Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 6mg/mL
tablet
- 2mg
Chronic Myelogenous (Myeloid, Myelocytic, Granulocytic) Leukemia
Pre-medicate with anticonvulsants (e.g. benzodiazepines, phenytoin, valproic acid or levetiracetam) and antiemetic
Remission induction: 60 mcg/kg/day or 1.8 mg/m²; 4-8 mg PO qDay usual range
Maintenance doses: 1-4 mg/day to 2 mg/week PO to maintain WBC 10,000-20,000 cells/mm³ may withhold drug when leukocyte count has declined to approximately 15,000/mcL
Examine patient at monthly intervals and resume treatment with induction dosage when total leukocyte count reaches approximately 50,000/mcL
Administered as component of busulfan/cyclophosphamide: 0.8 mg/kg IV q6hr for 4 days (in combo with cyclophosphamide) until WBC count= 15,000/mm³
Administration: take on empty stomach to decrease risk of N/V
Monitor: CBC, Hgb, LFTs
Brain Malignancies (Orphan)
Treatment of primary brain malignancies
Orphan indication sponsor
- SuperGen, Inc; Two Annabel Lane, Suite 220; San Ramon, CA 94583
Stem Cell Transplantation (Orphan)
Liposomal busulfan (Busulipo)
Orphan designation for use as a conditioning regimen for patients with malignancies undergoing autologous or allogenic hematopoietic stem cell transplantation
Orphan sponsor
- Pharmalink AB; Engelbrekts kyrkogata 7B, SE-114 26; Stockholm, Sweden
Hepatic Impairment
Not studied
Renal Impairment
Not studied
Other Indications & Uses
CML associated with Philadelphia chromosome
Safety and efficacy not established
Chronic Myelogenous (Myeloid, Myelocytic, Granulocytic) Leukemia
Remission induction: 60 mcg/kg/day or 1.8 mg/m²; 4-8 mg PO qDay usual range
Maintenance doses: 1-4 mg/day to 2 mg/week PO to maintain WBC 10,000-20,000 cells/mm³; may withhold drug when leukocyte count has declined to approximately 15,000/mcL
Examine patient at monthly intervals and resume treatment with induction dosage when total leukocyte count reaches approximately 50,000/mcL
Administered as component of busulfan/cyclophosphamide: 0.8 mg/kg IV q6hr for 4 days (in combo with cyclophosphamide) until WBC count= 15,000/mm³
Administration: take on empty stomach to decrease risk of N/V
Monitor: CBC, Hgb, LFTs
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (22)
- abametapir
abametapir will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concomitant use is warranted, carefully monitor, particularly during treatment initiation and dose adjustment. Discontinue oliceridine if serotonin syndrome is suspected.
- adenovirus types 4 and 7 live, oral
busulfan decreases effects of adenovirus types 4 and 7 live, oral by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressives may diminish therapeutic effects of vaccines and increase risk of adverse effects (increased risk of infection). Live-attenuated vaccines should be avoided for at least 3mo after cessation of immunosuppressive therapy.
- apalutamide
apalutamide will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- axicabtagene ciloleucel
busulfan, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- brexucabtagene autoleucel
busulfan, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- ciltacabtagene autoleucel
busulfan, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- didanosine
busulfan, didanosine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Pretomanid regimen associated with hepatotoxicity. Avoid alcohol and hepatotoxic agents, including herbal supplements and drugs other than bedaquiline and linezolid.
- fexinidazole
fexinidazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- idecabtagene vicleucel
busulfan, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- idelalisib
idelalisib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates
- influenza virus vaccine quadrivalent, adjuvanted
busulfan decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- influenza virus vaccine trivalent, adjuvanted
busulfan decreases effects of influenza virus vaccine trivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.
- lisocabtagene maraleucel
busulfan, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- lonafarnib
lonafarnib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- palifermin
palifermin increases toxicity of busulfan by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- pexidartinib
busulfan and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.
- pretomanid
busulfan, pretomanid. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Pretomanid regimen associated with hepatotoxicity. Avoid alcohol and hepatotoxic agents, including herbal supplements and drugs other than bedaquiline and linezolid.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, busulfan. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
- tisagenlecleucel
busulfan, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tofacitinib
busulfan, tofacitinib. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tucatinib
tucatinib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- voxelotor
voxelotor will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (55)
- acalabrutinib
acalabrutinib, busulfan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.
- acetaminophen
acetaminophen increases levels of busulfan by decreasing metabolism. Use Caution/Monitor. Use of acetaminophen prior to (< 72 hours) or concurrently with busulfan may result in decreased clearance of busulfan due to acetaminophen-induced decreases in glutathione levels.
- acetaminophen IV
acetaminophen IV increases levels of busulfan by decreasing metabolism. Use Caution/Monitor. Use of acetaminophen prior to (< 72 hours) or concurrently with busulfan may result in decreased clearance of busulfan due to acetaminophen-induced decreases in glutathione levels.
- belatacept
belatacept and busulfan both increase immunosuppressive effects; risk of infection. Use Caution/Monitor.
- belzutifan
belzutifan will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.
- bendamustine
bendamustine, busulfan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- carboplatin
busulfan, carboplatin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- carmustine
busulfan, carmustine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- cenobamate
cenobamate will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.
- chlorambucil
busulfan, chlorambucil. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- cholera vaccine
busulfan decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Immunosuppressive therapies, including irradiation, antimetabolites, alkylating agents, cytotoxic drugs and corticosteroids (used in greater than physiologic doses), may reduce the immune response to cholera vaccine.
- cisplatin
busulfan, cisplatin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- crofelemer
crofelemer increases levels of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- cyclophosphamide
cyclophosphamide, busulfan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor.
busulfan, cyclophosphamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression. - dabrafenib
dabrafenib will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- dacarbazine
busulfan, dacarbazine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- deferasirox
deferasirox increases toxicity of busulfan by unspecified interaction mechanism. Modify Therapy/Monitor Closely. Discontinue iron chelating agents well in advance of administration of busulfan to avoid increased exposure to busulfan.
- dengue vaccine
busulfan decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Use Caution/Monitor. Immunosuppressive therapies (eg, irradiation, antimetabolites, alkylating agents, cytotoxic drugs, corticosteroids [greater than physiologic doses]) may reduce immune response to dengue vaccine.
- denosumab
busulfan, denosumab. Other (see comment). Use Caution/Monitor. Comment: Caution should be taken in patients on concomitant immunosuppressants or with impaired immune systems because of increased risk for serious infections.
- dichlorphenamide
dichlorphenamide and busulfan both decrease serum potassium. Use Caution/Monitor.
- elagolix
elagolix will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.
- ethotoin
ethotoin decreases levels of busulfan by increasing hepatic clearance. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
- fingolimod
busulfan increases effects of fingolimod by immunosuppressive effects; risk of infection. Modify Therapy/Monitor Closely. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects. .
- fosphenytoin
fosphenytoin decreases levels of busulfan by increasing hepatic clearance. Use Caution/Monitor.
fosphenytoin will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - hydroxyurea
busulfan, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.
- ifosfamide
busulfan, ifosfamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
busulfan increases toxicity of ifosfamide by Other (see comment). Use Caution/Monitor. Comment: Coadministration with ifosfamide may increase the risk of immunosuppression and myelosuppression. Busulfan may increase the risk of hemorrhagic cystitis during ifosfamide treatment. Follow standard guidelines for hydration, mesna administration, and use of urinalysis. - iloperidone
iloperidone increases levels of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.
- influenza A (H5N1) vaccine
busulfan decreases effects of influenza A (H5N1) vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- influenza virus vaccine (H5N1), adjuvanted
busulfan decreases effects of influenza virus vaccine (H5N1), adjuvanted by pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce immune response to H5N1 vaccine.
- isavuconazonium sulfate
busulfan and isavuconazonium sulfate both decrease immunosuppressive effects; risk of infection. Use Caution/Monitor.
- istradefylline
istradefylline will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- itraconazole
itraconazole increases levels of busulfan by decreasing hepatic clearance. Use Caution/Monitor.
itraconazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - ketoconazole
ketoconazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lenacapavir
lenacapavir will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- levoketoconazole
levoketoconazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lomustine
busulfan, lomustine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- meningococcal group B vaccine
busulfan decreases effects of meningococcal group B vaccine by pharmacodynamic antagonism. Use Caution/Monitor. Individuals with altered immunocompetence may have reduced immune responses to the vaccine.
- mitotane
mitotane decreases levels of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.
- ofatumumab SC
ofatumumab SC, busulfan. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olaparib
busulfan and olaparib both increase pharmacodynamic synergism. Use Caution/Monitor. Coadministration with other other myelosuppressive anticancer agents, including DNA damaging agents, may potentiate and prolongate the myelosuppressive toxicity.
- phenytoin
phenytoin decreases levels of busulfan by increasing hepatic clearance. Use Caution/Monitor.
phenytoin will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. - posaconazole
posaconazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- siponimod
siponimod and busulfan both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- sipuleucel-T
busulfan decreases effects of sipuleucel-T by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- streptozocin
busulfan, streptozocin. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- tazemetostat
tazemetostat will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- thioguanine
thioguanine, busulfan. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Avoid concomitant administration of thioguanine with busulfan because of potential for hepatotoxicity. .
- thiotepa
busulfan, thiotepa. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Additive myelosuppression.
- trastuzumab
trastuzumab, busulfan. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, busulfan. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- voriconazole
voriconazole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
Minor (8)
- acetaminophen rectal
acetaminophen rectal increases levels of busulfan by decreasing metabolism. Minor/Significance Unknown.
- acetazolamide
acetazolamide will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- ribociclib
ribociclib will increase the level or effect of busulfan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- vitamin A
vitamin A, busulfan. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin A enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
- vitamin E
vitamin E, busulfan. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Antioxidants such as vitamin E enhance the efficacy, and reduce toxicity, of antineoplastic drugs.
Adverse Effects
>10%
Neutropenia (nearly 100%)
Myelosuppression (nearly 100%)
Thrombocytopenia (98%)
Nausea (97%)
Stomatitis (96%)
Anorexia (80%)
Diarrhea (80%)
Fever (80%)
Insomnia (80%)
Lymphopenia (79%)
Hypomagnesemia (77%)
Headache (69%)
Hyperglycemia (66%)
Hypokalemia (64%)
Abdominal pain (62%)
Anemia (62%)
Asthenia (52%)
Hypocalcemia (49%)
Chills (47%)
Dyspepsia (44%)
Tachycardia (44%)
Pain (41%)
Constipation (38%)
Hypertension (36%)
Hypersensitivity (32%)
Edema (27%)
Thrombosis (27%)
Dry mouth (26%)
Vasodilation (25%)
Mild epistaxis (25%)
Inflammation at injection site (25%)
Rectal disorder (25%)
Abdominal enlargement (23%)
Back pain (23%)
Chest pain (22%)
1-10%
Grade 3/4 Hypertension (7%, IV)
Hypotension (3%, IV)
Cardiac tamponade (2%, oral)
Third degree AV block (2%, IV)
Left heart failure (2%, IV)
Frequency Not Defined
Dizziness
Anxiety
Depression
Seizure
Cough
Dyspnea
Rhinitis
Bronchopulmonary dysplasia with pulmonary fibrosis (rare)
Aplastic anemia (rare)
Leukemia (rare)
Graft versus host disease
Adrenal gland disorder
Pruritis
Rash
Cataract
Hemorrhagic cystitis
Amenorrhea
Male infertility
Ovarian dysfunction
Postmarketing Reports
Febrile neutropenia
Tumor lysis syndrome
Thrombotic micro-angiopathy (TMA)
Severe bacterial, viral (eg, cytomegalovirus viremia), fungal infections, and sepsis
Tooth hypoplasia
Warnings
Black Box Warnings
Bone marrow suppression is a common occurrence; reduce dose or discontinue oral administration for unusual suppression (bond marrow biopsy may be necessary); hematopoietic progenitor cell transplantation is required to prevent potentially fatal complications of prolonged myelosuppression
Monitoring is very important after administering these doses
This drug should be administered under the supervision of an experienced cancer chemotherapy physician
Contraindications
Hypersensitivity, resistance to busulfan
Patients without definitive diagnosis of CML
Cautions
Bone marrow depression may occur
Seizures reported with use; initiate anticonvulsant prophylactic therapy prior to treatment with busulfan; monitor patients with history of seizure disorder, head trauma or receiving epileptogenic drugs
Cardiac temponade reported in children with thalassemia in combination with cyclophosphamide
Ovarian failure may occur
Secondary malignancies reported
Antiemetics may be recommended to prevent nausea and vomiting
Increased risk of developing hepatic veno-occlusive disease (HVOD) at AUC greater than 1,500 μM•min; monitor serum transaminases, alkaline phosphatase and bilirubin daily
Bronchopulmonary dysplasia with pulmonary fibrosis reported and can be fatal; toxicity may be additive if used with other agents that cause pulmonary toxicity; discontinue therapy if busulfan toxicity develops
Avoid pregnancy; can cause fetal harm; advise of potential risk to a fetus and use of effective contraception
Pregnancy & Lactation
Pregnancy
Can cause fetal harm when administered to a pregnant woman based on animal data; drug shown to be teratogenic in mice, rats, and rabbits following administration during organogenesis; the solvent, DMA, may also cause fetal harm when administered to a pregnant woman; in rats, DMA doses of approximately 40% of daily dose of DMA in dose on a mg/m² basis given during organogenesis caused significant developmental anomalies; there are no available human data informing drug-associated risk; advise pregnant women of potential risk to a fetus
Advise females of reproductive potential to use effective contraception during treatment and for 6 months following cessation of therapy
May damage spermatozoa and testicular tissue, resulting in possible genetic fetal abnormalities; males with female sexual partners of reproductive potential should use effective contraception during treatment and for 3 months after cessation of therapy
Infertility
- Females: Ovarian suppression and amenorrhea commonly occur in premenopausal women undergoing chronic, low-dose busulfan therapy for chronic myelogenous leukemia; therapy may also cause temporary or permanent infertility in prepubertal girls or in females of child-bearing potential treated with high-dose busulfan in the conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation
- Males: Sterility, azoospermia, and testicular atrophy reported in male patients
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Alkylating agent; interferes with DNA replication and RNA transcription; cross-links DNA strands; has little immunosuppressive activity; affects myeloid cells more than lymphoid cells; very toxic to hematopoietic stem cells
Absorption
Onset: 1-2 weeks
Duration: 24 hr
Time to peak serum: 1hr (PO); 5 min (IV)
Bioavailability: 68-80% depending on age
Distribution
Protein bound: 32%
Vd: 0.6-1.0 L/kg (adults); 1.4-1.6 L/kg (children)
Metabolism
Liver
Metabolites: Methanesulfonic acid & 3-hydroxytetrahydrothiophene-1,1-dioxide
Elimination
Half-life elimination: 2.5 hr
Clearance: 2.52 mL/min/kg
Excretion: Urine (25-60%)
Dialyzable: Yes
Administration
IV Preparation
Dilute and administer as intravenous infusion; do not administer as intravenous push or bolus
Do not infuse other medications simultaneously
Dilute busulfan injection in NS or D5W; do not use other diluents
Dilution volume should be 10x volume of busulfan concentrate, insuring final concentration is equal to or >0.5 mg/mL
IV Administration
Administer via a central venous catheter as a 2 hr infusion, q6hr for 4 consecutive days for a total of 16 doses
Do not use polycarbonate syringes
Storage
Store unopened ampules (injection) under refrigeration at 2-8°C
Prolonged storage (>8 hr) in D5W or NS at room temp causes 10%+ loss of potency
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Myleran oral - | 2 mg tablet |  | |
| Busulfex intravenous - | 60 mg/10 mL vial |  | |
| Busulfex intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  | |
| busulfan intravenous - | 60 mg/10 mL vial |  |
Copyright © 2010 First DataBank, Inc.
Formulary
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