Peringatan Keamanan

Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression.L10601,L10604,L10607,L10613,L10619,L10622,L10625 In the case of overdose, reduce the dosage of corticosteroids temporarily.L10601,L10604,L10607,L10613,L10619,L10622,L10625

A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.L10601,L10604,L10622

Budesonide

DB01222

small molecule approved

Deskripsi

Budesonide is a glucocorticoid that is a mix of the 22R and 22S epimer used to treat inflammatory conditions of the lungs and intestines such as asthma, COPD, Crohn's disease, and ulcerative colitis.A188529,A188532

Budesonide was granted FDA approval on 14 February 1994.L10598 It is also available in a combination product with formoterol.L10619

Struktur Molekul 2D

Berat 430.5339
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Budesonide has a plasma elimination half life of 2-3.6h.[L10601,L10604,L10607,L10622] The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.[L10613]
Volume Distribusi The volume of distribution of budesonide is 2.2-3.9L/kg.[L10601,L10604,L10607,L10613,L10622,L10625]
Klirens (Clearance) Budesonide has a plasma clearance of 0.9-1.8L/min.[L10601,L10604,L10622,L10625] The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.[L10607] The clearance in asthmatic children 4-6 years old is 0.5L/min.[L10613,L10619]

Absorpsi

Extended release oral capsules are 9-21% bioavailable.L10601,L10604 A 9mg dose reaches a Cmax of 1.50±0.79ng/mL with a Tmax of 2-8h and an AUC of 7.33ng\*hr/mL.L10601,L10604 A high fat meal increases the Tmax by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.L10601,L10604 180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a Cmax of 0.6-1.6nmol/L with a Tmax of 10 minutes.L10607 A 1mg nebulized dose is 6% bioavailable, reaching a Cmax of 2.6nmol/L with a Tmax of 20 minutes.L10613 A 9mg oral extended release tablet reaches a Cmax of 1.35±0.96ng/mL with a Tmax of 13.3±5.9h and an AUC of 16.43±10.52ng\*hr/mL.L10622 Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng\*hr/mL.L10625

Metabolisme

Budesonide is 80-90% metabolized at first pass.A188526 Budesonide is metabolized by CYP3A to its 2 major metabolites, 6beta-hydroxybudesonide and 16alpha-hydroxyprednisolone.A188526,A35818 The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.A188526 CYP3A4 is the strongest metabolizer of budesonide, followed by CYP3A5, and CYP3A7.A35818

Rute Eliminasi

Approximately 60% of a budesonide dose is recovered in the urine as the major metabolites 6beta-hydroxybudesonide, 16alpha-hydroxyprednisolone, and their conjugates.L10601,L10604,L10607,L10613,L10619,L10622,L10625 No unchanged budesonide is recovered in urine.L10601,L10604,L10607,L10613,L10619,L10622,L10625

Farmakogenomik

1 Varian
TBX21 (rs2240017)

The presence of this polymorphism in TBX21 may be associated with improved responsiveness to budenoside for the treatment of asthma.

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

Interaksi Obat

1707 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Budesonide.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Budesonide.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Budesonide.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Budesonide.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Budesonide.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Budesonide.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Budesonide.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Budesonide.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Budesonide.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Budesonide.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Budesonide.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Budesonide.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Budesonide.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Budesonide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Budesonide.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Budesonide.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Budesonide.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Budesonide.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Budesonide.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Budesonide.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Budesonide.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Budesonide.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Budesonide.
Cladribine Budesonide may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Budesonide.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Budesonide.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Budesonide.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Budesonide.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Budesonide.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Budesonide.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Budesonide.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Budesonide.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Budesonide.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Budesonide.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Budesonide.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Budesonide.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Budesonide.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Budesonide.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Budesonide.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Budesonide.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Budesonide.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Budesonide.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Budesonide.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Budesonide.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Budesonide.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Budesonide.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Budesonide.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Budesonide.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Budesonide.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Budesonide.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Budesonide.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Budesonide.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Budesonide.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Budesonide.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Budesonide.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Budesonide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Budesonide.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Budesonide.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Budesonide.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Budesonide.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Budesonide.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Budesonide.
Eculizumab The risk or severity of adverse effects can be increased when Budesonide is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Budesonide is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Budesonide is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Budesonide is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Budesonide is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Budesonide is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Budesonide is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Budesonide is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Budesonide is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Budesonide is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Budesonide is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Budesonide is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Budesonide is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Budesonide is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Budesonide is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Budesonide is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Budesonide is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Budesonide is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Budesonide is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Budesonide is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Budesonide is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Budesonide is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Budesonide is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Budesonide is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Budesonide is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Budesonide is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Budesonide is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Budesonide is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Budesonide is combined with Dinutuximab.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Budesonide is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Budesonide is combined with Antilymphocyte immunoglobulin (horse).
Ixekizumab The risk or severity of adverse effects can be increased when Budesonide is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Budesonide is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Budesonide is combined with Pirarubicin.
Voclosporin The risk or severity of adverse effects can be increased when Budesonide is combined with Voclosporin.
Peficitinib The risk or severity of adverse effects can be increased when Budesonide is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Budesonide is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Budesonide is combined with Sirukumab.

Target Protein

Glucocorticoid receptor NR3C1
Annexin A1 ANXA1

Referensi & Sumber

Synthesis reference: Peter Gruber, Hans Joachim Lach, Norbert Otterbeck, "Budesonide pellets with a controlled released pattern and process for producing the same." U.S. Patent US5932249, issued May, 1991.
Artikel (PubMed)
  • PMID: 30285357
    Yasir M, Sonthalia S: Corticosteroid Adverse Effects .
  • PMID: 23300763
    Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26.
  • PMID: 15634032
    Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003.
  • PMID: 23251737
    O'Donnell S, O'Morain CA: Therapeutic benefits of budesonide in gastroenterology. Ther Adv Chronic Dis. 2010 Jul;1(4):177-86. doi: 10.1177/2040622310379293.
  • PMID: 7002575
    Ellul-Micallef R, Hansson E, Johansson SA: Budesonide: a new corticosteroid in bronchial asthma. Eur J Respir Dis. 1980 Jun;61(3):167-73.
  • PMID: 7391935
    Roth G, Wikby A, Nilsson L, Thalen A: High-performance liquid chromatographic determination of epimers, impurities, and content of the glucocorticoid budesonide and preparation of primary standard. J Pharm Sci. 1980 Jul;69(7):766-70. doi: 10.1002/jps.2600690705.
  • PMID: 23143891
    Moore CD, Roberts JK, Orton CR, Murai T, Fidler TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9.

Contoh Produk & Brand

Produk: 225 • International brands: 7
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Menampilkan 8 dari 225 produk.
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