Loseasonique Generic Name & Formulations
Mechanism of Action
Loseasonique Dosage and Administration
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
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.
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%.
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.
Levonorgestrel: renal (~45%), fecal (~32%). Ethinyl estradiol: renal, fecal. Half-life: ~34 hours (levonorgestrel); ~18 hours (ethinyl estradiol).
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
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
Loseasonique Patient Counseling