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

1.4.1.1. excellent safety

1.4.1.2. excellent tolerability

1.4.2. Improved antimicrobial activity

1.4.2.1. Used for a variety of infections

1.4.2.1.1. skin

1.4.2.1.2. respiratory

1.4.2.1.3. 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

3.2.2.1. renal

3.2.2.2. gall bladder

3.2.2.3. bile

3.2.2.4. lung

3.2.2.5. bronchial

3.2.2.6. nasal

3.2.2.7. prostate

3.2.2.8. gentile tract

3.2.3. ciprofloxacin and ofloxacin

3.2.3.1. concentration in urine is 25 times higher than in serum

3.2.3.2. used for UTI

3.2.4. Trovafloxacin perpetrates non-inflammed meninges

3.3. Elimination

3.3.1. renal route only

3.3.1.1. ofloxacin

3.3.1.2. levofloxacin

3.3.2. renal and non-renal

3.3.2.1. nalidixic acid

3.3.2.2. norfloxacin

3.3.2.3. ciprofloxacin

3.3.2.4. enoxacin

3.3.2.5. lomefloxacin

3.3.2.6. gatifloxacin

3.3.2.7. moxifloxacin

3.3.2.8. sparfloxacin

3.3.3. facal route

3.3.3.1. Trovafloxacin

3.3.3.1.1. 50% conjugated in the liver

3.3.3.1.2. 43% excreted unchanged in the feces

4. Classification

4.1. First generation

4.1.1. spectrum

4.1.1.1. gm-ve except Pseudomonas

4.1.2. Indictions

4.1.2.1. uncomplicated UTI

4.2. Second generation

4.2.1. spectrum

4.2.1.1. gm-ve

4.2.1.2. some gm+ve

4.2.2. Indictions

4.2.2.1. All UTI

4.2.2.2. STDs

4.2.2.3. prostatiti

4.2.2.4. skin and soft tissue infection

4.3. Third generation

4.3.1. spectrum

4.3.1.1. gm-ve

4.3.1.2. extended gm+ve

4.3.2. Indictions

4.3.2.1. acute exacerbations of chronic bronchitis

4.3.2.2. community acquired pneumonia

4.4. Fourth generation

4.4.1. spectrum

4.4.1.1. same as 3rd generation

4.4.1.2. extended anaerobic coverage

4.4.2. Indictions

4.4.2.1. intra-abdominal infections

4.4.2.2. nosocomial pneumonia

4.4.2.3. 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

5.2.1.1. was treated with ofloxacin or ciprofloxacin (single dose)

5.2.1.2. now ceftriaxone

5.2.2. chancroid infection

5.2.2.1. ciprofloxacin (in three days)

5.3. GI & abdominal infections

5.3.1. typhoid fever

5.3.1.1. ciprofloxacin

5.3.1.2. ofloxacin

5.3.2. E. coli, shigella and salmonella

5.3.2.1. treated by quinolones

5.4. Respiratory tract infections

5.4.1. treated by respiratory fluroquinolones

5.4.1.1. gemifloxacin

5.4.1.2. moxifloxacin

5.4.1.3. gatifloxacin

5.4.1.4. ciprofloxacin

5.4.1.5. levofloxacin

5.5. Bone, joint & soft tissue infections

5.5.1. osteomyelitis and joint infections

5.5.1.1. 4-6 weeks

5.5.1.2. treated with fluoroquinolones

5.5.1.3. 500 mg twice a day

5.5.1.4. 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

6.3.2.1. quinidine

6.3.2.2. procanimide

6.3.2.3. amiodarone

6.3.3. under 18 years old

6.3.3.1. FQ damage growing cartilage causing arthropathy