SEASONALE Dosage & Rx Info | Uses, Side Effects

Seasonale Generic Name & Formulations

Legal Class

General Description

Levonorgestrel 0.15mg, ethinyl estradiol 30micrograms (84 tabs); inert (7 tabs).

Pharmacological Class

Progestin + estrogen.

How Supplied

Dispenser (13-week supply)—3

Manufacturer

Teva Pharmaceuticals

Generic Availability

YES

Mechanism of Action

COCs 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.

Seasonale Indications

Indications

Oral contraception.

Seasonale Dosage and Administration

Adult

1 tab daily for 91 days; repeat. Use Sunday start for first cycle.

Children

Premenarchal: not recommended.

Seasonale Contraindications

Contraindications

High risk of arterial or venous thrombotic disease (eg, smokers or migraineurs over age 35, DVT or PE, cerebrovascular or coronary artery disease, thrombogenic valvular disease, atrial fibrillation, subacute bacterial endocarditis, hypercoagulopathies, uncontrolled hypertension, hypertension with vascular disease, diabetes over age 35, diabetes with hypertension or vascular disease or other end-organ damage, diabetes of >20yrs duration, headaches with focal neurologic symptoms). Undiagnosed abnormal uterine bleeding. Breast or other estrogen- or progestin-sensitive neoplasms. Hepatic tumors, acute viral hepatitis, or severe (decompensated) cirrhosis. Concomitant ombitasvir/paritaprevir/ritonavir, with or without dasabuvir.

Seasonale Boxed Warnings

Boxed Warning

Cigarette smoking increases risk of serious cardiovascular events.

Seasonale Warnings/Precautions

Warnings/Precautions

Increased risk of cardiovascular and cerebrovascular events (eg, stroke, MI) esp. women over age 35, smokers, and females with hypertension, dyslipidemia, diabetes, or obesity. Evaluate any medical or family history of thrombotic or thromboembolic disorders prior to initiation. Discontinue if thrombotic event, unexplained visual changes, jaundice occurs, or at least 4 weeks before through 2 weeks after surgery associated with increased risk of thromboembolism and during and after prolonged immobilization. Gallbladder disease. Pregnancy-related cholestasis. Diabetes. Prediabetes. Uncontrolled dyslipidemia. Hypertriglyceridemia. Depression. Hereditary angioedema. Evaluate significant changes in headaches, irregular uterine bleeding, amenorrhea, retinal vein thrombosis. Cholasma gravidarum. Monitor blood pressure; discontinue if significant hypertension occurs. Do regular complete physical exams. May need barrier contraception with Sunday starts or postpartum use (see full labeling). Hepatic impairment: not studied. Pregnancy: discontinue if occurs. Nursing mothers: use other methods of contraception until breastfeeding is discontinued.

Seasonale Pharmacokinetics

Absorption

Levonorgestrel is rapidly and completely absorbed after oral administration (bioavailability nearly 100%). Ethinyl estradiol is rapidly and almost completely absorbed from the GI tract but due to first-pass metabolism, the bioavailability is ~43%.

Distribution

Apparent volume of distribution: 1.8 L/kg (levonorgestrel); 4.3 L/kg (ethinyl estradiol). Levonorgestrel is ~97.5–99% protein bound (primarily to sex hormone binding globulin). Ethinyl estradiol is ~95–97% bound to serum albumin.

Metabolism

Following absorption, levonorgestrel is conjugated at the 17β-OH position to form sulfate and to a lesser extent, glucuronide conjugates in plasma. Levonorgestrel and its phase I metabolites are excreted primarily as glucuronide conjugates.

First-pass metabolism of ethinyl estradiol (EE) involves formation of EE-3-sulfate in the gut wall, followed by 2-hydroxylation of a portion of the remaining untransformed EE by hepatic cytochrome P-450 3A4 (CYP3A4). Levels of CYP3A4 vary widely among individuals and can explain the variation in rates of EE hydroxylation.

Elimination

Levonorgestrel: renal (~45%), fecal (~32%). Ethinyl estradiol: renal, fecal. Half-life: ~30 hours (levonorgestrel); ~15 hours (ethinyl estradiol).

Seasonale Interactions

Interactions

See Contraindications. ALT elevations with HCV regimen ombitasvir/paritaprevir/ritonavir, with or without dasabuvir; discontinue Seasonale prior to starting HCV regimen and restart 2wks after completion. Concomitant glecaprevir/pibrentasvir: not recommended. May be antagonized by CYP3A4 or other enzyme inducers (eg, aprepitant, barbiturates, bosentan, carbamazepine, efavirenz, felbamate, griseofulvin, oxcarbazepine, phenytoin, rifampin, rifabutin, rufinamide, St. John’s wort, topiramate, certain protease inhibitors); use backup contraception. May be potentiated by atorvastatin, rosuvastatin, acetaminophen, ascorbic acid, or CYP3A4 inhibitors (eg, itraconazole, ketoconazole, voriconazole, fluconazole, grapefruit juice). May be affected by HIV/HCV protease inhibitors or NNRTIs. Concomitant colesevelam; give 4hrs apart. May antagonize acetaminophen, temazepam, salicylic acid, morphine, clofibric acid, lamotrigine. May potentiate cyclosporine, prednisolone, theophylline, tizanidine, voriconazole. May need dose adjustment of thyroid or cortisol hormones. May affect lab tests (eg, coagulation factors, lipids, glucose tolerance, binding proteins, sex hormone binding globulins).

Seasonale Adverse Reactions

Adverse Reactions

Headache, menorrhagia, nausea, dysmenorrhea, acne, migraine, breast tenderness, weight increased, depression; pulmonary embolus, cholecystitis, breakthrough bleeding, amenorrhea, oligomenorrhea, chloasma, liver disease.

Seasonale Clinical Trials

See Literature

Seasonale Note

Not Applicable

Seasonale Patient Counseling