Antimicrobial chemotherapeutic agents

Katzung PHARMACOLOGY, 9e > Section VIII. Chemotherapeutic Drugs > Chapter 50. Miscellaneous Antimicrobial Agents Disinfectants, Antiseptics, Sterilants > ... 

The sulfonamides are a group of organic compounds with chemotherapeutic activity they are antimicrobial agents and not antibiotics. They have a common chemical nucleus that is closely related to PABA, an essential component in the folic acid pathway of nucleic acid synthesis. The sulfonamides are synergistic with the diaminopyrim-idines, which inhibit an essential step further along the folate pathway. The combination of a sulfonamide and a diaminopyrimidine is advantageous because it is relatively non-toxic to mammalian cells (less sulfonamide is administered) and is less likely to select for resistant bacteria. Only these so-called potentiated sulfonamides are used in equine medicine. These drugs are formulated in a ratio of one part diaminopyrimidine to five parts sulfonamide, but the optimal antimicrobial ratio at the tissue level is 1 20, which is achieved because the diaminopyrimidines are excreted more rapidly than the sulfonamides. 

Protein synthesis and metabolism - Inhibitors of protein synthesis are effective antitumor, antiviral, and antimicrobial agents. Their specific site of action determines whether the desirable chemotherapeutic activities will predcminate over the untoward effects of these drugs. The effectiveness of chloramphenicol lies in its inhibitory effect on one of the few enzymatic reactions in protein synthesis that is specific to bacteria and its concomitant failure to affect protein synthesis in animal cells. 

Antimicrobial Agent A chemotherapeutic agent used to treat diseases caused by microbes. 

A.ntibiotic is an organic chemical substance produced by microorganisms that has the capacity in low concentration to selectively destroy or inhibit the growth of other microorganisms without injuring the host cells. It may be adrninistered systemicaHy and be an antimicrobial chemotherapeutic agent. 

Sulfur dioxide, sulfites, and metabisulfites have had extensive use as antimicrobial preservatives in the food industry. In pharmaceuticals they have had a dual role, acting as preservatives and antioxidants. The sulfa dmgs, or sulfonamides, the first effective chemotherapeutic agents to be employed... 

Power E.G.M. Russell A.D. (1998) Design of antimicrobial chemotherapeutic agents. In Introduction to Principles of Drug Design (ed. H.J. Smith), 3rd edn, Bristol Wright. 

Diazoimidazole-5-carboxylic acid esters have inhibitory activity in several different types of microorganisms. They can be used as sanitizing compounds (72USP3654257). In particular, methyl 4-diazoimidazole-5-carboxylate showed antimicrobial activity towards strains of microorganisms resistant to the action of certain known chemotherapeutic agents. 

Specific antimicrobial drugs are discussed in chapter Chemotherapeutic agents. ... 

H. J. Smith, "Design of Antimicrobial Chemotherapeutic Agents," in Smith and William s Introduction to the Principles of Drug Design, 2nd ed., Wright, London, 1988, pp. 285-288. 

Unfortunately, standardization of the methodology to be employed in these efficacy tests has proved difficult, if not impossible, to obtain, as has consensus on what level of killing represents a satisfactory and/or acceptable result. It must be stressed however, that unlike tests involving chemotherapeutic agents where the major aim is to establish antimicrobial concentrations that inhibit growth (i.e. MICs), disinfectant tests require determinations of appropriate cidal levels. 

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