Indications and Usage
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 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.
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
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.
Overdosage
OVERDOSAGE: Antihistamine overdosage reactions may vary from central nervous system depression to stimulation, especially in children. 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.
Description
DESCRIPTION: Cyproheptadine HCl, is an antihistaminic and antiserotonergic agent.
Cyproheptadine hydrochloride is a while to slightly yellowish, crystalline, solid. with a molecular weight of 350.89, 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 C 21H 21NHC1. and the structural formula of the anhydrous salt is:
Cyproheptadine hydrochloride is available in 4 mg tablets.
Each tablet contains:
Active Ingredient:
Cyproheptad1ne Hydrochloride ...................... 4 mg
Each tablet contains:
Inactive Ingredients:
Colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), stearic acid.
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.
How Supplied / Storage and Handling
HOW SUPPLIED: Each tablet contains 4 mg of cyproheptadine hydrochloride, are white to off-white, round, flat faced, beveled edge 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