Ebastine

 

Allergy holding you back from enjoying…..

KESTINE

Generic Name:                    Ebastine

Therapeutic Category:     Anti-allergy

Pharmacological Class:   Selective H1 antagonist (Second Generation)

Composition:                      Kestine 10

                                                Each film-coated tablet contains Ebastine BP 10 mg.

                                                Kestine 20

                                                Each film-coated tablet contains Ebastine BP 20 mg.

Pregnancy Category:        B

Presentation:                      Available in the pack size as 10 tablets X 10 blisters

Description

Ebastine is an H1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood-brain barrier to a significant amount and thus combines an effective block of the H1 receptor in peripheral tissue with a low incidence of central side effects. It is indicated mainly for allergic rhinitis and chronic idiopathic* urticaria*.

Mechanism of Action

Ebastine, a piperidine derivative, is a long-acting, non-sedating, second-generation histamine receptor antagonist that binds preferentially to peripheral H1 receptors. It is a prodrug* and is metabolized to the active metabolite, carebastine. It has antihistaminic, anti-allergic activity and prevents histamine-induced bronchoconstriction. It does not have a significant sedative or antimuscarinic actions.

Indications

·        Allergic Rhinitis

·        Pruritus

·        Dermographic Urticaria*

·        Idiopathic Chronic Urticaria

·        Acquired cold urticaria

Dosage

Route of administration: Oral

Adult: 10-20 mg once daily.

Child: >6 years: 5 mg once daily.

Pharmacokinetics

Absorption: Rapidly absorbed after oral administration

Metabolism: Hepatic

Protein binding: Approximately 95%

Route of elimination: Renal

Half-life: 15-19 hours

Adverse Effects

Common side effects are Headache, Dry mouth, Drowsiness, Pharyngitis, Abdominal pain, Dyspepsia, Asthenia*, Epistaxis*, Rhinitis, Sinusitis, Nausea, and Insomnia

It does not have systemic anticholinergic side effects and does no cause sedation.

Contraindications

KESTINE is contraindicated in the following situations:

·        Hypersensitivity to Ebastine or any of its ingredients

·        Cardiac arrhythmia

Precautions

·        Hypokalemia*

·        Hepatic impairment

·         Renal impairment

Drug Interactions

Concomitant use of ketoconazole, itraconazole, clarithromycin or erythromycin may increase plasma levels of ebastine and cause QTc interval prolongation