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 phosphate

DB09042

small molecule approved

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 450.323
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.[A7638, 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.[A7638, 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.A7638, 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.A7638, L11232, A199050

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food.

Interaksi Obat

424 Data
Clozapine The risk or severity of neutropenia can be increased when Tedizolid phosphate is combined with Clozapine.
Metamizole The risk or severity of myelosuppression can be increased when Metamizole is combined with Tedizolid phosphate.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Citalopram.
Eletriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Eletriptan.
Cabergoline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Cabergoline.
Venlafaxine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Venlafaxine.
Zolmitriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Zolmitriptan.
Dihydroergotamine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Dihydroergotamine.
Amitriptyline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Amitriptyline.
Protriptyline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Protriptyline.
Meperidine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Meperidine.
Imipramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Imipramine.
Fluoxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Fluoxetine.
Duloxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Duloxetine.
Dextromethorphan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Dextromethorphan.
Nortriptyline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Nortriptyline.
Amoxapine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Amoxapine.
Mazindol The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Mazindol.
Sumatriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Sumatriptan.
Ergotamine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Ergotamine.
Paroxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Paroxetine.
Trimipramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Trimipramine.
Tranylcypromine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Tranylcypromine.
Phenelzine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Phenelzine.
Fentanyl The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Fentanyl.
Almotriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Almotriptan.
Maprotiline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Maprotiline.
Naratriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Naratriptan.
Rizatriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Rizatriptan.
Frovatriptan The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Frovatriptan.
Selegiline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Selegiline.
Ergoloid mesylate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Ergoloid mesylate.
Promethazine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Promethazine.
Sertraline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Sibutramine.
Chlorpheniramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Chlorpheniramine.
Doxepin The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Doxepin.
Nefazodone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Nefazodone.
Desipramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Desipramine.
Procarbazine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Procarbazine.
Moclobemide The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Moclobemide.
Bromocriptine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Bromocriptine.
Clomipramine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Clomipramine.
Isocarboxazid The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Isocarboxazid.
Ergometrine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Ergometrine.
Lithium cation The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lithium cation.
Rasagiline The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Rasagiline.
Zimelidine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Zimelidine.
Lorcaserin The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lorcaserin.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Milnacipran.
Mianserin The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Mianserin.
Vilazodone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Vilazodone.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Desvenlafaxine.
Dexmethylphenidate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Dexmethylphenidate.
Seproxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Levomilnacipran.
Indalpine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Indalpine.
Vortioxetine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Vortioxetine.
Dosulepin The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Dosulepin.
Etoperidone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Etoperidone.
Tianeptine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Tianeptine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Alaproclate.
Lumateperone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lumateperone.
Lorpiprazole The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lorpiprazole.
Methadone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Methadone.
Linezolid The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Linezolid.
Tapentadol The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Tapentadol.
Tramadol The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Tramadol.
Mirtazapine The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Mirtazapine.
Trazodone The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Trazodone.
Escitalopram The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Escitalopram.
Tenamfetamine Tedizolid phosphate may increase the hypertensive activities of Tenamfetamine.
Amphetamine Tedizolid phosphate may increase the hypertensive activities of Amphetamine.
Phentermine Tedizolid phosphate may increase the hypertensive activities of Phentermine.
Midodrine Tedizolid phosphate may increase the hypertensive activities of Midodrine.
Norepinephrine Tedizolid phosphate may increase the hypertensive activities of Norepinephrine.
Phenylephrine Tedizolid phosphate may increase the hypertensive activities of Phenylephrine.
Phenylpropanolamine Tedizolid phosphate may increase the hypertensive activities of Phenylpropanolamine.
Labetalol Tedizolid phosphate may increase the hypertensive activities of Labetalol.
Metaraminol Tedizolid phosphate may increase the hypertensive activities of Metaraminol.
Epinephrine Tedizolid phosphate may increase the hypertensive activities of Epinephrine.
Methoxamine Tedizolid phosphate may increase the hypertensive activities of Methoxamine.
Orciprenaline Tedizolid phosphate may increase the hypertensive activities of Orciprenaline.
Phenmetrazine Tedizolid phosphate may increase the hypertensive activities of Phenmetrazine.
Dobutamine Tedizolid phosphate may increase the hypertensive activities of Dobutamine.
Pseudoephedrine Tedizolid phosphate may increase the hypertensive activities of Pseudoephedrine.
Benzphetamine Tedizolid phosphate may increase the hypertensive activities of Benzphetamine.
Ritodrine Tedizolid phosphate may increase the hypertensive activities of Ritodrine.
Terbutaline Tedizolid phosphate may increase the hypertensive activities of Terbutaline.
Oxymetazoline Tedizolid phosphate may increase the hypertensive activities of Oxymetazoline.
Diethylpropion Tedizolid phosphate may increase the hypertensive activities of Diethylpropion.
Dopamine Tedizolid phosphate may increase the hypertensive activities of Dopamine.
Isoprenaline Tedizolid phosphate may increase the hypertensive activities of Isoprenaline.
Acebutolol Tedizolid phosphate may increase the hypertensive activities of Acebutolol.
Lisdexamfetamine Tedizolid phosphate may increase the hypertensive activities of Lisdexamfetamine.
Fenoterol Tedizolid phosphate may increase the hypertensive activities of Fenoterol.
Ephedrine Tedizolid phosphate may increase the hypertensive activities of Ephedrine.

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: 24875463
    Ong V, Flanagan S, Fang E, Dreskin HJ, Locke JB, Bartizal K, Prokocimer P: Absorption, distribution, metabolism, and excretion of the novel antibacterial prodrug tedizolid phosphate. Drug Metab Dispos. 2014 Aug;42(8):1275-84. doi: 10.1124/dmd.113.056697. Epub 2014 May 29.
  • PMID: 24989138
    Flanagan S, Fang E, Munoz KA, Minassian SL, Prokocimer PG: Single- and multiple-dose pharmacokinetics and absolute bioavailability of tedizolid. Pharmacotherapy. 2014 Sep;34(9):891-900. doi: 10.1002/phar.1458. Epub 2014 Jul 3.
  • 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.
Menampilkan 8 dari 14 artikel.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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