Peringatan Keamanan

Patients experiencing a chronic overdose of ethambutol may present with disturbances in colour vision and reduced visual acuity as symptoms of optic neuropathy.A228993 In these cases, ethambutol should be stopped.A228993 Data regarding acute overdose of ethambutol are not readily available. Patients experiencing an acute overdose of ethambutol may be experience an increased risk and severity of adverse effects such as pruritus, joint pain, gastrointestinal upset, abdominal pain, malaise, headache, dizziness, mental confusion, disorientation, and possible hallucinations.L31663,L31748 Patients should be treated with symptomatic and supportive measures.

Ethambutol

DB00330

small molecule approved

Deskripsi

Ethambutol is a bacteriostatic agent indicated alongside medications such as isoniazid, rifampin, and pyrazinamide in the treatment of pulmonary tuberculosis.L31743 Ethambutol was first described in the literature in 1961.A229048 It was developed out of a need for therapies active against isoniazid resistant strains of Mycobacterium tuberculosis.A229048

Ethambutol was granted FDA approval on 6 November 1967.L31663

Struktur Molekul 2D

Berat 204.3098
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ethambutol has a half life of 3.3 hours in patients with normal renal function.[L31748] In patients with renal failure, the half life could be 7 hours or longer.[L31748]
Volume Distribusi Patients coinfected with tuberculosis and HIV have an estimated ethambutol volume of distribution of 76.2 L.[A228953]
Klirens (Clearance) Patients coinfected with tuberculosis and HIV have an estimated ethambutol oral clearance of 77.4 L/h.[A228953]

Absorpsi

Oral ethambutol is approximately 75-80% orally bioavailable.L31663,L31748 A 25 mg/kg oral dose of ethambutol reaches a Cmax of 2-5 µg/mL, with a Tmax of 2-4 hours.L31663,L31748 In a separate study, the AUC0-8 varied from 6.3 ± 5.5 h\*mg/L to 10.8 ± 7.6 h\*mg/L depending on CYP1A2 genetic polymorphisms.A228953

Metabolisme

Ethambutol is mainly oxidized by an aldehyde dehydrogenase to an aldehyde metabolite, followed by conversion to the dicarboxylic acid 2,2'-(ethylinediimino)di-butyric acid.A228948,A228963,L31663

Rute Eliminasi

Ethambutol is 50% eliminated in the urine as the unmetabolized parent compound and 8-15% as inactive metabolites.L31663,L31748 20-22% of a dose is eliminated unchanged in the feces.L31663,L31748

Interaksi Makanan

2 Data
  • 1. Take separate from antacids. Do not take aluminum hydroxide containing antacids for at least 4 hours after ethambutol administration.
  • 2. Take with food. Food reduces irritation.

Interaksi Obat

1225 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Ethambutol.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Ethambutol.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Ethambutol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Ethambutol.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Ethambutol.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Ethambutol.
Icosapent Icosapent may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Meloxicam The risk or severity of methemoglobinemia can be increased when Ethambutol is combined with Meloxicam.
Carprofen Carprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Ethambutol which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Ethambutol which could result in a higher serum level.

Target Protein

Probable arabinosyltransferase C embC
Probable arabinosyltransferase B embB
Probable arabinosyltransferase A embA

Referensi & Sumber

Synthesis reference: Sang-Woo Park, "Preparation of ethambutol-diisoniazide methane sulfonic acid salt." U.S. Patent US4450274, issued February, 1973.
Artikel (PubMed)
  • PMID: 17879380
    Becker C, Dressman JB, Amidon GL, Junginger HE, Kopp S, Midha KK, Shah VP, Stavchansky S, Barends DM: Biowaiver monographs for immediate release solid oral dosage forms: ethambutol dihydrochloride. J Pharm Sci. 2008 Apr;97(4):1350-60. doi: 10.1002/jps.21061.
  • PMID: 14260000
    PEETS EA, SWEENEY WM, PLACE VA, BUYSKE DA: THE ABSORPTION, EXCRETION, AND METABOLIC FATE OF ETHAMBUTOL IN MAN. Am Rev Respir Dis. 1965 Jan;91:51-8. doi: 10.1164/arrd.1965.91.1.51.
  • PMID: 31712201
    Sundell J, Bienvenu E, Birgersson S, Abelo A, Ashton M: Population Pharmacokinetics and Pharmacogenetics of Ethambutol in Adult Patients Coinfected with Tuberculosis and HIV. Antimicrob Agents Chemother. 2020 Jan 27;64(2). pii: AAC.01583-19. doi: 10.1128/AAC.01583-19. Print 2020 Jan 27.
  • PMID: 22155817
    Hall RG 2nd, Swancutt MA, Meek C, Leff RD, Gumbo T: Ethambutol pharmacokinetic variability is linked to body mass in overweight, obese, and extremely obese people. Antimicrob Agents Chemother. 2012 Mar;56(3):1502-7. doi: 10.1128/AAC.05623-11. Epub 2011 Dec 12.
  • PMID: 32644476
    Lee N, Nguyen H: Ethambutol .
  • PMID: 32327601
    Zhang L, Zhao Y, Gao Y, Wu L, Gao R, Zhang Q, Wang Y, Wu C, Wu F, Gurcha SS, Veerapen N, Batt SM, Zhao W, Qin L, Yang X, Wang M, Zhu Y, Zhang B, Bi L, Zhang X, Yang H, Guddat LW, Xu W, Wang Q, Li J, Besra GS, Rao Z: Structures of cell wall arabinosyltransferases with the anti-tuberculosis drug ethambutol. Science. 2020 Jun 12;368(6496):1211-1219. doi: 10.1126/science.aba9102. Epub 2020 Apr 23.
  • PMID: 19596878
    Goude R, Amin AG, Chatterjee D, Parish T: The arabinosyltransferase EmbC is inhibited by ethambutol in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2009 Oct;53(10):4138-46. doi: 10.1128/AAC.00162-09. Epub 2009 Jul 13.
  • PMID: 18647459
    Hasenbosch RE, Alffenaar JW, Koopmans SA, Kosterink JG, van der Werf TS, van Altena R: Ethambutol-induced optical neuropathy: risk of overdosing in obese subjects. Int J Tuberc Lung Dis. 2008 Aug;12(8):967-71.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 45 • International brands: 2
Produk
  • Ethambutol
    Tablet, film coated • 400 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet • 400 mg/1 • Oral • US • Approved
  • Ethambutol Hydrochloride
    Tablet, film coated • 400 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet, film coated • 100 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet • 400 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
  • Ethambutol Hydrochloride
    Tablet, film coated • 400 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 45 produk.
International Brands
  • Etibi — Valeant Canada Limited
  • Tibutol — Refasa

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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