Pharmacokinetics and efficacy of chlorpheniramine in children

Simons, F. Estelle R.; Luciuk, George H.; Simons, Keith J.

doi:10.1016/0091-6749(82)90149-x

Cited by 55 publications

(20 citation statements)

References 5 publications

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“…This lack of effect has been attributed to the high plasma protein binding of desipramine (Boulter et al 1993). The relatively lower plasma protein binding of chlorpheniramine (69-72%) (Simons et al 1982) compared to desipramine may be contributory to its enhancement of the antimalarial effect of chloroquine.…”

Section: Discussionmentioning

confidence: 99%

Enhancement of the antimalarial effect of chloroquine by chloropheniramine in vivo

Sowunmi

Oduola

Ogundahunsi

et al. 1998

Tropical Med Int Health

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SummaryThe efficacy of chloroquine and chloroquine plus chloropheniramine, a histamine H 1 receptor blocker which reverses chloroquine insensitivity in Plasmodium falciparum in vitro, was studied in 96 children with acute symptomatic uncomplicated falciparum malaria. The chloroquine/chloropheniramine combination produced a significantly higher cure rate than chloroquine alone and cured 77% of children with chloroquine treatment failures. Children with chloroquine treatment failure had mean plasma chloroquine concentrations above the minimum therapeutic concentration for the area. Chloroquine concentrations in plasma and red blood cells and ratio of red cell to plasma chloroquine concentrations on days 3 and 7 after initiation of therapy were not significantly different in the two groups. Chloroquine/ chloropheniramine produces a higher cure rate than chloroquine alone and reverses chloroquine insensitivity in Plasmodium falciparum in vivo. It may be a useful way of optimising the antimalarial effect of chloroquine.

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Section: Discussionmentioning

confidence: 99%

Enhancement of the antimalarial effect of chloroquine by chloropheniramine in vivo

Sowunmi

Oduola

Ogundahunsi

et al. 1998

Tropical Med Int Health

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“…We did not measure histamine-induced wheal and flare to evaluate blockade of peripheral H1 receptors by the treatment. However, various studies have shown that both cetirizine 10 mg 35,36 and chlorpheniramine 4 mg 24,37 are effective in suppressing histamine-induced wheal and flare in children. Another potential confounding factor was the different pharmacokinetics of both drugs.…”

Section: E118mentioning

confidence: 99%

Central Nervous System Side Effects of First- and Second-Generation Antihistamines in School Children With Perennial Allergic Rhinitis: A Randomized, Double-Blind, Placebo-Controlled Comparative Study

Chong

Wong

et al. 2004

Pediatrics

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ABSTRACT. Objective. Allergic rhinitis is common and on the rise. Antihistamines are the mainstay of treatment and are the most commonly prescribed drugs in Singapore. Treatment-related sedation and its effect on cognition are a major concern. First-and second-generation antihistamines show varying degrees of sedation, but to date, objective studies in children are lacking. The objective of this study was to assess the sedating effect of cetirizine (second-generation antihistamine) and chlorpheniramine (first-generation antihistamine) compared with placebo using an objective neurophysiological test.Methods. This was a prospective, double-blind, placebo-controlled, randomized, single-dose, 3-way crossover study. Twenty-four children aged 7 to 14 years with allergic rhinitis completed the study. All children were randomly allocated to medication sequences and received 3 different drugs on 3 different days, at least 1 week apart. The P300 event-related potential was used as an objective test of sedation. Subjective assessment was by a visual analog scale.Results. Chlorpheniramine and cetirizine increased P300 latency when compared with baseline. No significant increase was obtained with placebo. The significant increase in P300 latency was not accompanied by significant change in subjective somnolence as measured by the visual analog scale.Conclusion. We have shown that cetirizine has sedative properties in children. The lack of correlation between P300 latency and the visual analog scale indicates that sedation induced by these drugs may not be subjectively noted. Pediatrics 2004;113:e116 -e121. URL: http: //www.pediatrics.org/cgi/content/full/113/2/e116; sedation, cetirizine, chlorpheniramine, P300 event-related potential.ABBREVIATIONS. CNS, central nervous system; ERP, event-related potential; VAS, visual analog scale; Fz , frontal location; Cz, central location; Pz, parietal location; T max , time to peak plasma drug concentration.A llergic rhinitis is on the increase worldwide as well as in Singapore. A 1994 survey showed the prevalence of rhinitis in Singapore children to be at a staggering 44%. 1 In children with allergic rhinitis, inadequate symptom control may contribute to learning impairment; school absences; poor quality of life; and emotional, social, or behavioral disturbances. 2 Oral antihistamines are the mainstay of therapy for allergic rhinitis in children 3 and have been used effectively for managing symptoms of allergic rhinitis for Ͼ50 years. They are the most commonly prescribed drugs among outpatient doctors in the public service in Singapore. 4 The major limitation of the use of first-generation antihistamines is sedation. 3 Being lipophilic molecules, they easily cross the blood-brain barrier and may exacerbate the decrease in cognitive function already experienced by the patient with allergic rhinitis. Sedating antihistamines have been shown to reduce learning performance in children. 5 In contrast, second-generation antihistamines are relatively lipophobic and therefore cross the blood-br...

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“…3 Most of the orally administered H 1 -antihistamines are available in dosage formulations suitable for administration to children and even to infants; however, only 11 of the 40 H 1 -antihistamines have been studied prospectively in children with regard to their pharmacokinetics and pharmacodynamics. [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23] These studies have generally been conducted after administration of a single dose, 5-10,12-20 but 3 studies have been performed at steady state, 11,12,20 and in a few studies, a population pharmacokinetic design [21][22][23] has been used. The clinical pharmacology of a few of the first-generation H 1 -antihistamines, such as chlorpheniramine, brompheniramine, diphenhydramine, and hydroxyzine, was investigated after they had been used in children for several decades.…”

mentioning

confidence: 99%

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

Simons

2005

Journal of Allergy and Clinical Immunology

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Pharmacokinetics and efficacy of chlorpheniramine in children

Cited by 55 publications

References 5 publications

Enhancement of the antimalarial effect of chloroquine by chloropheniramine in vivo

Enhancement of the antimalarial effect of chloroquine by chloropheniramine in vivo

Central Nervous System Side Effects of First- and Second-Generation Antihistamines in School Children With Perennial Allergic Rhinitis: A Randomized, Double-Blind, Placebo-Controlled Comparative Study

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

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