Ebastine-second generation antihistaminics drug and its pharmacology

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, i.e. seldom causing sedation or drowsiness. The substance is often provided in micronised form due to poor water solubility.

PHARMACOKINETICS:

 After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete.

 Half life: 10-16 hours.

SIDE EFFECTS:

                   1.Headache.

                   2.Dry mouth.

                   3.Drowsiness.

                   4.Inflammation of pharynx/nose/sinus.

                   5.Abdominal pain.

                   6.Ingestion.

                   7.weakness.

                   8.Nose bleed.

                   9.Nausea and sleeplessness.

CONTRAINDICATION:

                   1.Hypersensitivity.

THERAPEUTIC USES:

                   1. Allergic disorder.

                   2. Pruritides.

                   3. Common cold.

                   4. Vertigo.

REFERENCE:-Tripathi K D"Essential of medical pharmacology",7th edition ,page no-164,167,528