Busulfan

[byou-SUL-fan] Pregnancy Category: D

Myleran (Abbreviation: Bus) [Rx] Classification: Antineoplastic, alkylat-ing agent

See also Antineoplastic Agents. Action/Kinetics: Busulfan is cell cycle-phase nonspecific and acts predominately against cells of the granulocytic type and is thought to act by alkylating cellular thiol groups. Cross-linking of nucleoproteins occurs. May cause severe bone marrow depression. Leukocyte count drops during the second or third week. Thus, close medical supervision, including weekly laboratory tests, is mandatory. Resistance may

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develop and is thought to be due to the altered transport into the cell

Band/or increased intracellular inacti-vation. Rapidly absorbed from the GI tract; appears in serum 0.5-2 hr after PO administration. tV2: 2.5 hr. Extensively metabolized and excreted in the urine.

Increased appetite and sense of well-being may occur a few days after therapy is started. Sometimes administered with allopurinol to prevent symptoms of clinical gout. Uses: Chronic myelogenous leukemia (granulocytic, myelocytic, myeloid). Less effective in individuals with chronic myelogenous leukemia who lack the Philadelphia (Ph1) chromosome. Not effective in individuals where the disease is in the "blastic" phase.

Contraindications: Use during lactation only if benefits outweigh risks.

Side Effects: Hematologic: Pancytopenia, severe bone marrow hypoplasia, anemia, leukopenia, thrombocy-topenia. Pulmonary: Bronchopul-monary dysplasia with interstitial pulmonary fibrosis. Ophthalmologic: Cataracts after prolonged use. Der-matologic: Hyperpigmentation, especially in clients with a dark complexion; also, urticaria, erythema multiforme, erythema nodosum, alopecia, porphyria cutanea tarda, excessive dryness and fragility of the skin with anhidrosis, dryness of the oral mucous membranes, cheilosis. Metabolic: Syndrome resembling adrenal insufficiency, including symptoms of weakness, severe fatigue, weight loss, anorexia, N&V, and melanoderma (especially after prolonged use). Also, hyperuricemia and hyperuricosuria in clients with chronic myelogenous leukemia. Oral: Dry mouth, stomatitis, cheilosis. Miscellaneous: Cellular dysplasia in various organs, including lymph nodes, pancreas, thyroid, adrenal glands, bone marrow, and liver. Also, gynecomastia, seizures after high doses, cataracts after prolonged use, hepatotoxicity, cholestatic jaundice, myasthenia gravis, sterility, en-

docardial fibrosis, and suppression of ovarian function.

Drug Interactions

Aspirin / T Increased risk of bleeding

How Supplied: Tablet: 2 mg

Dosage-

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