HALF-LIFE: 24 hours
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 SL BID and increase as needed up to 10mg SL BID
PREGNANCY: Minimal data on safety
BREASTFEEDING: Minimal data on safety
2) Bipolar Disorder (acute manic/mixed episodes), 10yo and older
- Asenapine is structurally very similar to Mirtazapine
- Binding profile similar to Clozapine (5HT2A, 5HT2C, H1, α2, D2) and mirtazapine but with little anticholinergic effects
- Sublingual (low bioavailability due to 1st pass metabolism)
- Oral Cavity surface area limits size of dose and extent of absorption (dosed BID)
- 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 antagonism of H1 receptors
- Akathisia may be dose related
- Low-moderate risk for
- Weight gain/dyslipidemia
- Prolactin elevation
- Possible antidepressant actions via antagonism of 5HT2C receptors
- Possible alleviating of negative symptoms via antagonism of α2, 5HT1D, and 5HT7 receptors
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