Peringatan Keamanan

Toxicity information regarding tedizolid is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as nausea, headache, dizziness, diarrhea, and vomiting. Symptomatic and supportive measures are recommended.L11232

Tedizolid

DB14569

small molecule approved investigational

Deskripsi

Drug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and penicillin-resistant Streptococcus penumoniae, represent a massive public health threat.A199086, A199131 Tedizolid is a member of the oxazolidinone class of antibiotics, which includes the previously approved linezolid and is generally effective against multidrug-resistant Gram-positive bacteria. Tedizolid is indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and is generally more effective and more tolerable than linezolid.L11232, A199086, A199050

Tedizolid was approved by the FDA on June 20, 2014, for sale by Cubist Pharmaceuticals as tedizolid phosphate (SIVEXTRO®). This product is currently available as both an oral tablet and as a powder for intravenous injection.L11232

Struktur Molekul 2D

Berat 370.344
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Tedizolid has a half-life of approximately 12 hours.[L11232, A199140, A7642]
Volume Distribusi The volume of distribution for tedizolid following a single intravenous dose of 200 mg is between 67 and 80 L.[L11232] In a study involving oral administration of 200 mg tedizolid to steady-state, the volume of distribution was 108 ± 21 L, while a single 600 mg oral dose resulted in an apparent volume of distribution of 113.3 ± 19.3 L.[A199152, A199155] Tedizolid has been observed to penetrate the interstitial space of both adipose and skeletal muscle tissue and is also found in the epithelial lining fluid as well as in alveolar macrophages.[L11232, A199152, A199155]
Klirens (Clearance) Tedizolid has an apparent oral clearance of 6.9 ± 1.7 L/hr for a single dose and 8.4 ± 2.1 L/hr at steady-state. The systemic clearance is 6.4 ± 1.2 L/hr for a single dose and 5.9 ± 1.4 L/hr at steady-state.[L11232, A199140, A7642]

Absorpsi

Tedizolid reaches peak plasma concentrations within three hours for oral administration and within one hour following intravenous administration; the absolute oral bioavailability is approximately 91%. Food has no effect on absorption. When given once daily, either orally or intravenously, tedizolid reaches steady-state concentrations in approximately three days.L11232, A7642, A199140 The Cmax for tedizolid after a single dose/at steady-state is 2.0 ± 0.7/2.2 ± 0.6 mcg/mL for oral administration, and 2.3 ± 0.6/3.0 ± 0.7 mcg/mL for intravenous administration, respectively. Similarly, the Tmax has a median (range) of 2.5 (1.0 - 8.0)/3.5 (1.0 - 6.0) hrs for the oral route and 1.1 (0.9 - 1.5)/1.2 (0.9 - 1.5) hrs when given intravenous. The AUC is 23.8 ± 6.8/25.6 ± 8.4 mcg\*hr/mL for oral and 26.6 ± 5.2/29.2 ± 6.2 mcg\*hr/mL for intravenous.L11232, A7642, A199140

Metabolisme

Tedizolid is administered as a phosphate prodrug that is converted to tedizolid (the circulating active moiety). Prior to excretion, the majority of tedizolid is converted to an inactive sulphate conjugate in the liver, though this is unlikely to involve the action of cytochrome P450-family enzymes.L11232, A199050

Rute Eliminasi

When given as a single oral dose, approximately 82% of tedizolid is excreted via the feces and 18% in urine. The majority is found as the inactive sulphate conjugate, with only 3% recovered unchanged. Over 85% of the elimination occurs within 96 hours.L11232, A199050

Interaksi Obat

55 Data
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Tedizolid.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Tedizolid.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Tedizolid.
Dicoumarol The risk or severity of bleeding can be increased when Tedizolid is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Tedizolid is combined with Phenindione.
Warfarin The risk or severity of bleeding can be increased when Tedizolid is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Tedizolid is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Tedizolid is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Tedizolid is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Tedizolid is combined with Coumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Tedizolid is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Tedizolid is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Tedizolid is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Tedizolid is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Tedizolid is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Tedizolid is combined with Tioclomarol.
(S)-Warfarin The risk or severity of bleeding can be increased when Tedizolid is combined with (S)-Warfarin.
Lactulose The therapeutic efficacy of Lactulose can be decreased when used in combination with Tedizolid.
Vibrio cholerae CVD 103-HgR strain live antigen The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Tedizolid.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Tedizolid.
Lidocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Tetrodotoxin.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Quinisocaine.
Cisatracurium Tedizolid may increase the neuromuscular blocking activities of Cisatracurium.
Ambroxol The risk or severity of methemoglobinemia can be increased when Tedizolid is combined with Ambroxol.
Fecal microbiota The therapeutic efficacy of Fecal microbiota can be decreased when used in combination with Tedizolid.

Target Protein

23S ribosomal RNA

Referensi & Sumber

Synthesis reference: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson. "Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate." U.S. Patent US9624250B2, issued April 18, 2017.
Artikel (PubMed)
  • 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.
  • PMID: 18757750
    Wilson DN, Schluenzen F, Harms JM, Starosta AL, Connell SR, Fucini P: The oxazolidinone antibiotics perturb the ribosomal peptidyl-transferase center and effect tRNA positioning. Proc Natl Acad Sci U S A. 2008 Sep 9;105(36):13339-44. doi: 10.1073/pnas.0804276105. Epub 2008 Aug 29.
  • PMID: 17499045
    Leach KL, Swaney SM, Colca JR, McDonald WG, Blinn JR, Thomasco LM, Gadwood RC, Shinabarger D, Xiong L, Mankin AS: The site of action of oxazolidinone antibiotics in living bacteria and in human mitochondria. Mol Cell. 2007 May 11;26(3):393-402. doi: 10.1016/j.molcel.2007.04.005.
  • PMID: 9333037
    Shinabarger DL, Marotti KR, Murray RW, Lin AH, Melchior EP, Swaney SM, Dunyak DS, Demyan WF, Buysse JM: Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother. 1997 Oct;41(10):2132-6.
  • PMID: 31426596
    Koulenti D, Xu E, Mok IYS, Song A, Karageorgopoulos DE, Armaganidis A, Lipman J, Tsiodras S: Novel Antibiotics for Multidrug-Resistant Gram-Positive Microorganisms. Microorganisms. 2019 Aug 18;7(8). pii: microorganisms7080270. doi: 10.3390/microorganisms7080270.
  • PMID: 22208312
    McCusker KP, Fujimori DG: The chemistry of peptidyltransferase center-targeted antibiotics: enzymatic resistance and approaches to countering resistance. ACS Chem Biol. 2012 Jan 20;7(1):64-72. doi: 10.1021/cb200418f. Epub 2011 Dec 30.
  • PMID: 16723564
    McKee EE, Ferguson M, Bentley AT, Marks TA: Inhibition of mammalian mitochondrial protein synthesis by oxazolidinones. Antimicrob Agents Chemother. 2006 Jun;50(6):2042-9. doi: 10.1128/AAC.01411-05.
  • PMID: 32059790
    Laxminarayan R, Van Boeckel T, Frost I, Kariuki S, Khan EA, Limmathurotsakul D, Larsson DGJ, Levy-Hara G, Mendelson M, Outterson K, Peacock SJ, Zhu YG: The Lancet Infectious Diseases Commission on antimicrobial resistance: 6 years later. Lancet Infect Dis. 2020 Apr;20(4):e51-e60. doi: 10.1016/S1473-3099(20)30003-7. Epub 2020 Feb 11.
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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