Peringatan Keamanan

Toxicity information regarding tobramycin is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as nephrotoxicity, ototoxicity, neuromuscular blockade, and respiratory failure/paralysis. Symptomatic and supportive measures are recommended; hemodialysis may help clear excess tobramycin. Accidental ingestion of tobramycin is unlikely to result in an overdose, as aminoglycosides are poorly absorbed in the gastrointestinal tract.L32739, L32749

Poor gastrointestinal absorption is reflected in animal studies. When administered by the intraperitoneal or subcutaneous route, the LD50 for mice and rats ranges from 367-1030 mg/kg while the oral LD50 values are more than 7500 mg/kg.L32838

Tobramycin

DB00684

small molecule approved investigational

Deskripsi

Aminoglycosides, many of which are derived directly from Streptomyces spp., are concentration-dependent bactericidal antibiotics with a broad spectrum of activity against Gram-positive and Gram-negative organisms.A232294 Inhaled tobramycin is notable for its use in treating chronic Pseudomonas aeruginosa infections in cystic fibrosis patients, as P. aeruginosa is notoriously inherently resistant to many antibiotics.A232294, A232299, L32739 However, tobramycin can also be administered intravenously and topically to treat a variety of infections caused by susceptible bacteria.L32744, L32749 Its use is limited in some cases by characteristic toxicities such as nephrotoxicity and ototoxicity, yet it remains a valuable option in the face of growing resistance to front-line antibiotics such as ?-lactams and cephalosporins.A232294, A232349, L32739, L32749

Tobramycin was approved by the FDA in 1975 and is currently available in a variety of forms for administration by inhalation, injection, and external application to the eye (ophthalmic).L32739, L32744, L32749

Struktur Molekul 2D

Berat 467.5145
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Tobramycin has an apparent serum terminal half-life of ~3 hours following a single 112 mg inhaled dose in cystic fibrosis patients.[L32739]
Volume Distribusi Inhalation tobramycin had an apparent volume of distribution in the central compartment of 85.1 L for a typical cystic fibrosis patient.[L32739]
Klirens (Clearance) Inhaled tobramycin has an apparent serum clearance of 14.5 L/h in cystic fibrosis patients aged 6-58 years.[L32739]

Absorpsi

Tobramycin administered by inhalation in cystic fibrosis patients showed greater variability in sputum as compared to serum. After a single 112 mg dose, the serum Cmax was 1.02 ± 0.53 ?g/mL, which was reached in one hour (Tmax), while the sputum Cmax was 1048 ± 1080 ?g/g. Comparatively, for a 300 mg dose, the serum Cmax was 1.04 ± 0.58 ?g/mL, which was also reached within one hour, while the sputum Cmax was 737 ± 1028 ?g/g. The systemic exposure (AUC0-12) was also similar between the two doses, at 4.6 ± 2.0 ?g?h/mL for the 112 mg dose and 4.8 ± 2.5 ?g?h/mL for the 300 mg dose. When tobramycin was administered over a four-week cycle at 112 mg twice daily, the Cmax measured one hour after dosing ranged from 1.48 ± 0.69 ?g/mL to 1.99 ± 0.59 ?g/mL.L32739

Metabolisme

Tobramycin is not appreciably metabolized.L32739

Rute Eliminasi

Tobramycin is primarily excreted unchanged in the urine.L32739

Interaksi Obat

916 Data
Succinylcholine The therapeutic efficacy of Succinylcholine can be increased when used in combination with Tobramycin.
Metocurine iodide The therapeutic efficacy of Metocurine iodide can be increased when used in combination with Tobramycin.
Gallamine triethiodide The therapeutic efficacy of Gallamine triethiodide can be increased when used in combination with Tobramycin.
Cisatracurium Tobramycin may increase the neuromuscular blocking activities of Cisatracurium.
Rocuronium The therapeutic efficacy of Rocuronium can be increased when used in combination with Tobramycin.
Atracurium besylate The therapeutic efficacy of Atracurium besylate can be increased when used in combination with Tobramycin.
Doxacurium The therapeutic efficacy of Doxacurium can be increased when used in combination with Tobramycin.
Mivacurium The therapeutic efficacy of Mivacurium can be increased when used in combination with Tobramycin.
Decamethonium The therapeutic efficacy of Decamethonium can be increased when used in combination with Tobramycin.
Metocurine The therapeutic efficacy of Metocurine can be increased when used in combination with Tobramycin.
Pancuronium The therapeutic efficacy of Pancuronium can be increased when used in combination with Tobramycin.
Pipecuronium The therapeutic efficacy of Pipecuronium can be increased when used in combination with Tobramycin.
Vecuronium The therapeutic efficacy of Vecuronium can be increased when used in combination with Tobramycin.
Rapacuronium The therapeutic efficacy of Rapacuronium can be increased when used in combination with Tobramycin.
Pyrantel The therapeutic efficacy of Pyrantel can be increased when used in combination with Tobramycin.
Neosaxitoxin The therapeutic efficacy of Neosaxitoxin can be increased when used in combination with Tobramycin.
Atracurium The therapeutic efficacy of Atracurium can be increased when used in combination with Tobramycin.
Gallamine The therapeutic efficacy of Gallamine can be increased when used in combination with Tobramycin.
Alcuronium The therapeutic efficacy of Alcuronium can be increased when used in combination with Tobramycin.
Tubocurarine The therapeutic efficacy of Tubocurarine can be increased when used in combination with Tobramycin.
Carboplatin The risk or severity of ototoxicity and nephrotoxicity can be increased when Tobramycin is combined with Carboplatin.
Foscarnet The risk or severity of nephrotoxicity can be increased when Tobramycin is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Tobramycin.
Tenofovir disoproxil Tobramycin may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Tobramycin.
Tenofovir Tobramycin may increase the nephrotoxic activities of Tenofovir.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Tobramycin.
Zoledronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Zoledronic acid.
Alendronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Alendronic acid.
Ibandronate The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Ibandronate.
Clodronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Clodronic acid.
Risedronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Risedronic acid.
Etidronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Etidronic acid.
Incadronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Tobramycin is combined with Incadronic acid.
Taxifolin The risk or severity of nephrotoxicity can be increased when Taxifolin is combined with Tobramycin.
Licofelone The risk or severity of nephrotoxicity can be increased when Licofelone is combined with Tobramycin.
Polmacoxib The risk or severity of nephrotoxicity can be increased when Polmacoxib is combined with Tobramycin.
Ebselen The risk or severity of nephrotoxicity can be increased when Ebselen is combined with Tobramycin.
Flurbiprofen axetil The risk or severity of nephrotoxicity can be increased when Flurbiprofen axetil is combined with Tobramycin.
Acetyldigitoxin The risk or severity of adverse effects can be increased when Tobramycin is combined with Acetyldigitoxin.
Deslanoside The risk or severity of adverse effects can be increased when Tobramycin is combined with Deslanoside.
Ouabain The risk or severity of adverse effects can be increased when Tobramycin is combined with Ouabain.
Digitoxin The risk or severity of adverse effects can be increased when Tobramycin is combined with Digitoxin.
Oleandrin The risk or severity of adverse effects can be increased when Tobramycin is combined with Oleandrin.
Cymarin The risk or severity of adverse effects can be increased when Tobramycin is combined with Cymarin.
Proscillaridin The risk or severity of adverse effects can be increased when Tobramycin is combined with Proscillaridin.
Metildigoxin The risk or severity of adverse effects can be increased when Tobramycin is combined with Metildigoxin.
Lanatoside C The risk or severity of adverse effects can be increased when Tobramycin is combined with Lanatoside C.
Gitoformate The risk or severity of adverse effects can be increased when Tobramycin is combined with Gitoformate.
Acetyldigoxin The risk or severity of adverse effects can be increased when Tobramycin is combined with Acetyldigoxin.
Peruvoside The risk or severity of adverse effects can be increased when Tobramycin is combined with Peruvoside.
Torasemide The serum concentration of Tobramycin can be increased when it is combined with Torasemide.
Bumetanide The serum concentration of Tobramycin can be increased when it is combined with Bumetanide.
Etacrynic acid The serum concentration of Tobramycin can be increased when it is combined with Etacrynic acid.
Piretanide The serum concentration of Tobramycin can be increased when it is combined with Piretanide.
Azosemide The serum concentration of Tobramycin can be increased when it is combined with Azosemide.
Tripamide The serum concentration of Tobramycin can be increased when it is combined with Tripamide.
Flucloxacillin The serum concentration of Tobramycin can be decreased when it is combined with Flucloxacillin.
Phenoxymethylpenicillin The serum concentration of Tobramycin can be decreased when it is combined with Phenoxymethylpenicillin.
Dicloxacillin The serum concentration of Tobramycin can be decreased when it is combined with Dicloxacillin.
Carbenicillin The serum concentration of Tobramycin can be decreased when it is combined with Carbenicillin.
Nafcillin The serum concentration of Tobramycin can be decreased when it is combined with Nafcillin.
Hetacillin The serum concentration of Tobramycin can be decreased when it is combined with Hetacillin.
Benzylpenicilloyl polylysine The serum concentration of Tobramycin can be decreased when it is combined with Benzylpenicilloyl polylysine.
Mezlocillin The serum concentration of Tobramycin can be decreased when it is combined with Mezlocillin.
Cyclacillin The serum concentration of Tobramycin can be decreased when it is combined with Cyclacillin.
Benzylpenicillin The serum concentration of Tobramycin can be decreased when it is combined with Benzylpenicillin.
Azlocillin The serum concentration of Tobramycin can be decreased when it is combined with Azlocillin.
Cloxacillin The serum concentration of Tobramycin can be decreased when it is combined with Cloxacillin.
Amdinocillin The serum concentration of Tobramycin can be decreased when it is combined with Amdinocillin.
Bacampicillin The serum concentration of Tobramycin can be decreased when it is combined with Bacampicillin.
Meticillin The serum concentration of Tobramycin can be decreased when it is combined with Meticillin.
Pivampicillin The serum concentration of Tobramycin can be decreased when it is combined with Pivampicillin.
Pivmecillinam The serum concentration of Tobramycin can be decreased when it is combined with Pivmecillinam.
Ticarcillin The serum concentration of Tobramycin can be decreased when it is combined with Ticarcillin.
Azidocillin The serum concentration of Tobramycin can be decreased when it is combined with Azidocillin.
Carindacillin The serum concentration of Tobramycin can be decreased when it is combined with Carindacillin.
Sultamicillin The serum concentration of Tobramycin can be decreased when it is combined with Sultamicillin.
Temocillin The serum concentration of Tobramycin can be decreased when it is combined with Temocillin.
Epicillin The serum concentration of Tobramycin can be decreased when it is combined with Epicillin.
Pheneticillin The serum concentration of Tobramycin can be decreased when it is combined with Pheneticillin.
Carfecillin The serum concentration of Tobramycin can be decreased when it is combined with Carfecillin.
Propicillin The serum concentration of Tobramycin can be decreased when it is combined with Propicillin.
Clometocillin The serum concentration of Tobramycin can be decreased when it is combined with Clometocillin.
Sulbenicillin The serum concentration of Tobramycin can be decreased when it is combined with Sulbenicillin.
Penamecillin The serum concentration of Tobramycin can be decreased when it is combined with Penamecillin.
Talampicillin The serum concentration of Tobramycin can be decreased when it is combined with Talampicillin.
Aspoxicillin The serum concentration of Tobramycin can be decreased when it is combined with Aspoxicillin.
Metampicillin The serum concentration of Tobramycin can be decreased when it is combined with Metampicillin.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Tobramycin.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Tobramycin.
Lymecycline The risk or severity of neuromuscular blockade can be increased when Lymecycline is combined with Tobramycin.
Clomocycline The risk or severity of neuromuscular blockade can be increased when Clomocycline is combined with Tobramycin.
Quinine The risk or severity of neuromuscular blockade can be increased when Quinine is combined with Tobramycin.
Tigecycline The risk or severity of neuromuscular blockade can be increased when Tigecycline is combined with Tobramycin.
Oxytetracycline The risk or severity of neuromuscular blockade can be increased when Oxytetracycline is combined with Tobramycin.
Demeclocycline The risk or severity of neuromuscular blockade can be increased when Demeclocycline is combined with Tobramycin.
Magnesium sulfate The risk or severity of neuromuscular blockade can be increased when Magnesium sulfate is combined with Tobramycin.
Metacycline The risk or severity of neuromuscular blockade can be increased when Tobramycin is combined with Metacycline.
Minocycline The risk or severity of neuromuscular blockade can be increased when Tobramycin is combined with Minocycline.

Target Protein

16S ribosomal RNA
23S ribosomal RNA
Bacterial outer membrane
Cytoplasmic membrane

Referensi & Sumber

Synthesis reference: Istvan Bakondi-Kovacs, "Metabolic controlled fermentation process for carbamoyl tobramycin production." U.S. Patent US20020197683, issued December 26, 2002.
Artikel (PubMed)
  • PMID: 30447062
    Serio AW, Keepers T, Andrews L, Krause KM: Aminoglycoside Revival: Review of a Historically Important Class of Antimicrobials Undergoing Rejuvenation. EcoSal Plus. 2018 Nov;8(1). doi: 10.1128/ecosalplus.ESP-0002-2018.
  • PMID: 25645838
    Bulitta JB, Ly NS, Landersdorfer CB, Wanigaratne NA, Velkov T, Yadav R, Oliver A, Martin L, Shin BS, Forrest A, Tsuji BT: Two mechanisms of killing of Pseudomonas aeruginosa by tobramycin assessed at multiple inocula via mechanism-based modeling. Antimicrob Agents Chemother. 2015 Apr;59(4):2315-27. doi: 10.1128/AAC.04099-14. Epub 2015 Feb 2.
  • PMID: 3013085
    Moore RA, Bates NC, Hancock RE: Interaction of polycationic antibiotics with Pseudomonas aeruginosa lipopolysaccharide and lipid A studied by using dansyl-polymyxin. Antimicrob Agents Chemother. 1986 Mar;29(3):496-500. doi: 10.1128/aac.29.3.496.
  • PMID: 6794444
    Hancock RE, Raffle VJ, Nicas TI: Involvement of the outer membrane in gentamicin and streptomycin uptake and killing in Pseudomonas aeruginosa. Antimicrob Agents Chemother. 1981 May;19(5):777-85. doi: 10.1128/aac.19.5.777.
  • PMID: 3325794
    Taber HW, Mueller JP, Miller PF, Arrow AS: Bacterial uptake of aminoglycoside antibiotics. Microbiol Rev. 1987 Dec;51(4):439-57.
  • PMID: 2426712
    Davis BD, Chen LL, Tai PC: Misread protein creates membrane channels: an essential step in the bactericidal action of aminoglycosides. Proc Natl Acad Sci U S A. 1986 Aug;83(16):6164-8. doi: 10.1073/pnas.83.16.6164.
  • PMID: 30113694
    O'Sullivan ME, Poitevin F, Sierra RG, Gati C, Dao EH, Rao Y, Aksit F, Ciftci H, Corsepius N, Greenhouse R, Hayes B, Hunter MS, Liang M, McGurk A, Mbgam P, Obrinsky T, Pardo-Avila F, Seaberg MH, Cheng AG, Ricci AJ, DeMirci H: Aminoglycoside ribosome interactions reveal novel conformational states at ambient temperature. Nucleic Acids Res. 2018 Oct 12;46(18):9793-9804. doi: 10.1093/nar/gky693.
  • PMID: 30413565
    Ying L, Zhu H, Shoji S, Fredrick K: Roles of specific aminoglycoside-ribosome interactions in the inhibition of translation. RNA. 2019 Feb;25(2):247-254. doi: 10.1261/rna.068460.118. Epub 2018 Nov 9.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 223 • International brands: 13
Produk
  • Aj-tobramycin
    Liquid • 40 mg / mL • Intramuscular; Intravenous • Canada • Generic • Approved
  • Apo-tobramycin
    Solution • 0.3 % • Ophthalmic • Canada • Generic • Approved
  • Bethkis
    Solution • 300 mg/4mL • Respiratory (inhalation) • US • Approved
  • Jamp-tobramycin
    Solution • 40 mg / mL • Intramuscular; Intravenous • Canada • Generic • Approved
  • Kitabis Pak
    Solution • 300 mg/5mL • Respiratory (inhalation) • US • Approved
  • Kitabis Pak
    Solution • 300 mg/5mL • Respiratory (inhalation) • US • Approved
  • Nebcin Inj 1.2gm/30ml
    Liquid • 1.2 g / vial • Intramuscular; Intravenous • Canada • Approved
  • Nebcin Inj 10mg/ml
    Liquid • 10 mg / mL • Intramuscular; Intravenous • Canada • Approved
Menampilkan 8 dari 223 produk.
International Brands
  • Aktob — Akorn
  • Alveoterol — Tetrafarm
  • Amgy — Kobec
  • Bactob — Solitaire
  • Belbarmicina — Quimica Luar
  • Bideon Biotic — Fecofar
  • Bioptic — Bausch & Lomb
  • Bramitob — Torrex
  • Gernebcin — Infectopharm
  • Nebcin — Lilly

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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