Quinolones

The first quinolone , nalidixic acid, is a urinary

antiseptic.
It is effective against gram-negative including
E.coli, proteus, Klebsiella, enterobacter,
salmonella.
• Nalidixic acid inhibits DNA gyrase enzyme

• Interferes with the replication of bacterial

DNA.

• It is useful in the treatment of uncomplicate

UTI due to gram negative bacteria

• Diarrhoea due to shigella or salmonella.

Fluroquinolones are synthtic, flurinated
analogues of nalidixic acid.

Norfloxacin
Ciprofloxacin
Pefloxacin
Ofloxacin
Levofloxacin
Gemifloxacin
moxifloxacin
Moa
DNA gyrase in gram negative bacteria

Nicking, formation of negative supercoils and

resealing of strands of DNA

Topoisomerase IV in gram – positive bacteria

Nicking and separation of daughter DNA strands

following DNA replication
Fluroquinolones inhibits bacterial DNA synthesis
(bactericidal)

They inhibit DNA gyrase

Thus blocking DNA replication in gram negattive

bacteria.

Inhibition of topoisomerase IV in gram positive

bacteria- prevents separation of replicated DNA.
p.K
Oral, i.v topical
Well absorbed from the gut
Food delays the absorption
Widely distributed in the body
Reaches high concentration in kidney, lungs,
prostatic tissue, bile , macrophages
Excreted mainly in liver.
AE
 Related to GIT
 CNS effects
 Hypersensitivity reactions
 Tenosynovitis and tendon rupture can occur in
athletes
 Cause prolongation of QT interval
 Contraindicated in pregnancy.
 Caused cartilage damage in immature animals-
hence should be avoided in young children.
Uses
1. Urinary tract infection:
2. Bacterial diarrhoeas:(GI infection caused by
E.coli,)
3. Typhoid fever: it is bactericidal, causes rapid
resolution of symp.
4. Sexually transmitted diseases
gonococcal infections:
chlamydial cervicitis and urethritis
5. Skin ,soft tissue and bone infections (diabetic
foot infections)

6. Eradicate meningococci from nasopharynx thus

eliminating carrier state,

7. Mycobacterial infection:in multi drug resistant

tuberculosis, atypical mycobacterial infections,AIDS
patients

8. Prophylaxis and treatment of infections in

neutropenic patients:
9. Uses topically for conjunctivitis
10.Respiratory infections
11.anthrax