this ppt gives brief discussion for under graduate examination

1. Dr. RAGHU PRASADA M S
MBBS,MD
ASSISTANT PROFESSOR
DEPT. OF PHARMACOLOGY
SSIMS & RC.
1

2. The quinolones (Qs) and fluoroquinolones (FQs)
are a family of broad-spectrum
synthetic antimicrobial agents.
The parent of the group is
nalidixic acid
The fluoroquinolones have a fluoro
group attached the central ring system.

3.  Qs and FQs are bactericidal drugs.
 FQs enter into the host cells  active against
intracellular pathogens  Legionella spp.,
Mycoplasma spp. and Chlamydia spp.

4.  They inhibit enzymes called topoisomerase, enzymes
needed for supercoiling, replication and separation
of circular bacterial DNA.
 1. G-VEDNA Gyrase is a topoisomerase II that
catalyzes the negative supercoiling of the circular
DNA found in bacteriaprevent replication of
bacterial DNA
 2. G+veTopoisomerase IV relaxation of the
supercoiled circular DNA, enabling the separation of
the interlinked daughter chromosomes at the end of
bacterial DNA replicationinhibition of cell division

5.  First Generantion- Norfloxacin, Ciprofloxacin,
Ofloxacin, Pefloxacin, Lomefloxacin
 Second Generation- Levofloxacin, Prulifloxacin,
 Third Generation- Gatifloxacin, Sparfloxacin,
Gemifloxacin
 Fourth Generation- Moxifloxacin, Trovafloxacin,
Alatrofloxacin, Finafloxacin

7. CIPROFLOXACIN
 The most potent of the fluoroquinolones for P.
aeruginosa.
 Long post-antibiotic effect.
 Well absorbed from GIT.
 Administration: orally, IV.
 Excreted in urine.
 Potent CYP450 inhibitor

8. CIPROFLOXACIN
 The most potent of the fluoroquinolones for P.
aeruginosa.
 Long post-antibiotic effect.
 Well absorbed from GIT.
 Administration: orally, IV.
 Excreted in urine.
 Potent CYP450 inhibitor

9.  Levofloxacin
 An isomer of Ofloxacin and has largely replaced it
clinically.
 Very well absorbed from GIT.
 Administration: orally, iv.
 Excreted unchanged
 Long post-antibiotic effects.
 Long-acting (single daily dose)

10.  Treatment respiratory tract infections due to S.
pneumonia (pneumonia, COPD exacerbation).
 Used in the treatment of prostitis due to E. coli and
of sexually transmitted diseases(gonorrhea), with
the exception of syphilis.
 levofloxacin is utilized in wide range of infections,
including skin infections, acute sinusitis, nosocomial
pneumonia

11. MOXIFLOXACIN
 Long-acting (single daily dose).
 Long post-antibiotic effect.
 Mostly used for the treatment respiratory tract
infections (pneumonia, COPD exacerbation).
 Used for the treatment severe bacterial infections
including sepsis, peritonitis.
 The most potent fluoroquinolones against M.
tuberculosis.
 Poor activity against P. aeruginosa.

12. FINAFLOXACIN
Novel, under phase III
Antibacterial activity increases at acidic pH
More efficacious in tissue and body compartments
acidified due to infection and inflammation
Widest spectrum of G+ve, G-ve, anaerobic, and
atypical pathogens
Very long t1/2
High safety profile-no incidence of hepato, renal,
cardio and phototoxicity.

14. GI: Nausea, vomiting
CNS: HA, dizziness, confusion, insomnia, delerium,
hallucinations, seizure (rare)
Cardiovascular: QT-prolongation Torsades de pointes
(III gen)
Endocrine -Blood glucose disturbances in DM
patients(levo, moxi)
Musculoskeletal: Rupture of tendon (prolonged use)
Hepatotoxicity- Trova, Alatro
Photo toxicity- Lome, Pefl, Gati,

15.  Ciprofloxacin is a potent CYP450 inhibitor. Increases
plasma levels and toxic effects of anticoagulants,
digoxin, theophylline
 FQs in combination with with class IA and class III
antiarrhythmics prolong QT and may cause
arrhythmias
 Antacids has been found to result in six to ten fold
decreases in the absorption of oral quinolones.

16.  Fluoroquinolones generally should not be
administered to patients younger than 18 years of
age.
 Fluoroquinolones should not be administerd to
pregnant or lactating women.
 Should not be given to arrythmic patient.

17.  Gemifloxacin has been approved for the treatment
of mild to moderate community-acquired
pneumonia and acute exacerbation of chronic
bronchitis but has increased risk of tendinitis
 Sparfloxacin-photosensitivity, cardiotoxicity- QTc
prolongation
 Trovafloxacin/Alatrofloxacin-was withdrawn because
of the risk of hepatic toxicity.
 Gatifloxacin was withdrawn because of an increased
frequency of hypoglycemia and hyperglycemia,
cardiotoxicity- QTc prolongation

18. NALIDIXIC ACID
 Non flourinated quinolone
 98% protein bound, excre- urine
 G-ve coliforms except pseudomonas
PHENAZOPYRIDINE
Dye with analgesic effects
Relives burning sensation, dysuria, urgency
ADR-Epigastric distress, orange coloured urine

19.  Nitrofurantoin niitroanion superoxidedamage
bacterial DNA
 Nitrofuron derivative
 MOA- blocks acetyl CoA synthesis carbohydrate
metabolism
 BacteriostaticBactericidal
 Loses its action at p H of 8
 E.coli, proteus, St.aureus, E.faecalis
 Prophylaxis of UTI
 ADR-Nausea, Ph.neuritis, hepatitis, pulmonary
fibrosis, hemolytic anemia
 D/I- probenacid, nalidixic acid

20. Acidic urine
 NITROFURANTOIN
 TETRACYCLINE
 METHICILLLIN
 CLOXACILLIN
Alkaline urine
 COTRIMOXAZOLE
 GENTAMYCIN
 CEPHALOSPORINS