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Journal of Clinical Endocrinology & Metabolism Vol. 68, No. 6 1167-1173
doi:10.1210/jcem-68-6-1167
Copyright © 1989 by the Endocrine Society.
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Serum Concentration and Urinary Excretion of the Luteinizing Hormone-Releasing Hormone Agonist Buserelin in Patients with Endometriosis

LUDWIG KIESEL, JÜRGEN SANDOW, KARIN BERTGES, GERTRAUD JERABEKSANDOW, HEIDRUN TRABANT and BENNO RUNNEBAUM

Division of Gynecological Endocrinology (L.K., K.B., B.R.), Department of Obstetrics and Gynecology, University of Heidelberg D-6900 Heidelberg, West Germany
Hoechst AG (J.S., G.J.-S., H.T.) D-6230 Frankfurt 80, West Germany

Address all correspondence and requests for reprints to: Dr. L. Kiesel, Universitats-Frauenklinik, Voss-Strasse 9, D-6900 Heidelberg, West Germany.

We studied the pharmacokinetics of iv and intranasally administered buserelin, a LHRH agonist peptide, in 14 women with endometriosis. Serum and urinary buserelin concentrations were determined by specific RIA (buserelin antiserum AS-639). Intact buserelin and the metabolites in urine were separated by reverse phase high performance liquid chromatography and measured by RIA. The mean serum buserelin concentrations were 101 ± 33 SD) ng/mL 20 min and 1.12 ± 0.12 ng/mL 360 min after its iv injection in 6 women, and the mean elimination half-life between 20 and 360 min was 51 min. In serum, intact buserelin was the main constituent (10 min, 90%; 120 min, 74%; 360 min, 52%), and the major metabolite was the buserelin-(5–9) pentapeptide (10 min, 0.6%; 120 min, 19%; 360 min, 12%). In the urine collected 0–1 h after buserelin administration, intact buserelin was 66% and the 5–9 pentapeptide was 28% of the total excretion. In the urine collected between 6–24 h after buserelin administration, intact buserelin accounted for 67% and the 5–9 pentapeptide for 32% of the total excretion. The urinary buserelin concentration was 1345 ± 156 µg/g creatinine 1 h and 25 ± 5 µg/g creatinine 6–24 h after buserelin administration. Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values; the mean peak LH, FSH, and estradiol values occurred at 180–240 min, 240 min, and 24 h, respectively. In therapeutic studies with buserelin nasal spray in 5 women, serum concentrations of 0.9–1.4 ng/mL were found 15 min after a single dose of 300 ng, intranasally, and the urinary excretion was 2.52–3.68 µg/24 h during daily administration of 3 doses of 300 µg at intervals of 8 h. These results confirm that buserelin is slowly inactivated and remains available to pituitary receptors for a prolonged period after its iv or intranasal administration.

Received June 14, 1988.







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Copyright © 1989 by The Endocrine Society