Drug intelligence / Profile preview

tramadol hydrochloride + acetaminophen

Development stage
Approved
Lead developer
OMJ Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tramadol hydrochloride + acetaminophen is a fixed-dose oral combination of two analgesics used for the short-term management (up to 5 days) of acute pain severe enough to require an opioid and when alternative treatments are inadequate. Tramadol is a centrally acting synthetic opioid analgesic that relieves pain primarily by binding to µ-opioid receptor and weakly inhibiting the reuptake of norepinephrine and serotonin in the central nervous system. Acetaminophen is a non-opioid analgesic and antipyretic that reduces pain and fever through inhibition of prostaglandin synthesis in the central nervous system. The combination provides better pain relief than either drug alone at lower doses. Tramadol carries risks typical of opioids including dependence and abuse potential; acetaminophen overdose can cause severe hepatotoxicity. This product is available only under restricted distribution programs due to its risk profile[1][3][4][5][8]. **Developers**: Janssen

Brand names
UltracetACT-traMADol/ACETAG-ACET-traMADolAPO-traMADol/ACETAuro-traMADol/AcetaminophenIPG-traMADol/ACETJAMP-ACET-traMADolLupin-traMADol/ACETMAR-traMADol/ACETMINT-traMADol/ACETMYLAN-traMADol/ACETNRA-traMADol/ACETPAT-traMADol/ACET
Other names
tramadol and acetaminophen
02

Targets

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

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