Letrozole film-coated pills 2.5 mg N30
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Description
Ingredients Letrozole 2.5 mg Excipients: lactose monohydrate 50 mg, carboxymethyl starch sodium 2.5 mg, colloidal silicon dioxide 500 μg, microcrystalline cellulose 28 mg, crospovidone 4 mg, corn starch pregelatinized 11.5 mg, magnesium stearate 1 mg. The composition of the film shell: opadry Y 1-7000 (hypromellose, titanium dioxide, macrogol (polyethylene glycol)) 3.73 mg, iron dye yellow oxide 270 mcg. Pharmacological action Antineoplastic drug, an inhibitor of estrogen synthesis. Letrozole has an antiestrogenic effect, selectively inhibits aromatase (an estrogen synthesis enzyme) by highly specific competitive binding to the subunit of this enzyme, the heme of cytochrome P450. Blocks the synthesis of estrogen in both peripheral and tumor tissues. In women in the postmenopausal period, estrogens are formed mainly with the participation of the aromatase enzyme, which converts androgens (primarily androstenedione and testosterone) synthesized into the adrenal glands into estrone and estradiol. Daily intake of letrozole in a daily dose of 0.1-5 mg leads to a decrease in the concentration of estradiol, estrone and estrone sulfate in the blood plasma by 75-95% of the initial content. Suppression of estrogen synthesis is maintained throughout the entire period of treatment. When using Letrozole in the dose range from 0.1 to 5 mg, there is no violation of the synthesis of steroid hormones in the adrenal glands, the test with ACTH does not reveal any abnormalities in the synthesis of aldosterone or cortisol. Additional administration of glucocorticoids and mineralocorticoids is not required. The blockade of estrogen biosynthesis does not lead to the accumulation of androgens, which are precursors of estrogen. While receiving Letrozole, there were no changes in the concentrations of LH and FSH in the blood plasma, changes in thyroid function, changes in the lipid profile, an increase in the incidence of myocardial infarction and stroke. During the treatment with letrozole, the incidence of osteoporosis increases to a small extent (6.9% compared with 5.5% against placebo). However, the incidence of bone fractures in patients receiving Letrozole is not different from that in healthy people of the same age. Adjuvant therapy with letrozole in early stages of breast cancer reduces the risk of relapse, increases survival without signs of disease for 5 years, reduces the risk of developing secondary tumors. Extended adjuvant therapy with letrozole reduces the risk of recurrence by 42%.A significant survival benefit without signs of disease in the letrozole group was noted regardless of the involvement of lymph nodes. Treatment with letrozole reduces mortality in patients with lymph node involvement by 40%.
Dosage and administration
: The drug is taken orally, regardless of the meal. The recommended dose of Letrozole is 2.5 mg 1 time per day, daily, for a long time (for 5 years or until relapse). As extended adjuvant therapy, treatment should continue for 4 years (not longer than 5 years). If there is evidence of disease progression, the administration of the drug Letrozole should be discontinued. In patients with late-stage disease or a metastatic tumor, the treatment with Letrozole should be continued until tumor progression is expressed. In elderly patients, dose adjustment of the drug Letrozole is not required. In case of impaired liver or kidney function (CC> 10 ml / min), dose adjustment is not required. However, in patients with severely impaired liver function (class C on the Child-Pugh scale), patients need constant medical supervision. Precautions During the period of treatment may worsen psoriasis. With pheochromocytoma, propranolol can be used only after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. Against the background of treatment with propranolol, IV administration of verapamil, diltiazem should be avoided. A few days before anesthesia, you must stop taking propranolol or pick up a remedy for anesthesia with minimal negative inotropic effects. Influence on the ability to drive vehicles and control mechanisms In patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient. Side Effects As a rule, side reactions were mild or moderate and were mainly associated with the suppression of estrogen synthesis. Determination of the frequency of adverse reactions: very often (> 10%), often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports digestive system: often - nausea, vomiting, dyspepsia, constipation, diarrhea. sometimes - abdominal pain, stomatitis, dry mouth, increased activity of liver enzymes.On the part of the nervous system: often - headache, dizziness, depression. sometimes - anxiety, nervousness, irritability, drowsiness, insomnia, memory impairment, dysesthesia, paresthesia, hypoesthesia, episodes of cerebral circulation. From the hemopoietic system: sometimes - leukopenia. Since the cardiovascular system: sometimes - a feeling of heartbeat, tachycardia, thrombophlebitis of the superficial and deep veins, increased blood pressure, coronary heart disease (angina, myocardial infarction, heart failure), thromboembolism. rarely - pulmonary embolism, arterial thrombosis, stroke. On the part of the respiratory system: sometimes - shortness of breath, cough. Dermatological reactions: often - alopecia, excessive sweating, skin rash (including erythematous, maculopapular, vesicular rash, psoriasis-like rash). sometimes - itching, dry skin, urticaria. very rarely - angioedema, anaphylactic reactions. From the musculoskeletal system: very often - arthralgia. often - myalgia, bone pain, osteoporosis, bone fractures, and sometimes - arthritis. On the part of the senses: sometimes - cataract, irritation of the eyes, blurred vision, impaired taste. On the part of the urinary system: sometimes - frequent urination, urinary tract infections. Reproductive system: sometimes - vaginal bleeding, vaginal discharge, vaginal dryness, pain in the mammary glands. On the part of metabolism: often - an increase in body weight, hypercholesterolemia, anorexia, increased appetite. sometimes - weight loss, thirst. Other: very often - hot flashes (hot flashes). often - increased fatigue, asthenia, malaise, peripheral edema. sometimes - hyperthermia (pyrexia), dry mucous membranes, generalized edema, pain in the tumor foci. Specific guidance Patients with severely impaired liver function should be under constant supervision. During therapy with Letrozole, taking into account the possibility of pregnancy, women in the perimenopausal and early postmenopausal period should use reliable methods of contraception until a stable postmenopausal hormonal status is established.Impact on the ability to drive vehicles and control mechanisms Some side effects of the drug, such as general weakness and dizziness, can affect the ability to perform potentially hazardous activities that require increased concentration of attention and psychomotor speed. Therefore, patients should be careful when driving and working with mechanisms. Use during pregnancy and breastfeeding Contraindicated use during pregnancy and lactation (breastfeeding). Type: Drug Quantity in the package, pcs: 30 Shelf life: 24 months Scope of application: Antineoplastic drugs, Oncology Active ingredient: Letrozole (Letrozole) Route of administration: Oral Vacation schedule: Prescription Release form: Prescription Storage conditions: In a dry place , In a dark place, Keep out of children Maximum storage temperature, ° С: 25 Pharmacological group: L02BG Enzyme inhibitors Minimum age: 18 yearsActive ingredients
Release form
Pills
Composition
Letrozole 2.5 mg. Excipients: lactose monohydrate 50 mg, sodium carboxymethyl starch 2.5 mg, colloidal silicon dioxide 500 µg, microcrystalline cellulose 28 mg, crospovidone 4 mg, pregelatinized corn starch 11.5 mg, magnesium stearate 1 mg. The composition of the film shell: opadry Y 1-7000 (hypromellose, titanium dioxide, macrogol (polyethylene glycol)) 3.73 mg, iron dye yellow oxide 270 mcg.
Pharmacological effect
Antitumor drug, estrogen synthesis inhibitor. Letrozole has an antiestrogenic effect, selectively inhibits aromatase (an estrogen synthesis enzyme) by highly specific competitive binding to the subunit of this enzyme, the heme of cytochrome P450. Blocks the synthesis of estrogen in both peripheral and tumor tissues. In women in the postmenopausal period, estrogens are formed mainly with the participation of the aromatase enzyme, which converts androgens (primarily androstenedione and testosterone) synthesized into the adrenal glands into estrone and estradiol. Daily intake of letrozole in a daily dose of 0.1-5 mg leads to a decrease in the concentration of estradiol, estrone and estrone sulfate in the blood plasma by 75-95% of the initial content.Suppression of estrogen synthesis is maintained throughout the entire period of treatment. When using Letrozole in the dose range from 0.1 to 5 mg, there is no violation of the synthesis of steroid hormones in the adrenal glands, the test with ACTH does not reveal any abnormalities in the synthesis of aldosterone or cortisol. Additional administration of glucocorticoids and mineralocorticoids is not required. The blockade of estrogen biosynthesis does not lead to the accumulation of androgens, which are precursors of estrogen. While receiving Letrozole, there were no changes in the concentrations of LH and FSH in the blood plasma, changes in thyroid function, changes in the lipid profile, an increase in the incidence of myocardial infarction and stroke. During the treatment with letrozole, the incidence of osteoporosis increases to a small extent (6.9% compared with 5.5% against placebo). However, the incidence of bone fractures in patients receiving Letrozole is not different from that in healthy people of the same age. Adjuvant therapy with letrozole in early stages of breast cancer reduces the risk of relapse, increases survival without signs of disease for 5 years, reduces the risk of developing secondary tumors. Extended adjuvant therapy with letrozole reduces the risk of recurrence by 42%. A significant survival benefit without signs of disease in the letrozole group was noted regardless of the involvement of lymph nodes. Treatment with letrozole reduces mortality in patients with lymph node involvement by 40%.
Indications
- early stages of breast cancer expressing estrogen receptors, in postmenopausal women, as adjuvant therapy. - the early stages of breast cancer in postmenopausal women after the completion of standard adjuvant therapy with tamoxifen - as an extended adjuvant therapy. - Common hormone-dependent forms of breast cancer in postmenopausal women - first-line therapy. - common forms of breast cancer in postmenopausal women (natural or artificially induced) who received prior anti-estrogen therapy.
Contraindications
- endocrine status characteristic of the reproductive period. - pregnancy. - lactation period (breastfeeding). - children's age (efficacy and safety for children has not been established). - hypersensitivity to the drug.With caution should use the drug with a deficiency of lactase, lactase intolerance, glucose-galactose malabsorption. There is no data on the use of letrozole in patients with QA less than 30 ml / min (before prescribing the drug, such patients should carefully weigh the ratio between the potential risk and the expected effect of treatment).
Use during pregnancy and lactation
Contraindicated use during pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is taken orally, regardless of the meal. The recommended dose of Letrozole is 2.5 mg 1 time per day, daily, for a long time (for 5 years or until relapse). As extended adjuvant therapy, treatment should continue for 4 years (not longer than 5 years). If there is evidence of disease progression, the administration of the drug Letrozole should be discontinued. In patients with late-stage disease or a metastatic tumor, the treatment with Letrozole should be continued until tumor progression is expressed. In elderly patients, dose adjustment of the drug Letrozole is not required. In case of impaired liver or kidney function (CC> 10 ml / min), dose adjustment is not required. However, in patients with severely impaired liver function (class C on the Child-Pugh scale), patients need constant medical supervision.
Side effects
As a rule, adverse reactions were mild or moderate and were mainly associated with the suppression of estrogen synthesis. Determination of the frequency of adverse reactions: very often (> 10%), often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports digestive system: often - nausea, vomiting, dyspepsia, constipation, diarrhea. sometimes - abdominal pain, stomatitis, dry mouth, increased activity of liver enzymes. On the part of the nervous system: often - headache, dizziness, depression. sometimes - anxiety, nervousness, irritability, drowsiness, insomnia, memory impairment, dysesthesia, paresthesia, hypoesthesia, episodes of cerebral circulation. From the hemopoietic system: sometimes - leukopenia. Since the cardiovascular system: sometimes - a feeling of heartbeat, tachycardia, thrombophlebitis of the superficial and deep veins, increased blood pressure, coronary heart disease (angina, myocardial infarction, heart failure), thromboembolism. rarely - pulmonary embolism, arterial thrombosis, stroke. On the part of the respiratory system: sometimes - shortness of breath, cough.Dermatological reactions: often - alopecia, excessive sweating, skin rash (including erythematous, maculopapular, vesicular rash, psoriasis-like rash). sometimes - itching, dry skin, urticaria. very rarely - angioedema, anaphylactic reactions. From the musculoskeletal system: very often - arthralgia. often - myalgia, bone pain, osteoporosis, bone fractures, and sometimes - arthritis. On the part of the senses: sometimes - cataract, irritation of the eyes, blurred vision, impaired taste. On the part of the urinary system: sometimes - frequent urination, urinary tract infections. Reproductive system: sometimes - vaginal bleeding, vaginal discharge, vaginal dryness, pain in the mammary glands. On the part of metabolism: often - an increase in body weight, hypercholesterolemia, anorexia, increased appetite. sometimes - weight loss, thirst. Other: very often - hot flashes (hot flashes). often - increased fatigue, asthenia, malaise, peripheral edema. sometimes - hyperthermia (pyrexia), dry mucous membranes, generalized edema, pain in the tumor foci.
special instructions
As a rule, adverse reactions were mild or moderate and were mainly associated with the suppression of estrogen synthesis. Determination of the frequency of adverse reactions: very often (> 10%), often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%), including individual reports digestive system: often - nausea, vomiting, dyspepsia, constipation, diarrhea. sometimes - abdominal pain, stomatitis, dry mouth, increased activity of liver enzymes. On the part of the nervous system: often - headache, dizziness, depression. sometimes - anxiety, nervousness, irritability, drowsiness, insomnia, memory impairment, dysesthesia, paresthesia, hypoesthesia, episodes of cerebral circulation. From the hemopoietic system: sometimes - leukopenia. Since the cardiovascular system: sometimes - a feeling of heartbeat, tachycardia, thrombophlebitis of the superficial and deep veins, increased blood pressure, coronary heart disease (angina, myocardial infarction, heart failure), thromboembolism. rarely - pulmonary embolism, arterial thrombosis, stroke. On the part of the respiratory system: sometimes - shortness of breath, cough.Dermatological reactions: often - alopecia, excessive sweating, skin rash (including erythematous, maculopapular, vesicular rash, psoriasis-like rash). sometimes - itching, dry skin, urticaria. very rarely - angioedema, anaphylactic reactions. From the musculoskeletal system: very often - arthralgia. often - myalgia, bone pain, osteoporosis, bone fractures, and sometimes - arthritis. On the part of the senses: sometimes - cataract, irritation of the eyes, blurred vision, impaired taste. On the part of the urinary system: sometimes - frequent urination, urinary tract infections. Reproductive system: sometimes - vaginal bleeding, vaginal discharge, vaginal dryness, pain in the mammary glands. On the part of metabolism: often - an increase in body weight, hypercholesterolemia, anorexia, increased appetite. sometimes - weight loss, thirst. Other: very often - hot flashes (hot flashes). often - increased fatigue, asthenia, malaise, peripheral edema. sometimes - hyperthermia (pyrexia), dry mucous membranes, generalized edema, pain in the tumor foci.