Ebastine - Wikipedia, The Free Encyclopedia

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.wikipedia.org/wiki/Ebastine

Ebaine

Semaic (IUPAC) name

4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-

1-one

Clinical daa

AHFS/Dg.com International Drug Names

Pegnanc ca. ?

Legal a ?

Roe Oral

Phamacokineic daa

Poein binding Greater than 95%

Meabolim Hepatic (CYP3A4-mediated), to

carebastine

Half-life 15 to 19 hours (carebastine)

Idenifie

CAS nmbe 90729-43-4

ATC code R06AX22

PbChem CID 3191

ChemSpide 3079

UNII TQD7Q784P1

ChEMBL CHEMBL305660

Chemical daa

Fomla C32H39NO2

Mol. ma 469.658 g/mol

SMILES eMolecules & PubChem

(ha i hi?) (eif)

EbaineFrom Wikipedia, the free encyclopedia

Ebaine (trade names Eain, Keine, Ebael, Alea)

is a non-sedating H1 antihistamine.

It does not penetrate the blood-brain barrier and thus allows

an effective block of the H1 receptor in peripheral tissuewithout 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.

Conen1 Introduction

2 Pharmacokinetic profile

3 Dosage And Directions For Use

4 Efficacy

5 Side-Effects And Special Precautions

6 Safety

7 References

8 External links

Inodcion

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, Ebe, Ebael

FLAS, Keine, KeineLIO, KeinLYO, EianLYO,

Eael Z, ETC.

Phamacokineic pofile

InChI


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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%.

Doage And Diecion Fo Ue

Allergic rhinitis

10 mg (one tablet) once a day

Idiopathic chronic urticaria

10 mg (one tablet) once a day.

Ebastine may be taken with or without food.

Efficac

Data from over 8.000 patients in more than 40 clinical trials and studies suggest efficacy of ebastine in the treatmen

of intermittent allergic rhinitis, persistent allergic rhinitis and other indications.

Side-Effec And Special Pecaion

The most common side-effects are headache, dry mouth and drowsiness. Other less commonly reported side

effects include pharyngitis, abdominal pain, dyspepsia, asthenia, epistaxis, rhinitis, sinusitis, nausea and insomnia.

Interactions: The interaction of ebastine in combination with either ketoconazole or erythromycin (both known toprolong the QTc interval) has been evaluated. A significant pharmacokinetic and pharmacodynamic interaction has

been observed with these combination; an 18-19 msec (4,7% - 5%) increase in QTc has been reported with eithe

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.

Safe

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 favourable safety profile. It should not be used by

pregnant women without consulting a doctor.


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Ebastine - Wikipedia, The Free Encyclopedia