Drug intelligence / Profile preview

ibuprofen + pregabalin + acetaminophen + tizanidine

Development stage
Phase 4
Lead developer
Henry Ford Health
Modality
Small Molecules
Administration
Oral
01

Overview

This multimodal non-opioid pain management regimen, studied by the Henry Ford Health System, consists of a combination of four medications: ibuprofen, pregabalin, acetaminophen, and tizanidine. Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase enzymes to reduce inflammation and pain. Pregabalin is a gabapentinoid that binds to the alpha-2-delta subunit of voltage-gated calcium channels, modulating the release of excitatory neurotransmitters to treat neuropathic and acute pain. Acetaminophen provides analgesic and antipyretic effects through central mechanisms, while tizanidine acts as a centrally acting alpha-2 adrenergic agonist to reduce muscle spasticity and provide supplemental analgesia. This regimen is being evaluated in Phase 4 clinical trials as an alternative to standard opioid-based analgesia for patients undergoing orthopedic procedures, such as open reduction and internal fixation (ORIF) of clavicle fractures, to mitigate the risks associated with opioid use.

Other names
Nonopioid Pain Control RegimenMultimodal nonopioid regimen
02

Targets

ADRA2A (α2A)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)

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