Quino-Lones

 Group of syn anti mibrobial Agents

 These Quinolony having Quinolone ring in the

structure
Nalidixic-acid: first quinolone that has
 It is not so popular because of narrow spectrum .

E.coli,
 It is a bactericidal Enlerobacter
againt Gram-ve Stigella, protein

Kle.b siella,
salmonella
MOA
 Some as that of fluro-quino

 inhibition of DNA gyrate in bacteria

PK
 well absorb orally

 plasma conc. Of free drug is in adequate to

produce systemic effects because it is rapidly
Excreted
 It attain high conc. In the urine and gut
Uses:
1. Urinary antiseptic in uncomplicated
UTI

shigella
2. Diarrhoea:
salmonella

ADR: haemolytic Anaemia: in G.DD deb

: allergic reaction
CNS: drowning's, headache, myalgia
Fluoro-quinolones
Fluorinated analogue of Nalidixic acidic
These five star drugs/ own used/popular

Goodoral-80 to 90%
absorption
Good sabtey
profile

Widely distributed

FQ and deeply
penetrated to
Highly potent tissues

Wider spectrum
 Classification
1ST GENERATION 2nd GENERATION

1. Norfloxacin 1. Levo flux

2. Ciprofluxacin 2. Moxiflux

3. Ofloxacin 3. Sparflux

4. Peflox 4. Lemoflux

5. Gemiflux

6. Gatiflux
Spectrum:
salmonella

1. GM-VE Gonucocci
Gonucocci
Shigella

E.coli
Meningococci
Meningococci

Influenza

Enterobactes, H. pylori
Proteus, V. cholerale

2. GM+VE staphylococci, pseudomonas

3. Intracellular micro organisms
o Legionella
M.TB, M.lepre
o Brucella Mycubacteria
o Chlymydia

o My co plasma Myco bacterium

Avium Complex
 MOA: Bactericadal action Newer FG
Newer FG
Effective against Anearobic
Effective against Anearobic
and staplococci
and staplococci
Called as Respiratory FQ.
Called as Respiratory FQ.
FQ

Inhibit
Inhibittapo-isomenage
tapo-isomenage
Inhibit
InhibitDNA
DNA iv
ivIN
INgm+VE
gm+VE
Gyrase
GyraseininGM-VE
GM-VE

Inhibit nicking (cutting)

Inhibit formation of negative (Inhibit of separation of daughter DNA)
supercoil STAND FOLLOWING DNA replication
Inhibit resealing of stand of DNA

Block Bocterial(DNA) synthesis

(Bactericidal )
 DNA gyrase

They inhibit the bacterial Enzyme

Topo isonerae IV

DNA replication
Which are required for

Transcription
During DNA replication
 Excessive +ve by DNA gyrase by

continuously introducing –ve super

coils DNA replication
 Human cells have topo- isomerage II

which function as DNA Gyrage.

 Topo- isomerase can inhibited by FG

but only at (500-1000 tiny) high conC

 Hence FQ reasonably safe drug
Resistance to FQ
 Mutation in target Enzyme

 Affinity of Enzyme for drug

 Protection of DNA Gyrase-by

some proteins- plasmid

mediated
Cross resistance: may be seen
PK Oral adm
 Well absorbed
 Widely distributed and deeply penetrated to
tissue
 Ferrous, food (ca+, Al, mg) antacids

delay the absorption FQ

Hence-2hrs before
-4hrs after food
Ciproflux
Crosses
Pefloxacin
BBB
All FQ Metaboised by hepatic
microsomal Enzyme
microsomal Enzyme inhibitors
 high conc. In –kidney , lungs (sputum)

- prostatic tissues,
- Bile, macrophages, muscles
and bones.
 Excreted in urine: dose reduction in

renal failure
ADR:
1) GI disturbance- N,V,AB discomfort, diarrhoea.
2) Tendinitis- risk of tendon rapture
3) Damage growing cartilage- result in arthropath in
weight hearing JT. Hence C.I in young children
(<18 yrs).
4) Cross BBB CNS disturnance- headache,
dizzings, insemmia, convulsions, hallusination
Due to GABA antagonistic action

5) Cross placemtal C/I pregnancy

6) QT prolongation- arrhythmia levo, Gati, moxi
and Gemi
Withdrawn from market
• Gati- cardiac adverse effect
• Thova- hepatic Toxicity
• Clina- photo Toxcity

pefloxacin
7) Hypersensitivity : photosensitivity pefloxacin

:I/ china, rashy moxi

moxi
: EQ sinoptilia
: Urticaria lome
lome

Spar
Spar
Uses of FQ
 DOC – Typhoid - now-a-days got resistance
 UTI - DOC- most commonly used because Effective

against GH-VE bacilli

 FG are superior to cotrimaxazole for the treat of UTI

 Bacterial prostatitis

 Bacterial Diarrhoea : GI infextions

 Ty poid fever- DOC- cipro, levo, oflex

rapid resolution of symptoms

As they attain Effective conc. In Bile and intestinal
mucosa.
 In case of multi drug resistant cases

- Azithro and ceftriaxome

STD:
Cervicitis
 Gonococal infection
Urethritis
Urethritis
 Chamcroid
cervicitis
cervicitis
 chlymydial
Urethritis
Urethritis
 Mycrobacterial infectiobs : TB, atypical my co
bacterial

MAC in AIDS
Used other AMA
 Respiratory infections: levo and moxi (respiratory
anti microbials) highly effective.
 Anthrax : prepsre for treatment and prophylaxisis
 Eye infections : ciprotloxacis