Anastrozole: use of the drug

When diagnosed with a malignant tumor of the breast in women, doctors can prescribe anastrozol tablets. This drug is an inhibitor of enzymes (suppresses their production) of hormone synthesis, eliminating the cause of the appearance of cancer. Familiarization with the instructions for use will help to use the tool correctly. Do not self-medicate, it is dangerous.




Instructions for use Anastrozole

Aromatase inhibitors (a group of drugs, including Anastrozole) are hormone antagonists, they act through the inhibition of the synthesis of the enzyme necessary for the production of hormones. The active ingredient of the drug – anastrozole inhibits estradiol (female hormone), but has no effect on cortisol, gonadotropin and aldosterone.

Composition and release form

Anastrozole is available only in pill format, the medicine has no other forms of release. Composition and description:

Description Yellow square tablets flat shape with rounded edges, notching and engraving
The concentration of anastrozole, mg per pc. one
Excipients Magnesium stearate, crospovidone, lactose, povidone, dye yellow Ludipress, hypromellose, colloidal silicon dioxide
Packaging Blisters of 20 pieces, three blisters in a pack

Pharmacodynamics and pharmacokinetics

The antitumor agent contains the active ingredient, which is a selective (selectively acting) nonsteroidal aromatase inhibitor. In the period of postmenopausal women, with the participation of this enzyme from androstenedione and estrone, estradiol is obtained. Reducing its level treats breast cancer. Anastrozole can reduce the amount of circulating hormone by 80%. The drug does not possess progestogenic, estrogenic and androgenic activity.

After taking the pill inside the active ingredient is rapidly absorbed from the gastrointestinal tract and reaches a maximum plasma concentration after two hours, provided that the medicine was taken on an empty stomach. Food reduces the rate of anastrozole absorption, but not the degree. The active substance binds to plasma proteins by 40%, not cumulated (does not accumulate).

Drug metabolism occurs in the liver by dealkylation, hydroxylation and glucuronization. The main metabolite triazole is determined in plasma and urine, is not an aromatase inhibitor. The substance itself and its metabolites are excreted by urine within three days after ingestion With stabilized liver cirrhosis, renal dysfunction, anastrozole clearance does not change. There are no differences in the pharmacokinetics of the active ingredient in postmenopausal women.


anastrozole drug


Indications for use

Anastrozole for men may be prescribed by specialists – the medicine is used in bodybuilding. Indications for the use of the drug in women are:

  • treatment of advanced postmenopausal breast cancer;
  • treatment of invasive estrogen-positive breast cancer in the early stages with positive hormone receptor indicators;
  • complex treatment of estrogen-positive breast cancer in the early stages after adjuvant treatment with Tamoxifen for 2–3 years.

How to take anastrozole

Tablets are intended for oral administration in a dosage of 1 mg times / day. The dosage is not dependent on age (in old age also 1 mg once). Dose adjustment is not carried out with minor or moderate violations of the liver and kidneys. The course of therapy with Anastrozolum is determined by the doctor individually, and can last for a long time (up to several years).

Anastrozole in bodybuilding

The drug inhibits the production of estrogen, so it can be used in bodybuilding with long courses of steroid hormones to reduce the negative impact of female sex hormones. Additionally, the drug removes an unnecessary amount of water from the body, allows for a clear relief. Anastrozole suppresses the problem of increasing the mammary glands (gynecomastia) in men. For female bodybuilders, the drug is not recommended.

It is recommended to take tablets in the morning on an empty stomach, so that the active substance is absorbed and absorbed faster. 10 days after taking anabolic steroids, you need to take a test for estradiol, and then start taking Anastrozole at a dose of 0.5 mg / day (when using Sustanon or anabolic steroids containing testosterone enanthate, tests are done after 3-4 weeks).


See also: Anastrozole in bodybuilding and fitness: how to use


Special instructions

Before treatment with Anastrozol, study the instructions for use. It contains special instructions:

  1. With the uncertainty of the hormonal status of the state of menopause must be confirmed by biochemical analyzes.
  2. The safety of treatment with the remedy in case of marked impaired liver function has not been established.
  3. It is forbidden to combine anastrozole with estrogen.
  4. During therapy, it is forbidden to control machinery and automobiles, because the concentration of attention and the speed of psychomotor reactions decrease.
  5. In the presence of osteoporosis or the risk of its development in women, bone mineral density is assessed using bone densitometry, scanning at the beginning and during treatment. If necessary, prevention of osteoporosis is prescribed.
  6. As part of claimed lactose, therefore, the drug can not be used in case of intolerance to galactose, lactase deficiency, impaired glucose-galactose absorption.


what is anastrozole used for in bodybuilding


During pregnancy

During childbearing and breastfeeding the use of Anastrozole is prohibited. This is due to the fact that the drug affects the production of hormones, which can lead to a negative impact on the development and growth of the fetus (especially female) and the newborn. It is not known whether the active ingredient penetrates into breast milk, but it is better to stop lactation during therapy.

In childhood

The drug Anastrozole is prohibited for use not only in childhood, but also in adult patients before the postmenopausal period. This is due to the suppression of the production of the female hormone estradiol, which will cause hormonal disruption in adolescents, and in young women – menstrual disorders. For the treatment of breast tumors using other drugs.

Drug interaction

During drug therapy, attention should be paid to its combination with other drugs. Combinations and risks:

  • The drug reduces the effectiveness of estrogen, this combination is prohibited due to the opposite pharmacological action.
  • According to the doctors, when combined with Antipyrine and Cimetidine, induction of microsomal liver enzymes is unlikely.
  • The combination of the drug with Tamoxifen is prohibited, as they mutually weaken each other’s effects.
  • The clinically significant effects of combinations of anastrozole with bisphosphonates have not been reported.
  • It is better to divide the time of taking the drug with drugs containing aluminum and magnesium salts, beta-blockers.

Side effects

According to reviews of patients receiving treatment with anastrozole, side effects are frequent. These include:

  • flushing, nervous agitation;
  • vaginal dryness, vaginal bleeding;
  • hair loss or thinning, alopecia;
  • elevated levels of bilirubin, hepatitis;
  • nausea, anorexia, diarrhea, vomiting;
  • headache, asthenia, drowsiness;
  • increased total cholesterol concentration (hypercholesterolemia);
  • allergic reactions, dermatological skin rash, hyperemia, anaphylactic shock;
  • arthralgia, carpal tunnel syndrome;
  • nervous excitement;
  • decrease in bone tissue mineral density;
  • Stevens-Johnson syndrome, angioedema;
  • urticaria, polymorphic erythema.


what is the drug anastrozole used for



Doctors rarely report drug overdose. Accidental or deliberate overdosing does not lead to the threat of death. Signs of overdose are enhanced side effects. When treatment should induce vomiting, dialysis, symptomatic therapy. There is no specific antidote to Anastrozol, general supportive care, regular monitoring of vital functions and careful monitoring of the patient’s condition are recommended.


Not all categories of patients are allowed to receive treatment of malignant tumors with Anastrozole. Contraindications for its use are:

  • premenopause;
  • coronary heart disease;
  • severe renal and hepatic impairment;
  • pregnancy, lactation;
  • children and adolescents;
  • hypersensitivity to the components;
  • concurrent therapy with estrogen or tamoxifen.

Terms of sale and storage

The drug is available by prescription, stored at a temperature of up to 25 degrees in a dark, dry place without access by children, valid for three years.

Anastrozole Analogs

Allocate direct and indirect substitutes for Anastrozole. The former coincide with it in composition and are generics, the latter differ in component elements, but have the same effect. Popular substitutes:

  • Celana, Vero-Anastrozole, Anabrez, Anamasten – direct analogues with the same active composition, are available in the form of tablets;
  • Arimidex is an anti-tumor agent based on anastrozole;
  • Aksatrol, Armotraz, Egistrozol – substitutes containing the same active substance.