Methicillin (sodium salt)

Methicillin is a narrow-spectrum beta-lactam antibiotic that acts by inhibiting penicillin-binding proteins (PBP). Methicillin has a good effect on penicillinase producing S. aureus. Methicillin is not absorbed orally and must be administered by injection. It can be used to treat septicemia, endocarditis, pneumonia, meningitis, brain abscess, pericarditis, urinary tract infection, skin soft tissue infection, osteomyelitis, pseudomembranous enteritis. Methicillin can also be used to screen for resistant strains ^[1-3].

Methicillin (20 μg/mL; 24 h) results in a rapid decrease in CFU of S. aureus^[4]. Methicillin (0-100 μg/mL; 24 h) has a high killing effect on CI-G S. aureus. Strain ^[5].

Methicillin (intramuscular administration; 40 mg/kg every 6 h; 5 days) reduced mortality in in S. aureus.-infected rabbits^[4]. Methicillin (9 μg/ml; 4days; 0.5 ml/day) and a bismuth metal-organic framework (Bi-MOF) can synergistically enhance the therapeutic effect and inhibit the recurrence of infection in the tolerant S. aureus-induced murine subcutaneous infection model ^[6].

References:

[1]. Katsipis G, Pantazaki AA. Serrapeptase impairs biofilm, wall, and phospho-homeostasis of resistant and susceptible Staphylococcus aureus. Appl Microbiol Biotechnol. 2023 Feb;107(4):1373-1389. doi: 10.1007/s00253-022-12356-5. Epub 2023 Jan 13. PMID: 36635396; PMCID: PMC9898353.

[2]. Khoshnood S, Heidary M,et,al. A review on mechanism of action, resistance, synergism, and clinical implications of mupirocin against Staphylococcus aureus. Biomed Pharmacother. 2019 Jan;109:1809-1818. doi: 10.1016/j.biopha.2018.10.131. Epub 2018 Nov 26. PMID: 30551435.

[3]. Xie X, Tong X, et,al. Use of mouse primary epidermal organoids for USA300 infection modeling and drug screening. Cell Death Dis. 2023 Jan 11;14(1):15. doi: 10.1038/s41419-022-05525-x. PMID: 36631452; PMCID: PMC9833019.

[4]. Carrizosa J, Santoro J, et,al. Treatment of experimental Staphylococcus aureus endocarditis: comparison of cephalothin, cefazolin, and methicillin. Antimicrob Agents Chemother. 1978 Jan;13(1):74-7. doi: 10.1128/AAC.13.1.74. PMID: 626493; PMCID: PMC352187.

[5]. Banerjee S, Sionov RV et,al. Anandamide alters the membrane properties, halts the cell division and prevents drug efflux in multidrug resistant Staphylococcus aureus. Sci Rep. 2021 Apr 22;11(1):8690. doi: 10.1038/s41598-021-88099-6. PMID: 33888802; PMCID: PMC8062478.

[6]. Yuan, Kai et al. “Multi-roles of nanoscale bismuth metal-organic frameworks: Infectious photoacoustic probe and inhibitor of antibiotics tolerant bacteria via targeting endogenous H2S.” Nano Today (2022): n. pag. 

甲氧西林Methicillin是一种窄谱β -内酰胺类抗生素，通过抑制青霉素结合蛋白(PBP)起作用。甲氧西林对产青霉素酶的金黄色葡萄球菌有良好的抑制作用。甲氧西林不能口服吸收，必须注射给药。可用于治疗败血症、心内膜炎、肺炎、脑膜炎、脑脓肿、心包炎、尿路感染、皮肤软组织感染、骨髓炎、假膜性肠炎等。甲氧西林也可用于筛选甲氧西林耐药菌株^[1-3]。

甲氧西林(20 μg/mL; 24 h)可迅速降低金黄色葡萄球菌的CFU^[4]。甲氧西林(0-100 μg/mL; 24 h)对CI-G金黄色葡萄球菌有较高的杀伤效果^[5]。

甲氧西林(intramuscular administration; 40 mg/kg every 6 h; 5 days)降低了感染金黄色葡萄球菌的兔子的死亡率^[4]。甲氧西林(9 μg/ml; 4days; 0.5 ml/day)和Bi-MOF在耐药金黄色葡萄球菌诱导的小鼠皮下感染模型中可协同增强治疗效果并抑制感染复发^[6]。