Objectives: To determine the single- and multiple-dose pharmacokinetics of oral thalidomide (200 mg/day, administered for 21 days) and to assess the effects of steady-state plasma concentrations of thalidomide on the single-dose pharmacokinetics of ethinyl estradiol (INN, ethinylestradiol) and norethindrone (INN, norethisterone).
Methods: A randomized, 2-period crossover study was performed in 10 healthy premenopausal female volunteers. The pharmacokinetic profiles of plasma concentrations of thalidomide were evaluated with both noncompartmental and compartmental methods, whereas those of ethinyl estradiol and norethindrone were calculated with noncompartmental methods. The effects of steady-state plasma thalidomide concentrations on the pharmacokinetics of ethinyl estradiol and norethindrone were determined with use of an ANOVA model that included treatment sequence, subject within sequence, period, and treatment as factors.
Results: Thalidomide plasma concentrations were best predicted by a 1-compartment model with first-order absorption and elimination and an absorption time-lag. There were no significant differences between pharmacokinetic parameters for thalidomide after 1 dose and those after 18 consecutive doses. Except for a minor decrease of the elimination rate constant (k(e)) for ethinyl estradiol, coadministration of thalidomide had no significant effects on the pharmacokinetic profiles for either ethinyl estradiol or norethindrone. The change in k(e) for ethinyl estradiol during thalidomide administration was not associated with any alteration in the clearance or elimination half-life for this hormone.
Conclusions: Multiple-dose pharmacokinetics of thalidomide is similar to the single-dose profile. This study did not investigate the efficacy of the 21-day fixed ethinyl estradiol-norethindrone regimen, but the results suggest that thalidomide is unlikely to affect the pharmacokinetics of orally administered hormonal contraceptives.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/S0009-9236(99)70067-6 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Increased ferritin with contraceptives containing ethinyl estradiol drospirenone in polycystic ovary syndrome: a paradox of iron storage and iron deficiency.
Endocrine
December 2024
Division of Endocrinology and Metabolism, Department of Internal Medicine, University of Health Sciences, Kartal Dr. Lutfi Kirdar City Hospital, Kartal, Istanbul, Turkey.
Objectives: The relationship between elevated ferritin levels and metabolic abnormalities in PCOS patients, and whether ferritin is a cause or a consequence, is still debated. This study aimed to evaluate the impacts of the fourth generation combined oral contraceptive containing ethinyl estradiol/drospirenone (EE 30 mcg/DRSP 3 mg), known for its favorable metabolic profile and lower side effect risk, on iron metabolism in PCOS patients, while also exploring the potential relationship between metabolic parameters and iron status.
Methods: The retrospective analysis was conducted on 81 women aged 18-45, diagnosed with PCOS according to the Rotterdam criteria and treated with EE/DRSP for six months.
UPDATE ON MEDICAL TREATMENT OF ENDOMETRIOSIS: NEW DRUGS OR NEW THERAPEUTIC APPROACHES?
Gynecol Obstet Invest
December 2024
Background: No conceptually new drugs for the safe and successful cure of endometriosis are likely to become available soon. Hormonal modulation of ovarian function and suppression of menstruation remain the pillars of disease control. However, existing drugs may be used following novel modalities to limit the consequences of endometriosis progression.
View Article and Find Full Text PDFOral administration of ethinyl estradiol and the brain-selective estrogen prodrug DHED in a female common marmoset model of menopause: Effects on cognition, thermoregulation, and sleep.
Horm Behav
December 2024
Department of Psychological and Brain Sciences, University of Massachusetts Amherst, Amherst, MA, United States of America.
Menopausal symptoms of sleep disturbances, cognitive deficits, and hot flashes are understudied, in part due to the lack of animal models in which they co-occur. Common marmosets (Callithrix jacchus) are valuable nonhuman primates for studying these symptoms, and we examined changes in cognition (reversal learning), sleep (48 h/wk of sleep recorded by telemetry), and thermoregulation (nose temperature in response to mild external warming) in middle-aged, surgically-induced menopausal marmosets studied at baseline, during 3-week phases of ethinyl estradiol (EE, 4 μg/kg/day, p.o.
View Article and Find Full Text PDFSummary: An oral contraceptive pill (OCP)-induced increase in total cortisol lead to reversible suppression of the hypothalamic-pituitary-adrenal (HPA) axis and insulin resistance (IR) in a patient with Addison's disease. We suggest that this might influence the choice of an OCP in such patients. A 20-year-old female was diagnosed with Addison's disease (cortisol: 44 nmol/L, adrenocorticotropic hormone (ACTH): >500 pg/mL) and started on hydrocortisone (HC).
View Article and Find Full Text PDFSmoking and contraception containing ethinylestradiol: A mixed-methods study into women's intentions to quit smoking.
Womens Health (Lond)
December 2024
Student Health Service, University of Amsterdam, Amsterdam, The Netherlands.
Background: Smoking while using contraception containing ethinylestradiol increases the risk of cardiovascular diseases. Therefore, it is especially important to stimulate women who use these contraceptives to quit smoking.
Objectives: This study aimed to examine the role of risk perception and coping in relation to the intention of these women to quit smoking, using the Protection Motivation Theory as the theoretical foundation.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!