Аксастрол®

General characteristics. Structure:

Active ingredient: 1 mg of an anastrozol.

Excipients: lactoses monohydrate, starch corn, K30 povidone, cellulose microcrystallic pH102, starch sodium glycollate (type A), silicon dioxide colloid anhydrous, magnesium stearate, talc.

Structure of a cover: gipromelloza 5spz, macrogoal 400, titanium dioxide (E171), talc.

Drug of antineoplastic action.

Pharmacological properties:

Pharmacodynamics. is strong and high-selection nonsteroid inhibitor of aromatase. At women in the postmenopauzny period oestradiol is produced, generally thanks to conversion of androstendion in estrone through an aromatazno-enzymatic complex in peripheral fabrics. Estrone turns further into oestradiol. Decrease in the circulating concentration of oestradiol as it became clear, has positive effect on women with a breast cancer. At women in the postmenopauzny period анастрозол in a daily dose of 1 mg suppressed oestradiol level more than for 80%. Has no progestagenny, androgenic or oestrogenic activity.

Pharmacokinetics. The pharmacokinetics of an anastrozol does not depend on age of women in the postmenopauzny period.

Absorption of an anastrozol, active agent of Aksastrol, – high (after intake 83-85% of the accepted dose are soaked up). The maximum concentration in plasma is usually reached within two hours after reception if medicine was taken on an empty stomach. Food reduces the absorption speed, but not its degree a little. Little change of speed of absorption does not result in clinically significant effect of achievement of equilibrium concentration of an anastrozol in plasma at reception of a single daily dose of Aksastrol in tablets. After reception of 7 daily doses concentration of an anastrozol in plasma makes 90-95% of equilibrium concentration. There are no confirmations of dependence of pharmacokinetic parameters of an anastrozol "time dose".

Anastrozol for 40% contacts proteins of plasma.

Anastrozol is intensively metabolized at women in the postmenopauzny period, less than 10% of the accepted dose are allocated in not changed view with urine within 72 hours after reception. Metabolism of an anastrozol happens through stages of Ndezalkilirovaniya, a hydroxylation and conjugation to glucuronic acid. Triazole, the main metabolite of an anastrozol in plasma, has no inhibiting effect on enzyme aromatase. Metabolites are allocated mainly with urine.

Anastrozol is brought slowly, eliminative plasma elimination half-life makes 40-50 hours.

With stable cirrhosis or a renal failure the clearance of an anastrozol after oral administration remained with volunteers in the limits observed at healthy volunteers.

Indications to use:

— treatment of a widespread breast cancer at women in a postmenopause. At patients with negative test result on receptors to estrogen Aksastrol's efficiency was not shown, except those cases when there was a previous affirmative clinical answer on Tamoxifenum;

— an early gormonopolozhitelny breast cancer at women in a postmenopause (adjuvant therapy);

— an early gormonopolozhitelny breast cancer at women in a postmenopause after therapy by Tamoxifenum within 2-3 years (adjuvant therapy).

Route of administration and doses:

The adult, including elderly, appoint on 1 mg in 1 times/days. Duration of treatment depends on a form and disease severity. At emergence of signs of progressing of a disease administration of drug should be stopped.

Correction of a dose is not required to patients with an easy or moderate form of a renal failure.

Correction of a dose is not required to patients with an easy form of a liver failure.

Features of use:

Drug is contraindicated at pregnancy and in the period of a lactation.

Approach of a menopause has to be confirmed by means of biochemical analysis if the hormonal status of the patient cannot be established by means of clinical methods.

At moderately expressed renal failures of dose adjustment it is not required.

Patients with osteoporosis or with risk of developing of this disease need to carry out check of density of bones by a densitometry method at the beginning of therapy and then through regular intervals. If it is necessary, it is recommended to carry out preventive and adjuvant therapy under strict medical control.

There are no data on a concomitant use of drug with analogs of luteinizing rileasing-hormone, therefore, this combination has to be limited to use in the conditions of clinical trials.

At preservation of a metrorrhagia against the background of treatment consultation of the gynecologist is necessary.

Aksastrol's tablets contain lactose. Patients with rare inborn intolerance of a galactose, deficit of lapp lactase or malabsorption of glucose galactose cannot appoint this drug.

During treatment it is necessary to be careful during the driving of transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From TsNS: a headache, a syndrome of a carpal tunnel (generally at patients with risk factors on this disease), drowsiness.

From the alimentary system: anorexia, nausea, vomiting, diarrhea, increase in activity of ShchF and GGT.

From a musculoskeletal system: an arthralgia, decrease in mineral density of a bone tissue with increase in risk of development of osteoporosis and fractures of bones.

From a reproductive system: dryness of a vagina, vaginal bleeding.

Allergic reactions: skin rash, small tortoiseshell, Quincke's disease, acute anaphylaxis, polymorphic erythema, Stephens-Johnson's syndrome.

Others: rushes of blood, thinning of hair, hypercholesterolemia, adynamy.

Interaction with other medicines:

Clinically significant interaction between anastrozoly and other drugs was not noted.

Tamoxifenum and/or estrogensoderzhashchy drugs should not be appointed along with Aksastrol since they can reduce his pharmacological and therapeutic action.

Contraindications:

— premenopauzny period;

— renal failure of heavy degree (KK of less than 20 ml/min.);

— the moderated or expressed insufficiency of function of a liver;

— the patients receiving treatment by estrogensoderzhashchy medicines;

— the accompanying therapy by Tamoxifenum;

— pregnancy;

— lactation period;

— children's and teenage age up to 18 years;

— hypersensitivity to an anastrozol or auxiliary components of drug.

Overdose:

The overdoses given researches anastrozoly are limited. Clinical tests were carried out with various doses of an anastrozol to 60 mg in the single dose appointed to healthy male volunteers and to 10 mg/days, to the appointed women in the postmenopauzny period with a widespread breast cancer; these doses were well transferred. The single dose of an anastrozol which could cause symptoms of threat of life was not established.

Treatment: the specific antidote does not exist, in case of overdose treatment has to be symptomatic. At treatment of overdose it is necessary to consider probability of reception also of other drug or several drugs.

If the patient is in consciousness, it is recommended to cause vomiting. Dialysis can be effective for removal of the absorbed part of drug since анастрозол does not possess high extent of linkng with proteins.

The general maintenance therapy, including frequent control of indicators of vitals and systems and careful observation of the patient is recommended.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 14 tablets in blister strip packagings, on 2 planimetric packagings in a cardboard pack.