Levodopa: Past, present, and future

European Neurology

Volumn 62, Issue 1, 2009, Pages 1-8

  Hauser, Robert A ^a  

^a UNIVERSITY OF SOUTH FLORIDA   (United States)

Author keywords

Catechol O methyltransferase inhibition; Dopa decarboxylase inhibition; Levodopa; Levodopa therapy, complications; Levodopa, historical perspective; Parkinson's disease

Indexed keywords

BENSERAZIDE; BENSERAZIDE PLUS LEVODOPA; CARBIDOPA; CARBIDOPA PLUS ENTACAPONE PLUS LEVODOPA; CARBIDOPA PLUS LEVODOPA; CATECHOL METHYLTRANSFERASE INHIBITOR; DOPA DECARBOXYLASE INHIBITOR; DOPAMINE RECEPTOR STIMULATING AGENT; ENTACAPONE; LEVODOPA; PLACEBO; TOLCAPONE;

ADD ON THERAPY; AKINESIA; ANOREXIA; ATHETOSIS; BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; CLINICAL TRIAL; DECARBOXYLATION; DOPAMINERGIC TRANSMISSION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG FORMULATION; DRUG HALF LIFE; DRUG INFUSION; DRUG INHIBITION; DRUG MEGADOSE; DRUG SAFETY; DRUG TOLERABILITY; DYSKINESIA; FOOD AND DRUG ADMINISTRATION; HUMAN; HYPERGLYCEMIA; INDUCED HYPOTENSION; INVOLUNTARY CHOREIFORM; LIVER TOXICITY; LONG TERM CARE; MONOTHERAPY; MORNING DOSAGE; MOTOR DYSFUNCTION; MUSCLE RIGIDITY; NAUSEA; NONHUMAN; OPEN STUDY; PARKINSON DISEASE; PARKINSONISM; POLARIZATION; PRIORITY JOURNAL; REVIEW; RISK REDUCTION; SIDE EFFECT; SYMPTOM; TABLET FORMULATION; TREATMENT DURATION; TREATMENT INDICATION; TREATMENT RESPONSE; TREMOR; VOMITING;

ANTIPARKINSON AGENTS; BRAIN; CATECHOL O-METHYLTRANSFERASE; DOPA DECARBOXYLASE; HISTORY, 20TH CENTURY; HISTORY, 21ST CENTURY; HUMANS; LEVODOPA; MODELS, NEUROLOGICAL; PARKINSON DISEASE;

EID: 65449135642     PISSN: 00143022     EISSN: None     Source Type: Journal    
DOI: 10.1159/000215875     Document Type: Review

References (79)

1. Bernheimer H, Birkmayer W, Hornykiewicz O, Jellinger K, Seitelberger F: Brain dopamine and the syndromes of Parkinson and Huntington. Clinical, morphological and neurochemical correlations. J Neurol Sci 1973;20:415-455.
2. Lloyd KG, Hornykiewicz O: Parkinson's disease: activity of L-dopa decarboxylase in discrete brain regions. Science 1970;170:1213.
3. Fahn S, Libsch LR, Cutler RW: Monoamines in the human neostriatum: topographic distribution in normals and in Parkinson's disease and their role in akinesia, rigidity, chorea, and tremor. J Neurol Sci 1971;14:427-455.
4. Lang AE: The progression of Parkinson disease: a hypothesis. Neurology 2007;68:948-952.
5. Hornykiewicz O: Biochemical aspects of Park inson's disease. Neurolog y 1998;51:S2-S9.
6. Kish SJ, Shannak K, Hornykiewicz O: Uneven pattern of dopamine loss in the striatum of patients with idiopathic Parkinson's disease. Pathophysiologic and clinical implications. N Engl J Med 1988;318:876-880.
7. Deleu D, Northway MG, Hanssens Y: Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease. Clin Pharmacokinet 2002;41:261-309.
8. Oldfield V, Keating GM, Perry CM: Rasagiline: a review of its use in the management of Parkinson's disease. Drugs 2007;67:1725-1747.
9. Pahwa R, Factor SA, Lyons KE, Ondo WG, Gronseth G, Bronte-Stewart H, Hallett M, Miyasaki J, Stevens J, Weiner WJ: Practice parameter: treatment of Parkinson disease with motor fluctuations and dyskinesia (an evidence-based review). Report of the Quality Standards Subcommittee of the American Academy of Neurology. Neurology 2006;66:983-995.
10. Hornykiewicz O: L-dopa: from a biologically inactive amino acid to a successful therapeutic agent. Amino Acids 2002;23:65-70.
11. Montagu KA: Catechol compounds in rat tissues and in brains of different animals. Nature 1957;180:244-245.
12. Weil-Malherbe H, Bone AD: Intracellular distribution of catecholamines in the brain. Nature 1957;180:1050-1051.
13. Carlsson A, Lindqvist M, Magnusson T:3,4-Dihydroxyphenylalanine and 5-hydroxy-tryptophan as reserpine antagonists. Nature 1957;180:1200.
14. Sano I, Gamo T, Kakimoto Y, Taniguchi K, Takegada M, Nishinuma K: Distribution of catechol compounds in human brain. Biochim Biophys Acta 1959;32:586-587.
15. Foley P: The L-dopa story revisited. Further surprises to be expected? J Neural Transm Suppl 2000;60:1-20.
16. Ehringer H, Hornykiewicz O: Distribution of noradrenaline and dopamine (3-hydroxy-tyramine) in the human brain and their behavior in diseases of the extrapyramidal system. Parkinsonism Relat Disord 1998;4:53-57.
17. Birkmayer W, Hornykiewicz O: The effect of L-3,4-dihydroxyphenylalanine (L-dopa) on akinesia in parkinsonism. Parkinsonism Relat Disord 1998;4:59-60.
18. McGeer PL, Zeldowicz LR: Administration of dihydroxyphenylalanine to parkinsonian patients. Can Med Assoc J 1964;90:463-466.
19. Bertler A, Rosengren E: Possible role of brain dopamine. Pharmacol Rev 1966;18:769-773.
20. Cotzias GC, Van Woert MH, Schiffer LM: Aromatic amino acids and modification of parkinsonism. N Engl J Med 1967;276:374-379.
21. Cotzias GC: L-Dopa for Parkinsonism. N Engl J Med 1968;278:630.
22. Cotzias GC, Papavasiliou PS, Vanwoert MH, Sakamoto A: Melanogenesis and extrapyramida l diseases. Fed Proc 1964;23:713-718.
23. Yahr MD, Duvoisin RC, Schear MJ, Barrett RE, Hoehn MM: Treatment of parkinsonism with levodopa. Arch Neurol 1969;21:343-354.
24. Lloyd KG, Davidson L, Hornykiewicz O: The neurochemistry of Parkinson's disease: effect of L-dopa therapy. J Pharmacol Exp Ther 1975;195:453-464.
25. Cotzias GC, Papavasiliou PS, Gellene R: Modification of Parkinsonism-chronic treatment with L-dopa. N Engl J Med 1969;280:337-345.
26. Ahlskog JE, Muenter MD: Frequency of le-vodopa-related dyskinesias and motor fluctuations as estimated from the cumulative literature. Mov Disord 2001;16:448-458.
27. Fahn S: Parkinson disease, the effect of le-vodopa, and the ELLDOPA trial. Earlier vs. later L-dopa. Arch Neurol 1999;56:529-535.
28. Witjas T, Kaphan E, Azulay JP, Blin O, Ceccaldi M, Pouget J, Poncet M, Cherif AA: Nonmotor fluctuations in Parkinson's disease: frequent and disabling. Neurology 2002;59:408-413.
29. Gunal DI, Nurichalichi K, Tuncer N, Bekiroglu N, Aktan S: The clinical profile of non-motor fluctuations in Parkinson's disease patients. Can J Neurol Sci 2002;29:61-64.
30. Olanow CW, Obeso JA, Stocchi F: Drug insight: continuous dopaminergic stimulation in the treatment of Parkinson's disease. Nat Clin Pract Neurol 2006;2:382-392.
31. Obeso JA, Rodriguez-Oroz MC, Chana P, Lera G, Rodriguez M, Olanow CW: The evolution and origin of motor complications in Parkinson's disease. Neurology 2000;55: S13-S20.
32. 1 receptor desen-sitization profile in MPTP-lesioned primates. Eur J Pharmacol 1996;309:13-20.
33. Olanow CW, Obeso JA, Stocchi F: Continuous dopamine-receptor treatment of Parkinson's disease: scientific rationale and clinical implications. Lancet Neurol 2006;5:677-687.
34. Stocchi F, Ruggieri S, Vacca L, Olanow CW: Prospective randomized trial of lisuride infusion versus oral levodopa in patients with Parkinson's disease. Brain 2002;125:2058-2066.
35. Nutt JG, Fellman JH: Pharmacokinetics of levodopa. Clin Neuropharmacol 1984;7:35-49.
36. Jankovic J: Levodopa strengths and weaknesses. Neurology 2002;58:S19-S32.
37. Pletscher A, DaPrada M: Pharmacotherapy of Parkinson's disease: research from 1960 to 1991. Acta Neurol Scand Suppl 1993;146:26-31.
38. Cedarbaum JM: Clinical pharmacokinetics of anti-parkinsonian drugs. Clin Pharmaco-kinet 1987;13:141-178.
39. Tolosa E, Marti MJ, Valldeoriola F, Molinuevo JL: History of levodopa and dopamine agonists in Parkinson's disease treatment. Neurology 1998;50:S2-S10.
40. Markham C, Diamond SG, Treciokas LJ: Carbidopa in Parkinson disease and in nausea and vomiting of levodopa. Arch Neurol 1974;31:128-133.
41. Lieberman A, Goodgold A, Jonas S, Leibowitz M: Comparison of dopa decarboxylase inhibitor (carbidopa) combined with levodopa and levodopa alone in Parkinson's disease. Neurology 1975;25:911-916.
42. LeWitt PA, Nelson M V, Berchou RC, Galloway MP, Kesaree N, Kareti D, Schlick P: Controlled-release carbidopa/levodopa (Sinemet 50/200 CR4): clinical and pharmacokinetic studies. Neurology 1989;39:45-53.
43. Koller WC, Hutton JT, Tolosa E, Capilldeo R: Immediate-release and controlled-release carbidopa/levodopa in PD: a 5-year randomized multicenter study. Carbidopa/Levodopa Study Group. Neurology 1999;53:1012-1019.
44. Hammerstad JP, Woodward WR, Nutt JG, Gancher ST, Block GA, Cyhan G: Controlled release levodopa/carbidopa 25/100 (Sinemet CR 25/100): pharmacokinetics and clinical efficacy in untreated parkinsonian patients. Clin Neuropharmacol 1994;17:429-434.
45. Block G, Liss C, Reines S, Irr J, Nibbelink D: Comparison of immediate-release and controlled release carbidopa/levodopa in Parkinson's disease. A multicenter 5-year study. The CR First Study Group. Eur Neurol 1997;37:23-27.
46. Mannisto PT, Kaakkola S: New selective COMT inhibitors: useful adjuncts for Parki nson'sdisease? Trends Pha rm acol Sci 1989;10:54-56.
47. Lee ES, Chen H, King J, Charlton C: The role of 3-O-methyldopa in the side effects of L-dopa. Neurochem Res 2008;33:401-411.
48. Dupont E, Burgunder JM, Findley LJ, Olsson JE, Dorf linger E: Tolcapone added to levodopa in stable parkinsonian patients: a double-blind placebo-controlled study. Tolcapone in Parkinson's Disease Study Group II (TIPS II). Mov Disord 1997;12:928-934.
49. Baas H, Beiske AG, Ghi ka J, Jackson M, Oertel WH, Poewe W, Ransmayr G: Catechol-O-methyltransferase inhibition with tolcapone reduces the 'wearing off' phenomenon and levodopa requirements in fluctuating parkinsonian patients. J Neurol Neurosurg Psychiatry 1997;63:421-428.
50. Adler CH, Singer C, O'Brien C, Hauser RA, Lew MF, Marek KL, Dorflinger E, Pedder S, Deptula D, Yoo K: Randomized, placebo-controlled study of tolcapone in patients with fluctuating Parkinson disease treated with levodopa-carbidopa. Tolcapone Fluctuator Study Group III. Arch Neurol 1998;55:1089-1095.
51. Fenelon G, Gimenez-Roldan S, Montastruc JL, Bermejo F, Durif F, Bourdeix I, Pere JJ, Galiano L, Schadrack J: Efficacy and tolerability of entacapone in patients with Parkinson's disease treated with levodopa plus a dopamine agonist and experiencing wearing-off motor fluctuations. A randomized, double-blind, multicentre study. J Neural Transm 2003;110:239-251.
52. Mizuno Y, Kanazawa I, Kuno S, Yanagisawa N, Yamamoto M, Kondo T: Placebo-controlled, double-blind dose-finding study of entacapone in fluctuating parkinsonian patients. Mov Disord 2007;22:75-80.
53. Grandas F, Hernandez B: Long-term effectiveness and quality of life improvement in entacapone-treated Parkinson's disease patients: the effects of an early therapeutic inter vention. Eur J Neurol 2007;14:282-289.
54. Larsen JP, Worm-Petersen J, Siden A, Gordin A, Reinika i nen K, Lei nonen M;NOMESAFE Study Group: The tolerability and efficacy of entacapone over 3 years in patients with Parkinson's disease. Eur J Neurol 2003;10:137-146.
55. Gershanik O, Emre M, Bernhard G, Sauer D: Efficacy and safety of levodopa with entacapone in Parkinson's disease patients sub-optimally controlled with levodopa alone, in daily clinical practice: an international, multicentre, open-label study. Prog Neuropsychopharmacol Biol Psychiatry 2003;27:963-971.
56. 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;45:111-118.
57. Roberts JW, Cora-Locatelli G, Bravi D, Amantea MA, Mouradian MM, Chase TN: Catechol-O-methyltransferase inhibitor tolcapone prolongs levodopa/carbidopa action in parkinsonian patients. Neurology 1993;43:2685-2688.
58. Limousin P, Pollak P, Gervason-Tournier CL, Hommel M, Perret JE: Ro 40-7592, a COMT inhibitor, plus levodopa in Parkinson's disease. Lancet 1993;341:1605.
59. Nutt JG, Woodward WR, Beckner RM, Stone CK, Berggren K, Carter JH, Gancher ST, Hammerstad JP, Gordin A: Effect of periph-eral catechol-O- methyltransferase inhibition on the pharmacokinetics and pharmacodynamics of levodopa in parkinsonian patients. Neurology 1994;44:913-919.
60. Entacapone to Tolcapone Switch Study Investigators: Entacapone to tolcapone switch: multicenter double-blind, randomized, active-controlled trial in advanced Parkinson's disease. Mov Disord 2007;22:14-19.
61. Borges N: Tolcapone in Parkinson's disease: liver toxicity and clinical efficacy. Expert Opin Drug Saf 2005;4:69-73.
62. Olanow CW, Watkins PB: Tolcapone: an efficacy and safety review. Clin Neuropharmacol 2007;30:287-294.
63. Parkinson Study Group: Entacapone improves motor fluctuations in levodopa-treated Parkinson's disease patients. Ann Neurol 1997;42:747-755.
64. Rinne UK, Larsen JP, Siden A, Worm-Petersen J;Nomecomt Study Group: Entacapone enhances the response to levodopa in par-kinsonian patients with motor fluctuations. Neurolog y 1998;51:1309-1314.
65. Poewe WH, Deuschl G, Gordin A, Kultalahti ER, Leinonen M: Efficacy and safety of entacapone in Parkinson's disease patients with suboptimal levodopa response: a 6-month randomized placebo-controlled double-blind study in Germany and Austria (Celomen Study). Acta Neurol Scand 2002;105:245-255.
66. Brooks DJ, Sagar H: Entacapone is beneficial in both fluctuating and non-fluctuating patients with Parkinson's disease: a randomised, placebo-controlled, double-blind, six-month study. J Neurol Neurosurg Psychiatry 2003;74:1071-1079.
67. Smith LA, Jackson MJ, Al Barghouthy G, Rose S, Kuoppamäki M, Olanow W, Jenner P: Multiple small doses of levodopa plus en-tacapone produce continuous dopaminergic stimulation and reduce dyskinesia induction in MPTP-treated drug-naive primates. Mov Disord 2005;20:306-314.
68. Hauser RA: Levodopa/carbidopa/entacapone (Stalevo). Neurology 2004;62:S64-S71.
69. Hauser R A, Panisset M, Abbruzzese G, Mancione L, Dronamraju N, Kakarieka A: Double-blind trial of levodopa/carbidopa/entacapone versus levodopa/carbidopa in early Parkinson's disease. Mov Disord 2008. [Epub ahead of print].
70. Schrag A: Entacapone in the treatment of Parkinson's disease. Lancet Neurol 2005;4:366-370.
71. Stocchi F: Optimising levodopa therapy for the management of Parkinson's disease. J Neurol 2005;252(suppl 4):I V43-IV48.
72. Nyholm D: Enteral levodopa/carbidopa gel infusion for the treatment of motor fluctuations and dyskinesias in advanced Parkinson's disease. Expert Rev Neurother 2006;6:1403-1411.
73. Antonini A, Isaias IU, Canesi M, Zibetti M, Mancini F, Manfredi L, Dal FM, Lopiano L, Pezzoli G: Duodenal levodopa infusion for advanced Parkinson's disease:12-month treatment outcome. Mov Disord 2007;22:1145-1149.
74. Syed N, Murphy J, Zimmerman T Jr, Mark MH, Sage JI: Ten years' experience with enteral levodopa infusions for motor fluctuations in Parkinson's disease. Mov Disord 1998;13:336-338.
75. Goole J, Deleuze P, Vanderbist F, Amighi K: New levodopa sustained-release floating minitablets coated with insoluble acrylic polymer. Eur J Pharm Biopharm 2008;68:310-318.
76. Di Stefano A, Sozio P, Cerasa LS: Antiparkinson prodrugs. Molecu les 2008;13:46-68.
77. Priano L, Gasco MR, Mauro A: Transdermal treatment options for neurological disorders: impact on the elderly. Drugs Aging 2006;23:357-375.
78. Kankkunen T, Huupponen I, Lahtinen K, Sundell M, Ekman K, Kontturi K, Hirvonen J: Improved stability and release control of levodopa and metaraminol using ion-exchange fibers and transdermal iontophoresis. Eur J Pharm Sci 2002;16:273-280.
79. Bonnet AM: Involvement of non-dopami-nergic pathways in Parkinson's disease: pathophysiology and therapeutic implications. CNS Drugs 2000;13:351-364.