Drug intelligence / Profile preview

tramadol + pethidine

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

Overview

Tramadol + pethidine is a combination of two synthetic opioid analgesics, each with distinct mechanisms of action, used for the management of moderate to severe pain. Tramadol acts as a centrally acting opioid agonist and also inhibits the reuptake of serotonin and norepinephrine, providing both opioid and monoaminergic analgesic effects[1][5][6]. Pethidine (also known as meperidine) is a strong opioid that primarily acts as an agonist at the μ-opioid receptor to inhibit pain signaling in the central nervous system[8]. While both drugs are effective for acute pain relief, their use together is not standard practice due to overlapping side effect profiles and increased risk of adverse events such as respiratory depression, sedation, constipation, nausea, vomiting, and potential for dependence or addiction. Both agents are prescription-only medications.

02

Targets

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

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