Ebastine

 

Mechanism of action

Newer second generation antihistaminic that rapidly gets converted to the active metabolite carebastine.  Ebastine and its active metabolite, carebastine, are selective histmine H1 peripheral receptor antagonists devoid of untoward CNS action and anticholinergic effects. Ebastine is rapidly absorbed and undergoes extensive hepatic and intestinal first pass metabolism. It is almost totally converted into the pharmacologically active metabolite. Food increases the plasma levels of carebastine 1-5-2.0 fold. Half life of carebastine is between 15-19 hours. Ebastine and carebastine are highly protein bound (>95%).

 

Indications

Allergic rhinitis (seasonal and perennial), allergic reactions to food and drugs,  chronic urticaria. 

 

Dosage Adults

10-20mg once a day

 

Children

Not recommended

 

Contraindications

Hypersensitivity to ebastine or any of the ingredients.

 

Special precaution

Exercise caution when using ebastine in patinets with known long QT syndrome, hypokalemiamoderate to severe hepatic and/or renal impairment.

 

Adverse drug reactions

Nausea and insomnia may occur. Rarely abdominal pain, dyspepsia, asthenia, headache, dry mouth and drowsiness.

 

Status in

1. Pregnancy   : Contraindicated

2. Lactation     : Contraindicated

3. Old age        : Use with caution.

4. Children      :  Not recommended.

 

Interactions

Azole antifungals, macrolide antibiotics (except azythromycin) : Produce an increase in QT interval as they inhibit CYP3A4 enzyme systems. Can cause cardiotoxicity.

 

Brands available and preparations of ebastine

 

EBAST                          Micro  Labs

10 Tab                  10mg         36.00            N.A

EROSTIN                       Eros Pharma

10 Tab                  10mg         36.00            N.A