
why is thioridazine not recommended for use in 2D6 poor metabolizers?
it has QT prolongation
what classification is clozapine?
dibenzazepine
how can you classify a drug as a dibenzazepine?
has a 7 membered ring
why does clozapine have a risk of granulocytosis?
it can be metabolized by 3A4 into a reactive nitrenium ion
what classification is olanzapine?
dibenzazepine
what is olanzapine pamoate used for?
IM injection
what classification is loxapine?
dibenzooxazepine
what classification is quetiapine?
dibenzothiazepine
what class is asenapine?
dibenzhydrooxepine
which antipsych is used as a transdermal patch?
asenapine
what is the major metabolism of asenapine?
direct glucuronidation
what is the minor metabolism of asenapine?
N-demethylation
what class is haloperidol?
fluorobutyrophenone
two major routes of metabolism of haloperidol?
n-dealkylation and reduction
what is haldol decanoate?
prodrug of haloperidol for injection
what is the minor route of metabolism of haloperidol?
what is it called?
3A4 oxidation
HPP+
what class is lumateperone?
fluorobutyrophenone
lumateperone should be avoided w/ strong _____ inhibitors/inducers
3A4
what is the active metabolite of risperidone?
paliperidone
what is paliperidone palmitate?
ester prodrug for injection
Ziprasidone undergoes 1) aldehyde oxidase then 2) S-methylation into?
S-methyl metabolite
what is aripiprazole lauroxil?
lipophilic prodrug for injection
what is pimavanserin used for?
parkinson’s associated psychoses
what is Tetrabenazine used for?
to treat tardive dyskinesia
what drug class is Tetrabenazine?
VMAT 2 inhibitor
Deutetrabenazine is used for?
to treat tardive dyskinesia
what drug class is Deutetrabenazine?
VMAT 2 inhibitor
what is Valbenazine used for?
to treat tardive dyskinesia
what drug class is Valbenazine?
VMAT 2 inhibitor
use caution with Valbenazine and _________ inhibitors
3A4 and 2D6
name the drugs with 3A4 metabolism as only CYP pathway
Quetiapine
Haloperidol
Ziprasidone
Lurasidone
Pimavanserin
name the drugs with 2D6 metabolism as only CYP pathway
Thioridazine
Risperidone
name the drugs with both 3A4 and 2D6 metabolism
Chlorpromazine
Iloperidone
Aripiprazole
Brexpiprazole
Cariprazine
name the drugs with 1A2 metabolism as only CYP pathway
olanzapine
name the drugs with both 3A4 and 1A2 metabolism
Clozapine
Lumateperone
which drugs have long acting injectable formulations?
fluphenazine
haloperidol
aripiprazole
risperidone
paliperidone
olanzapine
