Peringatan Keamanan

In case of suspected overdose, plazomicin therapy should be discontinued with initiation of supportive care. Maintenance of glomerular filtration and careful monitoring of renal function is recommended. Hemodialysis may be used to facilitate drug elimination, and this may be especially clinically useful in patients with compromised renal function FDA Label.

Plazomicin

DB12615

small molecule approved investigational

Deskripsi

Developed by Achaogen biopharmaceuticals, plazomicin is a next-generation aminoglycoside synthetically derived from DB12604. The structure of plazomicin was established via appending hydroxylaminobutyric acid to DB12604 at position 1 and 2-hydroxyethyl group at position 6' A33942. It was designed to evade all clinically relevant aminoglycoside-modifying enzymes, which contribute to the main resistance mechanism for aminoglycoside therapy A33942. However, acquired resistance of aminoglycosides may arise through over expression of efflux pumps and ribosomal modification by bacteria, which results from amino acid or rRNA sequence mutations A33942. Like other aminoglycosides, plazomicin is ineffective against bacterial isolates that produce 16S rRNA methyltransferases FDA Label. Plazomicin mediates the antibacterial activity against pathogens including carbapenem-resistant (CRE) and extended-spectrum beta-lactamase (ESBL) producing Enterobacteriaceae. It mediates the antibacterial activity by binding to bacterial 30S ribosomal subunit and inhibiting protein synthesis FDA Label. On June 28th, 2018, plazomicin sulfate was approved by the FDA for use in adult patients for the treatment of complicated urinary tract infections (cUTI) including Pyelonephritis. It is marketed as Zemdri and is administered via once-daily intravenous infusion.

Struktur Molekul 2D

Berat 592.691
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean (±SD) half-life of plazomicin was 3.5 h (±0.5) in healthy adults with normal renal function receiving 15 mg/kg plazomicin via intravenous infusion [FDA Label].
Volume Distribusi The mean (±SD) volume of distribution is 17.9 (±4.8) L in healthy adults and 30.8 (±12.1) L in cUTI patients [FDA Label].
Klirens (Clearance) Following administration of 15 mg/kg plazomicin by 30-minute IV infusion, the mean (±SD) total body clearance in healthy adults and cUTI patients is 4.5 (±0.9) and 5.1 (±2.01) L/h, respectively [FDA Label].

Absorpsi

Administration of 15 mg/kg plazomicin by 30-minute IV infusion resulted in peak plasma concentrations of 73.7 ± 19.7 ?g/mL in healthy adult subjects and 51.0 ± 26.7 ?g/mL in patients with complicated urinary tract infections (cUTI) FDA Label. The area under the curve (AUC) were 257 ± 67.0 ?g.h/mL in healthy adults and 226 ± 113 ?g.h/mL in cUTI patients FDA Label.

Metabolisme

Plazomicin is not reported to undergo significant metabolism FDA Label.

Rute Eliminasi

Plazomicin predominantly undergoes renal excretion, where 56% of the total administered drug was recovered in the urine within 4 hours following a single 15 mg/kg IV dose of radiolabeled plazomicin in healthy subjects. About less than 0.2% and 89.1% of the total drug were recovered within 168 hours in feces and urine, respectively FDA Label.

Interaksi Obat

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

Target Protein

rRNA methyltransferase 2, mitochondrial MRM2
30S ribosomal protein S11 rpsK
30S ribosomal protein S14 rpsN

Referensi & Sumber

Artikel (PubMed)
  • PMID: 26419762
    Karaiskos I, Souli M, Giamarellou H: Plazomicin: an investigational therapy for the treatment of urinary tract infections. Expert Opin Investig Drugs. 2015;24(11):1501-11. doi: 10.1517/13543784.2015.1095180. Epub 2015 Sep 30.
  • PMID: 29091226
    Denervaud-Tendon V, Poirel L, Connolly LE, Krause KM, Nordmann P: Plazomicin activity against polymyxin-resistant Enterobacteriaceae, including MCR-1-producing isolates. J Antimicrob Chemother. 2017 Oct 1;72(10):2787-2791. doi: 10.1093/jac/dkx239.
  • PMID: 29091224
    Zhang Y, Kashikar A, Bush K: In vitro activity of plazomicin against beta-lactamase-producing carbapenem-resistant Enterobacteriaceae (CRE). J Antimicrob Chemother. 2017 Oct 1;72(10):2792-2795. doi: 10.1093/jac/dkx261.
  • PMID: 27919895
    Lopez-Diaz MD, Culebras E, Rodriguez-Avial I, Rios E, Vinuela-Prieto JM, Picazo JJ, Rodriguez-Avial C: Plazomicin Activity against 346 Extended-Spectrum-beta-Lactamase/AmpC-Producing Escherichia coli Urinary Isolates in Relation to Aminoglycoside-Modifying Enzymes. Antimicrob Agents Chemother. 2017 Jan 24;61(2). pii: AAC.02454-16. doi: 10.1128/AAC.02454-16. Print 2017 Feb.
  • PMID: 19438282
    Dlugosz M, Trylska J: Aminoglycoside association pathways with the 30S ribosomal subunit. J Phys Chem B. 2009 May 21;113(20):7322-30. doi: 10.1021/jp8112914.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Zemdri (plazomicin)
    Injection • 500 mg/10mL • Intravenous • US • Approved
  • Zemdri (plazomicin)
    Injection • 500 mg/10mL • Intravenous • US • Approved
  • Zemdri (plazomicin)
    Injection • 500 mg/10mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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