Evaluation of the relationship between plasma concentrations of en- and zuclomiphene and induction of ovulation in anovulatory women being treated with clomiphene citrate

Ghobadi, Cyrus; Amer, Saad; Lashen, Hany; Lennard, M. S.; Ledger, William; Rostami‐Hodjegan, Amin

doi:10.1016/j.fertnstert.2008.01.058

Cited by 12 publications

(13 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…CC can be detected in the feces for up to 6 weeks. As latest literature showed that the concentration of CC is around 10 -8 -10 -7 M in women given a therapeutic dose of CC [12]. Our results showed that CC acts as antagonist at such a high concentration via ERα and ERβ.…”

Section: Discussionsupporting

confidence: 66%

“…It is possible that the estrogen agonistic activity of CC may not be observed at high concentrations of E2 via ERα. The serum concentration of CC in women given a therapeutic dose of CC is reported to be 10 -9 -10 -7 M [11,12]. In view of this, the present results serve to emphasize that CC elicits both estrogen agonistic and antagonistic activities in the usual clinical contexts.…”

Section: Discussionmentioning

confidence: 53%

See 1 more Smart Citation

Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors .ALPHA.and .BETA.

et al. 2010

View full text Add to dashboard Cite

Section: Discussionsupporting

confidence: 66%

Section: Discussionmentioning

confidence: 53%

Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors .ALPHA.and .BETA.

et al. 2010

View full text Add to dashboard Cite

“…Our data also demonstrated substantial intersubject variability in the amount of exposure to CC isomers, which might explain some of the large variation in the clinical response to the drug. 14,15 Such variation was evident from the mid-cycle LH surge, a physiologic surrogate of imminent ovulation, observed in 2 patients despite the use of subtherapeutic doses (1 single 50-mg dose vs 5 repeated 50-mg doses used in routine protocols). The possibility of a response to such a low dose of CC (equivalent to 10 mg/day in a typical 5-day treatment course) could be predicted from a previous meta-analysis of the cumulative population response rate.…”

Section: Discussionmentioning

confidence: 99%

“…[4][5][6] Furthermore, despite over 45 years of clinical use, there is very limited information on the pharmacokinetics of CC isomers in humans. Early studies with 14 C-labeled CC in healthy humans demonstrated that the drug is well absorbed and excreted principally in the feces. Thus, 50% of the dose was eliminated following oral administration and 37% following intravenous (IV) administration after 5 days.…”

mentioning

confidence: 99%

Single‐Dose Pharmacokinetic Study of Clomiphene Citrate Isomers in Anovular Patients With Polycystic Ovary Disease

Ghobadi

Mirhosseini

Shiran

et al. 2009

The Journal of Clinical Pharma

Self Cite

View full text Add to dashboard Cite

The pharmacokinetics of the zuclomiphene (Zu) and enclomiphene (En) isomers of clomiphene citrate following a single oral dose (50 mg) were characterized for the first time in patients receiving the drug (ie, infertile women with polycystic ovary syndrome). Plasma concentrations of Zu and En were measured in 9 patients from the second day of their menstrual cycle (day 1 of dosing) up to 21 days. The mean (+/- coefficient of variation) of C(max), t(max), and AUC of Zu was 15 +/- 41 ng/mL, 7 +/- 87 h, and 1289 +/- 34 ng/mL.h (AUC(0-456 h)), and that of En was 15 +/- 18 ng/mL, 3 +/- 68 h, and 65 +/- 35 ng/ml.h (AUC(0-72h)), respectively. These parameters appeared to be different for Zu from those reported previously in healthy participants, except for t(max). The pharmacokinetic parameters of En in patients with polycystic ovary syndrome were not generally different from the healthy subjects. The effect of obesity on Zu kinetics was stronger than that on En. The conventional model-dependent pharmacokinetics of clomiphene citrate isomers could not be determined due to a very flat terminal half-life and the long-tailed residence time, signifying the lipophilic nature and potentially extensive distribution of the compound.

show abstract

“…They are effective in both male and female mice [38,174]. However, the therapeutic dose against EBOV cannot be achieved with the oral clomiphene dose used for inducing ovulation in humans [175][176][177]. The therapeutic dose against EBOV with tolerable side effects can be achieved with toremifene at an oral dose used in the human trial for the treatment of advanced carcinoma of the breast [178][179][180][181].…”

Section: (4) Cationic Amphiphilesmentioning

confidence: 99%

Human Ebola virus infection in West Africa: a review of available therapeutic agents that target different steps of the life cycle of Ebola virus

Lai

Cheng

2014

Infect Dis Poverty

View full text Add to dashboard Cite

The recent outbreak of the human Zaire ebolavirus (EBOV) epidemic is spiraling out of control in West Africa. Human EBOV hemorrhagic fever has a case fatality rate of up to 90%. The EBOV is classified as a biosafety level 4 pathogen and is considered a category A agent of bioterrorism by Centers for Disease Control and Prevention, with no approved therapies and vaccines available for its treatment apart from supportive care. Although several promising therapeutic agents and vaccines against EBOV are undergoing the Phase I human trial, the current epidemic might be outpacing the speed at which drugs and vaccines can be produced. Like all viruses, the EBOV largely relies on host cell factors and physiological processes for its entry, replication, and egress. We have reviewed currently available therapeutic agents that have been shown to be effective in suppressing the proliferation of the EBOV in cell cultures or animal studies. Most of the therapeutic agents in this review are directed against non-mutable targets of the host, which is independent of viral mutation. These medications are approved by the Food and Drug Administration (FDA) for the treatment of other diseases. They are available and stockpileable for immediate use. They may also have a complementary role to those therapeutic agents under development that are directed against the mutable targets of the EBOV.Electronic supplementary materialThe online version of this article (doi:10.1186/2049-9957-3-43) contains supplementary material, which is available to authorized users.

show abstract

Evaluation of the relationship between plasma concentrations of en- and zuclomiphene and induction of ovulation in anovulatory women being treated with clomiphene citrate

Cited by 12 publications

References 30 publications

Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors .ALPHA.and .BETA.

Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors .ALPHA.and .BETA.

Single‐Dose Pharmacokinetic Study of Clomiphene Citrate Isomers in Anovular Patients With Polycystic Ovary Disease

Human Ebola virus infection in West Africa: a review of available therapeutic agents that target different steps of the life cycle of Ebola virus

Contact Info

Product

Resources

About