Cyproheptadine

Pronunciation

(si proe HEP ta deen)

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

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

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.

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)

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