Tapentadol: Use and Abuse

Tapentadol – Use and Abuse

  • CV Juvin Thomas Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India
  • R Sambathkumar Department of Pharmaceutics, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India https://orcid.org/0000-0003-1454-9582
  • N Venkateswaramurthy Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India https://orcid.org/0000-0002-8623-7898

Abstract

Tapentadol is a synthetic opioid analgesic that has been on the market in India since 2011. According to international studies, there is a low danger of abuse and diversion. Prescription opioid pain reliever abuse remains a major public health concern. Tapentadol, a prescription painkiller, differs from opioids such as oxycodone and morphine in that it has two modes of action: opioid receptor agonism and norepinephrine reuptake inhibition. Tapentadol has been on the market in India for eight and a half years. Our center was the topic of a single peer-reviewed research in 2017 that detailed two instances of abuse. Tapentadol is less likely to be diverted, abused, addicted, overdosed, or sold on the street than other prescribed opioids. This article reviews uses, pharmacological properties and abuse of tapentadol as it is the most serious issues like addiction, seeking behavior, withdrawal, and physical dependency .The main challenge with tapentadol use is controlling the ratio of MOR agonist to NRI. Finally, tapentadol provides both nociceptive and neuropathic pain relief, but there are concerns about abuse and reliance.


Keywords: Tapentadol, Abuse, Opioid, Addiction.

Keywords: Tapentadol, Abuse, Opioid, Addiction

Downloads

Download data is not yet available.

Author Biographies

CV Juvin Thomas, Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

R Sambathkumar, Department of Pharmaceutics, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

Department of Pharmaceutics, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

N Venkateswaramurthy, Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

Department of Pharmacy Practice, J.K.K. Nattraja College of Pharmacy, Kumarapalayam-638183, Tamil Nadu, India

References

1. Tzschentke TM, Christoph T, Kogel BY. The muopioid receptor agonist/noradrenaline reuptake inhibition (MOR-NRI) concept in analgesia: The case of tapentadol. CNS Drugs 2014; 28(4):319-29. https://doi.org/10.1007/s40263-014-0151-9
2. Tzschentke TM, Jahnel U, Kogel B, Christoph T, Englberger W, De Vry J. Tapentadol hydrochloride: A next-generation, centrally acting analgesic with two mechanisms of action in a single molecule. Drugs Today 2009; 45(7):483-96. https://doi.org/10.1358/dot.2009.45.7.1395291
3. Raffa RB, Elling C, Tzschentke TM. Does 'strong analgesic' equal 'strong opioid'? Tapentadol and the concept of 'micro-load'. AdvTher 2018; 35 (10):1471-84. https://doi.org/10.1007/s12325-018-0778-x
4. Stollenwerk A, Sohns M, Heisig F, Elling C, von Zabern D. Review of post-marketing safety data on tapentadol, a centrally acting analgesic. AdvTher 2018; 35(1):12-30 https://doi.org/10.1007/s12325-017-0654-0
5. Hartrick CT, Rozek RJ. Tapentadol in pain management: A mu-opioid receptor agonist and noradrenaline reuptake inhibitor. CNS Drugs 2011; 25(5):359-70. https://doi.org/10.2165/11589080-000000000-00000
6. Murphy DL, Lebin JA, Severtson SG, Olsen HA, Dasgupta N, Dart RC. Comparative rates of mortality and serious adverse effects among commonly prescribed opioid analgesics. Drug Saf 2018; 41 (8):787-95. https://doi.org/10.1007/s40264-018-0660-4
7. Kress HG. Tapentadol and its two mechanisms of action: is there a new pharmacological class of centrally-acting analgesics on the horizon? Eur J Pain 2010; 14:781 https://doi.org/10.1016/j.ejpain.2010.06.017
8. Torres-Sanchez S, Borges GDS, Mico JA, Berrocoso E. Opioid and noradrenergic contributions of tapentadol to the inhibition of locus coeruleus neurons in the streptozotocin rat model of polyneuropathic pain. Neuropharmacology. 2018; 135:202-210. https://doi.org/10.1016/j.neuropharm.2018.03.014
9. Walczyk H, Liu CH, Alafris A, Cohen H. Probable tapentadol-associated serotonin syndrome after overdose. Hosp Pharm. 2016; 51(4):320-327. https://doi.org/10.1310/hpj5104-320
10. Barkin RL, Barkin SJ. Treating postoperative pain in the patient who is in recovery or remission from opioid abuse: focus on tapentadol. J Opioid Manag. 2017;13(3):133-134. https://doi.org/10.5055/jom.2017.0378
11. Terlinden R, Ossig J, Fliegert F C et al. Absorption, metabolism, and excretion of 14C-labeled tapentadolHCl in healthy male subjects. Eur J Drug MetabPharmacokinet, 2007; 32(3):163-69. https://doi.org/10.1007/BF03190478
12. Terlinden R, Kogel BY, Englberger W, Tzschentke TM: In vitro and in vivo characterization of tapentadol metabolites. Methods Find ExpClinPharmacol, 2010; 32(1):31-38 https://doi.org/10.1358/mf.2010.32.1.1434165
13. Vadivelu N, Huang Y, Mirante B et al: Patient considerations in the use of tapentadol for moderate to severe pain. Drug, Healthc Patient Saf, 2013; 5:151-59. https://doi.org/10.2147/DHPS.S28829
14. Langford RM, Knaggs R, Farquhar-Smith P, Dickenson AH: Is tapentadol different from classical opioids? A review of the evidence. Br J Pain, 2016; 10(4):217-21 https://doi.org/10.1177/2049463716657363
15. Kress HG, Ahlbeck K, Aldington D, et al. Managing chronic pain in elderly patients requires a CHANGE of approach. Curr Med Res Opin. 2014; 30:1153-1164. https://doi.org/10.1185/03007995.2014.887005
16. Kress HG, Koch ED, Kosturski H, et al. Tapentadol prolongedrelease for managing moderate to severe, chronic malignanttumor-related pain. Pain Physician. 2014; 17:329- https://doi.org/10.36076/ppj.2014/17/329
17. Pergolizzi J, Alon E, Baron R, et al. Tapentadol in the managementof chronic low back pain: a novel approach to a complexcondition? J Pain Res. 2011; 4:203-210. https://doi.org/10.2147/JPR.S19625
18. Steigerwald I, Müller M, Davies A, et al. Effectiveness and safetyof tapentadol prolonged release for severe, chronic low back painwith or without a neuropathic pain component: results of anopen-label, phase 3b study. Curr Med Res Opin.2012; 28:911-936. https://doi.org/10.1185/03007995.2012.679254
19. Baron R, Eberhart L, Kern KU, et al. Tapentadol prolonged releasefor chronic pain: a review of clinical trials and 5 years of routineclinical practice data. Pain Pract. 2017; 17:678-700. https://doi.org/10.1111/papr.12515
20. Horgas AL. Pain management in older adults. NursClin North Am.2017; 52:e1-e7. https://doi.org/10.1016/j.cnur.2017.08.001
21. Available from: http://www.nucynta.com (accessed on11.01.2013).
22. Tzschentke TM, Christoph T, Kögel B, et al. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (TapentadolHCl): a novel μ-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J PharmacolExpTher. 2007; 323(1):265-76. https://doi.org/10.1124/jpet.107.126052
23. Schröder W, Tzschentke TM, Terlinden R, et al. Synergistic interaction between the two mechanisms of action of tapentadol in analgesia. J PharmacolExpTher. 2011; 337(1):312-20. https://doi.org/10.1124/jpet.110.175042
24. Schröder W, Vry JD, Tzschentke TM, et al. Diferential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Eur J Pain. 2010; 14(8):814-21. https://doi.org/10.1016/j.ejpain.2010.05.005
25. Grunenthal Ltd. Palexia SR prolonged release tablets: summary of product characteristics. 2017. https://www.medicines.org.uk/. Accessed 30 Oct 2018.
26. Gohler K, Brett M, Smit JW, et al. Comparative pharmacokinetics and bioavailability of tapentadol following oral administration of immediate- and prolonged-release formulations. Int J ClinPharmacolTher. 2013; 51(4):338-48. https://doi.org/10.5414/CP201722
27. Huntjens DR, Liefaard LC, Nandy P, et al. Population pharmacokinetic modeling of tapentadol extended release (ER) in healthy subjects and patients with moderate or severe chronic pain. Clin Drug Investig. 2016; 36(3):213-23. https://doi.org/10.1007/s40261-015-0371-x
28. Mick G, Serpell A, Makin AH. Acute pain physiology and pharmacological targets: the present and future. Acute pain1998; 3:31-7. https://doi.org/10.1016/S1366-0071(98)80018-1
29. Treede RD, Jensen TS, Campbell JN, Cruccu G, Dostrovsky JO,Griffin JW, et al. Neuropathic pain: redefinition and a gradingsystem for clinical and research purposes. Neurology2008; 70(18):1630-5. https://doi.org/10.1212/01.wnl.0000282763.29778.59
30. Paice JA. Mechanisms and management of neuropathic pain incancer. J Support Oncol 2003; 1(2):107-20. PMID: 15352654
31. Liu KKC, Sakya SM, O'Donnell CJ, Flick AC, Li J. Syntheticapproaches to the 2009 new drugs. Bioorg Med Chem2011; 19(3):1136-54. https://doi.org/10.1016/j.bmc.2010.12.038
32. Available from: (accessed26.12.12).
33. Cagnardi P, Villa R, Zonca A, Gallo M, Beccaglia M, Luvoni GC,et al. Pharmacokinetics, intraoperative effect and postoperativeanalgesia of tramadol in cats. Res Vet Sci 2011; 90:503-9. https://doi.org/10.1016/j.rvsc.2010.07.015
34. Babette K, Jean DV, Thomas MT, Thomas C. The antinociceptiveand antihyperalgesic effect of tapentadol is partially retained inOPRM1 ((-opioid receptor) knockout mice. NeurosciLett2011; 491:104-7. https://doi.org/10.1016/j.neulet.2011.01.014
35. Schneider J, Jahnel U, Linz K. Neutral effects of the novelanalgesic tapentadol on cardiac repolarization due to mixed ionchannel inhibitory activities. Drug Dev Res 2010; 71:197-208. https://doi.org/10.1002/ddr.20360
36. Tayal G, Grewal A, Mittal R, Bhatia N. Tapentadol- a novelanalgesic. J AnaesthClinPharmacol 2009; 25(4):463-6. https://doi.org/10.1016/j.bfopcu.2013.04.003
37. Australian Public Assessment Report for Tapentadol. Therapeuticgoods administration, Department of health and ageing, Australian government, Feb 2011.
38. BioCSL. Palexia Product Information. 2012. https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/PICMI?OpenForm&t=pi&q=Tapentadol (accessed 15 December 2013).
39. Raffa RB, Buschmann H, Christoph T, et al. Mechanistic and functional differentiation of tapentadol and tramadol. Expert opinion on pharmacotherapy 2012; 13:1437-49. [PubMed]. https://doi.org/10.1517/14656566.2012.696097
40. McNaughton EC, Black RA, Weber SE, Butler SF. Assessing abuse potential of new analgesic medications following market release: an evaluation of Internet discussion of tapentadol abuse. Pain Med. 2015; 16(1):131-140. https://doi.org/10.1111/pme.12547
41. Basu, A., Mahadevan, J., Ithal, D., Selvaraj, S., Chand, P., Murthy, P. Is tapentadol a potential Trojan horse in the postdextropropoxyphene era in India? Indian J. Pharmacol. 2018; 50(1):44. https://doi.org/10.4103/ijp.IJP_21_17
42. Indian Pharmacopoeia Commission, 2019. Pharmacovigilance Program of India Updates. [cited 30.08.19]; Available at:. https://www.ipc.gov.in/mandates/pvpi/pvpiupdates/8-category-en/416-drug-safety-alerts.html.
43. Faria J, Barbosa J, Moreira R, Queirós O, Carvalho F, Dinis-Oliveira RJ. Comparative pharmacology and toxicology of tramadol and tapentadol. Eur J Pain. 2018; 22(5):827-844. https://doi.org/10.1002/ejp.1196
44. Compton WM, Jones CM, Baldwin GT. Relationship between nonmedical prescription-opioid use and heroin use. N Engl J Med. 2016; 374(2):154-163. https://doi.org/10.1056/NEJMra1508490
45. Garland EL, Froeliger B, Zeidan F, et al. The downward spiral of chronic pain, prescription opioid misuse, and addiction: cognitive, affective, and neuropsychopharmacologic pathways. NeurosciBiobehav Rev. 2013; 37(10 Pt 2):2597-2607. https://doi.org/10.1016/j.neubiorev.2013.08.006
46. IOM Committee on Advancing Pain Research Care and Education. Relieving Pain in America: A Blueprint for Transforming Prevention, Care, Education, and Research. Washington, DC: The National Academies Press; 2011.
47. Scholten W, Henningfield JE. Negative outcomes of unbalanced opioid policy supported by clinicians, politicians, and the media. J Pain Palliat Care Pharmacother. 2016; 30(1):4-12. https://doi.org/10.3109/15360288.2015.1136368
48. Han B, Compton WM, Blanco C, et al. Prescription opioid use, misuse, and use disorders in U.S. adults: 2015 National Survey on Drug Use and Health. Ann Intern Med. 2017; 167(5):293-301. https://doi.org/10.7326/M17-0865
49. McCabe SE, West BT, Boyd CJ. Motives for medical misuse of prescription opioids among adolescents. J Pain. 2013; 14(10):1208-1216. https://doi.org/10.1016/j.jpain.2013.05.004
50. HHS. HHS Guide for Clinicians on the Appropriate Dosage Reduction or Discontinuation of Long-Term Opioid Analgesics. Washington, DC: US Department of Health and Human Services; 2019.
51. Pergolizzi JV, Jr., LeQuang JA, Taylor R, Jr., et al. Designing safer analgesics: a focus on mu-opioid receptor pathways. Expert Opin Drug Discov. 2018; 13(10):965-972. https://doi.org/10.1080/17460441.2018.1511539
52. Drewes AM, Jensen RD, Nielsen LM, et al. Differences between opioids: pharmacological, experimental, clinical and economical perspectives. Br J ClinPharmacol. 2013; 75(1):60-78. https://doi.org/10.1111/j.1365-2125.2012.04317.x
53. Caputi FF, Nicora M, Simeone R, et al. Tapentadol: an analgesic that differs from classic opioids due to its noradrenergic mechanism of action. Minerva Med. 2019; 110(1):62-78. https://doi.org/10.23736/S0026-4806.18.05909-8
54. Nucynta (tapentadol) tablets for oral use C-II [package insert]. Stoughton, MA: Collegium Pharmaceutical, Inc.; 2018.
55. Nucynta ER (tapentadol) extended-release oral tablets C-II [package insert]. Stoughton, MA: Collegium Pharmaceutical, Inc.; 2018.
56. McAnally H. Rationale for and approach to preoperative opioid weaning: a preoperative optimization protocol. Perioper Med (Lond). 2017; 6:19.
57. Fudin J, Raouf M, Wegrzyn EL. Opioid Dosing Policy: Pharmacological Considerations Regarding Equianalgesic Dosing. Lenexa, KS: AIPM; 2017.
58. Smith HS. Opioid metabolism. Mayo Clin Proc. 2009; 84(7):613-624. https://doi.org/10.1016/S0025-6196(11)60750-7
59. Pergolizzi JV, Jr, Taylor R, Jr, et al. Tapentadol extended release in the treatment of severe chronic low back pain and osteoarthritis pain. Pain Ther. 2018; 7(1):37-57. https://doi.org/10.1007/s40122-018-0095-8
Statistics
45 Views | 3 Downloads
How to Cite
1.
Juvin Thomas C, Sambathkumar R, Venkateswaramurthy N. Tapentadol: Use and Abuse. JDDT [Internet]. 15Nov.2021 [cited 1Dec.2021];11(6):238-43. Available from: https://jddtonline.info/index.php/jddt/article/view/5139