Anastrozole-Teva, pills 1mg 28pcs

Composition

Active ingredients:

Anastrozolee 1 mg.

Auxiliary substances:

lactose monohydrate (200 mesh),

lactose monohydrate (spray dried),

povidone K 30,

sodium carboxymethyl starch (Type A),

magnesium stearate.

Composition of the film shell:

opadray white 02G28619 (hypromellose (E 464),

titanium dioxide (E 171),

macrogol 6000,

macrogol 400).

Pharmacological action

Pharmacodynamics

Antitumor drug, an inhibitor of estrogen synthesis.

Anastrozolee 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 concentration of circulating estradiol in patients with breast cancer has a therapeutic effect. In postmenopausal women, Anastrozolee in a daily dose of 1 mg causes a decrease in the concentration of estradiol by 80%.

Anastrozolee does not have progestogenic, androgenic and estrogenic activity. In daily doses up to 10 mg, it has no effect on the secretion of cortisol and aldosterone, therefore, when using Anastrozolee, no replacement use of corticosteroids is required.

Pharmacokinetics

Suction and distribution

After oral use, Anastrozolee is rapidly absorbed from the gastrointestinal tract. _cmax in blood plasma is usually 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 C_ss of the drug in blood plasma with a single daily dose of Anastrozolee.

After 7 days of taking the drug, approximately 90-95% of the C_ss of Anastrozolee in blood plasma is achieved. There is no information about the dependence of the pharmacokinetic parameters of Anastrozolee on time or dose. Binding to plasma proteins is 40%.

Metabolism and elimination

Anastrozolee is extensively metabolized in postmenopausal women, with less than 10% excreted unchanged by the kidneys within 72 hours after taking the drug. T_1/2 of Anastrozolee from blood plasma is 40-50 h. Anastrozolee is metabolized by N-dealkylation, hydroxylation, and glucuronidation. Anastrozolee metabolites are mainly excreted by the kidneys. The main metabolite of Anastrozolee – triazole, determined in blood plasma, has no pharmacological activity.

Pharmacokinetics in specific clinical cases

, the pharmacokinetics of Anastrozolee do not depend on the age of postmenopausal women.

The clearance of Anastrozolee after oral use in patients with cirrhosis of the liver or impaired renal function does not change.

Indications

• Adjuvant therapy for early breast cancer with positive hormone receptors in postmenopausal women;
• first-line therapy for locally advanced breast cancer with positive or unknown hormone receptors in postmenopausal women;
• second-line therapy for advanced breast cancer that progresses after treatment with tamoxifen.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Contraindications

• Premenopausal period;
• severe hepatic insufficiency (safety and efficacy have not been established);
• concomitant therapy with tamoxifen or drugs containing estrogens;
• pregnancy;
• lactation (breastfeeding);
• childhood (safety and efficacy in children have not been established);
• hypersensitivity to Anastrozolee or other components of the drug.

With caution: the drug should be prescribed for osteoporosis, hypercholesterolemia, CHD, impaired liver function, severe renal failure (CC

Side effects

The frequency of adverse reactions listed below was determined according to the following criteria: :

• very often (≥ 1/10);
• often ( > 1/100, > < 1/10);
• sometimes ( > 1/1000, > < 1/100);
• rarely ( > 1/10 000, >< 1/1000);
• very rare (

From the cardiovascular system: very often – flushes of blood to the face.

Musculoskeletal disorders: very common – arthralgia; rarely-trigger finger.

From the genital system: often-dryness of the vaginal mucosa, vaginal bleeding (mainly during the first weeks after the withdrawal or replacement of previous hormone therapy with Anastrozolee).

Dermatological reactions: very often-skin rash; often-thinning hair, alopecia; very rarely-erythema multiforme (Stevens-Johnson syndrome).

From the digestive system: very often-nausea; often-diarrhea, vomiting, anorexia.

From the side of the hepatobiliary system: increased ALT, AST and alkaline phosphatase activity; rarely-increased GGT activity and bilirubin concentration, hepatitis.

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

From the side of metabolism: often-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.

Allergic reactions: often-allergic reactions; very rarely-anaphylactoid reactions, angioedema, urticaria, anaphylactic shock.

Other: very often – asthenia.

Interaction

Studies on drug interactions with phenazone and cimetidine indicate that the combined use of Anastrozolee with other drugs is unlikely to lead to a clinically significant drug interaction mediated by cytochrome P 450.

There is no clinically significant drug interaction when taking Anastrozolee concomitantly with other commonly prescribed medications.

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

Preparations containing estrogens reduce the pharmacological effect of Anastrozolee, and therefore they should not be prescribed simultaneously with Anastrozolee.

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

How to take, course of use and dosage

The drug is taken orally. The tablet is swallowed whole, washed down with water. It is recommended to take the drug at the same time, regardless of food intake.

Adults, including the elderly, are 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.

If renal function is impaired, no dose adjustment is required.

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

Overdose

Symptoms: isolated clinical cases of accidental overdose of the drug are described. A single dose of Anastrozolee that could lead to life-threatening symptoms has not been determined.

Treatment: there is no specific antidote; in case of overdose, symptomatic therapy is performed. Vomiting can be induced if the patient is conscious. Dialysis may be performed. General maintenance therapy, patient monitoring, and monitoring of vital organs and systems are recommended.

Special instructions

In case of doubt about the hormonal status of the patient, menopause should be confirmed by determining the concentration of sex hormones in the blood serum. If uterine bleeding persists while taking Anastrozolee, a gynecologist should be consulted and monitored.

There are no data on the use of Anastrozolee in patients with severe hepatic impairment.

In patients with osteoporosis or at increased risk of developing osteoporosis, bone mineral density should be assessed by densitometry, such as DEXA scanning (dual-energy X-ray absorptiometry), at the beginning of treatment and regularly throughout it. If necessary, treatment or prevention of osteoporosis should be prescribed and the patient’s condition should be carefully monitored. Since Anastrozolee reduces the concentration of circulating estradiol, this can lead to a decrease in bone mineral density. At the moment, there are insufficient data on the positive effect of bisphosphonates on the loss of bone mineral density caused by Anastrozolee or their benefits when used for prevention.

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

In women with an estrogen receptor-negative tumor, the efficacy of Anastrozolee has not been demonstrated, except in cases where there was a previous positive clinical response to tamoxifen.

Drugs containing estrogens should not be administered simultaneously with Anastrozolee, as these drugs will neutralize its pharmacological effect.

The efficacy and safety of Anastrozolee 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.

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

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

Some adverse reactions of Anastrozolee, such as asthenia and drowsiness, can negatively affect the ability to perform potentially dangerous activities that require increased concentration and speed of psychomotor reactions. In this regard, it is recommended to use caution when driving vehicles and 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