Universal reference book for medicines
Name of the preparation: EGISTRAZOL (EGISTRAZOL)

Active substance: anastrozole

Type: Antitumor drug.
Aromatase inhibitor
Manufacturer: EGIS Pharmaceuticals (Hungary) manufactured by NATCO PHARMA (India)
Composition, form of production and packaging
The tablets covered with a film cover of
white color, round, biconcave, with engraving "ANA 1" on one side;
on the bend - white or almost white.
1 tab.

anastrozole 1 mg

Excipients: lactose monohydrate, povidone, sodium carboxymethyl starch, magnesium stearate.

The composition of the film shell: opadray white (macrogol 400, hypromellose, titanium dioxide).

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
14 pcs.
- blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2012.

PHARMACHOLOGIC EFFECT

Antitumor drug.
Anastrozole is a strong and highly selective non-steroidal aromatase inhibitor, an enzyme that, with the help of women, androstenedione and testosterone in tissues is converted to estrone and estradiol, respectively. 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 level of estradiol concentration 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.
PHARMACOKINETICS

Suction and distribution

After oral administration anastrozole is rapidly absorbed from the digestive tract.
C max in blood plasma is usually achieved within 2 hours after ingestion on an empty stomach. Food slightly reduces the rate of absorption, but not its degree and does not lead to a clinically significant effect on the C ss of the drug in the blood plasma with a single daily intake of anastrozole. After a 7-day treatment, approximately 90-95% C ss of anastrozole is reached in the blood plasma. 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. Binding to blood plasma proteins - 40%.
Metabolism and excretion

Anastrozole metabolism is carried out by N-dealkylation, hydroxylation and glucuronation.
Metabolites of anastrozole are excreted mainly by the kidneys. The main metabolite of anastrozole - triazole, determined in blood plasma, does not have pharmacological activity. Anastrozole is extensively metabolized in postmenopausal women, with less than 10% excreted by the kidneys unchanged for 72 hours after taking the drug. T 1/2 anastrozole from the blood plasma is 40-50 h.
Pharmacokinetics in special clinical cases

The clearance of anastrozole after ingestion with cirrhosis of the liver or renal dysfunction does not change.

INDICATIONS

- adjuvant therapy of early breast cancer, with positive hormonal receptors in postmenopausal women;

- the first line of therapy for locally advanced or metastatic breast cancer with a positive or an unknown hormonal status in postmenopausal women.

- the second line of therapy for advanced breast cancer, progressing after previous therapy with tamoxifen.

DOSING MODE

The drug is prescribed 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, are prescribed 1 mg orally 1 time / 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.
Correction of the dose in patients with impaired renal function is not required.

Correction of the dose in patients with mild to moderate degree of liver dysfunction is not required.

SIDE EFFECT

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 1/10 000, less than 1/1000); very rarely (less than 1/10 000), including individual reports.
From the cardiovascular system: very often - flushes of blood to the face.

From the musculoskeletal system: very often - arthralgia;
rarely a trigger finger. Reception 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.
On the part of the reproductive system: often - dryness of the mucous membrane of the vagina, vaginal bleeding (mainly during the first weeks after reversing or changing the previous hormonal therapy for anastrozole).

From the skin and skin appendages: very often - skin rash;
often thinning hair, alopecia; very rarely - erythema multiforme (Stevens-Johnson syndrome).
From the side of the digestive system: very often - nausea;
often - diarrhea, vomiting, anorexia, increased activity of ALT, AST, APF; rarely - increased activity of GGT, hyperbilirubinemia, hepatitis.
From the nervous system: very often - headache;
often - increased drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors for this disease).
Allergic reactions: often - allergic reactions;
very rarely - anaphylactoid reactions, angioedema, hives, anaphylactic shock.
Other: very often - asthenia;
often - hypercholesterolemia.
CONTRAINDICATIONS

- Pregnancy;

- the period of breastfeeding;

- pre-menopause;

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

- concomitant therapy with tamoxifen or preparations containing estrogens;

- Children's age (safety and efficacy not established);

- Hypersensitivity to anastrozole or other components of the drug.

With caution: osteoporosis, hypercholesterolemia, IHD, impaired hepatic function, renal failure of severe degree (CC less than 20 ml / min), lactase insufficiency, lactose intolerance, glucose malabsorption / galactose syndrome (the drug contains lactose).

PREGNANCY AND LACTATION

The drug is contraindicated in pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution: renal failure of severe degree (CK less than 20 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution: a violation of the liver.

APPLICATION FOR CHILDREN

Contraindication: child age (safety and efficacy not established).

APPLICATION IN ELDERLY PATIENTS

The application is possible according to the dosing regimen.

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 impairment.

Since anastrozole reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density.
Therefore, in patients with osteoporosis or an increased risk of osteoporosis, the bone mineral density should be assessed by the method of densitometry, for example, 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. 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 usefulness for prevention.
There is no data on the simultaneous use of anastrozole and GnRH analogues.

With receptor-negative breast cancer or with ineffectiveness of previous therapy with tamoxifen, the efficacy of anastrozole is low.

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.

Influence on the ability to drive and drive machinery

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.
OVERDOSE

Single cases of accidental drug overdose are described.
A single dose of anastrozole, which could lead to life-threatening symptoms is not established.
Treatment: there is no specific antidote, in case of an overdose, treatment should be symptomatic.
You can induce vomiting if the patient is conscious. Dialysis is possible. General supportive therapy, patient monitoring and monitoring of vital organs and systems are recommended.
DRUG INTERACTION

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.

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

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

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 30 ° C.
Shelf life - 4 years. Do not use after the expiration date printed on the package.
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