Tapentadol – nowy opioid o unikalnym, podwójnym mechanizmie działania i szerokich możliwościach zastosowania Artykuł przeglądowy
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Opublikowane:
cze 30, 2025
Słowa kluczowe:
agonista receptora opioidowego mi, MOR, inhibitor wychwytu zwrotnego noradrenaliny, leczenie bólu, synergizm, tapentadol
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Abstrakt
Tapentadol jest nowym lekiem zaliczanym do silnych opioidów, przedstawicielem nowej klasy działających ośrodkowo leków przeciwbólowych określanej jako MOR-NRI. Ma on unikalny, podwójny mechanizm działania: jest agonistą receptora opioidowego μ (MOR) oraz inhibitorem wychwytu zwrotnego noradrenaliny (NRI). Lek ten mimo 50-krotnie niższego powinowactwa do receptora opioidowego μ niż morfina wywiera jedynie 3-krotnie słabsze niż morfina działanie analgetyczne, co jest następstwem synergizmu jego 2 mechanizmów działania. Uważa się, że noradrenergiczny mechanizm działania tapentadolu w znaczącym stopniu odpowiada za jego skuteczność w uśmierzaniu różnych zespołów bólu neuropatycznego, natomiast działanie na receptory opioidowe μ – za uśmierzanie bólu nocyceptywnego. W wielu badaniach klinicznych potwierdzono dobry efekt analgetyczny tapentadolu w leczeniu ostrego bólu pooperacyjnego oraz wielu zespołów bólu przewlekłego, w tym bólu w przebiegu choroby zwyrodnieniowej stawów, zespołu bólowego kręgosłupa (z komponentem neuropatycznym lub bez niego) oraz bólu neuropatycznego. Dostępne badania i codzienna praktyka kliniczna potwierdzają także skuteczność i bezpieczeństwo tapentadolu w leczeniu bólu o dużym natężeniu u chorych na nowotwory.
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Jak cytować
Zajączkowska, R. (2025). Tapentadol – nowy opioid o unikalnym, podwójnym mechanizmie działania i szerokich możliwościach zastosowania . Medycyna Faktów , 18(2(67), 253-259. https://doi.org/10.24292/01.MF.0225.13
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Bibliografia
1. Raffa RB, Buschmann H, Christoph T et al. Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012; 13(10): 1437-49.
2. Gressler LE, Hammond DA, Painter JT. Serotonin syndrome in tapentadol literature: systematic review of original research. J Pain Palliat Care Pharmacother. 2017; 31(3-4): 228-36.
3. Tzschentke TM, De Vry J, Terlinden R et al. Tapentadol hydrochloride. Drugs Fut. 2006; 31: 1053-61.
4. Zajączkowska R, Przewłocka B, Kocot-Kępska M et al. Tapentadol – A representative of a new class of MOR-NRI analgesics. Pharmacol Rep. 2018; 70(4): 812-20.
5. Tzschentke TM, Christoph T, Kögel B et al. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007; 323(1): 265-76.
6. Kögel B, De Vry J, Tzschentke TM et al. The antinociceptive and antihyperalgesic effect of tapentadol is partially retained in OPRM1 (μ-opioid receptor) knockout mice. Neurosci Lett. 2011; 491(2): 104-7.
7. Schroder W, De Vry JD, Tzschentke TM et al. Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Eur J Pain. 2010; 14(8): 814-21.
8. Palexia SR (tapentadol) prolonged-release oral tablets [summary of product characteristics]. Buckinghamshire, UK, Grunenthal Ltd., 2011.
9. Zajączkowska R, Kocot-Kępska M, Dobrogowski J et al. Tapentadol – stan wiedzy 2017. Terapia. 2017; 8: 1-8.
10. Etropolski M, Kuperwasser, B., Flügel, M. et al. Safety and tolerability of tapentadol extended release in moderate to severe chronic osteoarthritis or low back pain management: Pooled analysis of randomized controlled trials. Adv Ther. 2014; 31: 604-20.
11. Wild JE, Grond S, Kuperwasser B, Flügel M et al. Longterm safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Pain Pract. 2010; 10(5): 416-27.
12. van der Schrier R, Jonkman K, van Velzen M et al. An experimental study comparing the respiratory effects of tapentadol and oxycodone in healthy volunteers. Br J Anaesth. 2017; 119(6): 1169-77.
13. Webster L, Rauck RL. Atypical opioids and their effect on respiratory drive. J Opioid Manag. 2021; 17(7): 109-18.
14. Biondi D, Xiang J, Etropolski M et al. A post hoc pooled data analysis to evaluate blood pressure (BP) and heart rate (HR) measurements in patients with a current or prior history of hypertension who received tapentadol ER, oxycodone CR, or placebo in chronic pain studies. J Pain. 2011; 12(4 Suppl): P55.
15. Oh C, Rengelshausen J, Mangold B et al. A thorough Qt/QTc study of multiple doses of tapentadol immediate release in healthy subjects. Int J Clin Pharmacol Ther. 2010; 48(10): 678-87.
16. Eichenbaum G, Gohler K, Etropolski M et al. Does tapentadol affect sex hormone concentrations differently from morphine and oxycodone? An initial assessment and possible implications for opioid-induced androgen deficiency. J Opioid Manag. 2015; 11(3): 211-27.
17. Coluzzi F, Pergolizzi J, Raffa RB et al. The unsolved case of bone-impairing analgesics: the endocrine effects of opioids on bone metabolism. Ther Clin Risk Manag. 2015; 11: 515-23.
18. Hartrick CT, Rozek RJ. Tapentadol in pain management. CNS Drugs. 2011; 25(5): 359-70.
19. Pergolizzi J, Alegre C, Blake D et al. Current considerations for the treatment of severe chronic pain: the potential for tapentadol. Pain Practice. 2012; 12(4): 290-306.
20. Franchi S, Moschetti G, Amodeo G et al. Do All Opioid Drugs Share the Same Immunomodulatory Properties? A Review From Animal and Human Studies. Front Immunol. 2019; 10: 2914.
21. Kneip C, Terlinden R, Beier H et al. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Letters. 2008; 2: 67-75.
22. Mangold B, Oh C, Jaeger D et al. The pharmacokinetics of tapentadol are not affected by omeprazole: results of a 2-way crossover drug-interaction study in healthy subjects. Pain Pract. 2007; 7(Suppl 1): 55-7.
23. Smit JW, Oh C, Rengelshausen J et al. Effects of acetaminophen, naproxen and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010; 30(1): 25-34.
24. Charakterystyka produktu leczniczego Palexia retard.
25. Charakterystyka produktu leczniczego Palexia.
26. Charakterystyka produktu leczniczego Palexia roztwór doustny 4 mg/ml.
27. Charakterystyka produktu leczniczego Palexia roztwór doustny 20 mg/ml.
28. Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009; 31(12): 2804-18.
29. Kern KU, Sohns M, Heckes B et al. Tapentadol prolonged release for severe chronic osteoarthritis pain in the elderly: improvements in daily functioning and quality of life. Pain Manag. 2020; 10(2): 85-95.
30. Freo U, Furnari M, Ambrosio F et al. Efficacy and tolerability of tapentadol for the treatment of chronic low back pain in elderly patients. Aging Clin Exp Res. 2021; 33(4): 973-82.
31. Schwittay A, Sohns M, Heckes B et al. Tapentadol Prolonged Release for Severe Chronic Osteoarthritis Pain in the Elderly-A Subgroup Analysis of Routine Clinical Practice Data. Pain Res Manag. 2020; 2020: 5759265.
32. Pierce DM, Shipstone E. Pharmacology Update: Tapentadol for neuropathic pain. Am J Hosp Palliat Med. 2012; 29(8): 663-66.
33. Steigerwald I, Schenk M, Lahne U et al. Effectiveness and Tolerability of Tapentadol Prolonged Release Compared With Prior Opioid Therapy for the Management of Severe, Chronic Osteoarthritis Pain. Clin Drug Investig. 2013; 33: 607-19.
34. Davis MP, Davis A, McPherson ML et al. Opioid conversion in adults with cancer: MASCC‑ASCO‑AAHPM‑HPNA‑NICSO guideline. Supportive Care in Cancer. 2025; 33: 243.
35. Sanchez M, Shenk M, Kern KU et al. Practical Considerations for the Use of Tapentadol Prolonged Release for the Management of Severe Chronic Pain. Clin Ther. 2015; 27(1): 94-113.
36. Viscusi ER, Allard R, Sohns M et al. Tapentadol immediate release for moderate to severe acute post-surgery pain. J Opioid Manag. 2019; 15: 51-67.
37. Baron R, Jansen JP, Binder A et al. Tolerability, Safety, and Quality of Life with Tapentadol Prolonged Release (PR) Compared with Oxycodone/Naloxone PR in Patients with Severe Chronic Low Back Pain with a Neuropathic Component: A Randomized, Controlled, Open-label, Phase 3b/4 Trial. Pain Pract. 2016; 16(5): 600-19.
38. Kress HG, Koch ED, Kosturski H et al. Tapentadol prolonged release for managing moderate to severe, chronic malignant tumor-related pain. Pain Physician. 2014; 17: 329-43.
39. Mercadante S, Porzio G, Ferrera P et al. Tapentadol in cancer pain management: a prospective, open-label study. Curr Med Res Op. 2012; 28(11): 1775-9.
2. Gressler LE, Hammond DA, Painter JT. Serotonin syndrome in tapentadol literature: systematic review of original research. J Pain Palliat Care Pharmacother. 2017; 31(3-4): 228-36.
3. Tzschentke TM, De Vry J, Terlinden R et al. Tapentadol hydrochloride. Drugs Fut. 2006; 31: 1053-61.
4. Zajączkowska R, Przewłocka B, Kocot-Kępska M et al. Tapentadol – A representative of a new class of MOR-NRI analgesics. Pharmacol Rep. 2018; 70(4): 812-20.
5. Tzschentke TM, Christoph T, Kögel B et al. (-)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol hydrochloride (tapentadol HCl): a novel mu-opioid receptor agonist/norepinephrine reuptake inhibitor with broad-spectrum analgesic properties. J Pharmacol Exp Ther. 2007; 323(1): 265-76.
6. Kögel B, De Vry J, Tzschentke TM et al. The antinociceptive and antihyperalgesic effect of tapentadol is partially retained in OPRM1 (μ-opioid receptor) knockout mice. Neurosci Lett. 2011; 491(2): 104-7.
7. Schroder W, De Vry JD, Tzschentke TM et al. Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Eur J Pain. 2010; 14(8): 814-21.
8. Palexia SR (tapentadol) prolonged-release oral tablets [summary of product characteristics]. Buckinghamshire, UK, Grunenthal Ltd., 2011.
9. Zajączkowska R, Kocot-Kępska M, Dobrogowski J et al. Tapentadol – stan wiedzy 2017. Terapia. 2017; 8: 1-8.
10. Etropolski M, Kuperwasser, B., Flügel, M. et al. Safety and tolerability of tapentadol extended release in moderate to severe chronic osteoarthritis or low back pain management: Pooled analysis of randomized controlled trials. Adv Ther. 2014; 31: 604-20.
11. Wild JE, Grond S, Kuperwasser B, Flügel M et al. Longterm safety and tolerability of tapentadol extended release for the management of chronic low back pain or osteoarthritis pain. Pain Pract. 2010; 10(5): 416-27.
12. van der Schrier R, Jonkman K, van Velzen M et al. An experimental study comparing the respiratory effects of tapentadol and oxycodone in healthy volunteers. Br J Anaesth. 2017; 119(6): 1169-77.
13. Webster L, Rauck RL. Atypical opioids and their effect on respiratory drive. J Opioid Manag. 2021; 17(7): 109-18.
14. Biondi D, Xiang J, Etropolski M et al. A post hoc pooled data analysis to evaluate blood pressure (BP) and heart rate (HR) measurements in patients with a current or prior history of hypertension who received tapentadol ER, oxycodone CR, or placebo in chronic pain studies. J Pain. 2011; 12(4 Suppl): P55.
15. Oh C, Rengelshausen J, Mangold B et al. A thorough Qt/QTc study of multiple doses of tapentadol immediate release in healthy subjects. Int J Clin Pharmacol Ther. 2010; 48(10): 678-87.
16. Eichenbaum G, Gohler K, Etropolski M et al. Does tapentadol affect sex hormone concentrations differently from morphine and oxycodone? An initial assessment and possible implications for opioid-induced androgen deficiency. J Opioid Manag. 2015; 11(3): 211-27.
17. Coluzzi F, Pergolizzi J, Raffa RB et al. The unsolved case of bone-impairing analgesics: the endocrine effects of opioids on bone metabolism. Ther Clin Risk Manag. 2015; 11: 515-23.
18. Hartrick CT, Rozek RJ. Tapentadol in pain management. CNS Drugs. 2011; 25(5): 359-70.
19. Pergolizzi J, Alegre C, Blake D et al. Current considerations for the treatment of severe chronic pain: the potential for tapentadol. Pain Practice. 2012; 12(4): 290-306.
20. Franchi S, Moschetti G, Amodeo G et al. Do All Opioid Drugs Share the Same Immunomodulatory Properties? A Review From Animal and Human Studies. Front Immunol. 2019; 10: 2914.
21. Kneip C, Terlinden R, Beier H et al. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Letters. 2008; 2: 67-75.
22. Mangold B, Oh C, Jaeger D et al. The pharmacokinetics of tapentadol are not affected by omeprazole: results of a 2-way crossover drug-interaction study in healthy subjects. Pain Pract. 2007; 7(Suppl 1): 55-7.
23. Smit JW, Oh C, Rengelshausen J et al. Effects of acetaminophen, naproxen and acetylsalicylic acid on tapentadol pharmacokinetics: results of two randomized, open-label, crossover, drug-drug interaction studies. Pharmacotherapy. 2010; 30(1): 25-34.
24. Charakterystyka produktu leczniczego Palexia retard.
25. Charakterystyka produktu leczniczego Palexia.
26. Charakterystyka produktu leczniczego Palexia roztwór doustny 4 mg/ml.
27. Charakterystyka produktu leczniczego Palexia roztwór doustny 20 mg/ml.
28. Wade WE, Spruill WJ. Tapentadol hydrochloride: a centrally acting oral analgesic. Clin Ther. 2009; 31(12): 2804-18.
29. Kern KU, Sohns M, Heckes B et al. Tapentadol prolonged release for severe chronic osteoarthritis pain in the elderly: improvements in daily functioning and quality of life. Pain Manag. 2020; 10(2): 85-95.
30. Freo U, Furnari M, Ambrosio F et al. Efficacy and tolerability of tapentadol for the treatment of chronic low back pain in elderly patients. Aging Clin Exp Res. 2021; 33(4): 973-82.
31. Schwittay A, Sohns M, Heckes B et al. Tapentadol Prolonged Release for Severe Chronic Osteoarthritis Pain in the Elderly-A Subgroup Analysis of Routine Clinical Practice Data. Pain Res Manag. 2020; 2020: 5759265.
32. Pierce DM, Shipstone E. Pharmacology Update: Tapentadol for neuropathic pain. Am J Hosp Palliat Med. 2012; 29(8): 663-66.
33. Steigerwald I, Schenk M, Lahne U et al. Effectiveness and Tolerability of Tapentadol Prolonged Release Compared With Prior Opioid Therapy for the Management of Severe, Chronic Osteoarthritis Pain. Clin Drug Investig. 2013; 33: 607-19.
34. Davis MP, Davis A, McPherson ML et al. Opioid conversion in adults with cancer: MASCC‑ASCO‑AAHPM‑HPNA‑NICSO guideline. Supportive Care in Cancer. 2025; 33: 243.
35. Sanchez M, Shenk M, Kern KU et al. Practical Considerations for the Use of Tapentadol Prolonged Release for the Management of Severe Chronic Pain. Clin Ther. 2015; 27(1): 94-113.
36. Viscusi ER, Allard R, Sohns M et al. Tapentadol immediate release for moderate to severe acute post-surgery pain. J Opioid Manag. 2019; 15: 51-67.
37. Baron R, Jansen JP, Binder A et al. Tolerability, Safety, and Quality of Life with Tapentadol Prolonged Release (PR) Compared with Oxycodone/Naloxone PR in Patients with Severe Chronic Low Back Pain with a Neuropathic Component: A Randomized, Controlled, Open-label, Phase 3b/4 Trial. Pain Pract. 2016; 16(5): 600-19.
38. Kress HG, Koch ED, Kosturski H et al. Tapentadol prolonged release for managing moderate to severe, chronic malignant tumor-related pain. Pain Physician. 2014; 17: 329-43.
39. Mercadante S, Porzio G, Ferrera P et al. Tapentadol in cancer pain management: a prospective, open-label study. Curr Med Res Op. 2012; 28(11): 1775-9.