Piribedil

Piribedil

Clinical data
AHFS/Drugs.com	International Drug Names
Routes of administration	By mouth
ATC code	N04BC08 (WHO)
Legal status
Legal status	EU: Rx-only[1] In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	10% (peak at 1 hour)
Protein binding	70–80%
Metabolism	extensive liver
Elimination half-life	1.7–6.9 hours
Excretion	Kidney (68%) and bile duct (25%)
Identifiers
IUPAC name 2-[4-(benzo[1,3]dioxol-5-ylmethyl)piperazin-1-yl]pyrimidine
JSmol)	Interactive image
SMILES C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4
InChI InChI=1S/C16H18N4O2/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14/h1-5,10H,6-9,11-12H2 N Key:OQDPVLVUJFGPGQ-UHFFFAOYSA-N N
NY (what is this?)  (verify)

Piribedil (trade names Pronoran, Trivastal Retard, Trastal, Trivastan, Clarium and others) is an

• Treatment of
  levodopa
  ) or in combination with L-DOPA therapy, in the early stages of the disease as well as in the advanced ones
• Treatment of
  elderly (impaired attention, motivation, memory
  , etc.)
• Treatment of dizziness in the young patients
• Treatment of
  ischemic
  manifestations
• Adjunctive treatment of
  lower limbs
  (stage 2)
• Adjunctive treatment of
  off label
  )
• Treatment of gait disorders associated with Parkinson's disease (no related cause) and other forms of parkinsonism

Other uses

The drug has been shown to enhance working memory capacities in normal aging adults.^[4]

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.^[5]

It enhances cognitive skill learning in healthy older adults.^[6]

It showed a positive effect in restless legs syndrome.^[7]

Side effects

• Minor
  gastrointestinal upset (nausea, vomiting, flatulence, etc.) in predisposed individuals, or when taken between meals: adjust dosage individually, and/or add domperidone
  ;
• drowsiness
  may occur, particularly in predisposed individuals (underlying condition or causative illness);
• Mild dizziness, confusion and feeling "drunk" also may occur.

As with other dopamine agonists (like

Another rare side effect of piribedil is excessive daytime sleepiness and unintended sleep episodes.[9]^[10]

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.^{[medical citation needed]}

Interactions

Dopamine antagonists reduce the effect of piribedil.^{[medical citation needed]}

Pharmacology

Pharmacodynamics

• Dopamine receptor agonist, selective for subtypes D₂ and D₃.
• Dopamine receptor antagonist, selective for subtypes D₄.^[11][12][13]
• Adrenergic receptor antagonist, subtypes α_2A and α_2C.^[14]
• Lack of affinity to
  serotonin receptor 5-HT_2B.^[14]