Sufentanil

Mechanism of action:
Sufentanil is an opioid and a synthetic mu-opioid receptor agonist (synthetic mu-opioid receptor agonist). Sufentanil activates mu-opioid receptors in the central and peripheral nervous systems. Through Gi/o proteins, it inhibits adenylyl cyclase, reduces cAMP production, and thereby suppresses presynaptic voltage-gated Ca2+ channels, preventing calcium ions from entering the cell. This reduces the release of pain-related neurotransmitters such as glutamate and substance P and decreases transmission of pain signals. In addition, it activates postsynaptic potassium channels, causing membrane hyperpolarization and reducing the probability of neuronal firing.
Reference(s):
1. Miner JR et al. (2018). Sufentanil sublingual tablet 30mcg for moderate-to-severe acute pain in the ED. Am J Emerg Med.
2. Willsie SK et al. (2015). Pharmacokinetic properties of single- and repeated-dose sufentanil sublingual tablets in healthy volunteers. Clin Ther.
