Piribedil
From Wikipedia, the free encyclopedia
| Systematic (IUPAC) name | |
|---|---|
| 2-[4-(benzo[1,3]dioxol-5-ylmethyl)piperazin-1-yl]pyrimidine | |
| Identifiers | |
| CAS number | 3605-01-4 |
| ATC code | N04BC08 |
| PubChem | 4850 |
| Chemical data | |
| Formula | C16H18N4O2 |
| Mol. mass | 298.340 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 1.7 – 6.9 hours |
| Excretion | Renal (68%) and biliary (25%) |
| Therapeutic considerations | |
| Pregnancy cat. | ? |
| Legal status | |
| Routes | Oral |
Piribedil (trade names Trivastal, Pronoran, Trastal, Trivastan) is a piperazine derivative and selective dopamine D2 and D3 receptor agonist with additional α2-adrenergic antagonist properties.
Contents |
Indications
- Treatment of Parkinson's disease (PD), either as monotherapy (without L-DOPA (Levodopa)) or in combination with L-DOPA therapy, in the early stages as well as in the advanced stages of the disease.
- Treatment of pathological cognitive deficits in the elderly (impaired attention, motivation, memory, etc).
- Treatment of dizziness in the elderly.
- Treatment of retinal ischemic manifestations.
- Adjuvant treatment in intermittent claudication due to peripheral vascular disease (PVD) of the lower limbs (stage 2).
- Anhedonia and treatment-resistant depression in unipolar and bipolar depressives (off label).
Additional research and uses
The drug has been shown to enhance working memory capacities in normal aging adults.[1]
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.[2]
It enhances cognitive skill learning in healthy older adults.[3]
It showed a positive effect in restless legs syndrome [4]
Dosage
Parkinson's disease
Administration of piribedil should be initiated with one tablet daily during the first week. Dosage should then be gradually increased every week until achieving the optimal therapeutic dose:
- as monotherapy: three to five tablets in three to five doses daily.
- in combination with L-dopa therapy: one to three tablets daily.
Other indications
One tablet daily at the end of the main meal. In severe cases: two tablets daily in two doses.
Adverse effects
- Minor gastrointestinal upset (nausea, vomiting, flatulence, etc) in predisposed individuals, or when taken between meals: adjust dosage individually, and/or add domperidone (Motilium).
- Orthostatic hypotension or drowsiness may occur, particularly in predisposed individuals (underlying condition or causative illness).
Interactions
Dopamine antagonists reduce the effect of piribedil.
Overdosage
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.
Receptor affinities
- Dopamine receptor agonist, selective for subtypes D2 and D3.
- Adrenergic receptor antagonist, subtypes α2a and α2c: could be the reason why piribedil seems to cause less drowsiness than other dopamine agonists.[5]
- Lack of affinity to serotonin receptor 5-HT2B: theoretically no risk of heart valve impairment.[5]
See also
References
- ^ Gierski, F.; Peretti, C.; Ergis, A. (30 January 2007). [Expression error: Missing operand for > "Effects of the dopamine agonist piribedil on prefrontal temporal cortical network function in normal aging as assessed by verbal fluency"]. Progress in Neuro-Psychopharmacology and Biological Psychiatry 31 (1): 262–268. doi:. PMID 16876301.
- ^ Bochkarev, VK; Faĭzulloev, AZ; Avedisova, AS (2005). [Expression error: Missing operand for > "Efficacy of pronoran in age-related memory impairment"]. Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova / Ministerstvo zdravookhraneniia i meditsinskoi promyshlennosti Rossiiskoi Federatsii, Vserossiiskoe obshchestvo nevrologov [i] Vserossiiskoe obshchestvo psikhiatrov 105 (2): 46–50. PMID 15792142.
- ^ Peretti, C. S.; Gierski, F.; Harrois, S. (November 2004). [Expression error: Missing operand for > "Cognitive skill learning in healthy older adults after 2 months of double-blind treatment with piribedil"]. Psychopharmacology 176 (2): 176–182. doi:.
- ^ Evidente, VG (May 2001). [Expression error: Missing operand for > "Piribedil for restless legs syndrome: a pilot study"]. Movement disorders : official journal of the Movement Disorder Society 16 (3): 579–81. PMID 11391766.
- ^ a b Schubert-Zsilavecz, M. "Piribedil" (in German). Neue Arzneimittel 2008.
External links
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