Quinolones
Quinolones
-Are chemically related compounds of Nalidixicacid which was the first class of antimicrobialagents use for the treatment of UTI.
Nalidixic acid
Suboptimal pharmacokinetic profile
Narrow spectrum
Microbial resistance problem
Floroquinolones
-Differ from older compounds in that they afluorine at the position C
6
, and a piperazinylmoiety at C
7
position of the quinolonenucleus.
Mechanism of Action
They interfere with bacterial DNA synthesis byinhibiting topoisomerase II (DNA gyrase) andtopoisomerase IV.Antimicrobial Activity - BactericidalAntimicrobial Spectrum - broad
Gm (-) bacteriaGm (+) Orgs
1.E. coli2.Klebsiella3.Enterobacter 4.Serratiamarcescens5.Proteus
6.
Morganella1. Methicillin susceptible andresistant strain of a.S. Auerus b.S. Epidermidisc.Other coagulase (-) staph7. Providenica8. Citrobacter 9. Acidetobacter 10. Eikenellacorrodens2. Streptococcus pneumonia(same as M3)3. Strep A, B, C, D and G – are only marginallysusceptibleOther Organism11. Pasteurellamultocida12. Aeromonashydrophila13. Salmonella14. Shigella15. Campylobacter jejuni16. Yersiniaenterocolitica17. Vibrio18. P. acroginosa19. H. influenza1.M. Tuberculosis2.M. Kankasii3.M. fortuitum20. H. ducreyi21. Neisseriameningitis22. N. gonorrhoea23. BranhamellacatathalicActivity against anaerobic baderia is poor Poor activity against Anerobic bacteria (exceptTosufloxacin)
Members:
1.Ciprofloxacin8. EnoxacinSesquihydrate2.Norfloxacin9. Rosoxacin
3.
Pefloxacin10. Fleroxacin
4.
Ofloxacin11.Tosufloxacin5.Levofloxacin12.Sparfloxacin6.Moxifloxacin 13.Grepafloxacin7.Lumifloxacin
Pharmacokinetics
-Bioavailability after oral adm – 95-100%-Elimination is through renal excretion via activetubular secretion. Pefloxacin is metabolize bythe liver (non- renal excretion). Moxifloxacin,sparfloxacin, and trovafloxacin are eliminated partly by hepatic and biliary excretion.
Drug Interaction:
1.
Al(OH)
3
+ Mg(OH)
3
(Antacid)GI absorption
2.
Sucralfate
3.
Inhibits theophylline met. serum level of theophyllin
of 00
Quinolones
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| Category: | Uncategorized. |
| Rating: | (1 Rating) |
| Upload Date: | 01/26/2009 |
| Copyright: | Attribution Non-commercial |
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