Levocetirizine: Pharmacokinetics and pharmacodynamics in children age 6 to 11 years

Simons, F. Estelle R.; Simons, Keith J.

doi:10.1016/j.jaci.2005.04.010

Cited by 54 publications

(41 citation statements)

References 29 publications

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“…For example, it has been reported that sedative effects were not observed in school-aged children after administration of terfenadine (Simons et al 1996), fexofenadine (Simons et al 2003), and levocetirizine (Simons and Simons 2005). Moreover, Stevenson et al (2002) found that there were no adverse effects on behavioral or learning processes associated with prolonged use of cetirizine in young children even though this drug causes mild sedative effects in that population (Ng et al 2004).…”

Section: Discussionmentioning

confidence: 99%

Effects of sedative and nonsedative antihistamines on prefrontal activity during verbal fluency task in young children: a near-infrared spectroscopy (NIRS) study

et al. 2009

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Section: Discussionmentioning

confidence: 99%

Effects of sedative and nonsedative antihistamines on prefrontal activity during verbal fluency task in young children: a near-infrared spectroscopy (NIRS) study

et al. 2009

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“…A comparison of the elimination half-lives of levocetirizine and other commonly employed H 1 -antihistamines suggests that levocetirizine appears to be eliminated faster than the other H 1 -antihistamines also in this age group [60,61]. Moreover, as shown in younger children aged 1–2 years [57], the mean oral clearance rate of 0.82 ml/min/kg and the mean volume of distribution (0.4 l/kg) were also found to be low in this patient cohort [66] and were lower than those for desloratadine [61]. Assessment of histamine-induced wheal and flare responses further demonstrated that levocetirizine 5 mg significantly inhibited both histamine-induced wheals and flares from pre-dose baseline values from 1 to 28 h, with mean maximum 97% inhibition of wheals occurring from 2 to 10 h after dosing and mean maximum 93% inhibition of flares occurring from 2 to 24 h after dosing.…”

Section: Studies Investigating the Efficacy And Safety Of Levocetirizmentioning

confidence: 59%

“…The pharmacologic profile of levocetirizine has been investigated in children aged 6–11 years [66]. Fourteen children weighing 20–40 kg and suffering from mild AR were each administered a single dose of levocetirizine 5 mg tablet following an overnight fast.…”

Section: Studies Investigating the Efficacy And Safety Of Levocetirizmentioning

confidence: 99%

Evidence for Clinical Safety, Efficacy, and Parent and Physician Perceptions of Levocetirizine for the Treatment of Children with Allergic Disease

Пампура¹,

Papadopoulos

Špičák

et al. 2011

Int Arch Allergy Immunol

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Allergic rhinitis (AR) and chronic idiopathic urticaria (CIU) are highly burdensome diseases, which are increasing in prevalence, especially in the paediatric population. Despite the availability of a large number of medications for treatment of AR and CIU, their use in children has primarily been based on data obtained from a limited number of clinical trials in children and/or testing in adults. The H₁-antihistamines have traditionally been used as first-line treatment for the relief of both AR and CIU symptoms in children. The first-generation H₁-antihistamines are associated with marked adverse effects such as sedation, sleepiness/drowsiness as well as difficulties in learning and cognitive processing; thus, they are recommended for limited or discontinued use in children with AR or CIU. In contrast, second-generation H₁-antihistamines are more adapted for the use in children with AR and CIU due to better safety profiles. However, only a limited number of trials with these agents have been conducted and generally, data from well-designed trials in children are lacking. Levocetirizine is one of the most extensively investigated H₁-antihistamines for its pharmacologic properties, safety, efficacy as well as overall global satisfaction in children aged 2–12 years. Levocetirizine is the only H₁-antihistamine launched in the 21st century shown to lack clinically relevant adverse effects on physical and psychomotor development or routine laboratory tests over a long-term period of 18 months in 1- to 3-year-old children predisposed to development of allergic disease. Available data suggest that levocetirizine is a suitable treatment option for AR and CIU in children aged 6 months to 12 years.

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“…It is categorized in the second generation of oral non-sedative antihistamines for the treatment of mild-to-moderate seasonal allergic rhinitis and perennial allergic rhinitis (1,2) and is also considered as a first-line agent for treatment of chronic idiopathic urticarial (3). Structurally, levocetirizine belongs to the diphenylpiperazine class of compounds with selective H 1 -antagonist effects.…”

Section: Levocetirizine (2-[2-[4-[(r)-(4-chlorophenyl)phenylmethyl]-pmentioning

confidence: 99%

Determination of Levocetirizine in Human Plasma by LC–MS-MS: Validation and Application in a Pharmacokinetic Study

Wichitnithad

Jithavech²,

Sanphanya³

et al. 2015

Journal of Chromatographic Science

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A fast and simple sample cleanup approach for levocetirizine in human was developed using protein precipitation coupled with LC-MS-MS. Samples were treated with 6% trichloroacetic acid in water prior to LC-MS-MS analysis. Chromatographic separation was performed on a reverse phase column with an isocratic mobile phase of acetonitrile and 10 mM ammonium formate pH 3.5 (80:20, v/v) at a flow rate of 1.0 mL/min. The run time was 3.5 min. Mass parameters were optimized to monitor transitions at m/z [M+H] + 389.0→201.0 for levocetirizine and m/z [M+H] + 375.3→201.0 for hydroxyzine as internal standard. The lower limit of quantification and the dynamic range were 1.00 and 1.00-500 ng/mL, respectively. Linearity was good for intraday and interday validations (r 2 ≥ 0.995). The mean recoveries were 59 and 69% for levocetirizine and hydroxyzine, respectively. Matrix effect was acceptable with %CV < 15. Hemolytic effect was negligible. Levocetirizine was stable in human plasma for 27 h at room temperature (25°C), for 16 weeks frozen at −70°C, 4 weeks frozen at −20°C, for 24 h in an autosampler at 15°C and for three freeze/thaw cycles. The validated method was applied in a pharmacokinetic study to determine the concentration of levocetirizine in plasma samples. The study provides a fast and simple bioanalytical method for routine analysis and may be particularly useful for bioequivalence studies.

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Levocetirizine: Pharmacokinetics and pharmacodynamics in children age 6 to 11 years

Cited by 54 publications

References 29 publications

Effects of sedative and nonsedative antihistamines on prefrontal activity during verbal fluency task in young children: a near-infrared spectroscopy (NIRS) study

Effects of sedative and nonsedative antihistamines on prefrontal activity during verbal fluency task in young children: a near-infrared spectroscopy (NIRS) study

Evidence for Clinical Safety, Efficacy, and Parent and Physician Perceptions of Levocetirizine for the Treatment of Children with Allergic Disease

Determination of Levocetirizine in Human Plasma by LC–MS-MS: Validation and Application in a Pharmacokinetic Study

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