SAFYRAL Dosage & Rx Info | Uses, Side Effects

Safyral Generic Name & Formulations

Legal Class

General Description

Drospirenone 3mg, ethinyl estradiol 30micrograms, levomefolate calcium 0.451mg (21 tabs); levomefolate calcium 0.451mg (7 tabs).

Pharmacological Class

Progestin + estrogen + folate.

How Supplied

Packs—3 (blister cards)

Manufacturer

Bayer Corporation

Mechanism of Action

Combination oral contraceptives lower the risk of becoming pregnant primarily by suppressing ovulation. Other possible mechanisms may include cervical mucus changes that inhibit sperm penetration and endometrial changes that reduce the likelihood of implantation.

Safyral Indications

Indications

Oral contraception. To raise folate levels in women who choose to use an OC for contraception.

Safyral Dosage and Administration

Adult

1 tab daily for 28 days; repeat. Take at the same time daily. Use Day 1 or Sunday start for 1^st cycle; use backup method for first 7 days.

Children

Pre-menarche: not applicable.

Safyral Contraindications

Contraindications

Renal impairment. Adrenal insufficiency. High risk of arterial or venous thrombotic disease (eg, smokers or migraineurs over age 35, history of DVT or PE, 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). Current diagnosis or history of breast cancer, which may be hormone-sensitive. Hepatic disease or tumors. Undiagnosed abnormal uterine bleeding. Concomitant ombitasvir/paritaprevir/ritonavir, with or without dasabuvir.

Safyral Boxed Warnings

Boxed Warning

Cigarette smoking increases risk of serious cardiovascular events.

Safyral Warnings/Precautions

Warnings/Precautions

Increased risk of cardiovascular and cerebrovascular events (eg, stroke, MI) esp. in >35yrs of age, smokers, hypertensive females. Discontinue if thrombotic event, unexplained visual changes, or jaundice occurs, and at least 4 weeks before through 2 weeks after surgery associated with increased risk of thromboembolism. Hyperkalemia or risk thereof. Malignant neoplasms. Diabetes. Prediabetes. Uncontrolled dyslipidemias. Hypertriglyceridemia. Gallbladder disease. Pregnancy-related cholestasis. History of depression; monitor and discontinue if serious depression recurs. Hereditary angioedema. Evaluate significant changes in headaches, irregular uterine bleeding, amenorrhea. Do regular complete physical exams. Severe hepatic impairment: not studied. Monitor BP; discontinue if significant rise occurs. May need barrier contraception with Sunday starts or postpartum use (see full labeling). Postmenopausal women: not recommended. Pregnancy: discontinue if occurs. Nursing mothers: use other methods of contraception until breastfeeding is discontinued.

Safyral Pharmacokinetics

Absorption

Absolute bioavailability: ~76% (drospirenone); ~40% (ethinyl estradiol).
Serum concentrations of drospirenone and ethinyl estradiol reached peak levels within 1-2 hours after administration.

Distribution

Apparent volume of distribution: 4 L/kg (drospirenone); 4–5 L/kg (ethinyl estradiol).
~97% serum protein bound (drospirenone), ~98.5% serum protein bound (ethinyl estradiol).

Metabolism

Hepatic.

Elimination

Fecal, renal. Half-life: ~30 hours (drospirenone), ~24 hour (ethinyl estradiol).

Safyral Interactions

Interactions

See Contraindications. ALT elevations with HCV regimen ombitasvir/paritaprevir/ritonavir, with or without dasabuvir; discontinue Safyral prior to starting HCV regimen and restart 2wks after completion. Monitor serum K⁺ during 1^st cycle with drugs that increase potassium (eg, ACEIs, ARBs, NSAIDs, K⁺-sparing diuretics, K⁺ supplements, heparin, aldosterone antagonists); consider monitoring in high-risk patients taking concomitant long-term strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, voriconazole, indinavir, boceprevir, clarithromycin). May be antagonized by CYP3A4 or other enzyme inducers (eg, barbiturates, bosentan, carbamazepine, efavirenz, felbamate, griseofulvin, oxcarbazepine, phenytoin, rifampin, St. John's wort, topiramate, certain protease inhibitors) (use backup contraception). May be potentiated by atorvastatin, acetaminophen, ascorbic acid, or CYP3A4 inhibitors. May be affected by protease inhibitors, NNRTIs. May antagonize lamotrigine. May affect laboratory tests (eg, coagulation factors, lipids, glucose tolerance, binding proteins). May need dose adjustment of thyroid hormones. May mask vitamin B₁₂ deficiency (folate).

Safyral Adverse Reactions

Adverse Reactions

Premenstrual syndrome, headache/migraine, breast pain/tenderness, nausea, vomiting, mood changes, abdominal pain/tenderness/discomfort, breakthrough bleeding, amenorrhea, intolerance to contact lenses; chloasma, hypertension, serious thromboembolic events, liver disease.

Safyral Clinical Trials

See Literature

Safyral Note

Not Applicable

Safyral Patient Counseling