nomegestrol and estrogen

G03FB12

Forms & Strengths

Adult Dosing

1 tablet daily taken orally for 28 consecutive days per cycle, without a break between packs
Taken continuously, starting on day 1 of menstrual bleeding or as directed

Pediatric Dosing

Indications

Hormone replacement therapy (HRT) for estrogen deficiency symptoms in postmenopausal women (at least 12 months since last menses)
Prevention of osteoporosis in postmenopausal women at high risk of future fractures who are intolerant of other approved medications

Mechanism of Action

Estradiol replaces endogenous estrogen loss, relieving menopausal vasomotor symptoms and preventing bone resorption
Nomegestrol acetate is a potent progestogen that opposes estrogenic endometrial proliferation, reducing the risk of endometrial hyperplasia and carcinoma

Contraindications

Known or suspected breast cancer
Known or suspected estrogen- or progestogen-dependent malignant tumors
Undiagnosed genital bleeding
Active or previous venous thromboembolism (deep vein thrombosis, pulmonary embolism)
Active or recent arterial thromboembolic disease (angina, myocardial infarction)
Known hepatic impairment or active liver disease until liver function tests have returned to normal
Known hypersensitivity to the active substances or any excipients

Adverse Reactions

Common: Headaches, breast pain/tenderness, irregular uterine bleeding, weight fluctuations
Uncommon: Mood alterations, libido changes, dizziness, nausea, abdominal pain, acne, alopecia, peripheral edema
Rare: Venous and arterial thromboembolism, gallbladder disease, hepatocellular tumors

Drug Interactions

Hepatic enzyme inducers (e.g., barbiturates, carbamazepine, carbamazepine, phenytoin, rifampicin, St. John's wort) decrease plasma concentrations of estradiol and nomegestrol
Inhibitors of CYP3A4 (e.g., ketoconazole, erythromycin) may increase plasma concentrations of estradiol
Concomitant use with HCV combination therapies containing ombitasvir/paritaprevir/ritonavir and dasabuvir may increase the risk of ALT elevations

Curated Content: Needs Vetting Before Put to Clinical Use