Adult Dosing

CML

• 1.8 mg/m²/day PO or 60 mcg/kg/day PO until WBCs <15,000/mcL
• Usual dose: 4-8 mg/day; Range 1-12 mg/day
• During remission, treatment is resumed when a monthly WBC reaches 50,000/mcL
• Maintenance: 1-3 mg/day PO

Myelofibrosis [Not FDA approved]

• 2-4 mg PO 2-3 times per week

Pediatric Dosing

CML

• 1.8 mg/m²/day PO or 60 mcg/kg/day PO until WBCs <15,000/mcL
• Usual dose: 4-8 mg/day; Range 1-12 mg/day
• During remission, treatment is resumed when a monthly WBC reaches 50,000/mcL
• Maintenance: 1-3 mg/day PO

[Outline]

• Adult Dosing
• Pediatric Dosing

• Palliative treatment of chronic myelogenous (myeloid, myelocytic, granulocytic) leukemia

• Hypersensitivity to any of the ingredients of the product
• Failure to respond to previous courses
• Severe myelosuppression
• Blast crisis CML
• Concurrent live vaccination
• Pts in whom a definitive diagnosis of CML has not been firmly established

• Busulfan is a potent cytotoxic drug. It should be used only by physician trained in chemotherapy assessment and when diagnosis of chronic myelogenous leukemia (CML) has been established
• Busulfan can induce severe bone marrow hypoplasia. Decrease dose or discontinue immediately if unusual depression of bone marrow function seen by abnormal decrease in any of the formed elements of blood; perform bone marrow examination if uncertain bone marrow status

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined
• Hemodialysis: Not defined

Hepatic Dose Adjustment

• Hepatic impairment: Dose adjustments not defined

See Supplemental Patient Information

• Potential for cytotoxicity; severe granulocytopenia, thrombocytopenia, anemia may occur
• Treatment should be initiated only if a definitive diagnosis of CML has been established
• Busulfan should be used with extreme caution in patients whose bone marrow reserve may have been compromised by prior irradiation or chemotherapy
• Reports of bronchopulmonary dysplasia; may cause cellular dysplasia in many organs, in addition to the lung. Giant hyperchromatic nuclei have been reported in the adrenal glands, bone marrow, liver, lymph nodes, pancreas, and thyroid
• Hyperuricemia and hyperuricosuria have occurred; minimize adverse effects by increased hydration, urine alkalization, and the prophylactic administration of allopurinol
• Ovarian suppression and amennorrhea with menopausal symptoms can occur during busulfan therapy in premenopausal women
• Interstitial pulmonary fibrosis, bronchopulmonary dysplasia, secondary malignancies, cardiac temponade and endocardial fibrosis have been reported in patients receiving busulfan
• Esophageal varices and hepatic veno-occlusive disease has also been reported . Measure LFTs and serum bilirubin
• Other events reported include erythema multiforme, erythema nodosum, secondary malignancy, infertility and cataract formation
• Seizures may occur with high oral doses; prophylactic administration of phenytoin is recommended
• Monitor CBC, Platelet count, WBC with differential count qwk; bone marrow examination if the cause of fluctuation in formed elements of peripheral blood is obscure
• Overdosage has no antidote and it may lead to bone marrow depression and pancytopenia, therefore drug should be carefully administered

Cautions: Use cautiously in

• Bone marrow depression (extreme caution required)
• Hx of seizure disorder
• Thalassemia (risk of cardiac temponade)
• Concomitant use of multiple alkylating agents (danger of hepatotoxicity)
• Previous irradiation/therapy
• Head injury
• Elderly

Supplemental Patient Information

• Busulfan is hazardous to health. Proper precautions should be taken while handling and disposing the drug

Pregnancy Category:D

Breastfeeding: Most sources consider breastfeeding to be incompatible with breastfeeding. A single study of a woman receiving 4 mg qd (for 5 wks) for myeloid leukemia reported no adverse events on her nursing infant on weekly monitoring. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 10 September 2010). According to manufacturer's data, use during breastfeeding is contraindicated.

• HEMA: Myelosuppression, aplastic anemia
• CV: Cardiac tamponade (with high-dose cyclophosphamide), endocardial fibrosis
• RESP: Bronchopulmonary dysplasia, pulmonary fibrosis, pneumonia
• CNS: Seizures
• GI: Nausea, vomiting, drug-induced hepatitis, cholestatic jaundice,esophageal varices, hepatic veno-occlusive disease
• MUSC: Arthralgia, myalgia, back pain
• METABOLIC: Hyperuricemia, hyperuricosuria, adrenal suppression
• ENDO: Sterility, gynecomastia, amenorrhea
• DERM: Rash, hyperpigmentation, erythema multiforme,erythema nodosum, alopecia, porphyria cutanea tarda, excessive dryness/fragility of the skin
• EENT: Cataracts
• MISC: Allergic reactions, secondary malignancy, chills, fever

• Alkylating agent; interferes with DNA replication and RNA transcription by alkylating and cross-linking the DNA strands
• Rapidly absorbed from the GI tract
• Metabolized in liver predominantly by conjugation with glutathione and GST catalysis; CYP450: Unknown
• Renally excreted (none unchanged)
• Half-Life: 2.5 hrs

US Trade Name(s)

• Myleran

US Availability

Myleran

• TABS: 2 mg

Canadian Trade Name(s)

• Myleran

Canadian Availability

Myleran

• TABS: 2 mg

UK Trade Name(s)

• Myleran

UK Availability

Myleran

• TABS: 2 mg

Australian Trade Name(s)

• Myleran

Australian Availability

Myleran

• TABS: 2 mg

[Outline]

Hematology/Oncology

Antineoplastics

Alkylating Agents

Pricing data from www.DrugStore.com in U.S.A.

• Myleran 2 MG TABS [Bottle] (PRASCO LABORATORIES)
  60 mg = $267.79
  180 mg = $785.91

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

Drug Name: Myleran 2 MG Oral Tablet

Ingredient(s): Busulfan

Imprint: GX;EF3;M

Color(s): White

Shape: Round

Size (mm): 7.00

Score: 1

Inactive Ingredient(s): hypromellose / anhydrous lactose / magnesium stearate / starch, corn / triacetin / titanium dioxide

Drug Label Author:
SmithKline Beecham Corporation

DEA Schedule:
Non-Scheduled