|Systematic (IUPAC) name|
|Protein binding||Greater than 95%|
|Metabolism||Hepatic (CYP3A4-mediated), to carebastine|
|Half-life||15 to 19 hours (carebastine)|
|Mol. mass||469.658 g/mol|
|(what is this?)|
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.
Uses and availability
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 as 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, Ebet, Ebastel FLAS, Kestine, KestineLIO, KestinLYO, EstivanLYO, Evastel Z, Ebatrol, etc.
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.
Data from over 8,000 patients in more than 40 clinical trials[not in citation given] and studies suggest efficacy of ebastine in the treatment of intermittent allergic rhinitis, persistent allergic rhinitis and other indications.
Ebastine has shown overall safety and tolerability profile with no cognitive/psychomotor impairment and no sedation worse than placebo, and cardiac safety, that is, no QT prolongation. 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.
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- 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. PMID 17697901.
- 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. PMID 16224195.
- Antonijoan; 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. PMID 17563125.
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- Salvà, M; Carreño, B; Pintos, M (2004). "Phase I, single dose, open label, randomized, crossover bioequivalence studies of ebastine 10 mg and 20 mg regular tablets vs 10 and 20 mg fast-dissolving tablets in healthy male volunteers". J Invest Allergol Clin Immunol 14 (4 (Suppl 1)): S5.
- Peyri, J; Vidal, J; Marrón, J (1991). "Ebastine in chronic urticaria: a double-blind placebo controlled study". J Dermatol Treat 2: 51–3.
- "KESTINE Package Insert". South African Electronic Package Inserts. 1997-10-24. Retrieved 2007-04-01.