Cyproheptadine HCl USP, is an antihistaminic and antiserotonergic agent. Cyproheptadine hydrochloride USP is a white to slightly yellowish crystalline powder, with a molecular weight of 350.89, which is slightly soluble in water, freely soluble in methanol, sparingly soluble in alcohol, 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 C21H21N•HCl and the structural formula of the anhydrous salt is:

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.

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.

After a single 4 mg oral dose of 14C-labelled cyproheptadine HCI in normal subjects, given as tablets, 2 to 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 to 20 mg daily doses. The principle metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.

Perennial and seasonal allergic rhinitis

Vasomotor rhinitis

Allergic conjunctivitis due to inhalant allergens and foods

Mild, uncomplicated allergic skin manifestations of urticarial 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.

Newborn or Premature Infants

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

Nursing Mothers

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

Adverse reactions which have been reported with the use of antihistamines are as follows:

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 LD50 of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT.

Each tablet contains 4 mg of cyproheptadine hydrochloride.

Pediatric Patients

Age 2 to 6 years

The total daily dosage for pediatric patients may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day or 8 mg per square meter of body surface (8 mg/m2).

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. 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.

Cyproheptadine Hydrochloride Tablets USP are available as white to off white, round, flat-faced, beveled edged tablets, debossed with “MCR and 109” separated by functional score on one side and plain on the other side, containing 4 mg of cyproheptadine HCI packaged in bottles of 100 (NDC 52817-210-10) and 500 tablets (NDC 52817-210-50).

PHARMACIST: Dispense in a well-closed container as defined in the USP, with a child-resistant closure (as required).

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].

Manufactured by:

Appco Pharma LLC

Piscataway, NJ 08854

Distributed by:

TruPharma, LLC

Tampa, FL 33609

Revised: 06/2019

200223

Ver-03