Company: Bayer Healthcare Pharmaceuticals, Inc.
Pharmacologic class: Combination oral contraceptive (OC) (progestin + estrogen) + folate
Active ingredients: Drospirenone 3 mg, ethinyl estradiol 30 μg, levomefolate calcium 0.451 mg (21 tablets); levomefolate calcium 0.451 mg (seven tablets).
Indication: Oral contraception. To raise folate levels in women who choose to use an OC for contraception.
Pharmacology: Combination OCs reduce the risk of pregnancy primarily by inhibiting ovulation. This product combines drospirenone, an analogue of spironolactone that has both antimineralocorticoid and antiandrogenic activities, with an estrogen-plus-folate supplementation. Levomefolate calcium 0.451 mg (equivalent to folic acid 0.4 mg) is included for reducing the risk of neural tube defects in a pregnancy conceived while taking the product or shortly after discontinuing the product.
Clinical trials: The approval of Safyral (Yasmin + levomefolate calcium) was based on two clinical trials. One study, a multicenter, randomized, double-blind, active-control, parallel-group trial, investigated plasma folate and RBC folate levels over 24 weeks in a population that ate folate-fortified foods in the United States. Over the study period, the group given Yaz (drospirenone 3 mg/ethinyl estradiol 20 μg) + levomefolate 0.451 mg had higher plasma folate levels and higher RBC folate levels than the group given Yaz alone.
In a study conducted in Germany in a population that did not consume folate-fortified foods, the effect on the plasma and RBC folate and circulating folate metabolites was examined for Yasmin (drospirenone 3 mg/ethinyl estradiol 30 μg) + folic acid 0.4 mg compared with Yasmin + levomefolate calcium 0.451 mg. After achieving steady state by Week 24 (treatment phase), both plasma and RBC folate levels fell during the 20-week Yasmin-only (elimination) phase of the 44-week study.
In large clinical trials with Yasmin, pregnancy rates were <1 per 100 women-years of use.
Adults: One tablet daily for 28 days; repeat. Take at the same time daily. Use Day 1 or Sunday start for first cycle; use backup method for first seven days.
Children: Premenarchal: not applicable.
Contraindications: Renal impairment. Adrenal insufficiency. High risk of arterial or venous thrombotic disease (e.g., smokers or migraineurs older than age 35 years, history of deep venous thrombosis or thromboembolism, cerebrovascular or coronary artery disease, thrombogenic valvular disease, atrial fibrillation, subacute bacterial endocarditis, hypercoagulopathies, uncontrolled hypertension, diabetes with vascular disease, headaches with focal neurologic symptoms). Breast or other estrogen or progestin-sensitive neoplasms. Hepatic disease or tumors. Undiagnosed abnormal uterine bleeding. Pregnancy (Category X).
Warnings/Precautions: Discontinue if thrombotic event, unexplained visual changes, or jaundice occurs, and at least four weeks before through two weeks after surgery associated with increased risk of thromboembolism. Hyperkalemia or risk thereof. Diabetes. Prediabetes. Uncontrolled dyslipidemias. Pregnancy-related cholestasis. Depression. Evaluate significant changes in headaches, irregular uterine bleeding, amenorrhea. Monitor BP. Nursing mothers: not recommended.
Interactions: May potentiate drugs that can cause hyperkalemia in chronic use (e.g., ACE inhibitors, angiotensin II receptor blockers, nonsteroidal anti-inflammatory drugs, K+-sparing diuretics, K+ supplementation, heparin, aldosterone blockers) (check serum K+ during first cycle). May be antagonized by CYP3A4 or other enzyme inducers (e.g., barbiturates, bosentan, carbamazepine, felbamate, griseofulvin, oxcarbazepine, phenytoin, rifampin, St. John’s wort, topiramate) (use backup contraception). May be affected by protease inhibitors, acetaminophen, ascorbic acid, itraconazole, ketoconazole. May antagonize lamotrigine. May affect laboratory tests (e.g., coagulation factors, lipids, glucose tolerance, binding proteins). May need dose adjustment of thyroid hormones. May mask vitamin B12 deficiency (folate).
Adverse reactions: Hypertension, nausea, vomiting, breakthrough bleeding, amenorrhea, transient delay of ovulation after discontinuation, edema, chloasma, mastodynia, headache, intolerance to contact lenses. Increased risk of gallbladder disease, thromboembolic disorders.
How supplied: Packs—3 (3 x 28-day cycles)n
For more information,call 888.842.2937 or visit www.Safyral.com.