Top

Published in:

01-11-2005 | Review Article

Buprenorphine in cancer pain

Author: Mellar P. Davis

Published in: Supportive Care in Cancer | Issue 11/2005

Abstract

Buprenorphine is a broad spectrum, highly lipophilic, and long-acting partial mu opioid receptor agonist that is noncross tolerant to other opioids. Buprenorphine can be given by several routes. Metabolism is through CYP3A4 and CYP2C8 and by conjugases. Constipation and sexual dysfunction appear to be less with buprenorphine than with other opioids. The recent development of a polymer matrix patch delivery system for buprenorphine prevents “dose dumping” and facilitates pain management in those unable to take oral analgesics. Sublingual buprenorphine has been combined with naloxone to prevent illicit conversion to parenteral administration. Buprenorphine has been used extensively to control cancer pain. In certain clinical situations, buprenorphine may have particular advantages over other opioids.

Lewis JW, Husbands SM (2004) The orvinols and related opioids—high affinity ligands with diverse efficacy profiles. Curr Pharm Des 10(7):717–732PubMed

Cowan A (2003) Buprenorphine: new pharmacological aspects. Int J Clin Pract 133(Suppl):3–8

Leander JD (1988) Buprenorphine is a potent kappa-opioid receptor antagonist in pigeons and mice. Eur J Pharmacol 151(3):457–461PubMed

Leander JD (1987) Buprenorphine has potent kappa opioid receptor antagonist activity. Neuropharmacology 26(9):1445–1447PubMed

Pick CG, Peter Y, Schreiber S et al (1997) Pharmacological characterization of buprenorphine, a mixed agonist–antagonist with k3 analgesia. Brain Res 744:41–46PubMed

Kamei J, Sodeyama M, Tsuda M et al (1997) Antinociceptive effect of buprenorphine in mu1-opioid receptor deficient CXBK mice. Life Sci 60(22):333–337

Negus SS, Kykstra LA (1988) Kappa antagonist properties of buprenorphine in the shock titration procedure. Eur J Pharmacol 156(1):77–86PubMed

Ide S, Minami M, Satoh M et al (2004) Buprenorphine antinociception is abolished, but naloxone-sensitive reward is retained, in mu-opioid receptor knockout mice. Neuropsychopharmacology 29(9):1956–1963CrossRef

Recker MD, Higgins GA (2004) The opioid receptor like-1 receptor agonists Ro 64–6198 (1S, 3aS-8-2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl-1-phenyl-1,3,8-triaza-spiro [4.5] decan-4-one) produces a discriminative stimulus in rats distinct from that of a mu, kappa, and delta opioid receptor agonist cue. J Pharmacol Exp Ther 311(2):652–658. DOI 10.1124/jpet.104.071423PubMed

10.

Robbie DS (1979) Trial of sublingual buprenorphine in cancer pain. Clin Pharmacol 7(Suppl):315S–317S

11.

Campora E, Merlini L, Pace M et al (1991) The incidence of narcotic-induced emesis. J Pain Symptom Manage 6(7):428–430PubMed

12.

De Conno F, Ripamonti C, Sbanotto A et al (1991) A clinical study on the use of codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine in cancer pain. J Pain Symptom Manage 6(7):423–427PubMed

13.

Kjaer M, Henriksen H, Knudsen J (1982) A comparative study of intramuscular buprenorphine and morphine in the treatment of chronic pain of malignant origin. Br J Clin Pharmacol 13(4):487–492PubMed

14.

Ventafridda V, De Conno F, Guarise G et al (1983) Chronic analgesic study on buprenorphine action in cancer pain. Comparison with pentazocine. Arzneimittelforschung 33(4):587–590PubMed

15.

Zenz M, Piepenbrock S, Tryba M et al (1985) Long-term therapy of cancer pain. A controlled study on buprenorphine. Dtsch Med Wochenschr 110(12):448–453PubMed

16.

Skaer TL (2004) Practice guidelines for transdermal opioids in malignant pain. Drugs 64(23):2629–2638PubMed

17.

Evans HC, Easthope SE (2003) Transdermal buprenorphine. Drugs 63(19):1999–2010PubMed

18.

Ibrahim RB, Wilson JG, Thorsby ME et al (2000) Effect of buprenorphine on CYP3A activity in rat and human liver. Life Sci 66(14):1293–1298PubMed

19.

Sporer KA (2004) Buprenorphine: a primer for emergency physicians. Ann Emerg Med 43(5):1–7PubMed

20.

Greenwald MK, Johanson CE, Moody DE et al (2003) Effects of buprenorphine maintenance dose on mu-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteers. Neuropsychopharmacology 28(11):2000–2009PubMed

21.

Hou Y, Tan Y, Belcheva MM et al (2004) Differential effects of gestational buprenorphine, naloxone, and methadone on mesolimbic mu opioid and ORL1 receptor G protein coupling. Brain Res Dev Brain Res 151(1–2):149–157PubMed

22.

Lutfy K, Eitan S, Bryant CD, Yang YC, Saliminejad N, Walwyn W (2003) Buprenorphine-induced antinociception is mediated by mu-opioid receptors and compromised by concomitant activation of opioid receptor-like receptors. J Neurosci 23(32):10331–10337PubMed

23.

Negus SS, Bidlac JM, Mello NK et al (2002) Delta opioid antagonist effects of buprenorphine in rhesus monkeys. Behav Pharmacol 13(7):557–570PubMed

24.

Johnson RE, Fudala PJ, Payne R (2005) Buprenorphine: considerations for pain management. J Pain Symptom Manage 29(3):297PubMed

25.

Wallenstein SL, Kaiko RJ, Rogers AG et al (1986) Crossover trials in clinical analgesic assays: studies of buprenorphine and morphine. Pharmacotherapy 6(5):228–235PubMed

26.

Bulka A, Kouya PF, Bottiger Y et al (2004) Comparison of the antinociceptive effects of morphine, methadone, buprenorphine and codeine in two substrains of Sprague–Dawley rats. Eur J Pharmacol 492:27–34PubMed

27.

Thomas JM, Hoffman BB (1993) Buprenorphine prevents and reverses the expression of chronic etorphine-induced sensitization of adenylyl cyclase in SK-N-SH human neuroblastoma cells. J Pharamacol Exp Ther 264(1):368–374

28.

Shah MV, Jones DI, Rosen M (1986) “Patient demand” postoperative analgesia with buprenorphine. Comparison between sublingual and i.m. administration. Br J Anaesth 58(5):508–511PubMed

29.

Christoph T, Kogel B, Schiene K, Meen M, De Vry J, Friderichs E (2005) Broad analgesic profile of buprenorphine in rodent models of acute and chronic pain. Eur J Pharmacol 507(1–3):87–98PubMed

30.

Schuh KJ, Johanson CE (1999) Pharmacokinetic comparison of the buprenorphine sublingual liquid and tablet. Drug Alcohol Depend 56:55–60PubMed

31.

Tantucci C, Paoletti F, Bruni B et al (1992) Acute respiratory effects of sublingual buprenorphine: comparison with intramuscular morphine. Int J Clin Pharmacol Ther Toxicol 30(6):202–207PubMed

32.

Dahan A, Yassen A, Bijl H, Romberg R, Sarton E, Teppema L (2005) Comparison of the respiratory effects of intravenous buprenorphine and fentanyl in humans and rats. Br J Anaesth 94(6):825–834. DOI 10.1093/bja/aeil45PubMed

33.

Clarot F, Pierre GJ, Vaz E et al (2003) Tramadol-benzodiazepines and buprenorphine-benzodiazepines two potentially fatal cocktails. J Clin Forensic Med 10(2):125–126PubMed

34.

Kintz P (2002) A new series of 13 buprenorphine-related deaths. Clin Biochem 35(7):513–516PubMed

35.

Gaulier JM, Marquet P, Lacassie E, Dupuy JL, Lachatre G (2000) Fatal intoxication following self-administration of a massive dose of buprenorphine. J Forensic Sci 45(1):226–228PubMed

36.

Stock C, Shum JH (2004) Buprenorphine: a new pharmacotherapy for opioid addictions treatment. J Pain Palliat Care Pharmacother 18(3):35–54PubMed

37.

Gerra G, Borella F, Zaimovic A et al (2004) Buprenorphine versus methadone for opioid dependence: predictor variables for treatment outcome. Drug Alcohol Depend 75:37–45PubMed

38.

Oreskovich MR, Saxon AJ, Ellis MLK et al (2005) A double-blind, double-dummy, randomized, prospective pilot study of the partial Mu opiate agonist, buprenorphine, for acute detoxification from heroin. Drug Alcohol Depend 77:71–79PubMed

39.

Roy SD, Roos E, Sharma K (1994) Transdermal delivery of buprenorphine through cadaver skin. J Pharm Sci 83:126–130PubMed

40.

Berson A, Fau D, Fornacciari R et al (2001) Mechanisms for experimental buprenorphine hepatotoxicity: major role of mitochondrial dysfunction versus metabolic activation. J Hepatol 34:261–269PubMed

41.

Lasseter KC, Venitz J, Eltahtawy A, Miotto J, Munera C (2001) Systemic pharmacokinetic (PK) study of buprenorphine (B) in mild to moderate chronic hepatic impairment (CHI). Clin Pharmacol Ther 69:P2 Abstract PI-4

42.

Sbrenna S, Marti M, Morari M, Calo’ G et al (2000) Modulation of 5-hydroxytryptamine efflux from rat cortical synaptosomes by opioids and nociceptin. Br J Pharmacol 130(2):425–433PubMed

43.

Dean AJ, Bell J, Christie MJ et al (2004) Depressive symptoms during buprenorphine vs. methadone maintenance: findings from a randomised, controlled trial in opioid dependence. Eur Psychiatr 19:510–513CrossRef

44.

Lindhardt K, Bagger M, Andreasen KH, Bechgaard E (2001) Intranasal bioavailability of buprenorphine in rabbit correlated to sheep and man. Int J Pharm 217(2):121–126PubMed

45.

McAleer SD, Mills RJ, Polack T et al (2003) Pharmacokinetics of high-dose buprenorphine following single administration of sublingual tablet formulations in opioid naive healthy male volunteers under a naltrexone block. Drug Alcohol Depend 72:75–83PubMed

46.

Strain EC, Mood DE, Stoller KB et al (2004) Relative bioavailability of different buprenorphine formulations under chronic dosing conditions. Drug Alcohol Depend 74:37–43PubMed

47.

Nath RP, Upton RA, Everhart ET et al (1999) Buprenorphine pharmacokinetics: relative bioavailability of sublingual tablet and liquid formulations. J Clin Pharmacol 39(6):619–623PubMed

48.

Zenz M, Piepenbrock S, Tryba M et al (1983) Sublingual buprenorphine tablets: initial clinical experiences in long-term therapy of cancer pain. Fortschr Med 101(5):191–194PubMed

49.

Harris DS, Mendelson JE, Lin ET et al (2004) Pharmacokinetics and subjective effects of sublingual buprenorphine, alone or in combination with naloxone. Clin Pharmacokinet 43(5):329–340PubMed

50.

Picard N, Cresteil T, Djebli N, Marquet P (2005) In vitro metabolism study of buprenorphine: evidence for new metabolic pathways. Drug Metab Dispos 33(5):689–695PubMed

51.

Lotsch J, Skarke C, Liefhold J et al (2004) Genetic predictors of the clinical response to opioid analgesics. Clin Pharmaocokinet 43(14):983–1013

52.

Soars MG, Ring BJ, Wrighton SA (2003) The effect of incubation conditions on the enzyme kinetics of UDP-glucuronosyltransferases. Drug Metab Dispos 31(6):762–767PubMed

53.

Green MD, King CD, Mojarrabi B et al (1998) Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos 26(6):507–512PubMed

54.

Williams JA, Hyland R, Jones BC et al (2004) Drug–drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos 32(11):1201–1208PubMed

55.

Kobayashi K, Yamamoto T, Chiba T et al (1998) Human buprenorphine N-dealkylation is catalyzed by cytochrome P450 3A4. Drug Metab Dispos 26(8):818–821PubMed

56.

Umehara K, Shimokawa Y, Miyamoto G (2002) Inhibition of human drug metabolizing cytochrome P450 by buprenorphine. Biol Pharm Bull 25(5):682–685PubMed

57.

Zhang W, Ramamoorthy Y, Tyndale RF et al (2003) Interaction of buprenorphine and its metabolite norbuprenorpine with cytochromes P450 in vitro. Drug Metab Dispos 31(6):768–772PubMed

58.

Umeda S, Harakawa N, Yamamoto M, Ueno K (2005) Effect of nonspecific binding to microsomes and metabolic elimination of buprenorphine on the inhibition of cytochrome P4502D6. Biol Pharm Bull 28(2):212–216PubMed

59.

Jones HE, Johnson RE, Jasinki DR, Milio L (2005) Randomized controlled study transitioning opioid-dependent pregnant women from short-acting morphine to buprenorphine or methadone. Drug Alcohol Depend 78(1):33–38PubMed

60.

Pasqualucci V, Tantucci C, Paoletti F et al (1987) Buprenorphine vs. morphine via the epidural route: a controlled comparative clinical study of respiratory effect and analgesic activity. Pain 29:273–286PubMed

61.

Budd K (2003) Buprenorphine and the transdermal system: the ideal match in pain management. Int J Clin Pract (Suppl) 133:9–14

62.

Coffman BL, King CD, Rios GR et al (1998) The glucuronidation of opioids, other xenobiotics, and androgen by human UGT2B7Y (268) and UGT2B7H (268). Drug Metab Dispos 26(1):73–77PubMed

63.

Sittl R, Griessinger N, Likar R (2003) Analgesic efficacy and tolerability of transdermal buprenorphine in patients with inadequately controlled chronic pain related to cancer and other disorders: a multicenter, randomized, double-blind, placebo-controlled trial. Clin Ther 25(1):150–168PubMed

64.

Sorge J, Sittl R (2004) Transdermal buprenorphine in the treatment of chronic pain: results of a phase III, multicenter, randomized, double-blind, placebo-controlled study. Clin Ther 26(11):1808–1820PubMed

65.

Likar R, Griessinger N, Sadjak A et al (2003) Transdermal buprenorphine for treatment of chronic tumor and non-tumor pain. Wien Med Wochenschr 153(13–14):317–322PubMed

66.

Cone EJ, Gorodetzky CW, Yousefnejad D et al (1984) The metabolism and excretion of buprenorphine in humans. Drug Metab Dispos 12(5):577–581PubMed

67.

Manzi R, Rizzi M, D’Elia F et al (1991) Use of buprenorphine after right hepatectomy. Minerva Anestesiol 57(6):379–382PubMed

68.

Radbruch L (2003) Buprenorphine TDS: use in daily practice, benefits for patients. Int J Clin Pract (Suppl) 133:19–22

69.

Radbruch L, Vielvoye-Kerkmeer A (2003) Buprenorphine TDS: the clinical development rationale and results. Int J Clin Pract (Suppl) 133:15–18

70.

Noda J, Umeda S, Arai T et al (1989) Continuous subcutaneous infusion of buprenorphine for cancer pain control. Clin J Pain 5(2):147–152PubMed

71.

Hashimoto Y, Utsumi T, Tanioka H et al (1991) Epidural buprenorphine or morphine for the relief of head and neck cancer pain. Anesth Prog 38(2):69–71PubMed

72.

Francaviglia N, Silvestro C, Carta F et al (1990) Subarachnoid buprenorphine administered by implantable micropumps. Acta Neurochir (Wien) 102(1–2):62–68CrossRef

73.

Lari S, Fabbri G, Mattioli R et al (1995) Epidural buprenorphine versus morphine in bone cancer pain. Minerva Anestesiol 51(11–12):609–614

74.

Ferrari A, Coccia CPR, Bertolini A et al (2004) Methadone-metabolism, pharmacokinetics and interactions. Pharmacol Res 50:551–559PubMed

75.

Robertson SA, Taylor PM, Sear JW (2003) Systemic uptake of buprenorphine by cats after oral mucosal administration. Vet Rec 152(22):675–678PubMed

76.

Iribarne C, Picart D, Dreano Y et al (1998) In vitro interactions between fluoxetine or fluvoxamine and methadone or buprenorphine. Fundam Clin Pharmacol 12:194–199PubMed

77.

Giroud C, Michaud K, Sporkert F et al (2004) A fatal overdose of cocaine associated with coingestion of marijuana, buprenorphine, and fluoxetine. Body fluid and tissue distribution of cocaine and its metabolites determined by hydrophilic interaction chromatography–mass spectrometry (HILIC-MS). J Anal Toxicol 28(6):464–474PubMed

78.

Pirnay S, Borron SW, Giudicelli CP et al (2004) A critical review of the causes of death among post-mortem toxicological investigations: analysis of 34 buprenorphine-associated and 35 methadone-associated deaths. Addiction 99(8):978–988PubMed

79.

Jappinen A, Kokki H, Naaranlahti TJ et al (1999) Stability of buprenorphine, haloperidol and glycopyrrolate mixture in a 0.9% sodium chloride solution. Pharm World Sci 21(6):272–274PubMed

80.

Feeney GF, Fairweather P (2003) Groin tissue necrosis requiring skin graft following parenteral abuse of buprenorphine tablets. Drug Alcohol Rev 22(3):359–361PubMed

81.

Bliesener N, Albrecht S, Schwager A et al (2005) Plasma testosterone and sexual function in men on buprenorphine maintenance for opioid dependence. J Clin Endocrinol Metab 90(1):203–206PubMed

82.

De Conno F, Panzeri C, Brunelli C et al (2003) Palliative care in a National Cancer Center: results in 1987 vs. 1993 vs. 2000. J Pain Symptom Manage 25(6):499–511PubMed

83.

Ostrowski MJ, Jacson AW (1979) Intra-muscular buprenorphine—clinical experience in its use for relieving pain due to malignant disease. Br J Clin Pract 33(10):286, 293PubMed

84.

Taguchi T (1982) Effect of a long-acting analgesic, buprenorphine on cancer pain a single-blind crossover comparison with pentazocine. Gan To Kagaku Ryoho 9(2):250–257PubMed

85.

Dini D, Fassio T, Gottlieb A et al (1986) Controlled study of the analgesic effect and tolerability of buprenorphine in cancer patients. Minerva Med 77(3–4):93–104PubMed

86.

De Conno F, Ripamonti C, Tamburini M et al (1987) Buprenorphine in cancer pain: cross comparison with pentazocine. Minerva Med 78(15):1177–1181PubMed

87.

De Conno F, Ripamonti C, Sbanotto A et al (1993) A clinical note on sublingual buprenorphine. J Palliat Care 9(3):44–46PubMed

88.

Brema F, Pastorino G, Martini MD et al (1996) Oral tramadol and buprenorphine in tumour pain. An Italian multicentre trial. Int J Clin Pharmacol Res 16(4–5):109–116PubMed

89.

Bono AV, Cuffari S (1997) Effectiveness and tolerance of tramadol in cancer pain. A comparative study with respect to buprenorphine. Drugs 53(Suppl 2):40–49

90.

Schriek P (2004) Treatment of cancer-related pain with transdermal buprenorphine: a report of three cases. Support Care Cancer 12:882–884PubMed

91.

PDR (2004) Physicians’ desk reference, 58th edn. Thompson, Montvale, NJ, pp 2866–2869

92.

Reidenberg B, El-Tahtawy A, Munera C et al (2001) Absolute bioavailability of a novel buprenorphine transdermal system (BTDS) applied for seven days. J Clin Pharmacol 41:1026

93.

Reidenberg B, El-Tahtaway A, Munera C et al (2001) Daily pharmacokinetic performance of a buprenorphine transdermal system (BTDS) for up to seven days. J Clin Pharmacol 41:1027

94.

Sittl R, Likar R, Nautrup BP (2005) Equipotent doses of transdermal fentanyl and transdermal buprenorphine in patients with cancer and noncancer pain: results of a retrospective cohort study. Clin Ther 27(2):225–237PubMed

Title: Buprenorphine in cancer pain
Author: Mellar P. Davis
Publication date: 01-11-2005
Publisher: Springer-Verlag
Published in: Supportive Care in Cancer / Issue 11/2005
Print ISSN: 0941-4355
Electronic ISSN: 1433-7339
DOI: https://doi.org/10.1007/s00520-005-0849-9

Webinar | 19-02-2024 | 17:30 (CET)

Keynote webinar | Spotlight on antibody–drug conjugates in cancer

Watch now

Antibody–drug conjugates (ADCs) are novel agents that have shown promise across multiple tumor types. Explore the current landscape of ADCs in breast and lung cancer with our experts, and gain insights into the mechanism of action, key clinical trials data, existing challenges, and future directions.

Dr. Véronique Diéras

Prof. Fabrice Barlesi

Developed by: Springer Medicine

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Please log in to get access to this content

Other articles of this Issue 11/2005

Society News November 2005

Quality of life and a symptom cluster associated with breast cancer treatment-related lymphedema

Awareness of diagnosis, and information-seeking behavior of hospitalized cancer patients in Greece

Information needs of patients with incurable cancer

Neoplastic fever: a neglected paraneoplastic syndrome

Assessment and treatment of symptoms among Italian medical oncologists

Keynote webinar | Spotlight on antibody–drug conjugates in cancer