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Trimethoprim - Coggle Diagram
Trimethoprim
Side Effects
Fewer than with Co-trimoxazole
Nausea
Vomiting
Rashes
Folate deficiency
Megaloblastic anaemia
Give folic acid supplements
May not be safe to use in pregnancy
Hypersensitivity reactions
Caused by sulphonamide
Not dose related
Mechanism of Action
Structural analogue of pteridine moiety in folate
Folate antagonist
Competes with
folate
for
dihydrofolate reductase
enzyme
No folic acid synthesis
No DNA synthesis
Bacteriostatic
Bacterial enzyme more sensitive than mammalian enzyme
ADME
Administration
PO
Absorption
Fully absorbed in GIT
Wide distribution
High concentration in...
Kidney
Lungs
Relatively high concentration in CSF
Metabolism/Excretion
Renal excretion
Activity/Use
Active against most bacteria EXCEPT...
Enterococci
P. aeruginosa
Often combined with Sulphonamides (
Co-trimoxazole
)
Main indication: UTI
