Potential Risks in Modern Antibiotic Therapy

Abstract

Knowledge of the safety profile of antibacterial drugs is important for rational pharmacotherapy with antibiotics. The purpose of this information is to help the doctor, pharmacist and patient to (quickly) "navigate" in the safety of antibiotics to implement one of the basic principles of pharmacotherapy "Do no harm!". The aim of the study. Analysis of possible potential risks in modern antibiotic therapy. Materials and methods. Analysis of data from the scientific literature on the side effects of antibiotics. Results. Most antibiotics have a wide spectrum of antimicrobial action, much less of them have a narrow spectrum of activity, but all of them have side effects (SE). In particular, the neurotoxicity of penicillins and fluoroquinolones is a consequence of their antagonism with GABA. The latter mechanism is also responsible for the neurotoxicity of carbapenens, monobactams and cephalosporins. Cardiotoxicity and hematotoxicity of benzylpenicillins are the result of inhibition of tissue respiration and the process of converting fibrinogen to fibrin, which causes bleeding. The hematotoxicity of carbopenicillins, monobactams and cephalosporins is associated with the inhibition of the conversion of vicasol (vit. K) into its active form, as well as the obstruction of its synthesis due to the suppression of normal intestinal microflora (the main producer of endogenous vit. K). The nephrotoxicity of aminoglycosides and vancomycin is associated with the accumulation of these drugs in the cells of the proximal renal tubules and impaired enzyme activity (Na+-, K+-, ATP; respiratory, etc.), which leads to interstitial nephritis. Ototoxicity of antibiotics is observed when they are used over the age of 60 – a factor that predisposes to ototoxicity. Conclusions. In order to conduct effective antibiotic therapy, it is very important to take into account the side effects that are characteristic of certain groups of antibiotics and each is representatively individual.

Synthesis, Reactions, and Antimicrobial Evaluation of 2-(1,3-dioxoisoindolin-2-yl)acetohydrazide derivatives

“…Also, 5-(1H-indol-3-yl)dihydropyridazine-3,4,6(5H)trione (8) was synthesized through reaction of compound 1 diethyloxalate and Na metal in absolute ethanol at reflux for 12h (Scheme 1). While 2-(1Hindol-3-yl)acetyl azide (9) was prepared via reaction of hydrazide 1 in acidic medium with addition of sodium nitrite portion-wise till effervesces (Scheme 1). Their structures were elucidated through elemental and spectroscopic analyses (cf.…”

“…Besides, Acetic acid and αmethyl acetic acid derivatives as mentioned in literature possess high potency degree as antiinflammation drugs. [6][7][8][9][10] Literature survey indicated that nitrogen-rich heterocycles such as triazoles, thiadiazoles, and oxadiazoles have attracted attention of many researchers as they have notable biological properties, especially cytotoxic effects. [11][12][13] These molecules of azoles revealed very intensive antmicrobial, antitumor and anticancer activities.…”