Exemestane
Cytostatic · Aromatase inhibitor
Indications
Adjuvant treatment of post-menopausal oestrogen receptor positive invasive early breast cancer following 2 - 3 years of initial adjuvant tamoxifen therapy. Advance post-menopausal breast cancer that has progressed following anti- oestrogen therapy.
Dosage
Adults: 1 tab daily after a meal. In early breast cancer, continue treatment until completion of 5 yr combined sequential adjuvant therapy with tamoxifen, or earlier if tumour relapses. In advanced breast cancer continue treatment until tumour progression is evident. Children: Not recommended.
Adverse Effects
Hot flushes, nausea, arthralgia, fatigue, somnolence, carpal tunnel syndrome, sweating, dizziness, headache, depression, alopecia, leg and peripheral oedema, constipation, dyspepsia, GI upset, asthenia, paraesthesia, insomnia, pain, skin reactions, anorexia, alopecia, osteoporosis, fracture, altered LFTs. Increased alkaline phosphate and bilirubin. Rarely blood dyscrasias.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Pre-menopausal women. Precautions: Assess LH, FSH and oestradiol level before the treatment. Hepatic or renal impairment. Monitor bone mineral density during adjuvant therapy, treat for osteoporosis as appropriate.
Interactions
Drug metabolised by CYP3A4 that have a narrow therapeutic ratio, oestrogen.
Advice to Patient
Take after meals at the same time each day. Contact prescriber if there is acute headache, change in vision, unrelieved abdominal disturbances, chest pain, palpitations, joint pain, back pain, bone or muscle pain, burning or itching on urination, vaginal discharge, unusual cough, difficulty in breathing, flu-like symptoms. Avoid highly crowded places to prevent infection. Do not get vaccinated without consulting prescriber. To prevent hot flushes, stay in cold dark room or apply cold compresses.
Pharmacokinetics
Absorption: Rapid and moderate (Approx 42%) following oral administration: AUC and Cmax increased by 59% and 39%, respectively, following a high-fat breakfast. Metabolism: Extensively hepatic. Half-life elimination: Approx 24 hours. Time to peak: Women with breast cancer: 1.2 hours. Excretion: Urine (<1% as unchanged drug, 39% to 45% as metabolites); feces (36% to 48%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
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