Simplified guide to oral antipsychotic medications Flashcards
1
Q
First discovered antipsychotic
A
Chlorpromazine
2
Q
What makes it typical
A
D2 antagonism
3
Q
What makes it atypical
A
5ht2 antagonism
4
Q
Division of atypicals
A
1. PINES Olanzapine Quetiapine Asenapine Clozapine 2. DONES Lurasidone Risperidone Paliperidone Iloperidone 3. 2 PIPS Aripiprazole Brexiprazole 4. RIP Cariprazine
5
Q
Olanzapine need to know
A
D2 antagonist H1- weight gain, sedative 5HT2A- antidepressant 5HT2C- antidepressant and weight gain M3- weight gain Greatest cardiometabolic risk Half life- 21-54 hours Metabolised by CYP1A2 and CYP2D6, therefore inhibitors (Fluvox and Cipro) + Paroxetine, can increase levels. Smoking is CYP1A2 inducer and can decrease levels.
6
Q
Quetiapine need to know + triple effect
A
D2-5HT2A antagonist
Metabolite norquetiapine has 5HT2C/7 and alpha 2 antagonism, with 5HT1A agonism and NRI all which mediate antidepressant actions.
IR- short action, hypnotic, not suitable as antipsychotic. Reverse true for XR, more extended D2 occupancy.
50mg IR- hypnotic, 300mg XR antidepressant, 800mg XR antipsychotic
XR for depression because of day long receptor occupancy of 5HT2C and NRI
Minimal EPSE, preferred antipsychotic in Parkinson’s
Metabolised by CYP3A4, induced significantly by Carbamazepine.
HL- 7 hours, Norquetiapine 12 hours.
