Novel formulations and routes of administration for opioids in the treatment of breakthrough pain

Therapy

Volumn 6, Issue 5, 2009, Pages 695-706

  Christrup, Lona Louring ^a   Lundorff, Lena ^b   Werner, Mads ^c  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b HERNING HOSPITAL   (Denmark)

^c University of Copenhagen   (Denmark)

Author keywords

Administration routes; Breakthrough pain; Opioids; Pharmaceutical formulations

Indexed keywords

ABSTRAL; EFFENTORA; FENTANYL CITRATE; INSTANYL; MORPHINE; NASALFENT; OPIATE DERIVATIVE; PARACETAMOL; PLACEBO; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; CANCER PATIENT; CLINICAL TRIAL; DRUG ABSORPTION; DRUG ADMINISTRATION ROUTE; DRUG APPROVAL; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM COMPARISON; DRUG EFFICACY; DRUG FORMULATION; DRUG INDUCED DISEASE; DRUG METABOLISM; DRUG SAFETY; FIRST PASS EFFECT; HUMAN; LOZENGE; MAXIMUM PLASMA CONCENTRATION; NASAL CAVITY IRRITATION; NAUSEA; PAIN; REVIEW; SINGLE DRUG DOSE; TRANSMUCOSAL DRUG ADMINISTRATION; TREATMENT RESPONSE; VERTIGO;

EID: 70449512784     PISSN: 14750708     EISSN: 1744831X     Source Type: Journal    
DOI: 10.2217/thy.09.51     Document Type: Review

References (91)

1. Colleau SM: The significance of breakthrough pain in cancer. Cancer Pain Release 12, 1-4 (1999)
2. Zeppetella G, Ribeiro MD: Opioids for the management of breakthrough (episodic) pain in cancer patients. Cochrane Database Syst. Rev. 25(1), CD004311 (2007)
3. Davies AN, Dickman A, Reid C, Stevens AM, Zeppetella G: The management of cancer-related breakthrough pain: recommendations of a task group of the Science Committee of the Association for Palliative Medicine of Great Britain and Ireland. Eur. J. Pain 13(4), 331-338 (2008).
4. Portenoy RK, Forbes K, Lussier D, Hanks G: Difficult pain problems: an integrated approach. In: Oxford Textbook of Palliative Medicine (3rd Edition). Doyle D, Hanks G, Cherny N, Calman K (Eds). Oxford University Press, Oxford, UK, 438-458 (2004).
5. Simmonds MA: Management of breakthrough pain due to cancer. Oncology (Huntington) 13, 1103-1108 (1999).
6. Portenoy RK, Hagen NA: Breakthrough pain: definition, prevalence and characteristics. Pain 41, 273-281 (1990).
7. Portenoy RK, Payne D, Jacobsen P: Breakthrough pain: characteristics and impact in patients with cancer pain. Pain 81, 129-134 (1999). (Pubitemid 29199908)
8. Bennett DS, Burton AW, Fishman S et al.: Consensus panel recommendation fro assessment and management of breakthrough pain Part 1. Pharmacol. Ther. 30, 296-301 (2005).
9. Gómez-Batiste X, Madrid F, Moreno F et al.: Breakthrough cancer pain: prevalence and characteristics in patients in Catalonia, Spain. J. Pain Symptom Manage. 24, 45-52 (2002). (Pubitemid 34899626)
10. Caraceni A, Martini C, Zecca E et al.: Breakthrough pain characteristics and syndromes in patients with cancer pain. An international survey. Palliat. Med. 18(3), 177-183 (2004). (Pubitemid 38771657)
11. Portenoy RK, Bennett DS, Rauck R et al.: Prevalence and characteristics of breakthrough pain in opioid-treated patients with chronic noncancer pain. J. Pain 7(8), 583-591 (2006).
12. Svendsen KB, Andersen S, Arnason S et al.:Breakthrough pain in malignant and non-malignant diseases: a review of prevalence, characteristics and mechanisms. Eur. J. Pain 9(2), 195-206 (2005) (Pubitemid 40311842)
13. Zeppetella G, O'Doherty CA, Collins S: Prevalence and characteristics of breakthrough pain in patients with non-mailgnant terminal disease admitted to a hospice. Palliat. Med. 15(3), 243-246 (2001). (Pubitemid 32479462)
14. Fortner BV, Okon TA, Portenoy RK: A survey of pain-related hospitalizations, emergency department visits, and physician office visits reported by cancer patients with and without history of breakthrough pain. J. Pain 3(1), 38-44 (2002).
15. Bailey F, Farley A: Oral opioid drugs. In: Cancer-related Breakthrough Pain. Davies A (Ed.). Oxford University Press, Oxford, UK (2006).
16. Hanks G, Roberts CJ, Davies AN: Principles of drug use in palliative medicine. In Oxford Textbook of Palliative Medicine (3rd Edition). Doyle D, Hanks G, Cherny N, Calman K (Eds). Oxford University Press, Oxford, UK, 213-225 (2004).
17. Enting RH, Mucchiano C, Oldenmenger WH et al.: The 'pain pen' for breakthrough cancer pain: a promising treatment. J. Pain Symptom Manage. 29(2), 213-217 (2005).
18. Walker G, Wilcock A, Manderson C et al.: The acceptability of different routes of administration of analgesia for breakthrough pain. Palliat. Med. 17, 219-221 (2003). (Pubitemid 36432601)
19. Sinatra R: The fentanyl HCL patient controlled transdermal system (PCTS): an alternative to intravenous patient-controlled analgesia in the postoperative setting. Clin. Pharmacokinet. 44(Suppl. 1), 1-6 (2005).
20. Viscusi ER, Siccardi M, Damaraju CV, Hewitt DJ, Kershaw P: The safety an efficacy of fentanyl iontophoretic transdermal system compared with morphine intravenous patient-controlled analgesia for postoperative pain management: an analysis of pooled data from three randomized, active-controlled clinical studies. Anesth. Analg. 105(5), 1428-1436 (2007).
21. Mayes F, Ferrone M: Fentanyl HCL patient controlled iontophoretic transdermal system for the management postoperative pain. Ann. Pharmacother. 40(12), 2178-2186 (2006)
22. Zhang H, Zhang J, Streisand JB: Oral mucosal drug delivery: clinical pharmacokinetics and therapeutic apllications. Clin. Pharmacokinet. 41, 661-680 (2002) (Pubitemid 34899033)
23. Hanks G: Oral transmucosal fentanyl citrate for the management of breakthrough pain. Eur. J. Palliat. Care 8, 6-9 (2001).
24. Thompson JW: Clinical pharmacology of opioid agonist and partial agonist. In Opioids in the Treatment of Cancer Pain. Doyle D (Ed.). Royal Society of Medicine Services Ltd, London, UK, 17-38 (1990).
25. Dale O, Hjortkjaer R, Kharasch ED: Nasal administration of opioids for pain management in adults. Acta Anaesth. Scand. 46, 759-770 (2002). (Pubitemid 34803193)
26. Lim CB, Paech MJ, Sunderland VB et al.: Pharmacokinetics of nasal fentanyl. J. Pharm. Pract. Res. 33(1), 59-63 (2003).
27. Christrup LL, Foster D, Popper LD et al.: Pharmacokinetics, efficacy and tolerability of fentanyl following intranasal versus intravenous administration in adults undergoing third-molar extraction: a randomized, double-blind, double-dummy, two-way, crossover study. Clin. Ther. 30(3), 469-481 (2008)
28. Moksnes K, Fredheim OM, Klepstad K et al.: Early pharmacokinetics of nasal fentanyl: Is there a significant arterio-venous difference? Eur. J. Clin. Pharmacol. 64, 497-502 (2008).
29. Galinkin JL, Fazi LM, Cuy RM et al.: Use of intranasal fentanyl in children undergoing myringotomy and tube placement during halothane and sevoflurane anesthesia. Anesthesiology 93, 1378-1383 (2000).
30. Borland ML, Jacobs I, Geelhoed G: Intranasal fentanyl reduces acute pain in children in the emergency department: a safety and efficacy study. Emerg. Med. (Fremantle) 14, 275-280 (2002).
31. Striebel HW, Pommerening J, Rieger A: Intranasal fentanyl titration for postoperative pain management in an unselected population. Anaesthesia 48, 753-757 (1993). (Pubitemid 23268718)
32. Striebel HW, Koenigs D, Krämer J: Postoperative pain management by intranasal demand-adapted fentanyl titration. Anesthesiology 77, 281-285 (1992).
33. Striebel HW, Olmann T, Spies C, Brummer G: Patient-controlled intranasal analgesia (PCINA) for the management of postoperative pain: a pilot study. J. Clin. Anesth. 8, 4-8 (1996).
34. Striebel HW, Oelmann T, Spies C et al.: Patient-controlled intranasal analgesia: a method for noninvasive postoperative pain management. Anesth. Analg. 83, 548-551 (1996)
35. Toussaint S, Maidl J, Schwagmeier R, Striebel HW: Patient-controlled intranasal analgesia: effective alternative to intravenous PCA for postoperative pain relief. Can. J. Anaesth. 47, 299-302 (2000). (Pubitemid 30812244)
36. Manjushree R, Lahiri A, Ghosh BR et al.: Intranasal fentanyl provides adequate postoperative analgesia in pediatric patients. Can. J. Anaesth. 49, 190-193 (2002). (Pubitemid 34189346)
37. Paech MJ, Lim CB, Banks SL et al.: A new formulation of nasal fentanyl spray for postoperative analgesia: a pilot study. Anaesthesia 58, 740-744 (2003).
38. Wong P, Chadwick FD, Karovits J: Intranasal fentanyl for postoperative analgesia after elective Caesarean section. Anaesthesia 58, 818-819 (2003). (Pubitemid 36934601)
39. Finn J, Wright J, Fong J et al.: A randomised crossover trial of patient controlled intranasal fentanyl and oral morphine for procedural wound care in adult patients with burns. Burns 30, 262-268 (2004). (Pubitemid 38479907)
40. Borland ML, Bergesio R, Pascoe EM et al.: Intranasal fentanyl is an equivalent analgesic to oral morphine in paediatric burn patients for dressing changes: a randomised double blind crossover study. Burns 31, 831-837 (2005). (Pubitemid 41394138)
41. Zeppetalla G: An assessment of safety, efficacy, and acceptability of intranasal fentanyl citrate in the management of cancer related breakthrough pain: a pilot study. J. Pain Symptom Manage. 20, 253-258 (2000).
42. Duncan A: The use of fentanyl and alfentanil sprays for episodic pain. Palliat. Med. 16, 550 (2002).
43. Pavis H, Wilcock A, Edgecombe J et al.: Pilot study of nasal morphine-chitosan for the relief of breakthrough pain in patients with cancer. J. Pain Symptom Manage. 24, 598-602 (2002). (Pubitemid 36120449)
44. Coyne P: The use of nebulized fentanyl for the management of dyspnea. Clin. J. Oncol. Nurs. 7(3), 34-35 (2003).
45. Zeppetella G: Nebulized and intranasal fentanyl in the management of cancer-related breakthrough pain. Palliat. Med. 14, 57-58 (2000).
46. Overhoff KA, Clayborough R, Crowley M: Review of the TAIFUN® multidose dry powder inhaler technology. Drug Dev. Ind. Pharm.34, 960-965 (2008).
47. Streisand JB, Varvel JR, Stanski DR et al.: Absorption and bioavailability of oral transmucosal fentanyl citrate. Anesthesiology 75, 223-229 (1999).
48. Streisand JB, Busch MA, Egan TD, Smith BG, Gay M, Pace NL: Dose proportionality and pharmacokinetics of oral transmucosal fentanyl citrate. Anesthesiology 88(2), 305-309 (1998). (Pubitemid 28081188)
49. Portenoy RK, Payne R, Coluzzi P et al.: Oral transmucosal fentanyl citrate (OTFC) for the treatment of breakthrough pain in cancer patients: a controlled dose titration study. Pain 79(2-3), 303-312 (1999). (Pubitemid 29076765)
50. Coluzzi PH, Schwartzberg L, Conroy JD et al.: Breakthrough cancer pain: a randomized trial comparing oral transmucosal fentanyl citrate (OTFC) and morphine sulfate immediate release (MSIR). Pain 91(1-2), 123-130 (2001).
51. Taylor DR, Webster LR, Chun SY et al.: Impact of breakthrough pain on quality of life in patients with chronic, noncancer pain: patient perceptions and effect of treatment with oral transmucosal fentanyl citrate (OTFC, ACTIQ). Pain Med. 8(3), 281-288 (2007).
52. Farrar Jt, Cleray J, Rauch R et al.: Oral transmucosal fentanyl citrate: randomized, double blind, placebo-controlled trial for the treatment of breakthrough pain in cancer patients. J. Natl Cancer Inst. 90, 611-616 (1998).
53. Payne R, Coluzzi P, Hart L et al.: Long-term safety of oral transmucosal fentanyl citrate for breakthrough cancer pain. J. Pain Symptom Manage. 22, 575-583 (2001). (Pubitemid 32547445)
54. Mercadante S, Villari P, Ferrera P, Casuccio A, Mangione S, Intravaia G: Transmucosal fentanyl vs intravenous morphine in doses proportional to basal opioid regimen for episodic-breakthrough pain. Br. J. Cancer 96(12), 1828-1833 (2007).
55. Zeppetella G: Opioids for cancer breakthrough pain: a pilot study reporting patient assessment of time to meaningful pain relief. J. Pain Symptom Manage. 35, 563-567 (2008).
56. Mystakidou K, Katsouda E, Parpa E, Vlahos L, Tsiatas ML: Oral transmucosal fentanyl citrate: overview of pharmacological and clinical characteristics. Drug Deliv. 13(4), 269-276 (2006).
57. Mystakidou K, Tsilika , Tsiatas M, Vlahos L: Oral transmucosal fentanyl citrate in cancer pain management: a practical application of nanotechnology. Int. J. Nanomedicine 2(1), 49-54 (2007). (Pubitemid 46901781)
58. Durfee S, Messina J, Khankari R: Fentanyl effervescent buccal tablets. Am. J. Drug Deliv. 4, 1-5 (2006).
59. Pather SI, Siebert JM, Hontz J, Khankari RK, Gupte SV, Kumbale R: Enhanced buccal delivery of fentanyl using the oravescent drug delivery system. Drug Deliv. Technol. 1, 54-57 (2001).
60. Darwish M, Kirby M, Robertson P Jr, Tracewell W, Jiang JG: Absolute and relative bioavailability of fentanyl buccal tablet and oral transmucosal fentanyl citrate. J. Clin. Pharmacol. 47(3), 343-350 (2007). (Pubitemid 46294716)
61. Darwish M, Kirby M, Robertson P Jr, Hellriegel E, Jiang JG: Single-dose and steady-state pharmacokinetics of fentanyl buccal tablet in healthy volunteers. J. Clin. Pharmacol. 47(1), 56-63 (2007).
62. Darwish M, Tempero K, Kirby M, Thompson J: Pharmacokinetics and dose proportionality of fentanyl effervescent buccal tablets in healthy volunteers. Clin. Pharmacokinet. 44(12), 1279-1286 (2005).
63. Darwish M, Kirby M, Robertson P Jr, Tracewell W, Jiang JG: Pharmacokinetic properties of fentanyl effervescent buccal tablets: a phase I, open-label, crossover study of single-dose 100, 200, 400, and 800 microg in healthy adult volunteers. Clin. Ther. 28(5), 707-714 (2006).
64. Darwish M, Tempero K, Kirby M, Thompson J: Relative bioavailability of the fentanyl effervescent buccal tablet (FEBT) 1,080 pg versus oral transmucosal fentanyl citrate 1,600 pg and dose proportionality of FEBT 270 to 1,300 microg: a single-dose, randomized, open-label, three-period study in healthy adult volunteers. Clin. Ther. 28(5), 715-724 (2006).
65. Darwish M, Kirby M, Jiang JG: Effect of buccal dwell time on the pharmacokinetic profile of fentanyl buccal tablet. Expert Opin. Pharmacother. 8(13), 2011-2016 (2007).
66. Darwish M, Kirby M, Jiang JG, Tracewell W, Robertson P Jr: Bioequivalence following buccal and sublingual placement of fentanyl buccal tablet 400 microg in healthy subjects. Clin. Drug Investig. 28(1), 1-7 (2008) (Pubitemid 350274395)
67. Darwish M, Kirby M, Robertson P, Tracewell W, Jiang JG: Absorption of fentanyl from fentanyl buccal tablet in cancer patients with or without oral mucositis: a pilot study. Clin. Drug Investig. 27(9), 605-611 (2007). (Pubitemid 47295719)
68. Portenoy RK, Taylor D, Messina J, Tremmel L: A randomized, placebo-controlled study of fentanyl buccal tablet for breakthrough pain in opioid-treated patients with cancer. Clin. J. Pain 22(9), 805-811 (2006). (Pubitemid 44627444)
69. Weinstein SM, Messina J, Xie F: Fentanyl buccal tablet for the treatment of breakthrough pain in opioid-tolerant patients with chronic cancer pain: a long-tern open-label safety study. Cancer 115(11), 2571-12519 (2009).
70. Slatkin NE, Xie F, Messina J, Segal TJ: Fentanyl buccal tablet for relief of breakthrough pain in opioid-tolerant patients with cancer-related chronic pain. J. Support. Oncol. 5(7), 327-334 (2007). (Pubitemid 350055013)
71. Portenoy RK, Messina J, Xie F, Peppin J: Fentanyl buccal tablet (FBT) for relief of breakthrough pain in opioid-treated patients with chronic low back pain: a randomized, placebo-controlled study. Curr. Med. Res. Opin. 23(1), 223-233 (2007). (Pubitemid 46191684)
72. Simpson DM, Messina J, Xie F, Hale M: Fentanyl buccal tablet for the relief of breakthrough pian in opioid-tolerant adult patients with chronic neuropathic pain: a multicneter, randomized, double-blind, placebo-controlled study. Clin. Ther. 29, 588-601 (2007). (Pubitemid 47016640)
73. Blick SK, Wagstaff AJ: Fentanyl buccal tablet: in breakthrough pain in opioid-tolerant patients with cancer. Drugs 66(18), 2387-2393 (2006).
74. Lecybyl R, Hanna M: Fentanyl buccal tablet: fast rescue analgesia for breakthrough pain. Future Oncol. 3(4), 376-379 (2007).
75. Darwish M, Messina J: Clinical pharmacology of fentanyl buccal tablet for the treatment of breakthrough pain. Expert Rev. Clin. Pharmacol. 1(1), 39-47 (2008).
76. Messina J, Darwish M, Fine PG: Fentanyl buccal tablet. Drugs Today 44(1), 41-54 (2008).
77. Bredenberg S, Duberg M, Lennernäs B et al.: In vitro and in vivo evaluation of a new sublingual tablet system for rapid oromucocal absorption using fentanyl citrate as the active susbtance. Eur. J. Pharm. Sci. 20(3), 327-334 (2003). (Pubitemid 37338538)
78. Lennernäs B, Hedner T, Holmberg M, Bredenberg S, Nyström C, Lennernäs H: Pharmacokinetics and tolerability of different doses of fentanyl follwong sublingual administration of a rapidly dissolving tablet to cancer patients; a new approach to treatment of incident pain. Br. J. Clin. Pharmacol. 59(2), 249-253 (2005).
79. Loch U, Farrell F, Kilborn J, Tamaoka M, Derrick R, Howell J: Pharmacokinetics and tolerability of sublingual fentanyl in healthy Japenese and Caucasian volunteers: Phase I. Open-label single-dose study. Proceedings of the 13th International Pain Clinica Congress - World Society of Pain Clinicians. Seoul, Korea, 26-31 May, 2008 (Abstract WSPC01-027).
80. Lennernäs B, Derrick R, Howell J: Efficacy and tolerability of sublingual fentanyl tablet in opioid-tolerant cancer patients with breakthrough pain: Phase II, radomised double-blind crossover study. Presented at: The 13th International Pain Clinical Congress - World Society of Pain Clinicians. Seoul, Korea, 26-31 May 2008 (Abstract WSPC02-023).
81. Rauck R, Derrick R, Howell J: Efficacy and tolerability of sublingual fentanyl in opioid-tolerant cancer patients with break-through pain: interim findings from two long-term, Phase II multi-centre studies. Presented at: The 5th World Congress Worlds Institute of Pain (WIP). New York, NY, USA, 13-16 March 2009 (Abstract).
82. Kress HG, Oroñska A, Kaczmarek Z, Kaasa S, Colberg T, Nolte T: Efficacy and tolerability of fentanyl intranasal fentanyl spray 50 to 200 μg for breakthrough pain in patients with cancer: a Phase III, multinational, double-blind, randomized, placebo-controlled cross-over trial with a 10-month open-label extension treatment period. Clin. Ther. (2009) (Epub ahead of print).
83. Watts P, Smith A: PecSys: in situ gelling system for optimised nasal drug delivey. Expert Opin. Drug Deliv. 6(5), 543-552 (2009).
84. Davies G, Fisher A, Knight A, Love R: NasalFent, a novel intranasal formulation of fentanyl, is well-tolerated during treatment of breakthrough cancer pain. Proceedings of the 10th Congress of the European Association for Palliative Care. Budapest, Hungary, 7-9 June 2007 (Oral abstract 25).
85. Davies G, Fisher A, Knight A, Love R: NasalFent, a novel intranasal formulation of fentanyl, is rapidly effective and well-tolerated during treatment of breakthrough cancer pain. Proceedings of the 10th Congress of the European Association for Palliative Care. Budapest, Hungary, 7-9 June 2007 (Poster abstract 711).
86. Davies G, Fisher A, Knight A, Love R: Rapid pain relief with fentanyl citrate nasal spray (NasalFent) in cancer patients with breakthrough pain. Proceedings of the 10th Congress of the European Association for Palliative Care. Budapest, Hungary, 7-9 June 2007 (Poster abstract 712).
87. Portenoy R, Burton A, Wallace M, Rauck R, Galan V, TaylorD: The efficay, onset of action and tolerabilty of fentanyl pectin nasal spray (FPNS) with PecSys® in the treatment of breakthrough cancer pain (BTCP): a multicentre, placebo-controlled, doubleblind crossover study. Abstracts of the 11th Congress of the European Association for Palliative Care. Vienna, Austria, 7-10 May 2009 (Poster abstract PE.2.S312).
88. Markman JD: Not so fast: the reformulation of fentanyl and breakthrough chronic non-cancer pain. Pain 136(3), 227-229 (2008).
89. Hojsted J, Sjogren P: Addiction to opioids in chronic pain patients: a literature review. Eur. J. Pain 11, 490-518 (2007).
90. Hagen NA, Fisher K, Victorino C, Farrar JT: A titration strategy is needed to manage breakthrough cancer pain effectively: observations from data pooled from three clinical trials. J. Palliat. Med. 10, 47-55 (2007). (Pubitemid 46238952)
91. Akela Fentanyl Taifun® product overview www.akelapharma.com/products. html (Accessed August 26, 2009)