asenapine SAPHRIS

Class: Second Generation Antipsychotic/​Benzazepine Analog
FDA Indications: Schizophrenia, Bipolar I Disorder
Off-Label Use:
Prescribing
Forms: 2.5, 5, 10mg SL tablets
Dose Range: 10-20 mg/day
Starting: 5 mg SL bid, titrate to 10 mg SL bid
Stopping: Taper 6-8 weeks, rapid d/c can lead to rebound psychosis
Monitoring:

NAMI drug fact sheet

Precautions
Contraindications: Hepatic impairment (Child-PughC)
Serious Side Effects: , , ,
Possible Risk of TdP, Drugs to Avoid in Congenital Long QT
Side Effects: sedation/somnolence, dizziness, increased appetite, weight gain, nausea, akathisia, dysgeusia, EPS, oral hypoesthesia
Pharmacodynamics
1° MOA: 5HT2A–D2 antagonist
Target: Antagonism at: Partial agonist at Postsynaptic 5HT1A
Pharmacokinetics
t½: 24° TMAX:
Substrate of: UGT1A4 (major), 1A2 (minor)
Inhibits: 2D6; Induces:
Active Metabolites:
DDIs
  • - metabolized primarily through glucuronidation, making it less likely to cause drug interactions
  • - strong 1A2 inhibitors can ↑ levels, likewise 1A2 inducers can ↓ levels
Misc
  • - must be given sublingually to achieve ~30% bioavailability; oral administration is associated with <2% systemic availability due to extensive first-pass metabolism
  • - the surface area of the oral cavity may limit size of the dose and extent of drug absorption at high doses, so it is generally taken bid despite its long t½
  • - d/t its rapid sublingual absorption, theoretically may be used as a rapid-acting oral PRN
  • - patients may not eat or drink for 10 minutes following sublingual administration to avoid the drug being washed out of oral absorption sites and into the stomach
  • - can be sedating, especially at initial dosing
Special Populations

Category C—May cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure

Lactation studies have not been conducted to assess the presence of asenapine in human milk

All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.

There are no dosage adjustments required


Contraindicated in patients with severe hepatic impairment; no dosage adjustment required in mild to moderate hepatic impairment

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Last updated April 20 2018 09:28:33. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.