Login Register Cart 0
Generic placeholder image

Current Indian Science

Editor-in-Chief

ISSN (Print): 2210-299X
ISSN (Online): 2210-3007

Back
Journal Home About Journal Editorial Board Current Issue Volumes/Issues
Subscribe
Review Article

A State-of-the-Art Review on Opioids Induced Constipation and its Management

Author(s): Suraj Longare, Dhwani Rana, Sagar Salave and Derajram Benival*

Volume 1, 2023

Published on: 02 September, 2022

Article ID: e020922208451 Pages: 17

DOI: 10.2174/2210299X01666220902112122

open_access

Open Access Journals Promotions 2
Abstract

Background: Pain is a complex physiological and psychological response to a noxious stimulus, sometimes deteriorating a patient’s quality of life. Opioids remain the mainstay treatment modality for chronic pain. Several concerns are raised regarding the long-term use of opioids and the risks associated with their usage. Findings advocate that the longstanding practice of opioid consumption manifests in adverse effects. Objective: Due to the physiological changes opioids instigate in the gastrointestinal tract, opioid-induced constipation remains a common complication pragmatic in patients undergoing opioid medications. Several therapeutic interventions are made available, and the review describes the overall medications with practical examples, aiding in selecting a treatment plan.

Methods: The method comprises data collection from various search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding pain management, opioids, opioid-induced constipation, and its pharmacological interventions.

Results: The thoughtful custom of exploring several options to manage opioid-induced constipation must allow patients to benefit from opioid analgesia.

Conclusion: This paper reviews the role of opioids in pain management, the underlying mechanisms of their action, opioid-induced constipation, and pharmacological therapies, with experimental studies aiding clinicians to optimise treatment plans.

Keywords: Pain, Opioids, Opioid-induced constipation, Opioid receptors, Opioid inhibitors, Opioid antagonists.

[1]
Raja, S.N.; Carr, D.B.; Cohen, M.; Finnerup, N.B.; Flor, H.; Gibson, S.; Keefe, F.J.; Mogil, J.S.; Ringkamp, M.; Sluka, K.A.; Song, X.J.; Stevens, B.; Sullivan, M.D.; Tutelman, P.R.; Ushida, T.; Vader, K. The revised international association for the study of pain definition of pain: Concepts, challenges, and compromises. Pain, 2020, 161(9), 1976-1982.
[http://dx.doi.org/10.1097/j.pain.0000000000001939] [PMID: 32694387]
[2]
Treede, R.D.; Rief, W.; Barke, A.; Aziz, Q.; Bennett, M.I.; Benoliel, R.; Cohen, M.; Evers, S.; Finnerup, N.B.; First, M.B.; Giamberardino, M.A.; Kaasa, S.; Kosek, E.; Lavand’homme, P.; Nicholas, M.; Perrot, S.; Scholz, J.; Schug, S.; Smith, B.H.; Svensson, P.; Vlaeyen, J.W.S.; Wang, S.J. A classification of chronic pain for ICD-11. Pain, 2015, 156(6), 1003-1007.
[http://dx.doi.org/10.1097/j.pain.0000000000000160] [PMID: 25844555]
[3]
Sung, H.; Ferlay, J.; Siegel, R.L.; Laversanne, M.; Soerjomataram, I.; Jemal, A.; Bray, F. Global Cancer Statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J. Clin., 2021, 71(3), 209-249.
[http://dx.doi.org/10.3322/caac.21660] [PMID: 33538338]
[4]
Rosenblum, A.; Marsch, L.A.; Joseph, H.; Portenoy, R.K. Opioids and the treatment of chronic pain: Controversies, current status, and future directions. Exp. Clin. Psychopharmacol., 2008, 16(5), 405-416.
[http://dx.doi.org/10.1037/a0013628] [PMID: 18837637]
[5]
WHO. Opioid overdose. Available from: https://www.who.int/news-room/fact-sheets/detail/opioid-overdose (Accessed on: 8 June 2022).
[6]
Lang-Illievich, K.; Bornemann-Cimenti, H. Opioid-induced constipation: A narrative review of therapeutic options in clinical management. Korean J. Pain, 2019, 32(2), 69-78.
[http://dx.doi.org/10.3344/kjp.2019.32.2.69] [PMID: 31091505]
[7]
Farmer, A.D.; Holt, C.B.; Downes, T.J.; Ruggeri, E.; Del Vecchio, S.; De Giorgio, R. Pathophysiology, diagnosis, and management of opioid-induced constipation. Lancet Gastroenterol. Hepatol., 2018, 3(3), 203-212.
[http://dx.doi.org/10.1016/S2468-1253(18)30008-6] [PMID: 29870734]
[8]
Rana, D.; Salave, S.; Benival, D. Emerging trends in abuse-deterrent formulations: Technological insights and regulatory considerations. Curr. Drug Deliv., 2021, 18
[PMID: 34879799]
[9]
Dubin, A.E.; Patapoutian, A. Nociceptors: The sensors of the pain pathway. J. Clin. Invest., 2010, 120(11), 3760-3772.
[http://dx.doi.org/10.1172/JCI42843] [PMID: 21041958]
[10]
Okuse, K. Pain signalling pathways: From cytokines to ion channels. Int. J. Biochem. Cell Biol., 2007, 39(3), 490-496.
[http://dx.doi.org/10.1016/j.biocel.2006.11.016] [PMID: 17194618]
[11]
WHO. Cancer pain relief. Available from: https://apps.who.int/iris/bitstream/handle/10665/43944/9241561009_eng.pdf (Accessed on: 8 June 2022).
[12]
WHO. Cancer pain relief : With a guide to opioid availability. Available from: http://apps.who.int/iris/bitstream/handle/10665/37896/9241544821.pdf?sequence=1 (Accessed on: 8 June 2022).
[13]
WHO. Cancer pain relief and palliative care in children. Available from: http://apps.who.int/iris/bitstream/handle/10665/42001/9241545127.pdf?sequence=1 (Accessed on: 8 June 2022).
[14]
Nersesyan, H.; Slavin, K.V. Current aproach to cancer pain management: Availability and implications of different treatment options. Ther. Clin. Risk Manag., 2007, 3(3), 381-400.
[PMID: 18488078]
[15]
Academy, T.A.; Dentistry, P.; Affairs, C. Pain management in infants, children, adolescents and individuals with special health care needs. Pediatr. Dent., 2018, 40(6), 321-329.
[PMID: 32074903]
[16]
Prescription Opioids DrugFacts | National Institute on Drug Abuse (NIDA). Available from: https://nida.nih.gov/publications/drugfacts/prescription-opioids (Accessed on: 10 Feb 2022).
[17]
Omidian, A.; Mastropietro, D.J.; Omidian, H. Routes of opioid abuse and its novel deterrent formulations. J. Dev. Drugs, 2015, 4(5), 1-7.
[18]
Cohen, B.; Ruth, L.J.; Preuss, C.V. Opioid Analgesics. In: StatPearls; StatPearls Publishing: Treasure Island (FL), 2021.
[19]
Dydyk, A.M.; Jain, N.K.; Gupta, M. Opioid Use Disorder. In: StatPearls; StatPearls Publishing: Treasure Island (FL), 2021.
[20]
Zöllner, C.; Stein, C. Opioids. Handb. Exp. Pharmacol., 2007, 177(177), 31-63.
[PMID: 17087119]
[21]
Rastogi, R.; Swarm, R.A.; Patel, T.A.; Riou, B. Case scenario: Opioid association with serotonin syndrome: Implications to the practitioners. Anesthesiology, 2011, 115(6), 1291-1298.
[http://dx.doi.org/10.1097/ALN.0b013e31823940c0] [PMID: 22037635]
[22]
Crockett, S.D.; Greer, K.B.; Heidelbaugh, J.J.; Falck-Ytter, Y.; Hanson, B.J.; Sultan, S. American Gastroenterological Association Institute guideline on the medical management of opioid-induced constipation. Gastroenterology, 2019, 156(1), 218-226.
[http://dx.doi.org/10.1053/j.gastro.2018.07.016] [PMID: 30340754]
[23]
Center for Substance Abuse Treatment. Managing Chronic Pain in Adults With or in Recovery From Substance Use Disorders; Substance Abuse and Mental Health Services Administration (US): Rockville (MD), 2012.
[24]
Brownstein, M.J. A brief history of opiates, opioid peptides, and opioid receptors. Proc. Natl. Acad. Sci. USA, 1993, 90(12), 5391-5393.
[http://dx.doi.org/10.1073/pnas.90.12.5391] [PMID: 8390660]
[25]
Simon, E.J. Opioid receptors and endogenous opioid peptides. Med. Res. Rev., 1991, 11(4), 357-374.
[http://dx.doi.org/10.1002/med.2610110402] [PMID: 1652044]
[26]
Law, P.Y.; Loh, H.H. Opioid Receptors. In: Encyclopedia of Biological Chemistry, Second Edition; Lennarz, W.J.; Lane, M.D. Academic Press: Cambridge, Massachusetts, 2013; 2, pp. 354-358.
[http://dx.doi.org/10.1016/B978-0-12-378630-2.00347-9]
[27]
Pasternak, G.W.; Pan, Y.X. Mu opioids and their receptors: Evolution of a concept. Pharmacol. Rev., 2013, 65(4), 1257-1317.
[http://dx.doi.org/10.1124/pr.112.007138] [PMID: 24076545]
[28]
Al-Hasani, R.; Bruchas, M.R. Molecular mechanisms of opioid receptor-dependent signaling and behavior. Anesthesiology, 2011, 115(6), 1363-1381.
[http://dx.doi.org/10.1097/ALN.0b013e318238bba6] [PMID: 22020140]
[29]
McDonald, J.; Lambert, D.G. Opioid receptors. Contin. Educ. Anaesth. Crit. Care Pain, 2005, 5(1), 22-25.
[http://dx.doi.org/10.1093/bjaceaccp/mki004]
[30]
Zhang, J.; Ferguson, S.S.G.; Barak, L.S.; Bodduluri, S.R.; Laporte, S.A.; Law, P.Y.; Caron, M.G. Role for G protein-coupled receptor kinase in agonist-specific regulation of μ-opioid receptor responsiveness. Proc. Natl. Acad. Sci. USA, 1998, 95(12), 7157-7162.
[http://dx.doi.org/10.1073/pnas.95.12.7157] [PMID: 9618555]
[31]
Waldhoer, M.; Bartlett, S.E.; Whistler, J.L. Opioid receptors. Annu. Rev. Biochem., 2004, 73(1), 953-990.
[http://dx.doi.org/10.1146/annurev.biochem.73.011303.073940] [PMID: 15189164]
[32]
Kaserer, T.; Steinacher, T.; Kainhofer, R.; Erli, F.; Sturm, S.; Waltenberger, B.; Schuster, D.; Spetea, M. Identification and characterization of plant-derived alkaloids, corydine and corydaline, as novel mu opioid receptor agonists. Sci. Rep., 2020, 10(1), 13804.
[http://dx.doi.org/10.1038/s41598-020-70493-1] [PMID: 32796875]
[33]
Trescot, A.M.; Datta, S.; Lee, M.; Hansen, H. Opioid pharmacology. Pain Physician, 2008, 11(2 Suppl), S133-S153.
[http://dx.doi.org/10.36076/ppj.2008/11/S133] [PMID: 18443637]
[34]
Akil, H.; Owens, C.; Gutstein, H.; Taylor, L.; Curran, E.; Watson, S. Endogenous opioids: Overview and current issues. Drug Alcohol Depend., 1998, 51(1-2), 127-140.
[http://dx.doi.org/10.1016/S0376-8716(98)00071-4] [PMID: 9716935]
[35]
Bzdega, T.; Chin, H.; Kim, H.; Jung, H.H.; Kozak, C.A.; Klee, W.A. Regional expression and chromosomal localization of the delta opiate receptor gene. Proc. Natl. Acad. Sci. USA, 1993, 90(20), 9305-9309.
[http://dx.doi.org/10.1073/pnas.90.20.9305] [PMID: 8415697]
[36]
Wadenberg, M-L.G. A review of the properties of spiradoline: A potent and selective kappa-opioid receptor agonist. CNS Drug Rev., 2003, 9(2), 187-198.
[http://dx.doi.org/10.1111/j.1527-3458.2003.tb00248.x] [PMID: 12847558]
[37]
Walsh, S.; Strain, E.; Abreu, M.; Bigelow, G. Enadoline, a selective kappa opioid agonist: Comparison with butorphanol and hydromorphone in humans. Psychopharmacology (Berl.), 2001, 157(2), 151-162.
[http://dx.doi.org/10.1007/s002130100788] [PMID: 11594439]
[38]
Zaveri, N.T.; Jiang, F.; Olsen, C.; Polgar, W.E.; Toll, L. Designing bifunctional NOP receptor–mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I. Bioorg. Med. Chem. Lett., 2013, 23(11), 3308-3313.
[http://dx.doi.org/10.1016/j.bmcl.2013.03.101] [PMID: 23623415]
[39]
Zaveri, N.T. Nociceptin Opioid Receptor (NOP) as a therapeutic target: Progress in translation from preclinical research to clinical utility. J. Med. Chem., 2016, 59(15), 7011-7028.
[http://dx.doi.org/10.1021/acs.jmedchem.5b01499] [PMID: 26878436]
[40]
Janecka, A.; Fichna, J.; Janecki, T. Opioid receptors and their ligands. Curr. Top. Med. Chem., 2004, 4(1), 1-17.
[http://dx.doi.org/10.2174/1568026043451618] [PMID: 14754373]
[41]
Pathan, H.; Williams, J. Basic opioid pharmacology: An update. Br. J. Pain, 2012, 6(1), 11-16.
[http://dx.doi.org/10.1177/2049463712438493] [PMID: 26516461]
[42]
Dhawan, B.N.; Cesselin, F.; Raghubir, R.; Reisine, T.; Bradley, P.B.; Portoghese, P.S.; Hamon, M. International Union of Pharmacology. XII. Classification of opioid receptors. Pharmacol. Rev., 1996, 48(4), 567-592.
[PMID: 8981566]
[43]
Freye, E.; Levy, J.V. Mechanism of action of opioids and clinical effects. In: Opioids in Medicine; Freye, E.; Levy, J.V., Eds.; Springer: Dordrecht, 2008; pp. 85-187.
[http://dx.doi.org/10.1007/978-1-4020-5947-6_2]
[44]
Vallejo, R.; Barkin, R.L.; Wang, V.C. Pharmacology of opioids in the treatment of chronic pain syndromes. Pain Physician, 2011, 4(14), E343-E360.
[http://dx.doi.org/10.36076/ppj.2011/14/E343] [PMID: 21785485]
[45]
Machado, T.M.; Palatty, P.L. Opioid analgesic choices based on pharmacokinetics. J Anesth Pain Med., 2016, 1(2), 1-8.
[46]
Pergolizzi, J.V., Jr; Christo, P.J.; LeQuang, J.A.; Magnusson, P. The use of Peripheral μ-Opioid Receptor Antagonists (PAMORA) in the management of opioid-induced constipation: An update on their efficacy and safety. Drug Des. Devel. Ther., 2020, 14, 1009-1025.
[http://dx.doi.org/10.2147/DDDT.S221278] [PMID: 32210534]
[47]
Gupta, D.K.; Krejcie, T.C.; Avram, M.J. Essential drugs in anesthetic practice. Pharmacokinetics of opioids. Anesth Pharmacol, 2011, 509-530.
[48]
Machelska, H.; Celik, M.Ö. Advances in achieving opioid analgesia without side effects. Front. Pharmacol., 2018, 9, 1388.
[http://dx.doi.org/10.3389/fphar.2018.01388] [PMID: 30555325]
[49]
Boom, M.; Niesters, M.; Sarton, E.; Aarts, L.; Smith, T.W.; Dahan, A. Non-analgesic effects of opioids: Opioid-induced respiratory depression. Curr. Pharm. Des., 2012, 18(37), 5994-6004.
[http://dx.doi.org/10.2174/138161212803582469] [PMID: 22747535]
[50]
Rawal, H.; Patel, B.M. Opioids in cardiovascular disease: Therapeutic options. J. Cardiovasc. Pharmacol. Ther., 2018, 23(4), 279-291.
[http://dx.doi.org/10.1177/1074248418757009] [PMID: 29528698]
[51]
Nee, J.; Zakari, M.; Sugarman, M.A.; Whelan, J.; Hirsch, W.; Sultan, S.; Ballou, S.; Iturrino, J.; Lembo, A. Efficacy of treatments for opioid-induced constipation: Systematic review and meta-analysis. Clin. Gastroenterol. Hepatol., 2018, 16(10), 1569-1584.e2.
[http://dx.doi.org/10.1016/j.cgh.2018.01.021] [PMID: 29374616]
[52]
Müller-Lissner, S.; Bassotti, G.; Coffin, B.; Drewes, A.M.; Breivik, H.; Eisenberg, E.; Emmanuel, A.; Laroche, F.; Meissner, W.; Morlion, B. Opioid-induced constipation and bowel dysfunction: A clinical guideline. Pain Med., 2017, 18(10), 1837-1863.
[PMID: 28034973]
[53]
Kjellberg, F.; Tramèr, M.R. Pharmacological control of opioid-induced pruritus: A quantitative systematic review of randomized trials. Eur. J. Anaesthesiol., 2001, 18(6), 346-357.
[http://dx.doi.org/10.1097/00003643-200106000-00002] [PMID: 11412287]
[54]
Sternini, C.; Patierno, S.; Selmer, I.S.; Kirchgessner, A. The opioid system in the gastrointestinal tract. Neurogastroenterol. Motil., 2004, 16(s2)(Suppl. 2), 3-16.
[http://dx.doi.org/10.1111/j.1743-3150.2004.00553.x] [PMID: 15357847]
[55]
Holzer, P. Treatment of opioid-induced gut dysfunction. Expert Opin. Investig. Drugs, 2007, 16(2), 181-194.
[http://dx.doi.org/10.1517/13543784.16.2.181] [PMID: 17243938]
[56]
Labianca, R.; Sarzi-Puttini, P.; Zuccaro, S.M.; Cherubino, P.; Vellucci, R.; Fornasari, D. Adverse effects associated with non-opioid and opioid treatment in patients with chronic pain. Clin. Drug Investig., 2012, 32(Suppl. 1), 53-63.
[http://dx.doi.org/10.2165/11630080-000000000-00000]
[57]
McNicol, E.; Horowicz-Mehler, N.; Fisk, R.A.; Bennett, K.; Gialeli-Goudas, M.; Chew, P.W.; Lau, J.; Carr, D. Management of opioid side effects in cancer-related and chronic noncancer pain: A systematic review. J. Pain, 2003, 4(5), 231-256.
[http://dx.doi.org/10.1016/S1526-5900(03)00556-X] [PMID: 14622694]
[58]
Swegle, J.M.; Logemann, C. Management of common opioid-induced adverse effects. Am. Fam. Physician, 2006, 74(8), 1347-1354.
[PMID: 17087429]
[59]
Yee, J.D.; Berde, C.B. Dextroamphetamine or methylphenidate as adjuvants to opioid analgesia for adolescents with cancer. J. Pain Symptom Manage., 1994, 9(2), 122-125.
[http://dx.doi.org/10.1016/0885-3924(94)90165-1] [PMID: 7912710]
[60]
Dhingra, L.; Ahmed, E.; Shin, J.; Scharaga, E.; Magun, M. Cognitive effects and sedation. Pain Med., 2015, 16(Suppl. 1), S37-S43.
[http://dx.doi.org/10.1111/pme.12912] [PMID: 26461075]
[61]
Ganesh, A.; Maxwell, L.G. Pathophysiology and management of opioid-induced pruritus. Drugs, 2007, 67(16), 2323-2333.
[62]
Friedman, J.D.; Dello Buono, F.A. Opioid antagonists in the treatment of opioid-induced constipation and pruritus. Ann. Pharmacother., 2001, 35(1), 85-91.
[PMID: 17983254]
[63]
Dahan, A.; van der Schrier, R.; Smith, T.; Aarts, L.; van Velzen, M.; Niesters, M. Averting opioid-induced respiratory depression without affecting analgesia. Anesthesiology, 2018, 128(5), 1027-1037.
[http://dx.doi.org/10.1097/ALN.0000000000002184] [PMID: 29553984]
[64]
Coluzzi, F.; Bifulco, F.; Cuomo, A.; Dauri, M.; Leonardi, C.; Melotti, R.M.; Natoli, S.; Romualdi, P.; Savoia, G.; Corcione, A. The challenge of perioperative pain management in opioid-tolerant patients. Ther. Clin. Risk Manag., 2017, 13, 1163-1173.
[http://dx.doi.org/10.2147/TCRM.S141332] [PMID: 28919771]
[65]
Benyamin, R.; Trescot, A.M.; Datta, S.; Buenaventura, R.; Adlaka, R.; Sehgal, N.; Glaser, S.E.; Vallejo, R. Opioid complications and side effects. Pain Physician, 2008, 2(11), S105-S120.
[http://dx.doi.org/10.36076/ppj.2008/11/S105] [PMID: 18443635]
[66]
DuPen, A.; Shen, D.; Ersek, M. Mechanisms of opioid-induced tolerance and hyperalgesia. Pain Manag. Nurs., 2007, 8(3), 113-121.
[http://dx.doi.org/10.1016/j.pmn.2007.02.004] [PMID: 17723928]
[67]
Crofford, L.J. Adverse effects of chronic opioid therapy for chronic musculoskeletal pain. Nat. Rev. Rheumatol., 2010, 6(4), 191-197.
[http://dx.doi.org/10.1038/nrrheum.2010.24] [PMID: 20357788]
[68]
Farmer, A.D.; Drewes, A.M.; Chiarioni, G.; De Giorgio, R.; O’Brien, T.; Morlion, B.; Tack, J. Pathophysiology and management of opioid-induced constipation: European expert consensus statement. United European Gastroenterol. J., 2019, 7(1), 7-20.
[http://dx.doi.org/10.1177/2050640618818305] [PMID: 30788113]
[69]
Webster, L.R. Opioid-induced constipation. Pain Med., 2015, 16(Suppl. 1), S16-S21.
[http://dx.doi.org/10.1111/pme.12911] [PMID: 26461071]
[70]
Tabbers, M.M.; DiLorenzo, C.; Berger, M.Y.; Faure, C.; Langendam, M.W.; Nurko, S.; Staiano, A.; Vandenplas, Y.; Benninga, M.A. Evaluation and treatment of functional constipation in infants and children: Evidence-based recommendations from ESPGHAN and NASPGHAN. J. Pediatr. Gastroenterol. Nutr., 2014, 58(2), 258-274.
[http://dx.doi.org/10.1097/MPG.0000000000000266] [PMID: 24345831]
[71]
Klaschik, E.; Nauck, F.; Ostgathe, C. Constipation? Modern laxative therapy. Support. Care Cancer, 2003, 11(11), 679-685.
[http://dx.doi.org/10.1007/s00520-003-0525-x] [PMID: 14505158]
[72]
Portalatin, M.; Winstead, N. Medical management of constipation. Clin. Colon Rectal Surg., 2012, 25(1), 012-019.
[http://dx.doi.org/10.1055/s-0032-1301754] [PMID: 23449608]
[73]
Schiller, L.R. The therapy of constipation. Aliment. Pharmacol. Ther., 2001, 15(6), 749-763.
[http://dx.doi.org/10.1046/j.1365-2036.2001.00982.x] [PMID: 11380313]
[74]
Garner, CE; Matthews, HB; Burka, LT; Pharmacol, LTTA Phenolphthalein metabolite inhibits catechol-o-methyltransferase-mediated metabolism of catechol estrogens: A possible mechanism for carcinogenicity. Toxicol. Appl. Pharmacol, 2000, 162(2), 124-131.
[http://dx.doi.org/10.1006/taap.1999.8830]
[75]
French, D.; Wu, A.H.B. Cardiac markers. The Immunoassay Handbook, (4th ed. ) 2013, 1, 817-831.
[http://dx.doi.org/10.1016/B978-0-08-097037-0.00066-X]
[76]
Leppert, W.; Zajaczkowska, R.; Wordliczek, J. The role of oxycodone/naloxone in the management of patients with pain and opioid-induced constipation. Expert Opin. Pharmacother., 2019, 20(5), 511-522.
[http://dx.doi.org/10.1080/14656566.2018.1561863] [PMID: 30625013]
[77]
Mynttinen, E.; Wester, N.; Lilius, T.; Kalso, E.; Mikladal, B.; Varjos, I.; Sainio, S.; Jiang, H.; Kauppinen, E.I.; Koskinen, J.; Laurila, T. Electrochemical detection of oxycodone and its main metabolites with nafion-coated single-walled carbon nanotube electrodes. Anal. Chem., 2020, 92(12), 8218-8227.
[http://dx.doi.org/10.1021/acs.analchem.0c00450] [PMID: 32412733]
[78]
Liu, M.; Wittbrodt, E. Low-dose oral naloxone reverses opioid-induced constipation and analgesia. J. Pain Symptom Manage., 2002, 23(1), 48-53.
[http://dx.doi.org/10.1016/S0885-3924(01)00369-4] [PMID: 11779668]
[79]
Smith, K.; Hopp, M.; Mundin, G.; Bond, S.; Bailey, P.; Woodward, J.; Bell, D. Low absolute bioavailability of oral naloxone in healthy subjects. Int. J. Clin. Pharmacol. Ther., 2012, 50(5), 360-367.
[http://dx.doi.org/10.5414/CP201646] [PMID: 22541841]
[80]
Koopmans, G.; Simpson, K.; De Andrés, J.; Lux, E.A.; Wagemans, M.; Van Megen, Y. Fixed ratio (2:1) prolonged-release oxycodone/naloxone combination improves bowel function in patients with moderate-to-severe pain and opioid-induced constipation refractory to at least two classes of laxatives. Curr. Med. Res. Opin., 2014, 30(11), 2389-2396.
[http://dx.doi.org/10.1185/03007995.2014.971355] [PMID: 25265132]
[81]
Poelaert, J.; Koopmans-Klein, G.; Dioh, A.; Louis, F.; Gorissen, M.; Logé, D.; Van Op den bosch, J.; van Megen, Y.J.B. Treatment with prolonged-release oxycodone/naloxone improves pain relief and opioid-induced constipation compared with prolonged-release oxycodone in patients with chronic severe pain and laxative-refractory constipation. Clin. Ther., 2015, 37(4), 784-792.
[http://dx.doi.org/10.1016/j.clinthera.2015.02.010] [PMID: 25757607]
[82]
Bantel, C.; Tripathi, S.; Molony, D.; Heffernan, T.; Oommans, S.; Mehta, V.; Dickerson, S. Prolonged-release oxycodone/naloxone reduces opioid-induced constipation and improves quality of life in laxative-refractory patients: Results of an observational study. Clin. Exp. Gastroenterol., 2018, 11, 57-67.
[http://dx.doi.org/10.2147/CEG.S143913] [PMID: 29416370]
[83]
Jobski, K.; Kollhorst, B.; Garbe, E.; Schink, T. The risk of ischemic cardio- and cerebrovascular events associated with oxycodone–naloxone and other extended-release high-potency opioids: A nested case–control study. Drug Saf., 2017, 40(6), 505-515.
[http://dx.doi.org/10.1007/s40264-017-0511-8] [PMID: 28194654]
[84]
Sridharan, K.; Sivaramakrishnan, G. Drugs for treating opioid-induced constipation: A mixed treatment comparison network meta-analysis of randomized controlled clinical trials. J. Pain Symptom Manage., 2018, 55(2), 468-479.e1.
[http://dx.doi.org/10.1016/j.jpainsymman.2017.08.022] [PMID: 28919541]
[85]
Leppert, W.; Woron, J. The role of naloxegol in the management of opioid-induced bowel dysfunction. Therap. Adv. Gastroenterol., 2016, 9(5), 736-746.
[http://dx.doi.org/10.1177/1756283X16648869] [PMID: 27582887]
[86]
Culpepper-Morgan, J.A.; Inturrisi, C.E.; Portenoy, R.K.; Foley, K.; Houde, R.W.; Marsh, F.; Kreek, M.J. Treatment of opioid-induced constipation with oral naloxone: A pilot study. Clin. Pharmacol. Ther., 1992, 52(1), 90-95.
[http://dx.doi.org/10.1038/clpt.1992.106] [PMID: 1623695]
[87]
Wald, A. Update on the management of constipation. JAMA, 2019, 322(22), 2239-2240.
[http://dx.doi.org/10.1001/jama.2019.16029] [PMID: 31682683]
[88]
Chamberlain, B.H.; Cross, K.; Winston, J.L.; Thomas, J.; Wang, W.; Su, C.; Israel, R.J. Methylnaltrexone treatment of opioid-induced constipation in patients with advanced illness. J. Pain Symptom Manage., 2009, 38(5), 683-690.
[http://dx.doi.org/10.1016/j.jpainsymman.2009.02.234] [PMID: 19713070]
[89]
Iyer, S.S.; Randazzo, B.P.; Tzanis, E.L.; Schulman, S.L.; Zhang, H.; Wang, W.; Manley, A.L. Effect of subcutaneous methylnaltrexone on patient-reported constipation symptoms. Value Health, 2011, 14(1), 177-183.
[http://dx.doi.org/10.1016/j.jval.2010.11.003] [PMID: 21211500]
[90]
Tsuruda, P.R.; Vickery, R.G.; Long, D.D.; Armstrong, S.R.; Beattie, D.T. The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist. Naunyn Schmiedebergs Arch. Pharmacol., 2013, 386(6), 479-491.
[http://dx.doi.org/10.1007/s00210-013-0850-7] [PMID: 23549670]
[91]
Armstrong, S.R.; Campbell, C.B.; Richardson, C.L.; Vickery, R.G.; Tsuruda, P.R.; Long, D.D.; Hegde, S.S.; Beattie, D.T. The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity. Naunyn Schmiedebergs Arch. Pharmacol., 2013, 386(6), 471-478.
[http://dx.doi.org/10.1007/s00210-013-0844-5] [PMID: 23512167]
[92]
Vickery, R.; Webster, L.; Li, Y.; Singla, N.; Canafax, D. (406) Axelopran phase 2B study demonstrates a sustained increase in bowel movement frequency in patients regardeless of duration of opioid-induced constipation. J. Pain, 2014, 15(4), S77.
[http://dx.doi.org/10.1016/j.jpain.2014.01.317]
[93]
Coluzzi, F.; Scerpa, M.S.; Pergolizzi, J. Naldemedine: A new option for OIBD. J. Pain Res., 2020, 13, 1209-1222.
[http://dx.doi.org/10.2147/JPR.S243435] [PMID: 32547183]
[94]
Ohnishi, S.; Fukumura, K.; Kubota, R.; Wajima, T. Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects. Xenobiotica, 2019, 49(9), 1044-1053.
[http://dx.doi.org/10.1080/00498254.2018.1536815] [PMID: 30351180]
[95]
Blair, H.A. Naldemedine: A review in opioid-induced constipation. Drugs, 2019, 79(11), 1241-1247.
[http://dx.doi.org/10.1007/s40265-019-01160-7] [PMID: 31267482]
[96]
Inagaki, M.; Kume, M.; Tamura, Y.; Hara, S.; Goto, Y.; Haga, N.; Hasegawa, T.; Nakamura, T.; Koike, K.; Oonishi, S.; Kanemasa, T.; Kai, H. Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects. Bioorg. Med. Chem. Lett., 2019, 29(1), 73-77.
[http://dx.doi.org/10.1016/j.bmcl.2018.11.007] [PMID: 30446313]
[97]
Watari, R.; Matsuda, A.; Ohnishi, S.; Hasegawa, H. Minimal contribution of P-gp on the low brain distribution of naldemedine, a peripherally acting μ-opioid receptor antagonist. Drug Metab. Pharmacokinet., 2019, 34(2), 126-133.
[http://dx.doi.org/10.1016/j.dmpk.2018.12.002] [PMID: 30770183]
[98]
Kanemasa, T.; Koike, K.; Arai, T.; Ono, H.; Horita, N.; Chiba, H.; Nakamura, A.; Morioka, Y.; Kihara, T.; Hasegawa, M. Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation. Neurogastroenterol. Motil., 2019, 31(5), e13563.
[http://dx.doi.org/10.1111/nmo.13563] [PMID: 30821019]
[99]
Fukumura, K.; Yokota, T.; Baba, Y.; Arjona Ferreira, J.C. Phase 1, randomized, double-blind, placebo-controlled studies on the safety, tolerability, and pharmacokinetics of naldemedine in healthy volunteers. Clin. Pharmacol. Drug Dev., 2018, 7(5), 474-483.
[http://dx.doi.org/10.1002/cpdd.387] [PMID: 28960888]
[100]
Webster, L.R.; Yamada, T.; Arjona Ferreira, J.C. A phase 2b, randomized, double-blind placebo-controlled study to evaluate the efficacy and safety of naldemedine for the treatment of opioid-induced constipation in patients with chronic noncancer pain. Pain Med., 2017, 18(12), 2350-2360.
[http://dx.doi.org/10.1093/pm/pnw325] [PMID: 28371937]
[101]
Efficacy and safety of naldemedine in the treatment of opioid-induced constipation. 2017. Available from: https://www.clinicaltrials.gov/ct2/show/NCT01965158 (Accessed on: 10 Feb 2022).
[102]
Long term safety of naldemedine. Available from: https://www.clinicaltrials.gov/ct2/show/NCT01965652 (Accessed on: 10 Feb 2022).
[103]
McWilliams, V.; Whiteside, G.; McKeage, K. Linaclotide. Drugs, 2012, 72(16), 2167-2175.
[http://dx.doi.org/10.2165/11470590-000000000-00000] [PMID: 23083112]
[104]
Bryant, A.P.; Busby, R.W.; Bartolini, W.P.; Cordero, E.A.; Hannig, G.; Kessler, M.M.; Pierce, C.M.; Solinga, R.M.; Tobin, J.V.; Mahajan-Miklos, S.; Cohen, M.B.; Kurtz, C.B.; Currie, M.G. Linaclotide is a potent and selective guanylate cyclase C agonist that elicits pharmacological effects locally in the gastrointestinal tract. Life Sci., 2010, 86(19-20), 760-765.
[http://dx.doi.org/10.1016/j.lfs.2010.03.015] [PMID: 20307554]
[105]
Bassotti, G.; Usai Satta, P.; Bellini, M. Prucalopride for the treatment of constipation: A view from 2015 and beyond. Expert Rev. Gastroenterol. Hepatol., 2019, 13(3), 257-262.
[http://dx.doi.org/10.1080/17474124.2019.1568238] [PMID: 30791758]
[106]
Quigley, E.M.M. Prucalopride: Safety, efficacy and potential applications. Therap. Adv. Gastroenterol., 2012, 5(1), 23-30.
[http://dx.doi.org/10.1177/1756283X11423706] [PMID: 22282705]
[107]
Zuo, L.; Sun, Z.; Wang, Z.; Du, S.; Kong, X.; Li, L.; Yang, J.; Kang, J.; Zhang, X. Pharmacokinetics and tissue distribution study of prucalopride in rats by ultra high performance liquid chromatography with tandem mass spectrometry. J. Pharm. Biomed. Anal., 2016, 131, 246-255.
[http://dx.doi.org/10.1016/j.jpba.2016.08.030] [PMID: 27611096]
[108]
Carbone, F.; Van den Houte, K.; Clevers, E.; Andrews, C.N.; Papathanasopoulos, A.; Holvoet, L.; Van Oudenhove, L.; Caenepeel, P.; Arts, J.; Vanuytsel, T.; Tack, J. Prucalopride in gastroparesis: A randomized placebo-controlled crossover study. Am. J. Gastroenterol., 2019, 114(8), 1265-1274.
[http://dx.doi.org/10.14309/ajg.0000000000000304] [PMID: 31295161]
[109]
Camilleri, M.; Kerstens, R.; Rykx, A.; Vandeplassche, L. A placebo-controlled trial of prucalopride for severe chronic constipation. N. Engl. J. Med., 2008, 358(22), 2344-2354.
[http://dx.doi.org/10.1056/NEJMoa0800670] [PMID: 18509121]
[110]
Holder, R.M.; Rhee, D. Novel oral therapies for opioid-induced bowel dysfunction in patients with chronic noncancer pain. Pharmacotherapy, 2016, 36(3), 287-299.
[http://dx.doi.org/10.1002/phar.1711] [PMID: 26945548]
[111]
Cryer, B.; Katz, S.; Vallejo, R.; Popescu, A.; Ueno, R. A randomized study of lubiprostone for opioid-induced constipation in patients with chronic noncancer pain. Pain Med., 2014, 15(11), 1825-1834.
[http://dx.doi.org/10.1111/pme.12437] [PMID: 24716835]
[112]
Drossman, D.A.; Chey, W.D.; Johanson, J.F.; Fass, R.; Scott, C.; Panas, R.; Ueno, R. Clinical trial: Lubiprostone in patients with constipation-associated irritable bowel syndrome - Results of two randomized, placebo-controlled studies. Aliment. Pharmacol. Ther., 2009, 29(3), 329-341.
[http://dx.doi.org/10.1111/j.1365-2036.2008.03881.x] [PMID: 19006537]
[113]
Rekatsina, M.; Paladini, A.; Drewes, A.M.; Ayob, F.; Viswanath, O.; Urits, I.; Corli, O.; Pergolizzi, J., Jr; Varrassi, G. Efficacy and safety of peripherally acting μ-opioid receptor antagonist (PAMORAs) for the management of patients with opioid-induced constipation: A systematic review. Cureus, 2021, 13(7), e16201.
[http://dx.doi.org/10.7759/cureus.16201] [PMID: 34367804]

Rights & Permissions Print Cite
Article Metrics
36
5
1
1
Wayfinder Image
Open Access Journals Promotions
© 2024 Bentham Science Publishers | Privacy Policy