Arimidex, 1mg pills, 28pcs

Composition

Active ingredients:

Anastrozolee 1 mg.

Auxiliary substances:

lactose monohydrate,

povidone,

sodium carboxymethylene starch,

magnesium stearate,

purified water.

Shell composition:

macrogol 300, hypromellose, titanium dioxide, purified water.

Pharmacological action

Arimidex is a highly selective nonsteroidal aromatase inhibitor, an enzyme that converts androstenedione in peripheral tissues to estrone and then to estradiol in postmenopausal women. Reducing the level of circulating estradiol in breast cancer patients has a therapeutic effect. In postmenopausal women, the drug in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. The drug does not have progestogenic, androgenic and estrogenic activity. The drug in daily doses up to. 10 mg has no effect on the secretion of cortisol and aldosterone, therefore, when using the drug, no replacement use of corticosteroids is required. Effect on bone mineral density. It has been shown that in patients with hormone-positive early postmenopausal breast cancer who take the drug, changes in the bone system can be prevented in accordance with the standards established for the treatment of patients with a certain risk of fractures. Thus, the advantage of the drug in combination with bisphosphonates (compared with Arimidex alone) in patients with moderate to high risk of fractures was demonstrated after 12 months in terms of bone mineral density, structural changes in ‘bone tissue’ and markers of bone resorption. Moreover, in the low-risk group, there was no change in the bone mineral density index against the background of therapy with one drug and maintenance treatment with vitamin D and calcium. Lipids. During therapy with the drug, including when taken in combination with bisphosphonates; no changes in the level of lipids in plasma were detected. Pharmacokinetics. Absorption of Anastrozolee is rapid, the maximum plasma concentration is reached within 2 hours after oral use (on an empty stomach). Food slightly reduces the rate of absorption, but not its degree, and does not lead to a clinically significant effect on the steady-state concentration of the drug in plasma with a single daily dose of the drug. After 7 days of taking the drug, approximately 90-95% of the steady-state plasma concentration of Anastrozolee is reached. There is no information about the dependence of the pharmacokinetic parameters of Anastrozolee on time or dose. The pharmacokinetics of Anastrozolee do not depend on the age of postmenopausal women. Binding to plasma proteins is 40%. Anastrozolee is slowly excreted, with a plasma half-life of 40-50 hours. Extensively metabolized in postmenopausal women. Less than 10% of the dose is excreted unchanged in the urine within 72 hours after taking the drug. Anastrozolee is metabolized by N-dealkylation, hydroxylation, and glucuronidation. Metabolites are mainly excreted in the urine. Triazole, the main metabolite detected in plasma, does not inhibit aromatase. Clearance of Anastrozolee after oral use in patients with cirrhosis of the liver or impaired renal function does not change.

Indications

• Adjuvant therapy of early hormone-positive breast cancer in postmenopausal women;
• treatment of advanced breast cancer in postmenopausal women;
• adjuvant therapy of early hormone-positive breast cancer in postmenopausal women after tamoxifen therapy for 2-3 years.

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Contraindications

Hypersensitivity to Anastrozolee or other components of the drug. Pregnancy and lactation. In premenopausal women. Severe renal insufficiency (creatinine clearance less than 20 ml / min)Moderate or severe hepatic insufficiency (safety and efficacy have not been established). Concomitant therapy with tamoxifen or drugs containing estrogens. Children’s age (safety and efficacy in children have not been established).

Side effects

On the part of the reproductive system: often-dryness of the vaginal mucosa; vaginal bleeding (mainly during the first weeks after the withdrawal or change of previous hormone therapy to Arimidex®). From the skin and skin appendages: very often-skin rash; often-thinning hair (alopecia), allergic reactions; infrequently-urticaria; rarely-erythema multiforme, anaphylactoid reaction, cutaneous vasculitis (including isolated cases of purpura (Schonlein-Henoch syndrome)); very rarely – Stevens-Johnson syndrome, angioedema. From the digestive system: very often-nausea; often-diarrhea, vomiting. From the side of the hepatobiliary system: often-increased activity of 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 for this disease). From the side of metabolism: often – anorexia, hypercholesterolemia. Taking 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. From the vascular system: very often – hot flashes. Musculoskeletal disorders: very common – arthralgia/joint stiffness, arthritis; often-bone pain; infrequently-trigger finger. Other: very often – asthenia of mild or moderate severity.

Interaction

Clinical studies on drug interactions with antipyrine and cimetidine indicate that co-use of Arimidex with other drugs is unlikely to lead to a clinically significant interaction due to cytochrome P450.

There is no clinically significant drug interaction when Arimidex is administered concomitantly with other commonly prescribed medications.

Currently, there is no information about the use of Arimidex in combination with other antitumor drugs.

Preparations containing estrogens should not be administered simultaneously with Arimidex, as they reduce the pharmacological effect of the latter.

Tamoxifen should not be administered concomitantly with Arimidex, as it may weaken the pharmacological effect of the latter.

How to take, course of use and dosage

Adults, including elderly patients, the drug is prescribed 1 mg orally 1 time / day, for a long time. If there are signs of disease progression, the drug should be discontinued. As adjuvant therapy, the recommended duration of treatment is 5 years.

No dose adjustment is required in patients with mild to moderate renal impairment.

No dose adjustment is required in patients with mild hepatic impairment.

The tablet should be swallowed whole and washed down with water. It is recommended to take the drug at the same time of day.

Overdose

Isolated clinical cases of accidental overdose of the drug are described. A single dose of the drug that could lead to life-threatening symptoms has not been determined. There is no specific antidote, and in case of overdose, treatment should be symptomatic. You can induce vomiting if the patient is conscious. Dialysis can be performed. General maintenance therapy, patient monitoring, and monitoring of the function of vital organs and systems are recommended.

Special instructions

Arimidex has not been shown to be effective in women with an estrogen receptor-negative tumor, except in cases where there has been a previous positive clinical response to tamoxifen.

In case of doubt about the hormonal status of the patient, menopause should be confirmed by the determination of sex hormones in the blood serum.

There are no data on the safety of Arimidex in patients with severe hepatic impairment or in patients with severe renal insufficiency (creatinine clearance less than 20 ml / min).

In case of persistent uterine bleeding while taking Arimidex, a gynecologist should be consulted and monitored.

Preparations containing estrogens should not be administered simultaneously with Arimidex.

By reducing the level of circulating estradiol, Arimidex can cause a decrease in bone mineral density.

In patients with osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed by densometry (for example, DEXA scanning) at the beginning of treatment and over time. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a doctor.

There are no data on the concomitant use of Anastrozolee and GnRH analogs.

It is not known whether Anastrozolee improves treatment outcomes when used together with chemotherapy.

Safety data for long-term treatment with Anastrozolee have not yet been obtained.

When using Arimidex more often than with tamoxifen therapy, ischemic diseases were observed, but no statistical significance was noted.

The efficacy and safety of Arimidex and tamoxifen when used simultaneously, regardless of the status of hormone receptors, are comparable to those when using tamoxifen alone. The exact mechanism of this phenomenon is not yet known.

Use in pediatrics

The safety and efficacy of the drug in children have not been established.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Some side effects of Arimidex, such as asthenia and drowsiness, can negatively affect the ability to perform work that requires increased concentration and speed of psychomotor reactions. In this regard, it is recommended to use caution when driving a car or moving mechanisms when these symptoms occur.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Anastrozolee

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Cancer, Breast Cancer