exemestane HIGH ALERT!
(ecks-eh-MEHS-tayn) Aromasin
Pharmacologic class: Aromatase inhibitor
Therapeutic class: Antineoplastic Pregnancy
risk category: X
INDICATIONS AND DOSAGES
> Advanced breast cancer in postmenopausal
women whose disease has progressed after
treatment with tamoxifen or adjuvant treatment of
postmenopausal women with estrogen-receptor
positive early breast cancer who have received 2
to 3 years of tamoxifen and are switched for
completion of a total of five consecutive years of
adjuvant hormonal therapy
Adults: 25 mg P.O. once daily after a meal.
Adjust-a-dose: If patient is receiving a potent
CYP3A4 inducer such as rifampicin or phe-
nytoin. increase dose to 50 mg P.O. once daily
after a meal.
CONTRAINDICATIONS AND CAUTIONS
• Contraindicated in patients hypersensitive to
drug or its components.
Lifespan: In premenopausal women, don't give
drug.
Reactions may be common, uncommon, life-threatening. or COMMON \M» I.IH-IHIU MIMSG
ADVERSE REACTIONS
CXS: fever, depression, insomnia. anxiety,
fatigue, pain, dizziness, headache, paresthesia,
generalized weakness, asthenia, confusion,
hypoesthesia.
CV: hypertension, edema, chest pain.
EEXT: sinusitis, rhinitis, pharyngitis.
GI: nausea, vomiting, abdominal pain, anorexia.
constipation, diarrhea, dyspepsia.
GU: UTI.
Metabolic: increased appetite.
Musculoskeletal: pathologic fractures, arthralgia.
back pain, skeletal pain.
Respirator): dyspnea, bronchitis, coughing, upper
respiratory tract infection.
Skin: rash, increased sweating, alopecia, itching.
Other: infection, flu-like syndrome, hot flushes,
lymphedema.
INTERACTIONS
Drug-drug. Drugs that induce CYP3A4: May-
decrease exemestane level. Estrogen-containing
drugs: May affect drug. Don’t give together.
EFFECTS ON LAB TEST RESULTS None
reported.
tCanada
198
PHARMACOKINETICS
Absorption: Rapid, with about 42°o from the Gl
tract. Plasma level increases by 40% after a high-
fat breakfast. Distribution: Extensive; 90% bound
to proteins. Metabolism: I xten- sively
metabolized by the liver. The main liver
isoenzyme involved is CYP3A4. Excretion:
Equally in urine and feces. Less than l% is
excreted unchanged in urine. Half-life: About 24
hours.
Route Onset Peak Duration
P0 Unknown 1-2 hr Unknown
ACTION ■■■■■■■■■MS ~ .
Chemical effect: Is an irreversible, steroidal
aromatase inactivator that acts as a false substrate
for the aromatase enzyme, the main enzyme that
converts androgens to estrogens in
premenopausal and postmenopausal women.
Drug is then processed to an intermediate that
binds irreversibly to the enzyme's active site,
causing inactivation. This effect is known as
“suicide inhibition" and results in lower levels of
circulating estrogens. Deprivation of estrogen is
an effective and selective way to treat estrogen-
dependent breast cancer in postmenopausal
women.
OOTC ’Liquid contains alcohol.