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BP Letrozol 2.5 mg/tab

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Base price $12.37
Description

Pharmacological action

Letrozole has anti-estrogenic action, selectively inhibits aromatase (the enzyme of the synthesis of estrogen) by a highly specific competitive binding subunit of this enzyme — heme of cytochrome P450. Blocks the synthesis of estrogens in peripheral and tumor tissues.

in women in the postmenopausal period, estrogens are formed mainly with the involvement of the aromatase enzyme, which converts synthesized in the adrenal androgens (primarily Androstenedione and testosterone) to estrone and estradiol. A daily intake of letrozole in a daily dose of 0.1-5 mg leads to a decrease in concentration of estradiol, estrone and estrone sulfate in plasma at 75-95% of the original content. Suppression of the synthesis of estrogen is maintained throughout the treatment period.

When using letrozole in the dose range from 0.1 to 5 mg of a violation of the synthesis of steroid hormones in the adrenal glands not observed; test, ACTT does not detect violations of the synthesis of aldosterone or cortisol. Additional assignments of glucocorticoids and mineralocorticoids is required.

Testimony

— early stage breast cancer, whose cells have receptors for hormones, postmenopausal women as adjuvant treatment;

— early stage breast cancer in postmenopausal women after standard adjuvant therapy tamoxifen as extended adjuvant therapy;

— a common hormone-dependent forms of breast cancer in postmenopausal women (first-line therapy);

common forms of breast cancer among women postmenopause (natural or artificially induced) who received prior therapy with antiestrogens.

Dosage

Inside, regardless of meals.

Adults the recommended dose Etrail is 2.5 mg 1 times a day, every day, for a long time.

as an extended adjuvant therapy treatment should continue for 5 years (not longer).

With the advent of signs of disease progression, the drug Etrail should be discontinued.

older patients dose adjustment of the drug Etrail not required.

Patient with impaired liver and/or kidney disease: when impaired hepatic function or renal (creatine clearance >10 ml/min) correction dose is not required. However, in severe liver dysfunction (Child-Pugh C) patients should be under constant surveillance.

Side effects

generally, adverse reactions were mild or moderately expressed and are mainly connected with suppression of synthesis of estrogens.

the incidence of adverse reactions is estimated as follows: occurring very often - >10%, often 1-10%, sometimes 0.1-1%, rare - 0.01-0.1%, very rare <0.01%, including individual messages.

the part of the digestive system: often - nausea, vomiting, dyspepsia, constipation, diarrhea; sometimes - pain in the abdomen, stomatitis, dry mouth, increased liver enzymes; very rarely - hepatitis.

From the nervous system: often - headache, dizziness, depression; sometimes anxiety, nervousness, irritability, drowsiness, insomnia, memory impairment, disesthesias, paresthesia, hypoesthesia, impaired taste perception, episodes of cerebral circulation.

the part of the blood: sometimes - leukopenia.

From the side of cardiovascular system: sometimes - palpitations, tachycardia, thrombophlebitis superficial and deep veins, high blood pressure, coronary artery disease (angina, myocardial infarction, heart failure), thromboembolism; rarely pulmonary embolism, arterial thrombosis, stroke.

the respiratory system: sometimes - shortness of breath, coughing.

the part of the skin and skin appendages: often - alopecia, increased sweating, rash (including erythematous, maculopapular, vesicular rash, psoriasiform rash), sometimes - itchy skin, dry skin, urticaria; very rarely - angioneurotic edema, anaphylactic reactions, Lyell's syndrome (toxic epidermal necrolysis) syndrome Stevens-Johnson (erythema multiforme).

From the side of musculoskeletal system: very often - arthralgia; often - myalgia, bone pain, osteoporosis, bone fractures, and sometimes arthritis.

From the sensory organs: sometimes - cataract, eye irritation, blurred vision, a violation of taste sensations.

From the side of urinary system: sometimes - frequent urination, urinary tract infection.

From the reproductive system: sometimes - vaginal bleeding, vaginal discharge, vaginal dryness, breast pain.

other: very often - paroxysmal feeling the heat (hot flashes); often - fatigue, asthenia, malaise, peripheral edema, weight gain, hypercholesterolemia, anorexia, increased appetite; sometimes - reducing body weight, thirst, hyperthermia (pyrexia), dry mucous membranes, generalized swelling, pain in tumor lesions.

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