The Medical Letter on Drugs and Therapeutics
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Asenapine (Saphris) Sublingual Tablets for Schizophrenia and Bipolar Disorder

Asenapine (Saphris – Schering-Plough), a dibenzo-oxepino pyrrole, has been approved by the FDA in a sublingual tablet formulation for acute treatment of schizophrenia and manic or mixed episodes associated with bipolar disorder. It is the sixth second-generation antipsychotic approved by the FDA for use in bipolar disorder.1

MECHANISM OF ACTION — Asenapine, like most second-generation antipsychotics, is an antagonist at dopamine D2 and serotonin 5-HT2A receptors. It also has high affinity for other dopamine and serotonin receptors, as well as alpha-adrenergic and histaminergic (H1) receptors.2 Asenapine has low affinity for muscarinic receptors.

PHARMACOKINETICS — When swallowed, the bioavailability of asenapine is poor (< 2%) because of extensive first-pass metabolism. Placed under the tongue, the drug ... more      

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