Tapentadol and tramadol in pain management: similarities, differences, and the practical importance of drug choice Review article
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Abstract
Tapentadol and tramadol are mixed-action analgesics combining μ-receptor agonism with modulation of the monoaminergic system. However, they differ significantly in their pharmacodynamics, pharmacokinetics, and interaction profile. Tramadol, primarily used for the treatment of moderate pain, requires CYP2D6 for the formation of its active metabolite and exhibits serotonergic activity, which may contribute to variability in clinical response and increase the risk of drug interactions. Tapentadol, whose action is independent of the active metabolite, combines μ-receptor agonism with inhibition of norepinephrine reuptake and does not exhibit clinically significant effects on serotonin uptake. Its pharmacological profile may be particularly relevant in the treatment of chronic moderate to severe pain, especially mixed pain or pain with a neuropathic component, as well as in patients receiving multidrug pharmacotherapy. However, both medications are associated with the risk of opioid-specific adverse effects, including sedation, constipation, respiratory depression, tolerance, and dependence. Therefore, an individualized risk-benefit assessment is required. The choice between tramadol and tapentadol should take into account the nature and severity of pain, comorbidities, current treatment, and potential pharmacological interactions.
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References
2. Faria J, Barbosa J, Leal S et al. Comparative pharmacology and toxicology of tramadol and tapentadol. Eur J Pain. 2018; 22(5): 827-44.
3. Deeks ED. Tapentadol prolonged release: a review in pain management. Drugs. 2018; 78(17): 1805-16.
4. Freo U, Romualdi P, Kress HG. Tapentadol for neuropathic pain: a review of clinical studies. J Pain Res. 2019; 12: 1537-51.
5. Charakterystyka Produktu Leczniczego Tadomon, tabletki o przedłużonym uwalnianiu. Rejestr Produktów Leczniczych, Urząd Rejestracji Produktów Leczniczych/Centrum e-Zdrowia.
6. Polati E, Canonico PL, Schweiger V et al. Tapentadol: an overview of the safety profile. J Pain Res. 2019; 12: 1569-76.
7. Charakterystyka Produktu Leczniczego Tramal, kapsułki twarde 50 mg. Rejestr Produktów Leczniczych, Urząd Rejestracji Produktów Leczniczych/ Centrum e-Zdrowia.
8. Dean L, Kane M. Tramadol Therapy and CYP2D6 Genotype. In: Medical Genetics Summaries. Pratt VM, Scott SA, Pirmohamed M et al. (eds.). National Center for Biotechnology Information, Bethesda 2025 (updated).
9. Xiao JP, Li AL, Feng BM et al. Efficacy and safety of tapentadol immediate release assessment in treatment of moderate to severe pain: a systematic review and meta-analysis. Pain Med. 2017; 18(1): 14024.
10. Dowell D, Ragan KR, Jones CM et al. CDC Clinical Practice Guideline for Prescribing Opioids for Pain – United States, 2022. MMWR Recomm Rep. 2022; 71(3): 1-95.
11. Fitzcharles MA, Cohen SP, Clauw DJ et al. Nociplastic pain: towards an understanding of prevalent pain conditions. Lancet. 2021; 397(10289): 2098-110.
12. Duehmke RM, Derry S, Wiffen PJ et al. Tramadol for neuropathic pain in adults. Cochrane Database Syst Rev. 2017; 6: CD003726.
13. Juba KM, van Manen RP, Fellows SE. A review of the Food and Drug Administration Adverse Event Reporting System for tramadol-related hypoglycemia. Ann Pharmacother. 2020; 54(3): 247-53.
14. Baldo BA, Rose MA. The anaesthetist, opioid analgesic drugs, and serotonin toxicity: a mechanistic and clinical review. Br J Anaesth. 2020; 124(1): 44-62.
15. Chrétien B, Dolladille C, Hamel-Sénécal L et al. Comparative study of hypoglycaemia induced by opioids. Is it a class effect? Expert Opin Drug Saf. 2019; 18(10): 987-92.