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Clinical Pharmacology of the Anti-Tuberculosis Drugs
Published in Lloyd N. Friedman, Martin Dedicoat, Peter D. O. Davies, Clinical Tuberculosis, 2020
Gerry Davies, Charles Peloquin
IMP is dosed at 1,000 mg 12 hourly and MRP 1,000 mg 8 hourly intravenously. 125 mg clavulanic acid should be given orally with each dose. Because clavulanate is not currently separately formulated, this is usually given as co-amoxiclav 250/125 mg.
Surgical infection
Published in Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie, Bailey & Love's Short Practice of Surgery, 2018
Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie
Ampicillin and amoxicillin are b-lactam penicillins and can be taken orally or may be given parenterally. Both are effective against Enterobacteriaceae, Enterococcus faecalis and the majority of group D streptococci, but not species of Klebsiella or Pseudomonas. Clavulanic acid has no antibacterial activity itself, but it does inactivate P-lactamases, so can be used in conjunction with amoxicillin. The combination is known as co-amoxiclav and is useful against P-lactamase producing bacteria that are resistant to amoxicillin on its own. These include resistant strains of Staphylococcus aureus, E. coli, Haemophilus influenzae, Bacteroides and Klebsiella.
Beta-Lactamase Inhibitors
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Pascalis Vergidis, Matthew E. Falagas
Beta-lactamase inhibitors are used in combination with beta-lactam antibiotics to prevent their destruction by various beta-lactamases. Clavulanic acid is a potent inhibitor of many beta-lactamases (Reading et al., 1983). The drug binds initially beta-lactamases and functions as a competitive inhibitor; this is followed by acylation of these enzymes through the beta-lactam carbonyl part of the clavulanic acid molecule. This mechanism is similar to the reaction between a beta-lactamase and a labile beta-lactam antibiotic, such as penicillin G. In the latter case, the acyl enzyme undergoes rapid hydrolysis to release active enzyme, again together with penicillin-degradation products. By contrast, the acyl enzyme formed by reaction with clavulanic acid is hydrolyzed only very slowly, and therefore the enzyme is transiently inhibited. Beta-lactamases differ in their susceptibility to inhibition by clavulanic acid. Those that are readily inhibited include staphylococcal and E. faecalis beta-lactamases and the plasmid-mediated enzymes (e.g. TEM-1), which are widespread among the Enterobacteriaceae, P. aeruginosa, H. influenzae, N. gonorrhoeae, and M. catarrhalis. Clavulanic acid is a more potent inhibitor compared to sulbactam for both conventional- and extended-spectrum beta-lactamases (Payne et al., 1994). Overall, clavulanic acid and tazobactam had similar potency against both sets of enzymes.
A review on the mechanistic details of OXA enzymes of ESKAPE pathogens
Published in Pathogens and Global Health, 2023
Fatma Gizem Avci, Ilgaz Tastekil, Amit Jaisi, Pemra Ozbek Sarica, Berna Sariyar Akbulut
The alarming increase in the transmission of multidrug-resistant (MDR) pathogenic bacteria, especially those expressing extended-spectrum β-lactamases, makes it very difficult to cope with such bacteria using existing drugs and approaches. Furthermore, the most widely used β-lactamase inhibitors of combinatorial treatments in the clinic are commonly ineffective against class B, C, and D enzymes. Prudent support for the development of new antibiotics and alternative solutions are required to avoid antibacterial agents exhibiting cross-resistance [92]. In this context, the focus is turned to nature, which serves as a rich source for untapped novel bioactive compounds. Indeed, clavulanic acid, the first β-lactamase inhibitor introduced into clinical medicine, is a natural product [3]. These compounds can be administered alone or in combinatorial therapies to fight against increased incidences of antibiotic resistance. Thus, natural products obtained from different sources, which are not limited to microbial and plant cells, play key roles in the discovery of new molecules with distinct antimicrobial mechanisms and multi-target properties [93].
Amoxicillin-associated Stevens-Johnson syndrome or toxic epidermal necrolysis: systematic review
Published in Journal of Chemotherapy, 2023
Ana V. Pejcic, Milos N. Milosavljevic, Marko Folic, Diana Fernandes, João Bentes, Miralem Djesevic, Slobodan Jankovic
Amoxicillin is one of the most commonly used antibiotics in primary care setting [7]. It is a semisynthetic amino-penicillin with bactericidal activity toward a wide variety of gram-positive bacteria and some gram-negative organisms [7]. Amoxicillin is used for the treatment of tonsillitis, pharyngitis, otitis media, lower respiratory tract infections, skin and skin structure infections, urinary tract infections and for the eradication of Helicobacter pylori [8]. It can be administered alone or in combination with clavulanic acid, a beta-lactamase inhibitor that provides the efficacy of amoxicillin against resistant strains of bacteria [7]. Both amoxicillin and amoxicillin/clavulanate are generally well-tolerated [7,9]. Their use may occasionally be accompanied by mild gastrointestinal side effects, such as diarrhea, nausea, vomiting, while serious side effects such as hepatotoxicity and hypersensitivity reactions are rare [7,9]. SJS/TEN is one of very rare adverse drug reactions associated with the use of amoxicillin [10].
Appropriateness of empirical antibiotic therapy and added value of adjunctive gentamicin in patients with septic shock: a prospective cohort study in the ICU
Published in Infectious Diseases, 2021
Rob G. H. Driessen, Rald V. M. Groven, Johan van Koll, Guy J. Oudhuis, Dirk Posthouwer, Iwan C. C. van der Horst, Dennis C. J. J. Bergmans, Ronny M. Schnabel
Patients receiving gentamicin were more often treated with amoxicillin/clavulanic acid than patients receiving monotherapy in this study (44 vs 24%, p = .002). We believe this can be explained by the fact that in the gentamicin group, more patients are admitted directly from the emergency department (40 vs 21%). Amoxicillin/clavulanic acid is the first choice antibiotic therapy for patients admitted from out-of-hospital according to the antibiotic treatment protocol in our centre. Although more patients in the monotherapy group received meropenem, this difference was not statistically different between both groups (10 vs 5%, p = .175). The fact that less patients in the combination group received broad spectrum antibiotics, could also be explained as an advantage of gentamicin combination therapies.