CYPROHEPTADINE- cyproheptadine syrup
Pharmaceutical Associates, Inc.
Rx ONLY
DESCRIPTION
Each 5 mL (one teaspoonful) contains: Cyproheptadine hydrochloride 2 mg. Alcohol 5%.
Inactive ingredients: citric acid, D&C Yellow No.10, peppermint flavor, purified water, sodium benzoate, sodium citrate and sucrose.
Cyproheptadine hydrochloride is an antihistaminic and antiserotonergic agent. Cyproheptadine hydrochloride is a white to slightly yellowish, crystalline solid, with a molecular weight of 350.88, which is slightly soluble in water, freely soluble in methanol, sparingly soluble in ethanol, soluble in chloroform and practically insoluble in ether. It is the sesquihydrate of 4-(5H -Dibenzo [a,d ] cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride. The molecular formula of the anhydrous salt is C21 H21 N � HCl and the structural formula of the anhydrous salt is:
Chemical StructureChemical Structure
CLINICAL PHARMACOLOGY
Cyproheptadine is a serotonin and histamine antagonist with anticholinergic and sedative effects. Antiserotonin and antihistamine drugs appear to compete with serotonin and histamine, respectively, for receptor sites.
Pharmacokinetics and Metabolism
After a single 4 mg oral dose of 14 C-labeled cyproheptadine HCl in normal subjects, given as tablets or oral solution, 2-20% of the radioactivity was excreted in the stools. Only about 34% of the stool radioactivity was unchanged drug, corresponding to less than 5.7% of the dose. At least 40% of the administered radioactivity was excreted in the urine. No detectable amounts of unchanged drug were present in the urine of patients on chronic 12-20 mg daily doses of cyproheptadine oral solution. The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.
CYPROHEPTADINE Indications and Usage
Perennial and seasonal allergic rhinitis
Vasomotor rhinitis
Allergic conjunctivitis due to inhalant allergens and foods
Mild, uncomplicated allergic skin manifestations of urticaria and angioedema
Amelioration of allergic reactions to blood or plasma
Cold urticaria
Dermatographism
As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled.
