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22 Cards in this Set
- Front
- Back
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Sulfonamides
MoA (Pathway)? |
PABA ----(dihydropteroate Synthase)--> Folate
Folate ---(dihydrofolate reductase)--> THF --> Thymadine Sulfonamides are PABA analogues that inhibit dihydropteroate Synth = No Folic Acid synthesis Blocks NA Synthesis Inhibitors |
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Sulfonamide Pk
Route? BBB? Metabolism/cautions-Soln? Spectrum/use? |
Oral with good absorb, +BBB
Acetylated/Conjugated by liver and crystalizes in acidic urine; (drink lots of H2O or Rx Bicarb) Bacteriostatic agent for g+, g-, no mycoplasma |
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Tx of Abscess with Sulfas?
Problem/Soln? |
Abscess are full of PABA that will out compete the drug for dihydropteroate binding sites; abscess needs to be drained first
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Sulfonamides (5)
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Sulfamethoxazole
Sulfisoxazole Sulfadiazine Sulfadoxine Mafenide |
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General uses?
Trimethoprim + Sulfamethoxazole? Pyramethamine + Sulfadiazine? Pyramethamine + Sulfadoxine? |
Generally paired with others b/c of resistance
Jirovicci = Trimethoprim + Sulfamethoxazole Toxoplasma = Pyramethamine + Sulfadiazine Malaria = Pyramethamine + Sulfadoxine |
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Sulfacetimide
MoA? Spectrum? Tx (1)? |
Inhibits Dihydropteroate Synthase = No Folic acid = NA Synthesis inhibitor
Tx: Eye Infections |
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Mafenide
MoA? Spectrum? Tx (1)? Ae(2)? |
Inhibits Dihydropteroate Synthase = No Folic acid = NA Synthesis inhibitor
Tx: Burn Dressing Ae: Burning Sensation/Metabolic Acidosis |
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Silver Sulfadiazine
MoA? Spectrum? Tx(1)? |
Inhibits Dihydropteroate Synthase = No Folic acid = NA Synthesis inhibitor
Tx: Superior Tx for burn dressing than Mafenide |
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Trimethoprim
MoA? Distribution(1)? Tx (2)? Ae(2)? |
MoA: Inhibits Dihydrofolate reductase = No Folic Acid = NA Synthesis inhibitor
Distributes widely, especially into prostate Tx: Prostatitis, UTI Ae: APLASTIC ANEMIA, Enterocolitis |
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Cotrimethoxazole
MoA? Spectrum (2) ? What doesnt it cover? Synthesis/FDC? DoC(2)? Tx(1)? |
Co + Trimethoprim + Sulfamethoxazole
Bacterocidal -Seq inhib Dihydropteroate synth and dihydrofolate reductase. g+, g-; no Mycoplasma coverage Fixed drug combo of 5:1 Sulfa to Trimethoprim DoC: Nocardia (Nosocomial PNA); P. Jirovivi Tx: UTI |
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Sulfa Contraindications (1)?
Ae: (7)? |
C/I Prego - decreases folic acid = Neural Tube defects
Phototoxic, Stevens-Johnson(profuse mucosal bleeding), G6PD Hemol, Kernicterus(displaces BR), HSR , Crystalluria |
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Sulfamethoxazole Resistence
Trimethoprim Resistance (3)? |
Overproduction of PABA (Abscess)
Mutation in target Enzyme Permeability Change |
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Quinolones
MoA? cidal/static? Spectrum? |
Bacteriocidal Agent that inhib DNA Gyrase: Topo II - (clips but doesn't reseal) = Toxic DNA Fragments Accumulate; = no NA Synthesis
Spectr: g- |
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Nalidixic Acid
Class/Spectrum? MoA? Tx Problems? Ae(3)? |
Quinolone; Topo II Inhib; NA Synth Inhib
Doesn't reach high enough serum levels, high urine concentration Rapid Resistance, G6PD Hemol. SEIZURES |
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Fluoroquinolones
MoA? CDKE/PAE? Tx (2)? |
NA Synth Inhib; inhibits Topo II and Topo IV
+CDKR/PAE Tx: g+ streptococci, g- |
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Fluoroquinolone Pk
Route/admin? Metabolism (exception)? |
Orally Administetred; Take on empty stomache, will Chelate with cations;
B/D by liver, secreted via ATS (Probenecid will enhance) (moxifloxacin excreted via GI/Bile) |
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Ciprofloxacin/Levofloxacin
MoA? Spectrum? DoC(3)? |
NA Synth Inhib; inhibits Topo II and Topo IV
+CDKR/PAE Tx: g+ streptococci, g- DoC: Anthrax, Typhoid FV, MDR-TB, |
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Moxifloxacin
MoA? Worst against? |
NA Synth Inhib; inhibits Topo II and Topo IV
+CDKR/PAE Worst against Pseudomonas |
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Trovafloxacin
Tx? |
Fluoroquinolone not used b/c of Liver Toxicity
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Norfloxacin
MoA? Tx(2)? |
NA Synth Inhib; inhibits Topo II and Topo IV
+CDKR/PAE Tx: UTI/Prostatitis |
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Fluoroquinolone Ae (4)? C/I (2)?
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CNS
Phototoxic Prolonged QT Cartiladge/Achilles Rupture C/I: Prego or kids b/c it chelates cations |
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Fluoroquiolone Drug Interactions (2)? Resistance (2)?
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NSAIDS incr phototoxicity and seizures;
CYP450 inhib Inactivated by acetylatation (like AMG) Mutations in Topo II/IV |
