piribedil

Action and Spectrum

Actions and spectrum: 

piribedil is a dopamine agonist medication primarily used to treat Parkinson’s disease and certain related disorders. Its action involves stimulating dopamine receptors in the brain, particularly the D2 and D3 receptors.

This stimulation helps to compensate for the dopamine deficiency associated with Parkinson’s disease, leading to improved motor control and reduced tremors and rigidity.

The spectrum of piribedil’s action is focused on addressing motor symptoms and enhancing dopaminergic activity in Parkinson’s disease patients. 

Drug Interaction

Adverse Reaction

Frequency not defined 

increased libido 

abnormal behaviour 

peripheral oedema 

orthostatic hypotension 

Syncope 

Vomiting 

Malaise 

Hypotension 

Dizziness 

Flatulence 

Nausea 

Dyskinesia 

Black Box Warning

Black Box Warning: 

There are no black box warnings specifically associated with piribedil. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: piribedil should not be used in individuals who have a known hypersensitivity or allergy to the medication or any of its components. 
• Severe Cardiovascular Conditions: piribedil should be avoided in individuals with severe cardiovascular conditions, such as severe hypotension or uncontrolled hypertension. 
• Active Peptic Ulcer: Individuals with active peptic ulcers or a history of gastrointestinal bleeding should avoid piribedil due to its potential to increase the risk of bleeding. 
• Pregnancy and Breastfeeding: The use of piribedil during pregnancy and breastfeeding is not recommended due to limited safety data. Consultation with a healthcare provider is crucial in these situations. 
• Pheochromocytoma: piribedil may exacerbate the symptoms of pheochromocytoma, the adrenal gland that can causes high blood pressure & other symptoms.

Caution: 

• Cardiovascular Conditions: piribedil may have cardiovascular effects, including changes in blood pressure. Caution is advised in individuals with a history of cardiovascular diseases, including hypotension, hypertension, arrhythmias, and angina. 
• Renal and Hepatic Impairment: Patients with impaired kidney or liver function may require dose adjustments of piribedil. Close monitoring of these individuals is important to ensure the medication is well-tolerated. 
• Orthostatic Hypotension: piribedil can cause orthostatic hypotension, a drop in blood pressure upon standing. Patients should be cautious when changing positions to minimize the risk of falls. 
• Gastrointestinal Conditions: piribedil may cause gastrointestinal side effects, including nausea, vomiting, and abdominal discomfort. Caution is needed in individuals with a history of peptic ulcers or gastrointestinal bleeding. 
• Psychiatric Conditions: Careful monitoring is required in patients with a history of psychiatric disorders, as piribedil’s effects on the central nervous system can potentially impact mood and mental state. 
• Elderly Patients: They may be more sensitive to the effects of piribedil, including its cardiovascular and central nervous system effects. Dose adjustments and close monitoring are advisable.

Comorbidities: 

• Depression: Depression is a common comorbidity in people with Parkinson’s disease. The neurological changes associated with Parkinson’s can contribute to mood disorders. 
• Cognitive Impairment: Some individuals with Parkinson’s disease may experience cognitive impairment or dementia, which can affect memory, thinking, and decision-making. 
• Orthostatic Hypotension: Parkinson’s disease can lead to orthostatic hypotension. This condition may be comorbid with Parkinson’s. 
• Sleep Disorders: Sleep disturbances, such as insomnia and restless legs syndrome, are common comorbidities in Parkinson’s disease. 
• Gastrointestinal Issues: Constipation and other gastrointestinal problems may be comorbid with Parkinson’s disease. 
• Bladder Dysfunction: Bladder issues, including urinary urgency, frequency, or incontinence, can occur alongside Parkinson’s. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

piribedil is a medication with a multifaceted pharmacology primarily used in the management of Parkinson’s disease. It acts as a dopamine agonist, stimulating dopamine receptors in the brain, particularly the D2 and D3 receptor subtypes.

This stimulation compensates for the dopamine deficiency seen in Parkinson’s disease, alleviating motor symptoms such as tremors and rigidity.

Additionally, piribedil possesses alpha-2 adrenergic receptor antagonist properties, which contribute to its beneficial effects on motor function and its potential to improve cognitive function and mood in some patients.  

Pharmacodynamics: 

• Dopamine Agonism: piribedil acts as a dopamine agonist by stimulating dopamine receptors, particularly the D2 and D3 receptor subtypes. This stimulation helps compensate for the dopamine deficiency commonly seen in Parkinson’s disease. By enhancing dopaminergic activity, piribedil can alleviate motor symptoms such as tremors, rigidity, and bradykinesia (slowness of movement). 
• Alpha-2 Adrenergic Receptor Antagonism: In addition to its dopaminergic effects, piribedil possesses alpha-2 adrenergic receptor antagonist properties. This action contributes to its overall therapeutic benefits. By antagonizing alpha-2 adrenergic receptors, piribedil may enhance noradrenergic and serotonergic neurotransmission, potentially improving cognitive function, mood, and alertness in some patients. 
• Cognitive Enhancement: Some studies suggest that piribedil may have cognitive-enhancing effects, related to its actions on alpha-2 adrenergic receptors and its potential to modulate neurotransmitter systems involved in cognitive function. 
• Mood Improvement: piribedil may have mood-stabilizing effects, which can be particularly relevant for individuals with Parkinson’s disease who may experience mood disturbances, including depression and anxiety. 
• Motor Symptom Relief: By increasing dopaminergic activity, piribedil helps alleviate the motor symptoms of Parkinson’s disease, improving patient’s ability to perform daily activities.

Pharmacokinetics: 

Absorption 

piribedil is orally administered, typically in tablet form. It is well absorbed from the gastrointestinal tract after oral ingestion. Absorption may be influenced by food, with better absorption occurring when taken with a meal. Peak plasma concentrations are reached within a few hours after ingestion. 

Distribution 

piribedil is distributed throughout the body, including the central nervous system, due to its ability to cross the blood-brain barrier. It has a moderate volume of distribution, indicating that it is distributed to various tissues. 

Metabolism 

piribedil undergoes hepatic metabolism, primarily by cytochrome P450 enzyme, particularly the CYP3A4 and CYP2D6 enzymes. The metabolites of piribedil are less pharmacologically active than the parent compound. 

Elimination and excretion 

piribedil and its metabolites are excreted through the kidneys. Renal clearance plays a vital role in the elimination of piribedil from the body. The elimination half-life of piribedil is short, typically in the range of several hours. 

Adminstartion

Administration: 

• Dosage: The dosage of piribedil is determined by the treating healthcare provider and is based on the patient’s condition and response to treatment.  
• Frequency: piribedil is usually taken once or twice daily. The dosing frequency will be specified by the healthcare provider and is typically based on the product’s formulation and the patient’s needs. 
• Timing: piribedil may be taken with or without food, although taking it with a meal can improve its absorption. Follow the healthcare provider’s instructions regarding when and how to take the medication. 
• Tablets: piribedil tablets should be swallowed whole with a glass of water. Not to chew, break, crush the tablets unless directed otherwise by a healthcare provider. 
• Duration: Continue taking piribedil for the full duration prescribed by the healthcare provider, even if you start to feel better. It is essential to maintain a consistent treatment regimen to manage the symptoms effectively. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: piribedil 

Pronounced: (peer-ih-BEH-dil)  

Why do we use piribedil? 

• Parkinson’s Disease: piribedil is used as an adjunctive treatment in Parkinson’s disease, characterized by loss of dopaminergic neurons in the brain. It acts as a dopamine agonist, stimulating dopamine receptors to alleviate motor symptoms such as tremors, rigidity, and bradykinesia (slowness of movement).  
• Restless Legs Syndrome (RLS): piribedil may also be prescribed to treat restless legs syndrome, characterized by uncomfortable sensations in legs, often occurring at night or during periods of rest. 
• Cognitive Enhancement: Some studies suggest that piribedil may have cognitive-enhancing effects, particularly in patients with cognitive deficits associated with Parkinson’s disease. It may help improve memory and executive function. 
• Mood Stabilization: piribedil may have mood-stabilizing effects, which can be beneficial for individuals with Parkinson’s disease who experience mood disturbances, including depression and anxiety.