Safyral

Generic name:

Ethinylestradiol, levonorgestrel, and levomefolate calcium

Drug class:

Combined oral contraceptive with folate supplementation

Dosage form:

Oral tablets

Root of administration:

Oral

Dose:

One active tablet containing ethinylestradiol 30 µg, levonorgestrel 150 µg, and levomefolate calcium 0.451 mg once daily for 21 consecutive days followed by a 7-day tablet-free interval. Varies by indication; consult label.

Mechanism of action:

Ethinylestradiol and levonorgestrel inhibit ovulation by suppressing the hypothalamic-pituitary-gonadal axis, increase cervical mucus viscosity, and alter endometrial lining. Levomefolate calcium provides active folate to reduce the risk of folate deficiency in reproductive-aged women.

Drug usage cases:

• Prevention of pregnancy
• Reduction of folate deficiency in women of reproductive age
• Regulation of menstrual cycles
• Acne vulgaris (off-label)
• Hirsutism (off-label)
• Premenstrual syndrome management (off-label)

Drug contra indications:

• Thrombophlebitis or thromboembolic disorders (e.g., DVT, PE)
• Known thrombophilic conditions (e.g., protein C or S deficiency)
• History of cerebrovascular or coronary artery disease
• Uncontrolled hypertension (≥160/100 mmHg)
• Migraine with focal aura
• Current or history of breast carcinoma or estrogen-dependent tumors
• Severe hepatic impairment or liver tumors
• Cholestasis of pregnancy or previous oral contraceptive–related cholestasis
• Undiagnosed abnormal uterine bleeding
• Hypersensitivity to any component
• Pregnancy
• Polycythemia
• Bacterial endocarditis
• Prolonged immobilization with risk of thrombosis

Side effects:

• Nausea and vomiting
• Headache and migraine
• Breast tenderness and enlargement
• Weight changes
• Irregular uterine bleeding or spotting
• Menstrual disorders
• Mood changes, depression
• Libido changes
• Bloating and fluid retention
• Acne and other skin reactions
• Vaginal candidiasis
• Hypertension
• Thromboembolic events (rare but serious)
• Gallbladder disease
• Elevated liver enzymes
• Allergic reactions (rash, urticaria)

Warnings:

• Increased risk of venous and arterial thromboembolism, especially in smokers over 35 years
• Monitor blood pressure regularly
• Discontinue if signs of thrombotic events occur (e.g., leg pain, chest pain, dyspnea)
• Caution in migraine sufferers; discontinue if aura develops
• May worsen hepatic function in patients with liver disease
• Use with caution in diabetes due to potential effects on glucose tolerance
• Risk of chloasma; avoid excessive sun exposure
• Monitor for depression and mood changes
• May affect lipid metabolism
• Potential impact on bone mineral density with long-term use
• Drug interactions with enzyme inducers and inhibitors (e.g., rifampicin, anticonvulsants)
• Reduced contraceptive efficacy with certain antibiotics and herbs (e.g., St. John’s Wort)

Use during pregnancy or breastfeeding:

Use in pregnancy: Contraindicated. Discontinue immediately if pregnancy is confirmed; no therapeutic benefit and potential fetal risk. Use in breastfeeding: Not recommended. May reduce milk production and pass into breast milk; consider alternative contraception or delay use until after weaning.