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Cyproheptadine Hydrochloride Tablet
Cyproheptadine Hydrochloride Tablet is prescribed for treatment of various allergic conditions including hay fever, insect bites, conjunctivitis, & vasomotor rhinitis. It belongs to class of first generation antihistamine drugs that are potent H1 receptor antagonists. With excellent protein binding ability of 96 to 99%, this tablet gets metabolized in liver by CYP3A4. Cyproheptadine Hydrochloride Tablet is well absorbed in body after oral ingestion and is known for having weak antiandrogenic activity.
- Possesses anticholinergic, antiserotonergic, & antidopaminergic activities
- Excreted in feces & by kidney
- Has elimination half life of about 8.6 hours
Cyproheptadine Hydrochloride 4 mg Tablets is a serotonin and histamine antagonist with anticholinergic and sedative properties. This is a first-generation antihistamine and has a wide range of anti allergic and antipruritic activity, and can be used successfully in the treatment of acute and chronic allergic and pruritic conditions, such as dermatitis, including neurodermatitis and neurodermatitis circumscripta; eczema; eczematoid dermatitis; dermatographism; mild, local allergic reactions to insect bites; hay fever and other seasonal rhinitis; perennial allergic and vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; urticaria; angioneurotic oedema; drug and serumreactions; anogenital pruritus; pruritus of chicken pox.
It is also indicated as adjunctive therapy to adrenaline and other standard measures for the relief of anaphylactic reactions after the acute manifestations have been controlled.
Used for treating various types of allergic reactions and the skin manifestations of allergic reactions:
- skin allergies with itchiness, swelling, or red skin, eczema or nettle rash
- itchiness of chicken pox and reactions to insect bites and stings
- sneezing, watery eyes and blocked or runny nose caused by an allergy (allergic rhinitis)
- conjunctivis caused by an allergy â with red, watery, inflamed eyes
- migraine and other similar headaches
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 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 12to 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.
Use of Cyproheptadine HCl tablet is contraindicated in newborn or premature infants. Other contraindications include hypersensitivity to any ingredient of formulation, angle-closure glaucoma, stenosing peptic ulcer, symptomatic prostatic hypertrophy, bladder neck obstruction and pyloroduodenal obstruction.
Cyproheptadine has an atropine-like action therefore, should be used with caution in patients with history of bronchial asthma, increased intraocular pressure, hyperthyroidism, cardiovascular disease and hypertension. Antihistamines may diminish mental alertness; conversely, particularly, in the young child, they may occasionally produce excitation. Patients should be warned about engaging in activitiesrequiring mental alertness and motor coordination.
Overdose of antihistamines, particularly in infants and children, may produce hallucinations, central nervous system depression, convulsions and death.
Antihistamines are more likely to cause dizziness, sedation and hypotension in elderly.
Pregnancy and Lactation:
Because of the higher risk of antihistamines in newborns and prematures, antihistamine therapy is contraindicated in nursing mothers.
Caution: Since this drug produces drowsiness occasionally, it is advisable to avoid and operate machineries after taking this drug.
MAO inhibitors prolong and intensify the anticholinergic effects of antihistamines. This tablet may have additive effects with alcohol and other CNS depressants like, hypnotics, sedatives, tranquilizers and anti anxiety agents.
Adverse Drug Reactions:
- Heart and circulation
- Feeling like you have a missed heart beat
- Increased heart rate
- Low bloodpressure
Store in a cool, dry & dark place. Protected from direct sunlight.