Estradiol/​Levonorgestrel

DEA Class; Rx

Common Brand Names; Climara Pro

Indicated for treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae) in women with an intact uterus.

Hypersensitivity

Known anaphylactic reaction or angioedema

Estrogen-dependent neoplasia

Current/history of: DVT/PE, arterial thromboembolic disease, breast cancer, liver disease/tumours

Undiagnosed abnormal vaginal bleeding

Jaundice with previous OCP use

Prevention of CVD

Hepatic impairment or disease, Protein C, protein S, or antithrombin deficiency, or other thrombophilic disorders

—

Bone mineral density changes, current/history of depression, DM, HTN, hyperlipidemia, obesity, endometriosis, family history of breast cancer and DVT/PE, smoking, hypothyroidism, elderly, liver impairment, uterine leiomyomata, vaginal infection or irritation (ring & cream)

Discontinue if the following develop: 4-6 wk before major surgery, any symptoms of VTE, massive BP increase, unusually severe migraines or first-time migraines, depression

Increased risk of post-op thromboembolic complications, coronary heart disease, stroke, and venous thromboembolism

Estrogen therapy may cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, hepatic hemangiomas, and fluid retention; consider whether benefits of estrogen therapy outweigh risks in women with these conditions; discontinue estrogens plus progestogens therapy with evidence of medically concerning fluid retention

Patients on warfarin/oral anticoagulants: Estrogens increase thromboembolic risk; increase in anticoagulant dose may be warranted

Serum follicle-stimulating hormone (FSH) and estradiol levels have not been shown to be useful in management of postmenopausal women with moderate to severe vasomotor symptoms

Estrogen administration may lead to severe hypercalcemia in women with breast cancer and bone metastases; discontinue therapy if hypercalcemia occurs, and take appropriate measures to reduce serum calcium level

Contact with water may affect patch

Avoid prolonged exposure of patch to sunlight

Do not use with conditions that predispose to hyperkalemia

Increased risk of ovarian cancer reported in women who used hormonal therapy for menopausal symptoms

Studies of the addition of a progestogen for 10 or more days of a cycle of estrogen administration, or daily with estrogen in a continuous regimen, have reported a lowered incidence of endometrial hyperplasia, a precursor of endometrial cancer, than would be induced by estrogen treatment alone; there are, however, possible risks that may be associated with use of progestogens with estrogens compared to estrogen-alone regimens; these include an increased risk of breast cancer

Manage appropriately risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus)

A 2 to 4-fold increase in risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens reported

Retinal vascular thrombosis reported in patients receiving estrogens; discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine; if examination reveals papilledema or retinal vascular lesions, estrogens should be discontinued

The drug is not indicated for use in pregnancy; there are no data with use in pregnant women; however, epidemiologic studies and meta-analyses have not found an increased risk of genital or nongenital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to combined hormonal contraceptives (estrogens and progestins) before conception or during early pregnancy

Estrogens plus progestogens are present in human milk and can reduce milk production in breastfeeding women; this reduction can occur at any time but is less likely to occur once breastfeeding is well-established; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breastfed child from treatment or from underlying maternal condition