Lofentanil
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| Other names | Lofentanil; methyl (3S,4R)-1-(2-phenylethyl)-4 -(phenyl-propanoylamino)-3-methylpiperidine-4-carboxylate |
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Lofentanil or lofentanyl is one of the most potent
μ-opioid affinity from increasing much further. As with other 3-substituted fentanyl derivatives such as ohmefentanyl, the stereoisomerism
of lofentanil is very important, with some stereoisomers being much more potent than others.
Lofentanil is very similar to carfentanil in effects, but has a longer duration of action.Moscow hostage crisis.
Side effects of lofentanyl analogs are similar to those of fentanyl itself, which include
respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.[7] Side effects from lofentanil might be particularly problematic given its reportedly long duration of action. Another side effect which is characteristic of fentanyl and its derivatives is their tendency to rapidly induce tolerance, due to their high binding affinity triggering rapid internalization of chronically activated opiate receptors.[8]
This might be expected to be a particular problem with lofentanil as it is not only one of the most potent drugs in the series, but also is longer acting than most other fentanyl analogues, meaning that development of tolerance triggered by receptor over-activation could be rapid.
In addition to acting on the