Piribedil

Overview

Piribedil is an antiparkinsonian agent and piperazine derivative which acts as a D₂ and D₃ receptor agonist. It also has α₂-adrenergic antagonist properties.[1][2] WP

Uses, dosage and effects

Medical uses

• Treatment of Parkinson's disease (PD), either as monotherapy (without levodopa) or in combination with L-DOPA therapy, in the early stages of the disease as well as in the advanced ones WP⚠ Wikipedia itself has flagged this text: citation needed.
• Treatment of pathological cognitive deficits in the elderly (impaired attention, motivation, memory, etc.) WP⚠ Wikipedia itself has flagged this text: citation needed.
• Treatment of dizziness in the young patients WP⚠ Wikipedia itself has flagged this text: citation needed.
• Treatment of retinal ischemic manifestations WP⚠ Wikipedia itself has flagged this text: citation needed.
• Adjunctive treatment of intermittent claudication due to peripheral vascular disease (PVD) of the lower limbs (stage 2) WP⚠ Wikipedia itself has flagged this text: citation needed.
• Adjunctive treatment of anhedonia, apathy and treatment-resistant depression in unipolar and bipolar depressives (off-label) WP⚠ Wikipedia itself has flagged this text: citation needed.
• Treatment of gait disorders associated with Parkinson's disease (no related cause) and other forms of parkinsonism WP⚠ Wikipedia itself has flagged this text: citation needed.

Other uses

The drug has been shown to enhance working memory capacities in normal aging adults.[3] WP

In age-related memory impairment, it has a positive effect on psychophysiological state of elderly people, improving memory and attention and increasing the velocity of psychomotor reactions and lability of nervous processes.[4] WP

It enhances cognitive skill learning in healthy older adults.[5] WP

It showed a positive effect in restless legs syndrome.[6] WP

Risks and side effects

Side effects

• Minor gastrointestinal upset (nausea, vomiting, flatulence, etc.) in predisposed individuals, or when taken between meals: adjust dosage individually, and/or add domperidone WP⚠ Wikipedia itself has flagged this text: citation needed.
• Orthostatic hypotension or drowsiness may occur, particularly in predisposed individuals (underlying condition or causative illness) WP⚠ Wikipedia itself has flagged this text: citation needed.
• Mild dizziness, confusion and feeling "drunk" also may occur WP⚠ Wikipedia itself has flagged this text: citation needed.

As with other dopamine agonists (like pramipexole and ropinirole), compulsive behavior like pathological gambling, overeating, excessive shopping, increased libido, sexual and/or other intense urges, may develop.[7][8] WP

Another rare side effect of piribedil is excessive daytime sleepiness and unintended sleep episodes.[8][9] WP

Overdose

At very high doses, piribedil has an emetic action on the chemoreceptor trigger zone (CTZ). Tablets will thus be rapidly rejected, which explains why no data are currently available concerning the risk of overdosage. WP⚠ Part of this sentence could not be copied from the source. Open the source to read it in full.

Interactions

Interactions

Dopamine antagonists reduce the effect of piribedil. WP⚠ Part of this sentence could not be copied from the source. Open the source to read it in full.

Pharmacology

Pharmacodynamics

• Dopamine receptor agonist, selective for subtypes D₂ and D₃ WP⚠ Wikipedia itself has flagged this text: citation needed.
• Dopamine receptor antagonist, selective for subtypes D₄.[10][11][12] WP
• Adrenergic receptor antagonist, subtypes α2A and α2C.[13] WP
• Lack of affinity to serotonin receptor 5-HT2B.[13] WP

Chemistry

Formula

C16H18N4O2 PC

CAS number

3605-01-4 PC

Molar mass (g/mol)

298.34 PC

IUPAC name (computed by PubChem)

2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]pyrimidine PC

SMILES

C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4 PC

InChIKey

OQDPVLVUJFGPGQ-UHFFFAOYSA-N PC

PubChem CID

4850

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Millan MJ, Cussac D, Milligan G, Carr C, Audinot V, Gobert A, Lejeune F, Rivet JM, Brocco M, Duqueyroix D, Nicolas JP, Boutin JA, Newman-Tancredi A. Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization. The Journal of Pharmacology and Experimental Therapeutics. June 2001. PMID 11356907
2. Journal / agency Gobert A, Di Cara B, Cistarelli L, Millan MJ. Piribedil enhances frontocortical and hippocampal release of acetylcholine in freely moving rats by blockade of alpha 2A-adrenoceptors: a dialysis comparison to talipexole and quinelorane in the absence of acetylcholinesterase inhibitors. The Journal of Pharmacology and Experimental Therapeutics. April 2003. doi:10.1124/jpet.102.046383 · PMID 12649387
3. Journal / agency Gierski F, Peretti CS, Ergis AM. Effects of the dopamine agonist piribedil on prefrontal temporal cortical network function in normal aging as assessed by verbal fluency. Progress in Neuro-Psychopharmacology & Biological Psychiatry. January 2007. doi:10.1016/j.pnpbp.2006.06.017 · PMID 16876301
4. Journal / agency Bochkarev VK, Faĭzulloev AZ, Avedisova AS. Efficacy of pronoran in age-related memory impairment. Zhurnal Nevrologii I Psikhiatrii imeni S.S. Korsakova. 2005. PMID 15792142
5. Journal / agency Peretti CS, Gierski F, Harrois S. Cognitive skill learning in healthy older adults after 2 months of double-blind treatment with piribedil. Psychopharmacology. November 2004. doi:10.1007/s00213-004-1869-8 · PMID 15138753
6. Journal / agency Evidente VG. Piribedil for restless legs syndrome: a pilot study. Movement Disorders. May 2001. doi:10.1002/mds.1104 · PMID 11391766
7. Journal / agency Tschopp L, Salazar Z, Gomez Botello MT, Roca CU, Micheli F. Impulse control disorder and piribedil: report of 5 cases. Clinical Neuropharmacology. 2010. doi:10.1097/WNF.0b013e3181c4ae2e · PMID 19959959
8. Other TRIVASTAL Retard 50 (piribedil) Prescribing Information, Servier Laboratories, April 2008. link 2
9. Journal / agency Gouraud A, Millaret A, Descotes J, Vial T. Piribedil-induced sleep attacks in patients without Parkinson disease: a case series. Clinical Neuropharmacology. 2011. doi:10.1097/WNF.0b013e31821f0d8b · PMID 21586915
10. Journal / agency Arnsten AF, Murphy B, Merchant K. The selective dopamine D4 receptor antagonist, PNU-101387G, prevents stress-induced cognitive deficits in monkeys. Neuropsychopharmacology. October 2000. doi:10.1016/S0893-133X(00)00133-0 · PMID 10989267
11. Journal / agency Nagaraja D, Jayashree S. Randomized study of the dopamine receptor agonist piribedil in the treatment of mild cognitive impairment. The American Journal of Psychiatry. September 2001. doi:10.1176/appi.ajp.158.9.1517 · PMID 11532743
12. Journal / agency Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ. Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. The Journal of Pharmacology and Experimental Therapeutics. November 2002. doi:10.1124/jpet.102.039875 · PMID 12388667
13. Other Schubert-Zsilavecz M. Piribedil

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