Comparative Pharmacology
Head-to-head clinical analysis: RISPERIDONE versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: RISPERIDONE versus SAPHRIS.
RISPERIDONE vs SAPHRIS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Risperidone is an atypical antipsychotic that antagonizes dopamine D2 receptors and serotonin 5-HT2A receptors. It also has moderate affinity for alpha1-adrenergic and H1-histaminergic receptors, and low affinity for muscarinic 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 2 mg orally once daily, titrated to target dose of 4-6 mg orally once daily (or divided twice daily); maximum 16 mg/day. Alternatively, long-acting IM injection: 25 mg IM every 2 weeks.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
None Documented
None Documented
Clinical Note
moderateRisperidone + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Fluticasone propionate."
Clinical Note
moderateRisperidone + Methylphenidate
"The risk or severity of adverse effects can be increased when Risperidone is combined with Methylphenidate."
Clinical Note
moderateRisperidone + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Risperidone."
Clinical Note
moderateRisperidone: 3 hours (CYP2D6 extensive metabolizers), 20 hours (poor metabolizers); active metabolite 9-hydroxyrisperidone: 21-30 hours; steady-state reached in 5-6 days
Terminal elimination half-life is 30-40 hours, supporting once-daily dosing.
Renal (70% as metabolites, 14% as parent drug) and fecal (14%)
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
Risperidone + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Risperidone."