Expiration date: 05/2025
Composition
1 tablet contains:
Active substances: anastrozole 1 mg.
Excipients: lactose monohydrate (200 mesh), lactose monohydrate (spray dried), povidone K30, sodium carboxymethyl starch (type A), magnesium stearate.
The composition of the film shell: opadray white 02G28619 (hypromellose (E464), titanium dioxide (E171), macrogol 6000, macrogol 400).
Packaging
28 pcs.
Pharmacological action
Pharmacodynamics
Antitumor drug, an inhibitor of estrogen synthesis.
Anastrozole is a highly selective nonsteroidal aromatase inhibitor, an enzyme by which androstenedione in peripheral tissues is converted into estrone and then into estradiol in postmenopausal women. 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 concentration of estradiol by 80%.
Anastrozole does not have gestagenic, 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 anastrozole, replacement administration of corticosteroids is not required.
Pharmacokinetics
Suction and distribution
After oral administration, anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is usually reached within 2 hours after oral administration (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 Css of the drug in blood plasma with a single daily dose of anastrozole.
After 7 days of taking the drug, approximately 90-95% Css of anastrozole in blood plasma is achieved. There is no information about the dependence of the pharmacokinetic parameters of anastrozole on time or dose. Binding to plasma proteins is 40%.
Metabolism and excretion
Anastrozole is extensively metabolized in postmenopausal women, while less than 10% is excreted unchanged by the kidneys within 72 hours after taking the drug. T1/2 of anastrozole from blood plasma is 40-50 h. The metabolism of anastrozole is carried out by N-dealkylation, hydroxylation and glucuronidation. Metabolites of anastrozole are excreted mainly by the kidneys. The main metabolite of anastrozole - triazole, determined in blood plasma, has no pharmacological activity.
Pharmacokinetics in special clinical cases
The pharmacokinetics of anastrozole does not depend on the age of postmenopausal women.
Clearance of anastrozole after oral administration with cirrhosis of the liver or impaired renal function does not change.
Indications
Adjuvant therapy of early breast cancer with positive hormonal receptors in postmenopausal women, the
first line of therapy for locally advanced breast cancer, with positive or unknown hormonal receptors in postmenopausal women, the
second line of therapy for advanced breast cancer progressing after tamoxifen treatment.
Contraindications
Premenopausal period,
severe liver failure (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 anastrozole or other components of the drug.
With caution: the drug should be prescribed for osteoporosis, hypercholesterolemia, coronary heart disease, impaired liver function, severe renal insufficiency (CC <, 20 ml / min), lactase insufficiency, lactose intolerance, glucose / galactose malabsorption (the dosage form of the drug contains lactose).
Use during pregnancy and lactation
It is contraindicated to prescribe the drug during pregnancy and lactation.
Method of administration 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 the meal.
Adults, including the elderly, are prescribed 1 mg orally 1 time / day for a long time. If signs of disease progression appear, the drug should be discontinued. As adjuvant therapy, the recommended duration of treatment is 5 years.
In case of impaired renal function, dose adjustment is not required.
Dose adjustment in patients with mild to moderate hepatic impairment is not required.
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 rarely ( <, 1/10 000), including individual messages.
From the cardiovascular system: very often - flushes of blood to the face.
From the musculoskeletal system: very often - arthralgia, rarely - 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 replacement of previous hormone therapy with anastrozole).
Dermatological reactions: very often - skin rash, often - thinning of hair, alopecia, very rarely - polymorphic erythema (Stevens-Johnson syndrome).
From the digestive system: very often - nausea, often - diarrhea, vomiting, anorexia.
From the hepatobiliary system: increased activity of ALT, AST and alkaline phosphatase, rarely - increased activity of GGT 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.
Drug interaction
Studies on drug interaction with antipyrine and cimetidine indicate that clinically significant drug interaction mediated by cytochrome P450 isoenzymes with the combined use of anastrozole with other drugs is unlikely. There is no clinically significant drug interaction when using anastrozole simultaneously with other commonly prescribed drugs. At the moment there is no information about the use of anastrozole in combination with other antitumor drugs. Drugs containing estrogens reduce the pharmacological effect of anastrozole, therefore, they should not be prescribed simultaneously with anastrozole. Tamoxifen should not be prescribed simultaneously with anastrozole, since it can weaken the pharmacological effect of the latter.
Storage conditions
Keep out of reach of children, in a dry place at a temperature not exceeding 25 ° C.
