Label: CYPROHEPTADINE HYDROCHLORIDE- cyproheptadine hydrochloride tablet

  • NDC Code(s): 50742-190-01, 50742-190-10
  • Packager: Ingenus Pharmaceuticals LLC
  • Category: HUMAN PRESCRIPTION DRUG LABEL
  • DEA Schedule: None
  • Marketing Status:

Drug Label Information

Updated December 18, 2017

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  • 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:

    Chemical Structure

    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.

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  • 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 14C-labelled cyproheptadine HCl in normal subjects, given as tablets, 2 to 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 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.

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  • 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

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  • 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

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  • WARNINGS

    Pediatric Patients

    Overdosage 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).

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  • 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 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.

    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 pediatric patients below the age of two have not been established (see CONTRAINDICATIONS, Newborn or Premature Infants, and WARNINGS, Pediatric Patients).

    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).

    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

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  • ADVERSE REACTIONS

    To report SUSPECTED ADVERSE REACTIONS, please call Ingenus Pharmaceuticals NJ, LLC at 1-877-748-1970 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

    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
    Cholestasis, hepatic failure, hepatitis, hepatic function abnormality, 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.

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  • 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 LD50of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

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  • 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 mg to 20 mg a day, with the majority of patients requiring 12 mg 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.

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  • HOW SUPPLIED

    Cyproheptadine Hydrochloride Tablets USP, 4 mg are available as white to off- white, round, flat-faced, beveled-edged tablets, debossed “4” on left side, “9” on right side of the scoring on one side and plain on the other side, containing 4 mg of cyproheptadine HCl packaged in bottles of 100 (NDC 50742-190-01) and 1,000 (NDC 50742-190-10) tablets. Tablets have functional scoring.

    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 For:
    Ingenus Pharmaceuticals, LLC
    Orlando, FL 32839-6408

    Manufactured By:
    Ingenus Pharmaceuticals NJ, LLC
    Fairfield, NJ 07004

    5517 Rev. 06/2017

    5517

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  • PRINCIPAL DISPLAY PANEL

    Package Label - Principal Display Panel – 4 mg, 100 Tablets Label

    ingenus

    NDC 50742-190-01

    Cyproheptadine HCI Tablets, USP

    4 mg

    Rx only

    100 Tablets

    4 mg, 100 Tablets Label

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  • PRINCIPAL DISPLAY PANEL

    Package Label - Principal Display Panel – 4 mg, 1000 Tablets Label

    ingenus

    NDC 50742-190-10

    Cyproheptadine HCI Tablets, USP

    4 mg

    Rx only

    1000 Tablets

    4 mg, 1000 Tablets Label

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  • INGREDIENTS AND APPEARANCE
    CYPROHEPTADINE HYDROCHLORIDE 
    cyproheptadine hydrochloride tablet
    Product Information
    Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:50742-190
    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
    LACTOSE MONOHYDRATE (UNII: EWQ57Q8I5X)  
    MAGNESIUM STEARATE (UNII: 70097M6I30)  
    CELLULOSE, MICROCRYSTALLINE (UNII: OP1R32D61U)  
    SODIUM STARCH GLYCOLATE TYPE A CORN (UNII: AG9B65PV6B)  
    Product Characteristics
    Color WHITE (White to off-white) Score 2 pieces
    Shape ROUND (Round) Size 7mm
    Flavor Imprint Code 49
    Contains     
    Packaging
    # Item Code Package Description Marketing Start Date Marketing End Date
    1 NDC:50742-190-01 100 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product 09/23/2015
    2 NDC:50742-190-10 1000 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product 09/23/2015
    Marketing Information
    Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
    ANDA ANDA205087 09/23/2015
    Labeler - Ingenus Pharmaceuticals LLC (833250017)
    Registrant - Ingenus Pharmaceuticals NJ, LLC (964680206)
    Establishment
    Name Address ID/FEI Business Operations
    Ingenus Pharmaceuticals NJ, LLC 964680206 manufacture(50742-190) , analysis(50742-190) , pack(50742-190)
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