Doxylamine pharmacokinetics following single dose oral administration in children ages 2–17 years

Balan, Guhan; Thompson, Gary A.; Gibb, Roger; Li, Lijuan; Hull, D; Seeck, Molly

doi:10.1002/jcph.137

Cited by 7 publications

(3 citation statements)

References 8 publications

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“…Following allometric adjustment, no age‐related change in oral clearance was apparent, indicating no maturation effect on diphenhydramine clearance in children 2 years of age or greater. A similar result in children was observed for another OTC antihistamine, doxylamine, where oral clearance after allometric scaling was unrelated to age.…”

Section: Discussionsupporting

confidence: 78%

Single‐Dose Pharmacokinetic Study of Diphenhydramine HCl in Children and Adolescents

Gelotte

Zimmerman

Thompson³

2017

Clinical Pharm in Drug Dev

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Diphenhydramine pharmacokinetics were characterized following a single oral dose in children aged 2 to 17 years using a weight‐ and age‐based dosing schedule with more tiers than the current age‐based dosing schedule recommended by the nonprescription drug monograph. This study was conducted in 42 subjects, aged 2 to 17 years. Doses were based on a weight‐age dosing schedule, ranging from 6.25 to 50 mg. An oral dose was administered with water about 2 hours after a light breakfast. Plasma samples were obtained up to 48 hours after dosing and analyzed for diphenhydramine. Pharmacokinetic parameters were estimated using noncompartmental methods, and the relationship of oral clearance with age was assessed using linear regression. Over an 8‐fold range of doses, Cmax and AUC increased ∼90 % to ∼140% across age groups, with a similar Tmax (1.5 hours). Oral CL/F increased with age, but after allometric scaling, no maturation‐related change in CL/F was apparent. Mild somnolence was the most commonly reported adverse event (95% of the subjects). A weight‐age dosing schedule using an 8‐fold range of doses achieved Cmax and AUC that increased about 2‐fold across age groups. No effect of maturation on CL/F was observed after allometric scaling.

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Section: Discussionsupporting

confidence: 78%

Single‐Dose Pharmacokinetic Study of Diphenhydramine HCl in Children and Adolescents

Gelotte

Zimmerman

Thompson³

2017

Clinical Pharm in Drug Dev

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“…Common side effects may include blurred vision, dizziness or drowsiness and confusion. 5,6 Cases of abuse and dependence, voluntary or involuntary poisoning, and drug facilitated cases have already been reported in the literature. It has been also included in the United Nations Office on Drugs and Crime list of substances found in DFSA cases.…”

Section: Introductionmentioning

confidence: 99%

“…Because of its sedative effect, it is used in the short‐term management of insomnia as well as treatment for upper respiratory tract allergies. Common side effects may include blurred vision, dizziness or drowsiness and confusion 5,6 …”

Section: Introductionmentioning

confidence: 99%

Incorporation of doxylamine and N‐doxylamine‐oxide in human hair and the impact of a permanent oxidative hair dye

Fernández

Wille

Samyn

2022

Drug Testing and Analysis

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Knowledge of the drug incorporation in hair and impact of cosmetic treatments remains essential to correctly interpret forensic cases. The study shows the analysis of doxylamine and doxylamine‐N‐oxide and the evaluation of the relationship between dose and hair concentration and the impact of hair treatment (oxidative dying). The study included (A) three subjects participated to the study: a regular user (Subject 1) and two single‐dose users (Subject 2, 1 single dose; and Subject 3, 2 single doses spaced 5 months apart). Subject 3 applied a permanent oxidative hair dying monthly. (B) A permanent oxidative hair dying was applied twice to the hair collected from Subject 2. (A) The average concentrations in head hair for doxylamine and its N‐doxylamine‐oxide, respectively, were as follows: Subject 1, 1825 pg/mg and 16 pg/mg; Subject 2, 182 and <limit of quantification (LOQ); and Subject 3, Strand 1 (1 month after last single dose]; 1st cm: 367 pg/mg and 22 pg/mg; 2nd cm: 664 pg/mg and 37 pg/mg; 3rd cm 108 pg/mg and 13 pg/mg; 4th cm 13 pg/mg and 7 pg/mg); Strand 2 (5 months after last single dose: <LOQ). (B) The oxidative hair dying increased the concentration of the metabolite from undetected <LOQ up to 79 pg/mg (n = 3, RSD 6%). The concentration of the parent drug decreased from 128 pg/mg to 40 pg/mg (n = 3, RSD 4%). This is the first time the incorporation of doxylamine and its metabolite was evaluated with adequate and controlled information concerning dose and timing of ingestion for the evaluation of their incorporation and the impact of a cosmetic treatment.

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Dosing in Children: A Critical Review of the Pharmacokinetic Allometric Scaling and Modelling Approaches in Paediatric Drug Development and Clinical Settings

2014

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It should be recognized that children are not small adults, hence dosing in children should not be a 'small adult dose'. A mean population dose in all age groups is just an average dose and not necessarily the best or the correct dose for a given patient. The dose of a drug varies from patient to patient and individual adjustment of the dose is always ideal but is not always practical. Theoretically, dose selection in paediatric drug development or clinical settings can be done by using either body weight or the clearance of a drug. Over the years, a lot of approaches have been suggested for the prediction of drug clearance or dose in paediatrics. Although some proposed methods are useful for the prediction of clearance or dose in children, there remains a high degree of uncertainty in the prediction of drug clearance or dose in children. In particular, the prediction of clearance or dose in an individual patient remains highly erratic. This review takes a critical look at these approaches and highlights the application and limitations of these proposed methods.

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Doxylamine pharmacokinetics following single dose oral administration in children ages 2–17 years

Cited by 7 publications

References 8 publications

Single‐Dose Pharmacokinetic Study of Diphenhydramine HCl in Children and Adolescents

Single‐Dose Pharmacokinetic Study of Diphenhydramine HCl in Children and Adolescents

Incorporation of doxylamine and N‐doxylamine‐oxide in human hair and the impact of a permanent oxidative hair dye

Dosing in Children: A Critical Review of the Pharmacokinetic Allometric Scaling and Modelling Approaches in Paediatric Drug Development and Clinical Settings

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