|
|
|
|
|
Entacapone: profile and news
Orion Oyj: Orion group 2005 financial statements Feb 9, 2006 Orion Q4 pretax beats forecasts on strong pharma ops; sees pharma ... Feb 9, 2006 Orion Q4 pretax beats forecasts on strong pharma ops; sees pharma ... Feb 9, 2006 Orion more than doubles Q4 pre-tax yr/yr Feb 9, 2006 Orion Oyj: Orion group 2005 financial statements 09 Feb 2006 Orion Q4 pretax beats forecasts on strong pharma ops; sees pharma ... 09 Feb 2006 International Approvals: Tasmar, Amplimexon, IV Remodulin Jan 17, 2006 Orion Oyj: Orion group interim report 1-9/2005 Nov 7, 2005 Azilect offers new hope to levodopa treated patients with moderate ... Sep 21, 2005 Rasagiline Reduces Disability For Patients With Advanced ... Apr 8, 2005 CeNeS and Tripos advances COMT research Apr 13, 2005 New PBS drugs to help older Australians Mar 31, 2005 COSTA MESA, Californie -- (BUSINESS WIRE) -- March 8, 2005 - Mar 8, 2005 Once-Daily AGILECT(R) Demonstrated Improvement in Parkinson's ... Mar 10, 2005 Study Points to Tolcapone as Viable Therapy in the Management Mar 8, 2005 Once-daily AGILECT(R) demonstrated improvement in Parkinson's ... Mar 10, 2005 Valeant Pharmaceuticals International Mar 8, 2005 New drug offers hope for patients with advanced Parkinson's ... Mar 10, 2005 New drug helps Parkinson's patients: Mar 10, 2005 Valeant Pharmaceuticals Makes a Strong Showing at the Movement ... Mar 5, 2005 Rasagiline Significantly Reduces 'OFF' Time in Parkinson's - Study ... Feb 14, 2005 Attention News Editors: Feb 14, 2005 Study Showed AGILECT(R) Improved Motor Fluctuations and ... Feb 14, 2005 Other information Indication For as an adjunct to levodopa / carbidopa to treat patients with idiopathic Parkinson's Disease who experience the signs and symptoms of end-of-dose "wearing-off". Pharmacology Entacapone is used in the treatment of Parkinson’s disease as an adjunct to levodopa/carbidopa therapy. Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). In mammals, COMT is distributed throughout various organs with the highest activities in the liver and kidney. COMT also occurs in the heart, lung, smooth and skeletal muscles, intestinal tract, reproductive organs, various glands, adipose tissue, skin, blood cells and neuronal tissues, especially in glial cells. 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, and 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. Mechanism Of Action The mechanism of action of entacapone is believed to be through its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more 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. Drug Category Antiparkinson Agents; Antidyskinetics; Central Nervous System Agents; ATC:N04BX02 Brand Names/Synonyms Comtan; ENTACAPONE; Entacapona [Inn-Spanish]; Entacapone; Entacapone [Usan:Inn]; Entacaponum [Inn-Latin] Dosage Forms TABLET Absorption Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%. Interactions Interactions for Entacapone: In vitro studies of human CYP enzymes showed that entacapone inhibited the CYP enzymes 1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A only at very high concentrations (IC50 from 200 to over 1000 uM; an oral 200 mg dose achieves a highest level of approximately 5 uM in people); these enzymes would therefore not be expected to be inhibited in clinical use. Protein Binding: Entacapone is highly protein bound (98%). In vitro studies have shown no binding displacement between entacapone and other highly bound drugs, such as warfarin, salicylic acid, phenylbutazone, and diazepam. Drugs Metabolized by Catechol-O-methyltransferase (COMT): Hormone levels: Levodopa is known to depress prolactin secretion and increase growth hormone levels. Treatment with entacapone coadministered with levodopa/dopa decarboxylase inhibitor does not change these effects. No interaction was noted with the MAO-B inhibitor selegiline in two multiple-dose interaction studies when entacapone was coadministered with a levodopa/dopa decarboxylase inhibitor (n=29). More than 600 Parkinson's disease patients in clinical trials have used selegiline in combination with entacapone and levodopa/dopa decarboxylase inhibitor. As most entacapone excretion is via the bile, caution should be exercised when drugs known to interfere with biliary excretion, glucuronidation, and intestinal beta-glucuronidase are given concurrently with entacapone. These include probenecid, cholestyramine, and some antibiotics (e.g. erythromycin, rifamipicin, ampicillin and chloramphenicol). No interaction with the tricyclic antidepressant imipramine was shown in a single-dose study with entacapone without coadministered levodopa/dopa-decarboxylase inhibitor. Chemical IUPAC Name 2-cyano-3-(5-dihydroxyamino-3,4-dioxo-1-cyclohexa-1,5-dienyl)-N,N-diethyl-prop-2-enamide Chemical Formula C14H15N3O5 Half Life 0.4-0.7 hour Drug Type Approved Drug # Accession No APRD00416 CAS Registry Number 130929-57-6 |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |