Synonyms:
Cyproheptadine Hydrochloride; Periactin
Generic Available:
Yes
Canadian Brand Names:
Periactin®
Use:
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria
Use - Unlabeled/Investigational:
Appetite stimulation, blepharospasm, cluster headaches, migraine headaches, Nelson's syndrome, pruritus, schizophrenia, spinal cord damage associated spasticity, and tardive dyskinesia
Pregnancy Risk Factor:
B
Lactation:
Excretion in breast milk unknown/contraindicated
Contraindications:
Hypersensitivity to cyproheptadine or any component of the formulation; narrow-angle glaucoma; bladder neck obstruction; acute asthmatic attack; stenosing peptic ulcer; GI tract obstruction; concurrent use of MAO inhibitors; avoid use in premature and term newborns due to potential association with SIDS
Warnings/Precautions:
Do not use in neonates, safety and efficacy have not been established in children <2 years of age; symptomatic prostate hypertrophy; antihistamines are more likely to cause dizziness, excessive sedation, syncope, toxic confusion states, and hypotension in the elderly. In case reports, cyproheptadine has promoted weight gain in anorexic adults, though it has not been specifically studied in the elderly. All cases of weight loss or decreased appetite should be adequately assessed.
Adverse Reactions:
>10%:
Central nervous system: Slight to moderate drowsiness
Respiratory: Thickening of bronchial secretions
1% to 10%:
Central nervous system: Headache, fatigue, nervousness, dizziness
Gastrointestinal: Appetite stimulation, nausea, diarrhea, abdominal pain, xerostomia
Neuromuscular & skeletal: Arthralgia
Respiratory: Pharyngitis
<1%: Tachycardia, palpitation, edema, sedation, CNS stimulation, seizure, depression, photosensitivity, rash, angioedema, hemolytic anemia, leukopenia, thrombocytopenia, hepatitis, myalgia, paresthesia, bronchospasm, epistaxis, allergic reactions
Overdosage/Toxicology:
Symptoms of overdose include CNS depression or stimulation, dry mouth, flushed skin, fixed and dilated pupils, and apnea. There is no specific treatment for antihistamine overdose. Clinical toxicity is due to blockade of cholinergic receptors. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg I.V. slowly, may be given to reverse these effects.
Drug Interactions:
Cyproheptadine may potentiate the effect of CNS depressants.
MAO inhibitors may cause hallucinations when taken with cyproheptadine.
Ethanol/Nutrition/Herb Interactions:
Ethanol: Avoid ethanol (may increase CNS sedation).
Mechanism of Action:
A potent antihistamine and serotonin antagonist, competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract
Pharmacodynamics/Kinetics:
Absorption: Completely
Metabolism: Almost completely hepatic
Excretion: Urine (>50% primarily as metabolites); feces (~25%)
Dosage:
Oral:
Children:
Allergic conditions: 0.25 mg/kg/day or 8 mg/m2/day in 2-3 divided doses or
2-6 years: 2 mg every 8-12 hours (not to exceed 12 mg/day)
7-14 years: 4 mg every 8-12 hours (not to exceed 16 mg/day)
Migraine headaches: 4 mg 2-3 times/day
Children 12 years and Adults: Spasticity associated with spinal cord damage: 4 mg at bedtime; increase by a 4 mg dose every 3-4 days; average daily dose: 16 mg in divided doses; not to exceed 36 mg/day
Children >13 years and Adults: Appetite stimulation (anorexia nervosa): 2 mg 4 times/day; may be increased gradually over a 3-week period to 8 mg 4 times/day
Adults:
Allergic conditions: 4-20 mg/day divided every 8 hours (not to exceed 0.5 mg/kg/day)
Cluster headaches: 4 mg 4 times/day
Migraine headaches: 4-8 mg 3 times/day
Dosage adjustment in hepatic impairment: Reduce dosage in patients with significant hepatic dysfunction
Test Interactions:
Diagnostic antigen skin test results may be suppressed; false positive serum TCA screen
Patient Education:
Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience drowsiness or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth, nausea, or abdominal pain (small, frequent meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report persistent sedation, confusion, or agitation; changes in urinary pattern; blurred vision; chest pain or palpitations; sore throat respiratory difficulty or expectorating (thick secretions); or lack of improvement or worsening or condition. Breast-feeding precaution: Do not breast-feed.
Nursing Implications:
Raise bed rails, institute safety measures, assist with ambulation
Additional Information:
May stimulate appetite; in case reports, cyproheptadine has promoted weight gain in anorexic adults.
Anesthesia and Critical Care Concerns/Other Considerations:
May stimulate appetite; in case reports, cyproheptadine has promoted weight gain in anorexic adults.
Dental Health: Effects on Dental Treatment:
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions:
No information available to require special precautions
Mental Health: Effects on Mental Status:
Drowsiness is common; may cause nervousness or depression
Mental Health: Effects on Psychiatric Treatment:
Contraindicated with MAO inhibitors; concurrent use with psychotropic may produce additive sedation
Oncology: Emetic Potential:
Very low (<10%)
Dosage Forms:
Syrup, as hydrochloride: 2 mg/5 mL (473 mL) [contains alcohol 5%; mint flavor]
Tablet, as hydrochloride: 4 mg
International Brand Names:
Alphahist® (ID); Apeton® (ID); Arsigran® (ID); Cipla-Actin® (ZA); Ciplactin® (IN); Ciproactin® (CL); Cipro-Gal® (RO); Ciproheptadina® (RO); Cyheptine® (TH); Cylat® (ID); Cyprogin® (HK, TH); Cyproheptadine® (CY); Cypromin® (JP); Cyprono® (TH); Cyprosian® (TH); Ennamax® (ID); Esprocy® (ID); Glocyp® (ID); Grisetin con Carnitina® (CL); Heptasan® (ID); Ifrasarl® (JP); Klarivitina® (ES); Nebor® (ID); Operma® (ID); Oractine® (IL); Periactin® (AT, AU, BE, CA, CY, DK, EG, ES, GB, HK, IE, IT, JO, KW, LB, LU, NL, NZ, SE, SY, TH, ZA); Periactine® (FR); Periatin® (BR); Peritol® (CZ, DE, HU, IN, PL, RO, RU); Polytab® (TH); Poncohist® (ID); Practin® (IN); Prakten® (TR); Profut® (ID); Prohessen® (ID); Pronicy® (ID); Protadina® (PL); Sinapdin® (ID); Sipraktin® (TR); Viternum® (CL, CO, ES, MX, PT)
References
Carlton MC, Kunkel DB, and Curry SC, "Ergotism Treated With Cyproheptadine,"Clin Toxicol, 1995, 33(5):552.
Craven JL and Rodin GM, "Cyproheptadine Dependence Associated With an Atypical Somatoform Disorder,"Can J Psychiatry, 1987, 32(2):143-5.
Herzog DB and Copeland PM, "Eating Disorders,"N Engl J Med, 1985, 313(5):295-303.
Lappin RI and Auchincloss EL, "Treatment of the Serotonin Syndrome With Cyproheptadine,"N Engl J Med, 1994, 331(15):1021-2.
Wians FH, Norton JT, and Wirebaugh, "False-Positive Serum Tricyclic Antidepressant Screen With Cyproheptadine,"Clin Chem, 1993, 39(6):1355-6.