Peringatan Keamanan

Signs of overdose include allergic reaction, unusual bleeding or bruising, sudden weakness or unusual fatigue, persistent cough, congestion, or shortness of breath; flank, stomach or joint pain; pronounced nausea, vomiting, diarrhea, dizziness, confusion, or darkening of the skin, chills, fever, collapse, and loss of consciousness.

Busulfan

DB01008

small molecule approved investigational

Deskripsi

Busulfan is a bifunctional alkylating agent, having a selective immunosuppressive effect on bone marrow. It is not a structural analog of the nitrogen mustards. It has been used in the palliative treatment of chronic myeloid leukemia (myeloid leukemia, chronic), but although symptomatic relief is provided, no permanent remission is brought about. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), busulfan is listed as a known carcinogen.

Struktur Molekul 2D

Berat 246.302
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2.6 hours
Volume Distribusi -
Klirens (Clearance) * 2.52 ml/min/kg [Following an infusion of dose of 0.8 mg/kg every six hours, for a total of 16 doses over four days]

Absorpsi

Completely absorbed from the gastrointestinal tract. Busulfan is a small, highly lipophilic molecule that crosses the blood-brain-barrier. The absolute bioavailability, if a single 2 mg IV bolus injection is given to adult patients, is 80% ± 20%. In children (1.5 - 6 years old), the absolute bioavailability was 68% ± 31%. When a single oral dose is given to patients, the area under the curve (AUC) was 130 ng•hr/mL. The peak plasma concentration when given orally is 30 ng/mL (after dose normalization to 2 mg). It takes 0.9 hours to reach peak plasma concentration after dose normalization to 4 mg.

Metabolisme

Busulfan is extensively metabolizes in the hepatic. Busulfan is predominantly metabolized by conjugation with glutathione, both spontaneously and by glutathione S-transferase (GST) catalysis. GSTA1 is the primary GST isoform that facilitates the the metabolism of busulfan. Other GST isoforms that are also involved are GSTM1 and GSTP1. At least 12 metabolites have been identified among which tetrahydrothiophene, tetrahydrothiophene 12-oxide, sulfolane, and 3-hydroxysulfolane were identified. These metabolites do not have cytotoxic activity.

Rute Eliminasi

Following administration of 14C- labeled busulfan to humans, approximately 30% of the radioactivity was excreted into the urine over 48 hours; negligible amounts were recovered in feces. Less than 2% of the administered dose is excreted in the urine unchanged within 24 hours. Elimination of busulfan is independent of renal function.

Interaksi Makanan

4 Data
  • 1. Drink plenty of fluids.
  • 2. Exercise caution with grapefruit products.
  • 3. Exercise caution with St. John's Wort.
  • 4. Take at the same time every day.

Interaksi Obat

899 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Busulfan.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Busulfan.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Busulfan.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Busulfan.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Busulfan.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Busulfan.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Busulfan.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Busulfan.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Busulfan.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Busulfan.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Busulfan.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Busulfan.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Busulfan.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Busulfan.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Busulfan.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Busulfan.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Busulfan.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Busulfan.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Busulfan.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Busulfan.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Busulfan.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Busulfan.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Busulfan.
Cladribine Busulfan may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Busulfan.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Busulfan.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Busulfan.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Busulfan.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Busulfan.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Busulfan.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Busulfan.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Busulfan.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Busulfan.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Busulfan.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Busulfan.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Busulfan.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Busulfan.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Busulfan.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Busulfan.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Busulfan.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Busulfan.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Busulfan.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Busulfan.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Busulfan.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Busulfan.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Busulfan.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Busulfan.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Busulfan.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Busulfan.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Busulfan.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Busulfan.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Busulfan.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Busulfan.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Busulfan.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Busulfan.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Busulfan.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Busulfan is combined with Mycophenolic acid.
Mercaptopurine The risk or severity of adverse effects can be increased when Busulfan is combined with Mercaptopurine.
Thalidomide The metabolism of Busulfan can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Busulfan is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Busulfan is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Busulfan is combined with Flucytosine.
Capecitabine The risk or severity of adverse effects can be increased when Busulfan is combined with Capecitabine.
Procarbazine The risk or severity of adverse effects can be increased when Busulfan is combined with Procarbazine.
Idarubicin The risk or severity of adverse effects can be increased when Busulfan is combined with Idarubicin.
Eculizumab The risk or severity of adverse effects can be increased when Busulfan is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Busulfan is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Busulfan is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Busulfan is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Busulfan is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Busulfan is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Busulfan is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Busulfan is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Busulfan is combined with Pirfenidone.
Belinostat The risk or severity of adverse effects can be increased when Busulfan is combined with Belinostat.
Interferon alfa The risk or severity of adverse effects can be increased when Busulfan is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Busulfan is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Busulfan is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Busulfan is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Busulfan is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Busulfan is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Busulfan is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Busulfan is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Busulfan is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Busulfan is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Busulfan is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Busulfan is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Busulfan is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Busulfan is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Busulfan is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Busulfan is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Busulfan is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Busulfan is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Busulfan is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Busulfan is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Busulfan is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Busulfan is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Busulfan is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Busulfan is combined with Ixekizumab.

Target Protein

DNA

Referensi & Sumber

Synthesis reference: Timmis, G.M.; U S . Patent 2,917,432; December 15, 1959; assigned to Burroughs Wellcome & Co., Inc.
Artikel (PubMed)
  • PMID: 16601191
    Lesurtel M, Graf R, Aleil B, Walther DJ, Tian Y, Jochum W, Gachet C, Bader M, Clavien PA: Platelet-derived serotonin mediates liver regeneration. Science. 2006 Apr 7;312(5770):104-7.
  • PMID: 20577993
    Valdez BC, Andersson BS: Interstrand crosslink inducing agents in pretransplant conditioning therapy for hematologic malignancies. Environ Mol Mutagen. 2010 Jul;51(6):659-68. doi: 10.1002/em.20603.
  • PMID: 1422285
    Hall AG, Tilby MJ: Mechanisms of action of, and modes of resistance to, alkylating agents used in the treatment of haematological malignancies. Blood Rev. 1992 Sep;6(3):163-73.
  • PMID: 19361744
    Ciurea SO, Andersson BS: Busulfan in hematopoietic stem cell transplantation. Biol Blood Marrow Transplant. 2009 May;15(5):523-36. doi: 10.1016/j.bbmt.2008.12.489. Epub 2009 Feb 12.
  • PMID: 19611402
    McCune JS, Holmberg LA: Busulfan in hematopoietic stem cell transplant setting. Expert Opin Drug Metab Toxicol. 2009 Aug;5(8):957-69. doi: 10.1517/17425250903107764.
  • PMID: 18690982
    Krivoy N, Hoffer E, Lurie Y, Bentur Y, Rowe JM: Busulfan use in hematopoietic stem cell transplantation: pharmacology, dose adjustment, safety and efficacy in adults and children. Curr Drug Saf. 2008 Jan;3(1):60-6.
  • PMID: 18690856
    Nath CE, Shaw PJ: Busulphan in blood and marrow transplantation: dose, route, frequency and role of therapeutic drug monitoring. Curr Clin Pharmacol. 2007 Jan;2(1):75-91.

Contoh Produk & Brand

Produk: 35 • International brands: 8
Produk
  • Busilvex
    Injection, solution, concentrate • 6 mg/ml • Intravenous • EU
  • Busulfan
    Injection, solution, concentrate • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection, solution, concentrate • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection, solution, concentrate • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection, solution • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection • 6 mg/1mL • Intravenous • US • Generic • Approved
  • Busulfan
    Injection • 6 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 35 produk.
International Brands
  • Bisulfex
  • Busilvex — Pierre Fabre
  • Leucosulfan
  • Mablin
  • Mielucin
  • Misulban
  • Mitostan
  • Myeloleukon

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