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20 Cards in this Set
- Front
- Back
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Nitrofuratonin mechanism
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Reduction of the molecule, which then goes on to form double stranded breaks
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Nitrofuratonin resistance
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None, essentially
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Nitrofuratonin absorption
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High oral bioavalability
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Nitrofuratonin distribution
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Doesn't achieve bacteriocidal concentrations in the plasma!
Restricts use as an oral drug. |
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Nitrofuratonin metabolism
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Quick, like Nitro in cars!
T1/2 = .3 - 1 hr. |
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Nitrofuratonin excretion
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40% excreted unchanged in the urine
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Nitrofuratonin clinical uses
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UTIs
-Treatment -Prophylaxis |
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Nitrofuratonin adverse effects
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-GI disturbances
-Hematologic: hemolytic anemia in G6PD deficiency -Pulmonary reactions: acute and chronic; fever, cough, dyspnea -Hypersensitivity -Neurologic: headache, vertigo, polyneuropathies Fat albert in my room |
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Types of quinolones
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Flouroquinolones have -oxacin in the name. Ex: norfloxacin
Quinolone: Nalidixic acid |
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Flouroquinolones mechanism
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Adhering either the gyrase or topoisomerase when bound to double-strand broken DNA.
Gyrase in negative organism. Can't relieve torsional stress. TopoIV in positive organisms. Can't resolve interlinked daughter chromosmes |
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Quinolone resistance in gram - bugs
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-Transporters efflux all antimicrobials
- Mutations in DNA gyrase give intermediate resistance -Mutations in gyrase, topoisomerase give high level resistance -Qnr genes express proteins that give gyrase resistance -Aac genes acetylate compounds, preventing binding |
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Quinolones Gram positive mechanism
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Primarily acts against Topoisomerase IV
Can't dissociate from DS broken DNA BacterioCIDAL |
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Quinolones Gram negative mechanism
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Primarily acts against DNA Gyrase
Can't dissociate from dsDNA breaks BacterioCIDAL |
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Gram positive resistance to quinolones
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-Transporters efflux ONLY flouroquinolones
-Mutations in topoisomerase gives resistances -Mutations in the gyrases and topoisomerases gives high level resistance -Aac genes acetylate drugs, preventing binding to topoisomerase |
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Floroquinolones absorption
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70% ORAL bioavailability
Di, trivalent cations decrease absorption |
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Floroquinolones distribution
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Most tissue, body fluids
Variable CSF penetration Larger concentrations inside: urine (UTIs), lungs (respiratory infections), macrophages, kidneys, prostate, bones (osteomyelitis) than in serum - this is directly related to the kinds of infections treated! |
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Floroquinolones metabolism
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Liver
T1/2 = 3 - 8 hrs. |
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Floroquinolones excretion
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Renal, bile
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Floroquinolones adverse effects
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GI Irritation
CNS effects Photosensitivity TENDON RUPTURE!!! Damage to growing cartilage (don't give to mothers) |
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Floroquinolones uses
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Good against gram positive, gram negative bacteria
UTIs Respiratory infections Bacterial diarrheas Osteomyelitis |
