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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Raffa, Robert B. Buschmann, Helmut Christoph, Thomas Eichenbaum, Gary Englberger, Werner Flores, Christopher M. Hertrampf, Torsten Kögel, Babette Schiene, Klaus Straßburger, Wolfgang Terlinden, Rolf Tzschentke, Thomas M. |
| Description | Country affiliation: United States Author Affiliation: Raffa RB ( Temple University School of Pharmacy, Department of Pharmaceutical Sciences, Philadelphia, PA, USA.) |
| Abstract | INTRODUCTION: Many opioid analgesics share common structural elements; however, minor differences in structure can result in major differences in pharmacological activity, pharmacokinetic profile, and clinical efficacy and tolerability. AREAS COVERED: This review compares and contrasts the chemistry, pharmacodynamics, pharmacokinetics, and CNS 'functional activity' of tapentadol and tramadol, responsible for their individual clinical utilities. EXPERT OPINION: The distinct properties of tapentadol and tramadol generate different CNS functional activities, making each drug the prototype of different classes of opioid/nonopioid analgesics. Tramadol's analgesia derives from relatively weak µ-opioid receptor (MOR) agonism, plus norepinephrine and serotonin reuptake inhibition, provided collectively by the enantiomers of the parent drug and a metabolite that is a stronger MOR agonist, but has lower CNS penetration. Tapentadol's MOR agonist activity is several-fold greater than tramadol's, with prominent norepinephrine reuptake inhibition and minimal serotonin effect. Accordingly, tramadol is well-suited for pain conditions for which a strong opioid component is not needed-and it has the benefit of a low abuse potential; whereas tapentadol, a schedule-II controlled substance, is well-suited for pain conditions requiring a strong opioid component-and it has the benefit of greater gastrointestinal tolerability compared to classical strong opioids. Both drugs offer distinct and complementary clinical options. |
| File Format | HTM / HTML |
| ISSN | 14656566 |
| Issue Number | 10 |
| Volume Number | 13 |
| e-ISSN | 17447666 |
| Journal | Expert Opinion on Pharmacotherapy |
| Language | English |
| Publisher | Taylor & Francis |
| Publisher Date | 2012-07-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Analgesics, Opioid Pharmacology Phenols Tramadol Chemistry Therapeutic Use Animals Humans Pain Drug Therapy Receptors, Opioid, Mu Agonists Journal Article Review |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology Pharmacology (medical) |
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