Remifentanil Hydrochloride

Ultiva was launched in Germany and the US for use in general anesthesia and immediate post-operative pain management. This compound can be prepared via the Michael addition of a 4,4-disubstituted piperidine to methyl acrylate. It behaves as a specific μ-opiod agonist that is about 30 times more potent than its chemical relative alfentanil. While its pharmacodynamic properties are similar to other μ agonists, remifentanil has unique pharmacokinetic properties. It has a rapid onset (1.6 min) and a rapid offset (5.4 min) independent of duration of administration. This has been attributed to its rapid catabolism by general esterases to the corresponding acrylic acid derivative. The metabolite has 0.01 to 0.0005 times the activity of remifentanil and is excreted via the kidneys (80% recovery).