LOSEASONIQUE Dosage & Rx Info | Uses, Side Effects

Loseasonique Generic Name & Formulations

Legal Class

General Description

Levonorgestrel 0.1mg + ethinyl estradiol 20micrograms (84 orange tabs); ethinyl estradiol 10micrograms (7 yellow tabs).

Pharmacological Class

Progestin + estrogen.

How Supplied

Dispensers—2 (2 X 91 day cycles)

Manufacturer

Teva Pharmaceuticals

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.

Loseasonique Indications

Indications

Oral contraception.

Loseasonique Dosage and Administration

Adult

1 tab daily for 91 days; repeat. Take at the same time daily. Use Sunday start for 1st cycle; use backup method until orange tabs are taken for 7 consecutive days. Allow at least 4 weeks postpartum, if not breastfeeding, to begin cycle. Use backup method if 2 consecutive orange tabs are missed (see full labeling).

Children

Pre-menarchal: not recommended.

Loseasonique 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.

Loseasonique Boxed Warnings

Not Applicable

Loseasonique Warnings/Precautions

Warnings/Precautions

Increased risk of cardiovascular and cerebrovascular events 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, or jaundice occurs, and at least 4 weeks before through 2 weeks after surgery associated with increased risk of thromboembolism. Gallbladder disease. Pregnancy-related cholestasis. Diabetes. Prediabetes. Uncontrolled dyslipidemia. Hypertriglyceridemia. Depression. Hereditary angioedema. Evaluate significant changes in headaches, irregular uterine bleeding, amenorrhea. Cholasma gravidarum. Monitor blood pressure; discontinue if significant hypertension occurs. Do regular complete physical exams. Hepatic impairment: not studied. Pregnancy: discontinue if occurs. Nursing mothers: use other methods of contraception until breastfeeding is discontinued.

Loseasonique 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: ~34 hours (levonorgestrel); ~18 hours (ethinyl estradiol).

Loseasonique Interactions

Interactions

See Contraindications. ALT elevations with HCV regimen ombitasvir/paritaprevir/ritonavir, with or without dasabuvir; discontinue Loseasonique prior to starting HCV regimen and restart 2wks after completion. Concomitant glecaprevir/pibrentasvir: not recommended. May be antagonized by CPY3A4 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 affected by protease inhibitors. May antagonize lamotrigine. May affect lab tests (eg, coagulation factors, lipids, glucose tolerance, binding proteins). May need dose adjustment of thyroid hormones.

Loseasonique Adverse Reactions

Adverse Reactions

Irregular uterine bleeding, nausea, breast tenderness, headache, dysmenorrhea, vomiting, back pain, acne, weight gain; pulmonary embolus, breakthrough bleeding, amenorrhea, oligomenorrhea, chloasma, liver disease.

Loseasonique Clinical Trials

See Literature

Loseasonique Note