title: Temporal administration of entacapone with slow release L-dopa: pharmacokinetic profile and clinical outcome.
abstract: Entacapone is a specific, peripherally acting catechol- O-methyltransferase (COMT) inhibitor that prevents peripheral degradation of L-dopa, thus improving its bioavailability. Entacapone is known to have pharmacokinetics similar to standard L-dopa but not to that of controlled-release (CR) L-dopa. The aim was to determine whether delayed entacapone administration may prolong CR L-dopa half-life in comparison to the co-administration modality. We compared plasma L-dopa concentrations after co-administration of CR L-dopa and entacapone or after administration of CR and a delayed (30 and 90 minutes) entacapone dose in 10 parkinsonian patients. The area under the concentration-time curve and other pharmacokinetic parameters were not changed by the delayed administration of entacapone. Different temporal modalities of entacapone administration had similar effects on CR L-dopa pharmacokinetics and on L-dopa-induced clinical improvement.
authors.affiliation: Neurology Clinic, Tor Vergata University of Rome, Rome, Italy.
authors.forename: L
authors.initials: L
authors.lastname: Brusa
authors.forename: M
authors.initials: M
authors.lastname: Pierantozzi
authors.forename: A
authors.initials: A
authors.lastname: Bassi
authors.forename: E
authors.initials: E
authors.lastname: Fedele
authors.forename: G
authors.initials: G
authors.lastname: Lunardi
authors.forename: P
authors.initials: P
authors.lastname: Giacomini
authors.forename: P
authors.initials: P
authors.lastname: Stanzione
mesh_terms: D000368:Aged; D000704:Analysis of Variance; D000978:Antiparkinson Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D002230:Carbidopa / Q000008:administration & dosage; D065098:Catechol O-Methyltransferase Inhibitors; D002396:Catechols / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D007980:Levodopa / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D009570:Nitriles; D010300:Parkinson Disease / Q000188:drug therapy*; D016037:Single-Blind Method; D016896:Treatment Outcome
chemical_list: D000978:Antiparkinson Agents; D065098:Catechol O-Methyltransferase Inhibitors; D002396:Catechols; D003692:Delayed-Action Preparations; D004791:Enzyme Inhibitors; D009570:Nitriles; D007980:Levodopa; C071192:entacapone; D002230:Carbidopa