Levodopa/carbidopa and entacapone in the treatment of Parkinson's disease: Efficacy, safety and patient preference

Patient Preference and Adherence

Volumn 3, Issue , 2009, Pages 51-59

  Müller, Thomas ^a,b  

^a St Joseph Hospital Berlin Tempelhof   (Germany)

^b RUHR UNIVERSITY BOCHUM   (Germany)

Author keywords

Acceptance; Compliance; Entacapone; Levodopa; Parkinson's disease; Preference

Indexed keywords

EID: 77951278327     PISSN: None     EISSN: 1177889X     Source Type: Journal    
DOI: 10.2147/PPA.S4084     Document Type: Review

References (94)

1. Fahn S, Oakes D, Shoulson I, et al. Levodopa and the progression of Parkinson's disease. N Engl J Med. 2004;351(24):2498-2508.
2. Birkmayer W, Hornykiewicz O. [The L-3,4-dioxyphenylalanine (DOPA)-effect in Parkinson-akinesia]. Wien Klin Wochenschr. 1961;73:787-788.
3. Cotzias GC, Papavasiliou PS, Gellene R. Modification of Parkinsonism-chronic treatment with L-dopa. N Engl J Med. 1969;280(7):337-345.
4. Müller T. Tolcapone in the management of Parkinson's disease. Aging Health. 2006;2(5):709-720.
5. Ruottinen HM, Rinne UK. COMT inhibition in the treatment of Parkinson's disease. J Neurol. 1998;245(11 Suppl 3):25-34.
6. Ceravolo R, Piccini P, Bailey DL, Jorga KM, Bryson H, Brooks DJ. 18F-dopa PET evidence that tolcapone acts as a central COMT inhibitor in Parkinson's disease. Synapse. 2002;43(3):201-207.
7. Russ H, Müller T, Woitalla D, Rahbar A, Hahn J, Kuhn W. Detection of tolcapone in the cerebrospinal fluid of parkinsonian subjects. Naunyn Schmiedebergs Arch Pharmacol. 1999;360(6):719-720.
8. Sawle GV, Burn DJ, Morrish PK, et al. The effect of entacapone (OR-611) on brain [18F]-6-L-fluorodopa metabolism: implications for levodopa therapy of Parkinson's disease. Neurology. 1994;44(7):1292-1297.
9. Hauser RA, Panisset G, Abbruzzese G, Manzione L, Dronamraju R, Kakarieka A. Improved symptom control with fixed dose levodopa/ carbidopa/entacapone versus conventional levodopa/carbidopa as firstline levodopa therapy in early Parkinson's disease patients. Mov Disord. 2008;23(Suppl 1):208.
10. Olanow CW, Kieburtz K, Stern M, et al. Double-blind, placebocontrolled study of entacapone in levodopa-treated patients with stable Parkinson disease. Arch Neurol. 2004;61(10):1563-1568.
11. Müller T, Erdmann C, Muhlack S, Bremen D, Przuntek H, Woitalla D. Inhibition of catechol-O-methyltransferase contributes to more stable levodopa plasma levels. Mov Disord. 2006;21(3):332-336.
12. Olanow CW, Obeso JA. Pulsatile stimulation of dopamine receptors and levodopa-induced motor complications in Parkinson's disease: implications for the early use of COMT inhibitors. Neurology. 2000; 55(11 Suppl 4):S72-S77.
13. Müller T, Russ H. Levodopa, motor fluctuations and dyskinesia in Parkinson's disease. Expert Opin Pharmacother. 2006;7(13):1715-1730.
14. Riederer P, Gerlach M, Müller T, Reichmann H. Relating mode of action to clinical practice: dopaminergic agents in Parkinson's disease. Parkinsonism Relat Disord. 2007;13(8):466-479.
15. Nyholm D. Pharmacokinetic optimisation in the treatment of Parkinson's disease: an update. Clin Pharmacokinet. 2006;45(2):109-136.
16. Meiler B, Andrich J, Müller T. Rapid switch from oral antiparkinsonian combination drug therapy to duodenal levodopa infusion. Mov Disord. 2008;23(1):145-146.
17. Olanow CW, Stocchi F. COMT inhibitors in Parkinson's disease: can they prevent and/or reverse levodopa-induced motor complications? Neurology. 2004;62(1 Suppl 1):S72-S81.
18. Smith LA, Jackson MJ, Al Barghouthy G, et al. Multiple small doses of levodopa plus entacapone produce continuous dopaminergic stimulation and reduce dyskinesia induction in MPTP-treated drug-naive primates. Mov Disord. 2005;20(3):306-314.
19. Stocchi F, Vacca L, Ruggieri S, Olanow CW. Intermittent vs continuous levodopa administration in patients with advanced Parkinson disease: a clinical and pharmacokinetic study. Arch Neurol. 2005;62(6):905-910.
20. Lee MS, Kim HS, Cho EK, Lim JH, Rinne JO. COMT genotype and effectiveness of entacapone in patients with fluctuating Parkinson's disease. Neurology. 2002;58(4):564-567.
21. Woitalla D, Karwasz R, Müller T, Przuntek H, Kuhn W. The activity of catechol-O-methyltransferase in parkinsonian patients with "on-off fluctuations". J Neural Transm. 2000;107(1):105-111.
22. Muhlack S, Woitalla D, Welnic J, Twiehaus S, Przuntek H, Müller T. Chronic levodopa intake increases levodopa plasma bioavailability in patients with Parkinson's disease. Neurosci Lett. 2004;363(3):284-287.
23. Müller T, Woitalla D, Saft C, Kuhn W. Levodopa in plasma correlates with body weight of parkinsonian patients. Parkinsonism Relat Disord. 2000;6(3):171-173.
24. Müller T, Erdmann C, Bremen D, et al. Impact of gastric emptying on levodopa pharmacokinetics in Parkinson disease patients. Clin Neuropharmacol. 2006;29(2):61-67.
25. Müller T, Woitalla D, Goetze O, Erdmann C. Entacapone improves absorption of a coadministered salt in patients with Parkinson's disease. Mov Disord. 2008;23(10):1458-1461.
26. Kortejarvi H, Urtti A, Yliperttula M. Pharmacokinetic simulation of biowaiver criteria: the effects of gastric emptying, dissolution, absorption and elimination rates. Eur J Pharm Sci. 2007;30(2):155-166.
27. Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT. Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003;304(2):498-506.
28. Forsberg MM, Huotari M, Savolainen J, Mannisto PT. The role of physicochemical properties of entacapone and tolcapone on their efficacy during local intrastriatal administration. Eur J Pharm Sci. 2005;24(5):503-511.
29. Goetze O, Wieczorek J, Müller T, Przuntek H, Schmidt WE, Woitalla D. Impaired gastric emptying of a solid test meal in patients with Parkinson's disease using 13C-sodium octanoate breath test. Neurosci Lett. 2005;375(3):170-173.
30. Goetze O, Nikodem AB, Wiezcorek J, et al. Predictors of gastric emptying in Parkinson's disease. Neurogastroenterol Motil. 2006;18(5):369-375.
31. Lennernas H. Modeling gastrointestinal drug absorption requires more in vivo biopharmaceutical data: experience from in vivo dissolution and permeability studies in humans. Curr Drug Metab. 2007;8(7):645-657.
32. Thwaites DT, Anderson CM. H-coupled nutrient, micronutrient and drug transporters in the mammalian small intestine. Exp Physiol. 2007;92(4):603-619.
33. Mannisto PT. Catechol O-methyltransferase: characterization of the protein, its gene, and the preclinical pharmacology of COMT inhibitors. Adv Pharmacol. 1998;42:324-328.
34. Müller T, Erdmann C, Muhlack S, et al. Pharmacokinetic behaviour of levodopa and 3-O-methyldopa after repeat administration of levodopa/ carbidopa with and without entacapone in patients with Parkinson's disease. J Neural Transm. 2006;113(10):1441-1448.
35. Müller T, Kolf K, Ander L, Woitalla D, Muhlack S. Catechol-Omethyltransferase inhibition improves levodopa-associated strength increase in patients with Parkinson disease. Clin Neuropharmacol. 2008;31(3):134-140.
36. Müller T, Ander L, Kolf K, Woitalla D, Muhlack S. Comparison of 200 mg retarded release levodopa/carbidopa-with 150 mg levodopa/carbidopa/entacapone application: pharmacokinetics and efficacy in patients with Parkinson's disease. J Neural Transm. 2007;114(11):1457-1462.
37. Fabbrini G, Juncos JL, Mouradian MM, Serrati C, Chase TN. 3-Omethyldopa and motor fluctuations in Parkinson's disease. Neurology. 1987;37(5):856-859.
38. Soares-da-Silva P, Parada A, Serrao P. The O-methylated derivative of L-DOPA, 3-O-methyl-L-DOPA, fails to inhibit neuronal and non-neuronal aromatic L-amino acid decarboxylase. Brain Res. 2000;863(1-2):293-297.
39. Arnsten AF, Li BM. Neurobiology of executive functions: catecholamine influences on prefrontal cortical functions. Biol Psychiatry. 2005;57(11):1377-1384.
40. Müller T. Role of homocysteine in the treatment of Parkinson's disease. Expert Rev Neurother. 2008;8(6):957-967.
41. Ben Shlomo Y, Marmot MG. Survival and cause of death in a cohort of patients with parkinsonism: possible clues to aetiology? J Neurol Neurosurg Psychiatry. 1995;58(3):293-299.
42. Gorell JM, Johnson CC, Rybicki BA. Parkinson's disease and its comorbid disorders: an analysis of Michigan mortality data, 1970 to 1990. Neurology. 1994;44(10):1865-1868.
43. Nakaso K, Yasui K, Kowa H, et al. Hypertrophy of IMC of carotid artery in Parkinson's disease is associated with L-DOPA, homocysteine, and MTHFR genotype. J Neurol Sci. 2003;207(1-2):19-23.
44. O'Suilleabhain PE, Sung V, Hernandez C, et al. Elevated plasma homocysteine level in patients with Parkinson disease: motor, affective, and cognitive associations. Arch Neurol. 2004;61(6):865-868.
45. Ozer F, Meral H, Hanoglu L, et al. Plasma homocysteine levels in patients treated with levodopa: motor and cognitive associations. Neurol Res. 2006;28(8):853-858.
46. Zoccolella S, Lamberti P, Iliceto G, et al. Plasma homocysteine levels in L-dopa-treated Parkinson's disease patients with cognitive dysfunctions. Clin Chem Lab Med. 2005;43(10):1107-1110.
47. Hassin-Baer S, Cohen O, Vakil E, et al. Plasma homocysteine levels and Parkinson disease: disease progression, carotid intima-media thickness and neuropsychiatric complications. Clin Neuropharmacol. 2006;29(6):305-311.
48. O'Suilleabhain PE, Oberle R, Bartis C, Dewey RB Jr, Bottiglieri T, az-Arrastia R. Clinical course in Parkinson's disease with elevated homocysteine. Parkinsonism Relat Disord. 2006;12(2):103-107.
49. Miller JW, Selhub J, Nadeau MR, Thomas CA, Feldman RG, Wolf PA. Effect of L-dopa on plasma homocysteine in PD patients: relationship to B-vitamin status. Neurology. 2003;60(7):1125-1129.
50. Woitalla D, Kuhn W, Müller T. MTHFR C677T polymorphism, folic acid and hyperhomocysteinemia in levodopa treated patients with Parkinson's disease. J Neural Transm Suppl. 2004; (68):15-20.
51. Müller T, Kuhn W. Tolcapone decreases plasma levels of S-adenosyl-Lhomocysteine and homocysteine in treated Parkinson's disease patients. Eur J Clin Pharmacol. 2006;62(6):447-450.
52. Nissinen E, Nissinen H, Larjonmaa H, et al. The COMT inhibitor, entacapone, reduces levodopa-induced elevations in plasma homocysteine in healthy adult rats. J Neural Transm. 2005;112(9):1213-1221.
53. Ostrem JL, Kang GA, Subramanian I, et al. The effect of entacapone on homocysteine levels in Parkinson disease. Neurology. 2005;64(8):1482.
54. Zesiewicz TA, Wecker L, Sullivan KL, Merlin LR, Hauser RA. The controversy concerning plasma homocysteine in Parkinson disease patients treated with levodopa alone or with entacapone: effects of vitamin status. Clin Neuropharmacol. 2006;29(3):106-111.
55. Lamberti P, Zoccolella S, Iliceto G, et al. Effects of levodopa and COMT inhibitors on plasma homocysteine in Parkinson's disease patients. Mov Disord. 2005;20(1):69-72.
56. Valkovic P, Benetin J, Blazicek P, Valkovicova L, Gmitterova K, Kukumberg P. Reduced plasma homocysteine levels in levodopa/ entacapone treated Parkinson patients. Parkinsonism Relat Disord. 2005;11(4):253-256.
57. Zoccolella S, Lamberti P, Armenise E, et al. Plasma homocysteine levels in Parkinson's disease: role of antiparkinsonian medications. Parkinsonism Relat Disord. 2005;11(2):131-133.
58. Isobe C, Murata T, Sato C, Terayama Y. Increase of total homocysteine concentration in cerebrospinal fluid in patients with Alzheimer's disease and Parkinson's disease. Life Sci. 2005;77(15): 1836-1843.
59. Lee ES, Chen H, Soliman KF, Charlton CG. Effects of homocysteine on the dopaminergic system and behavior in rodents. Neurotoxicology. 2005;26(3):361-371.
60. Heider I, Lehmensiek V, Lenk T, Müller T, Storch A. Dopaminergic neurotoxicity of homocysteine and its derivatives in primary mesencephalic cultures. J Neural Transm Suppl. 2004;(68):1-13.
61. Huang G, Dragan M, Freeman D, Wilson JX. Activation of catechol-O-methyltransferase in astrocytes stimulates homocysteine synthesis and export to neurons. Glia. 2005;51(1):47-55.
62. Storch A, Blessing H, Bareiss M, et al. Catechol-O-methyltransferase inhibition attenuates levodopa toxicity in mesencephalic dopamine neurons. Mol Pharmacol. 2000;57(3):589-594.
63. Kuhn W, Woitalla D, Gerlach M, Russ H, Müller T. Tolcapone and neurotoxicity in Parkinson's disease. Lancet. 1998;352(9136):1313-1314.
64. Matsubara K, Aoyama K, Suno M, Awaya T. N-methylation underlying Parkinson's disease. Neurotoxicol Teratol. 2002;24(5):593-598.
65. Lee ES, Chen H, Soliman KF, Charlton CG. Effects of homocysteine on the dopaminergic system and behavior in rodents. Neurotoxicology. 2005;26(3):361-371.
66. Fuso A, Seminara L, Cavallaro RA, D'Anselmi F, Scarpa S. S-adenosylmethionine/homocysteine cycle alterations modify DNA methylation status with consequent deregulation of PS1 and BACE and beta-amyloid production. Mol Cell Neurosci. 2005;28(1):195-204.
67. Cavallaro RA, Fuso A, D'Anselmi F, Seminara L, Scarpa S. The effect of S-adenosylmethionine on CNS gene expression studied by cDNA microarray analysis. J Alzheimers Dis. 2006;9(4):415-419.
68. Hartz CS, Schalinske KL. Phosphatidylethanolamine N-methyltransferase and regulation of homocysteine. Nutr Rev. 2006;64(10 Pt 1):465-467.
69. Liu XX, Wilson K, Charlton CG. Effects of L-dopa treatment on methylation in mouse brain: implications for the side effects of L-dopa. Life Sci. 2000;66(23):2277-2288.
70. Morrison LD, Smith DD, Kish SJ. Brain S-adenosylmethionine levels are severely decreased in Alzheimer's disease. J Neurochem. 1996;67(3):1328-1331.
71. Müller T, Woitalla D, Hauptmann B, Fowler B, Kuhn W. Decrease of methionine and S-adenosylmethionine and increase of homocysteine in treated patients with Parkinson's disease. Neurosci Lett. 2001;308(1):54-56.
72. Nagatsu T. Isoquinoline neurotoxins in the brain and Parkinson's disease. Neurosci Res. 1997;29(2):99-111.
73. Aoyama K, Matsubara K, Okada K, et al. N-methylation ability for azaheterocyclic amines is higher in Parkinson's disease: nicotinamide loading test. J Neural Transm. 2000;107(8-9):985-995.
74. Aoyama K, Matsubara K, Kondo M, et al. Nicotinamide-Nmethyltransferase is higher in the lumbar cerebrospinal fluid of patients with Parkinson's disease. Neurosci Lett. 2001;298(1):78-80.
75. Naoi M, Maruyama W, Nakao N, Ibi T, Sahashi K, Benedetti MS. (R)salsolinol N-methyltransferase activity increases in parkinsonian lymphocytes. Ann Neurol. 1998;43(2):212-216.
76. Müller T, Sallstrom BS, Haussermann P, et al. Plasma levels of R-and S-salsolinol are not increased in "de-novo" Parkinsonian patients. J Neural Transm. 1998;105(2-3):239-246.
77. Müller T, Sallstrom BS, Haussermann P, Przuntek H, Rommelspacher H, Kuhn W. R-and S-salsolinol are not increased in cerebrospinal fluid of Parkinsonian patients. J Neurol Sci. 1999;164(2):158-162.
78. Brosnan JT, Jacobs RL, Stead LM, Brosnan ME. Methylation demand: a key determinant of homocysteine metabolism. Acta Biochim Pol. 2004;51(2):405-413.
79. Brooks DJ. Safety and tolerability of COMT inhibitors. Neurology. 2004;62(1 Suppl 1):S39-S46.
80. Durif F, Devaux I, Pere JJ, Delumeau JC, Bourdeix I. Efficacy and tolerability of entacapone as adjunctive therapy to levodopa in patients with Parkinson's disease and end-of-dose deterioration in daily medical practice: an open, multicenter study. Eur Neurol. 2001;45(2):111-118.
81. Gershanik O, Emre M, Bernhard G, Sauer D. Efficacy and safety of levodopa with entacapone in Parkinson's disease patients suboptimally controlled with levodopa alone, in daily clinical practice: an international, multicentre, open-label study. Prog Neuropsychopharmacol Biol Psychiatry. 2003;27(6):963-971.
82. Gordin A, Kaakkola S, Teravainen H. Clinical advantages of COMT inhibition with entacapone-a review. J Neural Transm. 2004;111 (10-11):1343-1363.
83. Illi A, Sundberg S, Ojala-Karlsson P, Scheinin M, Gordin A. Simultaneous inhibition of catecholamine-O-methylation by entacapone and neuronal uptake by imipramine: lack of interactions. Eur J Clin Pharmacol. 1996;51(3-4):273-276.
84. Koller W, Guarnieri M, Hubble J, Rabinowicz AL, Silver D. An openlabel evaluation of the tolerability and safety of Stalevo (carbidopa, levodopa and entacapone) in Parkinson's disease patients experiencing wearing-off. J Neural Transm. 2005;112(2):221-230.
85. Larsen JP, Worm-Petersen J, Siden A, Gordin A, Reinikainen K, Leinonen M. The tolerability and efficacy of entacapone over 3 years in patients with Parkinson's disease. Eur J Neurol. 2003;10(2): 37-146.
86. Lyytinen J, Kaakkola S, Ahtila S, Tuomainen P, Teravainen H. Simultaneous MAO-B and COMT inhibition in L-Dopa-treated patients with Parkinson's disease. Mov Disord. 1997;12(4):497-505.
87. Martignoni E, Blandini F, Pacchetti C, Nappi G. COMT inhibition and safety. Funct Neurol. 2001;16(4 Suppl):135-140.
88. Rinne UK, Larsen JP, Siden A, Worm-Petersen J. Entacapone enhances the response to levodopa in parkinsonian patients with motor fluctuations. Nomecomt Study Group. Neurology. 1998;51(5):1309-1314.
89. Zijlmans JC, Debilly B, Rascol O, Lees AJ, Durif F. Safety of entacapone and apomorphine coadministration in levodopa-treated Parkinson's disease patients: pharmacokinetic and pharmacodynamic results of a multicenter, double-blind, placebo-controlled, cross-over study. Mov Disord. 2004;19(9):1006-1011.
90. Martignoni E, Cosentino M, Ferrari M, et al. Two patients with COMT inhibitor-induced hepatic dysfunction and UGT1A9 genetic polymorphism. Neurology. 2005;65(11):1820-1822.
91. Grosset KA, Reid JL, Grosset DG. Medicine-taking behavior: implications of suboptimal compliance in Parkinson's disease. Mov Disord. 2005;20(11):1397-1404.
92. Grosset KA, Grosset DG. Effect of educational intervention on medication timing in Parkinson's disease: a randomized controlled trial. BMC Neurol. 2007;7:20.
93. Parkinson Study Group. Pramipexole vs levodopa as initial treatment for Parkinson disease: A randomized controlled trial. JAMA. 2000;284(15):1931-1938.
94. Rascol O, Brooks DJ, Korczyn AD, De Deyn PP, Clarke CE, Lang AE. A five-year study of the incidence of dyskinesia in patients with early Parkinson's disease who were treated with ropinirole or levodopa. 056 Study Group. N Engl J Med. 2000;342(20):1484-1491.