Pharmacology of Anastrozole (Arimidex; Overview, Pharmacokinetics, Mechanism of action, Uses, Effect

Описание: Anastrozole is a non-steroidal aromatase inhibitor used primarily in the treatment of hormone receptor-positive breast cancer in postmenopausal women. Here's an overview of its pharmacology:

Mechanism of Action:
Aromatase Inhibition: Anastrozole selectively inhibits the enzyme aromatase, which is responsible for converting androgens (testosterone and androstenedione) into estrogens (estradiol and estrone). By inhibiting this enzyme, anastrozole reduces estrogen levels in the body, which is crucial for the growth of estrogen receptor-positive breast cancer cells.

Pharmacokinetics:
Absorption: Anastrozole is administered orally and has excellent oral bioavailability.

Distribution: It is widely distributed throughout the body.

Metabolism: Anastrozole is extensively metabolized by the liver.

Excretion: The drug and its metabolites are primarily excreted via the feces.

Elimination Half-Life: The elimination half-life is approximately 40-50 hours.

Clinical Use:
Breast Cancer: Anastrozole is used as adjuvant therapy for early-stage breast cancer and as a first-line treatment for advanced breast cancer in postmenopausal women.

Tamoxifen Resistance: It is also used in women whose breast cancer has become resistant to tamoxifen.

Side Effects:
Common Side Effects: Joint pain, hot flashes, fatigue, and osteoporosis2.

Serious Side Effects: Potential for liver damage and cardiovascular events

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