|
|Section2= |Section6= |Section7= }} Taurolidine ([bis(1,1-dioxoperhydro-1,2,4-thiadiazinyl-4)-methane) is an active pharmaceutical ingredient (API) with antimicrobial and anti-lipopolysaccharide properties. Derived from the amino acid taurine, its immuno modulatory action is reported to be mediated with priming and activation of macrophages and polymorphonuclear leukocytes. Taurolidine has been used to treat patients with peritonitis and as an antiendoxic agent in patients with systemic inflammatory response syndrome. It is a live-saving antimicrobial for severe abdominal sepsis and peritonitis. For severe surgical infections and use in surgical oncology Taurolidine is active against a wide range of micro- organisms that include gram positive bacteria, gram negative bacteria, fungi, mycobateria and also bacteria that are resistant to various antibiotics such as MRSA, VISA VRSA ORSA VRE. Additionally, taurolidine demonstrates some anti-tumor properties, with positive results seen in early-stage clinical investigations using the drug to treat gastrointestinal malignancies and tumors of the central nervous system. Taurolidine is the active ingredient of anti-microbial catheter lock solutions for the prevention and treatment of catheter related blood stream infections (CRBSIs)〔Liu H., Liu H., Deng J., Chen L., Yuan L., Wu Y. (2014). Preventing Catheter-Related Bacteremia with Taurolidine-Citrate Catheter Locks: A Systematic Review and Meta-Analysis. Blood Purif 37: 179-187〕〔Liu Y., Zhang A.-Q., Cao L., Xia H.-T., Ma J.-J. (2013). Taurolidine Lock Solutions for the Prevention of Catheter-Related Bloodstream Infections: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. PLOS ONE 8(11): e79417. 〕〔Mermel LA. (2001). New technologies to prevent intravascular catheter-related bloodstream infections. Emerg Infect Dis. Mar-Apr; 7(2): 197–9〕〔Bouza E.,et al. (2004) . A European perspective on intravascular catheter-related infections: report on the microbiology workload, aetiology and antimicrobial susceptibility (ESGNI-005 Study). Clin. Microbiol. Infect.10: 838–42.〕 and is suitable for use in all catheter based vascular access devices. Bacterial resistance against taurolidine has never been observed in various studies.〔Olthof E.D., Rentenaar R.J., Rijs A.J.M.M., Wanten G.J.A. (2013). Absence of microbial adaption to taurolidine in patients on home parenteral nutrition who develop catheter related bloodstream infections and use taurolidine lock. Clin Nutr 32: 538-542〕 Taurolidine acts by a non selective chemical reaction. In aqueous solution, the parent molecule taurolidine forms equilibrium with taurultam and N-hydroxymethyl taurultam, with taurinamide being a downstream derivative. The active principle of taurolidine are N-methylol derivatives of taurultam and taurinamide, which react with the bacterial cell wall, cell membrane, proteins as well as with the primary amino groups of endo- and exotoxins. Microbes are killed and the resulting toxins are inactivated; the destruction time ''in vitro'' is 30 minutes. Pro-inflammatory cytokines and enhanced TNF-α levels are reduced when used as a catheter lock solution. Taurolidine decreases the adherence of bacteria and fungi to host cells by destructing the fimbriae and flagella and thus prevent the biofilm formation. Dose of 5g over 2 hours every 4 hours for at least 48 hours were given intravenously for the treatment of various sepsis condition.〔 〕 ==Pharmacokinetic properties== Absorption is rapid, with maximum concentrations of taurultam occurring between 10 and 15 minutes, and the half-life being less than one hour. Maximum plasma taurinamide concentration occurs between 0.5 and 2 hours, and the Taurolidine is metabolised with a short half-life to taurine, carbon dioxide and water. Elimination half-life lies between 5 and 5.5 hours. Urinary estimations show excretion of taurinamide accounts for 25% of the Taurolidine dose. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「taurolidine」の詳細全文を読む スポンサード リンク
|