Peringatan Keamanan

As with other aminoglycosides, nephrotoxicity and ototoxicity are associated with gentamicin.A232294 Signs of nephrotoxicity include an increase in plasma creatinine and urea, while signs of ototoxicity include issues with balance, nausea, tinnitus, and hearing loss.A234339 It is important to note that aminoglycoside-induced nephrotoxicity is typically reversible, while ototoxicity is more likely to be permanent.A232294 The risk of both toxicities increases with long-term gentamicin therapy.A234130 Gentamicin is considered to be more vestibulotoxic than cochleotoxic compared to other aminoglycosides.A232294,A234334 Unfortunately, gentamicin-related ototoxicity does not correlate with cumulative dosing, peak and trough levels, or dosing schedule.A234339 The unpredictability of ototoxicity supports close monitoring of the patient throughout treatment.A234339 In cases of toxicity or overdose, the medication should be discontinued immediately; hemodialysis may be initiated to lower gentamicin serum concentrations.L33254

Gentamicin

DB00798

small molecule approved vet_approved

Deskripsi

Gentamicin is a bactericidal aminoglycoside that was discovered and isolated from Micromonospora purpurea in 1963.A234349 It is one of the most frequently prescribed aminoglycosides due to its spectrum of activity, low cost, and availability.A234339,A234354 Gentamicin is effective against both gram-positive and gram-negative organisms but is particularly useful for the treatment of severe gram-negative infections including those caused by Pseudomonas aeruginosa.A233325,A234359,A234364 There is the added benefit of synergy when gentamicin is co-administered with other antibacterials such as beta-lactams.A234364 This synergistic activity is not only important for the treatment of complex infections, but can also contribute to dose optimization and reduced adverse effects.A234359,A234364

Although gentamicin is well-established and may be used in a variety of clinical applications, it is also associated with severe adverse effects including nephrotoxicity and ototoxicity which may limit its use.A234369

Struktur Molekul 2D

Berat 1390.728
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) One study assessing the pharmacokinetics of gentamicin in children and adults reported a mean half-life of 75 minutes after intravenous administration.[A234200] The mean half-life associated with intramuscular administration was about 29 minutes longer.[A234200] Fever and anemia may result in a shorter half-life although dose adjustments are not usually necessary.[A234200,L33254] Severe burns are also associated with a shorter half-life and may result in lower gentamicin serum concentrations.[L33254]
Volume Distribusi -
Klirens (Clearance) The renal clearance of gentamicin is comparable to individual creatinine clearance.[A234210,L33254]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Gentamicin undergoes little to no metabolism.L33254

Rute Eliminasi

Gentamicin is excreted primarily by the kidneys. In patients with normal renal function, 70% or more of an initial gentamicin dose can be recovered in the urine within 24 hours. Excretion of gentamicin is significantly reduced in patients with renal impairment.L33254

Interaksi Obat

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

Target Protein

30S ribosomal protein S12 rpsL
16S ribosomal RNA
23S ribosomal RNA
Bacterial outer membrane
Cytoplasmic membrane
NH(3)-dependent NAD(+) synthetase nadE
Dihydrofolate reductase DHFR

Referensi & Sumber

Synthesis reference: George H. Scherr, "Preparation of gentamicin sensitized particles for agglutination tests." U.S. Patent US4100268, issued August, 1975.
Artikel (PubMed)
  • PMID: 32491482
    Chaves BJ, Tadi P: Gentamicin .
  • PMID: 1202109
    Siber GR, Echeverria P, Smith AL, Paisley JW, Smith DH: Pharmacokinetics of gentamicin in children and adults. J Infect Dis. 1975 Dec;132(6):637-51. doi: 10.1093/infdis/132.6.637.
  • PMID: 20014601
    Jones TE, Peter JV, Field J: Aminoglycoside clearance is a good estimate of creatinine clearance in intensive care unit patients. Anaesth Intensive Care. 2009 Nov;37(6):944-52. doi: 10.1177/0310057X0903700611.
  • PMID: 22554194
    Ahmed RM, Hannigan IP, MacDougall HG, Chan RC, Halmagyi GM: Gentamicin ototoxicity: a 23-year selected case series of 103 patients. Med J Aust. 2012 Jun 18;196(11):701-4. doi: 10.5694/mja11.10850.
  • PMID: 15241236
    Black FO, Pesznecker S, Stallings V: Permanent gentamicin vestibulotoxicity. Otol Neurotol. 2004 Jul;25(4):559-69. doi: 10.1097/00129492-200407000-00025.
  • PMID: 31643557
    Authors unspecified: Aminoglycosides .
  • PMID: 6015651
    Authors unspecified: Gentamicin. Br Med J. 1967 Jan 21;1(5533):158-9.
  • PMID: 26719956
    Kushner B, Allen PD, Crane BT: Frequency and Demographics of Gentamicin Use. Otol Neurotol. 2016 Feb;37(2):190-5. doi: 10.1097/MAO.0000000000000937.
Menampilkan 8 dari 20 artikel.

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