Peringatan Keamanan

Nephrotoxicity can occur in patients as polymyxin B is thought to accumulate in renal cells after renal tubular reabsorptionA176390. This accumulation can lead to apoptosis of renal cells and decrease in renal functionA176399. In recent studies, acute kidney injury (AKI) has been seen in 31.3% to 39.4% of patients receiving polymyxin BA176399.

Overdose cases can cause neuromuscular block leading to apnea, muscular weakness, vertigo, transient facial parasthesia, slurred speed, vasomotor instability, visual disturbance, confusion, psychosis, and respiratory arrestF4151. Renal failure has also been seen through decreased urine output, and increased serum concentrations of blood urea nitrogenF4151.

Overdose of polymyxin B is treated by stopping the drug and beginning symptomatic treatmentF4151. Intravenous administration of mannitol may enhance renal clearance, and hemodialysis may manage renal complicationsF4151.

Safety of polymyxin B has not been established in pregnancy, breast feeding, pediatrics, and geriatricsF4151. Polymyxin B should no be used in pregnancy unless the benefit outweighs the riskF4151. Nursing mothers should either stop nursing or stop polymyxin B treatment depending on the risks to both the mother and childF4151. Pediatric patients should be frequently monitored for renal function and no dosing information is available in children under 2 years of ageF4151. Geriatric patients should have renal function assessed before and regularly during therapyF4151.

Polymyxin B

DB00781

biotech approved vet_approved

Deskripsi

Polymyxin B was discovered in the 1940sA176429. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranesA176426. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxicA176426,FDA Label. All gram-positive bacteria, fungi, and the gram-negative cocci, are resistantA176426. It is appropriate for treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosaFDA Label. Polymyxin B has a narrow therapeutic index and so its use is limited and unlikely to be used first lineA176429.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In one study the half life was 9 to 11.5 hours[A176390]. However, a Canadian monograph states the half life to be 6 hours, and 48-72 hours in patients with renal insufficiency[F4151].
Volume Distribusi 1 compartment models estimate the volume of distribution to be 34.3L to 47.2L[A176390]. However, the general consensus is that the volume of distribution is yet to be determined[F4151].
Klirens (Clearance) 1 compartment models estimate clearance to be 2.37L/h to 2.5L/h[A176390].

Absorpsi

Administration by the oral route does not lead to absorptionA176426.

Metabolisme

There is little data available for the metabolism of polymyxin BA176432. In one study, <1% of polymyxin B was eliminated through the kidneys and it had not been metabolisedA176432. Polymyxin B has also been found in bile, not having undergone metabolic processesA176390.

Rute Eliminasi

Polymyxin B is proposed to be primarily eliminated through renal tubular reabsorption and non-renal pathwaysA176390,F4151. Urine collection in humans and animals show <5% of polymyxin B eliminated from the kidneysA176390. However, a Canadian product monograph states the drug is primarily eliminated through the kidneys and that 60% of polymyxin B is recovered in the urineF4151. This discrepancy can be explained by the 12 to 24 hour lag time between administration and significant elimination of polymyxin BF4151. Non-renal elimination is not well understood but all 4 components of polymyxin B have been detected in bileA176390.

Interaksi Obat

393 Data
Colistimethate Polymyxin B may increase the nephrotoxic and neuromuscular blocking activities of Colistimethate.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Polymyxin B.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Polymyxin B.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Polymyxin B.
Dicoumarol The risk or severity of bleeding can be increased when Polymyxin B is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Polymyxin B is combined with Phenindione.
Warfarin The risk or severity of bleeding can be increased when Polymyxin B is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Polymyxin B is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Polymyxin B is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Polymyxin B is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Polymyxin B is combined with Coumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Polymyxin B is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Polymyxin B is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Polymyxin B is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Polymyxin B is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Polymyxin B is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Polymyxin B is combined with Tioclomarol.
(S)-Warfarin The risk or severity of bleeding can be increased when Polymyxin B is combined with (S)-Warfarin.
Succinylcholine Succinylcholine may increase the neurotoxic activities of Polymyxin B.
Reserpine Reserpine may increase the neurotoxic activities of Polymyxin B.
Ziprasidone Ziprasidone may increase the neurotoxic activities of Polymyxin B.
Cycloserine Cycloserine may increase the neurotoxic activities of Polymyxin B.
Amitriptyline Amitriptyline may increase the neurotoxic activities of Polymyxin B.
Protriptyline Protriptyline may increase the neurotoxic activities of Polymyxin B.
Vinorelbine Vinorelbine may increase the neurotoxic activities of Polymyxin B.
Clozapine Clozapine may increase the neurotoxic activities of Polymyxin B.
Thiethylperazine Thiethylperazine may increase the neurotoxic activities of Polymyxin B.
Sulpiride Sulpiride may increase the neurotoxic activities of Polymyxin B.
Loxapine Loxapine may increase the neurotoxic activities of Polymyxin B.
Remoxipride Remoxipride may increase the neurotoxic activities of Polymyxin B.
Promazine Promazine may increase the neurotoxic activities of Polymyxin B.
Prochlorperazine Prochlorperazine may increase the neurotoxic activities of Polymyxin B.
Teniposide Teniposide may increase the neurotoxic activities of Polymyxin B.
Droperidol Droperidol may increase the neurotoxic activities of Polymyxin B.
Imipramine Imipramine may increase the neurotoxic activities of Polymyxin B.
Chlorpromazine Chlorpromazine may increase the neurotoxic activities of Polymyxin B.
Haloperidol Haloperidol may increase the neurotoxic activities of Polymyxin B.
Triflupromazine Triflupromazine may increase the neurotoxic activities of Polymyxin B.
Cyclophosphamide Cyclophosphamide may increase the neurotoxic activities of Polymyxin B.
Nortriptyline Nortriptyline may increase the neurotoxic activities of Polymyxin B.
Vincristine Vincristine may increase the neurotoxic activities of Polymyxin B.
Amoxapine Amoxapine may increase the neurotoxic activities of Polymyxin B.
Fluphenazine Fluphenazine may increase the neurotoxic activities of Polymyxin B.
Stavudine Stavudine may increase the neurotoxic activities of Polymyxin B.
Thioridazine Thioridazine may increase the neurotoxic activities of Polymyxin B.
Moricizine Moricizine may increase the neurotoxic activities of Polymyxin B.
Trimipramine Trimipramine may increase the neurotoxic activities of Polymyxin B.
Risperidone Risperidone may increase the neurotoxic activities of Polymyxin B.
Trifluoperazine Trifluoperazine may increase the neurotoxic activities of Polymyxin B.
Perphenazine Perphenazine may increase the neurotoxic activities of Polymyxin B.
Flupentixol Flupentixol may increase the neurotoxic activities of Polymyxin B.
Ethanol Ethanol may increase the neurotoxic activities of Polymyxin B.
Didanosine Didanosine may increase the neurotoxic activities of Polymyxin B.
Cyclobenzaprine Cyclobenzaprine may increase the neurotoxic activities of Polymyxin B.
Mesoridazine Mesoridazine may increase the neurotoxic activities of Polymyxin B.
Acetophenazine Acetophenazine may increase the neurotoxic activities of Polymyxin B.
Promethazine Promethazine may increase the neurotoxic activities of Polymyxin B.
Pimozide Pimozide may increase the neurotoxic activities of Polymyxin B.
Doxepin Doxepin may increase the neurotoxic activities of Polymyxin B.
Desipramine Desipramine may increase the neurotoxic activities of Polymyxin B.
Clindamycin Clindamycin may increase the neurotoxic activities of Polymyxin B.
Tubocurarine Tubocurarine may increase the neurotoxic activities of Polymyxin B.
Paclitaxel Paclitaxel may increase the neurotoxic activities of Polymyxin B.
Aripiprazole Aripiprazole may increase the neurotoxic activities of Polymyxin B.
Chlorprothixene Chlorprothixene may increase the neurotoxic activities of Polymyxin B.
Clomipramine Clomipramine may increase the neurotoxic activities of Polymyxin B.
Decamethonium Decamethonium may increase the neurotoxic activities of Polymyxin B.
Alimemazine Alimemazine may increase the neurotoxic activities of Polymyxin B.
Paliperidone Paliperidone may increase the neurotoxic activities of Polymyxin B.
Methotrimeprazine Methotrimeprazine may increase the neurotoxic activities of Polymyxin B.
Imipenem Imipenem may increase the neurotoxic activities of Polymyxin B.
Periciazine Periciazine may increase the neurotoxic activities of Polymyxin B.
Acepromazine Acepromazine may increase the neurotoxic activities of Polymyxin B.
Aceprometazine Aceprometazine may increase the neurotoxic activities of Polymyxin B.
Molindone Molindone may increase the neurotoxic activities of Polymyxin B.
Pipotiazine Pipotiazine may increase the neurotoxic activities of Polymyxin B.
Thioproperazine Thioproperazine may increase the neurotoxic activities of Polymyxin B.
Thiothixene Thiothixene may increase the neurotoxic activities of Polymyxin B.
Zuclopenthixol Zuclopenthixol may increase the neurotoxic activities of Polymyxin B.
Lincomycin Lincomycin may increase the neurotoxic activities of Polymyxin B.
Amineptine Amineptine may increase the neurotoxic activities of Polymyxin B.
Fluspirilene Fluspirilene may increase the neurotoxic activities of Polymyxin B.
Osanetant Osanetant may increase the neurotoxic activities of Polymyxin B.
Bifeprunox Bifeprunox may increase the neurotoxic activities of Polymyxin B.
Iloperidone Iloperidone may increase the neurotoxic activities of Polymyxin B.
Pimavanserin Pimavanserin may increase the neurotoxic activities of Polymyxin B.
BL-1020 BL-1020 may increase the neurotoxic activities of Polymyxin B.
Cariprazine Cariprazine may increase the neurotoxic activities of Polymyxin B.
Sertindole Sertindole may increase the neurotoxic activities of Polymyxin B.
Asenapine Asenapine may increase the neurotoxic activities of Polymyxin B.
Amisulpride Amisulpride may increase the neurotoxic activities of Polymyxin B.
Lurasidone Lurasidone may increase the neurotoxic activities of Polymyxin B.
Perospirone Perospirone may increase the neurotoxic activities of Polymyxin B.
Amperozide Amperozide may increase the neurotoxic activities of Polymyxin B.
Dimetacrine Dimetacrine may increase the neurotoxic activities of Polymyxin B.
Cyamemazine Cyamemazine may increase the neurotoxic activities of Polymyxin B.
Butriptyline Butriptyline may increase the neurotoxic activities of Polymyxin B.
Brexpiprazole Brexpiprazole may increase the neurotoxic activities of Polymyxin B.
Sodium citrate Sodium citrate may increase the neurotoxic activities of Polymyxin B.
Dosulepin Dosulepin may increase the neurotoxic activities of Polymyxin B.

Target Protein

Bacterial outer membrane
Dihydropteroate synthase folP

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30909507
    Avedissian SN, Liu J, Rhodes NJ, Lee A, Pais GM, Hauser AR, Scheetz MH: A Review of the Clinical Pharmacokinetics of Polymyxin B. Antibiotics (Basel). 2019 Mar 22;8(1). pii: antibiotics8010031. doi: 10.3390/antibiotics8010031.
  • PMID: 30875778
    Nation RL, Rigatto MHP, Falci DR, Zavascki AP: Polymyxin Acute Kidney Injury: Dosing and Other Strategies to Reduce Toxicity. Antibiotics (Basel). 2019 Mar 14;8(1). pii: antibiotics8010024. doi: 10.3390/antibiotics8010024.
  • PMID: 26324262
    Abodakpi H, Gohlke J, Chang KT, Chow DS, Tam VH: Analytical and functional determination of polymyxin B protein binding in serum. Antimicrob Agents Chemother. 2015 Nov;59(11):7121-3. doi: 10.1128/AAC.01815-15. Epub 2015 Aug 31.
  • PMID: 28275006
    Poirel L, Jayol A, Nordmann P: Polymyxins: Antibacterial Activity, Susceptibility Testing, and Resistance Mechanisms Encoded by Plasmids or Chromosomes. Clin Microbiol Rev. 2017 Apr;30(2):557-596. doi: 10.1128/CMR.00064-16.
  • PMID: 23701329
    Velkov T, Roberts KD, Nation RL, Thompson PE, Li J: Pharmacology of polymyxins: new insights into an 'old' class of antibiotics. Future Microbiol. 2013 Jun;8(6):711-24. doi: 10.2217/fmb.13.39.
  • PMID: 18840079
    Zavascki AP, Goldani LZ, Cao G, Superti SV, Lutz L, Barth AL, Ramos F, Boniatti MM, Nation RL, Li J: Pharmacokinetics of intravenous polymyxin B in critically ill patients. Clin Infect Dis. 2008 Nov 15;47(10):1298-304. doi: 10.1086/592577.

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Menampilkan 8 dari 1172 produk.
International Brands
  • Aerosporin — GlaxoSmithKline
  • Metamyxin — Pola Pharma
  • Polomyxin B — Fuji Yakuhin
  • Poly-Rx — X-Gen
  • Polyfax — Intra
  • Polyxx — Celon

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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