Trimethoprim

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Infectotrimet, Motrim, Triprim; Czech Republic: Triprim; Estonia: Trimetop; Finland: Trimetin, Trimex, Trimopan; Germany: Infectotrimet; Ireland: Monotrim, Trimoptin; Latvia: Trimetop; Lithuania: Trimetop; Luxembourg: Wellcoprim; Netherlands: Trimethoprim; Poland: Trimesan, Urotrim; Slovakia: Triprim; Spain: Tediprima; Sweden: Idotrim, Trimetoprim; UK: Trimethoprim.

North America

Canada: Trimethoprim; USA: Primsol, Trimethoprim.

Drug combinations

Trimethoprim and Polymyxin B

Trimethoprim and Rifampin

Trimethoprim and Sulfamethoxazole

Trimethoprim and Sulfametrole

Trimethoprim, Bromhexine, and Sulfamethoxazole

Trimethoprim, Dexamethasone, and Polymyxin B

Trimethoprim, Bromhexine, Guaiacol, and Sulfamethoxazole

Chemistry

Trimethoprim: C~14~H~18~N~4~O~3~. Mw: 290.32. (1) 2,4-Pyrimidinediamine, 5-[(3,4,5-trimethoxyphenyl)methyl]. CAS-738-70-5 (1964).

Trimethoprim Sulfate: (C~14~H~18~N~4~O~3~)~2~ H~2~SO~4~. Mw: 678.71. (1) 2,4-Pyrimidinediamine, 5-[(3,4-trimethoxyphenyl)methyl]-, sulfate (2:1); (2) 2,4-Diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine sulfate (2:1). CAS-56585-33-2 (1984).

Pharmacologic Category

Urinary Anti-infectives. (ATC-Code: J01EA01).

Mechanism of action

Inhibits folic acid reduction to tetrahydrofolate, and thereby inhibits microbial growth.

Therapeutic use

Treatment of urinary tract infections due to susceptible strains of E. coli, P. mirabilis, K. pneumoniae, Enterobacter sp and coagulase-negative Staphylococcus including S. Saprophyticus. Acute otitis media in children. Acute exacerbations of chronic bronchitis in adults. In combination with other agents for treatment of toxoplasmosis, Pneumocystis carinii. Treatment of superficial ocular infections involving conjunctiva and cornea.

Pregnancy and lactiation implications

As trimethoprim may interfere with folic acid metabolism, consider use only if potential benefit to mother outweighs possible risk to fetus. Enters breast milk (use caution).

Unlabeled use

Contraindications

Hypersensitivity to trimethoprim or any component of the formulation. Megaloblastic anemia due to folate deficiency.

Warnings and precautions

Use with caution in potential folate deficiency (malnourished, chronic anticonvulsant therapy, or elderly). Use with caution in hepatic and renal impairment. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis.

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