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Titolo:
Pharmacokinetic and pharmacodynamic modeling of cetrorelix, an LH-RH antagonist, after subcutaneous administration in healthy premenopausal women
Autore:
Nagaraja, NV; Pechstein, B; Erb, K; Klipping, C; Hermann, R; Niebch, G; Derendorf, H;
Indirizzi:
Univ Florida, Coll Pharm, Dept Pharmaceut, Gainesville, FL 32610 USA Univ Florida Gainesville FL USA 32610 armaceut, Gainesville, FL 32610 USA ASTA Med AG, Corp Res, Frankfurt, Germany ASTA Med AG Frankfurt GermanyASTA Med AG, Corp Res, Frankfurt, Germany Dinox Bv, Nijmegen, Netherlands Dinox Bv Nijmegen NetherlandsDinox Bv, Nijmegen, Netherlands
Titolo Testata:
CLINICAL PHARMACOLOGY & THERAPEUTICS
fascicolo: 6, volume: 68, anno: 2000,
pagine: 617 - 625
SICI:
0009-9236(200012)68:6<617:PAPMOC>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
GONADOTROPIN-RELEASING-HORMONE; OVARIAN STIMULATION; SURGE; SINGLE; GNRH; DECONVOLUTION; INJECTION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Derendorf, H Univ Florida, Coll Pharm, Dept Pharmaceut, POB 100494, Gainesville, FL 32610 USA Univ Florida POB 100494 Gainesville FL USA 32610 FL 32610 USA
Citazione:
N.V. Nagaraja et al., "Pharmacokinetic and pharmacodynamic modeling of cetrorelix, an LH-RH antagonist, after subcutaneous administration in healthy premenopausal women", CLIN PHARM, 68(6), 2000, pp. 617-625

Abstract

Purpose. The purpose of this study was the development of pharmacokinetic and pharmacodynamic models for the luteinizing hormone (LH) suppression andsubsequent shift in LH surge and follicle-stimulating hormone by cetrorelix in women. Background. Cetrorelix is a potent luteinizing hormone-releasing hormone (LH-RH) antagonist and is used for the prevention of the premature ovulationindicated by an LH surge in in vitro fertilization. The pharmacokinetic and pharmacodynamic relationship for the suppression and the shift in the LH surge has not yet been established. Methods. In a placebo-controlled study, single subcutaneous doses of 1, 3,and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle. Cetrorelix, LH, follicle-stimulating hormone, estradiol, and progesterone were determined. Results. Cetrorelix pharmacokinetics were described by a 2-compartment model with a terminal half-life of 56.9 +/- 27.1 hours. Mean shift in LH surgewas by 4.1, 7.5, and 9.3 days with the 1-, 3-, and 5-mg doses, respectively. An indirect response sigmoid E-max model was developed for the suppression of LH and the shift in the LH surge. The inhibitory concentration of 50%(for LH suppression) and median effective concentration (for surge shift) estimates were 3.6 ng/mL and 1.6 ng/mL, respectively. The suppression of follicle-stimulating hormone was described by a similar E-max model, with an inhibitory concentration of 50% of 7.25 ng/mL. Conclusions. A pharmacokinetic and pharmacodynamic model was developed forthe transient initial suppression of LH and the subsequent shift in the LHsurge after 3 single subcutaneous doses of cetrorelix without ovarian stimulation. A separate model was developed for the suppression of follicle-stimulating hormone by cetrorelix. The shift in the LH surge could be adequately described by the model.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 07:30:40