busulfan (Rx)

Brand and Other Names:Myleran, Busulfex
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Dosing & Uses

AdultPediatricGeriatric

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

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Interactions

Interaction Checker

and busulfan

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (0)

              Serious - Use Alternative (15)

              • 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.

              • 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.

              • 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.

              • 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.

              • 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 (53)

              • 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.

              • 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 (4)

              • acetaminophen rectal

                acetaminophen rectal increases levels of busulfan by decreasing 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.

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              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

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              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

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              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.

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              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

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              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

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              Images

              BRAND FORM. UNIT PRICE PILL IMAGE
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              busulfan intravenous
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              60 mg/10 mL vial
              Busulfex intravenous
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              60 mg/10 mL vial
              Busulfex intravenous
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              60 mg/10 mL vial
              Myleran oral
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              2 mg tablet

              Copyright © 2010 First DataBank, Inc.

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              Patient Handout

              Select a drug:
              Patient Education
              busulfan intravenous

              BUSULFAN - INJECTION

              (bue-SUL-fan)

              COMMON BRAND NAME(S): Busulfex

              WARNING: This medication decreases bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause you to bruise or bleed more easily. Tell your doctor right away if you develop any of the following symptoms: signs of an infection (such as fever, chills, persistent sore throat), easy bruising/bleeding, pale skin, unusual tiredness.Your doctor will monitor you closely while you are using this medication. Keep all medical and laboratory appointments.

              USES: Busulfan is used as a pretreatment for patients who are undergoing stem cell transplant for chronic myelogenous leukemia (CML).

              HOW TO USE: This medication is given by injection into a vein over 2 hours by a health care professional. It is usually given every 6 hours or as directed by your doctor. While you receive busulfan, your doctor may also prescribe other medications to help prevent seizures and nausea/vomiting caused by the medication.Dosage is based on your weight, medical condition, laboratory test results, and response to treatment.

              SIDE EFFECTS: See also Warning section.Nausea, vomiting, diarrhea, constipation, loss of appetite, mouth sores, stomach/abdominal pain, dizziness, swelling ankles/feet/hand, flushing, headache, or trouble sleeping may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Nausea and vomiting can be severe. In some cases, your doctor may prescribe medication to prevent or relieve nausea and vomiting. Eating several small meals, not eating before treatment, or limiting activity may help lessen some of these effects.Many people using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, including: signs of liver disease (such as persistent nausea/vomiting, severe stomach/abdominal pain, yellowing skin/eyes, dark urine), mental/mood changes (such as depression, hallucinations, anxiety, confusion), muscle cramps, increased thirst/urination, fast/irregular heartbeat, coughing up blood, bloody urine, seizures, pain/redness/swelling at injection site, fainting.Busulfan has rarely caused very serious (possibly fatal) lung disease. Tell your doctor right away if you develop symptoms of lung disease, including chest pain, shortness of breath, persistent cough.Busulfan may cause other cancers (such as acute leukemia, tumors). Consult your doctor for more details. Tell your doctor right away if you notice any symptoms of cancer, including unusual lumps, sudden weight loss.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Before receiving busulfan, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood/bone marrow disorders (such as bone marrow suppression, neutropenia, thrombocytopenia, anemia), brain disorders (such as seizures, head injury).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Busulfan can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Do not have immunizations/vaccinations without the consent of your doctor. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication can affect fertility in both males and females. Ask your doctor for more details.Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using busulfan. Busulfan may harm an unborn baby. Men with female partners of childbearing age should use reliable forms of birth control while using this medication and for at least 3 months after stopping treatment. Women of childbearing age should ask about reliable forms of birth control while using this medication and for at least 6 months after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

              DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: nalidixic acid.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: Laboratory and/or medical tests (such as complete blood count, busulfan blood levels, liver function) must be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

              MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.

              STORAGE: Not applicable. This medication is given in a hospital and will not be stored at home.

              MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

              Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

              To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

              Adding plans allows you to:

              • View the formulary and any restrictions for each plan.
              • Manage and view all your plans together – even plans in different states.
              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.