Overview of Quinolones

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Overview of Quinolones by Mind Map: Overview of Quinolones

1. General information

1.1. Synthetic antimicrobial agents

1.2. First quinolone was nalidixic acid

1.3. Used traditionally for UTI

1.4. Addition of fluoride made a new class (fluroquinolones)

1.4.1. Has improved pharmacokinetics excellent safety excellent tolerability

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

1.4.3. New alternative for penicillin and cephalosporin

2. Mechanism of action

2.1. Gm -ve

2.1.1. inhibit DNA gyrase

2.2. Gm +ve

2.2.1. inhibit topoisomerase IV

3. Pharmacokinetics

3.1. Long half-life of new fluoroquinolones

3.1.1. once or twice a day dosing

3.2. absorption and distribution

3.2.1. Well absorbed by oral route (very near to IV)

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

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

3.2.4. Trovafloxacin perpetrates non-inflammed meninges

3.3. Elimination

3.3.1. renal route only ofloxacin levofloxacin

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

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

4. Classification

4.1. First generation

4.1.1. spectrum gm-ve except Pseudomonas

4.1.2. Indictions uncomplicated UTI

4.2. Second generation

4.2.1. spectrum gm-ve some gm+ve

4.2.2. Indictions All UTI STDs prostatiti skin and soft tissue infection

4.3. Third generation

4.3.1. spectrum gm-ve extended gm+ve

4.3.2. Indictions acute exacerbations of chronic bronchitis community acquired pneumonia

4.4. Fourth generation

4.4.1. spectrum same as 3rd generation extended anaerobic coverage

4.4.2. Indictions intra-abdominal infections nosocomial pneumonia pelvic infections

5. Therapeutic use

5.1. UTIs

5.1.1. Nalidxic acid for susceptible organisms only

5.1.2. fluroquinolones are more potent and more effective

5.2. STDs

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

5.2.2. chancroid infection ciprofloxacin (in three days)

5.3. GI & abdominal infections

5.3.1. typhoid fever ciprofloxacin ofloxacin

5.3.2. E. coli, shigella and salmonella treated by quinolones

5.4. Respiratory tract infections

5.4.1. treated by respiratory fluroquinolones gemifloxacin moxifloxacin gatifloxacin ciprofloxacin levofloxacin

5.5. Bone, joint & soft tissue infections

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

5.6. Other infections

5.6.1. prophylaxis

5.6.2. anthrax

5.6.3. multidrag resistant TB (with other drugs)

6. Adverse effects

6.1. common

6.1.1. nausea

6.1.2. vomiting

6.1.3. abdominal discofort

6.1.4. rashes

6.1.5. insomnia

6.1.6. dizziness

6.1.7. headache

6.2. hypo/hyperglycemia with gatifloxacin in old people

6.3. contraindications

6.3.1. pregnancy

6.3.2. cation with people using quinidine procanimide amiodarone

6.3.3. under 18 years old FQ damage growing cartilage causing arthropathy