Anastrozole San - instructions for use, dose, side effects, contraindications

Anastrozole is a highly selective nonsteroidal an aromatase inhibitor, an enzyme that, with post-menopausal women, androstenedione in peripheral tissues is converted to estrone and further into estradiol. In postmenopausal women anastrozole in a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%.

Anastrozole does not possess progestogen, androgenic and estrogenic activity. Anastrozole in daily doses up to 10 mg does not have an effect on the secretion of cortisol and aldosterone.

Pharmacokinetics:

Absorption of anastrozole is fast, the maximum concentration in the blood plasma is reached within 2 hours after ingestion (on an empty stomach). Food intake slightly reduces the rate of absorption, but not 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.

Connection with blood plasma proteins - 40%.

The half-life of plasma is about 50 hours. Less than 10% of the dose is excreted by the kidneys unchanged within 72 hours after taking the drug. Metabolism of anastrozole is carried out-N-dealkylation, hydroxylation and glucuronization. Metabolites (triazole, glucuronic conjugate of hydroxyanafactose and glucuron conjugate of anastrozole) are excreted mainly in the urine. Triazole - the main metabolite, determined in blood plasma, does not inhibit aromatase. The clearance of anastrozole after oral administration with liver cirrhosis or renal dysfunction does not change.

Indications:

Adjuvant therapy for early breast cancer, with positive hormonal receptors in postmenopausal women. including, after adjuvant therapy with tamoxifen for 2-3 years.

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, in postmenopausal women.

Contraindications:

Hypersensitivity to anastrozole or other components of the drug;

The Premenopausal Period;

Severe hepatic impairment (safety and efficacy not established);

Complementary therapy with tamoxifen or preparations containing estrogens;

Pregnancy and the period of breastfeeding;

Child age (safety and efficacy not established).

Carefully:

With CAUTION is accepted for osteoporosis, hypercholesterolemia, ischemic heart disease, impaired function liver, lactase deficiency,

lactose intolerance, glucose-galactose malabsorption.

Pregnancy and lactation:The use of the drug during pregnancy and lactation is contraindicated.

Dosing and Administration:

Inside. Swallow the whole tablet with water. It is recommended to take the drug at the same time.

Adults, including elderly: 1 mg orally once a day for a long time.

Impaired renal function: dose adjustment in patients with mild to moderate renal impairment is not required.

Dysfunction of the liver: dose adjustment in patients with mild impairment liver function is not required.

The duration of treatment depends on the form and severity of the disease (with adjuvant therapy, the recommended duration of treatment is 5 years). If signs of disease progression appear, the drug should be discontinued.

Side effects:

Determination of the frequency of adverse reactions: very often (more than or equal to 1/10); often (more than 1/100, less than 1/10); infrequently (more than 1/1000 less than 1/100), rarely (more than 1/10000, less than 1/1000); very rarely (less than 1/10000), including individual messages.

From the side of the vessels Often "Tides" of blood to the face.

From the side of the musculoskeletal and connective tissue: Often - arthralgia / joint stiffness, arthritis; often - pain in the bones, myalgia; infrequently - a trigger finger.

From the genitals and the breast: 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 side of the rut and subcutaneous tissues: very often - skin rash; often thinning hair, alopecia, allergic reactions; infrequently - hives; rarely - erythema multiforme, anaphylactoid reaction, skin vasculitis (including individual cases of purpura (Shenlaine-Henoch syndrome)); very rarely - Stevens-Johnson syndrome, angioedema.

From the gastrointestinal tract: very often - nausea; often - diarrhea, vomiting.

From the liver and bile ducts: often - increased activity Alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase; infrequently - increased activity of gamma-glutamyltransferase and bilirubin concentration, hepatitis.

From the nervous system: very often - headache; often - drowsiness, carpal tunnel syndrome (mainly observed in patients with risk factors of the disease), sensitivity disorders (including paresthesia, loss or perversion of taste sensations).

From the side of metabolism and nutrition: often - anorexia, hypercholesterolemia; infrequently - hypercalcemia (with / without increasing the concentration of parathyroid hormone). Admission of the drug may 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.

General disorders: very often - asthenia of mild to moderate severity.

Adverse events noted in clinical trials that are not associated with anastrozole use: anemia, constipation, dyspepsia, back pain, abdominal pain, increased blood pressure, weight gain, depression, insomnia, dizziness, anxiety, paresthesia.

Overdose:

Symptoms: A single dose of anastrozole, which could lead to symptoms, threatening life is not established.

Treatment: There is no specific antidote; when overdose treatment should be symptomatic. You can induce vomiting if the patient is conscious. Dialysis may be performed. General supportive therapy is recommended, Monitoring the patient and monitoring the function of vital organs and systems.

Interaction:

Clinically significant drug interaction with anastrozole administration simultaneously from other often prescribed drugs are absent.

Studies on the drug interaction with phenazone and cimetidine suggest that the combined use of anastrozole with other drugs with a low probability will lead to a clinically significant drug interaction mediated by cytochrome P450. 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 assign tamoxifen simultaneously with anastrozole, because it can weaken the pharmacological action of the latter.

Special instructions:

In women with a receptor-negative tumor to estrogens, the efficacy of anastrozole was not demonstrated, except in cases where there was a prior positive clinical response to tamoxifen.

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

There is no data on the use of anastrozole in patients with severe disorders liver function or in patients with severe renal dysfunction (creatinine clearance less than 20 ml / min).

Preparations containing estrogens should not be administered simultaneously with anastrozole, since these drugs will neutralize its pharmacological act. Reducing the concentration of circulating estradiol, anastrozole can cause a decrease in bone mineral density.

In patients suffering from osteoporosis or having a risk of osteoporosis, bone mineral density should be assessed by densitometry at the beginning of treatment and in dynamics. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a physician.

It is not known whether anastrozole results of treatment when used in conjunction with chemotherapy.

With the preservation of metrorrhagia against the background of treatment, a consultation with a gynecologist is necessary.

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 perform potentially dangerous species Activities that require increased concentration and speed of psychomotor reactions. In this regard, it is recommended that when these symptoms occur take care when driving vehicles and mechanisms.

Form release / dosage:

Tablets, film-coated 1 mg.

Packaging:

5 tablets in a blister made of PVC film and aluminum foil. For 5 blisters together with instructions for use are placed in a cardboard box.

For 14 tablets in a blister made of PVC film and aluminum foil. Two blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001327

Date of registration:06.12.2011

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp27.02.2015

Illustrated instructions

Instructions

Anastrozole San (Anastrozole Sun)