Asenapine

Asenapine Indications: FDA-Approved Uses

Source: Drug labeling information submitted to the Food and Drug Administration (FDA), updated by the National Library of Medicine (NLM). Asenapine (SAPHRIS) is a second generation antipsychotic approved for the treatment of schizophrenia and manic episodes in bipolar I disorder. The table below summarizes the dosing for each FDA-approved indication: Data from Clinical Trials Schizophrenia…

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Asenapine Interactions

Source: Drug labeling information submitted to the Food and Drug Administration (FDA), updated by the National Library of Medicine (NLM). The risks of using SAPHRIS in combination with other drugs have not been extensively evaluated. Given the primary CNS effects of SAPHRIS, caution should be used when it is taken in combination with other centrally acting…

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Asenapine Adverse Effects

Source: Drug labeling information submitted to the Food and Drug Administration (FDA), updated by the National Library of Medicine (NLM). Commonly observed adverse reactions (incidence ≥5% and at least twice that for placebo) were: Schizophrenia: akathisia, oral hypoesthesia, and somnolence. Bipolar Disorder (Monotherapy): somnolence, dizziness, extrapyramidal symptoms other than akathisia, and weight increased. Bipolar Disorder (Adjunctive):…

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Mechanism of Action and Pharmacodynamics of Asenapine

By Flavio Guzman, MD Asenapine is a second-generation antipsychotic that acts as antagonist at 5HT2A and D2 receptors. The image below shows a schematic view of the pharmacodynamic profile of the drug. The mechanism of action of asenapine, as with other drugs having efficacy in schizophrenia and bipolar disorder, is unknown. It has been suggested that…

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Asenapine (SAPHRIS) Pharmacokinetics

Source: Drug labeling information submitted to the Food and Drug Administration (FDA), updated by the National Library of Medicine (NLM). Following a single 5-mg dose of SAPHRIS, the mean Cmax was approximately 4 ng/mL and was observed at a mean tmax of 1 hour. Elimination of asenapine is primarily through direct glucuronidation by UGT1A4 and…

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