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An antitumor agent. Is a selective nonsteroidal inhibitor of aromatase. In postmenopausal women, estradiol is mainly produced from estrone, which is produced in peripheral tissues by conversion from Androstenedione (with the participation of the enzyme aromatase). The reduction of circulating levels of estradiol exerts a therapeutic effect in women with breast cancer. In postmenopausal women anastrozole at a daily dose of 1 mg causes a decrease in estradiol by 80%. Anastrozole does not possess progestogenic, androgenic and estrogenic activity; in therapeutic doses does not affect the secretion of cortisol and aldosterone.
Anastrozole reduces the production of estrogen in the body. Lowering the levels of the hormone down in postmenopausal women helps curbs the growth of certain breast tumours, which require estrogen for their growth. Anastrozole is normally prescribed to treat breast cancer in postmenopausal women, even when the cancer has reached an advanced stage. Even if treatment has begun with Soltamax or Nolvadex,(tamoxifen) and the cancer progressed Anastrozole may be used. Research has proven that with Anastrozole treatment you can stay cancer free at a higher rate than with Nolvadex (tamoxifen) or Soltamax.
This drug is usually taken once a day by mouth – with or without food. It is highly important to stick to the prescription provided by the physician. Do not make any changes to the dosage or the schedule without consulting your physician. You must not increase your dose without the healthcare provider’s advice. Increasing the dose will not enhance the effectiveness of the drug. Rather, it will interfere with the treatment and might even result in severe side effects.
Anastrozole works best when it is consumed on a regular basis. Therefore, do not forget to consume your medication on time. If you skip or miss a dose, take it as soon as you remember. Do not double the dosage in order to compensate.
This could lead to overdosing. Taking the drug at the same time every day can prevent you from missing your dose.
After intake of anastrozole is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached within 2 h (fasting). Food slightly reduces the rate but not extent of absorption. The plasma protein binding is 40%. Information on the cumulation no.
Metabolism of anastrozole is an N-dealkilirovanie, by hydroxylation and glukuronizatia. Triazole, the major metabolite of, determined in plasma and urine, does not inhibit aromatase.
Anastrozole and its metabolites are excreted mainly with urine (less than 10% in an unmodified form) within 72 h after a single dose. T1/2 of plasma – 40-50 hours
Clearance of anastrozole after ingestion in volunteers with stable hepatic cirrhosis or impaired renal function are not different from the clearance determined in healthy volunteers.
The above being the most commonly spotted side effects, it has been observed that Hot flashes are rather common in most women, closely followed by nausea, fatigue and mood swings. A minor portion of people also suffer from back pain, breathing difficulties, cough, slight withering away of bones indicating osteoporosis, swelling in the arm or leg, abdominal pain, breast pain, and loss of appetite.