Products
Asenapine is commercially available in the form of sublingual tablets (Sycrest). It was approved in many countries in 2012. In the United States, it has been registered since 2009.
Structure and properties
Asenapine (C17H16ClNO, Mr = 285.8 g/mol) is present in the drug as asenapine maleate. It belongs to the class of dibenzooxepin pyrroles.
Effects
Asenapine (ATC N05AH05) is antimanic, antidopaminergic at the D2 receptor, and antiserotonergic at the 5-HT2A receptor. Other receptor systems may be involved in the effects.
Indications
For the treatment of moderate to severe manic episodes in adult bipolar disorder. In the United States, asenapine is also approved for the treatment of schizophrenia.
Dosage
According to the SmPC. Sublingual tablets are administered in the morning and evening. The instructions in the leaflet should be followed carefully. The tablets should not be swallowed or chewed, but allowed to dissolve under the tongue. Do not eat or drink anything for 10 minutes after taking the tablets. This is because bioavailability is very low when swallowed. When administered sublingually, it is 35%.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Asenapine is metabolized by UGT1A4 and CYP1A2 and is a weak inhibitor of CYP2D6. Corresponding drug-drug interactions are possible. Other interactions may occur with antihypertensives, levodopa, and dopamine agonists.
Adverse effects
The most common potential adverse effects include anxiety, drowsiness, dullness, dizziness, taste disturbances, drug-induced Parkinson’s disease, movement disorders, increased appetite, weight gain, and anesthetized oral mucosa.
