Anastrozolee pills 0,001g, 30pcs

Composition

Active ingredients:

Anastrozolee 1 mg.

Auxiliary substances:

lactose monohydrate 72 mg,

microcrystalline cellulose 15.6 mg,

povidone 3 mg,

magnesium stearate 0.9 mg,

colloidal silicon dioxide 0.5 mg,

sodium carboxymethyl starch 2 mg.

Composition of the film shell:

hypromellose 1.65 mg,

macrogol-4000 0.45 mg,

titanium dioxide 0.9 mg

Pharmacological action

Pharmacodynamics

Antitumor drug. Highly selective nonsteroidal aromatase inhibitor, an enzyme that converts androstenedione in peripheral tissues to estrone and then to estradiol in postmenopausal women. Anastrozolee does not have progestogenic, androgenic and estrogenic activity.

In postmenopausal women, Anastrozolee in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Anastrozolee in daily doses up to 10 mg has no effect on the secretion of cortisol and aldosterone.

Pharmacokinetics

Suction and distribution

Anastrozolee after oral use on an empty stomach is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 hours. Food slightly reduces the rate of absorption (but not its degree) and does not lead to a clinically significant effect on the Css of the drug in plasma with a single daily dose of Anastrozolee. After 7-day use of the drug, the Css of Anastrozolee in plasma is approximately 90-95%. Binding to plasma proteins is 40%.

Metabolism and elimination

Anastrozolee is metabolized by N-dealkylation, hydroxylation, and glucuronidation. Triazole, the main metabolite detected in plasma, does not inhibit aromatase.

T1 / 2 from plasma is 40-50 hours. Less than 10% of the dose is excreted unchanged in the urine within 72 hours after taking the drug. Metabolites are mainly excreted in the urine.

Pharmacokinetics in special clinical cases

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

Indications

Advanced breast cancer in postmenopausal women.

Contraindications

• Severe renal insufficiency (creatinine clearance < 20 ml / min);
• moderate or severe hepatic insufficiency (safety and efficacy of the drug have not been established);
• concomitant tamoxifen therapy;
• premenopause;
• pregnancy;
• breast-feeding;
• childhood;
• hypersensitivity to Anastrozolee or other components of the drug.

Side effects

Determination of the frequency of adverse reactions:

• very common (> 10%);>
• common (1-10%);
• rare (0.1-1%);
• very rare (

From the reproductive system: often-vaginal dryness; rarely-vaginal bleeding (mainly during the first weeks after the withdrawal or change of previous hormone therapy to Anastrozolee).

From the digestive system: often – nausea, diarrhea; rarely-anorexia, vomiting, increased activity of GGT and alkaline phosphatase.

From the cardiovascular system: very often – “hot flashes” of heat.

From the central nervous system: often-headache; rarely-drowsiness.

From the musculoskeletal system: often-arthralgia.

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

From the side of metabolism: rarely-hypercholesterolemia; possibly-a decrease in bone mineral density due to a decrease in the level of circulating estradiol (risk of osteoporosis, bone fractures).

Other: often-asthenia; very rarely-allergic reactions (including angioedema, urticaria, anaphylactic shock).

Interaction

Studies on drug interactions with antipyrine and cimetidine indicate that a clinically significant drug interaction mediated by cytochrome P450 isoenzymes is unlikely when Anastrozolee is co-administered with other drugs.

There is no clinically significant drug interaction when using 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

Adults, including elderly patients, should take the drug orally at the same time at 1 mg (swallow the tablet whole, washed down with water) 1 time/day for a long time. If there are signs of disease progression, the drug should be discontinued.

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

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

Overdose

Symptoms: A single dose of Anastrozolee that could lead to life-threatening symptoms has not been determined.

Treatment: in case of overdose, treatment should be symptomatic.

If the patient is conscious, it is advisable to induce vomiting.

General maintenance therapy, monitoring of the patient and monitoring of the function of vital organs and systems are recommended. Dialysis may be performed. There is no specific antidote.

Special instructions

In women with an estrogen-receptor-negative tumor, Anastrozolee has not been shown to be effective, 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 use of Anastrozolee in patients with severe hepatic impairment or in patients with severe renal impairment (CC

If uterine bleeding persists while taking Anastrozolee, a gynecologist should be consulted and monitored.

Preparations containing estrogens should not be used simultaneously with Anastrozolee, since they will neutralize the pharmacological effect of the latter.

By reducing the level of circulating estradiol, Anastrozolee 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, you should start treatment or carry out prevention of osteoporosis under the close supervision of a doctor.

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

It is not known whether Anastrozolee improves the results of treatment when used together with chemotherapy.

Use in pediatrics

The drug is contraindicated in pediatric patients.

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

Some side effects 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

Keep out of reach of children in a dry place at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Anastrozolee

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Cancer, Breast Cancer