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Overview of Quinolones by Mind Map: Overview of Quinolones
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Overview of Quinolones

General information

Synthetic antimicrobial agents

First quinolone was nalidixic acid

was a bye product of chloroquine synthesis

Used traditionally for UTI

Addition of fluoride made a new class (fluroquinolones)

Has improved pharmacokinetics, excellent safety, excellent tolerability

Improved antimicrobial activity, Used for a variety of infections, skin, respiratory, UTI

New alternative for penicillin and cephalosporin

Mechanism of action

Gm -ve

inhibit DNA gyrase

Gm +ve

inhibit topoisomerase IV

Pharmacokinetics

Long half-life of new fluoroquinolones

once or twice a day dosing

absorption and distribution

Well absorbed by oral route (very near to IV)

concentration in some tissues is high, renal, gall bladder, bile, lung, bronchial, nasal, prostate, gentile tract

ciprofloxacin and ofloxacin, concentration in urine is 25 times higher than in serum, used for UTI

Trovafloxacin perpetrates non-inflammed meninges

Elimination

renal route only, ofloxacin, levofloxacin

renal and non-renal, nalidixic acid, norfloxacin, ciprofloxacin, enoxacin, lomefloxacin, gatifloxacin, moxifloxacin, sparfloxacin

facal route, Trovafloxacin, 50% conjugated in the liver, 43% excreted unchanged in the feces

Classification

First generation

Nalidixic acid

spectrum, gm-ve except Pseudomonas

Indictions, uncomplicated UTI

Second generation

NorfloxacinLomefloxacinCiprofloxacinOfloxacin

spectrum, gm-ve, some gm+ve

Indictions, All UTI, STDs, prostatiti, skin and soft tissue infection

Third generation

LevofloxacinSparfloxacinMoxifloxacin

spectrum, gm-ve, extended gm+ve

Indictions, acute exacerbations of chronic bronchitis, community acquired pneumonia

Fourth generation

Trovofloxacin

spectrum, same as 3rd generation, extended anaerobic coverage

Indictions, intra-abdominal infections, nosocomial pneumonia, pelvic infections

Therapeutic use

UTIs

Nalidxic acid for susceptible organisms only

fluroquinolones are more potent and more effective

STDs

N. Gonorrhoeae, was treated with ofloxacin or ciprofloxacin (single dose), now ceftriaxone

chancroid infection, ciprofloxacin (in three days)

GI & abdominal infections

typhoid fever, ciprofloxacin, ofloxacin

E. coli, shigella and salmonella, treated by quinolones

Respiratory tract infections

treated by respiratory fluroquinolones, gemifloxacin, moxifloxacin, gatifloxacin, ciprofloxacin, levofloxacin

Bone, joint & soft tissue infections

osteomyelitis and joint infections, 4-6 weeks, treated with fluoroquinolones, 500 mg twice a day, 750 mg in severe cases

Other infections

prophylaxis

anthrax

multidrag resistant TB (with other drugs)

Adverse effects

common

nausea

vomiting

abdominal discofort

rashes

insomnia

dizziness

headache

hypo/hyperglycemia with gatifloxacin in old people

contraindications

pregnancy

cation with people using, quinidine, procanimide, amiodarone

under 18 years old, FQ damage growing cartilage causing arthropathy