Clinical Pharmacokinetics of Oral Contraceptive Steroids

@article{Orme1983ClinicalPO,
  title={Clinical Pharmacokinetics of Oral Contraceptive Steroids},
  author={M. L' E. Orme and David Back and Alasdair M. Breckenridge},
  journal={Clinical Pharmacokinetics},
  year={1983},
  volume={8},
  pages={95-136}
}
SummaryOral contraceptive steroids are of 2 types: oestrogens, of which ethinyloestradiol is the most important, and progestagens, of which levonorgestrel and norethisterone are the most commonly used. All these steroids can be measured by a number of analytical techniques but there is little doubt that radioimmunoassay is the most convenient. All the steroids are well absorbed in humans but while levonorgestrel is completely bioavailable, norethisterone has an average bioavailability of 70… Expand
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Clinical Pharmacokinetics of Contraceptive Steroids An Update
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The role of other antibiotics remains controversial but there is probably a group of susceptible women who have lower plasma contraceptive hormone concentrations and experience breakthrough bleeding or pregnancy when given broad spectrum antibiotics. Expand
Pharmacokinetics and pharmacodynamics of oral contraceptive steroids: factors influencing steroid metabolism.
TLDR
It is concluded that ethinyl estradiol and nortestosterone derivatives may inhibit steroid-metabolizing enzymes in the liver, which results in a rise in the serum levels of contraceptive steroids. Expand
Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin.
TLDR
The binding of levonorgestrel and gestodene (the 18-methyl derivative of norethisterone) to sex hormone-binding globulin was much stronger than that of 3-keto-desogestrel, and the interindividual variation in these parameters was comparable with that observed with other contraceptive combinations containing ethinyl estradiol and norehisterone, lev onorgest Rel, or gestodenes. Expand
Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone‐binding globulin
TLDR
The binding of levonorgestrel and gestodene to sex hormone-binding globulin was much stronger than that of 3-keto-desogestrel or norethisterone and the interindividual variation in these parameters was comparable with that observed with other contraceptive combinations containing ethinyl estradiol and norehisterone, levonborgestrel, or gestodenes. Expand
Pharmacology of Contraceptive Steroids
TLDR
The use of 17α-ethynyl estrogens in contraceptive formulations originated by accident and was the basis of oral contraceptive formulations called “sequentials,” which had a brief career in the United States, but were used for a much longer period of time in other parts of the world. Expand
Pharmacokinetics of the contraceptive steroids levonorgestrel and gestodene after single and multiple oral administration to women.
  • W. Kuhnz
  • Medicine
  • American journal of obstetrics and gynecology
  • 1990
TLDR
Computer simulation, based on single-dose pharmacokinetics, allows an estimation of Ethinyl estradiol-induced production of sex hormone-binding globulin seems to be a major factor that contributes to the accumulation of the two progestins in the plasma. Expand
Pharmacokinetic Drug Interactions with Oral Contraceptives
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There is still no firm clinical pharmacokinetic evidence which indicates that blood concentrations of oral contraceptive steroids are altered by antibiotics, and perhaps this should not be a surprise, given that the incidence of the interaction may be very low. Expand
Pharmacokinetics of oestrogens and progestogens.
TLDR
Among the progestogens, the progesterone derivatives have less effects on liver metabolism than the norethisterone derivatives (13-methyl-gonane derivatives and 13-ethyl-gonanes). Expand
The effects of an oral contraceptive containing ethinyloestradiol and norgestrel on CYP3A activity.
TLDR
Concomitant administration of the oral contraceptive, Ovral for 2, 4, or 10 days did not significantly alter the area under the curve, clearance, or half-life of midazolam after either oral or intravenous administration. Expand
Oral Contraceptives
TLDR
It is suggested that all prescribers should remember to ask about OCs when taking a drug history and to consider the possibility of interactions with other drugs, as OCs have been shown to inhibit metabolism of many therapeutic drugs and increase their plasma concentrations. Expand
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