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VIJAY NAGDEV
H.O. MEDICAL UNIT-I
Background
In 1962 nalidixic acid was discovered by George lesher
during synthesis of chloroquine and was named as
quinolone
can enter cells easily via porins and are used to treat
intracellular pathogens (Legionella, pneumophila and
Mycoplasma)
RESISTANCE
Resistance to one FQL confers cross resistance to all
members of the class.
Resistance is due to one or more point mutations in
the quinolone binding region of the target enzyme
OR to a change in the permeability of the organism
Generations
Drugs Spectrum
1st nalidixic acid Gram- but not
cinoxacin Pseudomonas species
(Quinolone)
norfloxacin Gram- (including
ciprofloxacin Pseudomonas
2nd enoxacin species), some Gram+
(S. aureus) and some
ofloxacin atypicals
levofloxacin Same as 2nd generation
sparfloxacin with extended Gram+
3rd and atypical coverage
moxifloxacin
gemifloxacin
*trovafloxacin Same as 3rd generation
4th with broad anaerobic
coverage
Pharmacokinectics
Well absorbed orally (bioavailability 80-95% almost
equal to i.v.)
Half life 3-10 hours
Oral absorption impaired by divalent
cations(antacids containg Mg, Ca,or AL ).
Most of fluoroquinolones eleminated by renal
mechanism so adjustment required in patients with
creatinine clearance <50 ml/min.
Limited CSF penetration.
Cont…….
[Conc] > serum: [Conc] < serum:
Prostate tissue Prostatic fluid
Stool Bone
Bile CSF
Lung
Kidneys
Neutrophils
Macrophages
Drug interactions
Drugs increasing levels of FQL FQL increasing the levels of :
Theophyline antidepressants
NSAIDS Imipramine
corticosteroids caffene
theophyline
Warfarin (INR –monitored)
Adverse effects.
Generally safe antibiotics
G.I-nausea,vomiting,diarrhea and antibiotic
associated colitis have been reported.
CNS-confusion,insomnia,dizziness,anxiety,and
seizures(displacement of GABA from its receptors).
CVS-torsade de pointes,prolonged QTc interval.
May damage growing cartilage resulting in
arthropathy(but that’s reversible so may b used in
psudomonal infections in C.F where benefit
outweighs the risk.)
Cont.
Tendonitis and tendon rupture is rare but very
serious.
Phototoxicity-avoid excesive sun exposure.
Leukopenia,eosinophilia (rare)
Mild elevation in transaminases (rare)
Contraindication
Childrens (not absolute)
Pregnancy
Lactation
Epilepsy
QTc prolongation
Commonly used Fluoroquinolones
Ciprofloxacin
2nd generation fluoroquinolone
Mainly effective against G – bacteria :
Enterobacteriacae H. influenzae M. catarrhalis
Campylobacter Pseudomonas N. gonorrheae
Intracellular pathogens
M. Tuberculosis Mycoplasma Chlamydia
Legionella Brucella
Not effective against G+ and anaerobes
Clinical uses
1.Urinary tract infections (G- bacteria)
2. Osteomyelitis due to P. aeruginosa
3. Gonorrhea
4. Travellers’ diarrhea- ciprofloxacin commonly used
5. Tuberculosis
6. Prostatitis
7. Community- acquired pneumoniae
8. Diabetic foot infections ( P. aeruginosa )
9.Anthrax
Usual dosage is 7-14 days
Available forms
Oral Parentral Opthalmic
100 mg 200 mg iv 3mg/ml solution
250 mg 400 mg iv 3.3mg/mg
ointment
500 mg
ADRs
Blood glucose disturbances in DM patients
QTC prolongation, torsades de pointes, arrhythmias
Nausea, GI upset
Interstitial nephritis
Usual duration same 7-14 days
Available forms
Oral Parentral Opthalmic
100 mg 5 mg/ml iv 5mg/ml solution
250 mg 25 mg/ml iv
500mg
Brand name:leflox,l-cin,qumic
Moxifloxacin
Spectrum: Gram-, Gram+ (S. aureus including MRSA & S.
pneumoniae) & atypicals (L. pneumophila, C pneumonia & M.
pneumoniae), Mycobacterium tuberculosis, gram-negative anaerobes
Indications:
Chronic bronchitis
CAP
Bacterial conjuctivitis
Sinusitis
ADRs
Blood glucose disturbances in DM patients
QTC prolongation, torsades de pointes, arrhythmias
Nausea, GI upset
Interstitial nephritis
Available forms.
Oral Parentral
400 mg 400 mg iv bag
Brand name :