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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01367
rdf:type
n6:Drug
n6:description
Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson's disease or as an adjunct therapy in more advanced cases.
n6:dosage
n12:271B4308-363D-11E5-9242-09173F13E4C5 n12:271B4309-363D-11E5-9242-09173F13E4C5 n12:271B430A-363D-11E5-9242-09173F13E4C5 n12:271B430B-363D-11E5-9242-09173F13E4C5
n6:generalReferences
# Weinreb O, Amit T, Bar-Am O, Youdim MB: RASAGILINE; A NOVEL ANTI-PARKINSONIAN MONOAMINE OXIDASE-B INHIBITOR WITH NEUROPROTECTIVE ACTIVITY. Prog Neurobiol. 2010 Jun 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20600573 # Leegwater-Kim J, Bortan E: The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging. 2010 May 25;5:149-56. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20517484 # Chen JJ, Swope DM, Dashtipour K: Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther. 2007 Sep;29(9):1825-49. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18035186
n6:group
approved
n6:halfLife
Rasagiline has a mean steady-state half life of 3 hours but there is no correlation of pharmacokinetics with its pharmacological effect because of its irreversible inhibition of MAO-B.
n6:indication
For the treatment of the signs and symptoms of idiopathic Parkinsons disease as initial monotherapy and as adjunct therapy to levodopa.
owl:sameAs
n22:DB01367 n24:DB01367
dcterms:title
Rasagiline
adms:identifier
n4:3052776 n5:D02562 n8:68546-142-56 n9:DB01367 n17:PA164764584 n20:Rasagiline n27:10989 n29:2314553 n30:46506045 n31:RAS
n6:mechanismOfAction
The precise mechanisms of action of rasagiline is unknown. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline's beneficial effects seen in models of dopaminergic motor dysfunction.
n6:packager
n18:271B4305-363D-11E5-9242-09173F13E4C5 n18:271B4304-363D-11E5-9242-09173F13E4C5
n6:patent
n13:5387612 n13:2232310 n13:7572834 n13:2031714
n6:routeOfElimination
Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. Glucuronide conjugation of rasagiline and its metabolites, with subsequent urinary excretion, is the major elimination pathway. After oral administration of 14C-labeled rasagiline, elimination occurred primarily via urine and secondarily via feces (62% of total dose in urine and 7% of total dose in feces over 7 days), with a total calculated recovery of 84% of the dose over a period of 38 days. Less than 1% of rasagiline was excreted as unchanged drug in urine.
n6:synonym
RAS (R)-N-2-Propynyl-1-indanamine (1R)-N-Propargylindan-1-amine (R)-Indan-1-yl-prop-2-ynyl-amine
n6:toxicity
Signs and symptoms of overdosage may include, alone or in combination, any of the following: drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions, and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.
n6:volumeOfDistribution
* 87 L
n10:hasAHFSCode
n11:28-92-00
n6:foodInteraction
Avoid alcohol and caffeine.
n6:proteinBinding
Plasma protein binding ranges from 88-94% with mean extent of binding of 61-63% to human albumin over the concentration range of 1-100 ng/ml.
n6:synthesisReference
Jeffrey Sterling, David Lerner, Harel Rosen, Leonid Bronov, Dalia Medini-Green, Berta Iosefzon, Tirtsah Berger-Peskin, Ramy Lidor-Hadas, Eliezer Bahar, "Rasagiline formulations and processes for their preparation." U.S. Patent US07598420, issued October 06, 2009.
n25:hasConcept
n26:M0100095
foaf:page
n15:rasagiline.html n19:azilect.htm
n6:IUPAC-Name
n7:271B4310-363D-11E5-9242-09173F13E4C5
n6:InChI
n7:271B4316-363D-11E5-9242-09173F13E4C5
n6:Molecular-Formula
n7:271B4315-363D-11E5-9242-09173F13E4C5
n6:Molecular-Weight
n7:271B4312-363D-11E5-9242-09173F13E4C5
n6:Monoisotopic-Weight
n7:271B4313-363D-11E5-9242-09173F13E4C5
n6:SMILES
n7:271B4314-363D-11E5-9242-09173F13E4C5
n6:Water-Solubility
n7:271B430E-363D-11E5-9242-09173F13E4C5
n6:logP
n7:271B430C-363D-11E5-9242-09173F13E4C5 n7:271B430F-363D-11E5-9242-09173F13E4C5
n6:logS
n7:271B430D-363D-11E5-9242-09173F13E4C5
n10:hasATCCode
n16:N04BD02
n6:H-Bond-Acceptor-Count
n7:271B431C-363D-11E5-9242-09173F13E4C5
n6:H-Bond-Donor-Count
n7:271B431D-363D-11E5-9242-09173F13E4C5
n6:InChIKey
n7:271B4317-363D-11E5-9242-09173F13E4C5
n6:Polar-Surface-Area--PSA-
n7:271B4318-363D-11E5-9242-09173F13E4C5
n6:Polarizability
n7:271B431A-363D-11E5-9242-09173F13E4C5
n6:Refractivity
n7:271B4319-363D-11E5-9242-09173F13E4C5
n6:Rotatable-Bond-Count
n7:271B431B-363D-11E5-9242-09173F13E4C5
n6:absorption
Rasagiline is rapidly absorbed following oral administration. The absolute bioavailability of rasagiline is about 36%.
n6:affectedOrganism
Humans and other mammals
n6:casRegistryNumber
136236-51-6
n6:category
n6:containedIn
n28:271B4306-363D-11E5-9242-09173F13E4C5 n28:271B4307-363D-11E5-9242-09173F13E4C5
n6:Bioavailability
n7:271B4321-363D-11E5-9242-09173F13E4C5
n6:Ghose-Filter
n7:271B4323-363D-11E5-9242-09173F13E4C5
n6:MDDR-Like-Rule
n7:271B4324-363D-11E5-9242-09173F13E4C5
n6:Number-of-Rings
n7:271B4320-363D-11E5-9242-09173F13E4C5
n6:Physiological-Charge
n7:271B431F-363D-11E5-9242-09173F13E4C5
n6:Rule-of-Five
n7:271B4322-363D-11E5-9242-09173F13E4C5
n6:Traditional-IUPAC-Name
n7:271B4311-363D-11E5-9242-09173F13E4C5
n6:pKa--strongest-basic-
n7:271B431E-363D-11E5-9242-09173F13E4C5