Name the category.
Sex hormones and hormone antagonisits in malignant disease.
Name the main drug.
Tamoxifen
Name the drug class.
Selective estrogen receptor modulators (SERMs)
Describe the mechanism of action.
Competitive antagonist on the estrogen receptors of the breast → ↓ breast cancer cell growth
Agonist on estrogen receptors in the following tissues:
Bone tissue → inhibition of osteoclasts → ↓ risk of osteoporosis and fractures
Endometrium → ↑ proliferation
Myometrium → ↑ proliferation
List indications.
Premenopausal estrogen receptor-positive breast cancer
Vaginal atrophy (related to menopause)
Prostate cancer: prevention of gynecomastia
List side effects.
Hot flashes
↑ Risk of endometrial cancer
↑ Risk of thromboembolic events (e.g., pulmonary embolism, DVT)
↑ Risk of uterine sarcoma
List contraindications.
Known hypersensitivity to tamoxifen or any ingredient in the formulation.
When used in women with DCIS and women at high risk for breast cancer, history of DVT or pulmonary embolism.
When used in women with DCIS and women at high risk for breast cancer, concurrent anticoagulant therapy with a warfarin derivative.
List common adverse effects.
Hot flushes (flashes), mood disturbances, vaginal discharge, vaginal bleeding, menstrual irregularities, nausea, fluid retention, weight loss.
Last changed2 years ago