Pharmacokinetics of 10 mg of mifepristone
The results of several randomized studies have verified the efficacy of 10 mg mifepristone in emergency contraception. In the present study we characterized the pharmacokinetics of 10 mg mifepristone. Eight healthy female volunteers received a single oral dose of mifepristone on the day 10 or 11 of...
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Published in | Contraception (Stoneham) Vol. 68; no. 6; pp. 427 - 429 |
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Main Authors | , , , , |
Format | Journal Article Conference Proceeding |
Language | English |
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Elsevier Inc
01.12.2003
Elsevier Science |
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Abstract | The results of several randomized studies have verified the efficacy of 10 mg mifepristone in emergency contraception. In the present study we characterized the pharmacokinetics of 10 mg mifepristone. Eight healthy female volunteers received a single oral dose of mifepristone on the day 10 or 11 of their menstrual cycle. Blood samples were collected at 0, 1, 2, 4 and 8 h, daily for the next 6 days and on day 10 after mifepristone. Mifepristone concentrations were determined by radioimmunoassay preceded by column chromatography. A peak level of 1.41 ± 0.31 μmol/L (mean ± SD) was measured at 1 h. Individual elimination phase half-lives varied from 15.3 to 26.8 h, the mean (± SD) value being 19.6 ± 4.50 h. Serum mifepristone concentrations exceeded 10 nmol/L in all volunteers for an average of 4.9 days. The pharmacokinetic data on 10 mg mifepristone are in line with previous pharmacokinetic and clinical data, and encourage further development of the 10-mg dose in emergency contraception. |
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AbstractList | The results of several randomized studies have verified the efficacy of 10 mg mifepristone in emergency contraception. In the present study we characterized the pharmacokinetics of 10 mg mifepristone. Eight healthy female volunteers received a single oral dose of mifepristone on the day 10 or 11 of their menstrual cycle. Blood samples were collected at 0, 1, 2, 4 and 8 h, daily for the next 6 days and on day 10 after mifepristone. Mifepristone concentrations were determined by radioimmunoassay preceded by column chromatography. A peak level of 1.41 ± 0.31 μmol/L (mean ± SD) was measured at 1 h. Individual elimination phase half-lives varied from 15.3 to 26.8 h, the mean (± SD) value being 19.6 ± 4.50 h. Serum mifepristone concentrations exceeded 10 nmol/L in all volunteers for an average of 4.9 days. The pharmacokinetic data on 10 mg mifepristone are in line with previous pharmacokinetic and clinical data, and encourage further development of the 10-mg dose in emergency contraception. The results of several randomized studies have verified the efficacy of 10 mg mifepristone in emergency contraception. In the present study we characterized the pharmacokinetics of 10 mg mifepristone. Eight healthy female volunteers received a single oral dose of mifepristone on the day 10 or 11 of their menstrual cycle. Blood samples were collected at 0, 1, 2, 4 and 8 h, daily for the next 6 days and on day 10 after mifepristone. Mifepristone concentrations were determined by radioimmunoassay preceded by column chromatography. A peak level of 1.41 +/- 0.31 micromol/L (mean +/- SD) was measured at 1 h. Individual elimination phase half-lives varied from 15.3 to 26.8 h, the mean (+/- SD) value being 19.6 +/- 4.50 h. Serum mifepristone concentrations exceeded 10 nmol/L in all volunteers for an average of 4.9 days. The pharmacokinetic data on 10 mg mifepristone are in line with previous pharmacokinetic and clinical data, and encourage further development of the 10-mg dose in emergency contraception. |
Author | Ranta, Sirpa Oehler, Joachim Leminen, Riikka Heikinheimo, Oskari von Hertzen, Helena |
Author_xml | – sequence: 1 givenname: Riikka surname: Leminen fullname: Leminen, Riikka organization: Department of Obstetrics and Gynecology, University of Helsinki, P.O. Box 140, SF-00029, HUS, Helsinki, Finland – sequence: 2 givenname: Sirpa surname: Ranta fullname: Ranta, Sirpa organization: Institute of Biomedicine, University of Helsinki, Helsinki, Finland – sequence: 3 givenname: Helena surname: von Hertzen fullname: von Hertzen, Helena organization: World Health Organisation, Department of Reproductive Health Research, Geneva, Switzerland – sequence: 4 givenname: Joachim surname: Oehler fullname: Oehler, Joachim organization: The Concept Foundation, Bangkok, Thailand – sequence: 5 givenname: Oskari surname: Heikinheimo fullname: Heikinheimo, Oskari email: oskari.heikinheimo@helsinki.fi organization: Department of Obstetrics and Gynecology, University of Helsinki, P.O. Box 140, SF-00029, HUS, Helsinki, Finland |
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Cites_doi | 10.1016/S0140-6736(02)11767-3 10.1016/S0010-7824(03)00077-5 10.1093/oxfordjournals.humrep.a136283 10.1016/S0029-7844(02)02006-9 10.3109/07853899309147861 10.1016/S0010-7824(86)80017-8 10.1016/S0010-7824(96)00193-X 10.1016/S0140-6736(98)07190-6 10.1016/S0010-7824(01)00184-6 |
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Keywords | Inhibition of ovulation Dose–response relationships Radioimmunoassay Emergency contraception Human Healthy subject Dose-response relationships Low dose Single dose Oral administration Antihormone Abortifacient Antiprogesterone Female Mifepristone Pharmacokinetics |
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References_xml | – volume: 54 start-page: 229 year: 1996 end-page: 234 ident: BIB4 article-title: Pharmacokinetics of mifepristone after low oral doses publication-title: Contraception contributor: fullname: Lähteenmäki – volume: 25 start-page: 71 year: 1993 end-page: 76 ident: BIB7 article-title: Dose-response relationship of RU 486 publication-title: Ann Med contributor: fullname: Kekkonen – volume: 100 start-page: 65 year: 2002 end-page: 70 ident: BIB2 article-title: Emergency contraception with mifepristone and levonorgestrel publication-title: Obstet Gynecol contributor: fullname: Gemsell-Danielsson – volume: 10 start-page: 2270 year: 1995 end-page: 2276 ident: BIB10 article-title: Failure of oestrogen induced luteinizing hormone surge in women treated with mifepristone (RU 486) every day for 30 days publication-title: Hum Reprod contributor: fullname: Cameron – volume: 360 start-page: 1803 year: 2002 end-page: 1810 ident: BIB3 article-title: Low dose mifepristone and two regimens of levonorgestrel for emergency contraception publication-title: Lancet contributor: fullname: Ding – volume: 63 start-page: 111 year: 2001 end-page: 121 ident: BIB9 article-title: Mechanism of action of hormonal preparations used for emergency contraception publication-title: Contraception contributor: fullname: Durand – volume: 353 start-page: 697 year: 1999 end-page: 702 ident: BIB1 article-title: Comparison of three single doses of mifepristone as emergency contraception publication-title: Lancet – volume: 34 start-page: 613 year: 1986 end-page: 624 ident: BIB5 article-title: Quantitation of RU 486 in human plasma by HPLC and RIA after column chromatography publication-title: Contraception contributor: fullname: Lähteenmäki – volume: 360 start-page: 1803 year: 2002 ident: 10.1016/S0010-7824(03)00181-1_BIB3 article-title: Low dose mifepristone and two regimens of levonorgestrel for emergency contraception publication-title: Lancet doi: 10.1016/S0140-6736(02)11767-3 contributor: fullname: von Hertzen – ident: 10.1016/S0010-7824(03)00181-1_BIB8 doi: 10.1016/S0010-7824(03)00077-5 – volume: 10 start-page: 2270 year: 1995 ident: 10.1016/S0010-7824(03)00181-1_BIB10 article-title: Failure of oestrogen induced luteinizing hormone surge in women treated with mifepristone (RU 486) every day for 30 days publication-title: Hum Reprod doi: 10.1093/oxfordjournals.humrep.a136283 contributor: fullname: Baird – volume: 100 start-page: 65 year: 2002 ident: 10.1016/S0010-7824(03)00181-1_BIB2 article-title: Emergency contraception with mifepristone and levonorgestrel publication-title: Obstet Gynecol doi: 10.1016/S0029-7844(02)02006-9 contributor: fullname: Marions – volume: 25 start-page: 71 year: 1993 ident: 10.1016/S0010-7824(03)00181-1_BIB7 article-title: Dose-response relationship of RU 486 publication-title: Ann Med doi: 10.3109/07853899309147861 contributor: fullname: Heikinheimo – volume: 34 start-page: 613 year: 1986 ident: 10.1016/S0010-7824(03)00181-1_BIB5 article-title: Quantitation of RU 486 in human plasma by HPLC and RIA after column chromatography publication-title: Contraception doi: 10.1016/S0010-7824(86)80017-8 contributor: fullname: Heikinheimo – volume: 54 start-page: 229 year: 1996 ident: 10.1016/S0010-7824(03)00181-1_BIB4 article-title: Pharmacokinetics of mifepristone after low oral doses publication-title: Contraception doi: 10.1016/S0010-7824(96)00193-X contributor: fullname: Kekkonen – volume: 353 start-page: 697 year: 1999 ident: 10.1016/S0010-7824(03)00181-1_BIB1 article-title: Comparison of three single doses of mifepristone as emergency contraception publication-title: Lancet doi: 10.1016/S0140-6736(98)07190-6 – ident: 10.1016/S0010-7824(03)00181-1_BIB6 – volume: 63 start-page: 111 year: 2001 ident: 10.1016/S0010-7824(03)00181-1_BIB9 article-title: Mechanism of action of hormonal preparations used for emergency contraception publication-title: Contraception doi: 10.1016/S0010-7824(01)00184-6 contributor: fullname: Croxatto |
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Snippet | The results of several randomized studies have verified the efficacy of 10 mg mifepristone in emergency contraception. In the present study we characterized... |
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SubjectTerms | Adult Biological and medical sciences Contraceptives, Postcoital, Synthetic - administration & dosage Contraceptives, Postcoital, Synthetic - pharmacokinetics Dose-Response Relationship, Drug Dose–response relationships Emergency contraception Female Genital system. Reproduction Humans Inhibition of ovulation Medical sciences Mifepristone - administration & dosage Mifepristone - pharmacokinetics Pharmacology. Drug treatments Radioimmunoassay |
Title | Pharmacokinetics of 10 mg of mifepristone |
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