Tags

Type your tag names separated by a space and hit enter

Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated by μ-Opioid Receptors.
Biol Pharm Bull. 2020; 43(7):1128-1134.BP

Abstract

We investigated whether tramadol could suppress both neuropathic and inflammatory pain in mice at the same dose level. We also examined the effects of drugs metabolized by glucuronidase, such as acetaminophen (ACAP), indomethacin, probenecid, and valproate, on the antinociceptive activity of tramadol. The administration of 5.6 or 10 mg/kg tramadol suppressed cuff-induced mechanical allodynia, but 10 mg/kg tramadol did not suppress complete Freund's adjuvant (CFA)-induced mechanical allodynia. Although neither tramadol (10 mg/kg) nor ACAP (100 mg/kg) alone produced an antinociceptive effect, their combination suppressed CFA-induced mechanical allodynia. Moreover, pretreatment naloxone, an opioid receptor antagonist, significantly attenuated the antinociceptive effects induced by the combination of tramadol and ACAP and slowed gastrointestinal transit. Similar to ACAP, the combination of tramadol and probenecid or valproate, which has the potential to inhibit uridine 5'-diphosphate (UDP)-glucuronosyltransferase (UGT), also suppressed the CFA-induced mechanical allodynia and slowed gastrointestinal transit. We concluded that tramadol was more beneficial for the treatment of neuropathic pain than inflammatory pain. Furthermore, the antinociceptive effects of the tramadol and ACAP combination were mediated by the μ-opioid receptor, and were thought to be related, at least in part, to the accumulation of the active metabolite, M1.

Authors+Show Affiliations

Laboratory of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Preformulation Study, Faculty of Pharmaceutical Sciences, Tokyo University of Science.Laboratory of Preformulation Study, Faculty of Pharmaceutical Sciences, Tokyo University of Science.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32612076

Citation

Yoshizawa, Kazumi, et al. "Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated By μ-Opioid Receptors." Biological & Pharmaceutical Bulletin, vol. 43, no. 7, 2020, pp. 1128-1134.
Yoshizawa K, Arai N, Suzuki Y, et al. Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated by μ-Opioid Receptors. Biol Pharm Bull. 2020;43(7):1128-1134.
Yoshizawa, K., Arai, N., Suzuki, Y., Fujita, A., Takahashi, Y., Kawano, Y., & Hanawa, T. (2020). Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated by μ-Opioid Receptors. Biological & Pharmaceutical Bulletin, 43(7), 1128-1134. https://doi.org/10.1248/bpb.b20-00230
Yoshizawa K, et al. Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated By μ-Opioid Receptors. Biol Pharm Bull. 2020;43(7):1128-1134. PubMed PMID: 32612076.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Synergistic Antinociceptive Activity of Tramadol/Acetaminophen Combination Mediated by μ-Opioid Receptors. AU - Yoshizawa,Kazumi, AU - Arai,Narumaki, AU - Suzuki,Yukina, AU - Fujita,Ayumi, AU - Takahashi,Yukino, AU - Kawano,Yayoi, AU - Hanawa,Takehisa, PY - 2020/7/3/entrez KW - acetaminophen KW - complete Freund’s adjuvant model KW - glucuronidation KW - tramadol SP - 1128 EP - 1134 JF - Biological & pharmaceutical bulletin JO - Biol. Pharm. Bull. VL - 43 IS - 7 N2 - We investigated whether tramadol could suppress both neuropathic and inflammatory pain in mice at the same dose level. We also examined the effects of drugs metabolized by glucuronidase, such as acetaminophen (ACAP), indomethacin, probenecid, and valproate, on the antinociceptive activity of tramadol. The administration of 5.6 or 10 mg/kg tramadol suppressed cuff-induced mechanical allodynia, but 10 mg/kg tramadol did not suppress complete Freund's adjuvant (CFA)-induced mechanical allodynia. Although neither tramadol (10 mg/kg) nor ACAP (100 mg/kg) alone produced an antinociceptive effect, their combination suppressed CFA-induced mechanical allodynia. Moreover, pretreatment naloxone, an opioid receptor antagonist, significantly attenuated the antinociceptive effects induced by the combination of tramadol and ACAP and slowed gastrointestinal transit. Similar to ACAP, the combination of tramadol and probenecid or valproate, which has the potential to inhibit uridine 5'-diphosphate (UDP)-glucuronosyltransferase (UGT), also suppressed the CFA-induced mechanical allodynia and slowed gastrointestinal transit. We concluded that tramadol was more beneficial for the treatment of neuropathic pain than inflammatory pain. Furthermore, the antinociceptive effects of the tramadol and ACAP combination were mediated by the μ-opioid receptor, and were thought to be related, at least in part, to the accumulation of the active metabolite, M1. SN - 1347-5215 UR - https://www.unboundmedicine.com/medline/citation/32612076/Synergistic_Antinociceptive_Activity_of_Tramadol/Acetaminophen_Combination_Mediated_by_μ-Opioid_Receptors L2 - https://dx.doi.org/10.1248/bpb.b20-00230 DB - PRIME DP - Unbound Medicine ER -
Try the Free App:
Prime PubMed app for iOS iPhone iPad
Prime PubMed app for Android
Prime PubMed is provided
free to individuals by:
Unbound Medicine.