Fluoroquinolones are in two groups – based on antimicrobial spectrum and pharmacology – divided:
Fluoroquinolones (see Table: fluoroquinolones) include a concentration-dependent bactericidal activity (efficacy) by inactivation of DNA gyrase and -Topoisomerase, of essential for bacterial DNA replication enzymes. Fluoroquinolones are in two groups – based on antimicrobial spectrum and pharmacology – divided: Older group: ciprofloxacin, norfloxacin, ofloxacin Newer Group: gemifloxacin, levofloxacin and moxifloxacin Many newer fluoroquinolones have been withdrawn due to their toxicity; among them trovafloxacin (due to severe liver toxicity), gatifloxacin (due to hypoglycemia and hyperglycemia), Grepafloxacin (due to cardiac toxicity) temafloxacin (due to acute renal failure, hepatotoxicity, anemia, coagulopathy and hypoglycemia) and lomefloxacin, sparfloxacin and enoxacin. Fluoroquinolones drug application * Ciprofloxacin oral or parenteral gemifloxacin Oral Levofloxacin Oral or parenteral moxifloxacin oral or parenteral norfloxacin Oral Ofloxacin oral or parenteral * Some fluoroquinolones are also available as otological and ophthalmic preparations. Pharmacology The absorption after oral administration is reduced by concomitant administration of metallic cations (aluminum, magnesium, calcium, zinc, iron-containing preparations). After oral and parenteral administration, the fluoroquinolones spread generously in most extracellular and intracellular fluids and accumulate in the prostate, lung and bile. Most are metabolized in the liver and excreted in the urine, where they reach high levels. Moxifloxacin is excreted primarily via the bile. Indications fluoroquinolones are effective against: Haemophilus influenzae Moraxella catarrhalis Mycoplasma sp. Chlamydia sp. Chlamydophila sp. Legionella sp. Enterobacteriaceae Pseudomonas aeruginosa (especially ciprofloxacin) Mycobacterium tuberculosis Some atypical mycobacteria methicillin-sensitive Staphylococcus Nosocomial methicillin-resistant staphylococci are resistant generally. Older fluoroquinolones show only weak activity against streptococci and anaerobes. Newer fluoroquinolones have a reliable activity against streptococci (including Streptococcus pneumoniae with reduced penicillin sensitivity.) And some anaerobes; particularly moxifloxacin is effective against most clinically important obligate anaerobes. As the use has increased, develop primarily against older fluoroquinolones resistance in Enterobacteriaceae, P. aeruginosa, S. pneumoniae, and Neisseria sp. Nevertheless, many fluoroquinolones often find clinical use (see table: Clinical applications of fluoroquinolones). Fluoroquinolones are recommended in the US because of the increasing resistance not for the treatment of gonorrhea. Clinical applications of fluoroquinolones drug use comments except fluoroquinolones moxifloxacin UTIs in existing Escherichia coli resistance to trimethoprim / sulfamethoxazole> 15% drug of choice, but increasing resistance of E. coli in some communities fluoroquinolones Bacterial prostatitis: – Salmonella bacteremia – Usually typhoid effective Infectious diarrhea effective against most bacterial causes (Campylobacter sp, Salmonella, Shigella, Vibrio, Yersinia enterocolitica.); However, increasing resistance of C. jejuni in some regions not used for E. coli 0157: H7 and other enterohemorrhagic E. coli Not effective against Clostridium difficile ofloxacin infections by Chlamydia trachomatis 7-day application of newer fluoroquinolones Community-acquired pneumonia Other preferred drugs when patients have recently taken fluoroquinolones pneumonia due to Legionella drug of choice (or azithromycin) Ciprofloxacin Hospital-acquired pneumonia Empirical application due to the activity against Pseudomonas aeruginosa They are usually along with another pseudonomawirksamen medication used Long-term oral treatment of gram-negative bacilli or osteomyelitis due to Staphylococcus aureus – meningococcal prophylaxis – anthrax prophylaxis were particularly in 2001 after bioterrorist attacks in the USA used Contraindications Contraindications Past allergic reaction to the drug Certain diseases (cardiac arrhythmia z. B. QT interval prolongation, uncorrected hypokalemia or hypomagnesemia, significant bradycardia) lead use of drugs that prolong the QT interval or lead to bradycardia (eg. As metoclopramide, cisapride, erythromycin, clarithromycin, class Ia and III antiarrhythmics , antidepressants) Clinical calculator: QT interval correction (ECG) fluoroquinolones have been traditionally classified in children contraindicated because they can cause cartilage lesions, as long as the growth plates are not closed. This view is challenged by some experts because of weak evidence in question, it is recommended to prescribe fluoroquinolones as a second-line antibiotic and to limit the use of certain diseases. These include: P. aeruginosa infections in cystic fibrosis patients, prophylaxis and treatment of bacterial infections in immunocompromised patients, life-threatening multi-drug resistant bacterial infections in newborns and infants, and Salmonella or Shigella GI tract infections. Use during pregnancy and lactation fluoroquinolones are in Pregnancy Category C (animal studies show some risk indications in human and animal studies are insufficient, but the clinical benefit outweighs the risk sometimes). Fluoroquinolones are excreted into breast milk. Use during lactation is not recommended. Side effects Serious side effects are rare; the main concerns are the following: In about 5% of patients experience abdominal pain due to a direct Stomach / intestinal irritation. CNS side effects (eg. As weak headache, drowsiness, insomnia, dizziness, mood changes) occur in <5%. NSAIDs may enhance the CNS-stimulating effects of fluoroquinolones. Seizures are rare, but fluoroquinolones should not be administered to patients with CNS diseases. Peripheral neuropathy can occur soon after taking the drug and be permanent. When symptoms (eg. As pain, burning, tingling, numbness, weakness, changes in sensation), the use of fluoroquinolone should be stopped in order to prevent irreversible damage. Tendinopathy, including Achilles tendon injury, can occur even after short-term use of fluoroquinolones. There may be an extension of the QT interval, which may possibly lead to ventricular arrhythmias and sudden cardiac death. The use of fluoroquinolones has been with the occurrence of Clostridium difficile-associated diarrhea associated (pseudomembranous colitis), and in particular with the induced by the hyper virulent C. difficile ribotype 027th Diarrhea, leukopenia, anemia and photosensitivity are rare. A rash is rare, except in pursuance of gemifloxacin over> 1 week and is more likely in women <40 years of life. Nephrotoxic effects are rare. Considerations for dosing A dose reduction except for moxifloxacin, is required in patients with renal insufficiency. Older fluoroquinolones are usually given twice a day, newer and retard forms of ciprofloxacin once daily. Ciprofloxacin increases theophylline, which can sometimes lead to theophyllinassoziierten adverse reactions (Pharmacotherapy).