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

Composition:Composition per one tablet:

Active substance
Anastrozole 1.0 mg
Excipients
Lactose Monohydrate 65.0 mg
Microcrystalline cellulose 25.0 mg
Sodium carboxymethyl starch 5.0 mg
Hypromellose 3.0 mg
Magnesium stearate 1.0 mg
Core tablet weight 100.0 mg

Film sheath
Aquarius Prime BAP218010 white 3.0 mg [hypromellose - 65%, titanium dioxide -25%, macrogol (polyethylene glycol) -10%]
The weight of the film-coated tablet is 103.0 mg

Description:

The tablets are round biconvex, covered with a film coat of white color. The core of the tablet is white or almost white.

Pharmacotherapeutic group:An antineoplastic agent, an estrogen synthesis inhibitor.

ATX: & nbsp

L.02.B.G Enzyme Inhibitors

L.02.B.G.03 Anastrozole

Pharmacodynamics:

Selective non-steroidal aromatase inhibitor. Has antitumor activity against estrogen-dependent breast tumors in postmenopausal women. Reduces the content of circulating estradiol. Does not possess progestogen, androgenic and estrogenic activity, does not affect the secretion of endogenous glucocorticosteroids (GCS) and mineralocorticoids (MCS).

Pharmacokinetics:

Absorption - high (after intake of absorbed 83 - 85% of the dose), the maximum concentration (Tcmoh) -2 hours. The connection with plasma proteins is 40%.About 90 - 95% of the constant concentration in the plasma is achieved after 7 days of taking the drug. There is no information on cumulation.

Well metabolized in postmenopausal women. Metabolism is carried out in the process Ndealkylation, hydroxylation and conjugation with glucuronic acid. The main metabolite - triazole, determined in plasma and urine, does not inhibit aromatase. The half-life (T1 / 2) is 50 hours. Metabolites are excreted mainly by the kidneys, less than 10% of the dose is excreted in the urine unchanged for 72 hours.

The clearance of anastrozole after ingestion in volunteers with stabilized liver cirrhosis or renal dysfunction does not differ from the clearance determined in healthy volunteers.

Indications:

- Adjuvant therapy for early breast cancer, e positive hormonal receptors in postmenopausal women, including after adjuvant therapy with tamoxifen for 2-3 years.

- 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, in postmenopausal women.

Contraindications:

Hypersensitivity to anastrozole or other components of the drug, estrogen-dependent breast tumors in women in the pre-menopausal period, severe hepatic insufficiency (safety and efficacy not established), concomitant therapy with tamoxifen or preparations containing estrogens, children's age (safety and efficacy not established).

Carefully:

Osteoporosis, hypercholesterolemia, ischemic heart disease (IHD), impaired hepatic function, severe renal failure (creatinine clearance less than 20 ml / min).

In addition, for dosage forms containing lactose: lactase insufficiency, lactose intolerance, glucose-galactose malabsorption.

Pregnancy and lactation:

Contraindicated in pregnancy. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Inside, at the same time, regardless of food intake, 1 mg 1 time per day. The tablet should be swallowed whole, washed down with water. 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.

Impaired renal function: dose adjustment in patients with mild and moderate renal failure is not required. In patients with severe renal failure, the drug should be used with caution.

Dysfunction of the liver: dose adjustment in patients with mild to moderate liver function impairment is not required.

Side effects:

The frequency of adverse reactions listed below was determined according to the following criteria: very often (not less than 1/10); often (more than 1/100, less than 1/10); infrequently (more than 1/1000, less than 1/100); rarely (more than 1/10000, less than 1/1000); very rarely (less than 1/10000), including individual messages.

From the side of the vessels: Often - "tides" of blood to the face.

From the side of the musculoskeletal and connective tissue: very often - arthralgia / joint stiffness, arthritis; often - pain in the bones, myalgia; infrequently - a trigger finger.

From the genitals and the breast: often - dry mucous sheaths of the vagina, vaginal bleeding (mainly during the first weeks after cancellation or replacement of previous hormonal therapy on anastrozole).

From the skin and subcutaneous tissues: very often - skin rash; often thinning hair, alopecia, allergic reactions; infrequently - hives; rarely - erythema multiforme, anaphylactoid reaction, skin vasculitis (including individual cases of purpura (Shenlaine-Henoch syndrome)); very rarely Stevens-Johnson syndrome, angioedema.

From the gastrointestinal side tract: very often - nausea; often - diarrhea, vomiting.

From the liver and bile ducts: often - increased activity of alkaline phosphatase, alanine aminotransferase (ALT), aspartate aminotransferase (ACT); infrequently increased activity of gamma-glutamyltransferase and bilirubin concentration, hepatitis.

From the nervous system: very often - headache; often - drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors of the disease), impaired sensitivity (including paresthesia, loss or perversion of taste sensations).

From the side of metabolism and nutrition: often - anorexia, hypercholesterolemia; infrequently - hypercalcemia (e / without reducing the concentration of parathyroid hormone). Reception of the drug can cause a decrease in bone mineral density due to a decrease in the concentration of circulating estradiol,increasing the risk of osteoporosis and bone fractures.

General disorders: Often - asthenia of mild to moderate severity.

Adverse events noted in clinical trials that are not associated with anastrozole use: anemia, constipation, dyspepsia, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.

Overdose:

A single dose of anastrozole, which could lead to symptoms threatening life, is not established. Treatment: induction of vomiting, dialysis, maintenance therapy, control of the function of vital organs and systems. There is no specific antidote.

Interaction:

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

Weak non-specific inhibitor CYP Cimetidine does not affect the concentration of anastrozole in plasma. Effect of powerful inhibitors CYP the concentration of anastrozole is unknown.

Preparations containing estrogens reduce pharmacological action anastrozole, in connection with which they should not be administered simultaneously with anastrozole. Do not assign tamoxifen simultaneously with anastrozole, since it can weaken the pharmacological action of the latter. At the moment there is no information on the use of anastrozole in combination with other antitumor drugs.

Special instructions:

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.

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

Preparations containing estrogens should not be administered concomitantly with anastrozole. they will neutralize the pharmacological action of anastrozole. 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 still unknown.

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

Reducing the level of circulating estradiol, anastrozole can cause a decrease in bone mineral density.

In patients who suffer from osteoporosis or who are at risk for developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA scanning - dual-energy X-ray absorptiometry) at the beginning of treatment and in dynamics. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a physician. To date, there is insufficient data on the beneficial effects 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 analog preparations of gonadotropin-releasing hormone (GnRH).

It is not known whether anastrozole results of treatment when used in conjunction with chemotherapy.

Effect on the ability to drive transp. cf. and fur:

Some of the side effects of anastrozole, such as asthenia and drowsiness, can adversely affect the ability to perform potentially hazardous activities requiring 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.

Form release / dosage:Tablets, film-coated, 1 mg.

Packaging:By 7, 10, 14 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.
By 10, 14, 20, 28, 30 or 42 tablets in a can of polymer for medicines.
Free space in the bank is filled with cotton hygroscopic cotton.
Each can, 1 or 3 contour packs of 10 tablets, 1 or 2 contour packs of 14 tablets and 1 or 4 contour packs of 7 tablets together with instructions for use are placed in a pack of cardboard boxes.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000646

Date of registration:28.09.2011

The owner of the registration certificate:TECHNOLOGY OF DRUGS, LTD. TECHNOLOGY OF DRUGS, LTD. Russia

Manufacturer: & nbsp

TECHNOLOGY OF DRUGS, LTD. Russia

Information update date: & nbsp12.02.2015

Illustrated instructions

Instructions

Anastrozole-TL (Anastrozole-TL)