Peringatan Keamanan

Clinical signs of overdosage observed in rats were decreased activity and ataxia (2000 mg/kg/day) and in dogs were vomiting and tremors (3000 mg/kg/day).L32965 Treatment of overdose should involve symptomatic and supportive measures and may include hemodialysis if clinically necessary.

Linezolid

DB00601

small molecule approved investigational

Deskripsi

Linezolid is a synthetic antibiotic which is used for the treatment of infections caused by aerobic Gram-positive bacteria. Its effects are bacteriostatic against both enterococci and staphylococci and bactericidal against most isolates of streptococci.L32965 Linezolid exerts its antibacterial activity by inhibiting the initiation of bacterial protein synthesis - more specifically, it binds to the 23S ribosomal RNA of the 50S subunitA11227,A199050 and, in doing so, prevents the formation of the 70S initiation complex which is essential for bacterial reproduction.

Linezolid was initially approved in 2000 and was the first member of the oxazolidinone antibiotic class.A233425 A second member of this class, tedizolid, was approved by the FDA in 2014 and is considered generally more effective and tolerable than its predecessor.

Struktur Molekul 2D

Berat 337.3461
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life is estimated to be between 5 and 7 hours.[L33135]
Volume Distribusi At steady-state, the volume of distribution of linezolid in healthy adults is approximately 40-50 liters.[L32965]
Klirens (Clearance) Total clearance of linezolid is estimated to be 100-200 mL/min, the majority of which appears to be non-renal.[L33135] Mean renal clearance is approximately 40 mL/min, which suggests net tubular reabsorption,[L32965] while non-renal clearance is estimated to account for roughly 65% of total clearance,[L32965] or 70-150 mL/min on average.[L33135] Variability in linezolid clearance is high, particularly for non-renal clearance.[L33135]

Absorpsi

Linezolid is extensively absorbed following oral administration and has an absolute bioavailability of approximately 100%.L32965 Maximum plasma concentrations are reached within approximately 1 to 2 hours after dosing (Tmax) and range from 8.1-12.9 mcg/mL after single doses and 11.0-21.2 mcg/mL after multiple dosing.L32965 The absorption of orally administered linezolid is not significantly affected by co-administration with food and it may therefore be given without regard to the timing of meals.L32965

Metabolisme

Linezolid is primarily metabolized to two inactive metabolites: an aminoethoxyacetic acid metabolite (PNU-142300) and a hydroxyethyl glycine metabolite (PNU-142586), both of which are the result of morpholine ring oxidation.L32965,A233435 The hydroxyethyl glycine metabolite - the most abundant of the two metabolitesL33135 - is likely generated via non-enzymatic processes, though further detail has not been elucidated.L32965,A233435 While the specific enzymes responsible for the biotransformation of linezolid are unclear, it does not appear to be subject to metabolism via the CYP450 enzyme system, nor does it meaningfully inhibit or induce these enzymes.L33135 Linezolid is, however, a reversible and non-selective inhibitor of monoamine oxidase enzymes.L32965

Rute Eliminasi

Urinary excretion is the primary means by which linezolid and its metabolic products are excreted. Following the administration of a radiolabeled dose of linezolid under steady-state conditions, approximately 84% of radioactivity was recovered in the urine,A233435 of which approximately 30% is unchanged parent drug, 40% is the hydroxyethyl glycine metabolite, and 10% is the aminoethoxyacetic acid metabolite.L32965 Fecal elimination is comparatively minor, with no parent drug observed in feces and only 6% and 3% of an administered dose found in the feces as the hydroxyethyl glycine metabolite and the aminoethoxyacetic acid metabolite, respectively.L32965

Interaksi Makanan

2 Data
  • 1. Avoid tyramine-containing foods and supplements. Avoid food containing high amounts of tyramine (>100mg). Tyramine-containing foods include cheese, red wine, fava beans, pickled foods, cured foods, and alcoholic beverages.
  • 2. Take with or without food. Co-administration with food does not significantly alter the pharmacokinetics of linezolid.

Interaksi Obat

1515 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Linezolid.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Linezolid.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Linezolid.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Linezolid.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Linezolid.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Linezolid.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Linezolid.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Linezolid.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Linezolid.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Linezolid.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Linezolid.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Linezolid.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Linezolid.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Linezolid.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Linezolid.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Linezolid.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Linezolid.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Linezolid.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Linezolid.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Linezolid.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Linezolid.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Linezolid.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Linezolid.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Linezolid.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Linezolid.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Linezolid.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Linezolid.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Linezolid.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Linezolid.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Linezolid.
Cladribine Linezolid may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Linezolid.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Linezolid.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Linezolid.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Linezolid.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Linezolid.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Linezolid.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Linezolid.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Linezolid.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Linezolid.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Linezolid.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Linezolid.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Linezolid.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Linezolid.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Linezolid.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Linezolid.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Linezolid.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Linezolid.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Linezolid.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Linezolid.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Linezolid.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Linezolid.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Linezolid.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Linezolid.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Linezolid.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Linezolid.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Linezolid.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Linezolid.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Linezolid.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Linezolid.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Linezolid.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Linezolid.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Linezolid.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Linezolid.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Linezolid.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Linezolid.
Imatinib The risk or severity of adverse effects can be increased when Linezolid is combined with Imatinib.
Triamcinolone The risk or severity of adverse effects can be increased when Linezolid is combined with Triamcinolone.
Clofarabine The risk or severity of adverse effects can be increased when Linezolid is combined with Clofarabine.
Prednisone The risk or severity of adverse effects can be increased when Linezolid is combined with Prednisone.
Pemetrexed Linezolid may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Fludrocortisone The risk or severity of adverse effects can be increased when Linezolid is combined with Fludrocortisone.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Linezolid is combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of adverse effects can be increased when Linezolid is combined with Daunorubicin.
Tretinoin The risk or severity of elevated intracranial pressure can be increased when Linezolid is combined with Tretinoin.
Irinotecan The risk or severity of adverse effects can be increased when Linezolid is combined with Irinotecan.
Methimazole The risk or severity of adverse effects can be increased when Linezolid is combined with Methimazole.
Etoposide The risk or severity of adverse effects can be increased when Linezolid is combined with Etoposide.
Sulfasalazine The risk or severity of adverse effects can be increased when Linezolid is combined with Sulfasalazine.
Dacarbazine The risk or severity of adverse effects can be increased when Linezolid is combined with Dacarbazine.
Temozolomide The risk or severity of adverse effects can be increased when Linezolid is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Linezolid is combined with Penicillamine.
Prednisolone The risk or severity of adverse effects can be increased when Linezolid is combined with Prednisolone.
Sirolimus The risk or severity of adverse effects can be increased when Linezolid is combined with Sirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Linezolid is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Linezolid is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Linezolid is combined with Carboplatin.
Methylprednisolone The risk or severity of adverse effects can be increased when Linezolid is combined with Methylprednisolone.
Dactinomycin The risk or severity of adverse effects can be increased when Linezolid is combined with Dactinomycin.
Cytarabine The risk or severity of adverse effects can be increased when Linezolid is combined with Cytarabine.
Azathioprine The risk or severity of adverse effects can be increased when Linezolid is combined with Azathioprine.
Doxorubicin The risk or severity of adverse effects can be increased when Linezolid is combined with Doxorubicin.
Hydroxyurea The risk or severity of adverse effects can be increased when Linezolid is combined with Hydroxyurea.
Busulfan The risk or severity of adverse effects can be increased when Linezolid is combined with Busulfan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Linezolid is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Linezolid is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Linezolid is combined with Mercaptopurine.
Melphalan The risk or severity of adverse effects can be increased when Linezolid is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Linezolid is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Linezolid is combined with Flucytosine.

Target Protein

23S ribosomal RNA

Referensi & Sumber

Synthesis reference: Brickner SJ, Hutchinson DK, Barbachyn MR, Manninen PR, Ulanowicz DA, Garmon SA, Grega KC, Hendges SK, Toops DS, Ford CW, Zurenko GE: Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections. J Med Chem. 1996 Feb 2;39(3):673-9. doi: 10.1021/jm9509556.
Artikel (PubMed)
  • PMID: 16857689
    Park IN, Hong SB, Oh YM, Kim MN, Lim CM, Lee SD, Koh Y, Kim WS, Kim DS, Kim WD, Shim TS: Efficacy and tolerability of daily-half dose linezolid in patients with intractable multidrug-resistant tuberculosis. J Antimicrob Chemother. 2006 Sep;58(3):701-4. Epub 2006 Jul 19.
  • PMID: 30969615
    Azzouz A, Preuss CV: Linezolid .
  • PMID: 21434942
    Leach KL, Brickner SJ, Noe MC, Miller PF: Linezolid, the first oxazolidinone antibacterial agent. Ann N Y Acad Sci. 2011 Mar;1222:49-54. doi: 10.1111/j.1749-6632.2011.05962.x.
  • PMID: 21521707
    Dryden MS: Linezolid pharmacokinetics and pharmacodynamics in clinical treatment. J Antimicrob Chemother. 2011 May;66 Suppl 4:iv7-iv15. doi: 10.1093/jac/dkr072.
  • PMID: 11454733
    Slatter JG, Stalker DJ, Feenstra KL, Welshman IR, Bruss JB, Sams JP, Johnson MG, Sanders PE, Hauer MJ, Fagerness PE, Stryd RP, Peng GW, Shobe EM: Pharmacokinetics, metabolism, and excretion of linezolid following an oral dose of (14)Clinezolid to healthy human subjects. Drug Metab Dispos. 2001 Aug;29(8):1136-45.
  • PMID: 14531724
    Stalker DJ, Jungbluth GL: Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial. Clin Pharmacokinet. 2003;42(13):1129-40. doi: 10.2165/00003088-200342130-00004.
  • PMID: 12690106
    Colca JR, McDonald WG, Waldon DJ, Thomasco LM, Gadwood RC, Lund ET, Cavey GS, Mathews WR, Adams LD, Cecil ET, Pearson JD, Bock JH, Mott JE, Shinabarger DL, Xiong L, Mankin AS: Cross-linking in the living cell locates the site of action of oxazolidinone antibiotics. J Biol Chem. 2003 Jun 13;278(24):21972-9. Epub 2003 Apr 10.
  • PMID: 29063519
    Roger C, Roberts JA, Muller L: Clinical Pharmacokinetics and Pharmacodynamics of Oxazolidinones. Clin Pharmacokinet. 2018 May;57(5):559-575. doi: 10.1007/s40262-017-0601-x.

Contoh Produk & Brand

Produk: 86 • International brands: 12
Produk
  • Apo-linezolid
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Jamp Linezolid
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Linezolid
    Injection, solution • 2 mg/1mL • Intravenous • US • Generic • Approved
  • Linezolid
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
  • Linezolid
    Injection, solution • 200 mg/100mL • Intravenous • US • Generic • Approved
  • Linezolid
    Injection, solution • 600 mg/300mL • Intravenous • US • Generic • Approved
  • Linezolid
    Injection, solution • 2 mg/1mL • Intravenous • US • Generic • Approved
  • Linezolid
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 86 produk.
International Brands
  • Antizolid — Verisfield
  • Linosept — Orion
  • Linozid — Orion
  • Lizbid — Abbott
  • Lizemox — Molekule
  • Lizolid — Glenmark
  • Xolid — Corona
  • Zenix — Hemofarm
  • Zizolid — Biofarma
  • Zodlin — FDC

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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