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Drugs of Today (Barcelona, Spain : 1998) Feb 2008Drospirenone 3 mg/ethinyl estradiol 20 microg (24/4) is a new unique oral contraceptive formulation that combines in a novel dosing regimen the lowest dosage of ethinyl... (Review)
Review
Drospirenone 3 mg/ethinyl estradiol 20 microg (24/4) is a new unique oral contraceptive formulation that combines in a novel dosing regimen the lowest dosage of ethinyl estradiol commonly used today with drospirenone, an innovative progestin. Drospirenone is a compound closely resembling progesterone, but with the antimineralocorticoid and antiandrogenic properties of a related therapeutic agent, the diuretic, antihypertensive and androgen receptor antagonist, 17alpha-spironolactone. The prolongation of hormonally active pills in the monthly drospirenone/ethinyl estradiol cycle from 21 days to 24 days, followed by 4 days of inactive pills, is an interesting variant of the recently developed extended pill regimens (1). Recent contraceptive research has focused on improving side effect profiles and providing noncontraceptive health and lifestyle advantages. Many of these benefits are now supported with evidence-based medicine (2). Most available oral contraceptives improve cycle regularity, menstrual pain, excessive menstrual flow and acne. However, weight gain, bloating, food cravings, breast tenderness and mood alterations (especially irritability and depression and the complex of affective, behavioral and somatic symptoms of premenstrual syndrome [PMS] and the severe form of PMS, premenstrual dysphoric disorder [PMDD]) are not generally improved with the traditional oral contraceptive formulations (3). Drospirenone/ethinyl estradiol 24/4 is currently the only hormonally based contraceptive regimen with large, randomized, controlled trials demonstrating efficacy for PMDD. It has received U.S. Food and Drug Administration (FDA) indications not only for the prevention of pregnancy but also for PMDD and for moderate acne vulgaris in women who choose oral contraception for birth control (4, 5).
Topics: Acne Vulgaris; Androstenes; Contraceptives, Oral, Combined; Ethinyl Estradiol; Female; Humans; Premenstrual Syndrome
PubMed: 18389090
DOI: 10.1358/dot.2008.44.2.1191057 -
American Family Physician May 2020
Review
Topics: Contraceptive Devices, Female; Drug Combinations; Ethinyl Estradiol; Female; Humans; Pregnenediones
PubMed: 32412221
DOI: No ID Found -
Current Opinion in Obstetrics &... Dec 2021Combined oral contraceptive pills are among the most widely used contraceptive methods globally. Despite their popularity, the potential risks and side effects can lead... (Review)
Review
PURPOSE OF REVIEW
Combined oral contraceptive pills are among the most widely used contraceptive methods globally. Despite their popularity, the potential risks and side effects can lead to both high discontinuation rates and adverse outcomes including thromboembolic events. The quest for a safer alternative to the traditional ethinyl estradiol/progestin combination has led to the use of newer oestrogens. Ethinyl oestradiol alternatives will be reviewed including the newest option, estetrol, as it enters clinical use.
RECENT FINDINGS
Oestradiol, when combined with a progestin with strong endometrial activity, is a viable alternative to ethinyl estradiol in the form of oestradiol valerate and estradiol, which have been available since 2008 and 2011, respectively. Estetrol is the newest oestrogen available and is found naturally in the foetal liver. Estetrol was approved for use in 2021. All three of these alternatives have high contraceptive efficacy, similar if not improved cycle control and decreased impact on haemostatic factors as compared to ethinyl estradiol.
SUMMARY
Alternatives to ethinyl oestradiol, including the newest option of estetrol, show promise in providing comparable contraceptive efficacy with potentially lower risk of side effects and thromboembolic events.
Topics: Contraception; Contraceptives, Oral, Combined; Endometrium; Estradiol; Estrogens; Ethinyl Estradiol; Female; Humans
PubMed: 34747879
DOI: 10.1097/GCO.0000000000000751 -
British Medical Journal Nov 1948
Topics: Contraceptive Agents, Female; Estradiol Congeners; Estrogens; Ethinyl Estradiol; Female; Humans
PubMed: 18890306
DOI: 10.1136/bmj.2.4583.809 -
IARC Monographs on the Evaluation of... Dec 1979
Review
Topics: Animals; Carcinogens; Chemical Phenomena; Chemistry; Dogs; Ethinyl Estradiol; Female; Guinea Pigs; Haplorhini; Humans; Male; Mice; Pregnancy; Rabbits; Rats; Teratogens
PubMed: 120833
DOI: No ID Found -
Contraception Nov 1978Plasma levels of ethinyl estradiol were measured by radioimmunoassay in five women after oral administration of 30 microgram and of 50 microgram of ethinyl estradiol....
Plasma levels of ethinyl estradiol were measured by radioimmunoassay in five women after oral administration of 30 microgram and of 50 microgram of ethinyl estradiol. Peak levels of ethinyl estradiol were mostly observed within two hours after the tablet intake. The peak concentrations found were 50--90 pg and 95--135 pg for the two doses administered. Twenty-four hours after the administration of the tablets, the plasma concentration of ethinyl estradiol did not exceed the plasma blank values (25 pg/ml) in most women.
Topics: Administration, Oral; Dose-Response Relationship, Drug; Ethinyl Estradiol; Female; Humans; Time Factors
PubMed: 729373
DOI: 10.1016/0010-7824(78)90031-8 -
Clinical and Experimental Obstetrics &... 2010To demonstrate the usefulness of ethinyl estradiol, a drug no longer commercially produced in most countries, in treating various fertility related issues.
PURPOSE
To demonstrate the usefulness of ethinyl estradiol, a drug no longer commercially produced in most countries, in treating various fertility related issues.
METHODS
Twenty to 40 micrograms of ethinyl estradiol can be started on day 2 or 3 of the cycle and combined with exogenous gonadotropin can be useful in improving hostile cervical mucus or inducing ovulation in women with hypergonadotropic amenorrhea. It can be used from the day after stopping clomiphene citrate to help negate the adverse effect of this drug on cervical mucus.
RESULTS
Successful pregnancies have been achieved saving the couple the expense of intrauterine insemination (IUI) or using donor oocytes.
CONCLUSIONS
This drug can be very helpful for those physicians who treat each infertile woman on an individual basis and carefully ascertain the couple's input as to their preferences rather than a "herd" type of medicine.
Topics: Cervix Mucus; Coitus; Ethinyl Estradiol; Female; Follicular Phase; Humans; Infertility, Female; Insemination, Artificial; Luteinization; Ovulation Induction
PubMed: 21355449
DOI: No ID Found -
Contraception May 1998
Review
Topics: Contraceptives, Oral; Desogestrel; Estradiol Congeners; Ethinyl Estradiol; Female; Humans; Patient Satisfaction; Pregnancy; Progesterone Congeners
PubMed: 9673846
DOI: 10.1016/s0010-7824(98)00030-4 -
Journal of Clinical Pharmacology Aug 2023
Topics: Humans; Female; Ethinyl Estradiol; Contraceptives, Oral, Combined; Drug Interactions; Sulfotransferases; Estradiol
PubMed: 36919596
DOI: 10.1002/jcph.2235 -
Gynecologie, Obstetrique & Fertilite Feb 2012Estradiol 17-β, which is the natural estrogen in women, offers an alternative to ethinyl-estradiol to be used in combined oral contraceptives. Thanks to its biochemical... (Comparative Study)
Comparative Study
Estradiol 17-β, which is the natural estrogen in women, offers an alternative to ethinyl-estradiol to be used in combined oral contraceptives. Thanks to its biochemical structure, estradiol has a far lesser impact on the synthesis of hepatic proteins than ethinyl-estradiol, which is likely to result in a better metabolic and vascular profile. However and until lately, the different clinical trials that had investigated estradiol-containing oral contraceptives were limited by bleeding disturbances, with breakthrough and irregular bleeding and higher rates of discontinuation. Development of anti-gonadotropic progestins with a potent endometrial activity is likely to make possible their combination with estradiol in oral contraceptives. The objective of this current review is to provide an overview of the development of combined oral contraceptives containing natural estrogen from the respective biochemical and pharmacological characteristics of ethinyl-estradiol and estradiol.
Topics: Adolescent; Adult; Animals; Contraceptives, Oral, Combined; Estradiol; Ethinyl Estradiol; Female; Humans
PubMed: 22244780
DOI: 10.1016/j.gyobfe.2011.10.009