Drug intelligence / Profile preview

fentanyl + tramadol

Development stage
Unknown
Lead developer
Grünenthal
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Epidural, Intrathecal, Intramuscular
01

Overview

Fentanyl + tramadol is a combination of two opioid analgesics used together for the management of moderate to severe pain, particularly in clinical settings such as anesthesia or procedural sedation. Fentanyl is a potent synthetic opioid agonist with high affinity for the μ-opioid receptor, providing rapid and strong analgesia. Tramadol is an atypical centrally acting synthetic opioid that acts as a weak μ-opioid receptor agonist and also inhibits the reuptake of serotonin and norepinephrine, contributing to its analgesic effects through both opioid and monoaminergic pathways. The combination may be used in specific medical procedures (e.g., awake endotracheal intubation) to leverage their complementary mechanisms for effective pain control while aiming to minimize respiratory depression compared to higher doses of single agents. However, co-administration increases the risk of serotonin syndrome due to additive serotonergic effects, as well as other adverse events such as cardiac arrhythmias[2][5]. This combination should only be administered under close medical supervision.

02

Targets

SERT (Sodium-dependent serotonin transporter)MOR (Mu opioid receptor)NET (Norepinephrine Transporter)

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