FDA Label for Cyproheptadine Hydrochloride

Clinical Pharmacology:

Cyproheptadine HCI is a serotonin and histamine antagonist with anticholinergic and sedative effects. Antiserotonin and antihistamine drugs appears to compete with serotonin and histamine, respectively, for receptor sites.

Pharmacokinetics and Metabolism: After a single 4 mg oral dose of 14C-labeled cyproheptadine HCl normal subjects given as tablets or syrup, 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 significant difference in the mean urinary excretion exists between the tablet and syrup formulations. No detectable amounts of unchanged drug were present in the urine of patients of chronic 12-20 mg daily doses of cyproheptadine syrup. The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.

Contraindications

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.

Warnings

Children - Overdosage of antihistamines, particularly in infants and children, may produce hallucinations, central nervous system depression, convulsions, and death.

Antihistamines may diminish mental alertness conversely particularly in the young child they may occasionally produce excitation.

CNS Depressants - Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents.

Activities Requiring Mental Alertness - Patients should be warned about engaging in activities requiring mental alertness and motor coordination, such as driving a car or operating machinery. Antihistamines are more likely to cause dizziness, sedation and hypotension in elderly patients.

Precautions

General: Cyproheptadine has an atropine-like action and, therefore, should be used with caution in patients with History of bronchial asthma.  Increased intraocular pressure, Hyperthyroidism, Cardiovascular disease, Hypertension.

Information for Patients: Antihistamines may diminish mental alertness; conversely, particularly in the young child, they may occasionally produce excitation.

Patients should be warned about engaging in activities requiring mental alertness and motor coordination, such as driving a car or operating machinery.

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.

Carcinogenesis, Mutagenesis, Impairment of Fertility: Long-term carcinogenic studies have not been done with cyproheptadine.

Cyproheptadine had no effect on fertility in a two-litter study in rats or a two generation study in mice at about 10 times the human dose. Cyproheptadine did not produce chromosome damage in human lymphocytes or fibroblasts in vitro; high doses (10- ⁴M) were cytotoxic. Cyproheptadine did not have any mutagenic effect in the Ames microbial mutagen test; concentrations of above 500 mcg/plate inhibited bacterial growth.

Pregnancy

Pregnancy Category B: Reproduction studies have been performed in rabbits, mice, and rats at oral or subcutaneous doses up to 32 times the maximum recommended human oral dose and have revealed no evidence of impaired fertility or harm to the fetus due to cyproheptadine. Cyproheptadine has been shown to be fetotoxic in rats when given by intraperitoneal injection in doses four times the maximum recommended human oral dose. Two studies in pregnant women, however, have not shown that cyproheptadine increases the risk of abnormalities when administered during the first, second and third trimesters of pregnancy. No teratogenic effects were observed in any of the newborns. Nevertheless, because the studies in humans cannot rule out the possibility of harm, cyproheptadine should be used during pregnancy only if clearly needed.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from cyproheptadine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother (see CONTRAINDICATIONS).

Pediatric Use: Safety and effectiveness in children below the age of two years have not been established. (See CONTRAINDICATIONS, Newborn or Premature infants, and WARNINGS, Children.)

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: 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.

How Supplied

HOW SUPPLIED: Each tablet contains 4 mg of cyproheptadine hydrochloride, are white, round tablets debossed with “CE 73” on one side and a score on other side. They are supplied as follows: bottles of 90 count, NDC 62135-236-90.

Dispensing Information: Dispense in tight containers as defined by the USP/NF.

Caution: Federal law prohibits dispensing without prescription. KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

Manufactured for:

Chartwell RX, LLC

Congers, NY 10920

Telephone Number-1-845-232-1683

L70791

Rev. 01/2023

Package Label-Principal Display Panel

Cyproheptadine Hydrochloride Tablets, USP 4 mg NDC 62135-236-90 - 90s Bottle Label

image description - cyproheptadine hcl tab usp 4mg bottle label