section name header

Pronunciation ⬇

LET-roe-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.
  • Decreased risk of recurrence/metastatic disease.

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly and completely absorbed.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Mostly metabolized by the liver. Primarily excreted in the urine (90%), with 6% being excreted as unchanged drug.

Half-Life: 2 days.

Time/Action Profile ⬆ ⬇

(effect on lowering of serum estradiol concentrations)

ROUTEONSETPEAKDURATION
POunknown2–3 daysunknown



Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

CV: chest pain, DEEP VEIN THROMBOSIS, edema, hypertension

Derm: ↑sweating, alopecia, hot flush, pruritus, rash

F and E: hypercalcemia

GI: nausea, abdominal pain, anorexia, constipation, diarrhea, dyspepsia, vomiting

GU: ↓fertility

Metab: hypercholesterolemia, weight gain

MS: musculoskeletal pain, ↓bone density, arthralgia, fracture

Neuro: anxiety, depression, dizziness, drowsiness, fatigue, headache, STROKE/TIA, vertigo, weakness

Resp: cough, dyspnea, pleural effusion, PULMONARY EMBOLISM

Interactions ⬆ ⬇

Drug-drug:

Route/Dosage ⬆ ⬇

Hepatic Impairment

Availability ⬆ ⬇

(Generic available)

Assessment ⬆ ⬇

Lab Test Considerations:

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Femara

Code ⬆

NDC Code