Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies

Snidvongs, Kornkiat; Seresirikachorn, Kachorn; Khattiyawittayakun, Likhit; Chitsuthipakorn, Wirach

doi:10.1007/s40265-016-0682-0

Cited by 30 publications

(15 citation statements)

References 50 publications

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“…Our study demonstrates that the risk of fexofenadine on sedative effects was lower than that of the first-generation antihistamines and the second-generation antihistamines and even has been as low as placebo. A recent meta-analysis showed that levocetirizine had a mild sedative effects although it was a new generation antihistamine [69]. According to our study, fexofenadine with no sedative effect is more worthy of recommendation among the new generation antihistamines.…”

Section: Discussionsupporting

confidence: 49%

Antihistamine effects and safety of fexofenadine: a systematic review and Meta-analysis of randomized controlled trials

Huang

Jiang²,

Wang

et al. 2019

BMC Pharmacol Toxicol

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BackgroundAs a new generation antihistamine, fexofenadine has been widely used in allergic diseases. However, there is still a lack of collective evidence regarding the antihistamine effects and safety profiles of fexofenadine relative to other antihistamine drugs and placebo. Therefore, we aimed to systematically evaluate the antihistamine effects and safety of fexofenadine.MethodsAn electronic literature search of randomized controlled trials (RCTs) was performed using Embase, Cochrane and PubMed from establishment to January 1st, 2018. RCTs comparing the antihistamine effects or safety (adverse events, sedative effects, and cognitive/psychomotor function) of fexofenadine with either other antihistamines or placebo for healthy subjects and patients with allergy were selected.ResultsFifty-one studies of 14,551 participants met the inclusion criteria. When compared with the first-generation antihistamines, fexofenadine produced significantly lower adverse events frequency (OR = 0.446; 95% CI: 0.214 to 0.929, P = 0.031), significantly lower sedative effects frequency (OR = 0.265; 95% CI: 0.072 to 0.976, P = 0.046) and significantly less change of all cognitive/psychomotor function. When compared with the second-generation antihistamines, fexofenadine produced significantly marginal sedative effects (OR = 0.59; 95% CI, 0.38 to 0.93; P = 0.02) and significantly less change of most of the cognitive/psychomotor function. When compared with placebo, fexofenadine produced more significant antihistamine effects.ConclusionsFexofenadine has a positive antihistamine effect, which is probably no worse than the second-generation antihistamines. Fexofenadine probably has a favorable safety profile, which is more likely better than that of the first-generation antihistamines. There is lack of data to support that fexofenadine has a better overall safety profile compared to the second-generation antihistamines, however, some presently available evidence on sedative effects and certain aspects of cognitive/psychomotor function favors fexofenadine. Therefore, fexofenadine may be worthy of recommendation for safety related workers.

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Section: Discussionsupporting

confidence: 49%

Antihistamine effects and safety of fexofenadine: a systematic review and Meta-analysis of randomized controlled trials

Huang

Jiang²,

Wang

et al. 2019

BMC Pharmacol Toxicol

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“…Although cetirizine produced modest sedative effects, and both levocetirizine and desloratadine produced mild sedative effects, fexofenadine had no adverse effect. These data suggest that, of the oral antihistamines available, fexofenadine is the only one that does not impair cognitive and psychomotor function, though more head-to-head trials are needed to confirm this [ 41 , 42 , 44 , 63 ]. Overall, a limited number of antihistamines are devoid of sedative effects; however, since fexofenadine displays minimal CNS infiltration, and therefore does not appear to impair cognitive and psychomotor performance, it is considered one of the few truly non-sedating antihistamines, regardless of dose [ 64 , 65 ].…”

Section: Introductionmentioning

confidence: 99%

Fexofenadine: review of safety, efficacy and unmet needs in children with allergic rhinitis

Meltzer

Bever

Lucio

2021

Allergy Asthma Clin Immunol

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Allergic rhinitis (AR) is the most common undiagnosed chronic condition in children. Moderate/severe AR symptoms significantly impair quality of life, and cause sleep disruption, absenteeism and decreased productivity. Additionally, untreated AR predisposes children to asthma and other chronic conditions. Although intranasal corticosteroids are the most effective pharmacologic treatment for AR, oral antihistamines are often preferred. First-generation antihistamines may be chosen to relieve AR symptoms as they are inexpensive and widely available; however, they cause sedative and cardiovascular negative effects due to poor receptor selectivity. Therefore, second-generation antihistamines were developed to reduce adverse effects while retaining efficacy. There are fewer clinical trials in children than adults, therefore, efficacy and safety data is limited, particularly in children under 6 years, highlighting the need to generate these data in young children with AR. Fexofenadine, a highly selective second-generation antihistamine, effectively alleviates symptoms of AR, is non-sedating due to decreased blood–brain barrier permeability, and is devoid of cardiovascular side effects. Importantly, fexofenadine relieves the ocular symptoms of allergic conjunctivitis, which occur concomitantly with AR, improving quality of life. Overall, fexofenadine displays a favorable safety profile and results in greater treatment satisfaction in children compared with other second-generation antihistamines. This review aimed to evaluate and compare the safety and efficacy of fexofenadine with other available first- and second-generation antihistamines in children with AR.

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“…Unlike other H 1 receptor blockers, levocetirizine cannot penetrate the blood–brain barrier, which contributes to the weak central inhibitory effect. Although levocetirizine is well tolerated, some adverse effects were reported in patients under therapy with levocetirizine 3–5. Most of the adverse effects of levocetirizine were dose-dependent.…”

Section: Introductionmentioning

confidence: 99%

<p>The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers</p>

Cheng¹,

Lin²,

Guo³

et al. 2019

DDDT

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PurposeThe aim of this study is to assess the bioequivalence of a new generic formulation and the branded formulation of levocetirizine dihydrochloride in healthy Chinese volunteers under fasting and fed conditions, and food-intake effect on the pharmacokinetic properties is also evaluated.Patients and methodsVolunteers were randomly allocated into two groups to receive a single oral dose of generic formulation and branded formulation under fasting or fed conditions, respectively. Blood samples were collected at designated time points. Plasma concentrations of levocetirizine were determined by UFLC-MS/MS. Safety evaluations were carried out through the study. The main pharmacokinetic parameters of the two formulations of levocetirizine were calculated using non-compartmental analysis incorporated in WinNonlin® 7.0 software.ResultsForty-nine volunteers were enrolled; 46 completed the studies. Under fasting and fed conditions, the 90% confidence intervals for the geometric mean of generic/branded ratios were in the range of 94.75–107.24% and 99.98–114.69% for the maximum observed concentration, and 97.13–102.50% and 98.36–103.98% for the area under the concentration–time curve. As a result of food intake before administration, the reduced rate and extent of absorption of levocetirizine were observed. Both formulations were generally well tolerated, with no serious adverse reactions reported.ConclusionThe two formulations demonstrated essentially identical pharmacokinetic profiles and were all well within the FDA/CFDA bioequivalence standards. Meanwhile, food intake can delay the absorption rate and reduced the bioavailability of levocetirizine in healthy Chinese volunteers.

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Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies

Abstract: Levocetirizine has modest sedative effects with a risk ratio of 1.67 when compared with placebo. The sedative effects observed for levocetirizine are not different from other second-generation antihistamines.

Cited by 30 publications

References 50 publications

Antihistamine effects and safety of fexofenadine: a systematic review and Meta-analysis of randomized controlled trials

Antihistamine effects and safety of fexofenadine: a systematic review and Meta-analysis of randomized controlled trials

Fexofenadine: review of safety, efficacy and unmet needs in children with allergic rhinitis

<p>The Effect Of Food On The Pharmacokinetic Properties And Bioequivalence Of Two Formulations Of Levocetirizine Dihydrochloride In Healthy Chinese Volunteers</p>

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