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Pharmacokinetics, pharmacodynamics, and tolerability of tolcapone: a review of early studies in volunteers.
Neurology. 1998 May; 50(5 Suppl 5):S31-8.Neur

Abstract

Tolcapone is a potent, reversible inhibitor of catechol O-methyltransferase (COMT) intended for use as an adjunct to levodopa therapy for Parkinson's disease (PD). Findings from the first pharmacokinetics/pharmacodynamics and tolerability studies of tolcapone in volunteers are reviewed. Following linear and dose-proportional pharmacokinetics, tolcapone is rapidly absorbed and eliminated after single- or multiple-dose (i.e., tid) administration. Onset of COMT inhibition is rapid, substantial, and reversible, and is not affected by the co-administration of levodopa/decarboxylase inhibitor (levodopa/DCI). When given together with levodopa/DCI, tolcapone increases the relative bioavailability and plasma elimination half-life of levodopa, without affecting its peak plasma concentration. This leads to more stable plasma levels of levodopa, and the formation of 3-O-methyldopa is effectively reduced. Tolcapone was well tolerated alone or in combination with levodopa/DCI, and the results indicated that the effective dose in patients with PD would be in the range of 50-400 mg tid.

Authors+Show Affiliations

Department of Clinical Pharmacology, F. Hoffmann-La Roche, Ltd., Basel, Switzerland.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

9591520

Citation

Jorga, K M.. "Pharmacokinetics, Pharmacodynamics, and Tolerability of Tolcapone: a Review of Early Studies in Volunteers." Neurology, vol. 50, no. 5 Suppl 5, 1998, pp. S31-8.
Jorga KM. Pharmacokinetics, pharmacodynamics, and tolerability of tolcapone: a review of early studies in volunteers. Neurology. 1998;50(5 Suppl 5):S31-8.
Jorga, K. M. (1998). Pharmacokinetics, pharmacodynamics, and tolerability of tolcapone: a review of early studies in volunteers. Neurology, 50(5 Suppl 5), S31-8.
Jorga KM. Pharmacokinetics, Pharmacodynamics, and Tolerability of Tolcapone: a Review of Early Studies in Volunteers. Neurology. 1998;50(5 Suppl 5):S31-8. PubMed PMID: 9591520.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetics, pharmacodynamics, and tolerability of tolcapone: a review of early studies in volunteers. A1 - Jorga,K M, PY - 1998/5/20/pubmed PY - 1998/5/20/medline PY - 1998/5/20/entrez SP - S31 EP - 8 JF - Neurology JO - Neurology VL - 50 IS - 5 Suppl 5 N2 - Tolcapone is a potent, reversible inhibitor of catechol O-methyltransferase (COMT) intended for use as an adjunct to levodopa therapy for Parkinson's disease (PD). Findings from the first pharmacokinetics/pharmacodynamics and tolerability studies of tolcapone in volunteers are reviewed. Following linear and dose-proportional pharmacokinetics, tolcapone is rapidly absorbed and eliminated after single- or multiple-dose (i.e., tid) administration. Onset of COMT inhibition is rapid, substantial, and reversible, and is not affected by the co-administration of levodopa/decarboxylase inhibitor (levodopa/DCI). When given together with levodopa/DCI, tolcapone increases the relative bioavailability and plasma elimination half-life of levodopa, without affecting its peak plasma concentration. This leads to more stable plasma levels of levodopa, and the formation of 3-O-methyldopa is effectively reduced. Tolcapone was well tolerated alone or in combination with levodopa/DCI, and the results indicated that the effective dose in patients with PD would be in the range of 50-400 mg tid. SN - 0028-3878 UR - https://www.unboundmedicine.com/medline/citation/9591520/Pharmacokinetics_pharmacodynamics_and_tolerability_of_tolcapone:_a_review_of_early_studies_in_volunteers_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=linkout&SEARCH=9591520.ui DB - PRIME DP - Unbound Medicine ER -