Comparative Pharmacology
Head-to-head clinical analysis: CLOZAPINE versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CLOZAPINE versus SAPHRIS.
CLOZAPINE vs SAPHRIS
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.
Asenapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors; dopamine D2, D3, and D4 receptors; and alpha2-adrenergic receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic receptors, and low affinity for muscarinic M1 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.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
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 30-40 hours, supporting once-daily dosing.
Approximately 50% of the dose is excreted in urine (30% as unchanged drug and metabolites) and 30% in feces via biliary elimination.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
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."