[Gyrase inhibitors, a new class of therapeutic drugs]
1Institut für Pharmakologie und Toxikologie am Fachbereich Veterinärmedizin, Justus-Liebig-Universität Giessen.
Abstract:
Fluorinated inhibitors of gyrase open a new field in chemotherapy. For veterinary purposes one drug, enrofloxacin (Baytril), has been registered hitherto in Germany. Well known disadvantages of the old gyrase blockers (e.g. nalidixic acid and others) have been their limited clinical application (compounds were useful only for therapy of infections of kidney cavities) and their deficits in antimicrobial efficacy regarding Gram-positive bacteria, pseudomonas and mycoplasmas. Fluorinated 4-quinolones, however, exhibit broad antibiotic effects in addition to their useful pharmacokinetic properties. The compounds are indicated in therapy of infections by E. coli, Salmonella, Pasteurella, Mycoplasma and Haemophilus species as well as against CRD (chronic respiratory disease). Development of resistance is markedly slowed down compared with nalidixic acid due to a multi-step resistance. Resistance is unstable and may revert in bacteria. Nevertheless, resistant bacteria in the veterinary field are exceptions. Cross-resistance includes only compounds belonging to 4-quinolones. Adult animals show few side effects to gyrase blockers. In young animals a deficit in biotransformation and renal clearance has been observed. Most prominent are dose dependent irreparable deformations of joint cartilages which have forced to contraindicate the use of Baytril in growing dogs.
More Related Videos
10:28A Semi-High-Throughput Adaptation of the NADH-Coupled ATPase Assay for Screening Small Molecule Inhibitors
Published on: August 17, 2019
10:29Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Related Concept Videos
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers
Class 1A Antiarrhythmic Drugs: These drugs work by moderately blocking sodium channels,...
Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Inhibitors of Bacterial Protein Synthesis
Inhibitors of Bacterial DNA Synthesis
