Ethynodiol Diacetate resources


DRUG INFO
Ethynodiol Diacetate

Drug Name: Ethynodiol Diacetate

Indication: For the prevention of pregnancy in women who elect to use this product as a method of contraception.



Pharmacology: Ethynodiol Diacetate is used as a female contraceptive. Ethynodiol Diacetate is a progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Ethynodiol Diacetate tricks the body processes into thinking that ovulation has already occurred, by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.

Mechanism Of Action: Binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Ethynodiol Diacetate will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge.

Drug Category: Contraceptives, Oral, Synthetic; ATC:G03CA

Brand Names/Synonyms: 8080 C. B.; CCRIS 305; Cervicundin; Continuin; Demulen; Ethinodiol Diacetate; Ethynodiol; Ethynodiol Diacetate; Ethynodiol Diacetate [Progestins]; Ethynodiol Diacetate [Usan]; Etynodiol; Femulen; Luteonorm; Luto-Metrodiol; Metrodiol; Metrodiol Diacetate; Metrulen; Ovulen; Ovulen 50; SC 11800

Dosage Forms: CREAM; LIQUID; OINTMENT; SOLUTION; SUSPENSION; SYRUP

Absorption: Not Available

Interactions: Interactions for Ethynodiol Diacetate: Ethinyl estradiol: Substrate of CYP3A4 (major), 3A5-7 (minor); Inhibits CYP1A2 (weak), 2B6 (weak), 2C19 (weak), 3A4 (weak). Acetaminophen: May increase plasma concentration of synthetic estrogens, possibly by inhibiting conjugation. Combination hormonal contraceptives may also decrease the plasma concentration of acetaminophen. Acitretin: Interferes with the contraceptive effect of microdosed progestin-containing "minipill" preparations. The effect on other progestational contraceptives (eg, implants, injectables) is unknown. Aminoglutethimide: May increase CYP metabolism of progestins leading to possible decrease in contraceptive effectiveness. Use of a nonhormonal contraceptive product is recommended. Antibiotics (ampicillin, tetracycline): Pregnancy has been reported following concomitant use, however, pharmacokinetic studies have not shown consistent effects with these antibiotics on plasma concentrations of synthetic steroids. Use of a nonhormonal contraceptive product is recommended. Anticoagulants: Combination hormonal contraceptives may increase or decrease the effects of coumarin derivatives. Combination hormonal contraceptives may also increase risk of thromboembolic disorders. Anticonvulsants (carbamazepine, felbamate, phenobarbital, phenytoin, topiramate): Increase the metabolism of ethinyl estradiol and/or some progestins, leading to possible decrease in contraceptive effectiveness. Use of a nonhormonal contraceptive product is recommended. Ascorbic acid: Doses of ascorbic acid (vitamin C) 1 g/day have been reported to increase plasma concentration of synthetic estrogens by ~47%, possibly by inhibiting conjugation; clinical implications are unclear. Atorvastatin: Atorvastatin increases the AUC for norethindrone and ethinyl estradiol. Benzodiazepines: Combination hormonal contraceptives may decrease the clearance of some benzodiazepines (alprazolam, chlordiazepoxide, diazepam) and increase the clearance of others (lorazepam, oxazepam, temazepam). Clofibric acid: Combination hormonal contraceptives may increase the clearance of clofibric acid. Cyclosporine: Combination hormonal contraceptives may inhibit the metabolism of cyclosporine, leading to increased plasma concentrations; monitor cyclosporine levels. CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of ethinyl estradiol. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins. Griseofulvin: Griseofulvin may induce the metabolism of combination hormonal contraceptives causing menstrual changes; pregnancies have been reported. Use of barrier form of contraception is suggested while on griseofulvin therapy. Morphine: Combination hormonal contraceptives may increase the clearance of morphine. Non-nucleoside reverse transcriptase inhibitors (NNRTIs): Nevirapine may decrease plasma levels of combination hormonal contraceptives; use of a nonhormonal contraceptive product is recommended. No data for delavirdine; incomplete data for efavirenz. Prednisolone: Ethinyl estradiol may inhibit the metabolism of prednisolone, leading to increased plasma concentrations. Protease inhibitors: Amprenavir, lopinavir, nelfinavir, and ritonavir have been shown to decrease plasma levels of combination hormonal contraceptives; use of a nonhormonal contraceptive product is recommended. Indinavir has been shown to increase plasma levels of combination hormonal contraceptives. No data for saquinavir. Rifampin: Rifampin increases the metabolism of ethinyl estradiol and some progestins (norethindrone) resulting in decreased contraceptive effectiveness and increased menstrual irregularities. Use of a nonhormonal contraceptive product is recommended. Salicylic acid: Combination hormonal contraceptives may increase the clearance of salicylic acid. Selegiline: Combination hormonal contraceptives may increase the serum concentration of selegiline. Theophylline: Ethinyl estradiol may inhibit the metabolism of theophylline, leading to increased plasma concentrations. Tricyclic antidepressants (amitriptyline, imipramine, nortriptyline): Metabolism may be inhibited by combination hormonal contraceptives, increasing plasma levels of antidepressant; use caution. ETHANOL / NUTRITION / HERB INTERACTIONS: Food: CNS effects of caffeine may be enhanced if combination hormonal contraceptives are used concurrently with caffeine. Grapefruit juice increases ethinyl estradiol concentrations and would be expected to increase progesterone serum levels as well; clinical implications are unclear. Herb/Nutraceutical: St John's wort may decrease the effectiveness of combination hormonal contraceptives by inducing hepatic enzymes. Avoid dong quai and black cohosh (have estrogen activity). Avoid saw palmetto, red clover, ginseng.



Chemical IUPAC Name: (3-acetyloxy-17-ethynyl-13-methyl-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)ethanoate

Chemical Formula: C24H32O4

Half Life: Not Available

Drug Type: Approved Drug

# Accession No: APRD00760

CAS Registry Number: 297-76-7



Ethynodiol Diacetate News
(When available)


Crews Persevere Against Sugarloaf Blaze  Jan 9, 2006
HomeTown channel.com, They're also continuin to back-burn within that area. Officials said the smoke has grown incredibly thick from that back-burning. ...

Dietary soy isoflavones inhibit estrogen effects in the ...  16 Jan 2006
News-Medical.net, ...not apply to premenopausal women, who have higher and more dynamic hormone levels, or to women taking combined hormone therapy with an estrogen and a progestin ...

US study to test hormone benefits in younger women  Jan 5, 2006
Hindustan Times, In July 2002, women taking estrogen and progestin were told to visit their doctors and perhaps stop because of the risk of heart attack, stroke and some forms ...

FDA Approves Osteoporosis Indication for Once-a-Week Hormone ...  Jan 4, 2006
PR Newswire (press release), Estrogen/progestin combinations should not be used by women with known or suspected pregnancy, breast cancer, estrogen-dependent neoplasia, undiagnosed ...

Decision Expected Soon on ‘Morning After Pill’ Availability*  Jan 2, 2006
The NewStandard, Made with the hormone progestin*, Plan B prevents pregnancy up to 89 percent of the time if taken within 72 hours of unprotected intercourse. ...

Studies: Pill safe for women with lupus  Dec 20, 2005
Newsday, In Petri's study at 14 US sites, 91 women took estrogen-progestin combination pills, while 92 women in a comparison group got a placebo; all used barrier ...

In this article  Dec 30, 2005
Health24.com, Are receiving oestrogen administration, without progestin. ... Low doses can be used in older women who do not have progestin-related complications. ...

Women with lupus can take 'The Pill'?  Dec 18, 2005
myDNA.com, Petri's study compared women taking estrogen-progestin combination pills to women taking a placebo - all of them used barrier contraceptives as well. ...

Basu: Politics trumps science in stalling on morning-after pill  Jan 4, 2006
DesMoinesRegister.com, ...the process.". Plan B uses a high dose of progestin, a hormone in birth-control pills, to prevent pregnancy after intercourse. It's ...

Earlier hormone therapy trial scared women - but it was wrong!  Dec 19, 2005
News-Medical.net, Then in 2002, women taking estrogen and progestin were advised to stop taking the drug after the Women's Health Initiative (WHI) said a trial of Wyeth's ...

Intake of synthetic hormones affects sex drive in women  Jan 5, 2006
Hindustan Times, MPA is the synthetic progestin used in Prempro, the most widely prescribed hormone replacement therapy in the United States, and in the injectable form of the ...

Bio-identical hormone replacement a new approach  Jan 3, 2006
Wilkes Barre Times-Leader, Hormone replacement therapy _ providing women with estrogen or estrogen and progestin to ease hot flashes and other uncomfortable symptoms of menopause _ has ...

From a single cell to a complete organ  Jan 5, 2006
Ars Technica ...therapy (HRT) was halted prematurely following the shocking findings that patients taking a combination of oestrogen and progestin had significantly higher ...

News Feature: Hormone in the hot seat  Dec 29, 2005
Nature.com (subscription), In 1998, after the WHI was already under way, scientists announced the results of the Heart and Estrogen/Progestin Replacement Study 3 , which specifically ...

Compassion in the ER  Dec 25, 2005
Boston Globe, A form of progestin, one of the hormones found in regular birth control pills, emergency contraception works most often by inhibiting ovulation and/or ...

Consumer Reports Examines Weaknesses of Current Drug-safety System  Dec 27, 2005
Kansas City infoZine, The 12 drugs include: Celecoxib (Celebrex), a pain reliever; Estrogen alone (Premarin and others) or with progestin (Prempro and others) to treat symptoms of ...

Attempts to make morning-after pill more readily available blocked  Dec 26, 2005
Fort Lauderdale Sun Sentinel, The contraceptive -- two tablets containing high doses of progestin, one of the hormones in birth control pills that block ovulation and prevent sperm and egg ...

Plan B questions and answers  Dec 27, 2005
Sun-Sentinel.com, ...sex. It includes two pills containing a high dose. of the hormone progestin, one of the ingredients in birth control pills. Some ...

Long-term Use of Aspirin and Risk of Colorectal Cancer—Reply  Dec 29, 2005
Journal of American Medical Association (subscription), 3. Chlebowski RT, Wactawski-Wende J, Ritenbaugh C, et al. Estrogen plus progestin and colorectal cancer in postmenopausal women. N Engl J Med. ...

Long-term Use of Aspirin and Risk of Colorectal Cancer  Dec 29, 2005
Journal of American Medical Association (subscription), Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial ...

Lupus patients safe to go back on the pill  Dec 19, 2005
News-Medical.net, ...and also found that the flare-up rate and the severity of the flare-ups was the same whether patients got standard birth control pills, a progestin-only pill ...

New research: HRT not bad for health?  Dec 21, 2005
myDNA.com, Klaiber says Prempro combines estrogen and progestin in a daily pill - a regimen that hadn't been associated with heart protection. ...

Three years after HRT findings, navigating menopause has become a ...  Dec 20, 2005
Pittsburgh Post Gazette, National Institute of Health's Women's Health Inititative abruptly stopped part of a federally funded study of the hormones estrogen and progestin -- long the ...

New pill changes perception of birth control  Dec 19, 2005
Hagerstown Morning Herald, ...vagina. The ring stays in place for three weeks, releasing a continuous dose of estrogen and progestin to keep a woman from ovulating. ...

Herbs for menopausal comfort  Dec 17, 2005
Malaysia Star, ...therapy or HRT. HRT involves taking estrogen plus progestin. However, several studies have shown taking HRT has its risks. This is ...

Vitamin D: Dietary Supplement Fact Sheet  Dec 29, 2005
Food Consumer, ...on Hormone Therapy, in American College of Obstetricians and Gynecologists Web site response to the WHI Study Results on Estrogen and Progestin Hormone Therapy ...


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