Pharmacokinetics of levonorgestrel in the rat
Contraception (Impact Factor: 2.34). 08/1984; 30(1):81-8. DOI: 10.1016/0010-7824(84)90081-7
Levonorgestrel was administered intravenously as a bolus to adult female rats and blood samples were collected at various time intervals. Serum concentrations of levonorgestrel were measured by radioimmunoassay. Analysis of data for two- and three-compartment open models indicated that in the rat, as in the human and the rabbit, a tri-exponential equation provided a better fit of the data. The half-lives for the alpha, beta and gamma phases were 10.1 min, 42.7 min and 23.1 hours, respectively. These values were closer to those reported for women than were the half-lives reported for the rabbit. The alpha and the beta phases appeared to last for 51 min and 1.3 hours, respectively, and the gamma phase was longer than 45 hours.
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ABSTRACT: Adult female rats were given a single, subcutaneous injection of 8, 16 or 32 micrograms of levonorgestrel (LNG). Blood samples were collected at various time intervals and serum concentrations of LNG were determined by radioimmunoassay. The patterns of temporal decline in LNG concentrations in the three dose groups indicated that the pharmacokinetics of LNG during the post-absorptive, rapid-elimination (beta) phase in the rat may be dose-dependent. Half-life, Co and AUC increased with the dose and -beta decreased as the dose increased. Mathematical relationships have been presented which can be used to predict the four parameters as well as concentrations of LNG at any given time after subcutaneous administration during the beta-phase for a given dose in the range of 8-32 micrograms. Significance of dose-dependent pharmacokinetic studies is discussed.Contraception 01/1985; 30(6):599-605. DOI:10.1016/0010-7824(84)90009-X · 2.34 Impact Factor
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ABSTRACT: The synthesis of the 6 alpha-carboxymethylmercapto BSA and homologous histamine conjugate of D-(-)-norgestrel 17 beta-cyclopentanecarboxylate is reported. Using the BSA conjugate as an immunogen for the development of antibody in the rabbit and the 125I-histamine conjugate as the radioligand, a radioimmunoassay (RIA) for the ester was developed. Serum profiles of the free alcohol and ester were determined following IV or IM injection in macaques. Peak values for the ester (about 12 ng/mL) were observed 2 min following an IV bolus of 0.5 mg in one rhesus monkey. Blood levels dropped rapidly within the first 30 min and were barely detectable at 24 h. Serum levels of the free alcohol rose to a peak at 30 min and then declined slowly to very low values by 24 h. Following IM injection of 20 mg in cynomolgus monkeys, peak levels of the ester were observed within a few days while the free alcohol reached a maximum about day 30. Serum concentrations of D-(-)-norgestrel had fallen to about 0.4 ng/mL 160 days post-injection when levels of the ester fell below 0.2 ng/mL.Steroids 07/1986; 48(1-2):27-45. DOI:10.1016/0039-128X(86)90039-5 · 2.64 Impact Factor
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