ANAMASTEN - instructions for use, doses, side effects, contraindications

Anastrozole is a hormonal antitumor drug. It is a highly selective inhibitor of aromatase - an enzyme, with which in postmenopausal women Androstenedione in peripheral tissues is converted into estrone and further into estradiol. Reducing the concentration of circulating estradiol in patients with breast cancer has a therapeutic effect. 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 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:

After oral administration anastrozole quickly absorbed from the gastrointestinal tract. The maximum concentration (C_m_Oh) in the blood plasma is usually achieved within 2 hours after ingestion (fasting). Food intake slightly reduces the rate of absorption, but does not affect the degree of absorption and does not lead to a clinically significant effect on the equilibrium concentration of the drug in the blood plasma with a single daily intake of anastrozole. After 7 days of taking the drug, approximately 90-95% of the equilibrium concentration of anastrozole in the blood plasma is reached. 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, the pharmacokinetics in children have not been studied.

Connection with blood plasma proteins - 40%. Anastrozole is output slowly, the half-life (T_1/2) - 40-50 hours. Less than 10% of the dose is excreted by the kidneys unchanged for 72 hours after ingestion. Anastrozole metabolism is carried out N-dealkylation, hydroxylation and glucuronization. Metabolites are excreted mainly by the kidneys.Triazole, the main metabolite, determined in blood plasma, does not have pharmacological activity. The clearance of anastrozole after ingestion with cirrhosis of the liver or renal dysfunction does not change.

Indications:

- Adjuvant therapy for early breast cancer, with positive hormonal receptors in postmenopausal women.

- 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 treatment with tamoxifen.

Contraindications:

- Hypersensitivity to anastrozole or other components of the drug.

- The Premenopausal Period.

- Moderate or severe degree of hepatic impairment (efficacy and safety not established).

- Concomitant therapy with tamoxifen or estrogens.

- Pregnancy and the period of breastfeeding.

- Age under 18 years (safety and efficacy not established).

Carefully:Osteoporosis, hypercholesterolemia, ischemic heart disease, impaired liver function,severe renal failure (creatinine clearance (CC) <20 ml / min), hereditary lactose intolerance, lactase deficiency and malabsorption syndrome (lactose is contained in the drug form of the drug).

Pregnancy and lactation:

Application of the drug anastrozole during pregnancy and during breastfeeding is contraindicated.

At the time of drug treatment anastrozole should stop breastfeeding.

Dosing and Administration:

Inside. Swallow the whole tablet with water. It is recommended to take the drug at the same time of the day, regardless of food intake.

Adults, including the elderly - 1 tablet once a 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.

Renal impairment: dose adjustment is not required in patients with impaired renal function (QC more than 20 ml / min).

Dysfunction of the liver: dose adjustment is not required in patients with mild liver function abnormalities, and in patients with moderate and severe impairment of liver function, the drug intake anastrozole contraindicated (see section "Contraindications").

Side effects:

The incidence of side effects noted with anastrozole is given in accordance with the classification of the World Health Organization (WHO): very often - 1/10 appointments (> 10%), often - 1/100 appointments (> 1% and <10%), infrequently - 1/1000 appointments (> 0.1% and <1%), rarely - 1/10000 appointments (> 0.01% and <0.1%), very rarely - 1/10000 prescriptions (<0.01 %), including individual messages.

From the cardiovascular system: very often - "hot flashes" to the skin of the face; feeling of heat.

From the musculoskeletal system: very often - arthralgia; infrequently - "trigger finger".

On the part of the reproductive system: 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: very often - skin rash; often thinning hair (alopecia); very rarely - polymorphic erythema (Stevens-Johnson syndrome).

From the digestive system: very often - nausea; often - diarrhea, vomiting, anorexia, increased activity of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamintransferase, bilirubin, hepatitis.

From the nervous system: very often - headache, asthenia; often - drowsiness, carpal tunnel syndrome (mainly in patients with risk factors for this disease).

From the side of metabolism: rarely - hypercholesterolemia. Admission of the drug can cause a decrease in bone mineral density due to a decrease in the level of circulating estradiol, thereby increasing the risk of osteoporosis and bone fracture.

Allergic reactions: very rarely - angioedema, hives and anaphylactic shock.

Overdose:

Single clinical cases of drug overdose are described. A single dose of anastrozole, which could lead to symptoms threatening life, is not established.

Treatment: symptomatic therapy. There is no specific antidote. You can induce vomiting if the patient is conscious. Dialysis is possible.

Interaction:

Studies on drug interactions 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 the cytochrome P450 system.

Clinically significant interaction with the administration of anastrozole at the same time as other commonly used drugs is absent.

At present, 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 used simultaneously with anastrozole.

Do not use tamoxifen simultaneously with anastrozole, since it can weaken the pharmacological action of the latter.

Special instructions:

Safety and efficacy in children is not established.

In women with a receptor-negative tumor to estrogens, the efficacy of anastrozole has not been demonstrated, except in cases when a positive therapeutic effect of tamoxifen has been previously noted.

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.

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

Preparations containing estrogens should not be used concomitantly with anastrozole. these drugs will neutralize its pharmacological action.

In patients with osteoporosis or who are at risk for developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXAscan) at the beginning of treatment and during the therapy with anastrozole. If necessary, treatment or prevention of osteoporosis under the supervision of a physician should be initiated.

Because the anastrozole reduces the levels of circulating estrogen, this can lead to a decrease in bone mineral density. To date, there is insufficient data on the positive effects of bisphosphonates on the loss of mineral bone density caused by anastrozole or their benefits when used for the purpose of prevention.

There is no evidence of simultaneous use of anastrozole and analogue-releasing hormone-releasing hormone (LHRH) hormone. 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 the results of treatment when combined with chemotherapy.

Effect on the ability to drive transp. cf. and fur:

Some side effects of anastrozole, such as asthenia and drowsiness, can adversely affect the ability to drive vehicles and other mechanisms that require increased concentration and speed of the speed of psychomotor reactions. In this regard, it is recommended that when these symptoms occur, use caution when operating vehicles or mechanisms that require increased concentration.

Form release / dosage:

Tablets, film-coated, 1 mg.

Packaging:For 14 tablets in a planar cell package. For 1 or 2 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000589

Date of registration:21.09.2011 / 11.09.2012

Expiration Date:21.09.2016

The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia

Manufacturer: & nbsp

SOTEKS, ZAO Russia

Information update date: & nbsp27.08.2017

Illustrated instructions

Instructions

ANAMASTEN® (Anamasten®)