Vero-Anastrozole - instructions for use, doses, side effects, contraindications

Active substance
Anastrozole	1 mg
Excipients:
Corn starch	27 mg
Lactose Monohydrate	63 mg
Povidone K-17 (polyvinylpyrrolidone)	4 mg
Carboxymethyl starch sodium (primogel)	4 mg
Magnesium stearate	1 mg
Weight of tablet without film sheath	100 mg
Composition of the film shell:
Hypromellose (hydroxypropylmethylcellulose)	1.29 mg
Povidone K-17 (polyvinylpyrrolidone)	0.81 mg
Polysorbate (Tween 80)	0.27 mg
Talc	0.36 mg
Titanium dioxide	0.27 mg
Weight of film-coated tablet	103 mg

Description:

The tablets covered with a film shell of white or almost white color, round biconcave forms.

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. In postmenopausal women anastrozole in a daily dose of 1 mg causes a decrease in the level of estradiol by 80%.

Anastrozole does not possess progestogen, androgenic and estrogenic activity.

Anastrozole in daily doses up to 10 mg does not have an effect on the secretion of cortisol and aldosterone.

Pharmacokinetics:

Absorption of anastrozole is fast, the maximum concentration in the plasma is reached within 2 hours after ingestion (fasting). 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 plasma with a single daily intake of anastrozole. After a 7-day treatment, approximately 90-95% of the equilibrium concentration of anastrozole in plasma is achieved. Connection with blood plasma proteins - 40%.

The half-life of plasma is 40-50 hours. Less than 10% of the dose is excreted unchanged in urine within 72 hours after taking the drug. Anastrozole metabolism is carried out N-dealkylation, hydroxylation and glucuronization. Metabolites are excreted mainly with urine. Triazole, the main metabolite, determined in plasma, does not inhibit aromatase.

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 therapy in postmenopausal women.

Contraindications:

- Hypersensitivity to anastrozole or other constituents of the drug;

- the premenopausal women;

- atAcute renal failure (creatinine clearance less than 20 ml / min);

- themeasured or severe hepatic impairment (safety and efficacy not established);

- fromconcurrent therapy with tamoxifen;

- bPregnancy and period of breastfeeding;

- dThe Russian age.

Dosing and Administration:

Inside. Swallow the whole tablet with water. It is recommended to take the drug at the same time.

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.

Impaired renal function: dose adjustment in patients with mild to moderate renal impairment is not required

Dysfunction of the liver: dose adjustment in patients with mild 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); sometimes (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 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 - dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after the cancellation or change of previous hormone 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 isolated cases of purpura (Shenlaine-Henoch syndrome)), very rarely - Stephen-Johnson syndrome, angioedema.

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

From the liver and bile ducts: often - increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; 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 (with / without increasing the concentration of parathyroid hormone). Admission of the drug 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 during clinical trials, not associated with reception of anastrozole: anemia, constipation, indigestion, back pain, abdominal pain,increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.

Overdose:

A single dose of anastrozole, which could lead to life-threatening symptoms, is not defined.

There is no specific antidote; In case of an overdose, treatment should be symptomatic. If the patient is conscious, it is advisable to induce vomiting. Dialysis may be performed. General supportive therapy, patient monitoring and monitoring of the function of vital organs and systems are recommended.

Interaction:

Studies on the drug interaction with antipyrine and cimetidine indicate that clinically significant drug interaction mediated by cytochrome P450 in the joint use of anastrozole with other drugs is unlikely.

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 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.

There is no data on the use of anastrozole in patients with severe liver dysfunction or in patients with severe renal impairment (creatinine clearance less than 20 mL / min).

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

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

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

In patients suffering from osteoporosis or who are at risk for developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA scanning) 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.

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

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 or 28 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 28 tablets in a jar of polymer materials.

Each bank or 1 circuit cell package of 28 tablets or 2 contiguous cell packs of 14 tablets, or 3 contiguous cell packs of 10 tablets or 4 contour packs of 7 tablets together with instructions for use in a pack of cardboard.

Storage conditions:At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002520/07

Date of registration:31.08.2007 / 08.10.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Representation: & nbspVEROPHARM, AO VEROPHARM, AO Russia

Information update date: & nbsp03.02.2017

Illustrated instructions

Instructions

Vero-Anastrozole (Vero-Anastrosol)