Exemestane

Chemical name

6-Метиленандроста-1,4-д��ен-3,17-дион

Gross

C20-H24-O2

Characteristics

Steroidnyi inachtivator aromataza III generation, similar in structure to androstendionom. Crystalline powder from white to white with a yellowish sheen color. It 1e37c is soluble in N N-demetilformamide, soluble in methanol, nerastvorim almost in the water.

Of drugs

The drugs-protivoopujolevoe, antiestrogennoe. Ingibiruet aromatazu (irreversibly binds to the active centre and the enzyme is his inachtiwatia) and blocks estrogen education. Provides antiestrogennoe act has progestogenna and estrogenna activity does not affect the synthesis of cortisol and aldosterone in napochechnikah. In high doses, is a small androgennouu activity (due 17-gidroproizvodnam). Increases of LG and opened on the basis of feedback : lower concentrations of estrogen stimulates the secretion gonadotropinov in Gipofize.vazavaet dozozawisimoe decrease in estrona, seconds and estrona sulphate. Reduced estrogen concentrations in the serum of women in postmenopause is the dose of 5 mg and reaches its maximum (reduced by more than 90%) in the dose of 10-25 mg (maximum reduction of estrogen are within 3 days). The patients in postmenopause with breast cancer in the employment drug dose in the 25 mg / day total aromataza declined by 98%. In mnogocentrovom randomizirovannom double blind study of the Phase III has high efficiency and security eksemestana in the treatment of women in postmenopause with progressive metstaticski breast cancer, have prior therapy tamoksifenom was ineffective ... After intake of rapidly absorbed (food intake improves made with the plasma by 40% higher than in the employment prandial). In a single 25 mg after meals S_max (18 ng / ml) is achieved within 2 hours Linking blood plasma sostavlat 90% and is not dependent on the concentration. It is distributed in tissues. Metabolised by oxidation of methylene groups in the position in June with the participation of izofermenta CYP 3A4 and / or by restoring 17-ketogroup with aldoketoredouktaz education inactive or low metabolites. T_1/2-24 p.m. Return with urine (less than 1% in an unmodified form), and faeces approximately equal parts in 1 week.

Indications

Breast cancer among women postmenopause (natural or induced), advanced against antiestrogenami therapy, steroid inhibitors aromataza or progestinami.

Pregnancy and lactation

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : fatigue, dizziness, headache, insomnia, Deprescia.so part of the intestine : nausea, anorexia, constipation or neuralgia, abdominalnaya pain, increase in liver transaminaz (predominantly in patients with metastasis to the liver and bones, with the other losses liver). Allergic reactions : skin Sapi.prochie : tides, sweating, alopecia, peripheral edema (feet and the shins), and trombopenia lakopenia, limfopenia.

Specific guidance

Postmenopausny status should certify the level LG, and opened seconds.

Patient interaction

Estrogensoderjaschie drugs nullify effects. Inductive CYP 3A4 may reduce concentration in plasma.

Overdosing

Treatment : symptomatic (specific antidotes not), regular monitoring of the vital functions and closely monitored.

Precautions

Nor should appoint women with premenopauznam endocrine status (the effectiveness and safety of the products of this group of patients not studied). The patients with liver or renal insufficiency dose adjustment is not required. Not recommended for use in children. During treatment should refrain from activities that require concentration and psychomotor speed reactions (in the application of the drug had symptoms such as drowsiness, fatigue and dizziness).

Dosing and Administration

Inside, after delivery, 25 mg once a day. Treatment continues until progression of the secondary tumours.

Literature

1. MRLichinitser Ackzemestan (Aromazin) in the modern endokrinoterapii breast cancer / / Modern oncology .- 2001 .- T. 3-N 1.2. Makarenko NP, Poddubnaya IV New endocrine therapy for breast / / Modern oncology .- 2001 .- T. 3.-N 3.3. Kaufmann M., Bajetta E., Dirix L.-Y. et al. Exemestasane is superior to megestrol acetate after tamoxifen failure in postmenopausal women with advanced breast cancer : results of phase III randomized trial double-blind / / J. Clin. Oncol 2000 .- .- V. 18-N 7-P. 1399-1411.4. Kvinsland S., Anker G., Dirix L.-Y., et al. The high turnout and portability ackzemestana among women postmenopause with breast cancer previously unsuccessfully patients tamoksifenom / / Eur. J. Cancer-2000-N-36 P. 976-982.5. Lonning P. Exemestasane : a review of its clinical efficacy and safety / / The Breast-2001 - N-10 P. 198-208.

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