Drug intelligence / Profile preview

morphine + buprenorphine + pethidine + tramadol + metamizole + acetylsalicylic acid

Development stage
Unknown
Lead developer
Reckitt
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous (buprenorphine Depot/injection), Transdermal (buprenorphine Patch)
01

Overview

This is a combination drug containing six active pharmaceutical ingredients, each with distinct mechanisms of action primarily for pain management and anti-inflammatory effects. - **Morphine** is a classic opioid analgesic that acts as a full agonist at the μ-opioid receptor, providing potent pain relief. - **Buprenorphine** is a partial agonist at the μ-opioid receptor and antagonist at κ- and δ-opioid receptors, used for both pain management and opioid dependence therapy[3][7][9]. - **Pethidine (meperidine)** is a synthetic opioid analgesic acting mainly as an agonist at the μ-opioid receptor; it also has serotonergic properties[5][8]. - **Tramadol** is an atypical centrally acting analgesic with dual action as a weak μ-opioid receptor agonist and inhibitor of serotonin/norepinephrine reuptake (SNRI), contributing to its multimodal analgesic effect[1][5]. - **Metamizole (dipyrone)** is a non-opioid analgesic and antipyretic with spasmolytic properties, commonly used in some countries for severe pain or fever unresponsive to other treatments. Its mechanism involves inhibition of prostaglandin synthesis via cyclooxygenase inhibition. - **Acetylsalicylic acid (aspirin)** is an NSAID that irreversibly inhibits cyclooxygenase enzymes COX-1 and COX-2, reducing prostaglandin synthesis responsible for inflammation, pain, and fever. This combination would provide broad-spectrum analgesia through multiple pathways—opioidergic modulation of central nervous system pain signaling; monoaminergic modulation by tramadol; peripheral anti-inflammatory effects from metamizole and aspirin; plus potential antipyretic actions.

02

Targets

DOR (Opioid Receptor Delta 1)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)KOR (Kappa opioid receptor)NOP (Nociceptin/orphanin FQ peptide receptor)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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