• PO: Chronic myelogenous leukemia (CML) and bone marrow disorders.
• IV: Conditioning regimen before allogenic hematopoietic progenitor cell transplantation for CML (in combination with cyclophosphamide).

Contraindicated in:

• Hypersensitivity
• Failure to respond to previous courses
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Active infection
• ↓bone marrow reserve
• Obese patients (base dose on ideal body weight)
• Other chronic debilitating diseases
• Women of reproductive potential and men with female partners of reproductive potential
• Geri: Begin therapy at lower end of dose range in older adults due to ↑ frequency of impaired cardiac, hepatic, or renal function.

Incidence and severity of adverse reactions and side effects are increased with IV use

CV: PO: CARDIAC TAMPONADE (WITH HIGH-DOSE CYCLOPHOSPHAMIDE).
IV: chest pain, hypotension, tachycardia, thrombosis, arrhythmias, atrial fibrillation, cardiomegaly, ECG changes, edema, heart block, HF, hypertension, pericardial effusion, ventricular extrasystoles.

Derm: PO: itching, rash, acne, alopecia, erythema nodosum, exfoliative dermatitis, hyperpigmentation.

EENT: PO: cataracts.
IV: epistaxis, pharyngitis, ear disorders.

Endo: PO and IV: hyperuricemia.
IV: hyperglycemia.
PO: sterility, gynecomastia.

F and E: hypokalemia, hypomagnesemia, hypophosphatemia.

GI: PO: drug-induced hepatitis, nausea, vomiting.
IV: abdominal enlargement, anorexia, constipation, diarrhea, dry mouth, hematemesis, nausea, rectal discomfort, vomiting, abdominal pain, dyspepsia, hepatic veno-occlusive disease (↑ in allogenic transplantation), hepatomegaly, pancreatitis, stomatitis.

GU: oliguria, dysuria, hematuria, ↓ fertility.

Hemat: BONE MARROW DEPRESSION.

Local: inflammation/pain at injection site.

MS: arthralgia, myalgia, back pain.

Neuro: IV: anxiety, confusion, depression, dizziness, headache, weakness., CEREBRAL HEMORRHAGE/COMA, encephalopathy, mental status changes, SEIZURES.

Resp: PO: PULMONARY FIBROSIS.
IV: alveolar hemorrhage, asthma, atelectasis, cough, hemoptysis, hypoxia, pleural effusion, pneumonia, rhinitis, sinusitis.
Misc: allergic reactions, chills, fever, infection.

Drug-Drug:

• Concurrent or previous (within 72 hr) use of acetaminophen may ↓ elimination and ↑ toxicity.
• Concurrent use with high-dose cyclophosphamide in patients with thalassemia may result in cardiac tamponade.
• Itraconazole, metronidazole, or deferasirox may ↑ levels and risk of toxicity.
• Phenytoin may ↓ levels and effectiveness.
• Long-term continuous therapy with thioguanine may ↑ risk of hepatic toxicity.
• ↑bone marrow suppression with other antineoplastics or radiation therapy.
• May ↓ the antibody response to and ↑ risk of adverse reactions from live-virus vaccines.

(Generic available)

• Tablets: 2 mg;
• Solution for injection: 6 mg/mL;

• PO (Adults): Induction: 1.8 mg/m²/day or 0.06 mg/kg/day until WBCs <15,000/mm³. Usual dose is 4–8 mg/day (range 1–12 mg/day). Maintenance: 1–3 mg/day.
• PO (Children): 0.06–0.12 mg/kg/day or 1.8–4.6 mg/m²/day initially. Titrate dose to maintain WBC of approximately 20,000/mm³.
• IV (Adults): 0.8 mg/kg every 6 hr (dose based on ideal body weight or actual weight, whichever is less; in obese patients, dosage should be based on adjusted ideal body weight) for 4 days (total of 16 doses); given in combination with cyclophosphamide.

Busulfex, Myleran

• Disrupts nucleic acid function and protein synthesis (cell-cycle phase–nonspecific).

• Death of rapidly growing cells, especially malignant ones.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: alkylating agents

Absorption: Rapidly absorbed from the GI tract following oral administration. IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Extensively metabolized by the liver.

Half-life: 2.5 hr.

(effect on blood counts)

†Complete recovery may take up to 20 mo.

†After administration of last dose.

• Instruct patient to take medication as directed, at the same time each day, even if nausea and vomiting are a problem. Consult health care professional if vomiting occurs shortly after dose is taken. If a dose is missed, do not take at all; do not double doses.
• Advise patient to notify health care professional if fever; sore throat; signs of infection; lower back or side pain; difficult or painful urination; sores in the mouth or on the lips; chills; dyspnea; persistent cough; bleeding gums; bruising; petechiae; or blood in urine, stool, or emesis occurs. Instruct patient to use soft toothbrush and electric razor. Caution patient not to drink alcoholic beverages or take products containing aspirin or NSAIDs.
• Caution patient to avoid crowds and persons with known infections. Health care professional should be informed immediately if symptoms of infection occur.
• Discuss with patient the possibility of hair loss. Explore methods of coping.
• Instruct patient not to receive any vaccinations without advice of health care professional.
• Advise patient to notify health care professional if unusual bleeding; bruising; or flank, stomach, or joint pain occurs. Advise patients on long-term therapy to notify health care professional immediately if cough, shortness of breath, and fever occur or if darkening of skin, diarrhea, dizziness, fatigue, anorexia, confusion, or nausea and vomiting become pronounced.
• Inform patient of increased risk of a second malignancy with busulfan.
• May cause fetal harm. Advise female patients of reproductive potential to use effective contraception during and for 6 mo after last dose and to avoid breastfeeding during therapy. Advise men with female partners of reproductive potential to use effective contraception during and for 3 mo after last dose of therapy. Women need to use contraception even if amenorrhea occurs. May impair fertility in male and female patients.
• Advise patient of the importance of periodic blood counts.

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