Piribedil
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Piribedil
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| Systematic (IUPAC) name | |
| 2-[4-(benzo[1,3]dioxol-5-ylmethyl)piperazin-1-yl]pyrimidine | |
| Identifiers | |
| CAS number | |
| ATC code | N04 |
| PubChem | |
| 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. |
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| Legal status | |
| Routes | Oral |
Piribedil is a piperazine dopamine agonist; and marketed as TRIVASTAL Retard 50.
Trivastal retard 50 is also distributed as: Trastal, Trivastal 50 retard, Trivastal 50mg LP, Trivastan ritardo and Pronoran.
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[edit] Composition:
Piribedil 50 mg per tablet - sustained-release.
[edit] Indications:
- Treatment of Parkinson's disease, either as monotherapy (without L-dopa) or in combination with L-dopa therapy, in the early stages as well as in the advanced stages. - Treatment of pathological cognitive deficits in the elderly (impaired attention, memory, etc). Treatment of dizziness in the elderly. - Treatment of Retinal ischemic manifestations. Adjuvant treatment in intermittent claudication due to peripheral occlusive arterial disease of the lower limbs (stage 2). - (off label) anhedonia and treatment-resistant depression in unipolar and bipolar depressives
[edit] Dosage:
In Parkinson's disease: administration of Trivastal retard 50 should be initiated with 1 tablet daily during the first week. Dosage should then be gradually increased every week until achieving the optimal therapeutic dose: as monotherapy: 3 to 5 tablets in 3 to 5 divided doses daily. In combination with L-dopa therapy: 1 to 3 tablets daily. In other indications: 1 tablet daily at the end of the main meal. In severe cases: 2 tablets daily as 2 divided doses.
Trivastal retard 50 is a nonergot dopamine agonist, selective for D2 and D3 dopamine receptors subtypes at the cerebral and at the peripheral level.
Cardiogenic shock. Acute phase of myocardial infarction.
[edit] Adverse:
rare side effects: minor gastrointestinal disorders (nausea, vomiting, flatulence) in predisposed individuals, or when taken between meals. They may resolve with the following: individual dosage adjustment, and/or addition of domperidone. Orthostatic hypotension or drowsiness may occur, particularly in predisposed individuals (underlying condition or causative illness).
Dopaminergic antagonists.
[edit] Overdosage:
At very high doses, Trivastal retard 50 has an emetic action on the CTZ (chemoreceptive trigger zone). Tablets will thus be rapidly rejected, which explains why no data are currently available concerning the risk of overdosage.
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