Drug intelligence / Profile preview

pregabalin + tramadol + tricyclic antidepressants

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of pregabalin, tramadol, and tricyclic antidepressants used primarily for the treatment of neuropathic pain. This combination leverages multiple mechanisms of action to provide enhanced pain relief compared to monotherapy. Pregabalin binds to voltage-gated calcium channels, tramadol acts as a μ-opioid receptor agonist and inhibits serotonin/norepinephrine reuptake, while tricyclic antidepressants inhibit serotonin and noradrenaline reuptake. The combination has shown significant efficacy in animal models of neuropathic pain but carries risks of central nervous system depression, serotonin syndrome, and seizures.

02

Targets

NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)MOR (Mu opioid receptor)

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