Bayer HealthCare Pharmaceuticals, Inc. announced the US Food and Drug Administration (FDA) has approved a new oral contraceptive (OC), Safyral (drospirenone 3 mg/ ethinyl estradiol 30 mcg/ levomefolate calcium 451 mcg tablets and levomefolate calcium 451 mcg tablets). In women who choose an OC for birth control, Safyral raises folate levels for the purpose of reducing the risk of rare Neural Tube Defects (NTDs) in a pregnancy conceived while taking Safyral or shortly after discontinuing it. Safyral provides the birth control Yasmin (drospirenone 3 mg/ ethinyl estradiol 30 mcg) with 451 mcg levomefolate calcium, which is a B vitamin.
Safyral is the second Bayer OC which contains folate. In September, the FDA approved Beyaz (drospirenone 3 mg/ ethinyl estradiol 20 mcg/ levomefolate calcium 451 mcg tablets and levomefolate calcium 451 mcg tablets), the first OC approved by the FDA to raise folate levels in women who choose an OC for birth control.
“With the FDA approval of Safyral, Bayer now offers two oral contraceptives that contain folate,” said Leslie North, vice president of Marketing, Women’s HealthCare, Bayer HealthCare Pharmaceuticals. “Safyral and Beyaz are part of Bayer’s growing women’s health franchise, and these new products reinforce our commitment to providing women various contraceptive options.”
The Centres for Disease Control and Prevention, the US Preventive Services Task Force, the March of Dimes and other leading health authorities recommend that all women of childbearing age supplement their diet with at least 400 mcg of folic acid daily. A well-established body of evidence supports folate supplementation as a means to reduce the incidence of neural tube defects – rare birth defects of the brain and spinal cord. These rare birth defects happen in the first few weeks of pregnancy – often before a woman finds out she is pregnant. As a result, daily folate supplementation is particularly important at least one month before and three months after conception.
“Combining an oral contraceptive with folate is important, because women may become pregnant during OC use or shortly after discontinuation, possibly before seeking preconception counselling from their healthcare providers,” said Dr. Anita Nelson, Professor of Obstetrics and Gynaecology at the Harbour-UCLA Medical Centre, Torrance, California. “For women who already use Yasmin for contraception, Safyral offers these women a new option to receive daily folate supplementation as part of their OC routine.”
Women should not use Safyral if they smoke and are over age 35. Smoking increases the risk of serious side effects from the Pill, which can be life-threatening, including blood clots, stroke or heart attack. This risk increases with age and number of cigarettes smoked.
Patients are advised to alert their healthcare provider if they are taking folate supplements. Safyral is not indicated during pregnancy. Safyral has 99 per cent contraceptive efficacy when used as directed. If pregnancy occurs during treatment with Safyral, further intake must be stopped. If a woman discontinues use of Safyral either with the intention of becoming pregnant or if she discontinues due to pregnancy while on the product, she is strongly encouraged to speak with her healthcare provider about taking a multivitamin with folic acid or another folate to maintain recommended folate intake.
Safyral is in a 21/7 day regimen consisting of 21 days of drospirenone 3 mg/ethinyl estradiol 30 mcg with levomefolate calcium 451 mcg (Metafolin•) followed by seven days of Metafolin only. Safyral is expected to be available in mid-January 2011 by prescription only.
Women should not use Safyral if they have kidney, liver, or adrenal disease because this could cause serious heart and health problems, or if they have or have had blood clots, certain cancers, history of heart attack or stroke, or if they are or may be pregnant. Safyral increases the risk of serious conditions including blood clots, stroke and heart attack. Smoking increases these risks, especially in women over 35. The risk of blood clots is highest during the first year of use.
In addition, Safyral contains drospirenone, a different kind of hormone that for some may increase potassium too much. Women should consult with their healthcare provider if they are on daily long-term treatment for a chronic condition with medications that may also increase potassium, as they should have a blood test to check their potassium level during the first month of taking Safyral.
The FDA approval of Safyral to raise folate levels in women who choose an OC for contraception is based on two clinical trials. The first trial was a pivotal 24-week clinical trial involving 379 healthy women aged 18-40 years, which found that YAZ (drospirenone 3 mg/ ethinyl estradiol 20 mcg) in combination with 451 mcg of Metafolin increased folate levels from baseline. This multi-centre, randomized, double-blind, parallel group study conducted in a US population with folate fortified food evaluated the effect of YAZ in combination with 451 mcg of Metafolin on Red Blood Cell (RBC) folate and plasma folate levels compared to YAZ alone during 24 weeks of treatment.
At week 24, the mean changes from baseline were significantly (p<0.0001) higher for women who took YAZ in combination with 451 mcg of Metafolin, as compared to women who took YAZ alone, for RBC folate (420 ± 347 nmol/L vs. 34.3 ± 171 nmol/L, respectively) and plasma folate (15.8 ± 20.4 nmol/L vs. -2.2 ± 14.6 nmol/L, respectively) levels. In the US folate study, the most common side effects were headache/migraine, menstrual irregularities, nausea/vomiting and breast pain/tenderness.
The addition of folate to an OC was further evaluated in a separate European study, which looked at Yasmin in combination with either 451 mcg of Metafolin or 400 mcg of folic acid for 24 weeks, followed by 20 weeks of treatment with Yasmin only (no folate intake). This study found that the Metafolin treatment produced maximum mean increases in plasma folate (33.5 ± 14.5 nmol/L) and in RBC folate (782 ± 260 nmol/L) levels at 24 weeks. Upon discontinuation of folate intake, the average RBC and plasma folate levels gradually decreased to starting levels (or baseline) over 20 weeks.
In the European folate study, the most common side effects were premenstrual syndrome, headache/migraine, breast pain/tenderness/discomfort, nausea/vomiting, and abdominal pain/discomfort/tenderness.
Bayer HealthCare Pharmaceuticals Inc. is the US-based pharmaceuticals operation of Bayer HealthCare LLC, a division of Bayer AG. It is one of the world’s leading, innovative companies in the healthcare and medical products industry. Bayer HealthCare combines the global activities of the Animal Health, Consumer Care, Diabetes Care, and Pharmaceuticals divisions.