levomefolate-calcium and drospirenone-and-ethinyl-estradiol-combination

The incidence of pregnancies affected with neural tube defects (NTDs) has been reduced by food fortification programs and public health campaigns promoting folic acid supplementation, but the incidence of NTDs in the USA has not achieved the full potential reduction expected with adequate periconceptional folate utilization. In seeking new ways to access sexually active women at risk for pregnancy, one option would be to link folic acid supplementation to contraceptive use. Since birth control pills are the most popular method of reversible contraception in the USA, it would seem quite logical to find a way to supplement them. To this end, a very efficient folate, levomefolate calcium salt (metafolin), has been added to drospirenone-containing oral contraceptives in equimolar concentrations to the recommended supplements of folic acid to reduce the risk for pregnancy and to reduce the risk of NTDs in pregnancies that occur while women are taking the pill or shortly after they discontinue its use. This article will focus on the need for such folate supplementation and will summarize the contraceptive and noncontraceptive benefits of the 30 µg EE/3 mg drospirenone pill (Yasmin(®), Bayer Healthcare, NJ, USA) to which has been added 451 metafolin (Safyral(®), Bayer Healthcare). The new information about thromboembolism risks associated with use of drospirenone-containing pills is also discussed.

Topics: Androstenes; Calcium; Contraception; Contraceptives, Oral, Hormonal; Drug Administration Schedule; Ethinyl Estradiol; Evidence-Based Medicine; Female; Folic Acid; Glutamates; Humans; Neural Tube Defects; Pregnancy; United States; Women's Health

Beyaz(®) (Bayer HealthCare Pharmaceuticals, Berlin, Germany) consists of 28 film-coated tablets: 24 tablets each containing 3 mg drospirenone plus 20 µg ethinylestradiol (EE) and 451 µg levomefolate calcium followed by four tablets, each containing 451 µg levomefolate calcium. It has the same indications of the parent compound 20 µg EE/3 mg drospirenone in a 24/4-day regimen (i.e., contraception, moderate acne, premenstrual dysforic disorder). In addition, the 24-day regimen with 20 µg EE/3 mg drospirenone/levomefolate calcium assure significant increases in red blood cell and plasma folate levels reaching values indicated to be protective in reducing the risk of neural tube defects. A progressive decrease in folate levels has been observed in women taking a 30 µg EE pill fortified with the same dose of levomefolate calcium upon discontinuation. At 4 and 8 weeks following cessation of the oral contraceptive, red blood cell folate levels >906 nmol/l were measured in 85 and 60% of women respectively. Because of this, the folate-containing pill may aid in reducing the risk of neural tube defects in a pregnancy conceived during use or shortly after the discontinuation of the product.

Topics: Androstenes; Calcium; Contraception; Contraceptives, Oral, Combined; Drug Administration Schedule; Ethinyl Estradiol; Evidence-Based Medicine; Female; Glutamates; Humans; Neural Tube Defects; Patient Satisfaction; Tetrahydrofolates

A new tablet formulation containing 0.02 mg ethinylestradiol/3 mg drospirenone/0.451 mg levomefolate calcium (calcium salt containing 0.416 mg L-5-methyltetrahydrofolate) was assessed for bioequivalence compared to the approved oral contraceptive (OC) tablet containing identical amounts of ethinylestradiol and drospirenone and to a tablet containing 0.451 mg levomefolate calcium.. Forty-four subjects received in an intraindividual crossover design single doses of the new tablet formulation or the established ethinylestradiol/drospirenone tablet or the levomefolate calcium tablet.. Bioequivalence was demonstrated for ethinylestradiol, drospirenone and L-5-methyltetrahydrofolate (active moiety of levomefolate calcium) between the investigated tablet formulations. The geometric mean ratios of the AUC((0-tlast)) and C(max) values for all three compounds and their 90% confidence intervals were well within the 80%-125% range generally accepted to demonstrate bioequivalence.. The rate and extent of absorption of ethinylestradiol and drospirenone were not affected by the concomitant administration of levomefolate calcium and vice versa.

Topics: Adolescent; Adult; Androstenes; Calcium; Contraceptives, Oral, Combined; Cross-Over Studies; Estrogens; Ethinyl Estradiol; Female; Glutamates; Humans; Mineralocorticoid Receptor Antagonists; Therapeutic Equivalency; Young Adult