Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Drospirenone/ethinylestradiol/levomefolic acid: Difference between pages

{{Short description|Pharmaceutical combination}}

{{Use dmy dates|date=January 2024}}

| verifiedrevid = 470456527

| drug_name =

| type = combo

| image = Ethinylestradiol.svg

| width = 235

| alt =

| caption = Ethinylestradiol

| image2 = Drospirenone.svg

| width2 = 235

| alt2 =

| caption2 = Drospirenone

| component1 = Drospirenone

| class1 = [[Progestogen (medication)|Progestogen]]; [[Progestin]]; [[Antimineralocorticoid]]; [[Antiandrogen]]

| component2 = Ethinylestradiol

| class2 = [[Estrogen (medication)|Estrogen]]

| tradename = Beyaz, Safyral,<ref>{{cite web | title=Safyral- drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium kit | website=DailyMed | date=8 August 2017 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=97563516-306a-4e17-9690-edbda49ecd83 | access-date=14 August 2020}}</ref> Tydemy<ref>{{cite web | title=Tydemy- drospirenone, ethinyl estradiol and levomefolate calcium and levomefolate calcium kit | website=DailyMed | date=26 November 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9b1a133d-2ab0-44a7-8c3c-5ac0f8551813 | access-date=14 August 2020}}</ref>

| DailyMedID = Drospirenone, ethinyl estradiol and levomefolate calcium

| routes_of_administration = [[Oral administration|By mouth]]

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| ChemSpiderID = None

| UNII_Ref =

| UNII =

| KEGG = D12130

| synonyms = EE/DRSP/LMF; EE/DRSP/THF; EE/DRSP/THFA; EE/DRSP/FH4; EE/DRSP/VB9

'''Drospirenone/ethinylestradiol/levomefolic acid''' ('''EE/DRSP/LMF'''), sold under the brand name '''Beyaz''' among others, is a [[combination drug|combination]] of [[ethinylestradiol]] (EE), an [[estrogen (medication)|estrogen]], [[drospirenone]] (DRSP), a [[progestogen (medication)|progestogen]], [[antimineralocorticoid]], and [[antiandrogen]], and [[levomefolic acid]] (LMF), a form of [[vitamin B9|vitamin B₉]], which is used as a [[birth control pill]] to prevent [[pregnancy]] in women. The formulation contains [[folate]] as the [[calcium]] [[salt (chemistry)|salt]] of levomefolic acid to lower the risk of [[complications of pregnancy|complications]] such as [[fetal]] [[neural tube defects]] should the medication fail as a form of birth control.<ref name="FDA - 24 Sep 2010 - FDA approves combination contraceptive containing a folate">{{cite press release |url=https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm227237.htm|title=FDA approves combination contraceptive containing a folate|date=24 September 2010|publisher=U.S. [[Food and Drug Administration]] (FDA) |accessdate=6 February 2011}}</ref> EE/DRSP/LMF was approved for use by the US [[Food and Drug Administration]] (FDA) in September 2010.<ref name="FDA - 24 Sep 2010 - FDA approves combination contraceptive containing a folate"/><ref>{{cite web | title=Drug Approval Package: Beyaz (drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium) NDA #022532 | website=U.S. [[Food and Drug Administration]] (FDA) | date=4 April 2011 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022532_beyaz_toc.cfm | access-date=14 August 2020}}<br/>{{cite web | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022532Orig1s000SumR.pdf |type=Summary Review |date=24 September 2010 |title=Application Number: 022532sOrig1s000 |publisher=Center for Drug Evaluation and Research}}</ref>

In 2021, it was the 277th most commonly prescribed medication in the United States, with more than 800,000 prescriptions.<ref>{{cite web | title=The Top 300 of 2021 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=14 January 2024 | archive-date=15 January 2024 | archive-url=https://web.archive.org/web/20240115223848/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Drospirenone; EthinylEstradiol; Levomefolate - Drug Usage Statistics | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/DrospirenoneEthinylEstradiolLevomefolate | access-date = 14 January 2024}}</ref>

==Medical uses==

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.<ref name="mprpdf"/> 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.”<ref name="factiva">"Bayer Receives Approval for Beyaz in the U S." ENP Newswire [United Kingdom] 27 September 2010. Factiva. Web. 5 October 2011</ref> The drug combination will also increase folate levels due to its extra ingredient, levomefolic calcium. This is equivalent to folic acid 0.4&nbsp;mg and will help prevent neural tube defects in case of accidental pregnancy while taking, or shortly after stopping the drug.<ref name="mprpdf"/>

===Dosage and use===

Each 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&nbsp;mg, ethinylestradiol 20&nbsp;mcg, and levomefolate calcium 0.451&nbsp;mg and four light orange inactive pills containing of levomefolate calcium 0.451&nbsp;mg.<ref name="mprpdf">"Beyaz." MPR - Obstetrician & Gynecologist Edition (2010): A.5. Academic Search Complete. EBSCO. Web. 11 October 2011.</ref><ref name="Beyaz FDA label"/>

One tablet is taken by mouth at the same time every day. The failure rate may increase when pills are missed or taken incorrectly.<ref name="Beyaz FDA label">{{cite web | title=Beyaz- drospirenone/ethinyl estradiol/levomefolate calcium and levomefolate calcium kit | website=DailyMed | date=2 January 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8132454a-6135-4bac-b206-83a55eb8dbc6 | access-date=14 August 2020}}</ref> Single missed pills should be taken as soon as remembered.<ref name="Beyaz FDA label"/> 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.<ref name="Beyaz FDA label"/>

==Side effects==

Adverse reactions commonly reported by combined oral contraceptive users are irregular uterine bleeding, nausea, breast tenderness, and headache.<ref name="Beyaz FDA label"/>

==Interactions==

===Decreased efficacy===

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]], [[barbiturate|barbiturates]], [[carbamazepine]], [[bosentan]], [[felbamate]], [[griseofulvin]], [[oxcarbazepine]], [[rifampicin]], [[topiramate]] and products containing [[St. John’s Wort|St. John’s wort]]. Interactions between oral contraceptives and other drugs may lead to breakthrough bleeding and/or contraceptive failure.”<ref name="Beyaz FDA label"/> “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.”<ref name="Beyaz FDA label"/>

===Antivirals===

‘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.”<ref name="Beyaz FDA label"/>

===Antibiotics===

“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.”<ref name="Beyaz FDA label"/>

===Others===

“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.”<ref name="Beyaz FDA label"/>

==Pharmacology==

Combined oral contraceptives reduce the risk of pregnancy primarily by inhibiting ovulation.<ref name="mprpdf"/> 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&nbsp;mg is included for reducing the risk of neural tube defects in case of accidental pregnancy.<ref name="mprpdf"/>

==History==

EE/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.<ref name="factiva"/>

==See also==

* [[Birth control pill formulations]]

* [[Ethinylestradiol/drospirenone]]

* [[Estradiol/drospirenone]]

* [[Ethinylestradiol/drospirenone/prasterone]]

* [[List of combined sex-hormonal preparations]]

==References==

{{Reflist}}

{{Birth control methods}}

{{Hormonal contraceptives}}

{{Estrogen receptor modulators}}

{{Progesterone receptor modulators}}

{{Portal bar | Medicine}}

[[Category:Combined oral contraceptives]]

[[Category:Drugs developed by Bayer]]