Letrozole

Chemical name

4,4'-(1H-1,2,4-Триазол-1-илме тилен)дибензонитрил

Gross

C17-H11-N5

Of drugs

The drugs-protivoopujolevoe. Competitive contact prosteticescoy part (gem) zitohroma P450 - subjedinica aromataza participating in the transformation of androgenov in estron and estradiol, ingibiruet estrogen biosynthesis in the tissues and, in particular, to eliminate their stimulating effect on Cancer Rost.posle intake of fully absorbed, bioavailability is close to 100%. In sossoudistom with more than half (60%) associated with a protein (mainly albuminom) accumulate in erythrocytes. For the average dosage equilibrium concentration achieved through 2-6 Weeks The distribution is 1.9 l / mm The liver breaks down to form inactive derivative. T_1/2 about 48 hours. Return of products biotransformation mainly kidneys. Not Koumouliruet.inducyrovannoe, with a long daily admission, the reduction of estrogen in the plasma (by an average of 85% of baseline), with the common breast cancer in women after 50 years as sufficient, and the unknown receptors to oestrogens, leads to complete or partial tumor regression in 23% of cases reduce recurrence and mortality. Letrozol be tamoksifenu alternative for women in postmenopause, and the ineffectiveness of the tamoksifena (or toremifena).

Indications

Smaller breast cancer, mostly among women postmenopause, incl. in the resistance to medication antiestrogenami.

Side-Effects

Headache, dizziness, weakness, nausea, vomiting, change in appetite (often less), obstipation, peripheral edema, tides, mialgia, ossalgia, changes in body mass index, thinning hair gynaecological bleeding, mazhushchie krovanistye separated from the vagina, skin skin.

Precautions

Before therapy to the estrogenretseptonego status. Whether appointment patients without defeat lymph nodes determined individually : recorded zlokacestvennosti degree, the size of the tumor, the presence of estrogen receptors and age. During the period of treatment is not recommended driving and other activities that require greater attention and speed of reaction.

Dosing and Administration

Inside, in the 2.5 mg once a day, every day, long course (10 years and above).

Literature

MA ML, Filov VA, Akimov MA, Akimov AA Introduction to farmakoterapiu malignant tumors-St. : SOTIS, 1999-1989.

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