section name header

Pronunciation

a-NASS-troe-zole

Classifications

Therapeutic Classification: antineoplastics

Pharmacologic Classification: aromatase inhibitors

Indications

High Alert


Action

  • Inhibits the enzyme aromatase, which is partially responsible for conversion of precursors to estrogen.
Therapeutic effects:
  • Lowers levels of circulating estrogen, which may halt progression of estrogen-sensitive breast cancer.

Pharmacokinetics

Absorption: 83–85% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: 85% metabolized by the liver; 11% excreted renally.

Half-Life: 50 hr.

Time/Action Profile

(lowering of serum estradiol)

ROUTEONSETPEAKDURATION
POwithin 24 hr14 days6 days



Following cessation of therapy.



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: angina, MI, peripheral edema

Derm: hot flashes, rash, sweating

EENT: pharyngitis

F and E: hypercalcemia

GI: nausea, abdominal pain, anorexia, constipation, diarrhea, dry mouth, vomiting

GU: fertility (females), pelvic pain, vaginal bleeding, vaginal dryness

Metab: weight, hypercholesterolemia

MS: back pain, arthritis, bone pain, carpal tunnel syndrome, fracture, myalgia

Neuro: headache, weakness, dizziness., paresthesia

Resp: cough, dyspnea

Misc: pain, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions

Drug-drug:

Route/Dosage

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Arimidex