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Ebastine is a second-generation antihistamine which undergoes transformation to its active metabolite, carebastine. Its antihistaminic and antiallergic effects have been demonstrated in in vitro and in vivo studies, in addition to data obtained from clinical trials.
Patients with allergic rhinitis or chronic idiopathic urticaria experienced significant improvement in their symptoms with ebastine 10 or 20mg once daily. Some studies in patients with seasonal allergic rhinitis (SAR) have indicated trends towards greater efficacy with the 20mg than the 10mg dose, although only 1 study has shown statistically significant benefits. In comparative trials in patients with SAR, ebastine 10mg was as effective as most other second-generation antihistamines, including astemizole, azelastine, cetirizine, loratadine and terfenadine. Ebastine 20 mg/day was significantly superior to loratadine 10 mg/day in patients with SAR according to effects on secondary efficacy variables in comparative studies; 1 study found significantly greater changes from baseline in mean total symptom score with ebastine 20mg (−43 vs −36% with loratadine, p = 0.045). In patients with perennial allergic rhinitis, ebastine 10 or 20mg daily was significantly more effective than loratadine in reducing total symptom scores from baseline in 1 comparative study.
There have been no reports of serious adverse cardiac effects during ebastine therapy. Increases in corrected QT interval have been observed during clinical trials; however, these have not been considered clinically significant and were generally of similar magnitude to those seen with loratadine.The normal diurnal variation in QTc interval and the problems associated in correcting for changes in heart rate also complicate assessment of this issue. The incidence of adverse events during ebastine treatment is not significantly greater than that observed with placebo or other second-generation antihistamines.
Conclusions: Ebastine 10mg daily is a well tolerated and effective treatment for allergic rhinitis and chronic idiopathic urticaria. At this dosage, it is as effective as the other second-generation antihistamines against which it has been compared. Ebastine 20mg has similar tolerability to the 10mg dose, and trends towards greater efficacy with the higher dose have been shown in some studies. Ebastine does not appear to be associated with any significant cardiac adverse events. Ebastine is a useful treatment option for patients with allergic rhinitis or chronic idiopathic urticaria.
Single doses of ebastine (10mg or more) are significantly better than placebo in inhibiting histamine-induced wheal and flare. After a week of treatment, 1 study found that ebastine 10 mg/day was as active in inhibiting wheal and flare response as terfenadine 60mg twice daily and loratadine 10 mg/day. A number of trials found cetirizine 10 mg/day superior in activity to ebastine 10 mg/day at assessments performed 2 to 3 hours after drug administration; however, these differences were not detected at 24 hours. In addition, ebastine 20 mg/day was superior in activity to loratadine 10 mg/day; ebastine 20 mg/day was also more active than fexofenadine 120 mg/day at tests performed 24 hours after drug administration, although both agents were similar in effect at 4 hours.
There were no significant differences between placebo and ebastine recipients in wheal or flare responses to histamine challenge 5 days after stopping treatment (7 days of either placebo or ebastine 20 mg/day).
The antiallergic effects of ebastine have been demonstrated in in vitro and in vivo studies; assessment has included nasal challenge tests, skinprick testing, and measurement of the levels of allergic mediators in adults and children with allergies.
Single and multiple therapeutic doses of ebastine did not impair psychomotor performance or driving ability in volunteers. In addition, treatment with ebastine 20mg daily for 1 week did not potentiate the depressant effects of ethanol or the psychomotor performance impairing effects of diazepam.
Concerns regarding possible adverse cardiac effects of second-generation antihistamines have been complicated by contradicting results from in vivo and in vitro models. In clinical studies, difficulties have arisen because of diurnal variation in the QT interval and the use of differing heart rate correction formulae that may provide misleading results. However, most studies in animal in vivo or in vitro models have found that any changes in QTc interval associated with ebastine are noticeably less than those seen with similar concentrations of terfenadine and are not considered to be clinically significant. No clinically relevant abnormalities were found on 24-hour Holter monitoring of healthy elderly and young volunteers who received 10 days of treatment with ebastine 10 mg/day or placebo. Data obtained from >1000 patients enrolled in controlled trials also indicate that ebastine 10 or 20 mg/day is not associated with clinically significant changes in corrected QT (QTc) interval.
Although increased plasma levels of ebastine have been observed during coadministration with ketoconazole or erythromycin, any associated changes in QTc interval have been small and not clinically significant.
Plasma levels of ebastine are low or undetectable after oral administration; therefore, pharmacokinetic studies generally measure the concentrations of the active metabolite, carebastine. In vitro studies using human liver microsomes indicate that, although the metabolism of ebastine does involve the cytochrome P450 (CYP) CYP3A4 enzyme, the conversion of ebastine to carebastine appears to be mediated by other unidentified enzymes. The pharmacokinetics of carebastine are linear.
After oral administration of ebastine 10mg to healthy volunteers, peak plasma concentrations (Cmax) of carebastine ranged from 0.09 to 0.12 mg/L, with a time to reach Cmax of 2.6 to 5.7 hours. Values for the area under the plasma concentration-time curve (AUC) ranged from 1.75 to 2.94 mg/L·h. Results from 2 studies found the volume of distribution of carebastine to be 89.5 and 123L. The elimination half-life (t1/2β) of carebastine ranged from 10.3 to 19.3 hours, with the main route of excretion being the kidneys.
Pharmacokinetic parameters in children and elderly volunteers were generally similar to those seen in healthy adults, although values for Cmax and AUC were higher in children than in adults. Patients with hepatic or severe renal impairment (creatinine clearance <1.8 L/h/1.73m2) had significantly increased values for t1/2β compared with those obtained from healthy volunteers.
The metabolism of single doses of ebastine 20mg was significantly impaired in healthy volunteers receiving multiple doses of either ketoconazole or erythromycin (drugs that inhibit CYP metabolism). In contrast, cimetidine had no significant effects on the metabolism of a single dose of ebastine 20mg.
In clinical trials, ebastine 10 to 20mg once daily for 1 to 12 weeks was effective in the treatment of adults with allergic rhinitis. Although there is a lack of statistical data, studies in patients with seasonal allergic rhinitis (SAR) indicate a trend towards greater efficacy with ebastine 20mg than with 10mg, with 1 study showing significantly greater reductions in total symptom score with the higher dose (13.7 vs 11.8 with 10 mg, p = 0.027) in the subgroup of patients with more severe symptoms (defined as those with a baseline total symptom score greater than the mean for the study population).
In patients with SAR, comparative trials have shown ebastine 10 mg/day to be as effective at relieving symptoms as total daily doses of astemizole 10mg, azelastine 0.56mg (as an intranasal spray), cetirizine 10mg, loratadine 10mg and terfenadine 120mg. In 1 of 3 similarly designed trials (all unpublished, double-blind and placebo-controlled), ebastine 20 mg/day produced significantly greater percentage reductions from baseline in mean total symptom score than those seen with loratadine 10 mg/day (−43 vs −36%, p = 0.045). Although changes in mean total symptom score did not differ significantly between treatments in other studies, all found ebastine 20mg to be significantly superior to loratadine according to some or most of the secondary efficacy variables. Ebastine 20mg daily was also significantly superior to cetirizine 10mg daily in some of the variables assessed after 1 week in a double-blind study in 343 patients with SAR; however, at the end of the 2-week study, cetirizine had reached a similar level of efficacy.
Once-daily doses of ebastine 10mg and astemizole 10mg were similarly effective when used as prophylaxis against the onset of SAR symptoms in a non-blind randomised study in 217 patients with a history of SAR.
Data on efficacy of ebastine in children are limited; however, 1 double-blind study in 173 children with SAR found that ebastine 5 mg/day for 3 weeks significantly improved overall symptom scores compared with placebo.
Ebastine 10 and 20 mg/day are significantly more effective than placebo for improving symptoms of perennial allergic rhinitis (PAR). No significant differences have been found between the 2 doses. In 1 large comparative randomised double-blind trial in patients with PAR, ebastine 10 and 20mg were significantly more effective than loratadine 10mg at reducing total symptom scores from baseline. Ebastine 10mg daily was also as effective as cetirizine 10 mg/day in improving total PAR symptom scores from baseline during a 4-week trial; however, improvement was significantly faster with cetirizine, and significantly more cetirizine recipients were symptom-free by the end of the trial (17.8 vs 6.9% with ebastine, p = 0.02).
Ebastine 5 to 20mg daily is as effective in the treatment of chronic idiopathic urticaria as terfenadine 60mg twice daily, ketotifen 2mg once daily and astemizole 10mg once daily. Preliminary findings from studies also indicate benefits in the treatment of pruritic dermatoses, and significant improvements in morning peak expiratory flow rates in 20 patients with asthma were seen during treatment with ebastine.
Ebastine was well tolerated in clinical trials, with a similar incidence of adverse events to that observed with placebo. In comparative trials with other second-generation antihistamines, ebastine was at least as well tolerated as astemizole, cetirizine, loratadine and azelastine. There have been no significant differences in tolerability reported between ebastine 10 and 20mg.
The adverse events most commonly reported during treatment with ebastine 10 or 20mg were headache (≈6 to 13% of patients in individual trials), somnolence (1.4 to 9%) and dry mouth (4 to 7%). Less frequently occurring adverse events (<5% of patients) included asthenia, nausea, abdominal pain, gastrointestinal upset, altered appetite and insomnia.
Although both terfenadine and astemizole have been associated with serious cardiac abnormalities — in particular, ventricular arrhythmias — no such events have been reported during treatment with ebastine. Some studies have found small statistically significant increases in QTc interval (compared with baseline or placebo values) during treatment with ebastine 20mg daily; however, these differences were not considered clinically significant and were not sustained throughout the studies. Normal diurnal variation and the use of heart rate correction formulae also complicate the assessment of the significance of these changes. Comparative studies found similar percentages of patients with QTc intervals >0.444 seconds with ebastine (10 or 20mg) and loratadine 10mg. Analysis of pooled ECG data from a number of large clinical trials did not find any patients treated with ebastine who had QTc intervals of >0.5 seconds.
Laboratory tests failed to find any clinically significant differences between patients who received ebastine and those who received placebo or other second-generation antihistamines.
Dosage and Administration
Single daily oral doses of ebastine 10mg are effective in the treatment of adults with allergic rhinitis or chronic idiopathic urticaria; increasing the dose to 20mg daily does not significantly affect tolerability and may be of use in some patients. A dose of 5mg daily is recommended in children. Ebastine, like other antihistamines, should be used with caution in patients with known QTc prolongation.
- Lemanske Jr RF. A review of the current guidelines for allergic rhinitis and asthma. J Allergy Clin Immunol 1998 Feb; 101 (Pt 2): S392–396
- Durham S. Summer hay fever. BMJ 1998 Mar 14; 316: 843–5
- Levenson T, Greenberger PA. Pathophysiology and therapy for allergic and nonallergic rhinitis: an updated review. Allergy Asthma Proc 1997 Jul–Aug; 18: 213–20
- Fornadley JA, Corey JP, Osguthorpe JD, et al. Allergic rhinitis: clinical practice guideline. Otolaryngol Head Neck Surg 1996 Jul; 115: 115–22
- Bousquet J. Antihistamines in severe/chronic rhinitis. Clin Exp Allergy 1998; 28 Suppl. 6: 49–53
- Executive summary. Allergy Eur J Allergy Clin Immunol Suppl 1998; 53(41) Suppl.: 7–31
- Bachert C. Histamine — a major role in allergy? Clin Exp Allergy 1998; 28 Suppl. 6: 15–9
- Simons FER. Hi-Receptor antagonists: comparative tolerability and safety. Drug Saf 1994; 10: 350–80
- Simons FER, Simons KJ. Clinical pharmacology of new histamine H1 receptor antagonists. Clin Pharmacokinet 1999 May; 36(5): 329–52
- Wiseman LR, Faulds D. Ebastine: a review of its pharmacological properties and clinical efficacy in the treatment of allergic disorders. Drugs 1996 Feb; 51: 260–77
- Kukita A, Kawashima M, Harada S, et al. Clinicopharmacological study of LAS-90: inhibitory effect on wheal and erythema induced by intradermal injection of histamine [in Japanese]. Rinsho Iyaku 1994; 10 Suppl. 1: 103–11
- Buchmeier A, Nelson HS, Bucher B, et al. Dose-response of prick skin test (PST) suppression by ebastine [abstract]. J Allergy Clin Immunol 1994 Jan; 93 (1 Pt 2): 163
- Simons FER, Watson WTA, Simons KJ. Pharmacokinetics and pharmacodynamics of ebastine in children. J Pediatr 1993 Apr; 122: 641–6
- Gispert J, Antonijoan R, Barbanoj M, et al. Pharmacodynamic assessment of the efficacy of single and multiple doses of ebastine, cetirizine and loratadine against histamine-induced cutaneous challenge in healthy volunteers [abstract]. J Allergy Clin Immunol 1998 Jan; 101 (1 Pt 2): S221
- Cassel DA, Garcia JD, Alderfer VB, et al. Dose-response suppression of histamine-induced wheal and flare by ebastine in allergic rhinitis patients [abstract]. Allergy 1995; 50 Suppl. 26: 105
- Westra S. Duration of inhibited skin reactivity to allergens and histamine following discontinuation of ebastine 20 mg. 5/4/99. Rhone Poulenc. [Data on file]
- Almeda E, Daza JC, Reyes L, et al. A comparative study of ebastine and cetirizine effect on in-vivo test on children who are sensitive to olea pollen [abstract]. Allergy 1992; 47 Suppl. 12:99
- Almeda E, Daza JC, Reyes L, et al. A comparative study of ebastine and loratadine effect on in vivo test of children sensitive to olea pollen [abstract]. Allergy Clin Immunol News 1994 Suppl. 2:389
- de la Cuadra J, Teruel M, Teixido P, et al. Assessment of the wheal size and skin blood flow of the erythema induced by histamine and its modification with cetirizine and ebastine: a crossover, double-blind study. Dermatology 1994; 188: 131–4
- Rivest J, Despontin K, Ghys L. Pharmacological modulation by cetirizine and ebastine of the cutaneous reactivity to histamine. Dermatologica 1991; 183(3): 208–11
- Torrent Farnells J, Segura J. Study of the antihistamine effect of LAS W090 (INN ebastine) in healthy volunteers. Single oral administration of LAS W-090 (10 mg) in human volunteers and a pharmacokinetic study of its acid metabolite. Rhône-Poulenc Rorer (Collegeville), 1984. Report no. Clin 1/5 and Bio 3/2 (Data on file)
- Carrenca FJ, Farnells JT, Pulido II, et al. Study of safety, pharmacokinetics and antihistamine effects of LAS W-090 at repeated doses in healthy volunteers. Rh one-Poulenc Rorer (Collegeville), 1986. Report No. Clin 1/7 (Data on file)
- Frossard N, Melac M, Benabdesselam O, et al. Consistency of the efficacy of cetirizine and ebastine on skin reactivity. Ann Allergy Asthma Immunol 1998; 80(1): 61–5
- Aparicio S, Granel C, Randazzo L, et al. Studies of nonsedative antihistamines. II. Assessment of its antihistaminic potency. Allergol Immunopathol Madr 1992 Sep–Oct; 20: 207–10
- Antonijoan R, Gispert J, Gich I, et al. Double-blind, randomised, monocentre, placebo-controlled cross-over study to evaluate the inhibitory effects of single and repeated (5 days) oral doses of ebastine (20mg) and fexofenadine (120mg) against histamine-induced skin reactions in healthy volunteers. Almirall Prodesfarma, S.A. (Barcelona), 1999. (Data on file)
- Wood-Baker R, Holgate ST. Dose-response relationship of the H1-histamine antagonist, ebastine, against histamine and methacholine-induced bronchoconstriction in patients with asthma. Agents Actions 1990 Apr; 30: 284–6
- Roberts DJ. A preclinical overview of ebastine: studies on the pharmacological properties of a novel histamine H1 receptor antagonist. Drugs 1996; 52 Suppl. 1: 8–14
- Yakuo I, Inuj A, Yabuuchi M, et al. Effects of ebastine, a selective histamine H1 receptor antagonist, on experimental asthma in guinea pigs [abstract]. Jpn J Pharmacol 1997; 73 Suppl. I: 99P
- Fernández L, Fernández del Cotero JN, Rodríguez F, et al. Protective effect of ebastine on the conjunctival provocation test with histamine [abstract no. P-0300]. Allergy 1995; 50 Suppl.: 182
- Campbell A, Michel F-B, Bremard-Oury C, et al. Overview of allergic mechanisms: ebastine has more than an antihistamine effect. Drugs 1996; 52 Suppl. 1: 15–9
- Chanal I, Maudino G, Campbell AM, et al. Efficacy of ebastine assessed by nasal challenge in a double-blind placebo-controlled study [abstract]. J Allergy Clin Immunol 1994 Jan; 93: 272
- Horiguchi T, Tachikawa S, Kasahara J, et al. Effect of ebastine on serum eosinophil cationic protein levels in patients with bronchial asthma. Clin Drug Invest 1999 Jun; 17(6): 435–40
- Llupiá J, Llenas J, Palacios JM. In vitro and in vivo anti-leukotriene effects of ebastine [abstract]. Eur Respir J 1997 Sep; 10 Suppl. 25: 439s
- Leroy T, Tasset C, Valentin B, et al. Comparison of the effects of cetirizine and ebastine on the skin response to histamine iontophoresis monitored with laser Doppler flowmetry. Dermatology 1998 (197): 146–51
- Monroe EW, Daly AF, Shalhoub RF. Appraisal of the validity of histamine-induced wheal and flare to predict the clinical efficacy of antihistamines. J Allergy Clin Immunol 1997 Feb; 99: S798–806
- Bernstein L, Storms WW Summary statements of practice parameters for allergy diagnostic tests. Ann Allergy Asthma Immunol 1995 Dec; 75(2): 543–52
- Roberts DJ, Gispert J. The non-cardiac systemic side-effects of antihistamines: ebastine. Clin Exp Allergy 1999; 29 Suppl. 3: 151–5
- Mattila MJ, Kuitunen T, Plétan Y. Lack of pharmacodynamic and pharmacokinetic interactions of the antihistamine ebastine with ethanol in healthy subjects. Eur J Clin Pharmacol 1992 Aug; 43: 179–84
- Mattila MJ, Aranko K, Kuitunen T. Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine. Br J Clin Pharmacol 1993 Mar; 35: 272–7
- Matsunaga K, Sato T, Shuto H, et al. Inhibition of neuronal dopamine uptake by some antiallergic drugs. Eur J Pharmacol 1998 Jun 5; 350: 165–9
- Simons FER, Simons KJ. The pharmacology and use of H1-receptor-antagonist drugs. N Engl J Med 1994 Jun 9; 330(23): 1663–70
- Llenas J, Bou J, Massingham R. Preclinical safety studies with ebastine. II. Pharmacological effects on the cardiovascular system. Drugs Today 1992; 28 Suppl. B: 29–34
- Gras J, Llenas J, Palacios JM. Ebastine is without effect in a sensitive experimental model for detecting prolongation of the QTC interval [abstract]. Allergy 1996; 51 Suppl. 31: 188
- Mann Ko C, Ducic I, Fan J, et al. Suppression of mammalian K+ channel family by ebastine. J Pharmacol Exp Ther 1997 Apr; 281: 233–44
- Valenzuela C, Delpón E, Franqueza L, et al. Comparative effects of nonsedating histamine H1 receptor antagonists, ebastine and terfenadine, on human Kv1.5 channels. Eur J Pharmacol 1997 May 20; 326: 257–63
- Hey JA, del Prado M, Sherwood J, et al. Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects. Arzneimittel Forschung 1996 Feb; 46: 153–8
- Heredia A, Beleta J, Llenas J, et al. Terfenadine and the main metabolite of loratadine release histamine from cardiac mast cells: possible cardiotoxic consequences [abstract]. Annual Meeting American College of Allergy, Asthma & Immunology 1996 Nov 8–13; 64
- Moss A. Panel discussion. Drug Saf 1999; 21 (Assessing the cardiac safety of ebastine) Suppl. 1: 81–7
- Lindquist M, Edwards IR. Risks of non-sedating antihistamines. Lancet 1997 May; 349: 1322
- Funck-Bretano C, Jaillon P. Rate-corrected QT interval: techniques and limitations. Am J Cardiol 1993 Aug 26; 72: 17B–22B
- Molnar J, Weiss J, Zhang F, et al. Evaluation of five QT correction formulas using a software-assisted method of continuous QT measurement from 24-hour Holter recordings. Am J Cardiol 1996 Oct 15; 78: 920–6
- Sagie A, Larson MG, Goldberg RJ, et al. An improved method for adjusting the QT interval for heart rate (the Framingham Heart Study). Am J Cardiol 1992 Sep 15; 70: 797–801
- Garson Jr A. How to measure the QT interval — what is normal? Am J Cardiol 1993 Aug 26; 72: 14B–6B
- Morganroth J, Brozovich FV, McDonald JT, et al. Variability of the QT measurement in healthy men, with implications for selection of an abnormal QT value to predict drug toxicity and proarrhythmia. Am J Cardiol 1991 Apr 1; 67: 774–6
- Huang M-Y, Argenti D, Wilson J, et al. Pharmacokinetics and electrocardiographic effect of ebastine in young versus elderly healthy subjects. Am J Ther 1998 May; 5: 153–8
- Moss AJ, Morganroth J. Cardiac effects of ebastine and other antihistamines in humans. Drug Saf 1999; 21 Suppl. 1: 69–80
- Bruno R, Baille P, Rhodes G, et al. An evaluation of the pharmacokinetic/pharmacodynamic (PK/PD) relationships with ebastine at high exposures [abstract no. 593]. J Clin Pharmacol 1998 Sep; 38(9): 874
- Gillen M, Pentikis H, Rhodes G, et al. Pharmacokinetic (PK) and cardiac safety studies of ebastine (EBA) and loratidine (LOR) administered with ketoconazole (keto) [abstract no. 579]. J Clin Pharmacol 1998 Sep; 38(9): 867
- Wilson J, Huang M-Y, Garcia J, et al. An open-label interaction study between a single dose of ebastine and multiple doses of ketoconazole on the cardiac function and pharmacokinetic profile in healthy adult male volunteers. Rhône-Poulenc Rorer (Collegeville), 1994. Report No. EBA 127 (Data on file)
- Gillen M, Pentikis H, Rhodes G, et al. Pharmacokinetic (PK) and pharmacodynamic (PD) interaction of ebastine (EBA) and erythromycin (ERY) [abstract]. J Clin Pharmacol 1998 Sep; 38: 878
- Wilson J, Huang M-Y, Garcia J, et al. An open-label interaction study betweem a single dose of ebastine and a mulitple dose of erythromycin stearate on the cardiac function and pharmacokinetic profile in healthy adult male volunteers. Rhône-Poulenc Rorer (Collegeville), 1994. Report no. EBA 130 (Data on file)
- Nagasawa K, Saito H, Nomura A, et al. Effect of ebastine with concomitant use of erythromycin on electrocardiographic findings and pharmacokinetics [abstract]. 6th International Congress on Cardiovascular Pharmacotherapy 1996 Feb 26–29: Sydney, Australia
- Yamaguchi T, Hashizume T, Matsuda M, et al. Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects. Arzneimittel Forschung 1994 Jan; 44: 59–64
- Vincent J, Liminana R, Meredith PA, et al. The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects. Br J Clin Pharmacol 1988 Nov; 26: 497–502
- Martínez-Tobed A, Tarrús E, Segura J, et al. Pharmacokinetic studies of ebastine in rats, dogs and man. Drugs Today 1992; 28 Suppl. B: 57–67
- Nakamura T, Mizorogi Y, Matsuda M, et al. Pharmacokinetics of ebastine in the elderly. Rinsho Iyaku 1994; 10(9): 47–54
- Huang M-Y, Wilson J, Argenti D, et al. Comparative pharmacokinetics of ebastine/carebastine in liver cirrhosis and healthy volunteers following administration of a 10 mg ebastine tablet. Pharm Res 1993; 10 Suppl. 10: S–390
- Huang M-Y, Argenti D, Wilson J, et al. Single dose and steady-state pharmacokinetics of carebastine following administration of 10 mg ebastine tablets once daily in healthy elderly and young adults. Pharm Res 1993; 10 Suppl. 10: S–391
- Investigator’s Brochure. Rhône-Poulenc Rorer (Collegeville), 1995. (Data on file)
- Scheen AJ, Le Roux Y, Gaillard C, et al. Effect of food intake on the excretion balance, metabolism and pharmacokinetics of ebastine in healthy volunteers [abstract]. Therapie 1995; 50 Suppl.: 496
- Stamidis Pentikis H, Huang M-Y, Dorr MB, et al. The effect of food on the bioavailability of ebastine. Am J Ther 1997 Feb–Mar; 4: 80–4
- Fujii T, Matsumoto S, Amejima H, et al. Absorption, distribution, metabolism and excretion of [14C] ebastine after a single administration in rats. Arzneimittel Forschung 1994 Apr; 44: 527–38
- Hashizume T, Mise M, Terauchi Y, et al. N-dealkylation and hydroxylation of ebastine by human liver cytochrome P450. Drug Metab Dispos 1998 Jun; 26: 566–71
- Fujii T, Matsumoto S, Hatoyama T, et al. Studies on the first-pass metabolism of ebastine in rats. Arzneimittel Forschung 1997 Aug; 47(II): 949–53
- Van-Rooij J, Schoemaker HC, Bruno R, et al. Cimetidine does not influence the metabolism of the Hi-receptor antagonist ebastine to its active metabolite carebastine. Br J Clin Pharmacol 1993 Jun; 35: 661–3
- Ankier SI, Warrington SJ. A double-blind placebo-controlled study of the efficacy and tolerability of ebastine against hay-fever in general practice patients. J Intern Med 1989 Dec; 226: 453–8
- de Molina M, Cadahia L, Cano L, et al. Efficacy and tolerability of ebastine at two dose levels in the treatment of seasonal allergic rhinitis. Drug Invest 1989; 1(1): 40–6
- Peláez A. Clinical efficacy of ebastine in the treatment and prevention of seasonal allergic rhinitis. Drugs 1996; 52 Suppl. 1: 35–8
- Storms WW. Clinical studies of the efficacy and tolerability of ebastine 10 or 20mg once daily in the treatment of seasonal allergic rhinitis in the US. Drugs 1996; 52 Suppl. 1: 20–5
- Banov CH, Chervinsky P, Munk ZM, et al. Multicenter double-blind parallel-group randomized comparisons of ebastine and placebo in patients with seasonal allergic rhinitis. Rhône-Poulenc Rorer (Collegeville), 1992. Report no. EBA 124 (Data on file)
- Grossman J. Multicentre double-blind placebocontrolled dose response study of ebastine in ragweed SAR patients [abstract]. Allergy 1996; 51 Suppl. 31: 41
- Gehanno P, Bremard-Oury C, Zeisser P. Comparison of ebastine to cetirizine in seasonal allergic rhinitis in adults. Ann Allergy Asthma Immunol 1996 Jun; 76: 507–12
- Bernstein DI, Del Rio M, Georges GC, et al. Placebo controlled trial of ebastine 20 mg and 10 mg once daily versus loratidine 10 mg once daily in the treatment of seasonal allergic rhinitis (SAR) [abstract]. Eur J Allergy Clin Immunol 1999; 54 Suppl. 52: 150
- Vervloet D, Valleteau A. A double-blind placebo-controlled study of the efficacy and safety of ebastine 20mg, ebastine 10mg, and loratidine 10mg in seasonal allergic rhinitis in Europe [poster]. European Academy of Allergology and Clinical Immunology; 1999 Jul 3–7; Brussels
- Ratner PH, Del Rio M, Georges GC, et al. Ebastine 20mg once daily is superior to loratidine 10mg once daily in relieving seasonal allergic rhinitis (SAR) symptoms [poster]. European Academy of Allergology and Clinical Immunology; 1999 Jul 3–7; Brussels
- Ankier SI, Jay L, Warrington SJ. Report on a placebo-controlled study in general practice to compare the efficacy and tolerability of ebastine and astemizole 10 mg against the symptoms of hay fever. Aventis. Report No. 61 (Pt IV.B. 1) [Data on file]
- Antépara I, Jaúregui I, Basomba A, et al. Investigation of the efficacy and tolerability of azelastine nasal spray versus ebastine tablets in patients with seasonal allergic rhinitis [in Spanish]. Allergol Immunopathol Madr 1998 Jan–Feb; 26: 9–16
- Conde Hernández DJ, Palma Aqilar JL, Delgado Romero J. Comparison of azelastine nasal spray and oral ebastine in treating seasonal allergic rhinitis. Curr Med Res Opin 1996; 13(6): 299–304
- Antépara I, Basomba, Castillo, et al. Double-blind randomised parallel clinical trial to compare the efficacy and tolerability of ebastine 20 mg once daily with loratidine 10 mg once daily and placebo in the treatment of seasonal allergic rhinitis. Avenus. Report No. 72 (Pt IV.B.2) (Data on file)
- Ratner PH, Lim JC, Georges GC. Comparison of once-daily dosing of ebastine 20mg, ebastine 10mg, loratidine 10mg and placebo in the treatment of seasonal allergic rhinitis. Rhône-Poulenc Rorer Pharmaceuticals (Pennsylvania), 1999, July 12, 1999. (Data on file)
- Castro E, Molina E, Prieto L, et al. A comparative study of the efficacy and tolerability of ebastine (LAS W 0-90) and terfenadine in the treatment of seasonal allergic rhinitis. Aventis. Report No. 60 (Pt IV.B.1) [Data on file]
- Czarny D, Gillis D, Katelaris C, et al. A double-blind randomized controlled multicentre phase III efficacy and safety trial to assess the effect of ebastine (RP 64305) 10 mg (o.d) versus terfenadine 60 mg (b.i.d) and placebo given for a period of three weeks in the treatment of adult patients with seasonal allergic rhinitis. Aventis. Report No. 59 (Pt IV.B.1) [Data on file]
- Moreland TA, Pears JS, Mills MJ, et al. The effect of ebastine on warfarin kinetics and dynamics. 5th World Conference on Clinical Pharmacology & Therapeutics, 1992 Jul 26–31; Yokohama, Japan
- Luria X, Robert M, Antepara I, et al. A double-blind placebo controlled study of the efficacy and tolerability of ebastine and loratidine in seasonal allergic rhinitis patients [abstract no. P-0350]. Allergy 1995; 50: 199
- Ostrom N, Welch M, Morris R, et al. Evaluation of ebastine (Eba), a new non-sedating antihistamine in children with seasonal allergic rhinitis (SAR) [abstract no. 261586]. J Allergy Clin Immunol 1994 Jan; 93 (1 Pt 2): 163
- Picado Vallés C, Cadahia Garcia A, Cisteró Bahima A, et al. Ebastine in perennial allergic rhinitis. Ann Allergy 1991 Dec; 67: 615–8
- Bousquet J, Gaudaño EM, Parma Carlos AG, et al. 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 1999; 54: 562–8
- Bronsky EA, Jacobson KW, Klimas JT, et al. Ebastine 20 mg once daily for oral treatment of patients with perennial alllergic rhinitis: a multicenter, double-blind, placebo-controlled study. Rhône-Poulenc Rorer, Collegeville, PA, 8129; May 1998. (Data on file)
- Baba S, Ito H, Takagi I, et al. Early phase II study of LAS-90 on perennial allergic rhinitis [in Japanese]. Rinsho Iyaku 1994; 10 Suppl. 1: 113–24
- Baba S, Takagi I, Saito Y, et al. Clinical evaluation of LAS-90 on Japanese cedar pollinosis [in Japanese]. Rinsho Iyaku 1994; 10 Suppl. 1: 147–61
- Baba S, Takagi I, Okuda M, et al. Phase II study of LAS-90 on perennial allergic rhinitis: optimal dose finding study by double-blind technique [in Japanese]. Rinsho Iyaku 1994; 10 Suppl. 1: 125–45
- Baba S, Mamiya S, Sakakura Y, et al. Clinical trial of LAS-90 on perennial allergic rhinitis: a double blind study in comparison with ketotifen fumarate [in Japanese]. Rinsho Iyaku 1994; 10(5): 1143–62
- Cadahia A, Picado C, Cisteró A, et al. Efficacy and tolerability of the H1-antihistamine ebastine in the treatment of perennial allergic rhinitis. Laboratorios Almirall, Barcelona. (Data on file)
- Davies RJ, European Multicentre Study Group. Efficacy and tolerability comparison of ebastine 10 and 20mg with loratadine 10mg: a double-blind, randomised study in patients with perennial allergic rhinitis. Clin Drug Invest 1998 Dec; 16: 413–20
- Murris-Espin M, Melac M, Charpentier J-C, et al. Comparison of efficacy and safety of cetirizine and ebastine in patients with perennial allergic rhinitis. Ann Allergy Asthma Immunol 1998 May; 80: 399–403
- Bronsky EA. Efficacy and safety of ebastine 20mg once daily (AM) in the treatment of perennial allergic rhinitis (PAR) [abstract]. Allergy 1996; 51 Suppl. 31: 42
- Aliaga Boniche A, Olmos Acebes L, Kisis J, et al. Placebo controlled study of mizolastine 10 mg and ebastine 10 mg once daily in chronic idiopathic urticaria (CIU) [abstract no. P171]. Allergy 1999; 54 Suppl. 52: 113–4
- Kukita A, Harada S, Yoshida H, et al. Clinical study of LAS-90 on eczema/dermatitis, prurigo and pruritus cutaneus [in Japanese]. Rinsho Iyaku 1994; 10 Suppl. 1: 73–88
- Davies RJ. Comparative efficacy and safety of once-daily ebastine 10 or 20mg and loratadine 10 mg in the treatment of perennial allergic rhinitis [abstract]. Allergy 1997; 52 Suppl. 37: 168
- Cohen B, Gehanno P. Comparison of the efficacy of ebastine 10mg and 20mg once daily with that of cetirizine 10mg once daily in adults with seasonal allergic rhinitis: a multicentre double-blind study. Drugs 1996; 52 Suppl. 1: 26–9
- Dockhorn RJ. Ebastine relieves allergic rhinitis symptoms from l–24h post dose in a double-blind controlled field study [abstract]. Allergy 1996; 51 Suppl. 31: 42
- Chamorro M, Castellano A, Vigaray J, et al. Adverse reaction to antihistamines. Allergy 1998; 53 Suppl. 43: 102
- Bernstein DI, Lim JC, Georges GC. The comparative efficacy and safety of ebastine 20 mg and 10 mg once daily (OD) and loratidine 10 mg OD vs placebo during 4 week treatment of seasonal allergic rhinitis (SAR). J Allergy Clin Immunol 1999 Jan; 103 (1 Pt 2): S526–7
- Connell L, Alderfer V, Garcia J. Electrocardiographic evaluation of ebastine in double-blind allergic rhinitis clinical trials [abstract]. Allergy 1995; 50 Suppl. 26: 105
- Aoki Y, Funabashi H, Terada Y, et al. Reproductive and developmental toxicity studies of ebastine (2): teratogenicity study in rats [in Japanese]. Yakuri to Chiryo 1994 Mar; 22: 1193–215
- Jáuregui J, Roberts DJ. Preclinical safety studies with ebastine. IV. Acute, chronic and reproductive toxicity, mutagenicity and carcinogenicity. Drugs Today 1992; 28 Suppl. B: 45–56
- Parfitt K, editor. Martindale: the complete drug reference. 32nd ed. London: Pharmaceutical Press, 1999
- Paserchia LA, Hewett J, Woosley RL. Effects of ketoconazole on QTc [abstract no. PI-92]. Clin Pharmacol Ther 1994 Feb; 55: 146
- Ebastel: ebastina 10mg. Contraindicaciones [online]. Available from: URL: http://www.encolombia.com [Accessed 2000 Feb 10]
- Horak F, Stübner UP. New trends in allergic rhinitis. Allergy Clin Immunol Int 1998 May–Jun; 10: 81–7
- Kozma CM, Sadik MK, Watrous ML. Economic outcomes for the treatment of allergic rhinitis. PharmacoEconomics 1996 Jul; 10:4–13
- Mackay IS, Durham SR. Perennial rhinitis. BMJ 1998 Mar 21; 316:917–20
- Parikh A, Scadding GK. Seasonal allergic rhinitis. BMJ 1997 May 10; 314: 1392–5
- Nightingale CH. Treating allergic rhinitis with second-generation antihistamines. Pharmacotherapy 1996 Sep–Oct; 16: 905–14
- Lund VJ. Seasonal allergic rhinitis — a review of current therapy. Allergy 1996; 51 Suppl. 28: 5–7
- Milne T. International consensus report on diagnosing and managing rhinitis. Inpharma 1994 Jul 16; 946: 13–4
- Dykewicz MS, Fineman S. Executive summary of joint task force practice parameters on diagnosis and management of rhinitis. Ann Allergy Asthma Immunol 1998 Nov; 81 (5) part 2: 463–8
- Treatment of childhood allergic rhinitis is less than optimal. Drug Ther Perspect 1998 Jul 20; 122: 5–8
- Bousquet J, Demoly P. Specific immunotherapy for allergic rhinitis in children. Allergy Clin Immunol Int 1996 Sep–Dec; 8: 145–50
- Guarderas JC. Rhinitis and sinusitis: office management. Mayo Clin Proc 1996 Sep; 71: 882–8
- Physicians’ Desk Reference. 54th ed. Montvale: Medical Economics Company, 2000
- Handley DA, Magnetti A, Higgins AJ. Therapeutic advantages of third generation antihistamines. Expert Opin Invest Drug 1998 Jul; 7: 1045–54
- Markham A, Wagstaff AJ. Fexofenadine. Drugs 1998 Feb; 55: 269–74
- Pinto YM, van Gelder IC, Heeringa M, et al. QT lengthening and life-threatening arrhythmias associated with fexofenadine [letter]. Lancet 1999 Mar 20; 353(9157): 980
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