ポリミキシンB polymyxin B。硫酸ポリミキシンB
WordNet
- the 2nd letter of the Roman alphabet (同)b
- the blood group whose red cells carry the B antigen (同)type_B, group B
- convert into a sulfate
- a salt or ester of sulphuric acid (同)sulphate
- any of several toxic antibiotics obtained from a particular soil bacterium
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Polymyxin B
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| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
Pregnancy
category |
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Routes of
administration |
Topical, Intramuscular, Intravenous, Intrathecal, or Ophthalmic |
| ATC code |
- A07AA05 (WHO) J01XB02 (WHO) S01AA18 (WHO) S02AA11 (WHO) S03AA03 (WHO) QJ51XB02 (WHO)
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| Legal status |
| Legal status |
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| Identifiers |
IUPAC name
- N-[4-amino-1-[[1-[[4-amino-1-oxo-1-[[6,9,18-tris(2-aminoethyl)-15-benzyl-3-(1-hydroxyethyl)-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methyloctanamide
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| CAS Number |
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| PubChem CID |
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| DrugBank |
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| ChEMBL |
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| NIAID ChemDB |
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| ECHA InfoCard |
100.014.340 |
| Chemical and physical data |
| Formula |
C56H100N16O17S |
| Molar mass |
1301.56 g/mol |
| NY (what is this?) (verify) |
Polymyxin B is an antibiotic primarily used for resistant Gram-negative infections. It is derived from the bacterium Bacillus polymyxa. Polymyxin B is composed of a number of related compounds (see "Mixture composition"). It has a bactericidal action against almost all Gram-negative bacilli except the Proteus and Neisseria genera. Polymyxins bind to the cell membrane and alter its structure, making it more permeable. The resulting water uptake leads to cell death. Polymyxins are cationic, basic peptides that act like detergents (surfactants). Side effects include neurotoxicity and acute renal tubular necrosis. Polymyxins are used in the topical first-aid preparation Neosporin.
- Family of polypeptides with attached fatty acid; cationic detergent at physiological pH, both hydrophilic and hydrophobic properties
- Bactericidal for gram-negative; little to no effect on gram-positive, since cell wall is too thick to permit access to membrane
Contents
- 1 Mechanism of action
- 2 Mixture composition
- 3 Research application
- 4 Endotoxin adsorption cartridge
- 5 Spectrum of susceptibility
- 6 References
- 7 See also
Mechanism of action
- Alters bacterial outer membrane permeability by binding to a negatively charged site in the lipopolysaccharide layer, which has an electrostatic attraction for the positively charged amino groups in the cyclic peptide portion (this site normally is a binding site for calcium and magnesium counter ions); the result is a destabilized outer membrane
- Fatty acid portion dissolves in hydrophobic region of cytoplasmic membrane and disrupts membrane integrity
- Leakage of cellular molecules, inhibition of cellular respiration
- Binds and inactivates endotoxin[1]
- Relative absence of selective toxicity: nonspecific for cell membranes of any type, highly toxic.
Mixture composition
Polymyxin B is composed of polymyxins B1, B1-I, B2, B3, and B6. Polymyxins B1 and B2 are considered major components. These related components are structurally identical with the exception of a variable fatty acid group on each fraction. Results from in vitro studies have shown marginal differences in MIC data when comparing the fractions.[2]
Research application
In addition to its antibiotic function, polymyxin B has been used to clear endotoxin contamination in reagents. Polymyxin B is also used to induce envelope stress in order to study the organisms response to such stress. Polymyxin envelope stress assays such as this have been used for the study of sRNA responses in Salmonella enterica.[3]
Endotoxin adsorption cartridge
An endotoxin removal cartridge (Toraymyxin) is a blood purification medical device and it uses polymyxin B as immobilized adsorbent.[4] Toray Industries developed the treatment.
Spectrum of susceptibility
Polymyxin B has been used to treat urinary tract infections and meningitis caused by Pseudomonas aeruginosa and Haemophilus influenzae, respectively. The following represents MIC susceptibility data for a few medically significant microorganisms.
- Haemophilus influenzae: ≥0.8 μg/ml
- Pseudomonas aeruginosa: 0.25 μg/ml - 1 μg/ml
[5]
References
- ^ Cardoso LS, Araujo MI, Góes AM, Pacífico LG, Oliveira RR, Oliveira SC (2007). "Polymyxin B as inhibitor of LPS contamination of Schistosoma mansoni recombinant proteins in human cytokine analysis". Microb. Cell Fact. 6: 1. doi:10.1186/1475-2859-6-1. PMC 1766364. PMID 17201926.
- ^ Orwa, J. A., et al "Isolation and Structural Characterization of Polymyxin B Components." Isolation and Structural Characterization of Polymyxin B Components 912.2 (2001): 369-73. Sciencedirect. Web. 15 Jan. 2013.
- ^ Hinton, Jay; Magali Hébrard; Carsten Kröger; Shabarinath Srikumar; Aoife Colgan; Kristian Händler (April 2012). "sRNAs and the virulence of Salmonella enterica serovar Typhimurium". RNA Biology. 9 (4): 437–445. doi:10.4161/rna.20480. PMC 3384567. PMID 22546935.
- ^ Shoji H. (February 2003). "Extracorporeal endotoxin removal for the treatment of sepsis: endotoxin adsorption cartridge (Toraymyxin).". Therapeutic Apheresis and Dialysis. 7 (1): 108–114. doi:10.1046/j.1526-0968.2003.00005.x. PMID 12921125.
- ^ http://www.toku-e.com/Assets/MIC/Polymyxin%20B%20sulfate.pdf
See also
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Antibacterials: cell envelope antibiotics (J01C-J01D)
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| Intracellular |
- Inhibit peptidoglycan subunit synthesis and transport: NAM synthesis inhibition (Fosfomycin)
- DADAL/AR inhibitors (Cycloserine)
- bactoprenol inhibitors (Bacitracin)
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| Glycopeptide |
- Inhibit PG chain elongation: Vancomycin# (Oritavancin
- Telavancin)
- Teicoplanin (Dalbavancin)
- Ramoplanin
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β-lactams/
(inhibit PBP
cross-links) |
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| Other |
- polymyxins/detergent
- depolarizing
- Hydrolyze NAM-NAG
- Tyrothricin
- Isoniazid
- Teixobactin
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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Antidiarrheals, intestinal anti-inflammatory and anti-infective agents (A07)
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| Rehydration |
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| Intestinal anti-infectives |
- Antibiotics
- Amphotericin B
- Colistin
- Fidaxomicin
- Kanamycin
- Natamycin
- Neomycin
- Nystatin
- Paromomycin
- Polymyxin B
- Rifaximin
- Streptomycin
- Vancomycin
- Sulfonamides
- Phthalylsulfathiazole
- Succinylsulfathiazole
- Sulfaguanidine
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| Intestinal adsorbents |
- Charcoal
- Bismuth
- Pectin
- Kaolin
- Crospovidone
- Attapulgite
- Diosmectite
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| Antipropulsives (opioids) |
- Opium tincture (laudanum)
- Codeine
- Morphine
- Camphorated opium tincture (paregoric)
- crosses BBB: Diphenoxylate (Diphenoxylate/atropine)
- Difenoxin
- does not cross BBB: Eluxadoline
- Loperamide
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| Intestinal anti-inflammatory agents |
- corticosteroids acting locally
- Prednisolone
- Hydrocortisone
- Prednisone
- Betamethasone
- Tixocortol
- Budesonide
- Beclometasone
- antiallergic agents, excluding corticosteroids
- aminosalicylic acid and similar agents
- Sulfasalazine
- Mesalazine
- Olsalazine
- Balsalazide
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| Antidiarrheal micro-organisms |
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| Other antidiarrheals |
- Albumin tannate
- Ceratonia
- Crofelemer
- Octreotide
- Racecadotril
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Drugs used for diseases of the ear (S02)
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| Infection |
- Acetic acid
- Aluminium acetotartrate
- Aluminium triacetate (Burow's solution)
- Boric acid
- Chloramphenicol
- Chlorhexidine
- Ciprofloxacin
- Clioquinol
- Gentamicin
- Hydrogen peroxide
- Miconazole
- Neomycin
- Nitrofurazone
- Ofloxacin
- Polymyxin B
- Rifamycin
- Tetracycline
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| Corticosteroids |
- Betamethasone
- Dexamethasone
- Fluocinolone acetonide
- Hydrocortisone
- Prednisolone
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| Analgesics and anesthetics |
- Lidocaine
- Cocaine
- Phenazone
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UpToDate Contents
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English Journal
- Effect of organic toxicants on the activity of denitrifying granular sludge.
- Zhang Z1, Zheng P, Li W, Wang R, Ghulam A.
- Environmental technology.Environ Technol.2015 Mar;36(6):699-705. doi: 10.1080/09593330.2014.959065. Epub 2014 Sep 25.
- Denitrification plays a key role in the biological nitrogen removal from the wastewater using granular sludge as the integral part of a high-rate denitrification technology. It is helpful to evaluate the effect of typical organic toxicants on the activity of denitrifying granular sludge for the appl
- PMID 25220622
- Study results on the use of different therapies for the treatment of vaginitis in hospitalised pregnant women.
- Novakov Mikić A1, Stojic S.
- Archives of gynecology and obstetrics.Arch Gynecol Obstet.2015 Feb 5. [Epub ahead of print]
- PURPOSE: During pregnancy, many women experience vaginal infections due to a weakened immune system and changes in hormonal status. Treating these infections is of crucial importance, because women are at high risk for serious complications such as preterm birth and late miscarriage. For this reason
- PMID 25651828
- Tobramycin and Nebramine as Pseudo-oligosaccharide Scaffolds for the Development of Antimicrobial Cationic Amphiphiles.
- Berkov-Zrihen Y1, Herzog IM, Benhamou RI, Feldman M, Steinbuch KB, Shaul P, Lerer S, Eldar A, Fridman M.
- Chemistry (Weinheim an der Bergstrasse, Germany).Chemistry.2015 Feb 4. doi: 10.1002/chem.201406404. [Epub ahead of print]
- Antimicrobial cationic amphiphiles derived from aminoglycoside pseudo-oligosaccharide antibiotics interfere with the structure and function of bacterial membranes and offer a promising direction for the development of novel antibiotics. Herein, we report the design and synthesis of cationic amphiphi
- PMID 25652188
Japanese Journal
- 〈Cases Reports〉Successful treatment with intravenous colistin of sepsis caused by metallo-beta-lactamase-producing multidrug-resistant Pseudomonas aeruginosa in a patient with acute myeloid leukemia
- Hanamoto Hitoshi,Sano Keigo,Fujiwara Ryousuke,Yamazaki Keiko,Yagi Hideo,Tsubaki Kazuo
- ACTA MEDICA KINKI UNIVERSITY 39(1), 69-73, 2014-06
- … MDRP in stool samples fell to undetectable levels following oral doses of polymyxin B sulfate. …
- NAID 120005468714
- 土岐 典子,佐倉 徹,石埼 卓馬 [他],高田 覚,宮脇 修一
- The KITAKANTO medical journal 55(2), 141-144, 2005-05-01
- … 敗血症について検討するため, 1997年1月より2004年9月までに当科で移植を受けた117例対象にretrospectiveに解析した.【方法】全例がclass 100のクリーンルームで移植を受け, amphotericin Bの吸入を行った.polymyxin B sulfate (PL-B), amphotericin B, acyclovir, ST合剤を内服していたのが100例, これにvancomycin hydrochlorideの内服を追加投与されていたのが17例であった.【結果】117例中18例(15.2%)に敗血症を認めた.敗血症の侵入門戸 …
- NAID 110001801381
- 抗生物質起因性下痢時の豚大腸上皮縮織の組織学的な構造
- 塚原 隆充,岩崎 由恵中山,牛田 一成 [他],USHIDA Kazunari
- The journal of veterinary medical science 65(3), s・iii, 301-306, 2003-03-25
- 抗生物質赳囚性下痢(AAD)は広範囲スペクトラムの抗菌剤を投与すると大腸内炎菌叢が深刻な影響を受け発症すると考えられている.AADの発症は,主に病原菌の増殖や大腸内の短鎖脂肪酸濃度の減少によると考えられてきた.ところが最近,我々はAAD誘導豚糞便から著量足のコハク酸および乳酸の蓄績を認めた.これらの酸は,健康な豚の糞便および大腸内官物からは殆ど検出されず,炎症性腸疾患患者の糞便中に蓄積が認められ, …
- NAID 110003947924
Related Links
- Easy to read patient leaflet for polymyxin b sulfate. Includes indications, proper use, special instructions, precautions, and possible side effects. ... How to use polymyxin b sulfate: Use polymyxin b sulfate as directed by your doctor.
- [Polymyxin B Sulfate] [1405-20-5] | 価格や在庫、物性値などの詳細情報ページです。 ... ・川口の在庫は即日，つくばの在庫は2〜3日以内の出荷となります。・詳細につきましては，お手数ですが営業部までお問い合わせください。
★リンクテーブル★
[★]
- 英
- polymyxin B, PMXB, PL-B
- 化
- 硫酸ポリミキシンB polymyxin B sulfate
- 商
- テラマイシン
- 関
- 抗菌薬。ポリミキシン
[★]
- Mg2+存在下でC3, B, Dが反応してC3bBbとなり、これがC3転換酵素(C3bBb)あるいはC5転換酵素(C3bBb3b)を形成する。これらはP(properdin)と結合して活性化し、それぞれC3、C5を活性化する
[★]
- 関
- H2SO4、inorganic sulfate、sulfate ester、sulfated、sulfation、sulfuric acid、sulfuric acid ester、sulphate、sulphuric acid
[★]
- 関
- sulfate、sulfation、sulphate
[★]
スルファ、サルファ