Folate & DNA synthesis inhibitors Flashcards
What principle is used for Anti-folates?
Bacteria can’t produce folic acid exogenously; must be made from PABA
Sulfonamide - MOA
Inhibit dihydropteroate synthase
Trimethoprim - MOA
Inhibit dihydrofolate reductase
Cotrimoxazole - MOA
Combination of Sulfonamide & Trimethoprim
Are Sulfonamide & Trimethoprim bacteriostatic/cidal?
Both bacteriostatic, but if combine = bactericidal
Anti-folates - PK
Good oral
Good CSF - TMP > SMZ
Sulfonamide - Spectra
Gram +ve & -ve
Trimethoprim - Spectra
Same as sulfonamides; given when allergic to sulfonamides
Cotrimoxazole - Spectra
MRSA
Can be used in immunocompromised pts
Anti-folates - SE
GI Allergy (sulfa) Photosensitivity Renal Hyperkalemia BM suppression (give folinic acid if pregnant, malnourished)
Sulphonamides - DDI
1) Enhance oral anticoags
2) Potentiate sulfonylurea hypoglycemic agents & hydantoin anticonvulsants
Since 2) is via albumin displacement = cause Kernicterus
Trimethopirm - DDI
Enhance Warfarin
Increase Methotrexate
Increase half-life of Phenytoin
Name 2 groups of DNA synthesis inhibitors
Fluoroquinolones & Nirofurantoin
Fluoroquinolones - MOA
Inhibit DNA gyrase
High conc - inhibit Topoisomerase IV
Fluoroquinolones - PK
Good oral
Good CSF