Cyproheptadine
From Pharmacopedia
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First-generation antihistamine, Serotonin 5-HT2 antagonist, Appetite-promoting medicine (orexigenic)
Cyproheptadine (hydrochloride)
Periactin (US brand discontinued; generic widely available)
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Summary
Classes
Common uses
Allergic conditions including urticaria and seasonal allergies (FDA)0, Serotonin syndrome (off-label; the standard pharmacological antidote alongside supportive care and benzodiazepines)0, Appetite stimulation in failure to thrive, cachexia, and anorexia (off-label, evidence-supported in pediatric and adult populations)0, Pediatric migraine prophylaxis (off-label)0, SSRI-induced sexual dysfunction (off-label adjunct, modest evidence)0
Pharmacy
Starting dose
Allergy: 4 mg PO TID. Serotonin syndrome: 12 mg loading dose PO or by nasogastric tube, then 2 mg every 2 hours until clinical improvement. Appetite stimulation: 2-4 mg PO TID-QID
Preparations
Tablets 4 mg; oral syrup 2 mg/5 mL
US FDA Max
32 mg/day adult; weight-based pediatric ceiling
Pharmacology
Routes
Oral
Onset
30-60 minutes
Duration
6-8 hours
Half-life
8-16 hours[1]
Bioavailability
~95% (oral)[1]
Pregnancy
Limited human data; older agent with substantial use experience.[citation needed]
Legal status
Rx-only in US
Purported mechanism
First-generation H1 histamine receptor antagonist with substantial additional 5-HT2A and 5-HT2C serotonin receptor antagonism. The 5-HT2A antagonism is the basis of its role as the first-line pharmacological antidote for serotonin syndrome; the 5-HT2C antagonism underlies the appetite stimulation effect (the same receptor mechanism that drives weight gain with mirtazapine and olanzapine).0 Anticholinergic and sedating, with the standard first-generation antihistamine Beers-list concerns in elderly patients[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Periactin (cyproheptadine hydrochloride), Merck/various, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/010407s058lbl.pdf