Label: CYPROHEPTADINE HYDROCHLORIDE tablet
- NDC Code(s): 70710-1110-0, 70710-1110-1
- Packager: Zydus Pharmaceuticals USA Inc.
- Category: HUMAN PRESCRIPTION DRUG LABEL
- DEA Schedule: None
- Marketing Status: Abbreviated New Drug Application
Updated October 4, 2022
If you are a consumer or patient please visit this version.
Cyproheptadine hydrochloride, USP is a white to slightly yellow, odorless or practically odorless, crystalline powder, with a molecular weight of 350.89, which is slightly soluble in water, freely soluble in methanol, soluble in chloroform, sparingly soluble in alcohol, 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:
Molecular Weight: 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 (botanical source: potato).
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 14C-labelled cyproheptadine hydrochloride in normal subjects, given as tablets, 2 to 20 % of the radio activity was excreted in the stools. Only about 34 % of the stool radio activity was unchanged drug, corresponding to less than 5.7% of the dose. At least 40% of the administered radio activity 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.
INDICATIONS AND USAGE
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
As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the cute manifestations have been controlled.
Monoamine oxidase inhibitor therapy (See DRUG INT ERACT IONS.)
Stenosing peptic ulcer
Symptomatic prostatic hypertrophy
Bladder neck obstruction
Elderly, debilitated patients
Antihistamines may diminish mental alertness; conversely, particularly, in the young child, they may occasionally produce excitation.
Activities Requiring Mental Alertness
Antihistamines are more likely to cause dizziness, sedation, and hypotension in elderly patients (see PRECAUTIONS, Geriatric Use).
History of bronchial asthma Increased intraocular pressure Hyperthyroidism
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.
Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents.
Carcinogenesis, Mutagenesis, Impairment of Fertility
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 fibro blasts invitro; 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.
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.
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).
Clinical studies of cyproheptadine hydrochloride 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).
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.
Allergic manifestation of rash and edema, excessive perspiration, urticaria, photo sensitivity.
Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus.
Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock.
Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia.
Cholestasis, hepatic failure, hepatitis, hepatic function abnormality, dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice.
Urinary frequency, difficult urination, urinary retention, early menses.
Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness.
Fatigue, chills, headache, increased appetite/weight gain.
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 LD50 of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.
DOSAGE AND ADMINISTRATION
Each tablet contains 4 mg of cyproheptadine hydrochloride.
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.
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, 4 mg are available as white, round, flat-faced, beveled- edged tablets, bisected on one side and debossed with "11 10" on the other side, and are supplied as:
NDC 70710-1110-1 in bottle of 100 tablets with child-resistant closure
NDC 70710-1110-0 in bottle of 1,000 tablets
PHARMACIST: Dispense in a well-closed container as defined in the USP, with a child-resistant closure (as required).
Store at 20°C to 25°C (68°F to 77°F) [See USP Controlled Room Temperature].
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Please address medical inquiries to, (MedicalAffairs@zydususa.com) Tel.: 1-877-993-8779.
Package insert available at www.zydususa.com/products or call 1-877-993-8779.
- SPL UNCLASSIFIED SECTION
- PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
INGREDIENTS AND APPEARANCE
cyproheptadine hydrochloride tablet
Product Information Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:70710-1110 Route of Administration ORAL Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength CYPROHEPTADINE HYDROCHLORIDE (UNII: NJ82J0F8QC) (CYPROHEPTADINE - UNII:2YHB6175DO) CYPROHEPTADINE HYDROCHLORIDE 4 mg Inactive Ingredients Ingredient Name Strength CELLULOSE, MICROCRYSTALLINE (UNII: OP1R32D61U) LACTOSE MONOHYDRATE (UNII: EWQ57Q8I5X) MAGNESIUM STEARATE (UNII: 70097M6I30) SODIUM STARCH GLYCOLATE TYPE A POTATO (UNII: 5856J3G2A2) Product Characteristics Color WHITE (White) Score 2 pieces Shape ROUND (Round) Size 7mm Flavor Imprint Code 1110 Contains Packaging # Item Code Package Description Marketing Start Date Marketing End Date 1 NDC:70710-1110-1 100 in 1 BOTTLE; Type 0: Not a Combination Product 07/20/2017 2 NDC:70710-1110-0 1000 in 1 BOTTLE; Type 0: Not a Combination Product 07/20/2017 Marketing Information Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date ANDA ANDA208938 07/20/2017 Labeler - Zydus Pharmaceuticals USA Inc. (156861945) Registrant - Zydus Pharmaceuticals USA Inc. (156861945) Establishment Name Address ID/FEI Business Operations Zydus Lifesciences Limited 863362789 ANALYSIS(70710-1110) , MANUFACTURE(70710-1110)