Letoraype

Letoraype is a medication that slows down the activity of enzymes, and in addition, it is a hormone antagonist.

The active ingredient of the drug, letrozole, has an antitumor effect. It is competitively synthesized with the prosthetic region - the hemoprotein 450 heme. It acts as an aromatase subunit that takes part in the conversion of androgens into estradiol with estrone, and in addition slows down the biosynthesis of tissue estrogens and eliminates their stimulating effect on the growth of neoplasms. [1]

Indications Letoraype

It is used as a first-line agent in the treatment of common types of breast carcinoma in postmenopausal women .

In addition, it is prescribed during the preoperative treatment of local varieties of breast carcinoma (estrogen-dependent) in postmenopausal women, with the further performance of organ-preserving surgery in situations where such an operation was not initially planned (after the procedure, the decision regarding the subsequent use of Letorayp must be made, taking into account the generally accepted treatment regimens)...

Release form

The release of a therapeutic substance is made in tablets - 10 pieces inside a contour package; the pack contains 3 such packs. It can also be produced in 6 tablets inside the cell plate, 5 plates inside the pack.

Pharmacokinetics

After oral administration, the substance is fully absorbed; bioavailability indicators are about 100%. Inside the vascular bed, approximately 60% of drugs are synthesized with protein (mainly with albumin), and in addition, it accumulates inside erythrocytes.

In the case of taking average medicinal doses, equilibrium indicators are recorded after 0.5-1.5 months. Inside the liver, the drug is destroyed, forming inactive derivatives. [2]

The half-life is approximately 48 hours. Excretion is carried out in the form of biotransformation elements, mainly through the kidneys; the drug does not cumulate.

Caused, in the case of prolonged daily use, a decrease in estrogen levels in the case of a common form of breast carcinoma in women over 50 years old is equal to an average of 85% of the initial values. With both sufficient and unknown affinity of the endings for estrogens, the use of drugs leads to partial or complete regression of the neoplasm in 23% of the cases noted, and in addition to this, to a decrease in the number of deaths and relapses.

Letrozole is an alternative to toremifene (or tamoxifen) in postmenopausal women and is used when ineffective.

Dosing and administration

Adults (also the elderly) need to consume 2.5 mg of the substance once a day (daily). The therapy is continued for 5 years or until the disease recurs.

• Application for children

The medication is not used in pediatrics (in persons under the age of 18).

Use Letoraype during pregnancy

Cannot be administered to pregnant or breastfeeding women.

Contraindications

It is contraindicated to prescribe in case of severe intolerance associated with elements of drugs, severe disorders of the liver or kidneys (CC level below 10 ml per minute), as well as during premenopause.

Side effects Letoraype

Among the side signs:

• infectious lesions: sometimes infections of the urinary tract appear;
• disorders associated with neoplasms: pain sometimes appears;
• disorders affecting the hematopoietic system: sometimes leukopenia develops;
• metabolic problems: often anorexia appears or appetite increases. Sometimes there is general edema or hypercholesterolemia;
• mental manifestations: sometimes there is anxiety or depression;
• dysfunction of the NS: dizziness or headaches often occur. Sometimes there is insomnia or drowsiness, dysentesia, impaired memory and taste disorder. Cerebrovascular manifestations are singly noted;
• visual disturbances: sometimes there is eye irritation or blurred vision, as well as cataracts;
• lesions associated with CVS: sometimes tachycardia, palpitations, or thrombophlebitis appear. There is a single PE, myocardial infarction, arterial thrombosis, or an increase in blood pressure;
• respiratory disorders: dyspnea develops singly;
• problems affecting the gastrointestinal tract: vomiting, diarrhea, dyspepsia, constipation or nausea often appear. Sometimes stomatitis, pain in the peritoneal area or dryness of the oral mucous membranes occurs, and the rate of intrahepatic enzymes also increases;
• disorders associated with the epidermis: often hyperhidrosis, alopecia or rashes appear. Sometimes - urticaria, skin dryness or itching;
• musculoskeletal disorders: often arthralgia, myalgia, arthritis, or pain affecting the bones;
• violations of urinary function: sometimes there is an increase in urination;
• problems with reproductive activity: sometimes there is discharge or bleeding from the vagina, pain in the mammary glands, as well as dryness of the vaginal mucosa;
• immune disorders: anaphylactoid symptoms or Quincke's edema may develop;
• systemic lesions: mainly hot flushes. Peripheral edema or fatigue is common. Sometimes there is thirst, dryness of the mucous membranes, or the temperature rises.

Storage conditions

Letorayp must be kept out of the reach of small children and moisture. Temperature values - no more than 25 ° С.

Shelf life

Letoraype can be used for a 24-month term from the date of manufacture of the pharmaceutical product.

Analogs

The analogs of drugs are the substances Aralet, Letromara, Lezra with Letrozole, Femara, Letero and Letrotera, as well as Etruzil.