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Updated: Jun 16, 2026
02:26
Intracranial Pharmacotherapy and Pain Assays in Rodents
Published on: April 9, 2019
Is tapentadol an advance on tramadol?
1Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA. guayx001@umn.edu
Summary
Tapentadol, a dual-acting pain reliever, offers advantages over tramadol but carries risks like serotonin syndrome and dependence. Further research is needed for chronic pain and elderly populations.
Area of Science:
- Pharmacology and Therapeutics
- Pain Management
Background:
- Tapentadol is a novel analgesic acting as both a mu-opioid receptor agonist and a monoamine reuptake inhibitor.
- It represents the second drug in its class, following tramadol, approved for moderate-to-severe acute pain.
Purpose of the Study:
- To comprehensively review tapentadol's pharmacodynamics, pharmacokinetics, clinical efficacy, and tolerability.
- To compare tapentadol's profile with that of tramadol.
Main Methods:
- Systematic literature search of MEDLINE/PubMed and EMBASE databases (1986-2009).
- Inclusion of relevant meeting abstracts from pain specialty organizations (2000-2008).
- Focus on all papers and abstracts evaluating any aspect of tapentadol.
Main Results:
- Tapentadol hydrochloride (HCl) demonstrates activity in diverse animal and human pain models.
- It exhibits physical and psychological dependence potential similar to morphine and hydromorphone.
- Recommended oral dosage is 50-100 mg every 4-6 hours for acute pain, with no specific elder recommendations.
Conclusions:
- Tapentadol presents an improved profile over tramadol but retains liabilities.
- Potential risks include serotonin syndrome, anticholinergic effects, and opioid-like dependence.
- Gaps exist in data regarding chronic pain efficacy, frail elder populations, and drug-drug interactions.
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