CYPROHEPTADINE HYDROCHLORIDE TABLET [IMPAX GENERICS]

CYPROHEPTADINE HYDROCHLORIDE TABLET [IMPAX GENERICS]
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NDC 0115-1757-01, 0115-1757-03
Set ID 80e13d3f-f4db-4bb4-95d5-5ac1afa70e7e
Category HUMAN PRESCRIPTION DRUG LABEL
Packager Amneal Pharmaceuticals of New York LLC
Generic Name
Product Class
Product Number
Application Number ANDA040537
  • DESCRIPTION

    Cyproheptadine hydrochloride 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

    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 pregelatinized starch.

  • 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 hydrochloride 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 mg 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

    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.

  • 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

  • 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).

  • 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 in vitro; 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 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).


  • 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

    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.

    To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

  • 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 LD50 of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

  • 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.

  • HOW SUPPLIED

    Cyproheptadine hydrochloride tablets USP, 4 mg are supplied as white, round, compressed tablets, debossed "cor" above the bisect and "150" below the bisect and the other side is plain.
    They are supplied as follows:

    Bottles of 100:                    NDC 0115-1757-01
    Bottles of 1000:                  NDC 0115-1757-03

    Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

    Dispense in a well-closed container as defined in the USP. Use child-resistant closure (as required).

    KEEP THIS AND ALL DRUGS OUT OF THE REACH OF CHILDREN.

    Manufactured by:
    Amneal Pharmaceuticals Pvt. Ltd.
    Oral Solid Dosage Unit

    Ahmedabad 382213, INDIA

    Distributed by:
    Amneal Pharmaceuticals LLC

    Bridgewater, NJ 08807

    Product of Italy


    Rev. 05-2019-01

  • PRINCIPAL DISPLAY PANEL

    1
  • INGREDIENTS AND APPEARANCE
    CYPROHEPTADINE HYDROCHLORIDE 
    cyproheptadine hydrochloride tablet
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC:0115-1757
    Route of AdministrationORAL
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    CYPROHEPTADINE HYDROCHLORIDE (UNII: NJ82J0F8QC) (CYPROHEPTADINE - UNII:2YHB6175DO) CYPROHEPTADINE HYDROCHLORIDE4 mg
    Inactive Ingredients
    Ingredient NameStrength
    LACTOSE MONOHYDRATE (UNII: EWQ57Q8I5X)  
    MAGNESIUM STEARATE (UNII: 70097M6I30)  
    CELLULOSE, MICROCRYSTALLINE (UNII: OP1R32D61U)  
    STARCH, CORN (UNII: O8232NY3SJ)  
    Product Characteristics
    ColorWHITEScore2 pieces
    ShapeROUNDSize7mm
    FlavorImprint Code cor;150
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC:0115-1757-01100 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product07/29/2015
    2NDC:0115-1757-031000 in 1 BOTTLE, PLASTIC; Type 0: Not a Combination Product07/29/2015
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    ANDAANDA04053707/29/2015
    Labeler - Amneal Pharmaceuticals of New York LLC (123797875)
    Establishment
    NameAddressID/FEIBusiness Operations
    Amneal Pharmaceuticals Private Limited Oral Solid Dosage Unit650762060ANALYSIS(0115-1757) , LABEL(0115-1757) , MANUFACTURE(0115-1757) , PACK(0115-1757)

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