Drug intelligence / Profile preview

local anesthetic + tramadol hydrochloride

Development stage
Preclinical
Lead developer
Grünenthal
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Drug Delivery Systems
Administration
Infiltration, Injection, Nerve Block
01

Overview

A combination of a local anesthetic agent and tramadol hydrochloride, typically used in dental or minor surgical procedures to provide both anesthesia and analgesia. Tramadol hydrochloride acts as a centrally acting opioid analgesic with additional mechanisms including inhibition of serotonin and norepinephrine reuptake. When combined with a conventional local anesthetic (such as lidocaine) or vasoconstrictor agents like adrenaline, this formulation can enhance the duration and efficacy of anesthesia while providing postoperative pain relief. The mechanism involves both peripheral nerve blockade by the local anesthetic component and central/peripheral modulation of pain by tramadol through μ-opioid receptor agonism, serotonin reuptake inhibition, norepinephrine reuptake inhibition, sodium channel blockade, NMDA receptor antagonism, among others[2][3][5][7]. This combination is considered particularly useful when standard amide-type or ester-type local anesthetics are contraindicated.

Other names
local anesthetic and tramadol hydrochloridetramadol HCl with local anesthetictramadol-adrenaline combination (if adrenaline is the local anesthetic adjunct)lidocaine + tramadol (when lidocaine is used as the local anesthetic)
02

Targets

DOR (Opioid Receptor Delta 1)NET (Norepinephrine Transporter)M1 (Muscarinic acetylcholine receptor M1)KOR (Kappa opioid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)MOR (Mu opioid receptor)NaV (Voltage-gated sodium channels)SERT (Sodium-dependent serotonin transporter)

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