cyproheptadine PERIACTIN
Class: Antihistamine/AntiserotoninFDA Indications: Allergic Reaction
Off-Label Use: Decreased Appetite Secondary To Chronic Disease, Serotonin Syndrome, Spasticity Associated With Spinal Cord Damage, SSRI-induced Sexual Dysfunction, Anorexia Nervosa
Prescribing
Forms: 4mg tablet; 2 mg/5 mL po solnDose Range: 4-20 mg/day
Starting: Serotonin syndrome (off-label use): Oral: Initial: 12 mg followed 4-8 mg PO every 1-4 hours (max 32mg/day)
Precautions
Contraindications: Caution if high environmental temperature; glaucoma, angle-closure; bladder neck obstructionSerious Side Effects: Agranulocytosis,thrombocytopenia, heat stroke, can cause short-lived generalized chorea in overdose
Side Effects: xerostomia, nausea, drowsiness, vomiting, abdominal pain, dizziness, headache, fatigue, urinary retention, rash, diarrhea, photosensitivity
Pharmacokinetics
t½: 2.5 (1-4)° TMAX: 6-9°Substrate of: Glucuronidation
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - watch for anticholinergic effects and CNS depression when coprescribed with other anticholinergics and CNS depressants, respectively.
Misc
- - lack of antidepressant efficacy has been reported when given concurrently with fluoxetine and paroxetine
- - may reverse anorgasmia caused by SSRIs/TCAs
- - has appetite stimulating effects; was found to improve weight gain in patients with restricting-type AN but not those with binging/purging type AN
- - may actually exacerbate sleep problems in patients with PTSD
Special Populations
Category B—The animal reproduction data and limited human pregnancy experience suggests that cyproheptadine is low risk for structural anomalies. Although reporting bias is evident, preterm birth occurred in three women exposed to the drug during pregnancy. Because preterm birth has been associated with other serotonin antagonists (e.g., selective serotonin reuptake inhibitors), there might be a causal association with cyproheptadine.
No reports describing the use of cyproheptadine during lactation have been located. Chronic use of cyproheptadine will lower serum prolactin levels, and it has been used in the management of galactorrhea. No studies have been found, however, that evaluated its potential to interfere with the normal lactation process. Because of the increased sensitivity of newborns to antihistamines and the potential for adverse reactions, the manufacturer considers cyproheptadine to be contraindicated in nursing mothers.
In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy
CrCl <10: ↓ dose 0-50%
HD/PD: no supplement
There are no dosage adjustments provided in the manufacturer's labeling.