Anastrozole

Composition

One tablet of Anastrozole, regardless of the manufacturer, contains 1 mg of the same active substance.

Additional components: povidone, lactose monohydrate, silicon dioxide, microcrystalline cellulose, magnesium stearate, sodium carboxymethyl starch.

Sheath composition: macrogol-4000, hypromellose, titanium dioxide.

Package

White round tablets, covered with a shell, biconvex form, on the cut you can see a white core and a shell.

Pharmacological Effect

Antineoplastic, inhibits the synthesis of estrogens.

Pharmacodynamics and Pharmacokinetics

Pharmacodynamics
This agent is a potent and highly selective non-steroidal aromatase blocker. In postmenopausal women, estradiol is produced by the transformation of androstenedione into the tissues of peripheral organs in estrone with the participation of the aromatase enzyme. Estrone is converted to estradiol.

Lowering the level of estradiol causes a therapeutic effect in female patients suffering from malignant neoplasms of the breast. In postmenopause, the use of 1 mg of Anastrozole per day leads to a drop in the content of estradiol by 80%.

Pharmacokinetics
Absorption of the drug is rapid, the highest concentration in the blood is obtained after two hours with fasting. The half-life period reaches 50 hours. The food slows down the suction speed a little.

It binds to blood proteins by 40%. Metabolized extensively. It is excreted by the kidneys in its original form 72 hours after administration. Metabolites are also excreted mainly by the kidneys.

Indications for Use

• The first line of treatment for locally advanced malignant breast cancer in postmenopausal female patients.
• Adjuvant (accessory) treatment of early malignant breast cancer in the presence of positive hormonal receptors in postmenopausal women.
• The second line of treatment for a common malignant breast tumor, after the treatment with Tamoxifen, progressed the disease.

Contraindications

During the premenopause:

• Severe hepatic impairment;
• Concurrent therapy with Tamoxifen or with estrogens;
• Lactation period;
• Pregnancy;
• Sensitization to the components of the drug;
• Childhood age.

Caution should be used for hypercholesterolemia, osteoporosis, coronary heart disease, impaired liver function, severe renal failure, lactose intolerance, lactase deficiency, malabsorption of glucose or galactose.

Side Effects

• Reactions from the cardiovascular system: hot flashes.
• Reactions from the musculoskeletal system: arthralgia.
• Reactions from the genital system: vaginal bleeding, dry vaginal mucosa.
• Dermatological reactions: alopecia, rash, thinning of hair, polymorphic erythema.
• Reactions from the digestive system: vomiting, nausea, diarrhea, anorexia, increased content of ALT, AST and alkaline phosphatase, increased levels of gonadotropin and bilirubin, hepatitis.
• Reactions from the nervous system: drowsiness, headache, carpal tunnel syndrome.
• Reactions from the metabolism: hypercholesterolemia.
• Allergic reactions: urticaria, Quincke's edema, anaphylactic shock.
• Other reactions: asthenia.

Anastrozole, Instructions for Use (Method and Dosage)

Instructions for Anastrozole, instructions for Arimidex and instructions for Arimixyl are fundamentally similar to each other. It is recommended to take the drug inside, swallowing it whole and squeezed with a small amount of water. You should take the drug at the same time of day. Eating does not matter.

Anastrozole is used one tablet per day for a long period of time. If signs of disease progression are detected, the drug should be discontinued. The recommended duration of therapy as an adjuvant is 5 years.

Overdose

Treatment: there is no specific antidote, and symptomatic treatment is performed. You can induce vomiting if the patient is conscious. Dialysis is allowed. Supportive therapy, monitoring and control of vital systems and organs are recommended.

Interaction

Clinically significant pharmacological interaction with drug while taking other drugs is absent.

Drugs containing estrogens. inhibits the pharmacological effects of Anastrozole, therefore they should not be taken with Anastrozole.

Storage Conditions

Keep away from children, store at a temperature of up to 25° C.

Shelf Life

3 years.

Special Instructions

A number of adverse reactions of the drug may adversely affect the ability to drive a car.

Anastrozole Analogues

Analogues related to one group: Femara, Letroxyl, Letrozole, Aromasin, Aromadex, Aromaxyl, Exedrol.