Asenapine (Saphris)

 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
FDA INDICATIONS:
1) Schizophrenia
2) Bipolar Disorder (acute manic/mixed episodes), 10yo and older

ADDITIONAL INFORMATION

  • 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
    • EPS
    • 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

References:

  1. Cooper, J. R., Bloom, F. E., & Roth, R. H. (2003). The biochemical basis of neuropharmacology (8th ed.). New York, NY, US: Oxford University Press.
  2. Iversen, L. L., Iversen, S. D., Bloom, F. E., & Roth, R. H. (2009). Introduction to neuropsychopharmacology. Oxford: Oxford University Press.
  3. Puzantian, T., & Carlat, D. J. (2016). Medication fact book: for psychiatric practice. Newburyport, MA: Carlat Publishing, LLC.
  4. J. Ferrando, J. L. Levenson, & J. A. Owen (Eds.), Clinical manual of psychopharmacology in the medically ill(pp. 3-38). Arlington, VA, US: American Psychiatric Publishing, Inc.
  5. Schatzberg, A. F., & DeBattista, C. (2015). Manual of clinical psychopharmacology. Washington, DC: American Psychiatric Publishing.
  6. Schatzberg, A. F., & Nemeroff, C. B. (2017). The American Psychiatric Association Publishing textbook of psychopharmacology. Arlington, VA: American Psychiatric Association Publishing.
  7. Stahl, S. M. (2014). Stahl’s essential psychopharmacology: Prescriber’s guide (5th ed.). New York, NY, US: Cambridge University Press.
  8. Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY, US: Cambridge University Press.
  9. Whalen, K., Finkel, R., & Panavelil, T. A. (2015). Lippincotts illustrated reviews: pharmacology. Philadelphia, PA: Wolters Kluwer.

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