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Review

Designing safer analgesics: a focus on μ-opioid receptor pathways

, , , , &
Pages 965-972 | Received 22 May 2018, Accepted 10 Aug 2018, Published online: 03 Sep 2018

References

  • Centers for Disease C, Prevention. CDC grand rounds: prescription drug overdoses - a U.S. epidemic. MMWR Morb Mortal Wkly Rep. 2012;61(1):10–13.
  • Manchikanti L, Helm S 2nd, Fellows B, et al. Opioid epidemic in the United States. Pain Physician. 2012;15(3 Suppl):ES9–E38.
  • Bock A, Kostenis E, Trankle C, et al. Pilot the pulse: controlling the multiplicity of receptor dynamics. Trends Pharmacol Sci. 2014;35(12):630–638.
  • Schmid CL, Kennedy NM, Ross NC, et al. Bias factor and therapeutic window correlate to predict safer opioid analgesics. Cell. 2017;171(5):1165–75 e13.
  • Smith H, Peppin J. Toward a systematic approach to opioid rotation. J Pain Res. 2014;7:589–608.
  • Schepers R, Mahoney J, Shippenberg T. Inflammation-induced changes in rostral ventromedial medulla mu and kappa opioid receptor mediated antinociception. Pain Manag Nurs. 2008;136(3):320–330.
  • Petrillo P, Angelici O, Bingham S, et al. Evidence for a selective role of the delta-opioid agonist [8R-(4bS*,8aalpha,8abeta, 12bbeta)]7,10-Dimethyl-1-methoxy-11-(2-methylpropyl)oxycarbonyl 5,6,7,8,12,12b-hexahydro-(9H)-4,8-methanobenzofuro[3,2-e]pyrrolo[2,3-g]isoquinoline hydrochloride (SB-235863) in blocking hyperalgesia associated with inflammatory and neuropathic pain responses. J Pharmacol Exp Ther. 2003;307(3):1079–1089.
  • Yamamoto T, Nozaki-Taguchi N, Kimura S. Analgesic effect of intrathecally administered nociceptin, an opioid receptor-like1 receptor agonist, in the rat formalin test. Neuroscience. 1997;81:249–254.
  • Pergolizzi JV Jr., Scholten W, Smith KJ, et al. The unique role of transdermal buprenorphine in the global chronic pain epidemic. Acta Anaesthesiol Taiwan. 2015;53(2):71–76.
  • Lutfy K, Cowan A. Buprenorphine: a unique drug with complex pharmacology. Curr Neuropharmacol. 2004;2(4):395–402.
  • Pergolizzi J, Aloisi AM, Dahan A, et al. Current knowledge of buprenorphine and its unique pharmacological profile. Pain Pract. 2010;10(5):428–450.
  • Raffa RB, Haidery M, Huang HM, et al. The clinical analgesic efficacy of buprenorphine. J Clin Pharm Ther. 2014;39(6):577–583.
  • Ding Z, Raffa RB. Identification of an additional supraspinal component to the analgesic mechanism of action of buprenorphine. Br J Pharmacol. 2009;157(5):831–843.
  • Christoph T, Kogel B, Schiene K, et al. Broad analgesic profile of buprenorphine in rodent models of acute and chronic pain. Eur J Pharmacol. 2005;507(1–3):87–98.
  • Davis MP. Twelve reasons for considering buprenorphine as a frontline analgesic in the management of pain. J Support Oncol. 2012;10(6):209–219.
  • Rizzi A, Cerlesi M, Ruzza C, et al. Pharmacological characterization of cebranopadol a novel analgesic acting as mixed nociceptin/orphanin FQ and opioid receptor agonist. Pharmacol Res Perspect. 2016;4(4):e00247.
  • Tian J, Xu W, Fang Y, et al. Bidirectional modulatory effect of orphanin FQ on morphine-induced analgesia: antagonism in brain and potentiation in spinal cord of the rat. Br J Pharmacol. 1997;120:676–680.
  • Courteix C, Coudore-Civiale M, Privat A, et al. Evidence for an exclusive antinociceptive effect of nociceptin/orphanin FQ, an endogenous ligand for the ORL1 receptor, in two animal models of neuropathic pain. Pain Manag Nurs. 2004;110:236–245.
  • Ko M, Naughton N. Antinociceptive effects of nociceptin/orphanin FQ administered intrathecally in monkeys. J Pain Palliat Care Pharmacother. 2009;10:509–516.
  • Hu E, Calo G, Guerrini R, et al. Long-lasting antinociceptive spainal effects in primates of the novel nociceptin/orphanin FQ receptor agonist UFP-112. Pain Manag Nurs. 2010;148:107–113.
  • Cremeans C, Gruley E, Kyle D, et al. Roles of mu-opioid receptors and nociceptin/orphanin FQ peptide receptors in buprenorphine-induced physiological responses in primates. J Pharmacol Exp Ther. 2012;343:72–81.
  • Evaluate. Tapentadol–first member of a proposed new pharmacological class called MOR-NRI. Press release. 2010 [cited 2017 Jul 3]. Available from: http://www.evaluategroup.com/Universal/View.aspx?type=Story&id=214756
  • Raffa RB, Buschmann H, Christoph T, et al. Mechanistic and functional differentiation of tapentadol and tramadol. Expert Opin Pharmacother. 2012;13(10):1437–1449.
  • Pergolizzi JV Jr., Breve F, Taylor R Jr. et al. Considering tapentadol as a first-line analgesic: 14 questions. Pain Manag. 2017.7(4):331–339.
  • Van Der Schier R, Roozekrans M, Van Velzen M, et al. Opioid-induced respiratory depression: reversal by non-opioid drugs. F1000Prime Rep. 2014;6:79.
  • Stollenwerk A, Sohns M, Heisig F, et al. Review of post-marketing safety data on tapentadol, a centrally acting analgesic. Adv Ther. 2018;35(1):12–30.
  • Hartrick CT, Rozek RJ. Tapentadol in pain management: a μ-opioid receptor agonist and noradrenaline reuptake inhibitor. CNS Drugs. 2011;25(5):359–370.
  • Raffa RB, Friderichs E. The basic science aspect of tramadol hydrochloride. Pain Reviews. 1996;3(4):249–271.
  • Miotto K, Cho AK, Khalil MA, et al. Trends in tramadol: pharmacology, metabolism, and misuse. Anesth Analg. 2017;124(1):44–51.
  • Smith HS, Raffa RB, Pergolizzi JV, et al. Combining opioid and adrenergic mechanisms for chronic pain. Postgrad Med. 2014;126(4):98–114.
  • Raffa RB. Basic pharmacology relevant to drug abuse assessment: tramadol as example. J Clin Pharm Ther. 2008;33(2):101–108.
  • Rauck RL, Potts J, Xiang Q, et al. Efficacy and tolerability of buccal buprenorphine in opioid-naive patients with moderate to severe chronic low back pain. Postgrad Med. 2016;128(1):1–11.
  • Steiner D, Munera C, Hale M, et al. Efficacy and safety of buprenorphine transdermal system (BTDS) for chronic moderate to severe low back pain: a randomized, double-blind study. J Pain. 2011;12(11):1163–1173.
  • Christoph A, Eerdekens MH, Kok M, et al. Cebranopadol, a novel first-in-class analgesic drug candidate: first experience in patients with chronic low back pain in a randomized clinical trial. Pain. 2017;158:1813–1824.
  • Wiffen PJ, Derry S, Naessens K, et al. Oral tapentadol for cancer pain. Cochrane Database Syst Rev. 2015;9:CD011460.
  • Santos J, Alarcao J, Fareleira F, et al. Tapentadol for chronic musculoskeletal pain in adults. Cochrane Database Syst Rev. 2015;5:CD009923
  • Stegmann JU, Weber H, Steup A, et al. The efficacy and tolerability of multiple-dose tapentadol immediate release for the relief of acute pain following orthopedic (bunionectomy) surgery. Curr Med Res Opin. 2008;24(11):3185–3196.
  • Daniels S, Casson E, Stegmann JU, et al. A randomized, double-blind, placebo-controlled phase 3 study of the relative efficacy and tolerability of tapentadol IR and oxycodone IR for acute pain. Curr Med Res Opin. 2009;25(6):1551–1561.
  • Vadivelu N, Kai A, Maslin B, et al. Tapentadol extended release in the management of peripheral diabetic neuropathic pain. Ther Clin Risk Manag. 2015;11:95–105.
  • Grond S, Sablotzki A. Clinical pharmacology of tramadol. Clin Pharmacokinet. 2004;43(13):879–923.
  • Lee JH, Lee CS. A randomized, double-blind, placebo-controlled, parallel-group study to evaluate the efficacy and safety of the extended-release tramadol hydrochloride/acetaminophen fixed-dose combination tablet for the treatment of chronic low back pain. Clin Ther. 2013;35(11):1830–1840.
  • Lasko B, Levitt RJ, Rainsford KD, et al. Extended-release tramadol/paracetamol in moderate-to-severe pain: a randomized, placebo-controlled study in patients with acute low back pain. Curr Med Res Opin. 2012;28(5):847–857.
  • Desai SN, Badiger SV, Tokur SB, et al. Safety and efficacy of transdermal buprenorphine versus oral tramadol for the treatment of post-operative pain following surgery for fracture neck of femur: A prospective, randomised clinical study. Indian J Anaesth. 2017;61(3):225–229.
  • Conaghan PG, Serpell M, McSkimming P, et al. Satisfaction, adherence and health-related quality of life with transdermal buprenorphine compared with oral opioid medications in the usual care of osteoarthritis pain. Patient. 2016;9(4):359–371.
  • Conaghan PG, O’Brien CM, Wilson M, et al. Transdermal buprenorphine plus oral paracetamol vs an oral codeine-paracetamol combination for osteoarthritis of hip and/or knee: a randomised trial. Osteoarthritis Cartilage. 2011;19(8):930–938.
  • Pergolizzi JV, Raffa RB, Marcum Z, et al. Safety of buprenorphine transdermal system in the management of pain in older adults. Postgrad Med. 2017;129(1):92–101.
  • Lambert D, Bird M, Rowbotham D. Cebranopadol: a first in class example of a nociceptin/orphanin FQ receptor and opioid receptor agonist. Br J Anaesth. 2015;114:364–366.
  • Lambert D. The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential. Nat Rev Drug Discov. 2008;7:694–710.
  • Tzschentke TM, Christoph T, Kogel 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):265–276.
  • Vadivelu N, Timchenko A, Huang Y, et al. Tapentadol extended-release for treatment of chronic pain: a review. J Pain Res. 2011;4:211–218.
  • Beakley B, Kaye AD, Kaye AL. Tramadol, pharmacology, side effects, and serotonin syndrome: a review. Pain Physician. 2015;18:395–400.
  • Jovanovic-Cupic V, Martinovic Z, Nesic N. Seizures associated with intoxication and abuse of tramadol. Clin Toxicol. 2006;44(2):143–146.
  • Wu H, Wu G. In response: the cause of fatal respiratory depression is combination of clindamycin and fentanyl, rather than tramadol. Pain Physician. 2015;19:E359–E363.
  • CDC. Injury prevention and control: opioid overdose. [updated 2016 Mar 16; cited 2016 Apr 25]. Available from: http://www.cdc.gov/drugoverdose/
  • Manchikanti L, Kaye AM, Knezevic NN, et al. Responsible, safe, and effective prescription of opioids for chronic non-cancer pain: American Society of Interventional Pain Physicians (ASIPP) guidelines. Pain Physician. 2017;20(2s):S3–s92.
  • Wightman R, Perrone J, Portelli I, et al. Likeability and abuse liability of commonly prescribed opioids. J Med Toxicol. 2012;8(4):335–340.
  • Webster LR, Kopecky EA, Smith MD, et al. Double-blind, double-dummy study to evaluate the intranasal human abuse potential and pharmacokinetics of a novel extended-release abuse-deterrent formulation of oxycodone. Pain Med. 2016;17(6):1112–1130.
  • Setnik B, Roland CL, Pixton G, et al. Measurement of drug liking in abuse potential studies: a comparison of unipolar and bipolar visual analog scales. J Clin Pharmacol. 2016;57(2):266–274.
  • Cicero TJ, Ellis MS, Surratt HL, et al. The changing face of heroin use in the United States: a retrospective analysis of the past 50 years. JAMA Psychiatry. 2014;71(7):821–826.
  • DEA. National drug threat assessment summary. 2016 [cited 2017 Apr 14]. Available from: https://www.dea.gov/resource-center/2016_NDTA_Summary.pdf
  • Webster LR, Bath B, Medve RA, et al. Randomized, double-blind, placebo-controlled study of the abuse potential of different formulations of oral oxycodone. Pain Med. 2012;13(6):790–801.
  • Zacny JP. Profiling the subjective, psychomotor, and physiological effects of tramadol in recreational drug users. Drug Alcohol Depend. 2005;80(2):273–278.
  • Centers for Disease C, Prevention. Emergency department visits involving nonmedical use of selected prescription drugs - United States 2004-2008. MMWR Morb Mortal Wkly Rep. 2010;59(23):705–709.
  • Paone D, Tuazon E, Stajic M, et al. Buprenorphine infrequently found in fatal overdose in New York City. Drug Alcohol Depend. 2015;155:298–301.
  • Jasinski DR, Pevnick JS, Griffith JD. Human pharmacology and abuse potential of the analgesic buprenorphine: a potential agent for treating narcotic addiction. Arch Gen Psychiatry. 1978;35(4):501–516.
  • Johnson RE, Fudala PJ, Payne R. Buprenorphine: considerations for pain management. J Pain Symptom Manage. 2005;29(3):297–326.
  • Tompkins DA, Smith MT, Mintzer MZ, et al. A double blind, within subject comparison of spontaneous opioid withdrawal from buprenorphine versus morphine. J Pharmacol Exp Ther. 2014;348(2):217–226.
  • Rp M, Kimber J, Breen C, et al. Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence. Cochrane Database Syst Rev. 2004;3:CD002207.
  • Butler SF, McNaughton EC, Black RA. Tapentadol abuse potential: a postmarketing evaluation using a sample of individuals evaluated for substance abuse treatment. Pain Med. 2015;16(1):119–130.
  • Bush DM Emergency department visits for drug misuse or abuse involving the pain medication tramadol. The CBHSQ Report. Rockville (MD): Substance Abuse and Mental Health Services Administration (US); 2013.
  • McNaughton EC, Black RA, Zulueta MG, et al. Measuring online endorsement of prescription opioids abuse: an integrative methodology. Pharmacoepidemiol Drug Saf. 2012;21(10):1081–1092.
  • Preston KL, Jasinski DR, Testa M. Abuse potential and pharmacological comparison of tramadol and morphine. Drug Alcohol Depend. 1991;27(1):7–17.
  • Raffa R, Friderichs E. The basic science aspect of tramadol hydrochloride. Pain Rev. 1996;3:249–271.

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