Анастрэкс

General characteristics. Structure:

Active ingredient: 1 mg of an anastrozol.

Pharmacological properties:

Pharmacodynamics. Anastrozol is the high-selection nonsteroid inhibitor of aromatase - enzyme by means of which at women androstendion and testosterone in fabrics turn into estrone and oestradiol respectively. Decrease in concentration of the circulating oestradiol at patients with cancer of a mammary gland renders therapeutic effect. In a postmenopause анастрозол in a daily dose of 1 mg causes decrease in concentration of oestradiol by 80% in women.

Anastrozol has no progestagenny, androgenic and oestrogenic activity. In daily doses to 10 mg does not render effect on secretion of cortisol and Aldosteronum, therefore at use of an anastrozol replaceable introduction of corticosteroids is not required.

Pharmacokinetics. After intake анастрозол it is quickly soaked up from a GIT. Cmax in a blood plasma is usually reached during 2 h after intake (on an empty stomach). Food slightly reduces the absorption speed, but not its degree and does not lead to clinically significant influence on equilibrium concentration of an anastrozol in a blood plasma at a single dose of a daily dose. After 7-day administration of drug about 90-95% of equilibrium concentration of an anastrozol in a blood plasma are reached.

There are no data on dependence of pharmacokinetic parameters of an anastrozol from time or a dose. The pharmacokinetics of an anastrozol does not depend on age of women in a postmenopause.

Communication with proteins of a blood plasma - 40%.

Anastrozol is extensively metabolized at women in a postmenopause, at the same time less than 10% are excreted by kidneys in not changed look during 72 h after administration of drug.

T1/2 of an anastrozol makes 40-50 h of a blood plasma. Metabolism of an anastrozol is carried out by N-dealkylation, a hydroxylation and a glyukuronirovaniye.

Metabolites of an anastrozol are removed preferential by kidneys. The main metabolite of an anastrozol - the triazole defined in a blood plasma has no pharmacological activity.

The clearance of an anastrozol after oral administration at cirrhosis or at a renal failure does not change.

Indications to use:

• Adjuvant therapy of an early breast cancer, with positive receptors of a gormonalnykma at women in a postmenopause.
• The first line of therapy of a locally-spread or metastatic breast cancer, with the positive or unspecified status of hormonal receptors at women in a postmenopause.
• The second line of therapy of the widespread breast cancer progressing after the previous therapy by Tamoxifenum.

Route of administration and doses:

On 1 mg in 1 times a day it is long. At emergence of signs of progressing of a disease administration of drug should be stopped. As adjuvant therapy the recommended treatment duration — 5 years.

Features of use:

In case of doubts in the hormonal status of the patient the menopause has to be confirmed with definition of concentration of sex hormones in blood serum.

In case of the remaining uterine bleeding against the background of reception of an anastrozol consultation and observation of the gynecologist is necessary.

There are no data on use of an anastrozol for patients with heavy degree of abnormal liver functions.

As анастрозол reduces concentration of the circulating oestradiol, it can lead to decrease in mineral density of a bone tissue. Therefore at patients with osteoporosis or with the increased risk of development of osteoporosis, the mineral density of a bone tissue should be estimated by a densitometry method, for example, DEXA scanning (a two-power x-ray absorbtsiometriya) in an initiation of treatment and it is regular on its extent. If necessary it is necessary to appoint treatment or prevention of osteoporosis and to watch carefully a condition of the patient. At the moment there are no sufficient data of rather positive influence of bisfosfonat on loss of mineral density of the bone tissue caused anastrozoly, or their advantage for prevention.

There are no data on simultaneous use of an anastrozol and drugs analogs GNRG.

At a retseptornegativny breast cancer or at inefficiency of the previous therapy by Tamoxifenum, efficiency of an anastrozol rather low.

The drugs containing estrogen should not be appointed along with anastrozoly as these drugs will level its pharmacological action.

Efficiency and safety of an anastrozol and Tamoxifenum at their simultaneous use regardless of the status of hormonal receptors are comparable with those at use of one Tamoxifenum. The exact mechanism of this phenomenon is not known yet.

It is unknown whether improves анастрозол results of treatment at combined use with chemotherapy.

Influence on ability to driving of the car and to control of mechanisms. Some side effects of an anastrozol, such as adynamy and drowsiness, can negatively influence ability of performance of potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. In this regard it is recommended to be careful at emergence of these symptoms at control of vehicles and mechanisms.

Side effects:

The most often observed undesirable phenomena: "inflows" of blood to the person, an arthralgia, skin rash, nausea, a headache, an adynamy.

Other often observed undesirable phenomena: dryness of a mucous membrane of a vagina, vulval bleedings, thinning of hair, an alopecia, diarrhea, vomiting, anorexia, increase in activity of alaninaminotranspherase, aspartate aminotransferase and an alkaline phosphatase, the increased drowsiness, a syndrome of a carpal tunnel, allergic reactions.

Interaction with other medicines:

Researches on medicinal interaction with phenazone and Cimetidinum indicate that combined use of an anastrozol with other drugs will hardly lead to clinically significant medicinal interaction mediated by P450 cytochrome.

At the moment there are no data on use of an anastrozol in a combination with other antineoplastic drugs.

The drugs containing estrogen reduce pharmacological action of an anastrozol in this connection they should not be appointed along with anastrozoly.

It is not necessary to appoint Tamoxifenum along with anastrozoly as it can weaken pharmacological action of the last.

Contraindications:

• Hypersensitivity to an anastrozol or other components of drug.
• Pregnancy and period of feeding by a breast.
• Premenopauza.
• The expressed liver failure.
• The accompanying therapy by Tamoxifenum or drugs containing estrogen.

With care. Osteoporosis, hypercholesterolemia, coronary heart disease, abnormal liver function, heavy renal failure (clearance of creatinine <20 ml/min.), insufficiency of lactase, lactose intolerance, glyukozo-galaktozny malabsorption.

Overdose:

Isolated cases of accidental overdose of drug are described. The single dose of an anastrozol which could lead to symptoms life-threatening, is not established.

The specific antidote does not exist, in case of overdose treatment has to be symptomatic. It is possible to induce vomiting if the patient is in consciousness. Dialysis can be carried out. The general maintenance therapy, observation of the patient and control of functions of vitals and systems is recommended.

Storage conditions:

To store in the place, dry, unavailable to children, at a temperature not above 30 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 28 or 30 tablets in strip packagings and cardboard packs.