Drug of the week series 24.4 - Cotrimoxazole

Drug of the week - Cotrimoxazole

Meet this drug of the week’s duo of the pharmacy world - Sulfamethoxazole and Trimethoprim, better known by their ultimate team-name “Cotrimoxazole”

​Keep reading to dive into their background, mechanism of action, clinical uses, side effects, drug interactions and crucial contraindications!

Background

Cotrimoxazole is a fixed dose combination antibiotic composed of trimethoprim and sulphamethoxazole, used to treat a variety of bacterial infections. It consists of one part trimethoprim to five parts sulfamethoxazole. It is sold under the trade names Bactrim, Cotrim and Septra.

Mechanism of action

  • Cotrimoxazole produces the sequential block of bacterial folate metabolism i.e. its components -trimethoprim and sulfamethoxazole interfere with two successive steps in the folate metabolism pathway within bacteria.
  • Trimethoprim and sulphamethoxazole inhibits dihydrofolate reductase and folate synthetase respectively.
  • Blocking the folate metabolism will accelerate nucleotide depletion, resulting in a bactericidal effect (cell death).

Point to note**: Individually, both sulphamethoxazole and trimethoprim are bacteriostatic, but their combination i.e. cotrimoxazole becomes bactericidal against many organisms.**

Clinical uses

  • Treatment of tonsillitis, pharyngitis, sinusitis, otitis media, chronic bronchitis, urinary tract infections and diarrheas.
  • Used as an alternative drug for patients allergic to beta-lactam antibiotics and for chancroid.

Adverse effects

Include nausea, vomiting, stomatitis, headache, folate deficiency (megaloblastic anemia) and in some rare cases blood dyscrasias occur.

Contraindications

  • Pregnancy: Trimethoprim being an antifolate, poses a teratogenic risk. Neonatal hemolysis and methemoglobinemia can occur
  • Renal disease patients: Patients may develop uremia on consuming cotrimoxazole

Drug Interactions

  • Enhances anticoagulant activity of warfarin
  • Prolongs half-life of phenytoin
  • Increases toxicity of methotrexate

Thank you to everyone who participated in this week’s polls and discussions! Looking forward to the next Drug of the Week series.

MBH/PS

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Cotrimoxazole is a classic example of sequential blockade in bacterial folate synthesis

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