Anastrozole - instructions for use, reviews, analogs and formulations (1 mg of Teva, TL, Kabi) of a drug for the treatment of breast or breast cancer in adults, children and pregnancy. Composition of the antitumor agent

In this article, you can read the instructions for using the drug Anastrozole. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Anastrozole in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Anastrozole in the presence of existing structural analogues.Use to treat breast or breast cancer in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Anastrozole - an antitumor drug, an inhibitor of the synthesis of estrogens.

Anastrozole is a highly selective non-steroidal aromatase inhibitor, an enzyme that, in postmenopausal women, converts androstenedione into peripheral tissues to estrone and then to estradiol. Reducing the concentration of circulating estradiol in patients with breast cancer has a therapeutic effect. In postmenopausal women, anastrozole at a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%.

Anastrozole does not possess progestagenic, androgenic and estrogenic activity. In daily doses up to 10 mg does not have an effect on the secretion of cortisol and aldosterone, therefore, when anastrozole is used, it is not necessary to substitute corticosteroids.

Composition

Anastrozole + auxiliary substances.

Pharmacokinetics

After oral administration anastrozole is rapidly absorbed from the digestive tract. Food slightly reduces the rate of absorption, but not its degree and does not lead to a clinically significant effect on the equilibrium concentration of the drug in the blood plasma with a single daily intake of anastrozole.There is no information on the dependence of pharmacokinetic parameters of anastrozole on time or dose. Connection with blood plasma proteins - 40%. Anastrozole is extensively metabolized in postmenopausal women, with less than 10% excreted by the kidneys unchanged for 72 hours after taking the drug. Anastrozole metabolism is carried out by N-dealkylation, hydroxylation and glucuronidation. Metabolites of anastrozole are excreted mainly by the kidneys. The main metabolite of anastrozole - triazole, determined in blood plasma, does not have pharmacological activity. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women.

Indications

• adjuvant therapy of early breast cancer, with positive hormonal receptors in postmenopausal women, incl. after 2-3 years of adjuvant therapy with tamoxifen;
• the first line of therapy for locally advanced or metastatic breast cancer, with positive or unknown hormonal receptors in postmenopausal women;
• the second line of therapy for advanced breast cancer progressing after treatment with tamoxifen.

Forms of release

The tablets covered with a cover of 1 mg.

Instructions for use and dosing regimen

Assign 1 mg 1 time per day. The tablet should be swallowed whole, washed down with water.

It is recommended to take the drug at the same time, regardless of food intake.

The duration of treatment depends on the form and severity of the disease (with adjuvant therapy, the recommended duration of treatment is 5 years). If signs of disease progression appear, the drug should be discontinued.

Side effect

• "tides" of blood to the face;
• arthralgia;
• trigger finger;
• dryness of the vaginal mucosa;
• vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormonal therapy for anastrozole);
• skin rash;
• thinning hair;
• alopecia;
• erythema multiforme (Stevens-Johnson syndrome);
• nausea, vomiting;
• diarrhea;
• anorexia;
• increased activity of ALT, AST and APF;
• increased activity of GGT and bilirubin concentration;
• hepatitis;
• headache;
• increased drowsiness;
• carpal tunnel syndrome (mainly observed in patients with risk factors for this disease);
• hypercholesterolemia;
• osteoporosis and bone fractures;
• allergic reactions;
• anaphylactoid reactions;
• angioedema;
• hives;
• anaphylactic shock;
• asthenia.

Contraindications

• pre-menopausal period;
• severe hepatic impairment (safety and efficacy not established);
• concomitant therapy with tamoxifen or preparations containing estrogens;
• pregnancy;
• lactation period (lactation);
• children's age (safety and efficacy in children not established);
• hypersensitivity to anastrozole or other components of the drug.

Application in pregnancy and lactation

Contraindicated use of the drug Anastrozole during pregnancy and during breastfeeding.

Use in children

Contraindicated in children and adolescents under the age of 18 years. Safety and efficacy in children is not established.

special instructions

In case of doubt in the hormonal status of the patient, menopause should be confirmed by determining the concentration of sex hormones in the blood serum.

In the case of persisting uterine bleeding against the background of receiving anastrozole, consultation and supervision of the gynecologist is necessary.

There is no data on the use of the drug in patients with severe liver function disorders.

In patients with osteoporosis or an increased risk of osteoporosis, the bone mineral density should be assessed by densitometry, for example, by DEXA scanning (dual-energy X-ray absorptiometry) at the beginning of treatment and regularly throughout its duration. If necessary, prescribe the treatment or prevention of osteoporosis and carefully monitor the patient's condition.

Since anastrozole reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density. At the moment, there is insufficient data on the positive effect of bisphosphonates on the loss of bone mineral density caused by anastrozole or their benefits when used for the purpose of prevention.

There is no data on the simultaneous use of anastrozole and GnRH analogues.

In women with a receptor-negative tumor to estrogens, the efficacy of anastrozole has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.

Preparations containing estrogens should not be administered concomitantly with anastrozole.these drugs will neutralize its pharmacological action.

The efficacy and safety of anastrozole and Tamoxifen in their simultaneous application, regardless of the status of the hormonal receptors, are comparable to those of a single tamoxifen. The exact mechanism of this phenomenon is not yet known.

It is not known whether anastrozole improves the results of treatment when combined with chemotherapy.

Impact on the ability to drive vehicles and manage mechanisms

Some side effects of anastrozole, such as asthenia and drowsiness, can adversely affect the ability to perform work that requires increased concentration and speed of psychomotor reactions. In this regard, it is recommended that when these symptoms occur, exercise caution in the management of vehicles and mechanisms.

Drug Interactions

Studies on the drug interaction with phenazone and cimetidine indicate that the combined use of anastrozole with other drugs is unlikely to lead to a clinically significant drug interaction mediated by cytochrome P450.

Clinically significant drug interaction with the administration of anastrozole concomitantly with other commonly prescribed drugs is absent.

At the moment there is no information on the use of anastrozole in combination with other antitumor drugs.

Anastrozole reduces the effectiveness of estrogens.

Do not prescribe tamoxifen at the same time as anastrozole, since it can weaken the pharmacological action of the latter.

Analogues of the drug Anastrozole

Structural analogs for the active substance:

• Aksastrol;
• Anabrez;
• Anamasten;
• Anaster;
• Anastrozole Cubi;
• Anastrozole Teva;
• Anastrozole TL;
• Anastrax;
• Arimidex;
• Vero Anastrozole;
• Selana;
• Egistrazole.

Analogues on the curative effect (remedies for the treatment of neoplasms of the breast):

• Abitaxel;
• Avastin;
• Alkeran;
• Aminoglutethimide;
• Aromasine;
• Biel;
• Buserelin depot;
• Vepezid;
• Vinelbin;
• Vincristine;
• Gemcitabine medak;
• Herceptin;
• Hormoplex;
• Depostat;
• Doxol;
• Doxorubifer;
• Doxorubicin;
• Zitazonium;
• Zoladex;
• Zometa;
• Ikzempra;
• Intaksel;
• Kabetsin;
• Carboplatin;
• Kelix;
• Klobir;
• Xeloda;
• Ledoxine;
• Leukeran;
• Letrozole;
• Letrotera;
• Lomustine;
• Lucrin Depot;
• Mawerex;
• Mammoth;
• Methotrexate;
• Miltex;
• Mitoxantrone;
• Mitotax;
• Navelbin;
• Novanthron;
• Novofen;
• Nolvadex;
• Omnadren 250;
• Oncotron;
• Orimeten;
• Paclitaxel;
• Paxen;
• Rubid;
• Tayverb;
• Taxol;
• Taxotere;
• Tamoxen;
• Tamoxifen;
• Tautax;
• Thiotepa Thioplex;
• Fazlodex;
• Femara;
• Ftorafur;
• Fluorouracil;
• Halavan;
• Cyclophosphane;
• Cytoxan;
• Extrase;
• Aldesine;
• Endoxane;
• Episyndan
• Etoposide;
• Yutaksan.

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