Lethorayp

Letorape is a drug that slows down the activity of enzymes and, in addition, is a hormone antagonist.

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

Indications Lethorayp

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 preoperative treatment of local types of breast carcinoma (estrogen-dependent) in postmenopausal women, with subsequent organ-preserving surgery in situations where such surgery was not initially planned (after the procedure, the decision regarding the subsequent use of Letoraip must be made taking into account generally accepted treatment regimens).

Release form

The therapeutic substance is released in tablets - 10 pieces inside a blister pack; a pack contains 3 such packs. It can also be released with 6 tablets inside a cell plate, 5 plates inside a pack.

Pharmacokinetics

After oral administration, the substance is fully absorbed; bioavailability rates are approximately 100%. Within the vascular bed, approximately 60% of the drug is synthesized with protein (mainly with albumin), and in addition, it accumulates within erythrocytes.

In the case of taking average medicinal doses, equilibrium values are recorded after 0.5-1.5 months. Inside the liver, the drug is destroyed, forming derivatives that do not have activity. [ 2 ]

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

The reduction in estrogen levels caused by prolonged daily use in the case of widespread breast carcinoma in women over 50 years of age is on average 85% of the initial values. Both with sufficient and unknown affinity of the endings to estrogens, the use of the drug leads to partial or complete regression of the neoplasm in 23% of the noted cases, 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 these are ineffective.

Dosing and administration

Adults (also the elderly) are required to take 2.5 mg of the substance once a day (daily). Therapy is continued for 5 years or until the disease relapses.

• Application for children

The medication is not used in pediatrics (in people under 18 years of age).

Use Lethorayp during pregnancy

Should not be administered to pregnant or breastfeeding women.

Contraindications

Contraindicated for use in cases of severe intolerance associated with drug components, severe liver or kidney dysfunction (creatinine clearance level below 10 ml per minute), and during premenopause.

Side effects Lethorayp

Side effects include:

• infectious lesions: sometimes urinary tract infections occur;
• disorders associated with neoplasms: sometimes pain appears;
• disorders affecting the hematopoietic system: sometimes leukopenia develops;
• problems with metabolic processes: anorexia often appears or appetite increases. General edema or hypercholesterolemia are sometimes observed;
• mental manifestations: sometimes anxiety or depression is observed;
• dysfunction of the nervous system: dizziness or headaches often occur. Sometimes insomnia or drowsiness, dysentery, memory loss and taste disorders appear. Cerebrovascular manifestations are observed sporadically;
• visual disturbances: sometimes eye irritation or blurred vision occurs, as well as cataracts;
• CVS-related lesions: sometimes tachycardia, palpitations or thrombophlebitis occur. Occasionally, pulmonary embolism, myocardial infarction, arterial thrombosis occur, or blood pressure increases;
• respiratory disorders: dyspnea develops occasionally;
• problems affecting the gastrointestinal tract: vomiting, diarrhea, dyspepsia, constipation or nausea often occur. Sometimes stomatitis, pain in the peritoneum or dry mouth mucous membranes occur, and the intrahepatic enzyme level increases;
• disorders associated with the epidermis: hyperhidrosis, alopecia or rashes often appear. Sometimes – urticaria, dry skin or itching;
• musculoskeletal disorders: arthralgia, myalgia, arthritis or pain affecting the bones often occur;
• urinary dysfunction: sometimes there is an increase in the frequency of urination;
• problems with reproductive activity: sometimes there is vaginal discharge or bleeding, 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 blood flow occurs. Peripheral edema or fatigue is often observed. Sometimes thirst, dry mucous membranes or an increase in temperature appear.

Storage conditions

Letoraip must be stored in a place closed to small children and moisture. Temperature values - no more than 25 ° C.

Shelf life

Letorape can be used for a period of 24 months from the date of manufacture of the pharmaceutical product.

Analogues

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