Ebastine is a non-sedating

Sedative

A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....

 H₁ antihistamine

Antihistamine

An H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...

.

It does not penetrate the blood-brain barrier

Blood-brain barrier

The blood–brain barrier is a separation of circulating blood and the brain extracellular fluid in the central nervous system . It occurs along all capillaries and consists of tight junctions around the capillaries that do not exist in normal circulation. Endothelial cells restrict the diffusion...

 and thus allows an effective block of the H₁ receptor in peripheral tissue

Biological tissue

Tissue is a cellular organizational level intermediate between cells and a complete organism. A tissue is an ensemble of cells, not necessarily identical, but from the same origin, that together carry out a specific function. These are called tissues because of their identical functioning...

 without a central side effect, i.e not causing sedation or drowsiness.

The basic patent for ebastine in Europe is EP-B-134124. It is often provided in micronised form, due to poor water solubility.

Introduction

Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria

Urticaria

Urticaria is a kind of skin rash notable for pale red, raised, itchy bumps. Hives is frequently caused by allergic reactions; however, there are many non-allergic causes...

. It is available in 10 and 20 mg tablets and in the new formulation of 10 and 20 mg Fast-Dissolving Tablets, as well as in pediatric syrup. It has a recommended flexible daily dose of 10 or 20 mg, depending on disease severity.

Ebastine is available in different formulations (tablets, Fast Dissolving Tablets and syrup) and commercialized under different brand names around the world, Ebastel, Ebastel FLAS, Kestine, KestineLIO, KestinLYO, EstivanLYO, Evastel Z, ETC.

Pharmacokinetic profile

Ebastine has a unique chemical structure that differs from other second generation antihistamines. After oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This reaction has a conversion rate of 100%.

Efficacy

Data from over 8.000 patients in more than 40 clinical trials and studies suggest efficacy of ebastine in the treatment of intermittent allergic rhinitis, persistent allergic rhinitis and other indications.

Safety

Ebastine has shown overall safety and tolerability profile with no cognitive/psycomotor impairment, no sedation and cardiac safety. The incidence of most commonly reported adverse events was comparable between the ebastine and placebo groups, which confirms that ebastine has a favourable safety profile. It should not be used by pregnant women without consulting a doctor.