Plasma levels of antiprogestin RU 486 following oral administration to non-pregnant and early pregnant women

Swahn, Marja‐Liisa; Wang, G.; Aedo, A.-R.; Cekan, S.Z.; Bygdeman, M.

doi:10.1016/0010-7824(86)90056-9

Cited by 29 publications

(13 citation statements)

References 7 publications

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“…Various studies [8,9] have shown that peak serum concentration of mifepristone is more or less invariable for a dose that ranges between 100 mg and 800 mg. On the basis of this fact, 200 mg single dose of mifepristone was used in the study. Vaginal route of misoprostol is more efficacious than oral route at equivalent doses.…”

Section: Discussionmentioning

confidence: 99%

Efficacy of misoprostol administration 24 hours after mifepristone for termination of early pregnancy

Verma

Singh

et al. 2011

Indian J Med Sci

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Section: Discussionmentioning

confidence: 99%

Efficacy of misoprostol administration 24 hours after mifepristone for termination of early pregnancy

Verma

Singh

et al. 2011

Indian J Med Sci

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“…Various studies have shown that peak serum concentration of mifepristone is more or less equal for a dose that ranges between 100mg and 800mg. 7,8 On the basis of this fact 200 mg single dose of mifepristone was used in the study. Various studies reported 95% success rate with vaginal misoprostol compared to the 87% success rate of oral misoprostol at 48 hour interval.…”

Section: Discussionmentioning

confidence: 99%

Effectiveness of evidence based regimen for medical abortion over conventional methods

Gopal

Ganamurali

et al. 2017

Int J Reprod Contracept Obstet Gynecol

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Background: Medical abortion is a means of medical termination of pregnancy by drugs alone. This can be done upto 63 days using mifepristone and misoprostol tablets. For the conventional method, patient has to come to the hospital 3 times. In our study we reduced the interval between the drugs there by reducing the number of hospital visits. The objectives were to study the reduction of induction abortion interval following administration of evidence based regimen and to compare the proportion of patients developing complications in both the groups.Methods: It was a comparative study conducted at Department of Obstetrics and Gynecology, Govermnent MedicalCollege Kottayam, Kerala, India from May 2015 to November 2015.Results: The mean induction abortion interval in experimental group was 14.3 hours and in control group, it was 60.4 hours which was found to be statistically significant. Only 3 patients (7%) of experimental group had side effects whereas 12 patients. (17.4%) had side effects in the control group. Major side effects encountered were severe abdominal pain and severe bleeding per vaginum. Evidence based regimen consist of administration of mifepristone 200mg and vaginal misoprostol 600µg 6 hours later for termination of pregnancy up to 63 days could reduce the induction abortion interval by 46 hours and had less side effects.Conclusions: As it reduces the induction abortion Interval and complications we feel that the evidence based regimen for Medical Termination of Pregnancy is superior to the FDA approved regimen.

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“…After single dose administration of 100 -800 mg, mifepristone exhibited nonlinear kinetics; however concentrations of the metabolites were linear. 31,[35][36][37][38] The same was seen for multiple dose of mifepristone 100 mg or more. 37 When lower concentrations of mifepristone (2-25 mg: single dose and 12.5-50 mg multiple dose) were administered, linear pharmacokinetics was seen.…”

Section: Mifepristonementioning

confidence: 60%

“…During Stage II (Day 15), subjects received a single oral dose of 50 mg of telapristone in the fasting state and followed in the CRU for 72 hours post-dose. Blood samples were taken at the following time points: pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3,5,7,9,12,16,20,24,28,32,36,40,44 3,5,7,9,12,16,20,24,28,32,36,40,44 Inter-individual variability (IIV) of the pharmacokinetic parameters was modeled assuming a log-normal distribution, as follows:…”

Section: Methodsmentioning

confidence: 99%

“…Study ZP-006 was a phase I/II single dose open label parallel study to evaluate the pharmacokinetics and safety profile of telapristone in female patients with mild and moderate renal impairment versus healthy female volunteers.Subjects received a single 50 mg (given as two 25 mg capsules) oral dose of telapristone (fasted). Blood samples were taken at the following time points: pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5,3,5,7,9,12,16,20,24,28,32,36,40,44, and 48 hours post-dose Screening evaluations (renal function impairment test, physical examination, vital signs, laboratory testing, infectious disease, ECG, drug screens and urine pregnancy test) were performed within 21 days prior to treatment. Laboratory assessments (hematology, serum chemistry and urinalysis) were performed at Day 1 (treatment day) and Day 3 (48hours post-dose).…”

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confidence: 99%

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Population pharmacokinetics of telapristone and its active metabolite CDB-4453

Morris¹

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In this thesis, the population pharmacokinetics of telapristone and its active metabolite, CDB-4453 was evaluated using nonlinear mixed effects modeling (NONMEM ® ). A two-compartment (parent) one compartment (metabolite) mixture model with first order absorption and elimination adequately described the pharmacokinetics of telapristone and CDB-4453.For the Phase I/II pharmacokinetic analysis (effect of renal and hepatic impairment), telapristone was rapidly absorbed with an absorption rate constant (Ka) of 1.26 h -1 . Moderate renal impairment resulted in a 74% decrease in Ka. Population estimates for oral clearance (CL/F) for the high and low clearance groups were 11.6 L/h and 3.34 L/h, respectively. Twenty-five percent of the subjects were allocated to the high clearance group. Apparent volume of distribution for the central compartment (V2/F) was 37.4 L, apparent inter-compartmental clearance (Q/F) was 21.9 L/h, and apparent peripheral volume of distribution for the parent (V4/F) was 120 L. The ratio of the fraction of telapristone converted to CDB-4453 to the distribution volume of CDB-4453 (Fmet est ) was 0.20/L and apparent clearance of the metabolite (CLM/F) was 2.43 L/h. For the pharmacokinetic analysis evaluating the effect of food; food decreased the Ka of telapristone (Ka for the fed and fasted state was 0.467 and 5.06 h -1 , respectively). Population estimates of the high and low CL/F groups were 12.0 L/h and 3.15 L/h, respectively. Thirty-one percent of the subjects were allocated to the high clearance group. V2/F, Q/F and V/4 and Fmet est were 52.8 L, 7.53 L/h, 84.8 L and 0.193/L, respectively. CLM/F was 2.10 L/h. An external validation was performed using the final parameter estimates from the pooled pharmacokinetic analysis (effect of renal and hepatic impairment and the effect of food). From this pharmacokinetic analysis, Ka for the fed and fasted state was 0.299 and 2.35 h -1 , respectively. Population estimates for the high and low CL/F groups were 11.6 L/h and 3.22 L/h, respectively. The percentage of subjects allocated to the high clearance group was 29%. V2/F, Q/F, V/4 and Fmet est were 52.8 L, 11.6 L/h and 93.8 L and 0.186/L, respectively. CLM/F was 2.23 L/h. The final model did not meet the requirement for adequate predictability using the external validation dataset. However, the external validation dataset only included samples with limited early time points. Because of the limited sampling times, it is difficult to make a conclusion about the overall adequacy of the model. An external validation dataset with more extensive sampling will be needed in order to better assess the predictability final model. This is the first comprehensive review of the pharmacokinetics of telapristone and CDB-4453. Abstract Approved: ____________________________________ Thesis Supervisor ____________________________________ . Special thanks to Obie Ferguson, for making the "first steps" possible. Last but not least, I want to thank my pillars of strength. To my father, Tyrone "Rock" Morris, thank you for su...

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Plasma levels of antiprogestin RU 486 following oral administration to non-pregnant and early pregnant women

Cited by 29 publications

References 7 publications

Efficacy of misoprostol administration 24 hours after mifepristone for termination of early pregnancy

Efficacy of misoprostol administration 24 hours after mifepristone for termination of early pregnancy

Effectiveness of evidence based regimen for medical abortion over conventional methods

Population pharmacokinetics of telapristone and its active metabolite CDB-4453

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