Cyproheptadine Hydrochloride - Cyproheptadine Hydrochloride solution prescribing information
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.
Although intended primarily for administration to children, the syrup is also used for administration to adults who cannot swallow tablets.
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 ).
Age 2 to 6 years: The usual dose is 2 mg (one teaspoonful) 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 (two teaspoonsful) 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 (two teaspoonsful) 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.
To report SUSPECTED ADVERSE REACTIONS, contact Quagen Pharmaceuticals LLC at 1-888-344-9603 or FDA at 1-800-FDA-1088 or www.FDA.gov/medwatch.
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
Each 5 mL (one teaspoonful) contains: Cyproheptadine Hydrochloride 2 mg Inactive Ingredients: Citric acid, D&C Yellow #10, peppermint flavor, purified water, propylene glycol, sodium citrate, sorbic acid (0.1% as preservative) and sucrose syrup.
Inactive ingredients for Cyproheptadine Oral Solution (Sugar Free): alcohol 5% (v/v), butylated hydroxyanisole, citric acid, D&C Yellow #10, peppermint flavor, propylene glycol, purified water, sodium citrate, sorbic acid (0 . 1%, as preservative), sucralose.
Cyproheptadine HCl is an antihistaminic and antiserotonergic agent. Cyproheptadine hydrochloride is a white 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 21 H 21 N•HCl and the structural formula of the anhydrous salt is:
CLINICAL PHARMACOLOGY
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.
Pharmacokinetics and Metabolism: After a single 4 mg oral dose of 14 C-labeled cyproheptadine HCI in 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 detectable amounts of unchanged drug were present in the urine of patients on 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
Cyproheptadine Hydrochloride Oral Solution, USP, 2 mg/5 mL in a yellow, peppermint flavor vehicle, is supplied in a pint (473 mL) container (NDC 70752-101-12) & (NDC 70752-185-12)-Sugar Free
Store at 20°-25°C (68°-77°F) excursion permitted to 15°-30°C (59°-86°F) [See USP Controlled Room Temperature].
Dispense in a tight, light-resistant container as defined in the USP.
