Tolcapone
Tolcapone Brand names, Tolcapone Analogs
Tolcapone Brand Names Mixture
- No information avaliable
Tolcapone Chemical_Formula
C14H11NO5
Tolcapone RX_link
http://www.rxlist.com/cgi/generic3/tolcapone.htm
Tolcapone fda sheet
Tolcapone msds (material safety sheet)
Tolcapone Synthesis Reference
No information avaliable
Tolcapone Molecular Weight
273.241 g/mol
Tolcapone Melting Point
No information avaliable
Tolcapone H2O Solubility
No information avaliable
Tolcapone State
Solid
Tolcapone LogP
1.868
Tolcapone Dosage Forms
Tablet
Tolcapone Indication
For the treatment of Parkinson's Disease
Tolcapone Pharmacology
Tolcapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). In humans, COMT is distributed throughout various organs. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. In the presence of a decarboxylase inhibitor, COMT becomes the major metabolizing enzyme for levodopa catalyzing the metabolism to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD) in the brain and periphery. When tolcapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that these sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson's disease in patients as well as increased levodopa adverse effects, sometimes requiring a decrease in the dose of levodopa.
Tolcapone Absorption
rapidly absorbed (absolute bioavailability is about 65%)
Tolcapone side effects and Toxicity
LD50 = 1600 mg/kg (Orally in rats)
Tolcapone Patient Information
PATIENT INFORMATION
Tolcapone, an inhibitor of catechol-O-methyltransferase (COMT), is used in the treatment of Parkinson's disease as an adjunct to levodopa/carbidopa therapy.
Tolcapone, should not be used by patients until there has been a complete discussion of the risks and the patient has provided written informed consent.
Patients should know about clinical signs and symptoms that suggest the onset of hepatic injury (persistent nausea, fatigue, lethargy, anorexia, jaundice, dark urine, pruritus, and right upper quadrant tenderness)
Patients should know about the risk of hepatic failure while using Tolcapone.
There is a need to have regular blood tests to monitor liver enzymes for the patients.
Because of the possible additive sedative effects, caution should be used when patients are taking other CNS depressants in combination with Tolcapone.
Tolcapone, an inhibitor of catechol-O-methyltransferase (COMT), is used in the treatment of Parkinson's disease as an adjunct to levodopa/carbidopa therapy.
Tolcapone, should not be used by patients until there has been a complete discussion of the risks and the patient has provided written informed consent.
Patients should know about clinical signs and symptoms that suggest the onset of hepatic injury (persistent nausea, fatigue, lethargy, anorexia, jaundice, dark urine, pruritus, and right upper quadrant tenderness)
Patients should know about the risk of hepatic failure while using Tolcapone.
There is a need to have regular blood tests to monitor liver enzymes for the patients.
Because of the possible additive sedative effects, caution should be used when patients are taking other CNS depressants in combination with Tolcapone.
Tolcapone Organisms Affected
Humans and other mammals
