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Exemestane
U.S. Brand Names
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms

U.S. Brand Names
Aromasin®

Pharmacological Index

Antineoplastic Agent, Miscellaneous


Use

Treatment of advanced breast cancer in postmenopausal women whose disease has progressed following tamoxifen therapy


Pregnancy Risk Factor

D


Pregnancy/Breast-Feeding Implications

Exemestane can cause fetal harm when administered to a pregnant woman. It is not indicated for premenopausal women, but if exposure occurred during pregnancy, risk to the fetus and potential risk for loss of the pregnancy should be discussed.


Contraindications

Known hypersensitivity to exemestane or any component; pregnancy, or lactation


Warnings/Precautions

Not indicated for premenopausal women; not to be given with estrogen-containing agents. Use with caution in hepatic impairment or renal insufficiency.


Adverse Reactions

>10% :

Central nervous system: Fatigue (22%), pain (13%), depression (13%), insomnia (11%), anxiety (10%)

Endocrine & metabolic: Hot flashes (13%)

Gastrointestinal: Nausea (18%)

1% to 10%:

Central nervous system: Dizziness (8%), headache (8%), fever (5%), hypoesthesia, confusion

Cardiovascular: Edema (7%), hypertension (5%), chest pain

Dermatologic: Rash, itching, alopecia

Gastrointestinal: Vomiting (7%), abdominal pain (6%), anorexia (6%), constipation (5%), diarrhea (4%), increased appetite (3%), dyspepsia

Genitourinary: urinary tract infection

Neuromuscular & skeletal: Weakness, paresthesia, pathological fracture, arthralgia

Miscellaneous: Influenza-like symptoms (6%), sweating (6%), lymphedema, infection

Respiratory: Dyspnea (10%), cough (6%), bronchitis, sinusitis, pharyngitis, rhinitis

<1%: Increase in transaminases and GGT

A dose-dependent decrease in sex-hormone binding globulin has been observed with daily doses of 25 mg or more. Serum luteinizing hormone and follicle-stimulating hormone levels have increased with this medicine.


Overdosage/Toxicology

Daily doses as high as 800 mg have been used in healthy volunteers and 600 mg for 12 weeks in postmenopausal women with advanced breast cancer. If an overdose should occur, general supportive care would be indicated. Mice given 3200 mg/kg as a single dose died. This would be equivalent to 640 times the recommended human dose on a mg/m2 basis. Rats and dogs died at higher single doses equivalent to 2000-4000 times the recommended human dose on a mg/m2 basis.


Drug Interactions

CYP3A4 substrate; however, ketoconazole, a CYP3A4 inhibitor, did not change the pharmacokinetics of exemestane. No other potential drug interactions have been evaluated.


Stability

Store at 25°C (77°F)


Mechanism of Action

Exemestane is an irreversible, steroidal aromatase inactivator. It prevents conversion of androgens to estrogens by tying up the enzyme aromatase. In breast cancers where growth is estrogen-dependent, this medicine will lower circulating estrogens.


Pharmacodynamics/Kinetics
  • Absorption: Rapidly absorbed; mean AUC: 75.4 ngh/mL

Distribution: Extensive

Protein binding: 90%

Metabolism: Extensively metabolized. Oxidation (CYP3A4) of the methylene group, reduction of the 17-keto group with formation of many secondary metabolites. The metabolites are inactive or inhibit aromatase with decreased potency compared to the parent drug.

Half-life: 24 hours

Time to peak: Tmax (women with breast cancer): 1.2 hours

Elimination: <1% of parent drug excreted in urine; 42% of metabolites excreted in urine; 42% excreted in feces


Usual Dosage

Adults; Oral: 25 mg once daily after a meal; treatment should continue until tumor progression is evident


Dietary Considerations

Plasma levels increased by 40% when exemestane was taken with a fatty meal


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take after a meal; use caution if you have uncontrolled high blood pressure. Do not use in pregnancy or lactation. Avoid driving or doing other tasks or hobbies that require alertness until you know how this medicine affects you. Take at a similar time every day.


Nursing Implications

Educate patient about getting blood pressure checked while on medicine, especially if there is a history of poor control. Encourage patient not to drive until she sees how the medicine affects her; it can cause fatigue and dizziness. Medication should be taken at a similar time every day and after a meal to decrease nausea and increase absorption.


Dosage Forms

Tablet: 25 mg


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