Entacapone improves the availability of L-dopa in plasma by decreasing its peripheral metabolism independent of L-dopa/carbidopa dose

British Journal of Clinical Pharmacology

Volumn 54, Issue 4, 2002, Pages 363-371

  Heikkinen, Helena ^a   Varhe, Anu ^a   Laine, Tarmo ^a   Puttonen, Jaakko ^a   Kela, Marjo ^a   Kaakkola, Seppo ^a   Reinikainen, Kari ^a  

^a ORION CORPORATION   (Finland)

Author keywords

3 OMD; Carbidopa; DOPAC; Entacapone; HVA; L dopa; Pharmacokinetics

Indexed keywords

3 O METHYLDOPA; 3,4 DIHYDROXYPHENYLACETIC ACID; CARBIDOPA; CATECHOL METHYLTRANSFERASE INHIBITOR; DRUG METABOLITE; ENTACAPONE; HOMOVANILLIC ACID; LEVODOPA; PLACEBO;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG METABOLISM; DRUG POTENTIATION; DRUG RELEASE; DRUG TOLERABILITY; HUMAN; HUMAN EXPERIMENT; MALE; METABOLIC RATE; NORMAL HUMAN; PARKINSON DISEASE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADULT; ANALYSIS OF VARIANCE; ANTIPARKINSON AGENTS; BIOLOGICAL AVAILABILITY; CATECHOLS; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; HUMANS; LEVODOPA; MALE;

EID: 0036431658     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.2002.01654.x     Document Type: Article

References (30)

1. Nutt JG, Fellman JH. Pharmacokinetics of levodopa. Clin Neuropharmacol 1984; 7: 35-49.
2. Cedarbaum JM. Clinical pharmacokinetics of anti-parkinsonian drugs. Clin Pharmacokinet 1987; 13: 141-178.
3. Dingemanse J, Kleinbloesem CH, Zurcher G, et al. Pharmacodynamics of benserazide assessed by its effects on endogenous and exogenous levodopa pharmacokinetics. Br J Clin Pharmacol 1997; 44: 41-48.
4. Keränen T, Gordin A, Karlsson M, et al. Inhibition of soluble catechol-O-methyltransferase and single-dose pharmacokinetics after oral and intravenous administration of entacapone. Eur J Clin Pharmacol 1994; 46: 151-157.
5. Heikkinen H, Saraheimo M, Antila S, et al. Pharmacokinetics of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, in man. A study using a stable isotope technique. Eur J Clin Pharmacol 2001; 56: 821-826.
6. Kaakkola S. Clinical pharmacology, therapeutic use and potential of COMT inhibitors in Parkinson's disease. Drugs 2000; 59: 1233-1250.
7. Rinne UK, Larsen JP, Siden Å., et al. Entacapone enhances the response to levodopa in parkinsonian patients with motor fluctuations. Nomecomt Study Group Neurol 1998; 51: 1309-1314.
8. Parkinson Study Group. Entacapone improves motor fluctuations in levodopa-treated Parkinson's disease patients. Ann Neurol 1997; 42: 747-755.
9. Myllylä VV, Kultalahti E-R, Haapaniemi H, et al. The Filomen Study Group. Twelve-month safety of entacapone in patients with Parkinson's disease. Eur J Neurol 2001; 8: 53-60.
10. Waters C. Practical issues with COMT inhibitors in Parkinson's disease. Neurology 2000; 55: 57-59.
11. Kaakkola S, Ter̈väinen H, Ahtila S, et al. Entacapone in combination with standard or controlled-release levodopa/carbidopa. a clinical and pharmacokinetic study in patients with Parkinson's disease. Eur J Neurol 1995; 2: 341-347.
12. Ruottinen HM, Rinne UK. Entacapone prolongs levodopa response in a one month double blind study in parkinsonian patients with levodopa related fluctuations. J Neurol Neurosurg Psych 1996; 60: 36-40.
13. Heikkinen H, Nutt JG, LeWitt PA, et al. The effects of different repeated doses of entacapone on the pharmacokinetics of L-dopa and on the clinical response to L-dopa in Parkinson's disease. Clin Neuropharmacol 2001; 24: 150-157.
14. Wikberg T. Simultaneous determination of levodopa, its main metabolites and carbidopa in plasma by liquid chromatography. J Pharm Biomed Anal 1991; 9: 167-176.
15. Karlsson M, Wikberg T. Liquid chromatographic determination of a new catechol-O-methyltransferase inhibitor, entacapone, and its Z-isomer in human plasma and urine. J Pharm Biomed Anal 1992; 10: 593-600.
16. Wade D, Mearrick PT, Birkett DJ, Morris J. Variability of L-dopa absorption in man. Aust NZ J Med 1974; 4: 138-143.
17. Robertson DRC, George CF. Drug therapy for Parkinson's disease in the elderly. Br Med Bull 1990; 46: 124-146.
18. Kaakkola S, Männistö PT, Nissinen E, et al. The effect of an increased ratio of carbidopa to levodopa on the pharmacokinetics of levodopa. Acta Neurol Scand 1985; 72: 385-391.
19. Jorga K, Fotteler B, Schmitt M, et al. The effect of COMT inhibition by tolcapone on tolerability and pharmacokinetics of different levodopa/benserazide formulations. Eur Neurol 1997; 38: 59-67.
20. Jorga K, Fotteler B, Sedek G, et al. The effect of tolcapone on levodopa pharmacokinetics is independent of levodopa/carbidopa formulation. J Neurol 1998; 245: 223-230.
21. Muller T, Woitalla D, Schulz D, et al. Tolcapone increases maximum concentration of levodopa. J Neural Transm 2000; 107: 113-119.
22. Mouradian M, Heuser JE, Baronti F, et al. Pathogenesis of dyskinesias in Parkinson's disease. Ann Neurol 1989; 25: 523-526.
23. Pearce R, Heikkilä M, Linden I-B, Jenner P.L-dopa induces dyskinesia in normal monkeys. Behavioural and pharmacokinetic observations. Psychopharmacology 2001; 156: 402-409.
24. Ruottinen HM, Rinne UK. Effect of one month's treatment with peripherally acting catechol-O-methyltransferase inhibitor, entacapone, on pharmacokinetics and motor response to levodopa in advanced parkinsonian patients. Clin Neuropharmacol 1996; 19: 222-233.
25. Vickers S, Stuart EK, Bianchine JR, et al. Metabolism of carbidopa (L-(-) -alfa-hydrazino-3, 4,-dihydroxy-alfa-methylhydrocinnamic acid monohydrate), an aromatic amino acid decarboxylase inhibitor, in the rat, dog, rhesus monkey, and man. Drug Metab Dispos 1974; 2: 9-22.
26. Durso R, Evans JE, Josephs E, et al. Variable absorption of carbidopa affects both peripheral and central levodopa metabolism. J Clin Pharmacol 2000; 40: 854-860.
27. Hagan RM, Raxworthy MJ, Gulliver PA. Benserazide and carbidopa as substrates of catechol-O-methyltransferase: New mechanism of action in Parkinson's disease. Biochem Pharmacol 1980; 29: 3123-3126.
28. Keränen T, Gordin A, Harjola V-P, et al. The effect of catechol-O-methyl transferase inhibition by entacapone on the pharmacokinetics and metabolism of levodopa in healthy volunteers. Clin Neuropharmacol 1993; 16: 145-156.
29. Sharpless NS, Tyce GM, Owen CAJ. Effect of chronic administration of L-dopa on catechol-O-methyltransferase in rat tissues. Life Sci 1973; 12: 97-106.
30. Nissinen E, Tuominen R, Perhoniemi V, Kaakkola S. Catechol-O-methyltransferase activity in human and rat small intestine. Life Sci 1988; 42: 2609-2614.