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Mechanistic and functional differentiation of tapentadol and tramadol.
Expert Opin Pharmacother. 2012 Jul; 13(10):1437-49.EO

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.

Authors+Show Affiliations

Temple University School of Pharmacy, Department of Pharmaceutical Sciences, Philadelphia, PA, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

22698264

Citation

Raffa, Robert B., et al. "Mechanistic and Functional Differentiation of Tapentadol and Tramadol." Expert Opinion On Pharmacotherapy, vol. 13, no. 10, 2012, pp. 1437-49.
Raffa RB, Buschmann H, Christoph T, et al. Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012;13(10):1437-49.
Raffa, R. B., Buschmann, H., Christoph, T., Eichenbaum, G., Englberger, W., Flores, C. M., Hertrampf, T., Kögel, B., Schiene, K., Straβburger, W., Terlinden, R., & Tzschentke, T. M. (2012). Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opinion On Pharmacotherapy, 13(10), 1437-49. https://doi.org/10.1517/14656566.2012.696097
Raffa RB, et al. Mechanistic and Functional Differentiation of Tapentadol and Tramadol. Expert Opin Pharmacother. 2012;13(10):1437-49. PubMed PMID: 22698264.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Mechanistic and functional differentiation of tapentadol and tramadol. AU - Raffa,Robert B, AU - Buschmann,Helmut, AU - Christoph,Thomas, AU - Eichenbaum,Gary, AU - Englberger,Werner, AU - Flores,Christopher M, AU - Hertrampf,Torsten, AU - Kögel,Babette, AU - Schiene,Klaus, AU - Straβburger,Wolfgang, AU - Terlinden,Rolf, AU - Tzschentke,Thomas M, Y1 - 2012/06/15/ PY - 2012/6/16/entrez PY - 2012/6/16/pubmed PY - 2012/12/10/medline SP - 1437 EP - 49 JF - Expert opinion on pharmacotherapy JO - Expert Opin Pharmacother VL - 13 IS - 10 N2 - 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. SN - 1744-7666 UR - https://www.unboundmedicine.com/medline/citation/22698264/Mechanistic_and_functional_differentiation_of_tapentadol_and_tramadol_ L2 - http://www.tandfonline.com/doi/full/10.1517/14656566.2012.696097 DB - PRIME DP - Unbound Medicine ER -