Pharmacokinetics and Electrocardiographic Effect of Ebastine in Young Versus Elderly Healthy Subjects

Huang, Meiying; Argenti, Domenick; Wilson, Jennifer N.; García, Jorge A.; Heald, Don

doi:10.1097/00045391-199805000-00005

Cited by 16 publications

(10 citation statements)

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“…Generally, there are no clinically relevant differences in the pharmacokinetics of ebastine/carebastine between young adults and elderly patients. In one study, carebastine t max was statistically significantly shorter in elderly patients than in younger ones after a single dose of ebastine 10 mg (4.8 vs 5.7 h; P < 0.004), but did not differ between the age groups after multiple dosing (4.5 vs 5.1 h) (26). In another study, carebastine AUC last was increased (10 088 vs 7457 ng/ml/h) and t ½ prolonged (26 vs 19 h) in elderly patients compared with younger ones after 5 days administration of ebastine 20 mg (both P < 0.05); however, AUC 0-24 and C max values did not differ significantly, and the differences were not considered clinically significant (23).…”

Section: Pharmacokinetic Propertiesmentioning

confidence: 96%

“…After a single dose of ebastine 10 mg, the apparent volume of distribution of carebastine was reported to range from 90 to 143 l, which is indicative of extensive distribution throughout the body (26,27). Metabolism of ebastine is principally via cytochrome P450 (CYP) enzymes (28).…”

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

“…The clearance of ebastine was 4.8 l/h after a single dose of 10 mg (26). Urinary excretion accounts for 66% of the elimination of the administered dosage, principally in the form of conjugated metabolites (31), and the terminal elimination half-life (t ½ ) of carebastine is generally 16-25 h (23, 32).…”

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

“…The presence of mild to severe renal or hepatic impairment does not alter the pharmacokinetics of carebastine to a clinically significant extent, despite changes in t ½ occurring in some studies. Renal impairment had no significant effect on the pharmacokinetics of carebastine (6,31,34) except for a prolongation of t in patients with moderate or severe renal impairment in one study (23)(24)(25)(26) h vs 17-19 h in healthy volunteers; statistics not reported) (6). Hepatic impairment had no clinically relevant effect on the pharmacokinetic parameters of carebastine (32).…”

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

“…Data on the cardiac safety of ebastine are available from studies in healthy volunteers and clinical trials in patients, and show that at therapeutic doses of 10 and 20 mg daily, ebastine has no clinically relevant effect on the QTc interval (75), including in elderly patients (26).…”

Section: Cardiac Safetymentioning

confidence: 99%

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Ebastine in allergic rhinitis and chronic idiopathic urticaria

Sastre

2008

Allergy

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Histamine is a key mediator in the development of allergy symptoms, and oral H1‐antihistamines are among the most widely used treatments for symptomatic relief in conditions such as allergic rhinitis and chronic urticaria. Ebastine is a second‐generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis. In controlled clinical trials in adult and adolescent patients with allergic rhinitis, ebastine 10 mg once‐daily improved symptoms to a significantly greater extent than placebo and to a similar extent as loratadine 10 mg and cetirizine 10 mg (both once‐daily), while ebastine 20 mg proved to be more effective than these two comparator antihistamines. In addition, ebastine was significantly more effective than placebo at relieving the symptoms of chronic idiopathic urticaria. Ebastine provides efficacy throughout the 24‐h dosing interval with once‐daily administration and clinical benefit is seen from the first day of treatment. Small studies have found beneficial effects for ebastine in patients with other disorders, including cold urticaria, dermographic urticaria, atopic asthma, mosquito bites and (in combination with pseudoephedrine) the common cold. In addition to the regular ebastine tablet, a fast‐dissolving tablet (FDT) formulation, which disintegrates in the mouth without the aid of a drink, is also available. It has been shown to be bioequivalent to the regular tablet, and to be significantly more effective than desloratadine at reducing histamine‐induced cutaneous wheals. A number of patient surveys demonstrated that the majority of individuals who tried the fast‐dissolving formulation reported it to be convenient for use, fast‐acting and preferred it to their previous antihistamine medication. Perhaps most importantly, a large proportion of patients indicated that they would prefer to use this new formulation in the future. Ebastine has a rapid onset of action and it can be administered once‐daily, with or without food. Dose modifications are not needed in elderly patients, or in those with renal or mild to moderate hepatic impairment. Ebastine is generally well‐tolerated, and clinical studies showed that at usual therapeutic doses of 10 and 20 mg once‐daily, it had no clinically relevant adverse effects on cognitive function and psychomotor performance or on cardiovascular function. In conclusion, ebastine is an effective and generally well‐tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients.

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Section: Pharmacokinetic Propertiesmentioning

confidence: 96%

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

Section: Pharmacokinetic Propertiesmentioning

confidence: 99%

Section: Cardiac Safetymentioning

confidence: 99%

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Ebastine in allergic rhinitis and chronic idiopathic urticaria

Sastre

2008

Allergy

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Method development and validation for simultaneous determination of ebastine and its active metabolite carebastine in human plasma by liquid chromatography–tandem mass spectrometry and its application to a clinical pharmacokinetic study in healthy Chinese volunteers

Phiri

et al. 2020

Biomedical Chromatography

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A simple LC–tandem mass spectrometry (MS/MS) method to determine ebastine and carebastine (active metabolite) in human plasma was developed and validated. Analytes and internal standards were precipitated by protein precipitation and separated on Synergi Hydro‐RP 80A column (4 μm, 50 mm × 2.0 mm; Phenomenex) by gradient elution with mobile phase A comprising 0.1% formic acid in 5 mm ammonium acetate (NH4Ac) and B comprising 100% methanol at a flow rate 0.4 mL/min. Ions were detected in positive multiple reaction monitoring mode, and they exhibited linearity over concentration range 0.01–8.0 and 1.00–300 ng/mL for ebastine and carebastine, respectively. A clinical pharmacokinetic study was conducted in healthy Chinese volunteers under fasting and fed conditions after a single oral administration of 10 mg ebastine. The maximum plasma concentration (Cmax), time to Cmax (Tmax) and elimination half‐life for ebastine were 0.679 ± 0.762 ng/mL, 1.67 ± 1.43 h and 7.86 ± 6.18 h, respectively, whereas these for carebastine were 143 ± 68.4 ng/mL, 5.00 ± 2.00 h and 17.4 ± 4.97 h, respectively under fasting conditions; the corresponding values under fed conditions were 4.13 ± 2.53 ng/mL, 3.18 ± 1.09 h and 21.6 ± 7.77 h for ebastine and 176 ± 68.4 ng/mL, 6.14 ± 2.0 h and 20.0 ± 4.97 h for carebastine.

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Antihistamines

2006

Meyler's Side Effects of Drugs: The International Encyclopedia of Adverse Drug Reactions and Interactions

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Pharmacokinetics and Electrocardiographic Effect of Ebastine in Young Versus Elderly Healthy Subjects

Cited by 16 publications

References 0 publications

Ebastine in allergic rhinitis and chronic idiopathic urticaria

Ebastine in allergic rhinitis and chronic idiopathic urticaria

Method development and validation for simultaneous determination of ebastine and its active metabolite carebastine in human plasma by liquid chromatography–tandem mass spectrometry and its application to a clinical pharmacokinetic study in healthy Chinese volunteers

Antihistamines

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