Pharmacokinetics 2 Flashcards
Pharmacokinetics of Risperidone?
First-pass hepatic metabolism to 9-hydroxyrisperidone.
What enzyme forms active metabolite of Risperidone?
CYP 2D6 catalyzes hydroxylation
Protein binding of Risperidone?
90%
Protein binding of Risperidone metabolite?
77%
What is the major metabolite of Risperidone?
Paliperidone
Receptor effects of Paliperidone?
5HT2 receptor blocker
Partially blocks D2 receptors
Absorption of Paliperidone?
Gradual water absorption delivers drug molecules slowly
Half life of Quetiapine?
6-12 hours
Dosing of Quetiapine?
Multiple daily dosing is required, but with longer duration once daily dosing is sufficient.
Active metabolite of Aripriprazole?
Dihydroaripiprazole
Half-life of Aripriprazole?
75 hours
Half-life of Dihydroaripiprazole?
94 hours
When is steady state conc of Aripriprazole reached?
14 days
What metabolizes Aripriprazole?
CYP 3A4
CYP 2D6
Protein binding of Aripripraozle?
99%
Which atypical antipsychotics can be given as depots?
Aripiprazole
Palpiperidone
Risperidone microspheres
Olanzapine
Oral dose tapering needed for Aripiprazole depot?
2 weeks oral dose tapering
Oral tapering needed for Paliperidone depot?
Does not need oral tapering
How often is Paliperidone depot given?
Once a month
How is paliperidone depot excreted?
Renal
How does Risperidone microsphere depot work?
Releases active drug at therapeutic levels 3 weeks after injection
How should long-acting risperidone depot be supplemented?
With oral risperidone for 3 weeks
What is olanzapine depot composed of?
Olanzapine and pamoic acid
Half-life of olanzapine depot?
30 days