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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 a 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 metabolised to active metabolite, carebastine. It has antihistaminic, anti-allergic activity and prevents histamine-induced bronchoconstriction. It does not have 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

*Terminologies:

Idiopathic: Relating to or denoting any disease or condition which arises spontaneously or for which the cause is unknown.

Urticaria: A kind of skin rash with red, raised, itchy bumps.

Prodrug: A medication or compound that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug.

Dermographic Urticaria: Also known as dermographism, dermatographism or “skin writing; is an exaggerated wealing tendency when the skin is stroked.

Asthenia: Abnormal physical weakness or lack of energy.

Epistaxis: Bleeding from the nostril, nasal cavity, or nasopharynx.

Hypokalemia: The condition when  blood’s potassium levels are too low.