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15 Cards in this Set
- Front
- Back
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Quinolone derivatives |
1. Nalidixic acid 2. Fluroquinolones. |
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Why do we add fluorine with quinolone? |
1.To increase systemic activity. 2.To increase lipid solubility. 3.To increase potency (60 times more potent) |
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Classify of Fluoroquinolones according to nature |
1. Non fluorinated: Nalidixic acid 2. Fluorinated. |
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Classify fluoroquinolones according to generation |
1st gen: Nalidixic Acid 2nd gen: Ciprofloxacin, Ofloxacin, perfloxacin 3rd gen: Levofloxacin, Gatifloxacin, Gemifloxacin 4th gen: Moxifloxacin |
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On which organism fluoroquinolone works? |
1. Enterobactor 2. H. influenza 3. Methiciline susceptible |
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Pharmacokinetics of fluoroquinolone |
1. Lipid soluble 2. Bactericidal 3. Broad spectrum 4. Route of administration- Oral 5. Bioavailability 80-95% 6. Half life 3-10 hrs 7. Absorption is interfered by Antacid & Ferrous Sulfate. 8. Excretion- Renal(mainly), biliary. 9. Conc. dependent killing(Post Antibiotic Effect) 10. Enzyme inhibitor (CP450) 11. Drug interaction present. |
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Enzyme Needed for Dna Synthesis |
1. Topoisomerase 2/ DNA gyrase 2. Topoisomerase 4 |
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Mechanism of fluoroquinolones |
1. by inhibiting topoisomerase II they prevent relaxation of supercoiled DNA which is necessary for DNA replication.2. By inhibiting topoisomerase IV they prevent separation of daughter DNA . 2. By inhibiting topoisomerase IV they prevent separation of daughter DNA |
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What are the drugs for UTI |
1. Nalidixic acid 2. Ciprofloxacin |
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What are the indication of Quinolones? |
1. UTI 2. Diarrhoea caused by salmonella shigella 3. Soft tissue infection, infection in bones and joints. 4. Respiratory tract infection. 5. Urethritis, Cervicitis, Osteomyelitis, Gonorrhoea. 6. Prophylactic use in Anthrax. |
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How to differentiate between amoebic and bacillary dysentry? |
1. Presence of mucus- Amoebic 2. Abdominal pain more in Bacillary. |
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What are the respiratory Quinolones? Why they are called so? |
Respiratory quinolones: 1. Levofloxacin 2. Moxifloxacin 3. Gatifloxacin 4. Gemifloxacin.
These drugs are active against gram positive plus atypical organisms (klebsiella, mycoplasma, chlamydia) causing infection in respiratory tract so they are called respiratory quinolones. |
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what are the adverse effects of quinolones? |
1. GIT upset- nausea, vomiting. 2. Headache, dizziness, insomnia. 3. Skin rash, photosensitivity. 4. Damage to the growing cartilage- Arthropathy. (so can not be given in small children) 5. Rupture tendoachilis- Tendonitis. (So can not be given to athletes) 6. Glucose intolerance in both hypo and hyperglycemia. Hypoglycemia in patients taking antidiabetic drugs. mostly caused by Getifloxacin. 7. QT prolongation in ECG. 8. Hemolytic anemia in those who have Glucose 6 phosphate dehydrogenase deficiency and take Nalidixic Acid. 9. Enzyme inhibition |
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What are the contraindications of quinolones? |
1. Children 2. Pregnancy 3. Those who have- a. Malabsorption syndrome b. GIT mucus abnormality c. Renal impairment.
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write down drug interaction of quinolones |
1. NSAID + Ciprofloxacin has convulsive effect. 2. Ciprofloxacin+ Iron - decrease absorption |
