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QuickView for Rasagiline (compound)

Name: rasagiline
PubChem Compound ID: 122316
Molecular formula: C12H13N
Molecular weight: 171.238 g/mol
Agn-1135; Rasagiline; Agn 1135; 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-; 1875-50-9; N-2-Propynyl-1-indanamine; 2,3-Dihydro-N-2-propynyl-1H-inden-1-amine
Name: rasagiline
Name (isomeric): DB01367
Drug Type: small molecule
Brand: Azilect
Category: Monoamine Oxidase Inhibitors, Neuroprotective Agents
CAS number: 136236-51-6
Indication: For the treatment of the signs and symptoms of idiopathic Parkinsons disease as initial monotherapy and as adjunct therapy to levodopa.
Rasagiline is a propargylamine and an irreversible inhibitor of monoamine oxidase (MAO). MAO, a flavin-containing enzyme, regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. It is classified into two major molecular species, A and B, and is localized in mitochondrial membranes throughout the body i...
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Mechanism of Action:
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 mo...
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Absorption: Rasagiline is rapidly absorbed following oral administration. The absolute bioavailability of rasagiline is about 36%.
Protein binding: 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.
Biotransformation: Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. In vitro experiments indicate that both routes of rasagiline metabolism are dependent on the cytochrome P450 (CYP) system, with CYP 1A2 being the major isoenzyme involved in rasagiline metabolism.
Route of elimination: 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.
Half Life: 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.
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.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol and caffeine.
Drug interaction:
MethamphetaminePossible hypertensive crisis
ProcaterolIncreased arterial pressure
EphedrineIncreased arterial pressure
ImipraminePossibility of severe adverse effects
ClomipraminePossibility of severe adverse effects
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