Аримидекс

General characteristics. Structure:

1 tablet, film coated, contains:
active agent: анастрозол 1,0 mg
excipients: lactoses monohydrate of 93,0 mg, povidone of 2,0 mg, carboxymethylstarch of sodium of 3,0 mg, magnesium stearate of 1,0 mg
structure of a film cover: gipromelloza of 1,50 mg, macrogoal of 300 0,30 mg, titanium dioxide of 0,45 mg
Description
Round, biconvex tablets of white color, film coated; with an engraving And – on one party and Adx on another.

Pharmacological properties:

Pharmacodynamics. Аримидекс® is the high-selection nonsteroid inhibitor of aromatase - enzyme by means of which at women in a postmenopause androstendion in peripheral fabrics turns into estrone and further into oestradiol. Decrease in level of the circulating oestradiol at patients with cancer of a mammary gland renders therapeutic effect. In a postmenopause of Arimideks® in a daily dose of 1 mg causes decrease in level of oestradiol by 80% in women.
Аримидекс® has no progestogenny, androgenic and oestrogenic activity.
Аримидекс® in daily doses to 10 mg does not render effect on secretion of cortisol and Aldosteronum, therefore, at use of the drug Arimideks® replaceable introduction of corticosteroids is not required.
Influence on the mineral density of a bone tissue
It is shown that at patients with a gormonopozitivny early breast cancer in a postmenopause who accept Arimideks® changes of bone system can be prevented according to the standards established for treatment of patients with a certain risk of changes. So, advantage of the drug Arimideks® in a combination from bisfosfonata (in comparison with therapy only the drug Arimideks®) at patients with average and high risk of developing of fractures was shown in 12 months on indicators of mineral bone density, structural change of a bone tissue and markers of a bone resorption. Moreover, in group of low risk change of an indicator of mineral bone density against the background of therapy by one drug Arimideks® and the supporting treatment by vitamin D and calcium was not noted.
Lipids
At therapy the drug Arimideks®, including, at inclusion in combinations from bisfosfonata, did not reveal changes of level of lipids in plasma.

Pharmacokinetics. Absorption of an anastrozol bystry, the maximum concentration in plasma is reached within 2 hours 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 drug in plasma at a single dose of a daily dose of the drug Arimideks®. After 7-day administration of drug about 90-95% of equilibrium concentration of an anastrozol in 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 brought slowly, plasma elimination half-life makes 40-50 hours. It is extensively metabolized at women in a postmenopause. Less than 10% of a dose are allocated with urine in not changed look within 72 hours after administration of drug. Metabolism of an anastrozol is carried out by N-dealkylation, a hydroxylation and a glyukuronization. Metabolites are removed preferential with urine. Triazole, the main metabolite defined in plasma does not inhibit aromatase.
The clearance of an anastrozol after oral administration at cirrhosis or a renal failure does not change.

Indications to use:

Adjuvant therapy of an early gormonopolozhitelny breast cancer in a postmenopause.
Treatment of a widespread breast cancer at women in a postmenopause. Adjuvant therapy of an early gormonopolozhitelny breast cancer at women in a postmenopause after therapy by Tamoxifenum within 2-3 years.

Route of administration and doses:

Inside. To swallow a tablet entirely, washing down with water. It is recommended to accept drug in one and too time.
Adults, including elderly: 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.
Renal failures: correction of a dose with easy and moderate renal failures is not required from patients
Abnormal liver functions: correction of a dose with easy degree of an abnormal liver function is not required from patients.

Features of use:

Safety and efficiency at children is not established.
At women with a retseptorootritsatelny tumor to estrogen efficiency of the drug Arimideks® was not shown, except those cases when there was a previous affirmative clinical answer on Tamoxifenum.
In case of doubts in the hormonal status of the patient the menopause has to be confirmed with definition of sex hormones in blood serum.
There are no data on use of the drug Arimideks® for patients with the moderated or expressed liver failure and at patients with the expressed renal failure (clearance of creatinine less than 20 ml/min.).
In case of the remaining uterine bleeding against the background of administration of drug of Arimideks® consultation and observation of the gynecologist is necessary.
The drugs containing estrogen should not be appointed along with the drug Arimideks® as these drugs will level its pharmacological action.
Reducing the level of the circulating oestradiol, Arimideks® can cause decrease in mineral density of a bone tissue with the subsequent increase in risk of a change. Patients with such high risk are subject to treatment according to the guide to therapy of these complications.
At the patients having osteoporosis or having risk of development of osteoporosis, the mineral density of a bone tissue has to be estimated by a densitometry method, for example, of DEXA scanning (Dual-Energy X-ray Absorptiometry - a two-power x-ray absorbtsiometriya), in an initiation of treatment and in dynamics. If necessary treatment or prevention of osteoporosis, under careful observation of the doctor have to be begun.
There are no data on simultaneous use of an anastrozol and drugs analogs LGRG.
It is unknown whether improves анастрозол results of treatment when sharing with chemotherapy.
Data on safety at prolonged treatment anastrozoly are not obtained yet.
At drug Arimideks® use more often than at therapy Tamoxifenum, observed ischemic diseases, however the statistical importance at the same time is noted.
Efficiency and safety of the drug Arimideks® and Tamoxifenum at their simultaneous use regardless of the status of hormonal receptors are comparable with those when using one Tamoxifenum. The exact mechanism of this phenomenon is not known yet.
Influence on ability to drive the car and other mechanisms
Some side effects of the drug Arimideks®, such as adynamy and drowsiness, can negatively influence ability of performance of potentially dangerous types of activity demanding the increased concentration, 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:

Frequency of occurrence was calculated from number undesirable the phenomena observed within the III phase of a research at 9366 post-menopausal women with a resectable breast cancer receiving treatment within 5 years, at the same time the frequency of the undesirable phenomena in groups of comparison and opinion of the researcher concerning dependence of the undesirable phenomenon on the studied drug are not considered.
Determination of frequency of side reactions: very often (more or equally to 10%); often (from 1 to less than 10%); infrequently (from 0,1 to less than 1%); seldom (from 0,01 to less than 0,1%), it is very rare (less than 0,01%)
From vascular system:
very often – inflows.
From a musculoskeletal system:
very often – arthralgia / constraint of joints, arthritis
often – an ostealgia
infrequently – a trigger finger.
From reproductive system:
often – dryness of a mucous membrane of a vagina; vulval bleedings (generally within the first weeks after cancellation or change of the previous hormonal therapy with Arimideks®).
From skin and skin appendages:
very often – skin rash, it is frequent – thinning of hair (alopecia), allergic reactions,
infrequently – a small tortoiseshell,
seldom – a multiformny erythema, anaphylactoid reaction, a skin vasculitis (including separate cases of a purpura (Shenleyna-Genokh's syndrome)),
very seldom – Stephens-Johnson's syndrome, a Quincke's disease.
From system of digestion:
very often – nausea,
often – diarrhea, vomiting.
From gepatobiliarny system:
often – increase in activity of an alkaline phosphatase, aminotransferase alanine, aminotransferase aspartate,
infrequently – increase in activity gamma глютамилтрансферазы and concentration of bilirubin, hepatitis.
From a nervous system:
very often – a headache;
often – drowsiness, a syndrome of a carpal tunnel (it was generally observed at patients with risk factors of this disease).
From metabolism:
often – anorexia, a hypercholesterolemia. Administration of drug can cause decrease in mineral density of a bone tissue in connection with decrease in concentration of the circulating oestradiol, thereby, increasing risk of developing of osteoporosis and fractures of bones.
Others:
very often – an adynamy of easy or moderate degree of manifestation.

Interaction with other medicines:

Researches on medicinal interaction with phenazone (antipyrine) and Cimetidinum indicate that combined use of the drug Arimideks® with other drugs will hardly lead to clinically significant medicinal interaction mediated by P450 cytochrome.
Clinically significant medicinal interaction at administration of drug of Arimideks® along with other often appointed drugs is absent.
At the moment there are no data on use of the drug Arimideks® in a combination with other antineoplastic drugs.
The drugs containing estrogen reduce pharmacological effect of the drug Arimideks® in this connection, they should not be appointed along with the drug Arimideks®.
It is not necessary to appoint Tamoxifenum along with the drug Arimideks® 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
At women in a premenopauza
The expressed renal failure (clearance of creatinine less than 20 ml/min.)
The moderated or expressed liver failure (safety and efficiency is not established)
The accompanying therapy by Tamoxifenum or drugs containing estrogen
Children's age (safety and efficiency at children is not established)
With care: osteoporosis, hypercholesterolemia, coronary heart disease, abnormal liver function, insufficiency of lactase, glyukozo-galaktozny malabsorption.

Overdose:

Isolated clinical cases of accidental overdose of drug are described. The single dose of the drug Arimideks® 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 function of vitals and systems is recommended.

Storage conditions:

At a temperature not above 30 °C, in the place, unavailable to children. Period of validity of 5 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 1 mg. 14 tablets in the blister from PVC Is scarlet/; on 2 blisters in a cardboard pack with the application instruction.