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Chemical Compound Review

Nitrofenac     4-nitrooxybutyl 2-[2-[(2,6...

Synonyms: SureCN3332430, AC1L31XR, 154766-10-6, 156661-01-7
 
 
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Disease relevance of Nitrofenac

  • The present study was performed in order to determine if this derivative of diclofenac, called nitrofenac, would also have less toxicity in the small and large intestine when administered repeatedly over a 1-2 week period [1].
  • No deaths were observed in the rats treated with nitrofenac, and the only small intestinal abnormality observed was diffuse hyperemia [1].
  • The lack of the gastric ulcers in rats treated with nitrofenac could be due to the absorption of the drug as an inactive inhibitor of PG synthesis and/or to the fact that probably nitric oxide is released in the intestine and plays an important protective role in maintaining the tissue integrity [2].
 

High impact information on Nitrofenac

  • An accurate and sensitive HPLC method has been developed for the determination of nitrofenac, a new, original diclofenac derivate showing a good tolerability and a wide anti-inflammatory profile, diclofenac, and its metabolites in plasma [3].
  • The drugs were eluted from a 5 microns LC-8 column with a mobile phase consisting of acetonitrile/water (50/50 v/v) adjusted to pH 3.3 with glacial acetic acid, at a flow rate of 2 mL/min with UV detection at 280 nm for diclofenac and 275 nm for nitrofenac [3].
  • No damage was observed in the stomach or small intestine of rabbits receiving nitrofenac [4].
  • None of the doses of nitrofenac significantly augmented colonic injury or granulocyte infiltration (measured by myeloperoxidase activity) [1].
 

Analytical, diagnostic and therapeutic context of Nitrofenac

  • Plasma concentrations and pharmacokinetic parameters of nitrofenac using a simple and sensitive HPLC method [3].
  • This method has been applied to evaluate the pharmacokinetic parameters of the drugs, using a noncompartmental model, after the oral administration of 5 mg/kg nitrofenac to rats [3].

References

  1. Markedly reduced intestinal toxicity of a diclofenac derivative. Reuter, B.K., Cirino, G., Wallace, J.L. Life Sci. (1994) [Pubmed]
  2. Acute anti-inflammatory activity and gastrointestinal tolerability of diclofenac and nitrofenac. Conforti, A., Donini, M., Brocco, G., Del Soldato, P., Benoni, G., Cuzzolin, L. Agents Actions (1993) [Pubmed]
  3. Plasma concentrations and pharmacokinetic parameters of nitrofenac using a simple and sensitive HPLC method. Benoni, G., Terzi, M., Adami, A., Grigolini, L., Del Soldato, P., Cuzzolin, L. Journal of pharmaceutical sciences. (1995) [Pubmed]
  4. A diclofenac derivative without ulcerogenic properties. Wallace, J.L., Reuter, B., Cicala, C., McKnight, W., Grisham, M., Cirino, G. Eur. J. Pharmacol. (1994) [Pubmed]
 
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