Expiration date: 01/2026

Composition and form of issue:

Tablets, film-coated. 1 tablet contains:

busulfan 2 mg

excipients: lactose anhydrous starch pre-gelatinized magnesium stearate Opadry white (hypromellose, titanium dioxide, triacetin)

in bottles of dark glass 25 PCs. in a pack of cardboard 1 bottle.

Pharmacological action:

Inhibits granulocytopoiesis.

Indications:

Chronic myeloid leukemia (chronic stage), true polycythemia, essential plateletemia, myelofibrosis.

Contraindications:

Hypersensitivity, radiation therapy (including and soon after).

Use during pregnancy and breast-feeding:

Contraindicated (has Carcinogenicity, teratogenicity and embryotoxicity).

Side effect:

Myelosuppression (thrombocytopenia), skin hyperpigmentation, urticaria, erythema multiforme, alopecia, "allopourinolovaya" rash, dry skin (up to full agidrosa), dry mucous membranes of the mouth, halos, violations of liver function, changes of the crystalline lens, cataracts, ginekomastia, male gravis, haemorrhagic cystitis, prolonged treatment of diffuse pulmonary fibrosis syndrome resembling adrenal insufficiency at high doses — hyperbilirubinemia, jaundice, fibrosis with atrophy and necrosis of the skin. Women may develop ovarian suppression, amenorrhea, men-azoospermia, testicular atrophy, sterility.

Drug interaction:

Thioguanine increases the likelihood of development of nodular regenerative liver hyperplasia, portal hypertension, esophageal varicose veins.

Dosage and administration:

Inside (split the pill into parts is impossible).

Busulfan is usually prescribed courses or permanently. The dose is selected individually for each patient depending on the clinical condition and hematological parameters. If the patient needs a dose of less than 2 mg / day (less than 1 table.), the drug can be taken not daily, but at intervals of one or more days.

Chronic myelogenous leukemia

Adults

Induction of remission: treatment usually begins immediately after diagnosis. The dose is 0, 06 mg/kg/day the maximum initial dose is 4 mg / day, it can be prescribed in one dose. Individual response to busulfan is variable in some patients, high sensitivity of bone marrow cells to the drug is possible. During the induction of remission, it is necessary to monitor blood tests at least once a week. The dose should be increased only in the absence of the desired effect after 3 weeks of treatment. Treatment should be continued until the total number of leukocytes is reduced to 15-25·109/l (usually within 12-20 weeks). Then the treatment can be interrupted. After that, for another 2 weeks, there may be a further decrease in the number of leukocytes. Continued treatment in an induction dose after this point or after reducing the number of platelets less than 100·109/l is accompanied by a significant risk of long-term and possibly irreversible bone marrow aplasia.

Maintenance therapy: long-term remission of leukemia can be provided without further therapy with busulfan additional courses of treatment are usually carried out with an increase in the number of leukocytes to 50·109/l or with the appearance of symptoms of the disease.

Some specialists prefer to carry out continuous maintenance therapy. Permanent treatment is more reasonable with a short duration of remission. The purpose of treatment-to maintain the number of white blood cells at 10-15·109 / l number of blood cells should be monitored at least once every 4 weeks. Usually the maintenance dose is 0, 5-2 mg / day, but in individual cases it can be much lower. Busulfan should be administered in lower doses, if it is used in combination with other cytotoxic agents.

Children

Chronic myeloid leukemia in children is rare. Busulfan can be used to treat leukemia with the Philadelphia chromosome (Ph’-positive). Juvenile Ph’-negative on therapy with busulfan meets bad.

Osler

Usually the dose is 4-6 mg / day treatment is carried out for 4-6 weeks under careful control of the number of blood cells, especially platelets. With the development of relapses, course therapy can be resumed or, alternatively, maintenance therapy can be carried out at a dose of approximately half the induction dose. If the treatment of polycythemia is mainly carried out by venesection, then short courses can be prescribed to control the number of platelets.

Myelofibrosis

Usually the initial dose is 2-4 mg / day. Careful monitoring of hematological parameters is necessary, given the very high sensitivity of bone marrow cells in myelofibrosis.

Essential thrombocytemia

Usually the dose is 2-4 mg / day. Treatment should be discontinued if the total number of white blood cells decreases less than 5 * 109 / l or platelet count is less than 500·109 / l.

Precautionary measures:

It is necessary to constantly monitor the peripheral blood, kidney, liver, lung function.