Description

Simple

A medication used to treat Parkinson's disease.

Clinical

An irreversible inhibitor of monoamine oxidase used for the symptomatic management of idiopathic Parkinson's disease as initial monotherapy and as adjunct therapy to levodopa.

Overview

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.

Pharmacology

Indication

For the treatment of the signs and symptoms of idiopathic Parkinsons disease as initial monotherapy and as adjunct therapy to levodopa.

Pharmacodynamic

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 localize... Read more

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... Read more

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.

Volume of distribution

87 L

Clearance

Information currently not available.

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.

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... Read more

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 a... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Avoid alcohol.
  • Avoid caffeine.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The risk or severity of bleeding and hemorrhage can be increased when Rasagiline is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding and hemorrhage can be increased when Rasagiline is combined with (S)-Warfarin.
1-benzylimidazole
The risk or severity of hypertension can be increased when Rasagiline is combined with 1-benzylimidazole.
2,4-thiazolidinedione
Rasagiline may increase the hypoglycemic activities of 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylamphetamine
Rasagiline may increase the hypertensive activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
Rasagiline may increase the hypertensive activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
Rasagiline may increase the hypertensive activities of 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
The risk or severity of bleeding and hemorrhage can be increased when Rasagiline is combined with 4-hydroxycoumarin.
4-Methoxyamphetamine
Rasagiline may increase the hypertensive activities of 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Rasagiline.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Rasagiline.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Rasagiline is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Rasagiline is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Rasagiline.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Rasagiline.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Rasagiline.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Rasagiline.
Abacavir
Abacavir may decrease the excretion rate of Rasagiline which could result in a higher serum level.
Abatacept
The metabolism of Rasagiline can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding and hemorrhage can be increased when Rasagiline is combined with Abciximab.
3 References
  1. 1 . Weinreb O, Amit T, Bar-Am O, Youdim MB: Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol. 2010 Nov;92(3):330-44. doi: 10.1016/j.pneurobio.2010.06.008. Epub 2010 Jun 19.PubMed: 20600573
  2. 2 . 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: 20517484
  3. 3 . 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: 18035186