Mafenide hydrochloride
(Synonyms: 盐酸磺胺米隆) 目录号 : GC36529A sulfonamide antibiotic
Cas No.:138-37-4
Sample solution is provided at 25 µL, 10mM.
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Mafenide is a sulfonamide antibiotic that inhibits growth of bacteria.1,2 It inhibits growth of clinical isolates of S. pyogenes, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), Enterococcus, Enterobacteriaceae, and Gram-negative bacilli from burn patients in an agar well diffusion assay (mean zone of inhibition = 24-37 mm) but not in a broth dilution assay with MIC values ranging from 250 to greater than 5,000 μg/ml.1 Mafenide also inhibits growth of clinical isolates of K. pneumoniae that produce extended spectrum β-lactamase (ESBL), P. aeruginosa, and A. baumannii-calcoaceticus from burn patients in an agar well diffusion assay (mean zones of inhibition = 23.5, 28.9, and 25.8 mm, respectively) but not in a broth dilution assay (mean MICs = 1,024 μg/ml, 1,024 μg/ml, and 1,024 μg/ml, respectively).2 It decreases mortality in a rat model of burn wounds seeded with rat virulent P. aeruginosa.3 Mafenide also inhibits human carbonic anhydrase (CA) I and II (Kis = 41.91 and 0.612 μM, respectively).4 Formulations containing mafenide have been used in the treatment of severe burns.
1.Rodgers, G.L., Mortensen, J.E., Fisher, M.C., et al.In vitro susceptibility testing of topical antimicrobial agents used in pediatric burn patients: Comparison of two methodsJ. Burn Care Rehabil.18(5)406-410(1997) 2.Glasser, J.S., Guymon, C.H., Mende, K., et al.Activity of topical antimicrobial agents against multidrug-resistant bacteria recovered from burn patientsBurns36(8)1172-1184(2010) 3.Fox, C.L., Jr., Sampath, A.C., and Stanford, J.W.Virulence of Pseudomonas infection in burned rats and mice. Comparative efficacy of silver sulfadiazine and mafenideArch. Surg.101(4)508-512(1970) 4.Fidan, ?., Salmas, R.E., Arslan, M., et al.Carbonic anhydrase inhibitors: Design, synthesis, kinetic, docking and molecular dynamics analysis of novel glycine and phenylalanine sulfonamide derivativesBioorg. Med. Chem.23(23)7353-7358(2015)
Cas No. | 138-37-4 | SDF | |
别名 | 盐酸磺胺米隆 | ||
Canonical SMILES | O=S(C1=CC=C(CN)C=C1)(N)=O.[H]Cl | ||
分子式 | C7H11ClN2O2S | 分子量 | 222.69 |
溶解度 | DMSO:44 mg/mL (197.58 mM) ; Water:44 mg/mL (197.58 mM); Ethanol:8 mg/mL (35.92 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.4905 mL | 22.4527 mL | 44.9055 mL |
5 mM | 0.8981 mL | 4.4905 mL | 8.9811 mL |
10 mM | 0.4491 mL | 2.2453 mL | 4.4905 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Topical Mafenide hydrochloride aqueous spray in initial management of massive contaminated wounds with devitalized tissue
Prehosp Disaster Med 2001 Jul-Sep;16(3):172-4.PMID:11875802DOI:10.1017/s1049023x00025930.
Since at least WWII, some open, contaminated wounds involving massive soft tissue injury and vascular damage have resulted in "irreversible shock," despite prompt rescue, hemorrhage control, and blood and fluid replacement, without signs of clinical infection. In animal studies, survival time was related statistically to the dosage of Clostridium perfringens in multicontaminated explosive wounds. Survival time was lengthened by the application of some topical antibacterial agents, but actual recovery was achieved only with topical Mafenide hydrochloride solution aqueous spray, which resulted in negative clostridium. perfringens cultures. Although not related statistically to survival time, the Mafenide hydrochloride spray also controlled the Pseudomonas aeruginosa in these wounds. Mafenide hydrochloride had the American trade name of Sulfamylon from about 1942 until 1998, when another pharmaceutical company patented Sulfamylon as the trade name for mafenide acetate, a weaker antibacterial agent. However, Mafenide hydrochloride still is available from chemical companies. Mafenide hydrochloride solution spray has been used successfully in treatment of patients with severe by contaminated wounds and deep burns, and its use in initial care should be revisited.
Wet disc testing of Mafenide hydrochloride, chlorhexidine gluconate, and triple antibiotic solution against bacteria isolated from burn wounds
J Burn Care Rehabil 1990 Jul-Aug;11(4):301-4.PMID:2401684DOI:10.1097/00004630-199007000-00005.
Various antimicrobial solutions for topical use on burn wounds tested, in vitro with a newly described wet disc assay, for their activity against bacterial isolates from patients with burns. The antimicrobial activity of triple antibiotic solution was shown to reside in the neomycin component. The activity of 2.5% Mafenide hydrochloride solution was equal to that of 4% mafenide HCl and could be used clinically with significant savings and perhaps, fewer side effects. Chlorhexidine gluconate had broad antimicrobial activity in an 0.05% solution in water; however, dissolving the active ingredient in saline nullified its activity significantly. The wet disc assay appears to be a useful means by which to assess the efficacy of solutions for topical use.
Preventing postoperative burn wound aspergillosis
J Burn Care Rehabil 1991 Mar-Apr;12(2):132-5.PMID:2050719DOI:10.1097/00004630-199103000-00008.
Between January 1, 1984, and December 31, 1988, 35 patients at the Los Angeles County + University of Southern California Burn Center had postoperative cultures from their burn wounds that grew Aspergillus species; clinical burn-wound aspergillosis occurred in 66% of these cases and death occurred in 53% of these cases. Beginning in November 1984, several modifications in the air-conditioning system and topical antimicrobial wound therapy were undertaken. Cleaning and 8Cu-quinolinolate treatment of air ducts every 2 months did not reliably clear Aspergillus species from the air in patient care areas. Several changes in topical therapeutic regimen failed to prevent both burn wound culture positivity and clinical aspergillosis. Finally, installation of high-efficiency particulate air filters, installation of new air ducts, and inception of wound irrigation with a solution of Mafenide hydrochloride plus nystatin both during and after operation were associated with a reduction in wound culture positivity rate to one occurrence in 1988 (Poisson probability less than 0.01 versus the rate in 1984) and no occurrences during the 18 months after the false ceiling of the burn ward was sealed.
Comparison of battlefield-expedient topical antimicrobial agents for the prevention of burn wound sepsis in a rat model
J Burn Care Rehabil 2005 Jul-Aug;26(4):357-61.PMID:16006845DOI:10.1097/01.bcr.0000170276.33207.b4.
Topical antimicrobial therapy has the potential to limit the mortality and morbidity of contaminated battlefield injuries. Many agents available are ill-suited for use on the battlefield; however, mafenide acetate solution (MAS) has known efficacy as a burn dressing adjunct, and previous work with mafenide as a direct chemotherapeutic has shown promise. A total of 71 male Sprague-Dawley rats underwent a 20% TBSA full-thickness scald. Wounds were inoculated with a solution containing 1 x 10 colony-forming units per milliliter of Pseudomonas aeruginosa 1244 (ATCC 27317). Treatments with 10% mafenide acetate cream (MAC), 5% MAS, 5% Mafenide hydrochloride solution (MHS), and 4% chlorhexidine gluconate solution (CHG) were established. Agents were applied directly to the wound daily for 10 days. Animals were monitored for 21 days and euthanized if they manifested a moribund state as a result of sepsis. Survival to study completion in the negative control group (no treatment) was 25% (3/12). Survival in the positive control group (MAC) was 100%. None of the test agent groups demonstrated significant survival over the untreated controls; MAS resulted in 5/12 (42%) survival (P = .67), CHG in 4/12 (33%) survival (P = 1.0), and MHS resulted in 2/12 (17%) survival (P = 1.0). There were no significant differences in group weights on day 1. By day 6, all test agent groups were significantly underweight compared with the MAC group. This trend resolved as underweight animals died. We did not demonstrate significant prevention of wound sepsis with these agents as we used them. These techniques should not be substituted for established burn care. Aqueous direct topical antimicrobial agents have logistical advantages over creams and dressing soaks for field use, and the search for a battlefield-expedient agent for use at or near the point of wounding should continue.