Ebastine

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Ebastine
Ebastine Wiki Str.png
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATC code
Pharmacokinetic data
Protein bindingGreater than 95%
MetabolismHepatic (CYP3A4-mediated), to carebastine
Elimination half-life15 to 19 hours (carebastine)
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
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Chemical and physical data
FormulaC32H39NO2
Molar mass469.658 g/mol
3D model (JSmol)
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Ebastine (trade names Evastin, Kestine, Ebastel, Aleva, Ebatrol) 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.[1][2][3]

The patent in which the structure of ebastine is first mentioned is 134124 Patent EP via CAMBIA Patent Lens[2] – espacenet[3] in Europe and 4550116 Patent US via CAMBIA Patent Lens[4] – espacenet[5] in the US. The substance is often provided in micronised form due to poor water solubility.

Uses and availability

Ebastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.[4] It is available in 10 and 20 mg tablets[5] and as fast-dissolving tablets,[6] 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, Ebet, Ebastel FLAS, Kestine, KestineLIO, KestinLYO, EstivanLYO, Evastel Z, Ebatrol, etc.

Pharmacokinetic profile

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.

Ebastine PK.png

Efficacy

Data from over 8,000 patients in more than 40 clinical trials[not in citation given] and studies[3][4][5][7][8][9] 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/psychomotor impairment[5] and no sedation[5] worse than placebo,[2] and cardiac safety, that is, no QT prolongation.[5] 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.

While experiments in pregnant animals showed no risk for the unborn, no such data are available in humans. It is not known whether ebastine passes into the breast milk.[2]

References

  1. Tagawa, M; Kano, M; Okamura, N (2001). "Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-clorphrniramine, a classical antihistamine". Br J Clin Pharmacol. 52 (5): 501–509. doi:10.1046/j.1365-2125.2001.01471.x. PMC 2014616. PMID 11736858.
  2. 2.0 2.1 2.2 Dinnendahl, V, Fricke, U, ed. (2010). Arzneistoff-Profile (in German). 4 (23 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.
  3. 3.0 3.1 Bousquet, J; Gaudaño, EM; Palama Carlos, AG (1999). "A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis". Allergy. 54 (6): 562–568. doi:10.1034/j.1398-9995.1999.00984.x. PMID 10435469.
  4. 4.0 4.1 Van Cauwenberge, P; de Belder, T; Sys, L (2004). "A review of the second-generation antihistamine ebastine for the treatment of allergic disorders". Exp Rew Pharmacother. 5 (8): 1807–13. doi:10.1517/14656566.5.8.1807. PMID 15264995.
  5. 5.0 5.1 5.2 5.3 5.4 Sastre, J (2008). "Ebastine in allergic rhinitis and chronic idiopathic urticaria". Allergy. 63 (Suppl 89): 1–20. doi:10.1111/j.1398-9995.2008.01897.x. PMID 19032340.
  6. Antonijoan, R; García-Gea, C; Puntes, M (2007). "Comparison of inhibition of cutaneous histamine reaction of ebastine fast-dissolving tablet (20 mg) versus desloratadine capsules (5 mg): a randomized, double-blind, double-dummy, placebo-controlled, three period crossover study in healthy, nonatopic adults". Clin Ther. 29 (5): 814–22. doi:10.1016/j.clinthera.2007.05.001. PMID 17697901.
  7. Ratner, P; Falqués, M; Chuecos, F (2005). "Meta-analysis of the efficacy of ebastine 20 mg compared to loratadine 10 mg and placebo in the symptomatic treatment of seasonal allergic rhinitis". Int Arch Allergy Immunol. 138 (4): 312–8. doi:10.1159/000088869. PMID 16224195.
  8. Antonijoan, RM; García-Gea, C; Puntes, M (2007). "A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults". Clin Drug Invest. 27 (7): 453–61. doi:10.2165/00044011-200727070-00002. PMID 17563125.
  9. Gehanno, P; Bremard-Oury, C; Zeisser, P (1996). "Comparison of ebastine to cetirizine in seasonal allergic rhinitis in adults". Annals of Allergy, Asthma and Immunol. 76 (6): 507–12. doi:10.1016/S1081-1206(10)63269-3. PMID 8673684.

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