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Ebastine (Stin )

Clinical data

AHFS/Drugs.com International Drug Names
Pregnancy cat.  ?
Legal status  ?
Routes Oral

Pharmacokinetic data

Protein binding Greater than 95%
Metabolism Hepatic (CYP3A4-mediated), to carebastine
Half-life 15 to 19 hours (carebastine)

Identifiers

CAS number 90729-43-4
ATC code R06AX22
PubChem CID 3191
ChemSpider 3079
UNII TQD7Q784P1
ChEMBL CHEMBL305660

Chemical data

Formula C32H39NO2
Mol. mass 469.658 g/mol
SMILES[show]
InChI[show]

Ebastine (trade names Stin) is a non-sedating H1antihistamine.

It does not penetrate the blood–brain barrier and thus allows an effective block of the H1receptor in peripheral tissue 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 micronized 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. 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.

Pharmacokinetic profile

E 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%.

Dosage and Directions For Use

  • Allergic rhinitis
  • 20 mg (one tablet) once a day
  • Idiopathic chronic urticaria
  • 20 mg (one tablet) once a day.
  • Ebastine may be taken with or without food.

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.

Side-Effects and Special Precaution

The most common side-effects are headache, dry mouth and drowsiness. Other less commonly reported side effects include pharyngitis, abdominal pain, dyspepsia, asthenia, epitasis, rhinitis, sinusitis, nausea and insomnia. Interactions: The interaction of ebastine in combination with either ketoconazole or erythromycin (both known to prolong the QTc interval) has been evaluated. A significant pharmacokinetic and pharmacodynamic interaction has been observed with these combination; an 18-19 ms (4, 7% – 5%) increase in QTc has been reported with either combination. Ebastine does not interact with the kinetics of theophylline, warfarin, cimetidine, diazepam or alcohol. The sedation effect of alcohol and diazepam may be enhanced. When ebastine is administered with food, there is a 1, 5 to 2, 0 fold increase in the plasma levels and the AUC of the main active acid metabolite of ebastine. This increase does not alter the Tmax. The administration of ebastine with food does not cause a modification in its clinical effect. Ebastine lacks significant sedative effects. Patients should, however, be warned that a small number of individuals may experience sedation. It is therefore advisable to determine individual response before driving or performing complicated tasks. This effect may be compounded by the simultaneous intake of alcohol or other central nervous system depressants.

Safety

Ebastine has shown overall safety and tolerability profile with no cognitive/psychomotor 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 favorable safety profile. It should not be used by pregnant women without consulting a doctor.

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