1. Fluoroquioblones صيدلانية نظري / د . فارس رابع صيدلة 23 / 4 / 2016
4th Year Pharmacy
2016

2. Introduction
Quinolones ( Qs) and Fluoroquinolones (FQs) are a family of broad spectrum synthetic antibiotics.
Thee parent of the group is nalidixic acid which was intoduced in G (–ve )
1-Ethyl-7-methyl-4-oxo-[1,8]naphthyridine-3-carboxylic acid

3. Fluroquinolones (QFs) have a fluoride atom attach at position 6.
1-cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-quinoline-3-carboxylic acid

4. Classification of Fluoroquinolones

5. Qs & FQs are bacteroicidial drugs
The FQs work by inhibiting one or more of a group of enzymes called topoisomerase enzymes needed for supercoiling, replication and separation of circular bacterial DNA.
1- DNA Gyrase ( topoisomerase ll )
2- Topoisomerase IV
Block of bacterial DNA synthesis by
Inhibiting topoisomerase II, IV
Gram positive & negative bacteria
Mycoplasma & clamydia, legionella
Some mycobacteria
Anaerobic bacteria

6. Mechanism of action

7. Clinical Uses of FQs Urinary tract infection Bacterial diarrhea
Even with multi-drug resistant organisms
Bacterial diarrhea
Shigella, salmonella, toxigenic E. coli
Infections of soft tissues, bones and joints
Intra-abdominal and respiratory tract infections
Gonococcal infection
Chlamydial urethritis and cervicitis
Legionellosis
Tuberculosis and atypical mycobacterial infections

8. Summary of SAR for NALIDIXIC ACID & other quinolones as anti-infective TOPOISOMERASE ENZYME INHIBITION

10. Resistance of FQs

11. Synthesis of Ciprrofloxacin

12. Adverse effects Nausea, vomiting & diarrhea
Headache, dizziness, insomnia, skin rash, abnormal liver test
Acute hepatitis & hepatic failure: trovafloxacin
Photosensivity: lomefloxacin, pefloxacin
QT prolongation: sparfloxacin
Hyperglycemia or hypoglycemia
May damage growing cartilage: arthropathy
Tendinitis