Acute Porphyria Drug Database

L01BC03 - Tegafur
Not porphyrinogenic
NP

Rationale
No significant CYP-metaboism. No capacity for CYP-induction or irreversible CYP-inhibition. Side effects such as nausea, vomiting and anorexia may be potentially porphyrinogenic through reduction in caloric intake.
Chemical description
Tegafur is considered to be an orally active prodrug of fluorouracil (Chemical name: 5-Fluoro-1-(tetrahydro-2-furyl)uracil).
Therapeutic characteristics
The most common preparation of tegafur, UFT, contains of a mixture of tegafur and uracil in the optimal molar ratio of 1:4. It is used as the first line treatment of colorectal cancer complicated by metasatases. It is given as combination therapy with calciumfolinate. Common adverse reactions of tagafur that can be confused with an acute porphyric attack are nausea, vomiting, abdominal pain, diarrhoea or obstipation, myalgia dorsal pain and arthalgia. Side effects such as nausea, vomiting and anorexia may be potentially porphyrinogenic through reduction in caloric intake.
Metabolism and pharmacokinetics
Conversion of tegafur to 5-fluorouracil takes place via microsomal C-5´oxidation partly mediated by CYP2A6, and via C-2 cytosolic hydrolysis catalyzed by unknown enzymes. The metabolism of 5-fluorouracil formed from tegafur follows the usual metabolic pathway for formation of the naturally occurring pyrimidine uracil. Neither tegafur, uracil nor fluorouracil inhibit cytochroms P450 CYP1A2, 2C9, 2C19, 2D6 or 3A4. See the monograph of fluorouracil for further details.
IPNet drug reports
No.

References

  1. Drug reference publications
  2. Sweetman SC, editor. Martindale: The complete drug reference. Tegafur. Pharmaceutical Press 2009. #1948
  3. Summary of Product Characteristics
  4. Norwegian medicines agency. Summary of Product Characteristics (SPC). UFT. #1947

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