Ebastine

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Ebastine
Systematic (IUPAC) name
4-(4-benzhydryloxy-1-piperidyl)-1-
(4-tert-butylphenyl)butan-1-one
Identifiers
CAS number 90729-43-4
ATC code R06AX22
PubChem 3191
Chemical data
Formula C32H39NO2 
Mol. mass 469.658 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding Greater than 95%
Metabolism Hepatic (CYP3A4-mediated), to carebastine
Half life 15 to 19 hours (carebastine)
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes Oral

Ebastine (trade names Kestine, Evastin, Ebastel, Aleva) 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 tissue without a central side effect, i.e not causing sedation or drowsiness.

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

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