Drug Guide
Exemestane
Classification
Therapeutic: Antineoplastic agent, Aromatase inhibitor
Pharmacological: Steroid irreversible aromatase inhibitor
FDA Approved Indications
- Treatment of estrogen receptor-positive breast cancer in postmenopausal women
Mechanism of Action
Exemestane irreversibly binds to aromatase enzyme, decreasing estrogen synthesis, which reduces estrogen-dependent tumor growth in hormone receptor-positive breast cancer.
Dosage and Administration
Adult: 25 mg orally once daily, preferably after a meal
Pediatric: Not approved for pediatric use
Geriatric: Adjust dosage based on clinical response; no specific dosage change required solely due to age
Renal Impairment: No dose adjustment required
Hepatic Impairment: Use with caution; no specific dose adjustment recommended
Pharmacokinetics
Absorption: Well absorbed after oral administration
Distribution: Widely distributed; plasma protein binding approximately 90%
Metabolism: Metabolized in the liver primarily via reduction and conjugation
Excretion: Excreted mainly in urine as conjugates; minor fecal excretion
Half Life: Approximately 26 hours
Contraindications
- Hypersensitivity to exemestane or any components of the formulation
Precautions
- Use cautiously in patients with a history of osteoporosis or at risk for osteoporosis; monitor bone mineral density.
- Not recommended for premenopausal women. Use in pregnancy is contraindicated due to potential fetal harm and teratogenic effects.
- Lactation: No data available; caution advised, breastfeeding is not recommended.
Adverse Reactions - Common
- Hot flashes (Common)
- Fatigue (Common)
- Night sweats (Common)
- Nausea (Common)
- Arthralgia (Common)
Adverse Reactions - Serious
- Osteoporosis and fractures (Less common)
- Hyperglycemia (Less common)
- Allergic reactions including rash, pruritus, angioedema (Rare)
Drug-Drug Interactions
- Tamoxifen (may reduce effectiveness)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor bone mineral density periodically; assess for symptoms of osteoporosis; evaluate liver function before and during treatment.
Diagnoses:
- Risk for osteoporosis
- Ineffective coping due to menopausal symptoms
Implementation: Administer with food; counsel patient on calcium and vitamin D intake to support bone health; monitor liver function tests periodically.
Evaluation: Assess for relief of tumor symptoms; monitor bone density and calcium levels.
Patient/Family Teaching
- Report any new or worsening symptoms such as bone pain, fractures, or severe hot flashes.
- Maintain adequate calcium and vitamin D intake.
- Inform about potential osteoporosis risk.
- Do not double dose if a dose is missed.
- Avoid pregnancy; use effective contraception during treatment and for some time after discontinuation.
Special Considerations
Black Box Warnings:
- Potential to cause osteoporosis and fractures; monitor bone health regularly.
Genetic Factors: Limited data on genetic variations affecting response.
Lab Test Interference: May affect liver function tests.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, hypotension, somnolence
Treatment: Supportive care; standard measures for overdose; no specific antidote.
Storage and Handling
Storage: Store at room temperature (20°C to 25°C / 68°F to 77°F), away from moisture and light.
Stability: Stable under recommended storage conditions.