The Effect of Food on the Bioavailability of Norethindrone and Ethinyl Estradiol from Norethindrone Acetate/Ethinyl Estradiol Tablets Intended for Continuous Hormone Replacement Therapy

@article{Boyd2003TheEO,
  title={The Effect of Food on the Bioavailability of Norethindrone and Ethinyl Estradiol from Norethindrone Acetate/Ethinyl Estradiol Tablets Intended for Continuous Hormone Replacement Therapy},
  author={Rebecca A. Boyd and E A Zegarac and Michael A. Eldon},
  journal={The Journal of Clinical Pharmacology},
  year={2003},
  volume={43}
}
As part of the development of a combination product containing norethindrone acetate and low‐dose ethinyl estradiol for continuous hormone replacement therapy in postmenopausal women, a study was conducted to determine the effect of a high‐fat meal on the bioavailability of norethindrone and ethinyl estradiol from tablets containing 1 mg norethindrone acetate/10 μg ethinyl estradiol. Eighteen healthy postmenopausal women participated in an open‐label, single‐dose, randomized, three‐way… Expand
Bioequivalence of Two Oral Contraceptive Drugs Containing Ethinylestradiol and Gestodene in Healthy Female Volunteers
TLDR
The bioavailability and bioequivalence of two different film coated tablets containing ethinylestradiol and gestodene formulations are bioequivalent in their rate and extent of absorption. Expand
Bioequivalence of of Two Oral Contraceptive Drugs Containing Ethinylestradiol and Drospirenone in Healthy Female Volunteers
The bioavailability and bioequivalence of two different film coated tablets containing ethinylestradiol and drospirenone were investigated in 36 healthy female volunteers after oral single-doseExpand
Effect of exenatide on the pharmacokinetics of a combination oral contraceptive in healthy women: an open-label, randomised, crossover trial
TLDR
The observed reduction in Cmax is likely of limited importance given the unaltered oral contraceptive bioavailability and trough concentrations; however, for oral medications that are dependent on threshold concentrations for efficacy, such as contraceptives and antibiotics, patients should be advised to take those drugs at least 1 hour before exenatide injection. Expand
Simultaneous determination of norethindrone and ethinyl estradiol in human plasma by high performance liquid chromatography with tandem mass spectrometry--experiences on developing a highly selective method using derivatization reagent for enhancing sensitivity.
TLDR
A liquid chromatographic method with tandem mass spectrometric detection (LC-MS/MS) for the simultaneous analysis of norethindrone, and ethinyl estradiol, was developed and validated over the concentration range of 50-10000pg/ml and 2.5-500PG/ml, and could be used for pharmacokinetic and drug-drug interaction studies in human subjects. Expand
Pharmacology of estrogens and progestogens: influence of different routes of administration
  • H. Kuhl
  • Medicine
  • Climacteric : the journal of the International Menopause Society
  • 2005
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormoneExpand
A UPLC-MS/MS Method for Therapeutic Drug Monitoring of Etonogestrel
TLDR
A rapid, sensitive, and robust ultra performance liquid chromatography-tandem mass spectometry (UPLC-MS/MS) method for the quantification of ENG in serum that is useful to study the progestin's pharmacokinetics and inform physicians about successful implantation or potential failure to remove a subdermal device is developed. Expand
Sex hormones and related compounds, including hormonal contraceptives
TLDR
This chapter discusses sex hormones and related compounds including hormonal contraceptives, and Diethylstilbestrol has clearly been shown to cause primary vaginal carcinoma in the second generation and tumors continue to occur in women in middle age. Expand
Pharmaco- and toxicokinetics of selected exogenous and endogenous estrogens: A review of the data and identification of knowledge gaps
TLDR
A review of the current state of the science on the potential for EACs to interfere with endocrine activity, factors which contribute to endocrine-related clinical outcomes, and existing knowledge gaps is assessed. Expand
Pharmacotherapeutic options for the treatment of menopausal symptoms
TLDR
The pharmacokinetics and pharmacodynamics of hormonal (androgens, estrogens, progestogens, tibolone, TSEC, SERMs) and non-hormonal treatments for menopausal symptoms are described and essential clinical trial data in humans is reported. Expand
Development and validation of a HPLC method for determination of levonorgestrel and quinestrol in rat plasma.
TLDR
A sensitive reverse-phase high-performance liquid chromatography with ultraviolet detection (RP-HPLC-UV) method for quantification of levonorgestrel and quinestrol in rat plasma has been developed and can be applied to the further pharmacokinetic study of lev onorgest Rel and qu in rat Plasma. Expand
...
1
2
3
...

References

SHOWING 1-10 OF 24 REFERENCES
The Bioavailability of Desogestrel/Ethinyl Estradiol Tablets Relative to the Oral Solution
TLDR
The results of these studies demonstrated that the mean relative bioavailabilities of DSG and EE from the combination tablet were 100% and 93%, respectively, and that ofEE from the EE tablet was 99%; therefore the performance of both tablet formulations was near optimal. Expand
The effect of varying low-dose combinations of norethindrone acetate and ethinyl estradiol (femhrt®) on the frequency and intensity of vasomotor symptoms
TLDR
There were significant reductions in hot flash frequency and severity with continuous treatment with norethindrone acetate and ethinyl estradiol combinations and the opportunity for lower-dose options of a new continuous-combined hormone replacement therapy provides therapeutic flexibility for women who are recently menopausal. Expand
Kinetics of norethindrone in women; II. Single‐dose kinetics
TLDR
The bioavailability of norethindrone was significantly less (between 32% and 70%) than that after 1 mg N acetate and 50 µg EE2 explaining, at least in part, the lower than expected plasma concentrations in women on long‐term treatment with 3 mg Nacetate and50 µgEE2. Expand
Identification and measurement by gas chromatography-mass spectrometry of norethindrone and metabolites in human urine and blood.
Abstract Urinary metabolites of norethindrone (17β-hydroxy-17α-ethynyl-4-estren-3-one) in the free, sulfate, and glueuronide fractions were identified by gas chromatography-mass spectrometryExpand
The comparative effect on bone density, endometrium, and lipids of continuous hormones as replacement therapy (CHART study). A randomized controlled trial.
TLDR
Daily treatment with NA-EE2 was well tolerated and protected the endometrium from EE2-induced proliferation and hyperplasia and the overall effect of NA- EE2 treatments on lipid measures was favorable. Expand
The clinical pharmacology of oral contraceptive steroids.
TLDR
The total dose level cannot be reduced much further without impairing the contraceptive efficacy of the drug, and it is likely that the majority of women are not at risk of contraceptive failure when using a broad spectrum antibiotic at the same time as the OC. Expand
Pharmacokinetics of norethindrone: effect of particle size.
TLDR
It was found that the smaller the particle size of norethindrone (NET) administered, the higher was the plasma NET level obtained and there is no evidence that such faster dissolution leads to a significant difference in efficacy. Expand
Can grapefruit juice influence ethinylestradiol bioavailability?
TLDR
It is shown that grapefruit juice increases the bioavailable amount of EE2, and a possible explanation may be that grape fruit juice inhibits the metabolic degradation ofEE2. Expand
Influence of absorbable and nonabsorbable lipids and lipidlike substances on drug bioavailability
TLDR
There were no statistical differences observed in the absorption of the various drugs evaluated in this study when administered with olestra, triglyceride oil, or water, except that the time to peak concentration of diazepam was significantly longer with the triglycerideOil than with olESTra or water. Expand
Pharmacology of the Contraceptive Steroids
TLDR
The present work focuses on the pharmacokinetics and intermediate metabolism of steroid hormones and antagonists in the female breast of Joseph W. Goldzieher, and their effects on the skin and immune system. Expand
...
1
2
3
...