EXEMESTANE

EXEMESTANE
(ex-e-mes'tain)
Aromasin
Classifications: antineoplastic; aromatase inhibitor, steroidal; antiestrogen;
Therapeutic: antineoplastic
; steroidal aromatase inhibitor
Prototype: Anastrozole
Pregnancy Category: D

Availability

25 mg tablet

Action

Steroidal aromatase inhibitor that suppresses plasma estrogens estradiol and estrone without affecting cortisol or aldosterone synthesis in the adrenal glands. The enzyme, aromatase converts estrone to estradiol.

Therapeutic Effect

Breast tumor regression is possible in postmenopausal women. Effectiveness is indicated by evidence of tumor regression.

Uses

Estrogen-receptor positive early breast cancer following treatment with tamoxifen, treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy.

Contraindications

Hypersensitivity to exemestane; pregnancy (category D), lactation. Safety and efficay in children not established.

Cautious Use

Hepatic or renal insufficiency; GI disorders; cardiovascular disease; hyperlipidemia.

Route & Dosage

Early and Advanced Breast Cancer
Adult: PO 25 mg q.d. after a meal

Administration

Oral
  • Give following a meal.
  • Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

Body as a Whole: Fatigue, hot flashes, pain, flu-like symptoms; edema; fever; paresthesia. CNS: Depression, insomnia, anxiety; dizziness; headache. CV: Hypertension. GI: Nausea, vomiting, abdominal pain, anorexia, constipation, diarrhea, increased appetite. Respiratory: Dyspnea, cough, bronchitis, sinusitis. Skin: Increased sweating, rash, itching. Other: UTI; lymphedema.

Pharmacokinetics

Absorption: Rapidly, approximately 42% reaches systemic circulation. Distribution: Extensive tissue distribution, 90% protein bound. Metabolism: Extensively in liver (CYP3A4). Elimination: Equally in urine and feces. Half-Life: 24 h.

Nursing Implications

Assessment & Drug Effects

  • Lab tests: Baseline liver function, BUN and creatinine; periodic WBC with differential, lipid profile, routine blood chemistry.

Patient & Family Education

  • Review manufacturer's patient literature thoroughly to reinforce understanding of likely adverse effects.
  • Report bothersome adverse effects to physician.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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