Comparative Pharmacology
Head-to-head clinical analysis: CLOZAPINE versus INVEGA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CLOZAPINE versus INVEGA.
CLOZAPINE vs INVEGA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Atypical antipsychotic; binds to dopamine D4, serotonin 5-HT2A, and adrenergic α2 receptors; weak D2 antagonist with rapid dissociation; also affects histaminergic and cholinergic receptors.
Paliperidone is the major active metabolite of risperidone. It is a benzisoxazole derivative antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also acts as an antagonist at α1 and α2 adrenergic receptors and H1 histaminergic receptors. It has no affinity for muscarinic receptors.
Initial: 12.5 mg orally once or twice daily; titrate gradually by 25-50 mg/day to target dose 300-450 mg/day in divided doses; max 900 mg/day.
Oral: 6 mg once daily; may increase to 9 mg/day if needed. IM (extended-release): 234 mg on day 1, 156 mg on day 8, then 117 mg monthly; adjust within range 39-234 mg per month.
None Documented
None Documented
Clinical Note
moderateClozapine + Norfloxacin
"Clozapine may increase the QTc-prolonging activities of Norfloxacin."
Clinical Note
moderateClozapine + Torasemide
"The risk or severity of adverse effects can be increased when Clozapine is combined with Torasemide."
Clinical Note
moderateClozapine + Etacrynic acid
"The risk or severity of adverse effects can be increased when Clozapine is combined with Etacrynic acid."
Clinical Note
moderateClozapine + Furosemide
Terminal elimination half-life is 8 to 12 hours (steady-state), but can range from 4 to 66 hours; requires dose adjustment in renal/hepatic impairment.
Terminal elimination half-life is approximately 23-29 hours for oral administration (paliperidone extended-release). Once-daily dosing achieves steady-state within 4-5 days.
Approximately 50% of the dose is excreted in urine (30% as unchanged drug and metabolites) and 30% in feces via biliary elimination.
Primarily renal: 59-80% of dose excreted unchanged in urine (as parent drug and metabolites). Fecal: ~20-30%. Biliary elimination is minimal.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic
"The risk or severity of adverse effects can be increased when Clozapine is combined with Furosemide."