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ANASTROZOL (ANASTROLOZOLUM) 0,25 mg. #20 tablets

ANASTROZOL (ANASTROLOZOLUM) 0,25 mg. #20 tablets

Brand: Balkan Pharmaceuticals
Product Code: anastrozol-025
Availability: In Stock
Price: $70.00
Qty:     - OR -  
1 tablet contains:
active ingredient: anastrozole - 0.25 mg and 1.0 mg;
excipients: magnesium stearate, Colledon CL (crospovidone), dye FD & C Yellow nr. 5, LudipressÃ’ (lactose, povidone, crospovidone).
Tablets of yellow color, square shape, compact and homogeneous structure, with a risk and engraving "BP" on one side, and on the other - "1" for a dose of 1.0 mg, with a bevel and rounded edges. Marbling on the surface of tablets is allowed.
Pharmacotherapeutic group and ATC code:
Antihormone, aromatase inhibitor, L02B G03.
Anastrozole belongs to a new generation of nonsteroidal aromatase inhibitors used in disseminated breast cancer in postmenopausal women. Under the influence of anastrozole, estrogen-dependent multiplication and growth of mammary gland cells are inhibited. The mechanism of action of anastrozole is associated with selective inhibition of aromatase, an enzyme of the cytochrome P450 system. The main source of circulating estrogens in postmenopausal women are androgens, primarily androstenedione and testosterone. Aromatase provides their multiple hydroxylation with transformation into estrone, and then into estradiol in adipose and muscle tissue, liver, adrenal glands and in tumor tissue. Anastrozole selectively inhibits aromatase by competitive binding to the iron atom of cytochrome P450 heme. In this way, the drug inhibits the activity of the enzyme, which leads to a maximum decrease in estrogen levels both in the peripheral bloodstream and in tumor tissues and has a therapeutic effect in patients with breast cancer. In postmenopausal women, anastrozole in a daily dose of 1 mg causes a decrease in estradiol levels by 80%. Non-steroidal inhibitors, as compared with aromatase inactivators, have a reversible effect and depend on the presence of the drug.
Anastrozole does not possess progestogenic, androgenic and estrogenic activity. The drug does not affect the secretion of cortisol and aldosterone.
After ingestion, anastozol is absorbed quickly and completely from the gastrointestinal tract. Food slightly reduces the rate of absorption, but not its degree and does not lead to a clinically significant effect on the equilibrium concentration of the drug in plasma with a single daily dose. Cmax is reached after 2 h (fasting). In blood, plasma proteins bind up to 40%. Equilibrium concentration in the blood with a daily intake is achieved in about 7 days. Information about the cumulation of the drug and the dependence of the pharmacokinetic parameters of anastrozole on time or dose no. Anastrozole is metabolized by N-dealkylation, hydroxylation and glucuronization with the formation of inactive metabolites, the main of which is triazole, which does not inhibit aromatase, but is determined in plasma and urine. Anastozol and its metabolites are excreted slowly, mainly with urine (less than 10% unchanged) within 72 hours after administration. The half-life is 40-50 hours. The clearance of anastrozole after oral administration with cirrhosis of the liver or impaired renal function does not change. The pharmacokinetics of anastrozole does not depend on the age of women in menopause.
Treatment of common forms of breast cancer in postmenopausal women (natural or artificially induced).
Breast cancer in postmenopausal women with the progression of the disease compared to other antiestrogens.
Inside Swallow the pill whole with water. It is recommended to take the drug at the same time.
In disseminated forms of breast cancer in postmenopausal women (adults and the elderly), the recommended dose of anastozol is 1.0 mg once a day, for a long time. If there is evidence of disease progression, the drug should be discontinued.
In patients with mild and moderately impaired renal function, as well as with a mild degree of liver dysfunction, dose adjustment is not required.
Anastozol can cause the following side reactions with different frequency (very often (> 10%); often (from 1 to 10%); rarely (from 0.1 to 1%); very rarely (
- on the part of the reproductive system: often - vaginal dryness; rarely, vaginal bleeding (mostly during the first weeks after the cancellation or change of previous hormonal therapy with anastrozole);
- on the part of the digestive system: often - nausea, diarrhea; rarely - anorexia, vomiting, increased activity of gamma-glutamine transferase and alkaline phosphatase;
- on the part of the vascular system: very often - “tides”;
- on the part of the nervous system: often - headache, asthenia; rarely, drowsiness;
- from the musculoskeletal system: often - arthralgia; rarely - taking the drug may cause a decrease in bone mineral density due to a decrease in circulating estradiol, thereby increasing the risk of osteoporosis and bone fractures;
- from the skin and skin appendages: often - thinning hair;
- on the part of the metabolism: rarely - hypercholesterolemia;
- allergic reactions: often - skin rash; very rarely, urticaria, polymorphic erythema, Stevens-Johnson syndrome, angioedema and anaphylactic shock.
Anastrozole is contraindicated:
- in premenopausal women;
- during pregnancy and lactation;
- with severe renal failure (Cl creatinine less than 20 ml / min);
- with moderate or severe liver failure (safety and efficacy not established);
- in case of hypersensitivity to anastrozole or other components of the drug.
There is no information about overdose.
Not recommended for use in women in the reproductive period. In case of doubts about the hormonal status of the patient, the menopause should be confirmed by determining the sex hormones in the blood serum.
There is insufficient data on the use of anastozol in patients with moderate or severe hepatic impairment or in patients with severe impaired renal function (Cl creatinine. Safety and efficacy in children has not been established.
In case of persistent uterine bleeding while receiving anastrozole, consultation and supervision of a gynecologist is necessary.
By reducing circulating estradiol, anastrozole may cause a decrease in bone mineral density. In patients suffering from osteoporosis or at risk of developing osteoporosis, bone mineral density should be assessed by densitometry (for example, DEXA-scan) at the beginning of treatment and in the dynamics. If necessary, treatment or prevention of osteoporosis should be initiated under the close supervision of a physician.
Influence on ability to drive motor transport and control mechanisms
Some side effects of anastozol, such as asthenia and drowsiness, may adversely affect the ability to perform potentially hazardous activities that require increased concentration and psychomotor reactions.
Estrogen-containing preparations reduce the pharmacological effect of anastrozole, and therefore they should not be administered simultaneously. Tamoxifen should not be administered concurrently with anastrozole, since it may weaken the pharmacological action of the latter.
Store at a temperature of 15-25 ° C, in a dry, dark place and out of reach of children.
3 years. Do not use after the expiration date printed on the package.