PharmacologyNeuropharmacologyAntiparkinsonian Drugs

Antiparkinsonian Drugs

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Introduction

Parkinsons disease
Parkinsons disease Normal and Depreciated Substantia Nigra

Antiparkinsonian drugs are a group of medications used to treat the symptoms of Parkinson’s disease, a neurodegenerative disorder characterized by tremors, rigidity, and bradykinesia. These drugs work by either increasing dopamine levels in the brain or blocking the effects of acetylcholine. Here is a classification of antiparkinsonian drugs along with examples, their mechanism of action, uses, adverse effects, drug interactions, and contraindications:

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  1. Dopamine Precursors:

a) Levodopa (L-dopa):

Mechanism of action: Levodopa is a precursor of dopamine that crosses the blood-brain barrier and is converted to dopamine in the brain. It increases dopamine levels in the brain, improving motor function in Parkinson’s disease.

Levodopa MOA in Parkinsons disease
Levodopa Mechanism of Action

b) Carbidopa:

Mechanism of action: Carbidopa is a peripheral dopa-decarboxylase inhibitor that prevents the breakdown of levodopa before it reaches the brain. It enhances the effect of levodopa in the brain, reducing the dosage needed to achieve therapeutic effects.

Levodopa and Carbidopa (combination)

Mechanism of Action: Levodopa is converted to dopamine in the brain, thereby increasing the levels of dopamine. Carbidopa prevents the peripheral breakdown of levodopa, allowing more levodopa to reach the brain.

Uses: These drugs (combination) are the most effective for treating the motor symptoms of Parkinson’s disease.

Adverse Effects: Nausea, vomiting, orthostatic hypotension, dyskinesia, hallucinations, and confusion.

Drug Interactions: Antipsychotic medications, MAO inhibitors, and vitamin B6 can interfere with the effectiveness of these drugs.

Contraindications: Narrow-angle glaucoma, active psychosis, and recent myocardial infarction.

  1. Dopamine Agonists:

a) Pramipexole:

Mechanism of action: Pramipexole is a dopamine agonist that binds to dopamine receptors in the brain, stimulating dopamine release and improving motor function in Parkinson’s disease.

Uses: Pramipexole is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, vomiting, orthostatic hypotension, dyskinesia, hallucinations, compulsive behavior.

Drug interactions: Other dopamine agonists, antipsychotics, antidepressants.

Contraindications: Hypersensitivity to pramipexole.

b) Ropinirole:

Mechanism of action: Ropinirole is a dopamine agonist that binds to dopamine receptors in the brain, stimulating dopamine release and improving motor function in Parkinson’s disease.

Uses: Ropinirole is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, vomiting, orthostatic hypotension, dyskinesia, hallucinations, compulsive behavior.

Drug interactions: Other dopamine agonists, antipsychotics, antidepressants.

Contraindications: Hypersensitivity to ropinirole.

  1. Anticholinergics:

a) Benztropine:

Mechanism of action: Benztropine is an anticholinergic drug that blocks the effects of acetylcholine in the brain, reducing tremors and rigidity in Parkinson’s disease.

Uses: Benztropine is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Dry mouth, blurred vision, constipation, urinary retention, confusion, hallucinations.

Drug interactions: Other anticholinergic drugs, tricyclic antidepressants, antipsychotics.

Contraindications: Glaucoma, prostatic hypertrophy, myasthenia gravis.

b) Trihexyphenidyl:

Mechanism of action: Trihexyphenidyl is an anticholinergic drug that blocks the effects of acetylcholine in the brain, reducing tremors and rigidity in Parkinson’s disease.

Uses: Trihexyphenidyl is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Dry mouth, blurred vision, constipation, urinary retention, confusion, hallucinations.

Drug interactions: Other anticholinergic drugs, tricyclic antidepressants, antipsychotics.

Contraindications: Glaucoma, prostatic hypertrophy, myasthenia gravis.

  1. MAO-B Inhibitors:

a) Rasagiline:

Mechanism of action: Rasagiline is a selective MAO-B inhibitor that inhibits the breakdown of dopamine in the brain, increasing dopamine levels and improving motor function in Parkinson’s disease.

Uses: Rasagiline is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, headache, orthostatic hypotension, dyskinesia.

Drug interactions: Other MAO inhibitors, antidepressants, opioids.

Contraindications: Hypersensitivity to rasagiline.

b) Selegiline:

Mechanism of action: Selegiline is a selective MAO-B inhibitor that inhibits the breakdown of dopamine in the brain, increasing dopamine levels and improving motor function in Parkinson’s disease.

Uses: Selegiline is used to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, headache, orthostatic hypotension, dyskinesia.

Drug interactions: Other MAO inhibitors, antidepressants, opioids.

Contraindications: Hypersensitivity to selegiline.

  1. COMT Inhibitors:

a) Entacapone:

Mechanism of action: Entacapone is a COMT inhibitor that blocks the breakdown of levodopa in the peripheral tissues, increasing the amount of levodopa available in the brain and improving motor function in Parkinson’s disease.

Uses: Entacapone is used in combination with levodopa to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, diarrhea, dyskinesia, confusion, hallucinations.

Drug interactions: Other COMT inhibitors, levodopa, dopamine agonists.

Contraindications: Hypersensitivity to entacapone.

b) Tolcapone:

Mechanism of action: Tolcapone is a COMT inhibitor that blocks the breakdown of levodopa in the peripheral tissues and in the brain, increasing the amount of levodopa available and improving motor function in Parkinson’s disease.

Uses: Tolcapone is used in combination with levodopa to treat the symptoms of Parkinson’s disease.

Adverse effects: Nausea, diarrhea, dyskinesia, confusion, hallucinations, hepatotoxicity.

Drug interactions: Other COMT inhibitors, levodopa, dopamine agonists.

Contraindications: Liver disease, history of liver problems.

In summary, antiparkinsonian drugs can be classified into dopamine precursors, dopamine agonists, anticholinergics, MAO-B inhibitors, and COMT inhibitors. These drugs work by increasing dopamine levels in the brain or by blocking the effects of acetylcholine. The choice of drug and dosage depends on the severity of symptoms, the age of the patient, and the presence of comorbidities. It is essential to monitor patients closely for adverse effects and drug interactions.

Disclaimer: This article is for informational purposes only and should not be taken as medical advice. Always consult with a healthcare professional before making any decisions related to medication or treatment.

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Disclaimer: This article is for informational purposes only and does not constitute medical advice. Always seek the advice of a healthcare provider with any questions regarding a medical condition.

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