Pharmacokinetics and pharmacodynamics of terfenadine and chlorpheniramine in the elderly

Simons, Keith J.; Martin, Tara J.; Watson, Wade; Simons, F. Estelle R.

doi:10.1016/0091-6749(90)90091-h

Cited by 159 publications

(15 citation statements)

References 20 publications

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“…These findings agree with those of previous studies where maximal activity of fexofenadine occurred at 4 h and decreased thereafter [4, 16]. The 4 h maximal effect was also found with terfenadine, the precursor of fexofenadine [17], although the following rapid decrease in fexofenadine activity contrasts with the plateau of effect that was previously reported for terfenadine [17]. This might be related to the metabolization of terfenadine into the active metabolite fexofenadine, thus lengthening its action.…”

Section: Discussioncontrasting

confidence: 49%

A Study Comparing the Inhibitory Effects of Single and Repeated Oral Doses of Ebastine and Fexofenadine against Histamine-Induced Skin Reactivity

Barbanoj¹,

Antonijoan

García-Gea³

et al. 2003

Int Arch Allergy Immunol

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Objective: The aim of this double-blind, randomized, crossover, placebo-controlled clinical trial was to compare the inhibition of the histamine-induced skin reaction induced by ebastine 20 mg with respect to that induced by fexofenadine 120 mg or placebo. Methods: Eighteen volunteers (10 males, 8 females) received the three treatments once daily for 5 days, with a mean 7-day washout period between treatments. Intradermal tests, using 0.05 ml from a solution containing 100 µg/ml of histamine, were performed at baseline and at 1, 1.5, 2, 3, 10 and 24 h after a single dose and repeated 5-day dose, and in addition after 34, 48, 58 and 72 h after repeated 5-day dose. Results:After 24 h of acute administration, ebastine 20 mg was significantly more effective than fexofenadine 120 mg in reducing the wheal and flare induced by histamine challenge (p < 0.001). Although fexofenadine 120 mg had the shortest onset of action (1.5 vs. 3 h in ebastine 20 mg), the duration of its antihistamine effect was the shortest (24 vs. 58 h in ebastine 20 mg) and wheal reduction after 24 h was not significantly different from placebo. The overall effect after single and repeated 5-day dose, expressed as the AUC of reduction of wheal and flare area (%/h), showed the following order of magnitude: ebastine 20 mg > fexofenadine 120 mg > placebo. No significant differences in the incidence of adverse events were found between the three treatments. Conclusions: The present results clearly show a superior and long-acting effect of ebastine 20 mg compared with fexofenadine 120 mg on the skin response to histamine 24 h after dosing.

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Section: Discussioncontrasting

confidence: 49%

A Study Comparing the Inhibitory Effects of Single and Repeated Oral Doses of Ebastine and Fexofenadine against Histamine-Induced Skin Reactivity

Barbanoj¹,

Antonijoan

García-Gea³

et al. 2003

Int Arch Allergy Immunol

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“…The second–generation drugs offer advantages of greater potency and reduced side effects. Simons et al [1] compared these drugs and showed the order of potency for blocking the wheal and flare response to histamine in the skin was cetirizine, terfenadine, loratadine, astemizole, and chlorpheniramine. Juhlin [2] reviewed multiple clinical trials showing superiority for cetirizine.…”

Section: Introductionmentioning

confidence: 99%

A Comparison of Cetirizine, Ebastine, Epinastine, Fexofenadine, Terfenadine, and Loratadine versus Placebo in Suppressing the Cutaneous Response to Histamine

Danielson

Rihoux

Devos

1999

Int Arch Allergy Immunol

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“…Cetirizine is a potent, second-generation antihistamine with a high specificity for the H1 receptor [1], a rapid onset of activity and a full 24-hour duration of effect [2]. The efficacy of the drug has been established in seasonal allergic rhinitis [3, 4], perennial allergic rhinitis [5, 6, 7], and chronic idiopathic urticaria [8].…”

Section: Introductionmentioning

confidence: 99%

Controlled Comparison of the Efficacy and Safety of Cetirizine 10 mg o.d. and Fexofenadine 120 mg o.d. in Reducing Symptoms of Seasonal Allergic Rhinitis

Horak

Stübner

Zieglmayer

et al. 2001

Int Arch Allergy Immunol

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Background: The efficacy, onset and duration of action and safety of cetirizine 10 mg o.d., fexofenadine 120 mg o.d., and placebo were compared in this investigator-blinded, crossover study involving the use of the Vienna Challenge Chamber. Methods: 40 volunteers with seasonal allergic rhinitis were exposed to a controlled grass pollen concentration for 6 h on 2 consecutive days. Subjective symptoms and objective measurements were recorded during the allergen exposure periods. Results: Both active medications were significantly more effective than placebo and had a comparable onset of action in alleviating the symptoms of seasonal allergic rhinitis. The efficacy of both active drugs was comparable for the first 4 h after administration of the drugs on day 1 and day 2. However from 22 to 24 h after the first dose cetirizine was significantly superior to fexofenadine for the major symptom complex score and for sneezing. Concerning the total symptom complex score at day 2 fexofenadine could not reach superiority to placebo. No serious adverse events were reported. Conclusions: Cetirizine and fexofenadine were significantly better than placebo, also in reducing the symptom of nasal congestion. However cetirizine appears to have a longer duration of action than fexofenadine.

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Pharmacokinetics and pharmacodynamics of terfenadine and chlorpheniramine in the elderly

Cited by 159 publications

References 20 publications

A Study Comparing the Inhibitory Effects of Single and Repeated Oral Doses of Ebastine and Fexofenadine against Histamine-Induced Skin Reactivity

A Study Comparing the Inhibitory Effects of Single and Repeated Oral Doses of Ebastine and Fexofenadine against Histamine-Induced Skin Reactivity

A Comparison of Cetirizine, Ebastine, Epinastine, Fexofenadine, Terfenadine, and Loratadine versus Placebo in Suppressing the Cutaneous Response to Histamine

Controlled Comparison of the Efficacy and Safety of Cetirizine 10 mg o.d. and Fexofenadine 120 mg o.d. in Reducing Symptoms of Seasonal Allergic Rhinitis

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