Drug intelligence / Profile preview

Ultracet

Development stage
Phase 4
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

Ultracet (tramadol hydrochloride/acetaminophen) is an immediate-release, fixed-dose combination analgesic containing tramadol hydrochloride (37.5 mg) and acetaminophen (325 mg). Originally developed by Ortho-McNeil and marketed globally by Janssen, this small molecule combination product is indicated for the short-term management of moderate to severe acute pain, including postoperative pain (such as pain following total knee replacement surgery). Tramadol acts as a centrally acting synthetic opioid analgesic with dual mechanisms: it binds weakly to mu-opioid receptors and inhibits the reuptake of serotonin and norepinephrine in the central nervous system. Acetaminophen provides complementary analgesic and antipyretic effects, potentially through the inhibition of cyclooxygenase (COX) enzymes in the central nervous system. The immediate-release formulation is typically administered orally as 2 tablets every 4 to 6 hours as needed, up to a maximum of 8 tablets per day.

Brand names
TramacetTramapapUltracetUltracet Semi
Other names
paracetamol + tramadolparacetamol + tramadol hydrochloridetramadol + paracetamolTramadol HCl/Acetaminophen IRtramadol hydrochloride + acetaminophentramadol hydrochloride/acetaminophentramadol/acetaminophentramadol/paracetamol
02

Targets

MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)

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