Product Name: Anastrover
Active substance: Anastrozole
Anastrover refers to a new generation of selective nonsteroidal aromatase inhibitor used in the treatment of disseminated breast cancer in women after menopause. Under the action of Anastrover is inhibit the multiplication and growth of estrogen-dependent mammary gland cells by endogenous estrogen. The mechanism of action of Anastrover reduces the selective inhibition of the activity of aromatase cytochrome P450 enzyme. The primary source of estrogen in postmenopausal women are androgens, mainly androatendionul and testosterone. Aromatase provide them with processing multiple hydroxylation to estrone and then to estradiol in adipose tissue and muscle, liver, adrenals and tumor tissue. Anastrover selectively inhibits aromatase by interacting with the heme iron atom citrocromului P-450. Thus, the formulation provides a marked inhibition of the enzyme activity that contributes to the reduction of estrogen levels within both the peripheral blood and in the tumor, which provides therapeutic effect in patients suffering from breast cancer. In postmenopausal Anastrover at a dose of 1 mg / day estradiol cause a reduction in the level of 80%. Non-steroidal inhibitors, aromatase inactivator contrary, acting reversible and depends on the presence of the preparation. Anastrover does not have activity progestagen, androgen and estrogen. The drug does not affect the secretion of cortisol and aldosterone.
Anastrover after internal administration is rapidly and completely absorbed from the gastrointestinal tract. Food least reduce the speed, but do not affect the degree of absorption and the equilibrium concentration (Css) in daily use. The maximum concentration in the blood is achieved 2 hours after administration on an empty stomach. Anastrover is 40% coupled plasma proteins. Css is reached after 7 days of preparation. Aggregating data on the pharmacokinetics of Anastrover and dependence on the duration and doses are not. Anastrover is metabolized by N-dealkylation, hydroxylation and glucuronidation. In the metabolism is formed triazole, an inactive metabolite does not inhibit aromatase, which is determined in plasma and urine. Anastrover and its metabolites is slowly eliminated mainly in the urine (less than 10% of the dose in unchanged form) for 72 hours after preparation. The half life is 40-50 hours. Clearance Anastrover after internal administration in patients with liver cirrhosis or renal disorders do not change. Anastrover pharmacokinetics is independent of age in postmenopausal women. Treatment of advanced breast cancer in postmenopausal natural or induced. Advanced breast cancer when antiestrogen not ensure efficacy.
Contraindications and Cautions:
Anastrover is contraindicated:
- In premenopausal women;
- During pregnancy and lactation;
- In advanced renal insufficiency (creatinine clearance below 20 ml / min.)
- In moderate or advanced liver failure (harmlessness and effectiveness are not confirmed);
- In case of hypersensitivity to anastrozole or any component of the preparation.
Not recommended in women of reproductive. Menopausal status must be confirmed biochemically where doubt hormonal status of the patient. Insufficient data on safety of Anastrover in patients with moderate and marked liver disorders or those with severe kidney disease (creatinine clearance below 20 ml / min.). Anastrover is not recommended for use in children because harmlessness and efficacy not established. Anastrover, by reducing circulating estradiol levels may reduce bone mineral density. In patients suffering from osteoporosis or are at risk of developing osteoporosis by densitometry method (DEXA scanning) should be determined mineral density at baseline and dynamic. If necessary, it will perform the treatment or prophylaxis of osteoporosis under medical supervision.
Effects on ability to drive and use machines:
Driving and work that requires attention and vigilance can be dangerous because of somnolence, asthenia and dizziness it causes.
Anastrover may cause a different frequency (very common - over 10% frequently - 1-10%, rarely - 0.1-1%, very rarely - less than 0.1%) following adverse effects:
- The reproductive system: frequently - vaginal dryness, rarely - vaginal bleeding (mainly in the first weeks after suspension or substitution of previous hormonal therapy with anastrozole);
- From the gastrointestinal tract: frequently - nausea, diarrhea, rarely - anorexia, vomiting, increased activity of gamma-glutamyltransferase and alkaline phosphatase;
- In the cardiovascular system: very often - sensation of heat;
- From the CNS: frequently - headache, fatigue, rarely - drowsiness;
- From the musculoskeletal system: frequently - arthralgia, rarely - use of the preparation can cause the decrease of bone mineral density by lowering estradiol levels will increase the risk of osteoporosis and fractures;
- From the skin and annexes: frequently - thinning hair;
- From the metabolism: rarely - hypercholesterolemia.
- Allergic reactions: often - skin rash, very rarely - rash, erythema multiform, Stevens-Johnson syndrome, angioedema and anaphylactic shock.
Anastrover is indicated internally. Tablets by mouth with water without chewing. It is recommended that the preparation have to be used in the same time. Anastrover in postmenopausal women, including the elderly, indicate 1 mg once a day for a long time. The disease progression is interrupted preparation administration. Correction doses in patients with mild to moderate disorders of liver and kidney function is not required.
Preparations containing estrogens reduce the pharmacologic effects of Anastrover in which considerations are not used concurrently. It is not recommended to use Tamoxiver with Anastrover, as last effect will be reduced.
Store in a dry place protected from light, at a temperature of 15-25 ° C. Keep out of reach of children.