Urinary excretion of chlorpheniramine and its metabolites in children
The pharmacokinetics and urinary excretion of chlorpheniramine were studied in 11 patients, aged 6-16 years, with allergic rhinitis. In these children, chlorpheniramine had a mean elimination half-life of 13.1 +/- 6.6 h, a mean clearance rate of 7.23 +/- 3.16 mL/min/kg, and a mean apparent volume of distribution of 7.0 +/- 2.8 L/kg. Over 48 h, the recovery in urine was as follows: chlorpheniramine, 11.3 +/- 6.7%; demethylchlorpheniramine , 23.3 +/- 11.1%; and didemethylchlorpheniramine , 9.6 +/- 9.4%. Urine flow rate and urine pH were uncontrolled and ranged from 2.2 to 113.3 mL/h and 5.1-7.9, respectively, over the 48-h period. In some children urine flow rate and pH were constant, while in others there was great variability. When drug and metabolite excretion rates versus both urine flow rates and pH values were analyzed by multiple linear regression, the results were significantly better (p less than or equal to 0.05) than when each factor was analyzed independently. The excretion rate of chlorpheniramine and its two demethylated metabolites decreased as urine pH increased and urine flow rate decreased. This information must be considered in future pharmacokinetic studies of this drug.
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ABSTRACT: Some important facts about the chromatographic separation of a number of selected categories of drugs are summarized. The data refer to the chromatographic method of choice, stationary phase, mobile phase (carrier gas), detection procedure and (where available) method sensitivity. Also, fundamental instrumental parameters, namely injector, column and detector temperature, carrier gas and mobile phase flow-rate and gradient set-up are reported here. In all cases also the source material used for analysis is specified. The data are presented in table form, each table dealing with a particular category of drugs. The following categories of drugs are being dealt with: anthelmintics, antiarteriosclerotics, antibacterials, anticholinergics and cholinergics, anticoagulants, antidiabetics, antiemetics, antimycotics, antihistamines, antimalarials, antiparasitics, antiparkinsonics, antitussives, antiulcer drugs, antiviral compounds, appetite depressants and immunosuppressives.Journal of Chromatography A 06/1985; 340:401-79. DOI:10.1016/0378-4347(85)80203-6 · 4.17 Impact Factor
- Journal of Chromatography A 02/1986; 351(3):580-4. DOI:10.1016/S0021-9673(01)83542-1 · 4.17 Impact Factor
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ABSTRACT: Subsensitivity to H1-receptor antagonists has been attributed to autoinduction of enzyme systems and increased clearance rates during chronic drug administration. We studied the changes in serum half-life values and clearance rates in dogs who were administered hydroxyzine, 0.7 mg/kg, intramuscularly, daily, for 150 days. Pharmacokinetic studies were performed on the first day of drug administration, and on days 30, 60, 90, 120, and 150. The mean serum half-life value on day 30, 60, and 120 was significantly longer (p less than 0.05) than that of 2.4 +/- 0.3 hours obtained on day 1. The mean clearance values obtained on days 30, 60, 90, 120, and 150 were significantly slower (p less than 0.05) than the value of 25.12 +/- 4.13 ml/min/kg obtained on day 1 but were not significantly different from each other. Mean serum hydroxyzine concentrations were often significantly higher on the later study days than on day 1. The mean apparent volume of distribution values obtained on days 30, 60, 90, 120, and 150 did not differ significantly from the value of 5.0 +/- 1.5 L/kg obtained on day 1. This study adds to the mounting evidence that subsensitivity to the effects of an H1-receptor antagonist is not due to autoinduction of enzyme systems, more rapid clearance of the drug, and lower concentrations of the drug in serum and tissue.Journal of Allergy and Clinical Immunology 07/1987; 79(6):928-32. DOI:10.1016/0091-6749(87)90242-9 · 11.48 Impact Factor
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