Ebastine is 4'-tert-butyl-4-[4-(diphenylmethoxy)piperidino]butyrophenone.
Antiallergic.
Ebastine is a 2nd-generation antihistamine which undergoes transformation to its active metabolite, carebastine. Its antihistaminic and antiallergic effects have been demonstrated in in vitro and in vivo studies. Ebastine is a long-acting, nonsedating histamine H1-receptor antagonist which binds preferentially to peripheral H1-receptors in vivo. It has shown antihistamine and antiallergic activity in healthy volunteers and patients with allergies and protected against histamine-induced bronchoconstriction in patients with asthma. Significant symptom improvement is observed in patients with seasonal or perennial allergic rhinitis or chronic idiopathic urticaria. Most of the new H1 antagonists do not accumulate in tissues during repeated administration and have a residual action of <3 days after a short course has been completed. Tachyphylaxis or loss of peripheral H1-receptor blocking activity during regular daily use has not been found for ebastine.
Pharmacokinetics: Orally administered ebastine is well absorbed and is extensively distributed into body tissues. It is protein-bound. Most of the new H1 antagonists do not accumulate in tissues during repeated administration and have a residual action of <3 days after a short course has been completed. Ebastine is extensively and rapidly metabolized to its active metabolite; carebastine has a half-life of approximately 15 hrs and duration of action of at least 24 hrs.
Patients with allergic rhinitis or chronic idiopathic urticaria. Patients with seasonal allergic rhinitis (SAR) have indicated trends towards greater efficacy with the 20-mg than the 10-mg dose. Also indicated in the inhibition of histamine-induced wheal and flare reactions of the skin due to allergens or medications that may produce allergic reactions in certain hypersensitive patients. Ebastine does not appear to be associated with any significant cardiac adverse events. Once-daily ebastine offers an effective and well-tolerated alternative to other 2nd-generation antihistamines in current use for the 1st-line treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria.
Histamine-Induced Wheal and Flare: 10 mg/day. Pruritus: 10 mg/day. Severe Pruritus: 20 mg/day may be given initially. Reduce to 10 mg/day upon improvement of itching. Allergic Rhinitis or Chronic Idiopathic Urticaria: A daily single dose of 10 mg can be given. Seasonal Allergic Rhinitis (SAR): 20 mg/day.
Symptoms and Treatment: On overdosage, drowsiness, headache and dry mouth may be seen. There is no specific antidote for antihistamine overdose and treatment is supportive.
Patients who are hypersensitive to ebastine and any of the constituents of Ebast.
Not to be used in large amounts or for long term in people driving vehicles or operating machinery. Not to be taken with alcohol.
Modification in the dosage regimen may be needed in special populations, including elderly patients, and those with hepatic or renal dysfunction. Although psychomotor and sleep studies in healthy subjects in the laboratory may predict that an antihistamine does not cause drowsiness, the safety margin can be narrow enough to cause a central sedating effect during actual treatment. This might result from a patient's individual sensitivity, disease-induced sedation or drug dosages that are for various reasons relatively or absolutely larger (patient's weight, poor response, reduced drug clearance, interactions). Mild to even moderate sedation is not necessarily a major nuisance, particularly if stimulants are added to the regimen (eg, in perennial rhinitis).
Use in pregnancy & lactation: Reports of effect on pregnant women and nursing mothers are not available. Ebast should be used only if the potential benefit to the mother outweighs the potential risk to the foetus.
Reports of effect on pregnant women and nursing mothers are not available. Ebast should be used only if the potential benefit to the mother outweighs the potential risk to the foetus.
The most frequent adverse events reported during ebastine therapy were drowsiness, headache and dry mouth, the incidence being similar to that reported in placebo recipients. Serious adverse cardiac events, observed on rare occasions with some other histamine H
1-receptor antagonists, have not been reported with ebastine and there has been no evidence of QT interval prolongation related to ebastine therapy.
In combination with 1st-generation antihistamines, quinidine-like effects on the cardiac conducting tissues and clinically significant interactions have raised the question of the drug safety. This prodysrhythmic effect has also been briefly mentioned in comparisons of nonsedative H1 antihistamines. In combination with drugs used to treat arrhythmias, ebastine may increase the risk of tachycardia. Large doses of alcohol may cause cardiac and respiratory depression. In combination with macrolides (eg, erythromycin and clarithromycin that induce cytochrome P-450) that is responsible for the biotransformation of antihistamine to its active metabolite, an increase in the antihistaminic effect may be seen.
Store in a cool, dry place.
R06AX22 - ebastine ; Belongs to the class of other antihistamines for systemic use.
FC tab 10 mg x 10 x 10's. 20 mg x 10 x 10's.
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