Quinolones Flashcards
What is sourse?
Synthestic
Chemically ?
derivatives of adouble ringed hetrocyclic nucleus known as quonoline
Mode of action?
Act by inhibition of the enzyme DNA gyrase leading to blocking of DNA replication of sensitive bacteria
Mode of action?
Act by inhibition of the enzyme DNA gyrase leading to blocking of DNA replication of sensitive bacteria
What is first clinincally used quinolone ?
Nalidixic acid
Chemically have 6 fluoro ?
Yes to increase specturm , stability of drug
Secnd name of DNA gyrase ?
Topoisomerase ll in (-)
Topoisomerase lV in(+)
Spectrum ?
With exception of nalidix acid ,which is active only against gram negative bacilli , other quinolones have broad spectrum
Spectrum including ?
Esheria coli Salmonella ssp Shigella Enterobacter Campylobacter Neisseria ssp Pseudomonas aurigenosa Enterococci Pneumococci Staphyllococci
Pharmacokinetics?
Well absorbed orally and widely distributed in body tissues , peak serum concentration is reached within 1- 3 hours . can pass BBB metabolized in liver , most are excreted urinary
What is therapeutic uses ?
1 urinary tract infections ( UTI)
2 prostatitis cased by sensitive bacteria
3sexully transmitted diseases ( syphillis, gonorrhea, trichomoniasis )
4 gastrointestinal and abdominal infections
5 respiratory tract infections
6 bone joint and soft tissue infection
Adverse effects ?
Mild effects including , nausea , abdominal discomfort , headache , dizziness and rashes
- interact Ca , antiacids
× in children , lactation
Name same quinolones ?
Nitrofurantoin
Nalidixic acid
Norfloxacin
Ciprofloxacin
Dose of nitrofurantoin ( furadantin ) ?
50-100 mg ( with meals and at bedtime ) for 7-14 days
Dose of nalidixic acid ( wintomylon )?
Used only for UTI
500 mg every 6 hour for at least one week