HALF-LIFE: 13-39 hours
METABOLISM: Liver (primarily CYP1A2)
STARTING DOSE: 2.5mg-5mg sublingual (SL) BID
TARGET DOSING RANGE: 2.5mg-10mg SL BID
BEST TIME TO DOSE: Any
HOW TO DOSE: Initial 2.5mg-5mg sublingual (SL) twice daily and increase as needed up to 10mg SL twice daily
PREGNANCY: Minimal data on safety
BREASTFEEDING: Minimal data on safety
- Inhibitor of CYP2D6
- Constipation, dry mouth, blurry vision, tachycardia, orthostatic hypotension, seizures (rare but may occur at high doses), sedation, weight gain, increased cardio-metabolic risk (↑triglycerides, insulin resistance), oral numbness (transient), Akathisia, Arrhythmias, Extrapyramidal Symptoms (EPS), Neuroleptic Malignant Syndrome (Rare)
- Bipolar Disorder (acute manic/mixed episodes), 10yo and older
Off Label Uses: Agitation, Insomnia, Irritability
Mechanism(s) of Action
- Dopamine 2 receptor antagonist, 5HT2A Receptor Antagonist, 5HT2C Receptor Antagonist, 5HT7 Receptor Antagonist, Alpha-2 Receptor Antagonist
- Asenapine is structurally very similar to Mirtazapine
- Sublingual absorption (Asenapine has very low bioavailability if swallowed due to first pass metabolism in the liver)
- Oral Cavity surface area limits size of dose and extent of absorption
- Rapidly absorbed and has rapid peak drug levels
- Completely dissolves within 5-10 seconds after contact with sublingual mucosa
- Oral hypoesthesia (numbness/tingling) is common
- No eating or drinking for 10 minutes following administration
- Sedation is common due to antihistamine effects
- Akathisia may be dose related
- Low-moderate risk for extrapyramidal symptoms (movement disorders), Weight gain, and Prolactin elevation
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