Cyproheptadine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Periactin; Bulgaria: Cyprotol; Czech Republic: Peritol; France: Periactine; Germany: Peritol; Hungary: Peritol; Italy: Periactin; Luxembourg: Periactin; Netherlands: Periactin; Poland: Peritol, Protadina; Romania: Biohept, Ciproheptadina, Peritol; Slovakia: Peritol; Spain: Periactin, Viternum; UK: Periactin.

North America

Canada: Cyproheptadine; USA: Cyproheptadine.

Latin America

Brazil: Periatin.

Asia

Japan: Cyproheptadine, Cypromin, Ifrasal, Periactin.

Drugs Combinations

Cyproheptadine: Ascorbic Acid (Vitamin C); Calcium Lactate; Calcium Phosphate; Clonixin; Cobamamide; Cyanocobalamin (Vitamin B~12~); Dexamethasone; Ergocalciferol (Vitamin D~2~); Ergotamine; Gentamicin; Ginkgo biloba; Hydrocortisone; Ketoconazole; Levoglutamina; Niacinamide; Pantothenic Acid (Vitamin B~5~); Pyridoxine (Vitamin B~6~); Retinol (Vitamin A); Riboflavin (Vitamin B~2~); Thiamine (Vitamin B~1~)

Drug combinations

Chemistry

Cyproheptadine Hydrochloride: C~21~H~21~N HCl 1½H~2~O. Mw: 350.88. (1) Piperidine, 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-methyl-, hydrochloride, sesquihydrate; (2) 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride sesquihydrate. CAS-41354-29-4; CAS-969-33-5 (anhydrous); CAS-129-03-3 (cyproheptadine).

Pharmacologic Category

First Generation Antihistamines; Histamine H~1~ Antagonist. (ATC-Code: R06AX02).

Mechanism of action

Potent histamine and serotonin antagonist properties. Competes with histamine for H~1~-receptor sites on effector cells in the GI tract, blood vessels, and respiratory tract. Has anticholinergic and sedative effects, and calcium-channel blocking activity.

Therapeutic use

Perennial and seasonal allergic rhinitis. Other allergic symptoms including urticaria.

Pregnancy and lactiation implications

Reproduction studies in animals have not revealed evidence of harm to the fetus. No adequate studies developed in humans. Use during pregnancy only when clearly needed. It is not known whether cyproheptadine hydrochloride is distributed into milk.

Unlabeled use

Appetite stimulation, blepharospasm, cluster headaches, migraine headaches, Nelson’s syndrome, pruritus, schizophrenia, spinal cord damage-associated spasticity, and tardive dyskinesia.

Contraindications

Hypersensitivity to cyproheptadine or any component of the formulation. Narrow-angle glaucoma. Bladder neck obstruction. Symptomatic prostatic hyperplasia. Acute asthmatic attack. Stenosing peptic ulcer. GI tract obstruction. Concurrent use of MAO inhibitors. Avoid use in premature and term newborns (potential association with sudden infant death syndrome). Women who are breast-feeding. Debilitated geriatric patients.

Warnings and precautions

May cause CNS depression. Use with caution in the following cases: cardiovascular disease, increased intraocular pressure, asthma or other chronic breathing disorders, thyroid dysfunction, and the elderly. Effects may be potentiated when used with other sedative drugs or ethanol. Some case reports have described a weight gain in anorexic adults with cyproheptadine. Antihistamines may cause excitation in young children.

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