Pharmacokinetics of Intravenous Chlorpheniramine in Children

Thompson, John A.; Bloedow, Duane C.; Leffert, Fred

doi:10.1002/jps.2600701127

Cited by 23 publications

(5 citation statements)

References 10 publications

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“…When clearance values were calculated using a fraction of the dose absorbed of 0.6 (9). the mean value (4.32 f 1.92 mL/min/kg) was not significantly different (I, = 0.05) from the value of5.39 f 1.45 mL/min/kg obtained from a previous study in children (8) in which thc dose was given intravenously. It wassignificantlydifferent (I, 5 0.05) from thc clearance rate of 7.92 f 1.81 mL/min/kg found in one other study in adults (7).…”

Section: Resultsmentioning

confidence: 66%

“…Serum chlorpheniramine concentrations are shown in Table I. The results of pharmacokinetic studies for each subject are shown in Table 11. The mean elimination half-life for I of 13.1 f 6.6 h obtained in the study (15) was not significantly different (p = 0.05) from the mean value of 9.6 f 3.6 h found in seven children given an intravenous dose of this drug (8). In adults, a wide range of elimination half-life values have been reported following oral (4-6) and intravenous (7,9) (6) were not significantly different (p = 0.05).…”

Section: Resultsmentioning

confidence: 66%

“…Recently, the development of sensitive, specific HPLC (2) and GLC-MS (3) assays have facilitated bioavailability (4-6) and pharmacokinetic (7)(8)(9)) studies with chlorpheniramine. The metabolism of chlorpheniraminc has been investigated in dogs (10) and humans ( 1 I), and the effect of induced, constant urine pH and flow rate on the rate of excretion of the unchanged drug has been evaluated (12).…”

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confidence: 99%

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Urinary Excretion of Chlorpheniramine and Its Metabolites in Children

Simons

Luciuk

et al. 1984

Journal of Pharmaceutical Sciences

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Section: Resultsmentioning

confidence: 66%

Section: Resultsmentioning

confidence: 66%

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confidence: 99%

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Urinary Excretion of Chlorpheniramine and Its Metabolites in Children

Simons

Luciuk

et al. 1984

Journal of Pharmaceutical Sciences

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“…Monitoring salivary levels may be feasible with chlorpheniramine. Further studies on a larger number of subjects are needed to resolve some of the following questions before recommendations for modifying current clinical regimens can be given: (1) correlation between antihistaminic effect and serum and tissue concentration; (2) magnitude of hepatic first-pass effect; (3) influence of age, sex, race, genetic factors, smoking, states of health, types and quantities of food and liquids, acid-base balance, and concomitant administration of other drugs; and (4) kinetic and biological difference between the syrup, tablet, controlled-release, and injection formulations.R eferences…”

Section: Discussionmentioning

confidence: 99%

“…Thompson suggests that younger children may require slightly larger doses than older children. 1 Clinical pharmacokinetics in geriatric patients have not been investigated.…”

Section: Clinical Application Of Pharmacokinetic Parametersmentioning

confidence: 99%

Clinical Pharmacokinetics of Chlorpheniramine

Rumore¹

1984

Drug Intelligence & Clinical Pharmacy

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The clinical pharmacokinetics of chlorpheniramine are reviewed. Recent studies have established that the half-life of chlorpheniramine is longer than previously reported. Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. The half-life is increased in the presence of renal dysfunction and decreased in children. The exact mechanism of the presystemic first-pass elimination and the effects of dose levels on the process presently are unclear. Biopharmaceutical and pharmacokinetic studies after single or multiple doses in humans reveal wide interindividual variations in pharmacokinetics. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine. Attention is brought to major issues that need further clarification to optimize drug therapy with this antihistamine. The use of pharmacokinetic parameters of chlorpheniramine for clinical application is discussed.

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Diphenhydramine: Pharmacokinetics and Pharmacodynamics in Elderly Adults, Young Adults, and Children

Simons

Watson

Martin

et al. 1990

The Journal of Clinical Pharma

101

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The pharmacokinetics and pharmacodynamics of the H1-receptor antagonist diphenhydramine were studied in 21 fasting subjects divided into three age groups: elderly, (mean age 69.4 +/- 4.3 years), young adults, (mean age 31.5 +/- 10.4 years), and children, (mean age 8.9 +/- 1.7 years). All subjects ingested a single dose of diphenhydramine syrup 1.25 mg/kg, in mean doses of 86.0 +/- 7.3 mg, 87.9 +/- 12.4 mg, and 39.5 +/- 8.4 mg, respectively. Blood samples were collected hourly for 6 hours, every 2 hours until 12 hours, at 24 hours, and, in the adults, up to 72 hours after diphenhydramine administration. At these times, histamine skin tests were performed and wheal and flare areas were computed. The mean serum elimination half-life values for diphenhydramine differed significantly in elderly adults, young adults, and children, with values of 13.5 +/- 4.2 hours, 9.2 +/- 2.5 hours, and 5.4 +/- 1.8 hours being found respectively in each age group. Clearance rates for diphenhydramine also differed significantly with age, being 11.7 +/- 3.1 mL/min/kg in elderly adults, 23.3 +/- 9.4 mL/min/kg in young adults and 49.2 +/- 22.8 mL/min/kg in children. Diphenhydramine produced a maximum wheal suppression of 39.6 +/- 22.5% and a maximum flare suppression of 46.5 +/- 32.1% at 5 and 6 hours respectively in the elderly; a maximum wheal suppression of 45.5 +/- 25.0% and a maximum flare suppression of 53.4 +/- 16.9% at 6 and 4 hours respectively in young adults; and a maximum wheal suppression of 68.4 +/- 10.2% and a maximum flare suppression of 87.2 +/- 4.2% at 2 hours in children.

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Pharmacokinetics of Intravenous Chlorpheniramine in Children

Cited by 23 publications

References 10 publications

Urinary Excretion of Chlorpheniramine and Its Metabolites in Children

Urinary Excretion of Chlorpheniramine and Its Metabolites in Children

Clinical Pharmacokinetics of Chlorpheniramine

Diphenhydramine: Pharmacokinetics and Pharmacodynamics in Elderly Adults, Young Adults, and Children

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