Anastrozole - instructions for use, dose, side effects, contraindications

Selective non-steroidal aromatase inhibitor - an enzyme that ensures the conversion of androstenedione to estrone and then to estradiol. Therapeutic effect in women with breast cancer during the postmenopause is achieved by reducing the amount of estradiol and, as a consequence, reducing the stimulating effect on the growth of tumor cells.

The drug does not have progestagenic, androgenic and estrogenic effects.

Pharmacokinetics:

Absorption is high. After ingestion, up to 85% of the dose is absorbed. Moderate association with blood proteins - about 40%.

The half-life is 50 hours.

Metabolism in the liver with the formation of inactive metabolites. Elimination with feces (85%) and kidneys (11%) within 72 hours.

Indications:

It is used for postmenopausal women as an adjuvant means of breast cancer in the early stages of the disease.

With metastatic breast cancer constitutes the first line of therapy.

As a second line of therapy used in advanced advanced breast cancer.

ICD-10

II.C50.C50 Malignant neoplasm of breast

Contraindications:

Individual intolerance, nPremenopausal period, renal failure.

Carefully:

It is used with caution in women with osteoporosis, ischemic heart disease, impaired liver function, with impaired renal function (creatinine clearance less than 20 ml per minute).

Pregnancy and lactation:Recommendations for Food and Drug Administration (US Food and Drug Administration) - category D. Absolute contraindications.

Dosing and Administration:

It is taken orally 1 mg once a day. Duration of treatment up to 5 years. When the disease progresses, the drug is stopped.

The highest daily dose is 1 mg.

The highest single dose is 1 mg.

Side effects:

The system of hematopoiesis: anemia, leukopenia.

Central nervous system: asthenia.

Respiratory system: cough, dyspnea.

The cardiovascular system: arterial hypertension, thrombophlebitis.

The digestive system: nausea, diarrhea, anorexia.

Hepatitis, increased activity alanine aminotransferase and aspartate aminotransferase, total bilirubin.

The musculoskeletal system: the phenomenon of osteoporosis.

Reproductive system: vaginal dryness, uterine bleeding.

Allergic reactions.

Overdose:

In clinical trials after taking 60 mg by men and 10 mg in women during the postmenopause, life-threatening conditions did not develop.

Treatment: gastric lavage, hemodialysis.

Interaction:

The rate of absorption of the drug decreases after eating.

Tamoxifen weakens the action of anastrozole with simultaneous administration.

The effectiveness of the drug decreases with the simultaneous administration of preparations containing estrogens.

Special instructions:

Before the appointment of the drug should receive a laboratory confirmation of the state of postmenopause - to determine the concentration of sex hormones in the blood serum.

When taking anastrozole, it is recommended to prevent osteoporosis.

Given the side effects of the drug on the central nervous system, patients are advised to exercise caution when driving vehicles and working with moving mechanisms.

Instructions

Anastrozole (Anastrozolum)