What does tienilic acid mean?
Definitions for tienilic acid
tie·nil·ic acid
Here are all the possible meanings and translations of the word tienilic acid.
Wiktionary
tienilic acidnoun
A diuretic drug with uricosuric action, formerly marketed for the treatment of hypertension.
Freebase
Tienilic acid
Tienilic acid or ticrynafen is a loop diuretic drug with uric acid-lowering action, formerly marketed for the treatment of hypertension. It was approved by FDA on May 2, 1979, and withdrawn in 1982, after case reports in the United States indicated a link between the use of ticrynafen and hepatitis. Criminal charges were brought against SmithKline executives with regard to hiding data related to toxicity while gaining FDA approval. The company pleaded guilty to 14 counts of failure to report adverse reactions and 20 counts of selling a misbranded drug. Tienilic acid was found to act as a suicide substrate at the cytochrome P450 enzymes involved in drug metabolism. Unfortunately, the metabolic reaction carried out by these enzymes converted tienilic acid to a thiophene sulfoxide which proved highly electrophilic. This encouraged a Michael reaction leading to alkylation of a thiol group in the enzyme's active site. Loss of water from the thiophene sulfoxide restored the thiophene ring and resulted in tienilic acid being covalently linked to the enzyme, thus inhibiting the enzyme irreversibly. The above explanation is a hypothesis. It is still not known if the reactive intermediate which inactivates the CYP2C9 is the thiophene sulfoxide or the thiophene epoxide. The target on the protein is also not known. However tienilic acid is a good mechanism based inhibitor of CYP2C9 and seems to inactivate it stoichiometrically. Progress in proteomics may one day give the answer.
Numerology
Chaldean Numerology
The numerical value of tienilic acid in Chaldean Numerology is: 5
Pythagorean Numerology
The numerical value of tienilic acid in Pythagorean Numerology is: 8
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"tienilic acid." Definitions.net. STANDS4 LLC, 2021. Web. 24 Jul 2021. <https://www.definitions.net/definition/tienilic+acid>.
