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Trimethoprim

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Topic updated on 09/03/17 7:28pm

Introduction
  • Classification
    • antibiotic
      • miscellaneous
        • trimethoprim
  • Drugs
    • trimethoprim
Mechanism
  • Action
    • bacteriostatic
    • competitive inhibitor of dihydrofolate reductase
    • like sulfonamides, inhibits the THF synthesis pathway, but inhibits a different enzyme further downstream
      • see Sulfonamides  for more detail
    • humans also have dihydrofolate reductase
      • although bacterial enzyme's affinity for drug is much higher
      • leads to antifolate side effects
  • Synergy with sulfonamides
  • Resistance
    • ↓ affinity of dihydrofolate reductase for trimethoprim
Uses
  • Used in combination with sulfonamides (as TMP-SMX -- "Bactrim")
  • See Sulfonamides  or a list of diseases
Adverse effects
  • Give folinic acid (not folic) to prevent adverse effects 
  • Adverse effects are similar to other antifolate drugs (e.g. methotrexate)
    • megaloblastic anemia
    • leukopenia
    • granulocytopenia


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