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

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.