PharmGKB contains no prescribing info for this . Contact us to report known genotype-based dosing guidelines, or if you are interested in developing guidelines.
- Annotation of FDA Label for drospirenone,ethinyl estradiol and CYP2C19
- Annotation of EMA Label for ethinyl estradiol,norelgestromin and F5
- Annotation of HCSC Label for drospirenone,ethinyl estradiol and F5,PROC,PROS1,SERPINC1
- Annotation of HCSC Label for ethinyl estradiol,norelgestromin and F2,F5,MTHFR,PROC,PROS1,SERPINC1
The FDA-approved drug label for drospirenone and ethinyl estradiol (Yaz) notes that in vitro studies showed an inhibitory effect of drospirenone on the turnover of model substrates of CYP1A1, CYP2C9, CYP2C19 and CYP3A4. However, in vivo studies using omeprazole as a marker substrate showed that drospirenone has little propensity to interact to a significant extent with cytochrome P450 enzymes at a clinical dose level.
There's more of this label. Read more.
The EMA European Public Assessment Report (EPAR) for norelgestromin and ethinyl estradiol (Evra) contains information regarding its contraindication in women with known predisposition to venous thromboembolism (including Factor V Leiden, rs6025).
There's more of this label. Read more.
The product monograph for drospirenone and ethinyl estradiol (YAZ) states that the drug is contraindicated in women with Factor V Leiden mutation, antithrombin-III-deficiency, protein C deficiency and protein S deficiency (among other contraindications), due to the risk for arterial or venous thrombosis.
There's more of this label. Read more.
The product monograph for norelgestromin and ethinyl estradiol (EVRA) states that the drug is contraindicated in women with Factor V Leiden mutation, antithrombin-III-deficiency, protein C deficiency, protein S deficiency, hyperhomocysteinaemia due to mutations in the MTHFR gene and prothrombin mutation G20210A (among other contraindications), due to the risk for arterial or venous thrombosis.
There's more of this label. Read more.
PharmGKB contains no Clinical Variants that meet the highest level of criteria.
Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.
The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.
- 17 alpha-Ethinylestradiol
- 17 alpha-Ethynylestradiol
- 17 alpha-Ethynyloestradiol
- Aethinyoestradiol [German]
- Ethinylestradiolum [INN-Latin]
- Etinilestradiol [INN-Spanish]
- ethynyl estradiol
- Diogyn E
- Ethy 11
- Primogyn C
- Primogyn M
- Progynon C
- Progynon M
- Alesse 21 Tablets (Ethinyl Estradiol + Levonorgestrel)
- Alesse 28 Tablets (Ethinyl Estradiol + Levonorgestrel)
- Brevicon (Ethinyl Estradiol + Norethindrone)
- Cyclen (Ethinyl Estradiol + Norgestimate)
- Demulen 30 (Ethinyl Estradiol + Ethynodiol Diacetate)
- Demulen 50 (Ethinyl Estradiol + Ethynodiol Diacetate)
- Diane-35 (Cyproterone Acetate + Ethinyl Estradiol)
- Evra (Ethinyl Estradiol + Norelgestromin)
- Femhrt 1/5 (Ethinyl Estradiol + Norethindrone Acetate)
- Geri Bons Tab (Calcium (Calcium Phosphate (Dibasic)) + Copper + Dl-Methionine + Ethinyl Estradiol + Fatty Acids + Folic Acid + Iodine + Iron Peptonized + Magnesium + Manganese + Methyltestosterone + Nicotinamide + Phosphorus (Calcium Phosphate (Dibasic)) + Pyridoxine Hydrochloride + Thiamine Hydrochloride + Thyroid + Vitamin a + Vitamin B12 + Vitamin B2 + Vitamin D + Vitamin E)
- Geri Tabs (Calcium (Calcium Phosphate (Dibasic)) + Copper Sulfate + Dl-Methionine + Ethinyl Estradiol + Folic Acid + Iodine + Iron Peptonized + Magnesium Oxide + Manganese Sulfate + Methyltestosterone + Nicotinamide + Phosphorus (Calcium Phosphate (Dibasic)) + Pyridoxine Hydrochloride + Thiamine Hydrochloride + Thyroid + Vitamin a + Vitamin B12 + Vitamin B2 + Vitamin D + Vitamin E)
- Lo-Femenal 21 Tablets (Ethinyl Estradiol + Norgestrel)
- Loestrin 1.5/30 21day Pak (Ethinyl Estradiol + Norethindrone Acetate)
- Loestrin 1.5/30 28day Pack (Ethinyl Estradiol + Norethindrone Acetate)
- Marvelon 21 Tab (Desogestrel + Ethinyl Estradiol)
- Marvelon 28 Tab (Desogestrel + Ethinyl Estradiol)
- Min-Ovral 21 (Ethinyl Estradiol + Levonorgestrel)
- Min-Ovral 21 Tab (Ethinyl Estradiol + Levonorgestrel)
- Min-Ovral 28 (Ethinyl Estradiol + Levonorgestrel)
- Min-Ovral 28 Tab (Ethinyl Estradiol + Levonorgestrel)
- Minestrin 1/20 21 (Ethinyl Estradiol + Norethindrone Acetate)
- Minestrin 1/20 28 (Ethinyl Estradiol + Norethindrone Acetate)
- Neo Mens Tab (Ethinyl Estradiol + Ethisterone)
- Nuvaring (Ethinyl Estradiol + Etonogestrel)
- Ortho Tablets (0.5/35, 1/35, 10/11, 7/7/7) (Ethinyl Estradiol + Norethindrone)
- Ortho-Cept Tablets (Desogestrel + Ethinyl Estradiol)
- Ovral 21 Tab (Ethinyl Estradiol + Norgestrel (Norgestrel))
- Ovral 21 Tablets (Ethinyl Estradiol + Norgestrel (Norgestrel))
- Ovral 28 Tablets (Ethinyl Estradiol + Norgestrel (Norgestrel))
- Ovral 28tab (Ethinyl Estradiol + Norgestrel)
- Preven Tablets (Ethinyl Estradiol + Levonorgestrel)
- Select 1/35 (Ethinyl Estradiol + Norethindrone)
- Synphasic 21 Tablets (Ethinyl Estradiol + Norethindrone)
- Synphasic 28 Tablets (Ethinyl Estradiol + Norethindrone)
- Synphasic-28 Tablets (Ethinyl Estradiol + Norethindrone)
- Tri-Cyclen Lo (Ethinyl Estradiol + Norgestimate)
- Tri-Cyclen Tablets - 21-Day (Ethinyl Estradiol + Norgestimate)
- Tri-Cyclen Tablets - 28-Day (Ethinyl Estradiol + Norgestimate)
- Triphasil 21 (Ethinyl Estradiol + Levonorgestrel)
- Triphasil 21 Tab (Ethinyl Estradiol + Levonorgestrel)
- Triphasil 28 (Ethinyl Estradiol + Levonorgestrel)
- Triphasil 28 Tab (Ethinyl Estradiol + Levonorgestrel)
- Triquilar 21 Tab (Ethinyl Estradiol + Levonorgestrel)
- Triquilar 28 Tab (Ethinyl Estradiol + Levonorgestrel)
- Yasmin 21 (Drospirenone + Ethinyl Estradiol)
- Yasmin 28 (Drospirenone + Ethinyl Estradiol)
PharmGKB Accession Id
ORTHO EVRA (norelgestromin/ethinyl estradiol)
ORTHO EVRA is a transdermal contraceptive patch used to prevent ovulation and pregnancy. This medicine combines two types of female hormones, an estrogen (ethinyl estradiol) and a progestin (norelgestromin).
Since ORTHO EVRA® is applied transdermally, hormones from ORTHO EVRA get into the bloodstream and are processed by the body differently than hormones from birth control pills that are taken orally [Articles:17389559, 11849630, 11851637].The contraceptive patch delivers hormones (norelgestromin (NGMN) and ethinyl estradiol (EE)) transdermally into systemic circulation, bypassing the first-pass metabolism (via the gastrointestinal tract and/or liver). Patients will be exposed to about 60% more estrogen with ORTHO EVRA® than with a typical birth control pill containing 35 micrograms of estrogen (http://www.orthoevra.com/isi.html; [Article:16368722]). The increased estrogen concentration may increase the risk of venous thromboembolism and other estrogen-related adverse effects, although the degree of risk is still unclear. Norelgestromin undergoes hepatic metabolism and metabolites include norgestrel, which is highly bound to SHBG, and various hydroxylated and conjugated metabolites. Ethinyl estradiol is also metabolized to various hydroxylated products by cytochrome P450 (CYP) 2B1, 1A1, 1A2, 3A4, 3A5, 3A7 and 2C9 [Articles:9625734, 12865317, 14623547, 16024767, 14657266, 15784278]. Estradiol and its metabolites further undergo sulfation by sulfotransferases (SULTs) [Articles:12922923, 15860265, 10963623] and glucuronidation by glucoronyltransferases (UGTs) [Articles:17374650, 11457662, 9848110]. Studies showed that ethinyl estradiol inactivated purified, reconstituted rat hepatic cytochrome P450 (P450) 2B1 and human P450 2B6 in a mechanism-based manner [Article:11805216]. For graphical description of estrogen metabolism, please see estrogen metabolism pathway (https://www.pharmgkb.org/do/serve?objId=PA145011118&objCls=Pathway).
The ORTHO EVRA Patch is worn on the body to prevent pregnancy by delivering continuous levels of hormones (progestin and estrogen, respectively) into the bloodstream through the skin. Although the primary mechanism of action is inhibition of ovulation, other alterations occur, including changes in the cervical mucus (which increase the difficulty of sperm entry into the uterus) and the endometrium (which reduce the likelihood of implantation) [Articles:11849630, 11851637]. Norelgestromin is the active progestin largely responsible for the progestational activity that occurs in women following application of ORTHO EVRA®. Both progestins and estrogens exert their effect through binding to their receptors. Estrogens elicit their effects via estrogen receptors (ER/ESR1 and ESR2) [Articles:16876190, 18854778, 17986456, 17584965, 17673513, 14668813, 16033996]. Progestin affects both menstruation and gestation via the progesterone receptor (PGR) [Articles:17013809, 18321550]. The combination of an estrogen with a progestin in ORTHO EVRA suppresses the hypothalamic-pituitary system, decreases the secretion of gonadotropin-releasing hormone (GNRH1) from the hypothalamus and blunts the preovulatory LH (luteinizing hormone (LHB/CGA)) surge [Articles:17013809, 19434887]. In vitro studies showed that NGMN is a very potent inhibitory agent for sulfatase activity (STS) in the hormone-dependent breast cancer cells [Article:12711003]. The use of ORTHO EVRA Patch also increased the serum concentrations of estrogen-sensitive hepatic proteins such as sex hormone binding globulin (SHBG), corticosteroid binding globulin (SERPINA6/CBG), thyroid-binding globulin (SERPINA7/TBG), and affected biomarkers of vascular disease risk (increases in C-reactive protein (CRP) and fibrinogen (FGA, FGB), declines in free and total protein S (PROS1) and antithrombin (SERPINC1))[Articles:16982228, 18238963].
Serious as well as minor side effects have been reported with the use of the ORTHO EVRA Patch. "Serious risks, which can be life threatening, include blood clots, stroke and heart attacks and are increased if you smoke cigarettes. Cigarette smoking increases the risk of serious cardiovascular side effects, especially if you are over 35. Women who use the Patch are strongly advised not to smoke. Some women should not use the Patch, including women who have blood clots, certain cancers, a history of heart attack, blood clots, or stroke, as well as those who are or may be pregnant" (http://www.orthoevra.com/isi.html).
Publications related to ethinyl estradiol: 8
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- DG Dosing Guideline information is available
- DL Drug Label information is available
- CA High-level Clinical Annotation is available
- VA Variant Annotation is available
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- PW Pathway is available
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These are trials that mention ethinyl estradiol and are related to either pharmacogenetics or pharmacogenomics.
No NURSA datasets available.