Quinolone & Fluoroquinolones

1. Quinolone & Fluoroquinolones
Presented By
Dr. Manoj Kumar
Assistant Professor
Department of Pharmacology
Adesh Medical College & Hospital Ambala Can’t

2.  The fluoroquinolones are a family of broad spectrum,
systemic antibacterial agents that have been used
widely as therapy of respiratory and urinary tract
infections.
Defination

3. Quinolone
NALIDIXICACID
• Available for the managementofUTI.
• Limited therapeutic ability.
•A/E–GI upset, rashes,neurological toxicity, hemolysis.
• Bacterialresistance.

4. 4

5.  Fluroquinolones are bactericidal agents.
 They block bacterial DNA synthesis by
inhibiting bacterial DNA gyrase and
topoisomerase IV.
 Inhibition of DNA gyrase prevents the
relaxation of positively supercoiled
 DNA is required for normal transcription and
replication
 Inhibition of topoisomerase IV interferes
with separation of replicated chromosomal
DNA into the respective daughter cells
during cell division.
Mechanism of Action

6. Mechanism of Resistance

7.  Well absorbed orally, except norfloxacin.
 Bioavailability highest in gatifloxacin (>98%).
 Attend higher concentrations in urine, kidney, bone, genital tract,
prostate, lung & bronchial mucosa.
 CSF penetration low except in pefloxacin.
 Elimination renal.
 Food delays absorption of ciprofloxacin, norfloxacin, pefloxacin &
lomefloxacin.
 Have prolonged post antibiotic effect (6 hours).
Pharmacokinetics

8.  GIT :Nausea, abdominal discomfort, vomiting, diarrhoea.
 CNS :Headache, dizziness, agitation, alteration of mood, sleep
disturbances, seizures, hallucinations, delirium.
 Hypersensitivity : Allergic reactions, rash, purities, rarely fever,
urticaria, angioedema.
 Lomefloxacin, sparfloxacin and moxifloxacin cause phototoxicity.
 Sparfloxacin, moxifloxacin and gatifloxacin prolong QT interval on
ECG.
 Crystalluria, Arthralgias and cartilage erosions with joint swellings.
Adverse effects

9.  Food,Antacids & Iron: Decreaseabsorption
 Theophylline, caffeine, warfarin: increased serum
concentration.
 EnzymeInhibition.
 NSAIDsmayincreaseCNStoxicity. (Seizures)
Drug interactions

10.  UTI
 TB
 Typhoid
 Diarrhoea
 Gonorrhoea
 Chancroid
 Respiratory tract infections.
 Eye infection.
 Anthrax.
 Neutropenic patients.
 Gram-negative septicaemias
 Bone, Joint, Soft tissue and
intra-abdominal infections.
Therapeutic Uses

12.  Most commonly used (FQ).
 Very active against gram negative aerobes and Staphylococci.
 Food delays absorption.
 Bioavailability 60-70 % & t1/2 3-5 hours.
 Excretion in urine and faces.
 Dose: 250 -750 mg 12hourly.
 Gonorrhoea: 500 mg BD.
 Chancroid: 500 mg BD for 3 days.
Ciprofloxacin

13.  Serum concentrations low outside genitourinary and intestinal tract.
 Food decreases absorption.
 Bioavailability 35-40 % & t1/2 4.5 hours.
 No interaction with theophylline and caffeine.
 Useful in long term prophylaxis in recurrent UTI & travelling
diarrhoea.
 Dose: 400 mg 12 hourly.
 Gonorrhoea: 800 mg OD.
 UTI prophylaxis: 200 mg OD.
Norfloxacin

14.  More active against some anaerobes, M. tuberculosis, M.
leprae.
 Use in multidrug regimens in leprosy & TB (300-800
mg/day.)
 Food does not interfere with absorption.
 Penetrates CSF & t1/2 5-7.5 hours.
 Bioavailability 95%
 Crosses BBB & excreted unchanged by the kidneys.
 No interaction with theophylline and caffeine.
Ofloxacin

15.  Highly lipid soluble derivative of norfloxacin.
 Food delays absorption.
 Bioavailability 90% & t1/2 8-13 hours.
 Better tissue penetration
 Higher concentration in CSF.
 Dose to be reduced in hepatic insufficiency.
 Increases levels of theophylline and caffeine.
Pefloxacin

16.  Oral bioavailability >95% & Food delays absorption.
 Widely distributed & t1/2 6-7.5 hours.
 Excreted unchanged over 24 hours.
 Incidence of phototoxicity highest.
 No interaction with theophylline and caffeine.
 Used in respiratory infection, urinary, skin and soft tissue infection.
 Dose: 400 mg OD.
Levofloxacin

17.  More active than ciprofloxacin against Staphylococci, Streptococci,
Mycobacteria, Mycoplasma.
 Food does not interfere with absorption.
 Longest t1/2 16-3O hours & Bioavailability 90%
 Phototoxicity seen in 8% patients,
 Increases QT interval on ECG.
 No interaction with theophylline, caffeine and warfarin.
 Banned in many countries including India.
 Dose: 200 mg OD.
Sparfloxacin

18.  Oral bioavailability >90% & t1/2 6-8 hours.
 Active as ofloxacin.
 CSF penetration good remains in the tissues for a longer
period.
 Used in the treatment of urinary and respiratory tract
infection.
 Dose: 500 mg OD.
Lomefloxacin

19.  Second generation FQ & Oral bioavailability >85%.
 t1/2 12hours & excretion in urine.
 Improved gram positive activity including penicillin-resistant S.
pneumoniae and anaerobes.
 Less active against enterobacteriacea, Pseudomonas.
 Phototoxicity, CNS adverse effects common & prolongs QT interval on
ECG.
 Not interfere with theophyllin or warfarin.
 Dose: 400 mg OD
Moifloxcin

20.  Second generation FQ
 Oral bioavailability 95% & t1/2 7-10 hours.
 Increased activity against penicillin resistant S. pneumonia.
 Excreted unchanged by the kidneys
 Can prolong QT interval on ECG.
 Used in respiratory and genitourinary infection.
 Banned in many countries, available in India.
 Dose: 400 mg OD.
Gatifloxacin

21.  Potent broad spectrum quinolone used topically.
 Good activity against gram positive bacteria and
anaerobes.
 Can be absorbed systemically on topical application.
 Not recommended for simple infections like acne.
 Indicated for bacterial skin infections.
Nadifloxacin

22.  Children (not absolute)
 Pregnancy
 Lactation
 Epilepsy
 QTc prolongation
Contraindication

23. THANK YOU
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