|Trade names||Beyaz, Safyral|
Ethinylestradiol/drospirenone/levomefolic acid (trade names Beyaz, Safyral) is an oral contraceptive developed by Bayer. Its contraceptive ingredients are ethinylestradiol, an estrogen and drospirenone, a synthetic progestogen, making it a combined oral contraceptive (COC). It also contains folate as levomefolic acid calcium salt, to lower the risk of complications such as fetal neural tube defects should the drug fail as contraceptive. The drug was approved by the United States Food and Drug Administration on 24 September 2010.
- 1 Dosage and administration
- 2 Indications and usage
- 3 Side effects
- 4 Interactions
- 5 Mechanism of action
- 6 News
- 7 See also
- 8 References
Dosage and administration
Each box, as supplied by the manufacturer, contains 3 blister packs of 28 tablets packaged in individual boxes. Each blister pack of 28 tablets contains 24 pink active pills containing drospirenone 3 mg, ethinylestradiol 20 mcg, and levomefolate calcium 0.451 mg and four light orange inactive pills containing of levomefolate calcium 0.451 mg. Take one tablet by mouth at the same time every day. The failure rate may increase when pills are missed or taken incorrectly. Single missed pills should be taken as soon as remembered. It is important to know that when experiencing stomach upset in the form of diarrhea or vomiting (within 3–4 hours of taking), backup contraception methods should be utilized to account for possible absorption failure.
Indications and usage
Studies have shown its uses to be oral contraception, lessening premenstrual dysphoric disorder (PMDD), and treatment of moderate acne in women over 14 years of age who choose an oral contraceptive for contraception. Five clinical trials were carried out for these labeled uses, “including a one-year contraceptive efficacy study, two 3-cycle studies in women with premenstrual dysphoric disorder (PMDD), and two 6-cycle studies in women with moderate acne.” The drug combination will also increase folate levels due to its extra ingredient, levomefolic calcium. This is equivalent to folic acid 0.4 mg and will help prevent neural tube defects in case of accidental pregnancy while taking, or shortly after stopping the drug.
Adverse reactions commonly reported by combined oral contraceptive users are irregular uterine bleeding, nausea, breast tenderness, and headache.
Substances diminishing the efficacy of COCs
Drugs or herbal products that induce certain enzymes, including CYP3A4, may decrease the effectiveness of COCs or increase breakthrough bleeding. Some drugs or herbal products that may decrease the effectiveness of hormonal contraceptives include phenytoin, barbiturates, carbamazepine, bosentan, felbamate, griseofulvin, oxcarbazepine, rifampicin, topiramate and products containing St. John’s wort. Interactions between oral contraceptives and other drugs may lead to breakthrough bleeding and/or contraceptive failure.” “Use an alternative method of contraception or a back-up method when enzyme inducers are used with COCs, and to continue back-up contraception for 28 days after discontinuing the enzyme inducer to ensure contraceptive reliability.CYP3A4 inhibitors such as itraconazole or ketoconazole may increase plasma hormone levels.”
HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors
‘Significant changes (increase or decrease) in the plasma levels of estrogen and progestin have been noted in some cases of co-administration with HIV protease inhibitors or with non-nucleoside reverse transcriptase inhibitors.”
“There have been reports of pregnancy while taking hormonal contraceptives and antibiotics, but clinical pharmacokinetic studies have not shown consistent effects of antibiotics on plasma concentrations of synthetic steroids.”
Effects of combined oral contraceptives on other drugs
“COCs containing EE may inhibit the metabolism of other compounds. COCs have been shown to significantly decrease plasma concentrations of lamotrigine. This may reduce seizure control; therefore, dosage adjustments of lamotrigine may be necessary.”
Mechanism of action
Combined oral contraceptives reduce the risk of pregnancy primarily by inhibiting ovulation. This product combines drospirenone, an analogue of spironolactone that has both antimineralocorticoid and antiandrogenic effects with an estrogen plus folate supplementation. Levomefolate calcium 0.451 mg is included for reducing the risk of neural tube defects in case of accidental pregnancy.
It is the first and only birth control approved by the FDA for four indications: pregnancy prevention, symptomatic treatment of premenstrual dysphoric disorder, treatment of moderate acne, and raising folate levels to prevent neural tube defects for women who chose an oral contraceptive method.
- "FDA approves combination contraceptive containing a folate". Food and Drug Administration. 24 September 2010. Retrieved 6 February 2011.
- "BEYAZ." MPR - Obstetrician & Gynecologist Edition (2010): A.5. Academic Search Complete. EBSCO. Web. 11 Oct. 2011.
- Bayer HealthCare Pharmaceuticals Inc. Beyaz Prescribing Information. Wayne, NJ, 2010. PDF.
- "Bayer Receives Approval for Beyaz in the U S." ENP Newswire [United Kingdom] 27 Sept. 2010. Factiva. Web. 5 Oct. 2011