Estramustine

Chemical name

(17бета)-Эстра-1,3,5(10)-три ен-3,17-диол-3-[бис(2-хлор��тил)карбамат] (in the form of 17beta-dinatria phosphate)

Gross

C23-H31-Cl2-N-O3

Characteristics

White or colourless powder, soluble in water.

Of drugs

The drugs-protivoopujolevoe (zitostaticescoe) mode. Entered into the cell nucleus selectively ingibiruet processes mitoticeski division; In addition, acting on the front of pituitary reduce product gonadotroponah hormones, reducing testosterone levels in Krovi.posle intake of rapidly and completely absorbed, bioavailability is about 75%. In microcirkulatornom line is defosfaurilirovaniu education estramustina which gidrolizuacy passed estron and estradiol. Estramustin interact with the specific protein vnutricletocnam, koumouliruet. T_1/2 mnogofazny-and, on average, 20 hours Excreted mainly jelchew.

Indications

Cancer prostate gland.

Contraindications

Hypersensitivity, cerebrovascular insufficiency, heart failure, ischemic heart disease, bronchial asthma, violations of the liver and kidneys, jelchnokamennaya disease holetsaticeski hepatitis, chronic viral diseases pepticalkie stomach ulcers, osteoporosis, diabetes mellitus, gipoplasia bone marrow, tromboflebita, the propensity to embolism.

Side-Effects

Diarrhoeal phenomenon : nausea, vomiting, diarrhoea; Sleeping, oedema, the increase in the amount of swelling and thoracic surgery, the propensity to tromboobrazovaniu, reduced libido, lakopenia, thrombocytopenia, anemia, allergic reactions.

Patient interaction

Calcium and calzisodergaszczye to weaken activity; Mineralokortikoida glukokortikoida and increase the toxicity. Do side effects gepatotoksicskih and nicotine.

Dosing and Administration

Inside (1 hour before or two hours after meals) 10-16 mg / kg / day in 3-4 reception. In / in 450 mg once a day for 3 weeks and then 300 mg twice a week.

Directory → Antineoplastic funds → Antineoplastic hormonal and hormone antagonists → Estramustine