Exemestane
Pronunciation: (ex-e-MES-tane)Class: Aromatase inhibitor
Trade Names:
Aromasin
- Tablets for oral use 25 mg
Pharmacology
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An irreversible, steroidal aromatase inactivator. It lowers circulating estrogen concentrations in postmenopausal women. Exemestane is 90% bound to plasma proteins. Exemestane is extensively metabolized.
Pharmacokinetics
Absorption
Rapidly absorbed. At least 42% if the dose is absorbed. T max is 1.2 h (women with breast cancer) and 2.9 h (healthy women). When taken after a high-fat breakfast, the plasma levels increased approximately 40%.
Distribution
90% protein bound.
Metabolism
Extensively metabolized. CYP3A4 is the principal isoenzyme involved in the oxidation of exemestane. The metabolites are inactive or inhibit aromatase with decreased potency compared to exemestane.
Elimination
The t 1/2 is 24 h. Approximately 42% is excreted in the urine and approximately 42% is excreted in the feces. Less than 1% is excreted unchanged in the urine.
Special Populations
Renal Function ImpairmentAUC is about 3 times higher in those with moderate or severe renal insufficiency. No dosage adjustment necessary.
Hepatic Function ImpairmentAUC increased approximately 3 times in those with moderate or sever hepatic insufficiency. No dosage adjustment necessary.
Indications and Usage
Advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy.
Unlabeled Uses
Prevention of prostate cancer.
Contraindications
Standard considerations.
Dosage and Administration
Breast CancerAdults
PO 25 mg once daily.
Storage/Stability
Store at controlled room temperature.
Drug Interactions
Agents that inhibit or induce CYP-4503A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole, and others)A possible decrease of exemestane by agents which inhibit or induce CYP-450 3A4 (eg, rifampin, phenobarbital, erythromycin, ketoconazole).
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Chest pain; hypertension; peripheral edema.
CNS
Fatigue; depression; insomnia; anxiety; headache; dizziness.
Dermatologic
Rash; increased sweating; androgenic effects reported including hypertrichosis, hair loss, and acne.
Endocrine
Hot flushes; weight gain.
GI
Low potential for nausea and vomiting; abdominal pain; anorexia; constipation; diarrhea; and increased appetite.
Hematologic
Lymphopenia.
Musculoskeletal
Musculoskeletal pain; arthralgia.
Respiratory
Dyspnea; coughing.
Miscellaneous
Flu-like symptoms with fever; hoarseness.
Precautions
Pregnancy
Category D .
Lactation
Undetermined.
Children
Safety and efficacy not established in patients younger than 18 yr of age.
Endocrine effects
Increases in testosterone and androstenedione levels observed.
Premenopausal women
Do not administer exemestane tablets to premenopausal women.
Lymphocytopenia
Approximately 20% of patients receiving exemestane in clinical studies experienced common toxicity criteria. Grade 3 or 4 lymphocytopenia.
Patient Information
- Androgenic effects have been reported with exemestane. Inform patients that hypertrichosis, hair loss, acne, or hoarseness may occur.
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exemestane - Includes detailed dosage instructions.
