Combined analgesics in (headache) pain therapy: Shotgun approach or precise multi-target therapeutics?

BMC Neurology

Volumn 11, Issue , 2011, Pages

  Straube, Andreas ^a   Aicher, Bernhard ^b   Fiebich, Bernd L ^c   Haag, Gunther ^d  

^a LUDWIG MAXIMILIANS UNIVERSITY   (Germany)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

^c UNIVERSITY OF FREIBURG   (Germany)

^d Michael Balint Klinik   (Germany)

Author keywords

Analgesics fixed dose combinations; Headache; Migraine; Multi target therapeutics; Over the counter (OTC); Pain; Side effects; Tension type headache

Indexed keywords

ACECLOFENAC; ACETYLSALICYLIC ACID; ALMOTRIPTAN; ANALGESIC AGENT; ANTIINFLAMMATORY AGENT; ANTIPYRETIC AGENT; CAFFEINE; CAFFEINE DERIVATIVE; CAFFEINE PLUS INDOMETHACIN PLUS PROCHLORPERAZINE; CYCLOOXYGENASE 2 INHIBITOR; DICLOFENAC; EXCEDRIN; IBUPROFEN; INDOMETACIN; NAPROXEN PLUS SUMATRIPTAN; NIMESULIDE; NONSTEROID ANTIINFLAMMATORY AGENT; PARACETAMOL; PARACETAMOL DERIVATIVE; PHENACETIN; PLACEBO; PROCHLORPERAZINE; PROSTAGLANDIN DERIVATIVE; RIZATRIPTAN; ROFECOXIB; SUMATRIPTAN; TOLFENAMIC ACID; TRIMEBUTINE; TRIPTAN DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ADJUVANT THERAPY; ANALGESIC ACTIVITY; CANCER PAIN; COMBINATION CHEMOTHERAPY; DRUG DEPENDENCE; DRUG EFFICACY; DRUG INDICATION; DRUG POTENTIATION; DRUG SAFETY; DRUG TARGETING; DYSMENORRHEA; HEADACHE; HUMAN; MEDICAL LITERATURE; MIGRAINE; MOLECULARLY TARGETED THERAPY; MONOTHERAPY; MYALGIA; NOCICEPTION; NONHUMAN; PAIN; PAIN ASSESSMENT; POSTOPERATIVE PAIN; POSTPARTUM PAIN; REVIEW; RISK ASSESSMENT; SINGLE DRUG DOSE; SORE THROAT; TENSION HEADACHE; THERAPY EFFECT; UPREGULATION; CLINICAL TRIAL (TOPIC); DRUG COMBINATION;

ANALGESICS; CLINICAL TRIALS AS TOPIC; DRUG COMBINATIONS; DRUG THERAPY, COMBINATION; HEADACHE; HUMANS; PAIN;

EID: 79953166836     PISSN: None     EISSN: 14712377     Source Type: Journal    
DOI: 10.1186/1471-2377-11-43     Document Type: Review

References (147)

1. Kennedy JD. Neuropathic pain: molecular complexity underlies continuing unmet medical need. J Med Chem 2007, 50:2547-2556. 10.1021/jm061023c, 17489577.
2. Cox JJ, Reimann F, Nicholas AK, Thornton G, Roberts E, Springell K, Karbani G, Jafri H, Mannan J, Raashid Y, Al-Gazali L, Hamamy H, Valente EM, Gorman S, Williams R, McHale DP, Wood JN, Gribble FM, Woods CG. An SCN9A channelopathy causes congenital inability to experience pain. Nature 2006, 444(7121):894-898. 10.1038/nature05413, 17167479.
3. Piguet V, Allaz AF. Complexite de la douleur: du savoir a la provocation [The complexity of pain and its origins - in French]. Rev Medicale Suisse 2005, 1(25):1651-1652.
4. Brooks J, Tracey I. From nociception to pain perception: imaging the spinal and supraspinal pathways. J Anat 2005, 207(1):19-33. 10.1111/j.1469-7580.2005.00428.x, 1571498, 16011543.
5. Benedetti F, Mayberg HS, Wager TD, Stohler CS, Zubieta JK. Neurobiological mechanisms of the placebo effect. J Neurosci 2005, 25(45):10390-10402. 10.1523/JNEUROSCI.3458-05.2005, 16280578.
6. Powell A, Dupré J. From molecules to systems: the importance of looking both ways. Studies in History and Philosophy of Biological and Biomedical Sciences 2009, 40:54-64. 10.1016/j.shpsc.2008.12.007, 19268874.
7. Lehar J, Krueger AS, Avery W, Heilbut AM, Johansen LM, Price ER, Rickles RJ, Short GF, Staunton JE, Jin X, Lee MS, Zimmermann GR, Borisy AA. Synergistic drug combinations tend to improve therapeutically relevant selectivity. Nature Biotechnology 2009, 27:659-666. 10.1038/nbt.1549, 2708317, 19581876.
8. Keith CT, Borisy AA, Stockwell BR. Multicomponent therapeutics for networked systems. Nature Reviews 2005, 4:1-8.
9. Zimmermann GR, Lehar J, Keith TK. Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discovery Today 2007, 12(1/2):34-42. 10.1016/j.drudis.2006.11.008, 17198971.
10. WHO Expert Committee on Specifications for Pharmaceutical Preparations Annex 5 - Guidelines for registration of fixed-dose combination medicinal products. World Health Organization. WHO Technical Report Series 2005, Geneva, No. 929, WHO Expert Committee on Specifications for Pharmaceutical Preparations.
11. Wertheimer AI, Morrison A. Combination drugs: innovation in pharmacotherapy. P&T 2002, 27:44-49.
12. Prescott LF. Pharmacological actions and therapeutic use of Paracetamol. Paracetamol (acetaminophen) - a critical bibliographic review 1996, 197-239. London, Philadelphia: Taylor and Francis, Prescott LF.
13. Insel PA. Analgesic-antipyretic and antiinflammatory agents and drugs employed in the treatment of gout. Goodman & Gilman's The Pharmacological Basis of Therapeutics 1996, 617-657. New York: Mc-Graw-Hill, Hardman JG, Limbird LE, 9.
14. Rainsford KD. Pharmacology and toxicology of ibuprofen. Ibuprofen - a critical bibliographic review 1996, 143-275. London: Taylor and Francis Ltd, Bristol, Rainsford KD.
15. Sandrini G, Cerbo R, Del Bene E, Ferrari A, Genco S, Grazioli I, Martelletti P, Nappi G, Pinessi L, Sarchielli P, Tamburro P, Uslenghi C, Zanchin G. Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, doubledummy, randomised, parallel group, multicentre study. Int J Clin Pract 2007, 61:1256-1269. 10.1111/j.1742-1241.2007.01458.x, 1974802, 17627707.
16. Galeotti N, Ghelardini C, Grazioli I, Uslenghi C. Indomethacin, caffeine and prochlorperazine alone and combined revert hyperalgesia in "in vivo" models of migraine. Pharmacol Res 2002, 46:245-50. 10.1016/S1043-6618(02)00126-3, 12220967.
17. Ghelardini C, Galeotti N, Grazioli I, Uslenghi C. Indomethacin, alone and combined with prochlorperazine and caffeine, but not sumatriptan, abolishes peripheral and central sensitization in in vivo models of migraine. J Pain 2004, 5:413-419. 10.1016/j.jpain.2004.06.008, 15501422.
18. Ghelardini C, Galeotti N, Vivoli E, Grazioli I, Uslenghi C. The central analgesia induced by antimigraine drugs is independent from Gi proteins: superiority of a fixed combination of indomethacin, prochlorperazine and caffeine, compared to sumatriptan, in an in vivo model. J Headache Pain 2009, 10:435-440. 10.1007/s10194-009-0151-1, 2778775, 19756945.
19. Cerbo R, Centonze V, Grazioli I, Tavolato B, Trenti T, Uslenghi C, Sternieri E. Efficacy of a fixed combination of indomethacin, prochlorperazine, and caffeine in the treatment of episodic tension-type headache: a double-blind, randomized, nimesulide-controlled, parallel group, multicentre trial. Eur J Neurol 2005, 12:759-767. 10.1111/j.1468-1331.2005.01056.x, 16190913.
20. Peroutka SJ. Beyond monotherapy: rational polytherapy in migraine. Headache 1998, 38:18-22. 10.1046/j.1526-4610.1998.3801018.x, 9504998.
21. Panconesi A, Pavone E, Franchini M, Mennuti N, Bartolozzi ML, Guidi L, Banfi R. Triptans: low utilization and high turnover in the general population. Cephalalgia 2010, 30:576-581.
22. Ifergane G, Wirguin I, Shvartzman P. Triptans--Why Once?. Headache 2006, 46:1261-1263. 10.1111/j.1526-4610.2006.00435.x, 16942470.
23. Krymchantowski AV. Acute treatment of migraine. Breaking the paradigm of monotherapy. BMC Neurol 2004, 4:4. 10.1186/1471-2377-4-4, 341456, 15005810.
24. Krymchantowski AV, Adriano M, Fernandes D. Tolfenamic acid decreases migraine recurrence when use with sumatriptan. Cephalalgia 1999, 19:186-187. 10.1046/j.1468-2982.1999.1903186.x, 10234467.
25. Krymchantowski AV. Naproxen sodium decreases migraine recurrence when administered with sumatriptan. Arq Neuropsiquiatr 2000, 58:428-430. 10.1590/S0004-282X2000000300006, 10920403.
26. Smith TR, Sunshine A, Stark SR, Littlefield DE, Spruill SE, Alexander WJ. Sumatriptan and naproxen sodium for the acute treatment of migraine. Headache 2005, 45:983-991. 10.1111/j.1526-4610.2005.05178.x, 16109111.
27. Brandes JL, Kudrow D, Stark SR, O'Carrol CP, Adelman JU, O'Donnell FJ, Alexander WJ, Spruill SE, Barrett PS, Lener SE. Sumatriptan-naproxen for acute treatment of migraine: a randomized trial. JAMA 2007, 297:1443-1454. 10.1001/jama.297.13.1443, 17405970.
28. Lipton RB, Dodick DW, Adelman JU, Kaniecki RG, Lener SE, White JD, Nelsen AC. Consistency of response to sumatriptan/naproxen sodium in a placebocontrolled, crossover study. Cephalalgia 2009, 29:826-836. 10.1111/j.1468-2982.2008.01806.x, 19220307.
29. Krymchantowski AV, Barbosa JS. Rizatriptan combined with rofecoxib vs. rizatriptan for the acute treatment of migraine: an open label pilot study. Cephalalgia 2002, 22:309-312. 10.1046/j.1468-2982.2002.00369.x, 12100094.
30. Krymchantowski AV, Bigal ME. Rizatriptan versus rizatriptan plus rofecoxib versus rizatriptan plus tolfenamic acid in the acute treatment of migraine. BMC Neurol 2004, 4:10. 10.1186/1471-2377-4-10, 449711, 15222892.
31. Krymchantowski AV, Filho PFM, Bigal ME. Rizatriptan vs. rizatriptan plus trimebutine for the acute treatment of migraine: a double-blind, randomized, cross-over, placebo-controlled study. Cephalalgia 2006, 26:871-874. 10.1111/j.1468-2982.2006.01136.x, 16776704.
32. Freitag F, Diamond M, Diamond S, Janssen I, Rodgers A, Skobieranda F. Efficacy and tolerability of coadministration of rizatriptan and acetaminophen vs rizatriptan or acetaminophen alone for acute migraine treatment. Headache 2008, 48:921-930. 10.1111/j.1526-4610.2007.01053.x, 18572432.
33. Schoenen J, De Klippel N, Giurgea S, Herroelen L, Jacquy J, Louis P, Monseu G, Vandenheede M, . the Belgian Headache Society Almotriptan and its combination with aceclofenac for migraine attacks: a study of efficacy and the influence of auto-evaluated brush allodynia. Cephalalgia 2008, 28:1095-1105. 10.1111/j.1468-2982.2008.01654.x, 18644036, the Belgian Headache Society.
34. Krymchantowski A, Bigal ME. Rizatriptan in migraine. Expert Rev Neurother 2005, 5:597-603. 10.1586/14737175.5.5.597, 16162083.
35. Mannix LK. A review of the 5-HT1B/1D agonist rizatriptan: update on recent research and implications for the future. Expert Opin Pharmacother 2008, 9:1001-1011. 10.1517/14656566.9.6.1001, 18377342.
36. Zhang XC, Kainz V, Jakubowski M, Burstein R, Strassman A, Levy D. Localization of COX-1 and COX-2 in the intracranial dura mater of the rat. Neurosci Lett 2009, 452:33-36. 10.1016/j.neulet.2009.01.032, 2775514, 19444941.
37. Sawynok J, Yaksh TL. Caffeine as an analgesic adjuvant: a review of pharmacology and mechanisms of action. Pharm Reviews 1993, 45:43-85.
38. Camann WR, Murray RS, Mushlin PS, Lambert DH. Effects of oral caffeine on postdural puncture headache: a double-blind, placebo-controlled trial. Anesth Analg 1990, 70:181-184. 10.1213/00000539-199002000-00009, 2405733.
39. Yücel A, Ozyalcin S, Talu GK, Yücel EC, Erdine S. Intravenous administration of caffeine sodium benzoate for postdural puncture headache. Reg Anesth Pain Med 1999, 24:51-54.
40. Halker RB, Demaerschalk BM, Wellik KE, Wingerchuk DM, Rubin DI, Crum BA, Dodick DW. Caffeine for the prevention and treatment of postdural puncture headache: debunking the myth. The Neurologist 2007, 13:323-327. 10.1097/NRL.0b013e318145480f, 17848873.
41. Ward N, Whitney C, Avery D, Dunner D. The analgesic effects of caffeine in headache. Pain 1991, 44:151-155. 10.1016/0304-3959(91)90129-L, 2052380.
42. Myers DE, Shaikh Z, Zullo TG. Hypoalgesic effect of caffeine in experimental ischemic muscle contraction pain. Headache 1997, 37:654-658. 10.1046/j.1526-4610.1997.3710654.x, 9439087.
43. Forbes JA, Beaver WT, Jones KF, Kehm CJ, Smith WK, Gongloff CM, Zeleznock JR, Smith JW. Effect of caffeine on ibuprofen analgesia in postoperative oral surgery pain. Clin Pharmacol Ther 1991, 49:674-684. 10.1038/clpt.1991.85, 2060256.
44. McQuay HJ, Angell K, Carroll D, Moore RA, Juniper RP. Ibuprofen compared with ibuprofen plus caffeine after third molar surgery. Pain 1996, 66:247-251. 10.1016/0304-3959(96)03043-6, 8880847.
45. Diamond S, Balm TK, Freitag FG. Ibuprofen plus caffeine in the treatment of tension-type headache. Clin Pharmacol Ther 2000, 68:312-319. 10.1067/mcp.2000.109353, 11014413.
46. Dooley JM, Gordon KE, Wood EP, Brna PM, MacSween J, Fraser A. Caffeine as an adjuvant to ibuprofen in treating childhood headaches. Pediatr Neurol 2007, 37:42-46. 10.1016/j.pediatrneurol.2007.02.016, 17628221.
47. Peroutka SJ, Lyon JA, Swarbrick J, Lipton RB, Kolodner K, Goldstein J. Efficacy of diclofenac sodium softgel 100 mg with or without caffeine 100 mg in migraine without aura. A randomized, double-blind, crossover study. Headache 2004, 44:136-141. 10.1111/j.1526-4610.2004.04029.x, 14756851.
48. Migliardi JR, Armellino JJ, Friedman M, Gillings DB, Beaver WT. Caffeine as an analgesic adjuvant in tension headache. Clin Pharmacol Ther 1994, 56:576-586. 10.1038/clpt.1994.179, 7955822.
49. Ali Z, Burnett I, Eccles R, North M, Jawad M, Jawad S, Clarke G, Milsom I. Efficacy of a paracetamol and caffeine combination in the treatment of the key symptoms of primary dysmenorrhoea. Cur Med Res Opinion 2007, 23:841-851.
50. Renner B, Clarke G, Grattan T, Beisel A, Mueller C, Werner U, Kobal G, Brune K. Caffeine accelerates absorption and enhances the analgesic effect of acetaminophen. J Clin Pharmacol 2007, 47:715-726. 10.1177/0091270007299762, 17442681.
51. Iqbal N, Ahmad B, Janbaz KH, Gilant AH, Niazi SK. The effect of caffeine on the pharmacokinetics of acetaminophen in man. Biopharm Drug Dispos 1995, 16:481-487. 10.1002/bdd.2510160606, 7579030.
52. Kraetsch HG, Hummel T, Lotsch J, Kussat R, Kobal G. Analgesic effects of propyphenazone in comparison to its combination with caffeine. Eur J Clin Pharmacol 1996, 49:377-382. 10.1007/BF00203781, 8866632.
53. Pini LA, Del Bene E, Zanchin G, Sarchielli P, Di Trapani G, Prudenzano MP, LaPegna G, Savi L, Di Loreto G, Dionisio P, Granella F. Tolerability and efficacy of a combination of paracetamol and caffeine in the treatment of tension-type headache: a randomised, double-blind, double-dummy, cross-over study versus placebo and naproxen sodium. J Headache Pain 2008, 9:367-373. 10.1007/s10194-008-0071-5, 18815727.
54. Forbes JA, Jones KF, Kehm CJ, Smith WK, Gongloff CM, Zeleznock JR, Smith JW, Beaver WT. Evaluation of aspirin, caffeine, and their combination in postoperative oral surgery pain. Pharmacotherapy 1990, 10:387-393.
55. Schachtel BP, Fillingim JM, Lane AC, Thoden WR, Baybutt RI. A double-blind study comparing aspirin with caffeine to aspirin and placebo in patients with sore throat. Arch Intern Med 1991, 161:733-737.
56. Laska EM, Sunshine A, Mueller F, Elvers WB, Siegel C, Rubin A. Caffeine as an analgesic adjuvant. JAMA 1984, 251:1711-1718. 10.1001/jama.251.13.1711, 6366275.
57. Bosse K, Kühner A. Behandlung von Kopfschmerzen verschiedenster Genese - Ergebnisse einer Doppelblind-Multicenter-Studie [Treatment of headache of different genesis - results of a double-blind multicenter study -in german]. Therapiewoche 1987, 38:3879-3884.
58. Lipton RB, Stewart WF, Ryan RE, Saper J, Silberstein S, Sheftell F. Efficacy and safety of acetaminophen, aspirin, and caffeine in alleviating migraine headache pain: three double-blind, randomized, placebo-controlled trials. Arch Neurol 1998, 55:210-217. 10.1001/archneur.55.2.210, 9482363.
59. Diener HC, Pfaffenrath V, Pageler L, Peil H, Aicher B. The fixed combination of acetylsalicylic acid, paracetamol and caffeine is more effective than single substances and dual combination for the treatment of headache: A multicentre, randomized, double-blind, single-dose, placebo-controlled parallel group study. Cephalalgia 2005, 25:776-787. 10.1111/j.1468-2982.2005.00948.x, 16162254.
60. Goldstein J, Silberstein SD, Saper JR, Elkind AH, Smith TR, Gallagher RM, Battikha JP, Hoffman H, Baggish J. Acetaminophen, acetylsalicyclic acid, and caffeine versus sumatriptan succinate in the early treatment of migraine: results from the ASSET trial. Headache 2005, 45:973-982. 10.1111/j.1526-4610.2005.05177.x, 16109110.
61. Goldstein J, Silberstein SD, Saper JR, Ryan RE, Lipton RB. Acetaminophen, acetylsalicyclic acid, and caffeine in combination versus ibuprofen for acute migraine: results from a multicenter, double-blind, randomized, parallel-group, single-dose, placebo-controlled study. Headache 2006, 46:444-453. 10.1111/j.1526-4610.2006.00376.x, 16618262.
62. Pageler L, Diener HC, Pfaffenrath V, Peil H, Aicher B. Clinical relevance of efficacy endpoints in OTC trials. Headache 2009, 49:646-654. 10.1111/j.1526-4610.2008.01242.x, 19472440.
63. Bergmann JF. Self-medication: from European regulatory directives to therapeutic strategy. Fundament Clin Pharmacol 2003, 17:275-280.
64. Hersh EV, Moore PA, Ross GL. Over-the-counter analgesics and antipyretics: a critical assessment. Clin Ther 2000, 22:500-548. 10.1016/S0149-2918(00)80043-0, 10868553.
65. Bundesgesundheitsamt BGA. Acetylsalicylsäure plus Coffein in fixer Kombination [Acetylsalicylic acid plus caffeine in fixed combination- in german]. Monografie der Aufbereitungskommission B 3 (Neurologie/Psychiatrie). Bundesanzeiger 1994, 46:1247-1249.
66. Bundesgesundheitsamt BGA. Paracetamol plus Coffein in fixer Kombination [Paracetamol plus caffeine in fixed combination- in german]. Monografie der Aufbereitungskommission B 3 (Neurologie/Psychiatrie). Bundesanzeiger 1988, 40:4778-4779.
67. Bach PH, Berndt WO, Delzell E, Dubach U, Finn WF, Fox JM, Hess R, Michielsen P, Sandler DP, Trump B, Williams G. A safety assessment of fixed combinations of acetaminophen and acetylsalicylic acid, coformulated with caffeine. Renal Failure 1998, 20:749-762. 10.3109/08860229809045173, 9834974.
68. McLaughlin JK, Lipworth L, Chow WH, Blot W. Analgesic use and chronic renal failure: A critical review of the epidemiologic literature. Kidney Int 1998, 54:679-686. 10.1046/j.1523-1755.1998.00043.x, 9734593.
69. Feinstein AR, Heinemann LA, Curhan GC, Delzell E, DeSchepper PJ, Fox JM, Graf H, Luft FC, Michielsen P, Mihatsch MJ, Suissa S, van der woude F, Willich S, . Ad Hoc Committee of the International Study Group on Analgesics and Nephropathy Relationship between nonphenacetin combined analgesics and nephropathy: A review. Kidney Int 2000, 58:2259-2264. 10.1046/j.1523-1755.2000.00410.x, 11115060, Ad Hoc Committee of the International Study Group on Analgesics and Nephropathy.
70. Headache Classification Subcommittee of the International Headache Society The International Classification of Headache Disorders, 2nd edition (ICHD-II). Cephalalgia 2004, 24:S9-S160. Headache Classification Subcommittee of the International Headache Society.
71. Mihatsch MJ, Khanlari B, Brunner FP. Obituary to analgesic nephropathy--an autopsy study. Nephrol Dial Transplant 2006, 21:3139-3145. 10.1093/ndt/gfl390, 16891638.
72. van der Woude FJ, Heinemann LAJ, Graf H, Lewis M, Moehner S, Assmann A, Kühl-Habich D. Analgesics use and ESRD in younger age: a case-control study. BMC Nephrology 2007, 8:15. 10.1186/1471-2369-8-15, 2222021, 18053232.
73. Michielsen P, Heinemann L, Mihatsch M, Schnülle P, Graf H, Koch KM. Non-phenacetin analgesics and analgesic nephropathy. Nephrol Dial Transplant 2009, 24:1253-1259. 10.1093/ndt/gfn643, 19037086.
74. Rexrode KM, Buring JE, Glynn RJ, Stampfer MJ, Youngman LD, Gaziano JM. Analgesic use and renal function in men. JAMA 2001, 286:315-321. 10.1001/jama.286.3.315, 11466097.
75. Hughes JR, Oliveto AH, Helzer JE, Higgins ST, Bickel WK. Should caffeine abuse, dependence, or withdrwal be added to DSM-IV and ICD-10?. Am J Psychiatry 1992, 149:33-40.
76. Dalessio DJ. On the safety of caffeine as an analgesic adjuvant. Headache Quarterly 1994, 5:125-127.
77. Fox JM, Siebers U. Caffeine as a promoter of analgesic-associated nephropathy - where is the evidence?. Fundamental Clin Pharmacol 2003, 17:377-392.
78. Murray RM. Genesis of analgesic nephropathy in the United Kingdom. Kidney Int 1978, 13:50-57. 10.1038/ki.1978.7, 713268.
79. Grimlund K. Phenacetin and renal damage at a Swedish factory. Acta Med Scand 1963, 174(Suppl. 405):1-26.
80. Fox JM. Use of analgesics in self-medication. Therapie 2002, 57:115-118.
81. Feinstein AR, Heinemann LAJ, Dalessio D, Fox JM, Goldstein J, Haag G, Ladewig D, O'Brien CP. Ad Hoc Review Committee. Do caffeine-containing analgesics promote dependence? A review and evaluation. Clin Pharmacol Ther 2000, 68:457-467. 10.1067/mcp.2000.110974, 11103748.
82. Diener HC, Tfelt-Hansen P. Headache associated with chronic use of substances. The Headaches 1993, 721-727. New York: Raven Press, Olesen J, Tfelt-Hansen P, Welch KMA.
83. Diener HC, Dahlöf CGH. Headache associated with chronic use of substances. The Headaches 2000, 871-877. Philadelphia: Williams& Williams, Olesen J, Tfelt-Hansen P, Welch KMA, 2.
84. Diener HC, Silberstein SD. Medication overuse headaches. The Headaches 2006, 971-979. Philadelphia: Lippincott Williams& Williams, Olesen J, Goadsby PJ, Ramadan NM, Tfelt-Hansen P, Welch KMA, 3.
85. Limmroth V, Katsarava Z. Medication overuse headache. Curr Opin Neurol 2004, 17:301-306. 10.1097/00019052-200406000-00011, 15167065.
86. Obermann M, Bartsch T, Katsarava Z. Medication overuse headache. Expert Opin Drug Saf 2006, 5:49-56. 10.1517/14740338.5.1.49, 16370955.
87. Haag G. Headache and medication overuse: are clinical case series appropriate to reveal differential risks of different medications?. Expert Opin Drug Saf 2010, 9:397-406. 10.1517/14740331003598857, 20166835.
88. Scher AI, Lipton RB, Stewart WF, Bigal M. Patterns of medication use by chronic and episodic headache sufferers in the general population: results from the frequent headache epidemiology study. Cephalalgia 2010, 30:321-328. 10.1177/0333102410372426, 19614708.
89. Delzell E, Haag G. Comments on results of Scher et al. pertaining to nonprescription caffeine containing combination analgesics. Cephalalgia 2010, 30:1145-1146. 10.1177/0333102410361540, 20713567.
90. Bendtsen L, Evers S, Linde M, Mitsikostas DD, Sandrini G, Schoenen J. EFNS guideline on the treatment of tension-type headache - report of an EFNS task force. Eur J Neurol 2010, 17:1318-1325.
91. Bigal ME, Serrano D, Buse D, Scher A, Stewart WF, Lipton RB. Acute migraine medications and evolution from episodic to chronic migraine: a longitudinal population-based study. Headache 2008, 48:1157-1168. 10.1111/j.1526-4610.2008.01217.x, 18808500.
92. Taubes G. Epidemiology faces its limits. Science 1995, 269:164-169. 10.1126/science.7618077, 7618077.
93. Sun-Edelstein C, Bigal ME, Rapoport AM. Chronic migraine and medication overuse headache: clarifying the current International Headache Society classification criteria. Cephalalgia 2009, 29:445-452. 10.1111/j.1468-2982.2008.01753.x, 19291245.
94. Haag G. Medication overuse headache - comments on the current International Headache Society classification criteria. Cephalalgia 2010, 30:1409-1410. 10.1177/0333102410365569, 20959438.
95. Bigal ME, Sun-Edelstein C, Rapoport A. Medication overuse headache - comments on the current International Headache Society classification criteria - author's reply. Cephalalgia 2010, 30:1410-1411.
96. Goadsby PJ. Is medication-overuse headache a distinct biological entity?. Nature Clin Pract Neurol 2006, 2:401.
97. Rueda-Sánchez M, Díaz-Martínez LA. Prevalence and associated factors for episodic and chronic daily headache in the Colombian population. Cephalalgia 2008, 28:216-225.
98. Ushikubi F, Segi E, Sugimoto Y, Murata T, Matsuoka T, Kobayashi T. Impaired febrile response in mice lacking the prostaglandin E receptor subtype EP3. Nature 1998, 395:281-284. 10.1038/26233, 9751056.
99. Zeilhofer HU, Brune K. Analgesic strategies beyond the inhibition of cyclooxygenases. Trends Pharmacol Sci 2006, 27:467-474. 10.1016/j.tips.2006.07.007, 16876882.
100. Jasmin L, Tien D, Janni G, Ohara PT. Is noradrenaline a significant factor in the analgesic effect of antidepressants?. Pain 2003, 106:3-8. 10.1016/j.pain.2003.08.010, 14581104.
101. Meves H. The action of prostaglandins on ion channels. Curr Neuropharmacol 2006, 4:41-57. 10.2174/157015906775203048, 2430679, 18615137.
102. Jenkins DW, Feniuk W, Humphrey PP. Characterization of the prostanoid receptor types involved in mediating calcitonin gene-related peptide release from cultured rat trigeminal neurones. Br J Pharmacol 2001, 134:1296-1302. 10.1038/sj.bjp.0704357, 1573048, 11704650.
103. Doods H, Hallermayer G, Wu D, Entzeroth M, Rudolf K, Engel W, Eberlein W. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol 2000, 129:420-423. 10.1038/sj.bjp.0703110, 1571877, 10711339.
104. Ho TW, Mannix LK, Fan X, Assaid C, Furtek C, Jones CJ. Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Neurology 2008, 70:1304-1312. 10.1212/01.WNL.0000286940.29755.61, 17914062.
105. Bertolini A, Ferrari A, Ottani A, Guerzoni S, Tacchi R, Leone S. Paracetamol: new vistas of an old drug. CNS Drug Rev 2006, 12:250-275. 10.1111/j.1527-3458.2006.00250.x, 17227290.
106. Hinz B, Cheremina O, Brune K. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J 2008, 22:383-390. 10.1096/fj.07-8506com, 17884974.
107. Boutaud O, Aronoff DM, Richardson JH, Marnett LJ, Oates JA. Determinants of the cellular specificity of acetaminophen as an inhibitor of prostaglandin H(2) synthases. Proc Natl Acad Sci USA 2002, 99:7130-7135. 10.1073/pnas.102588199, 124540, 12011469.
108. Graham GG, Scott KF. Mechanism of action of paracetamol. Am J Ther 2005, 12:46-55. 10.1097/00045391-200501000-00008, 15662292.
109. Fiebich BL, Lieb K, Hull M, Aicher B, van Ryn J, Pairet M, Engelhardt G. Effects of caffeine and paracetamol alone or in combination with acetylsalicylic acid on prostaglandin E(2) synthesis in rat microglial cells. Neuropharmacology 2000, 39:2205-2213. 10.1016/S0028-3908(00)00045-9, 10963764.
110. Miranda HF, Puig MM, Prieto JC, Pinardi G. Synergism between paracetamol and nonsteroidal anti-inflammatory drugs in experimental acute pain. Pain 2006, 121:22-28. 10.1016/j.pain.2005.11.012, 16480830.
111. Fiebich BL, Biber K, Lieb K, Van Calker D, Berger M, Bauer J, Gebicke-Haerter PJ. Cyclooxygenase-2 expression in rat microglia is induced by adenosine A2a-receptors. Glia 1996, 18:152-160. 10.1002/(SICI)1098-1136(199610)18:2<152::AID-GLIA7>3.0.CO;2-2, 8913778.
112. Fernandez-Duenas V, Sanchez S, Planas E, Poveda R. Adjuvant effect of caffeine on acetylsalicylic acid anti-nociception: prostaglandin E2 synthesis determination in carrageenan-induced peripheral inflammation in rat. Eur J Pain 2008, 12:157-163. 10.1016/j.ejpain.2007.03.485, 17507271.
113. Cupini LM, Bari M, Battista N, Argiro G, Finazzi-Agro A, Calabresi P, Maccarrone M. Biochemical changes in endocannabinoid system are expressed in platelets of female but not male migraineurs. Cephalalgia 2006, 26:277-281. 10.1111/j.1468-2982.2005.01031.x, 16472333.
114. Akerman S, Kaube H, Goadsby PJ. Anandamide is able to inhibit trigeminal neurons using an in vivo model of trigeminovascular-mediated nociception. J Pharmacol Exp Ther 2004, 309:56-63. 10.1124/jpet.103.059808, 14718591.
115. Patwardhan AM, Jeske NA, Price TJ, Gamper N, Akopian AN, Hargreaves KM. The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin. Proc Natl Acad Sci USA 2006, 103:11393-11398. 10.1073/pnas.0603861103, 1544096, 16849427.
116. Dani M, Guindon J, Lambert C, Beaulieu P. The local antinociceptive effects of paracetamol in neuropathic pain are mediated by cannabinoid receptors. Eur J Pharmacol 2007, 573:214-215. 10.1016/j.ejphar.2007.07.012, 17651722.
117. Slanina KA, Schweitzer P. Inhibition of cyclooxygenase-2 elicits a CB1-mediated decrease of excitatory transmission in rat CA1 hippocampus. Neuropharmacology 2005, 49:653-659.
118. Hogestatt ED, Jonsson BA, Ermund A, Andersson DA, Bjork H, Alexander JP. Conversion of acetaminophen to the bioactive N-acylphenolamine AM404 via fatty acid amide hydrolase-dependent arachidonic acid conjugation in the nervous system. J Biol Chem 2005, 280:31405-31412. 10.1074/jbc.M501489200, 15987694.
119. Ottani A, Leone S, Sandrini M, Ferrari A, Bertolini A. The analgesic activity of paracetamol is prevented by the blockade of cannabinoid CB1 receptors. Eur J Pharmacol 2006, 531:280-281. 10.1016/j.ejphar.2005.12.015, 16438952.
120. Dani M, Guindon J, Lambert C, Beaulieu P. The local antinociceptive effects of paracetamol in neuropathic pain are mediated by cannabinoid receptors. Eur J Pharmacol 2007, 573:214-215. 10.1016/j.ejphar.2007.07.012, 17651722.
121. Liu QS, Qiao JT, Dafny N. D2 dopamine receptor involvement in spinal dopamine-produced antinociception. Life Sci 1992, 51:1485-1492. 10.1016/0024-3205(92)90313-E, 1435058.
122. Sagen J, Proudfit HK. Evidence for pain modulation by pre- and postsynaptic noradrenergic receptors in the medulla oblongata. Brain Res 1985, 331:285-293. 10.1016/0006-8993(85)91554-9, 2859092.
123. Coquoz D, Porchet HC, Dayer P. Central analgesic effects of desipramine, fluvoxamine, and moclobemide after single oral dosing: a study in healthy volunteers. Clin Pharmacol Ther 1993, 54:339-344. 10.1038/clpt.1993.156, 8375130.
124. Finnerup NB, Otto M, McQuay HJ, Jensen TS, Sindrup SH. Algorithm for neuropathic pain treatment: an evidence based proposal. Pain 2005, 118:289-305. 10.1016/j.pain.2005.08.013, 16213659.
125. Dello RC, Boullerne AI, Gavrilyuk V, Feinstein DL. Inhibition of microglial inflammatory responses by norepinephrine: effects on nitric oxide and interleukin-1beta production. J Neuroinflammation 2004, 1:9. 10.1186/1742-2094-1-9, 500870, 15285793.
126. Pini LA, Sandrini M, Vitale G. The antinociceptive action of paracetamol is associated with changes in the serotonergic system in the rat brain. Eur J Pharmacol 1996, 308:31-40. 10.1016/0014-2999(96)00261-0, 8836629.
127. Bonnefont J, Daulhac L, Etienne M, Chapuy E, Mallet C, Ouchchane L. Acetaminophen recruits spinal p42/p44 MAPKs and GH/IGF-1 receptors to produce analgesia via the serotonergic system. Mol Pharmacol 2007, 71:407-415. 10.1124/mol.106.025775, 17088403.
128. Bonnefont J, Chapuy E, Clottes E, Alloui A, Eschalier A. Spinal 5-HT1A receptors differentially influence nociceptive processing according to the nature of the noxious stimulus in rats: effect of WAY-100635 on the antinociceptive activities of paracetamol, venlafaxine and 5-HT. Pain 2005, 114:482-490. 10.1016/j.pain.2005.01.019, 15777873.
129. Pelissier T, Alloui A, Caussade F, Dubray C, Cloarec A, Lavarenne J, Eschalier A. Paracetamol exerts a spinal antinociceptive effect involving an indirect interaction with 5-hydroxytryptamine3 receptors: In vivo and in vitro evidence. J Pharmacol Exp Ther 1996, 278:8-14.
130. Pickering G, Loriot MA, Libert F, Eschalier A, Beaune P, Dubray C. Analgesic effect of acetaminophen in humans: first evidence of a central serotonergic mechanism. Clin Pharmacol Ther 2006, 79:371-378. 10.1016/j.clpt.2005.12.307, 16580905.
131. Dropic AJ, Brailoiu E, Cooper RL. Presynaptic mechanism of action induced by 5-HT in nerve terminals: possible involvement of ryanodine and IP3 sensitive 2+ stores. Comp Biochem Physiol A Mol Integr Physiol 2005, 142:355-361. 10.1016/j.cbpa.2005.08.025, 16182580.
132. Bach-Rojecky L. Analgesic effect of caffeine and clomipramine: a possible interaction between adenosine and serotonin systems. Acta Pharm 2003, 53:33-39.
133. Ghelardini C, Galeotti N, Bartolini A. Caffeine induces central cholinergic analgesia. Naunyn Schmiedebergs Arch Pharmacol 1997, 356:590-595. 10.1007/PL00005094, 9402038.
134. Fiebich BL, Candelario-Jalil E, Mantovani M, Heinzmann M, Akundi RS, Hüll M, Knörle R, Schnierle P, Finkenzeller G, Aicher B. Modulation of catecholamine release from rat striatal slices by the fixed combination of aspirin, paracetamol, and caffeine. Pharmacol Res 2006, 53:391-396. 10.1016/j.phrs.2006.02.002, 16574428.
135. Fanciullacci M, Alessandri M, Del Rosso A. Dopamine involvement in the migraine attack. Funct Neurol 2000, 15(Suppl 3):171-181.
136. Shioda K, Nisijima K, Nishida S, Kato S. Possible serotonin syndrome arising from an interaction between caffeine and serotonergic antidepressants. Hum Psychopharmacol 2004, 19:353-354. 10.1002/hup.592, 15252829.
137. Stovner LJ, Tronvik E, Hagen K. New drugs for migraine. J Headache Pain 2009, 10:395-406. 10.1007/s10194-009-0156-9, 19795182.
138. WHO Cancer pain relief. 1986, WHO, Geneva, WHO.
139. Borisy AA, Elliott PJ, Hurst NW, Lee MS, Lehar J, Price ER, Serbedzija G, Zimmermann GR, Foley MA, Stockwell BR, Keith CT. Systematic discovery of multicomponent therapeutics. PNAS 2003, 100:7977-7982. 10.1073/pnas.1337088100, 164698, 12799470.
140. Berenbaum MC. The expected effect of a combination of agents: the general solution. J Theor Biol 1985, 114:413-431. 10.1016/S0022-5193(85)80176-4, 4021503.
141. Berenbaum MC. What is synergy?. Pharmacol Reviews 1989, 41:93-141.
142. Phero JC, Becker D. Rational use of analgesic combinations. Dent Clin N Am 2002, 46:691-705. 10.1016/S0011-8532(02)00022-8, 12436825.
143. Forth W. Risikoabwägung schwachwirksamer Analgetika Paraminiphenol- und Pyrazol-Derivate - Schlussfolgerungen. Münch med Wschr 1982, 124:216-218.
144. Adam O, Forth W. Coffein. Dt Ärztebl 2001, 98(43A):2816-2818.
145. Forth W. Sinnvolle Medikamenten-Kombinationen. Lehrbuch der Schmerztherapie 1993, 187-195. Stuttgart: Wissenschaftliche Verlagsgesellschaft mbH, Zenz M, Jurna I.
146. Edwards JE, McQuay HJ, Moore RA. Combination analgesic efficacy: individual patient data meta-analysis of single-dose oral tramadol plus acetaminophen in acute postoperative pain. J Pain Symptom Manage 2002, 23:121-130. 10.1016/S0885-3924(01)00404-3, 11844632.
147. Janga SC, Tzakos A. Structure and organization of drug-target networks: insights from genomic approaches for drug discovery. Mol BioSyst 2009, 5:1536-1548. 10.1039/b908147j, 19763339.