Quinolones

Dr S A Jayaratne
Senior lecturer
Dept of pharmacology

Mechanism of action
Act by inhibiting DNA gyrase which is
necessary for supercoiling of DNA
Supercoiling is necessary for compacting DNA
in to bacterial cell
Bactericidal

Pharmaokinetics
Exhibit concentration dependent bacterial
killing
Not predictably synergistic when used in
combination with other antibiotics

Pharmacokinetics contd--

Well absorbed from gut

Widely distributed in body tissues
Moderate-excellent bioavailability
Similar blood levels with oral & iv
administration
Transition from iv to oral is easier

Pharmacokinetics contd--

Most given 12hrly

Elimination mostly renal
Dose adjustments are necessary in renal &
hepatic impairment

Antimicrobial effect
Extremely active against Gram ve organisms
- E-coli, Salmonella sp, shigella sp,
- Neisseria sp, Haemophilus sp
- Pseudomonas aeruginosa
- Legionella
Less active against Gram+ ve organisms
No effect on anaerobes

Adverse effects
Git disturbances,
allergic reactions
CNS effects-dizziness, headache, confusion
(caution against driving vehicles)
Can precipitate convulsionsavoid in those with a H/o epilepsy
concurrent use of NSAIDs

Adverse effects contd--

Increase risk of tendon damage( rupture )

caution in elderly
concomitant use of corticosteroids
If tendinitis is suspected quinolones should be
discontinued
Caution in children & in growing adolescents
(probable risk of arthropathy in wt bearing
joints )
G6PD deficiency, myasthenia gravis

Types of quinolones
Nalidixic acid
Used in treatment of uncomplicated UTI

Types of quinolones contd--

norfloxacin
ciprofloxacin
used in- UTI(Gram ve)
typhoid (salmonella)
shigellosis
bone & joint infections
infections caused by pseudomonas
aeruginosa
Less active against Gram +ve

Types of quinolones contd--

Levofloxacin
Norfloxacin Ofloxacin
Gatifloxacin
Used in UTI, relapsing UTI, prostatitis
Acute bacterial sinusitis (2nd line)

Special drugs for UTI

Nalidixic acid
Nitrofurantoin
Nitrofurantoin
Synthetic antimicrobial
Well absorbed from GIT
Concentrated in urine
Plasma levels are too low to treat infections of
kidney tissue

Nitrofurantoin contd--

Uses Acute uncomplicated UTI

Severe chronic recurrent UTI
Prophylaxis of UTI 50-100mg nocte

Nitrofurantoin contd--

Adverse Effects
Nausea & vomiting & diarrhoea
Peripheral neuropathy ( esp those with renal
impairment
Allergic reactions-urticaria, rashes , lung
consolidation , pleural effusion
Safe in pregnancy
C/I near term ( causes neonatal haemolysis)