Integrated pharmacokinetics and pharmacodynamics of the novel catechol‐O‐methyltransferase inhibitor tolcapone during first administration to humans

To assess the tolerability, pharmacokinetics and pharmacodynamics of single oral doses of the novel catechol‐O‐methyltransferase (COMT) inhibitor tolcapone in healthy volunteers.

[1]  P. T. Ménnistó Clinical Potential of Catechol-OMethyltransferase (COMT) Inhibitors as Adjuvants in Parkinson’s Disease , 1994, CNS drugs.

[2]  S. Fahn Adverse Effects of Levodopa in Parkinson’s Disease , 1989 .

[3]  M. Prada,et al.  Improved Therapy of Parkinson's Disease with Tolcapone, a Central and Peripheral COMT Inhibitor with an S‐Adenosyl‐L‐Methionine‐Sparing Effect , 1994 .

[4]  C. Négre [Treatment of Parkinson's disease]. , 1986, Soins; la revue de reference infirmiere.

[5]  R. Erdin,et al.  Determination of the catechol-O-methyltransferase inhibitor Ro 40-7592 in human plasma by high-performance liquid chromatography with coulometric detection. , 1992, Journal of chromatography.

[6]  A Colzi,et al.  Ro 40-7592: inhibition of COMT in rat brain and extracerebral tissues. , 1990, Journal of neural transmission. Supplementum.

[7]  W. Haefely,et al.  Inhibition of decarboxylase and levels of dopa and 3-O-methyldopa: a comparative study of benserazide versus carbidopa in rodents and of Madopar standard versus Madopar HBS in volunteers. , 1987, European neurology.

[8]  J. Cedarbaum Clinical Pharmacokinetics of Anti-Parkinsonian Drugs , 1987, Clinical pharmacokinetics.

[9]  L. Rivera-calimlim,et al.  Catechol‐O‐methyltransferase activity: A determinant of levodopa response , 1980, Clinical pharmacology and therapeutics.

[10]  M. Karlsson,et al.  The effect of catechol-O-methyl transferase inhibition by entacapone on the pharmacokinetics and metabolism of levodopa in healthy volunteers. , 1993, Clinical neuropharmacology.

[11]  M. da Prada,et al.  Ro 40-7592, a novel, very potent, and orally active inhibitor of catechol-O-methyltransferase: a pharmacological study in rats. , 1990, Advances in neurology.

[12]  S. Fahn,et al.  3‐O‐Methyldopa inhibits rotations induced by levodopa in rats after unilateral destruction of the nigrostriatal pathway , 1982, Neurology.

[13]  R. Katzman.,et al.  3-0-Methyldopa uptake and inhibition of L-dopa at the blood-brain barrier , 1975 .

[14]  J. Nutt,et al.  3‐O‐Methyldopa and the response to levodopa in Parkinson's disease , 1987, Annals of neurology.

[15]  J. Borgulya Ro 40-7592 , 1991 .

[16]  R. Weinshilboum,et al.  Genetics of red cell COMT activity: analysis of thermal stability and family data. , 1981, American journal of medical genetics.

[17]  M. Danhof,et al.  Pharmacokinetic-pharmacodynamic modeling of CNS drug effects: an overview. , 1988, Pharmacology & therapeutics.

[18]  J. Boissel,et al.  The place of simultaneous pharmacokinetic pharmacodynamic modeling in new drug development: trends and perspectives * , 1990, Fundamental & clinical pharmacology.

[19]  S. Kaakkola,et al.  Rationale for selective COMT inhibitors as adjuncts in the drug treatment of Parkinson's disease. , 1990, Pharmacology & toxicology.

[20]  C. Marsden,et al.  Catechol-O-methyl transferase: pharmacological aspects and physiological role. , 1975, Pharmacological reviews.

[21]  R. Weinshilboum Human erythrocyte catechol-O-methyltransferase: correlation with lung and kidney activity. , 1978, Life sciences.

[22]  R. Kettler,et al.  New Therapeutic Strategies in Parkinson’s Disease: Inhibition of MAO-B by Ro 19-6327 and of COMT by Ro 40-7592 , 1991 .

[23]  N H Holford,et al.  Concepts and usefulness of pharmacokinetic‐pharmacodynamic modelling , 1990, Fundamental & clinical pharmacology.

[24]  C. T. Viswanathan,et al.  Opportunities for Integration of Pharmacokinetics, Pharmacodynamics, and Toxicokinetics in Rational Drug Development , 1992, Clinical pharmacology and therapeutics.

[25]  Max B. Streifler,et al.  Parkinson's disease : anatomy, pathology and therapy , 1990 .

[26]  L. Wetterberg,et al.  The Inheritance of human erythrocyte catechol‐O‐methyltransferase activity , 1981, Clinical genetics.

[27]  P. Pentikäinen,et al.  Effect of a novel catechol-O-methyltransferase inhibitor, nitecapone, on the metabolism of L-dopa in healthy volunteers. , 1990, Clinical neuropharmacology.

[28]  R. Weinshilboum,et al.  Human liver catechol‐O‐methyltransferase pharmacogenetics , 1990, Clinical pharmacology and therapeutics.