Paper
Trimethoprim: Mechanisms of Action, Antimicrobial Activity, Bacterial Resistance, Pharmacokinetics, Adverse Reactions, and Therapeutic Indications
Published Jul 8, 1981 · R. Gleckman, N. Blagg, D. Joubert
Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
125
Citations
2
Influential Citations
Abstract
Trimethoprim has recently been marketed as a single‐entity product for the treatment of initial episodes of uncomplicated symptomatic urinary tract infections; it was previously available only in combination with sulfamethoxazole. Trimethoprim exerts antimicrobial activity by blocking the reduction of dihydrofolate to tetrahydrofolate, the active form of folic acid, by susceptible organisms. It has inhibitory activity for most gram‐positive aerobic cocci and some gram‐negative aerobic bacilli. Resistance to trimethoprim may be either intrinsic or acquired. Acquired resistance most commonly stems from a chromosomal mutation that results in the production of a dihydrofolate reductase enzyme which is less vulnerable to trimethoprim inhibition.
Trimethoprim effectively treats uncomplicated urinary tract infections by blocking the reduction of dihydrofolate to tetrahydrofolate by susceptible organisms.
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