万古霉素

Vancomycin是用于治疗细菌感染的抗生素。

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

万古霉素是一种大的糖肽化合物,分子量为1450 Da [1]。万古霉素是一种独特的糖肽,在结构上与任何目前可用的抗生素无关。它还具有抑制易感细菌的细胞壁合成的第二阶段的独特作用模式。万古霉素对大量革兰氏阳性细菌有活性,例如金黄色葡萄球菌(Staphylococcus aureus),金黄色葡萄球菌(Staph)。表皮葡萄球菌无乳链球菌博维斯,Str。变形链球菌,草绿色链球菌,肠球菌[2]。

万古霉素静脉内给药,标准输注时间至少为1小时,以最大限度地减少输注相关的不良反应。具有正常肌酸酐清除率的受试者,万古霉素具有30分钟至1小时的α-分布期和6-12小时的β-消除半衰期。分布容积为0.4-1L/kg。万古霉素与蛋白质的结合范围为10％至50％。影响万古霉素总活性的因素包括其组织分布,接种量和蛋白结合效应[1]。感染小鼠的万古霉素治疗与改善临床,腹泻和组织病理学评分以及治疗期间的存活率相关[3]。

小鼠：进行一组实验，其中感染的小鼠每天用万古霉素（50mg / kg）治疗1,2,3或5天，并在感染后观察21天或每天用万古霉素（20mg / kg）观察持续5天或10天，并在感染后监测15天[3]。

[1]. Rybak MJ, et al. The pharmacokinetic and pharmacodynamic properties of vancomycin. Clin Infect Dis. 2006 Jan 1;42 Suppl 1:S35-9.

[2]. Watanakunakorn C, et al. Mode of action and in-vitro activity of vancomycin. J Antimicrob Chemother. 1984 Dec;14 Suppl D:7-18.

[3]. Warren CA, et al. Vancomycin treatment's association with delayed intestinal tissue injury, clostridial overgrowth, and recurrence of Clostridium difficile infection in mice. Antimicrob Agents Chemother. 2013 Feb;57(2):689-96.

嘌呤霉素二盐酸盐 | G-418 硫酸盐 | 衣霉素 | 潮霉素B | 盐霉素 | 阿维巴坦钠 | 硫酸新霉素 | 法硼巴坦 | 甲氧西林钠 | 利福平 | 甲硝唑 | 羧苄青霉素钠 | 头孢他啶 | 盐酸依拉环素 | 头孢噻肟钠

MOLECULAR FORMULA :

C66-H75-Cl2-N9-O24

MOLECULAR WEIGHT :

1449.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - infant

DOSE/DURATION :

119 mg/kg

TOXIC EFFECTS :

Cardiac - pulse rate increase, without fall in BP Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - cyanosis

REFERENCE :

JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 34,83,1996

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

15 mg/kg/90M-C

TOXIC EFFECTS :

Skin and Appendages - dermatitis, allergic (after systemic exposure)

REFERENCE :

NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 313,756,1985

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

170 mg/kg/19D-I

TOXIC EFFECTS :

Blood - agranulocytosis

REFERENCE :

CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 132,39,1985

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - infant

DOSE/DURATION :

295 mg/kg/3D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - interstitial nephritis

REFERENCE :

JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 30,285,1992

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Multiple routes

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

30 mg/kg/2D-I

TOXIC EFFECTS :

Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :

AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 115,410,1991

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1734 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,675,1967

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

5 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 1,315,1980

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

430 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 43,913,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

640 mg/kg/4D-I

TOXIC EFFECTS :

Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :

NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 42,200,1995 *** REVIEWS *** TOXICOLOGY REVIEW DICPBB Drug Intelligence and Clinical Pharmacy. (POB 42435, Cincinnati, OH 45242) V.3- 1969- Volume(issue)/page/year: 8,520,1974 TOXICOLOGY REVIEW AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 38,409,1965 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3663 No. of Facilities: 324 (estimated) No. of Industries: 1 No. of Occupations: 7 No. of Employees: 14913 (estimated) No. of Female Employees: 13290 (estimated)