Cyproheptadine Hydrochloride

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.

DOSAGE AND ADMINISTRATION: DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT. Children: The total daily dosage for children may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day (0.11 mg/lb/day) or 8 mg per square meter of body surface (8 mg/m 2 ). In small children for whom the calculation of the dosage based upon body size is important, it may be necessary to use cyproheptadine syrup to permit accurate dosage. Age 2 to 6 years: The usual dose is 2 mg (1/2 tablet) two or three times a day, adjusted as necessary to the size and response of the patient. The dose is not to exceed 12 mg a day. Age 7 to 14 years: The usual dose is 4 mg (1 tablet) two or three times a day, adjusted as necessary to the size and response of the patient. The dose is not to exceed 16 mg a day. Adults: The total daily dose for adults should not exceed 0.5 mg/kg/day (0.23 mg/lb/day). The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 to 16 mg, a day. An occasional patient may require as much as 32 mg a day for adequate relief. It is suggested that dosage be initiated with 4 mg (1 tablet) three times a day and adjusted according to the size and response of the patient.

CONTRAINDICATIONS Newborn or Premature Infants This drug should not be used in newborn or premature infants. Lactation Because of the higher risk of antihistamines for infants generally and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers. Other Conditions Hypersensitivity to cyproheptadine and other drugs of similar chemical structure. Monoamine oxidase inhibitor therapy (See DRUG INTERACTIONS ). Angle-closure glaucoma Stenosing peptic ulcer Symptomatic prostatic hypertrophy Bladder neck obstruction Pyloroduodenal obstruction Elderly, debilitated patients

Newborn or Premature Infants This drug should not be used in newborn or premature infants.

Lactation Because of the higher risk of antihistamines for infants generally and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.

ADVERSE REACTIONS Adverse reactions which have been reported with the use of antihistamines are as follows: Central Nervous System Sedation and sleepiness (often transient), dizziness, disturbed coordination, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, paresthesias, neuritis, convulsions, euphoria, hallucinations, hysteria, faintness. Integumentary Allergic manifestation of rash and edema, excessive perspiration, urticaria, photosensitivity. Special Senses Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus. Cardiovascular Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock. Hematologic Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia. Digestive System Cholestasis, hepatic failure, hepatitis, hepatic function abnormality, dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice. Genitourinary Urinary frequency, difficult urination, urinary retention, early menses. Respiratory Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness. Miscellaneous Fatigue, chills, headache, increased appetite/weight gain.

Central Nervous System Sedation and sleepiness (often transient), dizziness, disturbed coordination, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, paresthesias, neuritis, convulsions, euphoria, hallucinations, hysteria, faintness.

Integumentary Allergic manifestation of rash and edema, excessive perspiration, urticaria, photosensitivity.

Special Senses Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus.

Cardiovascular Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock.

Hematologic Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia.

Digestive System Cholestasis, hepatic failure, hepatitis, hepatic function abnormality, dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice.

Genitourinary Urinary frequency, difficult urination, urinary retention, early menses.

Respiratory Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness.

Miscellaneous Fatigue, chills, headache, increased appetite/weight gain.

Drug Interactions MAO inhibitors prolong and intensify the anticholinergic effects of antihistamines. Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents.

DESCRIPTION Cyproheptadine hydrochloride, USP is an antihistaminic and antiserotonergic agent. Cyproheptadine hydrochloride, USP is a white to slightly yellow, odorless or practically odorless, crystalline powder, with a molecular weight of 350.89, which is slightly soluble in water, freely soluble in methanol, soluble in chloroform, sparingly soluble in alcohol, 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 C 21 H 21 N•HCl and the structural formula of the anhydrous salt is: Molecular Formula: C 21 H 21 N• HCl Molecular Weight: 350.89 Cyproheptadine hydrochloride, USP is available for oral administration in 4 mg tablets. Inactive ingredients include: lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate (botanical source: potato). Cyproheptadine HCl tablet

OVERDOSAGE Antihistamine overdosage reactions may vary from central nervous system depression to stimulation especially in pediatric patients. Also, atropine-like signs and symptoms (dry mouth; fixed, dilated pupils; flushing, etc.) as well as gastrointestinal symptoms may occur. If vomiting has not occurred spontaneously , the patient should be induced to vomit with syrup of ipecac. If patient is unable to vomit , perform gastric lavage followed by activated charcoal. Isotonic or 1⁄2 isotonic saline is the lavage of choice. Precautions against aspiration must be taken especially in infants and children. When life threatening CNS signs and symptoms are present, intravenous physostigmine salicylate may be considered. Dosage and frequency of administration are dependent on age, clinical response, and recurrence after response. (See package circulars for physostigmine products.) Saline cathartics , as milk of magnesia, by osmosis draw water into the bowel and, therefore, are valuable for their action in rapid dilution of bowel content. Stimulants should not be used. Vasopressors may be used to treat hypotension. The oral LD 50 of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

HOW SUPPLIED Cyproheptadine hydrochloride tablets USP, 4 mg are available as white to off-white color, round flat face tablet with debossed “B137” on one side and scored on the other, containing 4 mg of cyproheptadine HCl packaged in HDPE bottles of 100 and 1000 tablets. PHARMACIST: Dispense in a well-closed container as defined in the USP, with a child-resistant closure (as required). Bottles of 100 tablets: NDC 76385- 130 -01 Bottles of 1000 tablets: NDC 76385- 130 -10

STORAGE Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature.] To report SUSPECTED ADVERSE REACTIONS, contact Beximco Pharmaceuticals USA Inc. at 877-372-6093 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . Manufactured by: BEXIMCO PHARMACEUTICALS PLC. 126, Kathaldia, Tongi, Gazipur, 1711, Bangladesh Made in Bangladesh Distributed by: UNICHEM PHARMACEUTICALS (USA), INC. East Brunswick, NJ 08816 USA. 3020013025 Rev. 11/2025