How is dipyrone metabolized in peripheral tissue, and what is the significance of this metabolism in its analgesic effect?

Label:chem

Topic
Dipyrone is a prodrug that undergoes hydrolysis to form 4-methylaminoantipyrine (4-MAA) and further metabolites. The study investigates whether dipyrone is hydrolyzed locally in peripheral tissue and if this metabolism is crucial for its analgesic effect.

From: "Dipyrone is locally hydrolyzed to 4-methylaminoantipyrine and its antihyperalgesic effect depends on CB2 and kappa-opioid receptors activation", European Journal of Pharmacology, Volume 874, 5 May 2020, 173005
Answer
Dipyrone is completely hydrolyzed to 4-MAA in the peripheral tissue, as confirmed by mass spectrometry. This local hydrolysis is significant because 4-MAA is the active metabolite responsible for the analgesic effect of dipyrone, suggesting that the local metabolism of dipyrone to 4-MAA is essential for its pain-relieving properties.
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