Cyproheptadine hydrochloride 4 MG Oral Tablet
WARNINGS
Pediatric Patients Overdosage of antihistamines, particularly in infants and young children, may produce hallucinations, central nervous system depression, convulsions, respiratory and cardiac arrest, 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 (see PRECAUTIONS, Geriatric Use).
DRUG INTERACTIONS
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.
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 ½ 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
Cyproheptadine HCl USP, is an antihistaminic and antiserotonergic agent.
Cyproheptadine hydrochloride USP is a white to slightly yellowish crystalline solid, with a molecular weight of 350.89, which is 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 C21H21N•HCl and the structural formula of the anhydrous salt is: C21H21N• HCl M.W.
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.
chemical structure
HOW SUPPLIED
Cyproheptadine Hydrochloride Tablets USP, 4 mg are available as white, round, flat-faced, beveled-edged tablets, bisected on one side with debossed “93” above the bisect and debossed “2929” below the bisect, plain on the other side, containing 4 mg of cyproheptadine HCl packaged in bottles of 100 and 1000 tablets and unit-dose boxes of 100 tablets.
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 In India By: EMCURE PHARMACEUTICALS LTD.
Hinjwadi, Pune, India Manufactured For: TEVA PHARMACEUTICALS USA Sellersville, PA 18960 Iss.
7/2009
GERIATRIC USE
Geriatric Use Clinical studies of cyproheptadine HCl tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.
Other reported clinical experience has not identified differences in responses between the elderly and younger patients.
In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy (see WARNINGS, Activities Requiring Mental Alertness).
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.
PEDIATRIC USE
Pediatric Use Safety and effectiveness in pediatric patients below the age of two have not been established (see CONTRAINDICATIONS, Newborn or Premature Infants, and WARNINGS, Pediatric Patients).
PREGNANCY
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.
NUSRING MOTHERS
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).
INFORMATION FOR PATIENTS
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.
DOSAGE AND ADMINISTRATION
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 (½ 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.