Trimethoprim: A Review of its Antibacterial Activity, Pharmacokinetics and Therapeutic Use in Urinary Tract Infections

  title={Trimethoprim: A Review of its Antibacterial Activity, Pharmacokinetics and Therapeutic Use in Urinary Tract Infections},
  author={Rex N. Brogden and A. A. Carmine and Rennie C. Heel and Trevor M. Speight and Graeme S. Avery},
SummarySynopsis: Trimethoprim,1 which has been widely available for several years in combination with sulphamethoxazole as co-trimoxazole, 2 is now available for use alone in the treatment of acute uncomplicated urinary tract infections. Trimethoprim, which is active against a wide range of Gram-positive and Gram-negative aerobic bacteria, is readily absorbed by the oral route and is widely distributed in body fluids and tissues. In therapeutic trials, trimethoprim 200 to 400mg daily has been… 


Co-trimoxazole has made an important contribution to the treatment of infectious diseases, and will continue to do so for some time to come, as additional clinical experience and newer developments further clarify its optimum role in antimicrobial chemotherapy.

Efficacy and safety properties of Lumefantrine-Trimethoprim-Copper complex in mice

The observed modifications in the biochemical indices and the presence of chromosomal aberrations in the organs studied, suggested a selective and functional toxicity of the drug.

The effectiveness of nitrofurantoin, fosfomycin and trimethoprim for the treatment of cystitis in relation to renal function.

Bioavailability of a Combination Preparation of Trimethoprim and Folic Acid

This new type of formulation of trimethoprim and folic acid has been developed in order to prevent in long-term use the adverse haematological effects induced by trimethOPrim alone.

Rational Prescribing of Antibacterials in Ambulatory Children

Rational antimicrobial treatment of common paediatric bacterial infections such as streptococcal tonsillopharyngitis, acute otitis media, acute sinusitis, bacterial pneumonia, pertussis, Lyme borreliosis (early stage) and lower urinary tract infection is reviewed.

Trimethoprim, Creatinine and Creatinine-Based Equations

Evidence of the differential effects of trimethoprim and Sfx on serum creatinine concentrations and GFR and their relevance to clinical practice is focused on, with particular attention to kidney transplantation.

Pneumocystis Pneumonia: Immunity, Vaccines, and Treatments

The immune response to Pneumocystis spp.

Tetramorphs of the Antibiotic Drug Trimethoprim: Characterization and Stability

Trimethoprim (TMP) is a well-known antifolate drug and one of the most widely used broad-spectrum antibiotics. TMP was first approved by the United States FDA in combination with sulfamethoxazole




It was concluded that combined treatment with sulfamethoxazole and trimethoprim is indicated in sulfonamide‐resistant infections as well, and the treatment is significantly more effective than treatment with trimETHoprim alone.

Trimethoprim and co-trimoxazole in the treatment of acute urinary tract infections: patient compliance and efficacy.

Patient compliance and drug efficacy and side-effects were compared in two groups of patients with symptoms of acute lower urinary tract infections and trimethoprim and co-trimoxazole were of equivalent effectiveness in the control of symptoms.

Efficacy of trimethoprim, sulfamethoxazole and the combination of both in acute urinary tract infection. Clinical and pharmacokinetical studies.

Treatment with TMP alone is superior to the combined regimen due to a smaller incidence of side effects; thus, in addition to the combination with SMZ, introduction of T MP alone on the market is recommended.

Trimethoprim in the treatment of acute urinary tract infections in children.

It is concluded that trimethoprim is as effective as sulphisoxazole in the treatment of simple acute urinary tract infections of children and recommend it, in the dosage used, as an alternative first-choice drug, especially for patients who have had side effects from sulphonamides or nitrofurantoin.

Treatment of urinary tract infections with sulphonamide and/or trimethoprim

Patients with bacteriologically diagnosed urinary tract infection were randomly selected for treatment with either 1 g sulphamethizole twice daily, 200 mg trimethoprim once daily, or 410 mg sulphadiazine plus 90 mg trimETHoprim twice daily.

Pharmacokinetic Studies of Co‐Trimoxazole in Man After Single and Repeated Doses

The original in vitro findings were confirmed in vivo using experimental septicemias in mice; the CD50 of co-tnimoxazole in these experiments compared very favorably with those of ampicillin, oxytetracycline, penicillin G, and chloramphenicol.

Double-blind Trial to Compare Ampicillin, Cephalexin, Co-trimoxazole, and Trimethoprim in Treatment of Urinary Infection

In domiciliary infections and bacteriuria in pregnancy trimethoprim alone proved to be at least as effective as the other three compounds and caused fewer than half the number of side effects.

Synergism between trimethoprim and sulfonamide in urine: does it exist?

Concentration of trimethoprim in the urine from both preparations was found to be greatly in excess of the MIC for trimETHoprim-sensitive urinary pathogens.