Drug intelligence / Profile preview

local anesthetics + opioids

Development stage
Unknown
Lead developer
Heron Therapeutics
Modality
Small Molecules
Administration
Epidural, Intrathecal, Perineural
01

Overview

A combination of local anesthetics and opioids is used primarily for regional anesthesia and analgesia, including neuraxial (epidural or spinal) and peripheral nerve block techniques. Local anesthetics act by blocking voltage-gated sodium channels in neuronal membranes, thereby inhibiting the initiation and propagation of nerve impulses responsible for pain sensation. Opioids exert their effects mainly through activation of opioid receptors (primarily mu-opioid receptors) in the central nervous system, leading to inhibition of pain transmission pathways. When combined, these agents provide synergistic analgesic effects—enhancing pain relief while allowing lower doses of each drug to be used, which can reduce side effects associated with higher doses of either agent alone. This multimodal approach is widely employed in perioperative settings for improved intraoperative anesthesia and postoperative pain control[2][4][5][6]. Commonly used local anesthetics include lidocaine, bupivacaine, levobupivacaine; commonly used opioids include morphine, fentanyl, codeine, tramadol.

Other names
local anesthetic and opioid combinationlocal anesthetic plus opioid
02

Targets

MOR (Mu opioid receptor)NaV (Voltage-gated sodium channels)

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