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

Excipientslactose monohydrate (200 mesh) 64.0 mg, povidone-K30 4.0 mg, lactose monohydrate (spray-dried) 23.0 mg, sodium carboxymethyl starch, type A 7.0 mg, magnesium stearate 1.0 mg, opadrai white 02G28619 (hypromellose E464 1.8750 mg, titanium dioxide E171 0.6375 mg, macrogol-6000 0.3000 mg, macrogol-400 0.1875 mg).

Description:

Round biconvex tablets covered with a film shell, white or almost white with an engraving "93" on one side and "A 10" on the other.

Pharmacotherapeutic group:Antitumor agent, estrogen synthesis inhibitor

ATX: & nbsp

L.02.B.G Enzyme Inhibitors

L.02.B.G.03 Anastrozole

Pharmacodynamics:

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

Anastrozole does not possess progestogen, 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 replace corticosteroids.

Pharmacokinetics:

After oral administration anastrozole quickly absorbed from the gastrointestinal tract. The maximum concentration in the blood plasma is usually achieved within 2 hours after ingestion (fasting). Food insignificantly 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. After 7 days of taking the drug, approximately 90-95% of the equilibrium concentration of anastrozole in the blood plasma is reached. There is no information on the dependence of pharmacokinetic parameters of anastrozole on time or dose. The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women. Connection with blood plasma proteins - 40%. Anastrozole Extensively metabolized in postmenopausal women, with less than 10% excreted by the kidneys unchanged for 72 hours after taking the drug. The half-life of anastrozole from the blood plasma is 40-50 hours. Anastrozole metabolism is carried out 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 clearance of anastrozole after oral administration with liver cirrhosis or renal dysfunction does not change.

Indications:

- Adjuvant therapy for early breast cancer with 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 tamoxifen treatment in postmenopausal women.

Contraindications:

- Hypersensitivity to anastrozole or other components of the drug.

- The Premenopausal Period.

- Severe hepatic impairment (safety and efficacy not established).

- Concomitant therapy with tamoxifen or preparations containing estrogens.

- Pregnancy and lactation.

- Child age (safety and efficacy in children not established).

- Insufficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:

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

Dosing and Administration:

Inside. The tablet is swallowed whole, washed down with water. It is recommended to take the drug at the same time, regardless of food intake.

Adults, including the elderly: 1 mg orally once a day for a long time. If signs of disease progression appear, the drug should be discontinued. As an adjuvant therapy, the recommended duration of treatment is 5 years.

Impaired renal function: correction of the dose in patients with impaired renal function is not required.

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: very often - "tides" of blood to the face.

From 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 breast: often - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after cancellation or change 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 tract: very often - nausea; often - diarrhea, vomiting.

From the liver and biliary tract: often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamyl-transferase and bilirubin concentration, hepatitis.

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

From the side of metabolism and nutrition: often - anorexia, hypercholesterolemia; infrequently - hypercalcemia (with / without increasing the concentration of parathyroid hormone).

Admission of anastrozole can cause a decrease in bone mineral density due to a decrease in the concentration of circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures.

General disorders: very often asthenia of mild or 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:

Single clinical cases of accidental drug overdose are described.A single dose of anastrozole, which could lead to symptoms threatening life, is not established.

Specific antidote does not exist, in case of an overdose, treatment should be symptomatic. You can induce vomiting if the patient is conscious. Dialysis may be performed. General supportive therapy, patient monitoring and monitoring of the functions of vital organs and systems are recommended.

Interaction:

Studies on the drug interaction with phenazone (Antipyrine) 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.

Preparations containing estrogens reduce the pharmacological effect of anastrozole, and therefore they should not be administered simultaneously with anastrozole.

Do not assign tamoxifen simultaneously with anastrozole because it can weaken the pharmacological action of the latter.

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 anastrozole in patients with severe liver function disorders.

In patients with osteoporosis or an increased risk of osteoporosis, bone mineral density should be assessed by densitometry, for example, DEXAScanning (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. Because the anastrozole reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density. Nowadays There is insufficient data on the positive effect of bisphosphonates on loss of bone mineral densitytissue 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-gonadotropin-releasing hormone.

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 simultaneously with anastrozole, since 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 results of treatment when used in conjunction with chemotherapy.

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

Some side effects of anastrozole, such as asthenia and drowsiness, can negatively affect the ability to perform potentially dangerous activities that require 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:For 7 tablets in a blister of PVC / PVDC / aluminum foil; 4 or 8 blisters with instructions for use in a cardboard bundle.

Storage conditions:

List B.

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001175/10

Date of registration:19.02.2010

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Industries, Ltd. Israel

Representation: & nbspTeva Teva Israel

Information update date: & nbsp28.08.2017

Illustrated instructions

Instructions

Anastrozole-Teva (Anastrozole-Teva)