Exemestane

Indications

Exemestane is used for: Breast cancer in postmenopausal women

Adult Dose

Oral Advanced or locally advanced breast cancer Adult: In women who are no longer responsive to anti-oestrogen therapy: 25 mg once daily.

Child Dose

Renal Dose

Administration

Should be taken with food. Take after a meal.

Contra Indications

Hypersensitivity. Premenopausal women. Pregnancy and lactation.

Precautions

Hepatic and renal impairment. Monitor bone mineral density at regular intervals especially in patients at risk of osteoporosis. Lactation: Excretion in milk unknown; because of potential for serious adverse reactions in breast-fed infants, advise women not to breastfeed during treatment and for 1 month after final dose

Pregnancy-Lactation

Pregnancy Category: X Lactation: Excretion in milk unknown; because of potential for serious adverse reactions in breast-fed infants, advise women not to breastfeed during treatment and for 1 month after final dose

Interactions

May result in reduced plasma levels of exemestane when used with CYP3A4 enzyme inducers. Oestrogen-containing drugs; St. John's wort, black cohosh, dong quai.

Adverse Effects

Side effects of Exemestane : >10% Fatigue (22%), Nausea (18%), Hot flashes (13%), Depression (13%), Pain (13%), Insomnia (11%) 1-10% Anxiety (10%), Dyspnea (10%), Dizziness (8%), Headache (8%), Edema (7%), Vomiting (7%), Flu-like syndrome (6%), Abdominal pain (6%), Anorexia (6%), Cough (6%), Hypertension (5%), Constipation (5%), Diarrhea (4%) <1% Cardiac failure, Uterine polyps, Endometrial hyperplasia, Gastric ulcer Frequency not defined Hepatitis, Visual disturbances

Mechanism of Action

Exemestane is an irreversible selective aromatase inhibitor which acts as a false substrate for the aromatase enzyme, forming an intermediate that binds irreversibly to the active site causing its inactivation. It also lowers circulating oestrogens in estrogen-dependent breast carcinoma.