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CG 5503;tapentadol
Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor that provides analgesia through dual mechanisms.
Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor that provides analgesia through dual mechanisms. Used for Moderate to severe acute pain, Moderate to severe chronic pain.
At a glance
| Generic name | CG 5503;tapentadol |
|---|---|
| Sponsor | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
| Drug class | Opioid analgesic with norepinephrine reuptake inhibition |
| Target | Mu-opioid receptor; norepinephrine transporter |
| Modality | Small molecule |
| Therapeutic area | Pain Management |
| Phase | Phase 3 |
Mechanism of action
Tapentadol binds to mu-opioid receptors in the central nervous system to produce opioid-mediated pain relief, while simultaneously inhibiting the reuptake of norepinephrine, which enhances descending pain inhibitory pathways. This dual mechanism allows for effective analgesia at lower doses compared to pure opioid agonists, potentially reducing opioid-related side effects.
Approved indications
- Moderate to severe acute pain
- Moderate to severe chronic pain
Common side effects
- Nausea
- Dizziness
- Somnolence
- Vomiting
- Constipation
- Headache
Key clinical trials
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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