Fentanyl buccal tablet for the treatment of breakthrough pain: Pharmacokinetics of buccal mucosa delivery and clinical efficacy

Perspectives in Medicinal Chemistry

Volumn 2010, Issue 4, 2010, Pages 11-21

  Darwish, Mona ^a   Hamed, Ehab ^b   Messina, John ^a  

^a CEPHALON INC   (United States)

^b CIMA Labs Inc Minnesota   (United States)

Author keywords

Breakthrough pain; Buccal mucosal delivery; Clinical efficacy; Fentanyl buccal tablet

Indexed keywords

FENTANYL CITRATE; MORPHINE; OPIATE; OTFC; OXYCOCET; OXYCODONE; PLACEBO; UNCLASSIFIED DRUG;

ANALGESIA; ANALGESIC ACTIVITY; APPLICATION SITE REACTION; ARTHRALGIA; ASTHENIA; BACKACHE; BLOOD BRAIN BARRIER; BREAKTHROUGH PAIN; CANCER PAIN; CHEEK MUCOSA; CLINICAL TRIAL; CONSTIPATION; DIZZINESS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM COMPARISON; DRUG EFFICACY; DRUG FORMULATION; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG OVERDOSE; DRUG PENETRATION; DRUG SAFETY; DRUG SOLUBILITY; DRUG TOLERABILITY; DRUG TOLERANCE; DRUG UPTAKE; DRUG WITHDRAWAL; DYSGEUSIA; FATIGUE; GASTROINTESTINAL ABSORPTION; HUMAN; LOW BACK PAIN; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NEUROPATHIC PAIN; OUTCOME ASSESSMENT; PAIN; PLASMA CONCENTRATION-TIME CURVE; PNEUMONIA; REVIEW; SOMNOLENCE; THORAX PAIN; TIME TO MAXIMUM PLASMA CONCENTRATION; VOMITING; XEROSTOMIA;

EID: 77955546409     PISSN: None     EISSN: 1177391X     Source Type: Journal    
DOI: 10.4137/pmc.s3928     Document Type: Review

References (37)

1. Portenoy RK, Hagen NA. Breakthrough pain: definition, prevalence and characteristics. Pain. 1990;41:273-81.
2. Portenoy RK, Payne D, Jacobsen P. Breakthrough pain: characteristics and impact in patients with cancer pain. Pain. 1999;81:129-34.
3. Bennett D, Burton AW, Fishman S, et al. Consensus panel recommendations for the assessment and management of breakthrough pain. Part 2. Management. P&T. 2005;30:354-61.
4. Portenoy RK, Bennett DS, Rauck R, et al. Prevalence and characteristics of breakthrough pain in opioid-treated patients with chronic noncancer pain. J Pain. 2006;7:583-91.
5. Hwang SS, Chang VT, Kasimis B. Cancer breakthrough pain characteristics and responses to treatment at a VA medical center. Pain. 2003;101:55-64.
6. FENTORA [package insert]. Salt Lake City, UT: Cephalon, Inc.; December 2009.
7. Stanley TH. Fentanyl. J Pain Symptom Manage. 2005;29(5 Suppl):S67-71.
8. Fine PG, Portenoy RK. A Clinical Guide to Opioid Analgesia. 2nd ed. New York, NY: Vendome Group Health Care Division; 2007.
9. Ballantyne JC. The Massachusetts General Hospital Handbook of Pain Management. 3rd ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005.
10. Labroo RB, Paine MF, Thummel KE, Kharasch ED. Fentanyl metabolism by human hepatic and intestinal cytochrome P450 3A4: implications for interindividual variability in disposition, efficacy, and drug interactions. Drug Metab Dispos. 1997;25:1072-80.
11. Streisand JB, Varvel JR, Stanski DR, et al. Absorption and bioavailability of oral transmucosal fentanyl citrate. Anesthesiology. 1991;75:223-9.
12. Nicolazzo JA, Reed BL, Finnin BC. Buccal penetration enhancers-how do they really work? J Control Release. 2005;105:1-15.
13. Shojaei AH. Buccal mucosa as a route for systemic drug delivery: a review. J Pharm Pharm Sci. 1998;1:15-30.
14. ACTIQ [package insert]. Salt Lake City, UT: Cephalon, Inc.; 2009.
15. Durfee S, Messina J, Khankari R. Fentanyl effervescent buccal tablets: enhanced buccal absorption. Am J Drug Deliv. 2006;4:1-5.
16. 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. 2007;47:343-50.
17. Eichman JD, Robinson JR. Mechanistic studies on effervescent-induced permeability enhancement. Pharm Res. 1998;15:925-30.
18. ® drug delivery system: a novel technology for the transmucosal delivery of drugs. In: Rathbone MJ, Hadgraft J, Roberts MS, Lane ME, editors. Modified-Release Drug Delivery Technology. 2nd Edition ed. Vol 1. New York, NY: Informa Healthcare USA, Inc.; 2008. p. 83-92.
19. Pather SI, Siebert JM, Hontz J, Khankari R, Kumbale R, Gupte S. Enhanced buccal delivery of fentanyl using the OraVescent drug delivery system. Drug Deliv Technol. 2001;1:54-7.
20. Darwish M, Tempero K, Kirby M, Thompson J. Pharmacokinetics and dose proportionality of fentanyl effervescent buccal tablets in healthy volunteers. Clin Pharmacokinet. 2005;44:1279-86.
21. Darwish M, Kirby M, Robertson P Jr, Tracewell W, Jiang JG. Pharmacokinetic properties of fentanyl effervescent buccal tablets: a phase I, openlabel, crossover study of single-dose 100, 200, 400, and 800 microg in healthy adult volunteers. Clin Ther. 2006;28:707-14.
22. Darwish M, Tempero K, Kirby M, Thompson J. Relative bioavailability of the fentanyl effervescent buccal tablet (FEBT) 1,080 mcg versus oral transmucosal fentanyl citrate 1,600 mcg and dose proportionality of FEBT 270 to 1,300 mcg: a single-dose, randomized, open-label, three-period study in healthy adult volunteers. Clin Ther. 2006;28:715-24.
23. 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. 2007;47:56-63.
24. Darwish M, Kirby M, Robertson P, Tracewell W, Xie F. Dose proportionality of fentanyl buccal tablet 600 to 1300 μg in healthy volunteers [abstract 278]. J Pain. 2009;10(Suppl):S44.
25. Darwish M, Kirby M, Jiang JG. Effect of buccal dwell time on the pharmacokinetic profile of fentanyl buccal tablet. Expert Opin Pharmacother. 2007;8:2011-6.
26. Darwish M, Kirby M, Jiang JG, Tracewell W, Robertson P Jr. Bioequivalence following buccal and sublingual placement of fentanyl buccal tablet 400 g in healthy subjects. Clin Drug Investig. 2008;28:1-7.
27. Farrar JT, Michna E, Messina J, Xie F. Fentanyl buccal tablet (FBT) in opioid-tolerant patients with non-cancer-related breakthrough pain (BTP) on around-the-clock opioids: a 12-week study using a novel double-blind, placebo-controlled design [abstract 130]. Pain Med. 2008;9:102.
28. 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. 2006;22:805-11.
29. 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. 2007;23:223-33.
30. Simpson DM, Messina J, Xie F, Hale M. Fentanyl buccal tablet for the relief of breakthrough pain in opioid-tolerant adult patients with chronic neuropathic pain: a multicenter, randomized, double-blind, placebo-controlled study. Clin Ther. 2007;29:588-601.
31. 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. 2007;5:327-34.
32. Farrar JT, Portenoy RK, Berlin JA, Kinman JL, Strom BL. Defining the clinically important difference in pain outcome measures. Pain. 2000;88:287-94.
33. Moore RA, McQuay HJ. Prevalence of opioid adverse events in chronic non-malignant pain: systematic review of randomised trials of oral opioids. Arthritis Res Ther. 2005;7:R1046-51.
34. 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-term, open-label safety study. Cancer. 2009;11:2571-2579.
35. Fine PG, Messina J, Xie F, Rathmell J. Long-term safety and tolerability of fentanyl buccal tablet for the treatment of breakthrough pain in opioidtolerant patients with chronic pain: an 18-month study. J Pain Symptom Manage. 2010. Accepted for publication.
36. Bredenberg S, Duberg M, Lennernas B, et al. In vitro and in vivo evaluation of a new sublingual tablet system for rapid oromucosal absorption using fentanyl citrate as the active substance. Eur J Pharm Sci. 2003;20:327-34.
37. Vasisht N, Gever LN, Tagarro I, et al. Formulation selection and pharmacokinetic comparison of fentanyl buccal soluble film with oral transmucosal fentanyl citrate: a randomized, open-label, single-dose, crossover study. Clin Drug Investig. 2009;29:647-54.