Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. It has much lower affinity (pKi < 5) for the muscarinic acetylcholine receptors. Asenapine behaves as an antagonist at all receptors.
Indications and usage
Asenapine has been approved by the FDA for the acute treatment of adults with schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features in adults.
Common side effects: (incidence at least 5% or greater and at least twice that for placebo or greater than 10% regardless of placebo rate) Akathisia, oral hypothesia, somnolence, dizziness, extrapyramidal symptoms other than akathisia, weight gain, insomnia, headache.
Rare side effects: Neuroleptic malignant syndrome (Combination of fever, muscle stiffness, faster breathing, sweating, reduced consciousness, and sudden change in blood pressure and heart rate.), tardive dyskinesia.
- "Bipolar Disorder". Clinical Trials Update (Genetic Engineering & Biotechnology News): pp. 52,55. 2007-06-15.
- ^ Schering-Plough "Schering-Plough Announces Asenapine NDA Accepted for Filing by the U.S. FDA". Press release. http://www.schering-plough.com/news/news_article.aspx?reqid=1080771. Retrieved 2008-12-29.
- ^ a b c Shahid M, Walker GB, Zorn SH, Wong EH. (2009). "Asenapine: a novel psychopharmacologic agent with a unique human receptor signature.". J Psychopharmacol. 23 (1): 65-73.
- ^ a b "Saphris (asenapine) prescribing information" (PDF). Schering Corporation. 2009-08-01. http://www.spfiles.com/pisaphrisv1.pdf. Retrieved 2009-09-05.