Drospirenone/ethinylestradiol/levomefolic acid
Drospirenone/ethinylestradiol/levomefolic acid (EE/DRSP/LMF), sold under the brand name Beyaz among others, is a combination of ethinylestradiol (EE), an estrogen, drospirenone (DRSP), a progestogen, antimineralocorticoid, and antiandrogen, and levomefolic acid (LMF), a form of vitamin B9, which is used as a birth control pill to prevent pregnancy in women. The formulation contains folate as the calcium salt of levomefolic acid to lower the risk of complications such as fetal neural tube defects should the medication fail as a form of birth control.[3] EE/DRSP/LMF was approved for use by the US Food and Drug Administration (FDA) in September 2010.[3][4]
 Ethinylestradiol | |
 Drospirenone | |
| Combination of | |
|---|---|
| Drospirenone | Progestogen; Progestin; Antimineralocorticoid; Antiandrogen |
| Ethinylestradiol | Estrogen |
| Levomefolic acid | Vitamin |
| Clinical data | |
| Trade names | Beyaz, Safyral,[1] Tydemy[2] |
| Other names | EE/DRSP/LMF; EE/DRSP/THF; EE/DRSP/THFA; EE/DRSP/FH4; EE/DRSP/VB9 |
| MedlinePlus | a601050 |
| License data | |
| Routes of administration | By mouth |
| Legal status | |
| Legal status |
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| Identifiers | |
| ChemSpider |
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| KEGG | |
| (verify) | |
In 2021, it was the 277th most commonly prescribed medication in the United States, with more than 800,000 prescriptions.[5][6]
Medical uses
editStudies 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.[7] 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.”[8] 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.[7]
Dosage and use
editEach box, as supplied by the manufacturer, contains three 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.[7][9]
One tablet is taken by mouth at the same time every day. The failure rate may increase when pills are missed or taken incorrectly.[9] Single missed pills should be taken as soon as remembered.[9] 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.[9]
Side effects
editAdverse reactions commonly reported by combined oral contraceptive users are irregular uterine bleeding, nausea, breast tenderness, and headache.[9]
Interactions
editDecreased efficacy
editDrugs 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.”[9] “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.”[9]
Antivirals
edit‘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.”[9]
Antibiotics
edit“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.”[9]
Others
edit“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.”[9]
Pharmacology
editCombined oral contraceptives reduce the risk of pregnancy primarily by inhibiting ovulation.[7] 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.[7]
History
editEE/DRSP/LMF 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.[8]
See also
editReferences
edit- ^ "Safyral- drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium kit". DailyMed. 8 August 2017. Retrieved 14 August 2020.
- ^ "Tydemy- drospirenone, ethinyl estradiol and levomefolate calcium and levomefolate calcium kit". DailyMed. 26 November 2019. Retrieved 14 August 2020.
- ^ a b "FDA approves combination contraceptive containing a folate" (Press release). U.S. Food and Drug Administration (FDA). 24 September 2010. Retrieved 6 February 2011.
- ^ "Drug Approval Package: Beyaz (drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium) NDA #022532". U.S. Food and Drug Administration (FDA). 4 April 2011. Retrieved 14 August 2020.
"Application Number: 022532sOrig1s000" (PDF) (Summary Review). Center for Drug Evaluation and Research. 24 September 2010. - ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Drospirenone; EthinylEstradiol; Levomefolate - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- ^ a b c d e "Beyaz." MPR - Obstetrician & Gynecologist Edition (2010): A.5. Academic Search Complete. EBSCO. Web. 11 October 2011.
- ^ a b "Bayer Receives Approval for Beyaz in the U S." ENP Newswire [United Kingdom] 27 September 2010. Factiva. Web. 5 October 2011
- ^ a b c d e f g h i j "Beyaz- drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium kit". DailyMed. 2 January 2019. Retrieved 14 August 2020.
