Peringatan Keamanan

LD50 and Nonclinical Toxicity

The oral LD50 value in rats is 5000 mg/kg.MSDS Studies evaluating the carcinogenic potential of mupirocin have not been performed. In various in vivo animal and in vitro bacterial assays, there was no evidence of genotoxicity caused by mupirocin. In reproduction studies using male and female rats, there were no signs of impaired fertility upon subcutaneous administration of mupirocin.L10580

Use in special populations

Mupirocin was found to be excreted in human milk. As there is limited data on the use of topical mupirocin in pregnant women, the use of this drug in these patients should be undertaken with caution. Based on the findings in clinical trials, topical mupirocin was shown to be safe and effective in pediatric patients aged 2 months to 16 years.L10580

Mupirocin

DB00410

small molecule approved investigational vet_approved

Deskripsi

Mupirocin, formerly termed pseudomonic acid A,A178531 is a novel antibacterial agent with a unique chemical structure and mode of action apart from other antibiotic agents. Produced by fermentation using the organism Pseudomonas fluorescens, mupirocin is a naturally-occurring antibiotic that displays a broad-specturm activity against many gram-positive bacteria and certain gram-negative bacteria in vitro.L10580 It primarily works by inhibiting bacterial protein synthesis. Due to its unique mode of action of inhibiting the activity of bacterial isoleucyl-tRNA synthetase, mupirocin does not demonstrate cross-resistance with other classes of antimicrobial agents, giving it a therapeutic advantage.L10580 It is available in topical formulations only due to extensive systemic metabolismA178531 and is used in the treatment of impetigo caused by Staphylococcus aureus and Streptococcus pyogenes and traumatic skin lesions due to secondary skin infections caused by S. aureus and S. pyogenes. There is also some clinical evidence that suggests the potential role of mupirocin in eradicating nasal carriage of Staphylococci when administered intranasally.A178531,A178591 Mupirocin is commonly marketed under the brand name Bactroban.

Struktur Molekul 2D

Berat 500.6222
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy male volunteers, the elimination half-life of mupirocin was about 20 to 40 minutes following intravenous administration. The elimination half-life of monic acid was about 30 to 80 minutes.[L6349]
Volume Distribusi No information available.
Klirens (Clearance) No information available.

Absorpsi

Systemic or percutaneous absorption of mupirocin following dermal application is expected to be minimal in adults and children.L10580 Occlusive dressings do not significantly enhance drug absorption, but damaged skin may allow enhanced penetration of the drug across the skin barrier.A178552

Metabolisme

Following intravenous or oral administration, mupirocin undergoes rapid hepatic metabolism to form the principal metabolite monic acid, which has no antibacterial activity.L10580

Rute Eliminasi

Any mupirocin reaching the systemic circulation is rapidly metabolized to form the inactive monic acid, which is eliminated by renal excretion. Following the application of Centany (mupirocin ointment),2% to a 400 cm2 area on the back of 23 healthy volunteers once daily for 7 days, the mean (range) cumulative urinary excretion of monic acid over 24 hrs following the last administration was 1.25% (0.2% to 3.0%) of the administered dose of mupirocin.L10580

Interaksi Obat

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

Target Protein

Isoleucine--tRNA ligase ileS

Referensi & Sumber

Synthesis reference: Harvey Lee Zimmerman, "Pharmaceutical and veterinary compositions of mupirocin and methods for their preparation." U.S. Patent US6025389, issued January, 1988.
Artikel (PubMed)
  • PMID: 3146455
    Parenti MA, Hatfield SM, Leyden JJ: Mupirocin: a topical antibiotic with a unique structure and mechanism of action. Clin Pharm. 1987 Oct;6(10):761-70.
  • PMID: 2502615
    Putnam CD, Reynolds MS: Mupirocin: a new topical therapy for impetigo. J Pediatr Health Care. 1989 Jul-Aug;3(4):224-7.
  • PMID: 1684188
    Lamb YJ: Overview of the role of mupirocin. J Hosp Infect. 1991 Sep;19 Suppl B:27-30.
  • PMID: 2112164
    Pappa KA: The clinical development of mupirocin. J Am Acad Dermatol. 1990 May;22(5 Pt 1):873-9.
  • PMID: 26142407
    Poovelikunnel T, Gethin G, Humphreys H: Mupirocin resistance: clinical implications and potential alternatives for the eradication of MRSA. J Antimicrob Chemother. 2015 Oct;70(10):2681-92. doi: 10.1093/jac/dkv169. Epub 2015 Jul 3.

Contoh Produk & Brand

Produk: 124 • International brands: 5
Produk
  • Bactroban
    Cream • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Cream • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Ointment • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Cream • 21.5 mg/1g • Topical • US • Approved
  • Bactroban
    Ointment • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Ointment • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Cream • 20 mg/1g • Topical • US • Approved
  • Bactroban
    Ointment • 20 mg/1g • Topical • US • Approved
Menampilkan 8 dari 124 produk.
International Brands
  • Bactroban Nasal — GlaxoSmithKline
  • Plasimine — GlaxoSmithKline
  • Spectroderm — GlaxoSmithKline
  • T-Bact — GlaxoSmithKline
  • Turixin — GlaxoSmithKline

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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