Parkinson's Disease Medications Quiz
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Questions and Answers

What is the primary mechanism of action for Amantadine in treating Parkinson's disease?

  • Direct stimulation of dopamine receptors
  • Inhibition of acetylcholinesterase
  • Release and reuptake of dopamine (correct)
  • Release and reuptake of serotonin

Why are anticholinergics considered less effective for treating bradykinesia in Parkinson's disease?

  • They enhance motor neuron excitability
  • They only alleviate tremor and rigidity (correct)
  • They have sedative effects that impair movement
  • They primarily target serotonin pathways

What is a significant side effect associated with the use of Amantadine?

  • Cognitive decline
  • Urinary retention (correct)
  • Severe hypertension
  • Severe hallucinations

Which statement about Rasagiline is true?

<p>It can be used alone in early Parkinson's disease (B)</p> Signup and view all the answers

What condition should be avoided when prescribing Amantadine?

<p>Renal failure (C)</p> Signup and view all the answers

What is the primary reason neurodegenerative diseases are often difficult to treat?

<p>CNS neurons cannot divide or regenerate once damaged. (D)</p> Signup and view all the answers

Which of the following is NOT one of the cardinal motor features of Parkinson’s disease?

<p>Loss of sensation (A)</p> Signup and view all the answers

Which neurotransmitter is primarily involved in regulating muscle movement in Parkinson’s disease?

<p>Dopamine (A)</p> Signup and view all the answers

Which of the following describes a characteristic pathway of dopaminergic neurons?

<p>Tuberoinfundibular pathway regulates prolactin secretion. (A)</p> Signup and view all the answers

What is a non-motor symptom associated with Parkinson’s disease?

<p>Visual hallucinations (A)</p> Signup and view all the answers

Excessive excitotoxicity in the central nervous system is primarily caused by which substance?

<p>Glutamate (B)</p> Signup and view all the answers

Which age group is primarily affected by Parkinson’s disease?

<p>Elderly people over 65 (B)</p> Signup and view all the answers

Which process is NOT a cause of neuronal damage in neurodegenerative diseases?

<p>Increased neurotransmitter synthesis (D)</p> Signup and view all the answers

What is a common central side effect of levodopa therapy?

<p>Dyskinesia (C)</p> Signup and view all the answers

Which of the following is a known peripheral side effect of levodopa?

<p>Tachycardia (A)</p> Signup and view all the answers

What medication is commonly used to manage levodopa-induced nausea?

<p>Domperidone (D)</p> Signup and view all the answers

Which receptor type is primarily overstimulated in the development of dyskinesia due to levodopa?

<p>D2 receptors (B)</p> Signup and view all the answers

How does long-term levodopa use affect dopamine receptors in the brain?

<p>It increases receptor sensitivity. (A)</p> Signup and view all the answers

What is the primary risk associated with the use of tolcapone?

<p>Hepatotoxicity (C)</p> Signup and view all the answers

Which atypical antipsychotic is mentioned as being used to treat levodopa-induced psychosis?

<p>Quetiapine (A)</p> Signup and view all the answers

What is the primary reason a D2 blocker like metoclopramide is not used for levodopa-induced nausea?

<p>It crosses the blood-brain barrier. (B)</p> Signup and view all the answers

What characterizes Primary Parkinson’s Disease?

<p>Degeneration of more than 80% of DA neurons (D)</p> Signup and view all the answers

Which of the following is a form of Secondary Parkinsonism?

<p>Drug-induced Parkinsonism (B)</p> Signup and view all the answers

What is the primary goal of Parkinson's treatment?

<p>Restore DA and reduce Ach levels (B)</p> Signup and view all the answers

Why does levodopa require large doses for effectiveness?

<p>Most is converted to dopamine in the gut and liver (C)</p> Signup and view all the answers

How does carbidopa benefit the treatment of Parkinson’s disease?

<p>It enhances the availability of levodopa to the CNS (D)</p> Signup and view all the answers

What does the presence of oxidative stress correlate with in Parkinson’s Disease?

<p>Aging and neuron degeneration (D)</p> Signup and view all the answers

Which treatment specifically targets tremors and rigidity in Parkinson's disease?

<p>Anticholinergic drugs (B)</p> Signup and view all the answers

What is a significant challenge in using levodopa for treatment?

<p>It does not cross the blood-brain barrier (D)</p> Signup and view all the answers

What is a significant advantage of dopamine receptor agonists over levodopa?

<p>They do not require presynaptic conversion to dopamine. (A)</p> Signup and view all the answers

Which of the following is an adverse effect associated with dopamine receptor agonists?

<p>Pulmonary fibrosis with prolonged use. (D)</p> Signup and view all the answers

In what scenario is apomorphine predominantly used?

<p>As a subcutaneous injection during OFF periods of L-dopa. (B)</p> Signup and view all the answers

Which is true about the MAOB inhibitor deprenyl?

<p>It serves as a free radical scavenger. (D)</p> Signup and view all the answers

What is a potential drug-disease interaction with bromocriptine?

<p>Exacerbation of peripheral vascular disease. (C)</p> Signup and view all the answers

Which statement about the effects of dopamine receptor agonists is correct?

<p>Over time, they may cause more neuropsychiatric issues than levodopa monotherapy. (C)</p> Signup and view all the answers

Which medication is taken orally as a dopamine receptor agonist?

<p>Pramipexole (A)</p> Signup and view all the answers

What is a common side effect of deprenyl?

<p>Insomnia if administered too late in the day. (C)</p> Signup and view all the answers

What is the physiological effect of D1 receptor stimulation in renal blood vessels?

<p>Increases sodium excretion (C)</p> Signup and view all the answers

What phenomenon describes the gradual fading of improvement from levodopa medication before the next dose?

<p>Wear-off phenomenon (A)</p> Signup and view all the answers

How can high protein diets affect the absorption of L-dopa?

<p>Decrease absorption of L-dopa (B)</p> Signup and view all the answers

Which strategy can not help overcome the on-off phenomenon of levodopa?

<p>Taking levodopa with high-protein food (A)</p> Signup and view all the answers

What effect does Vitamin B6 (pyridoxine) have on the efficacy of L-dopa?

<p>Enhances peripheral conversion of L-dopa to dopamine (C)</p> Signup and view all the answers

What is a potential risk of combining levodopa with nonselective MAO inhibitors?

<p>Hypertensive crisis (B)</p> Signup and view all the answers

Which side effect may occur in patients taking anti-psychotics that block D2 receptors?

<p>Parkinsonian syndrome (D)</p> Signup and view all the answers

What condition should cardiac patients be monitored for when using dopaminergic drugs?

<p>Cardiac arrhythmias (D)</p> Signup and view all the answers

Flashcards

Parkinson's Disease

Progressive neurological disorder affecting muscle movement, characterized by slowness of movement (bradykinesia), muscle rigidity, resting tremor, and abnormal gait. In late stages, it can lead to akinesia, where the patient is immobile.

Akinesia

A state of complete or almost complete loss of movement.

Bradykinesia

A decrease in the ability to move quickly and smoothly

Muscle Rigidity

A state of increased muscle tone, resulting in stiffness and resistance to movement.

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Resting Tremor

Involuntary quivering or shaking, especially noticeable when at rest.

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Abnormal Gait

Characterized by slow, shuffling steps and a forward-bent posture.

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Neurodegenerative Disease

A group of brain disorders characterized by the progressive loss of neurons in specific areas of the brain.

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Apoptosis

A process of programmed cell death that occurs naturally in the body.

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What is Primary Parkinson's disease?

Primary PD, also known as idiopathic PD, is the most common type of Parkinson's disease. It occurs due to the degeneration of more than 80% of dopamine (DA) neurons in the substantia nigra, leading to a significant decrease in DA levels and an increase in acetylcholine (Ach). This imbalance contributes to the symptoms of PD.

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What is Secondary Parkinson's disease?

Secondary Parkinsonism, or Atypical Parkinsonism, is a group of conditions that mimic the symptoms of PD but arise from different underlying causes. These causes include:

  • Vascular Parkinsonism: Due to multiple small strokes affecting brain regions involved in movement control.
  • Post-Traumatic Parkinsonism: Resulting from repeated head trauma.
  • Toxin-Induced Parkinsonism: Caused by exposure to certain toxins like carbon monoxide, manganese, or pesticides.
  • Infectious Parkinsonism: Infection-related damage to brain motor regions.
  • Drug-induced Parkinsonism: Induced by certain medications, particularly dopamine blockers like antipsychotics.
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What is the treatment goal for PD?

Anti-Parkinsonian medications aim to restore the balance between dopamine (DA) and acetylcholine (Ach) in the brain. There are two main types:

  1. Dopaminergic drugs: Increase DA levels by various mechanisms.
  2. Anticholinergic drugs: Decrease Ach levels, mainly targeting tremors and rigidity.
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How does Levodopa (L-dopa) work?

Levodopa (L-dopa) is a precursor to dopamine. Unlike dopamine itself, L-dopa can cross the blood-brain barrier and is converted into dopamine inside the brain. This helps restore the balance between dopamine (DA) and Acetylcholine (Ach) levels in the brain.

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Why are large doses of Levodopa needed?

Large doses of Levodopa are required because most of it is broken down into dopamine in the body (gut, blood, liver) before reaching the brain. This causes side effects.

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What is the purpose of Carbidopa and Benserazide?

Carbidopa and Benserazide are medications used alongside Levodopa. They inhibit an enzyme called dopa decarboxylase that converts Levodopa to dopamine outside of the brain. This increases the amount of Levodopa that reaches the brain, allowing for a smaller dosage to be used.

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What is 'Wear-off phenomenon' in Parkinson's treatment?

The gradual decrease in the effectiveness of levodopa medication over time, leading to the return of Parkinson's symptoms before the next dose is due.

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What is the 'On-Off phenomenon' in Parkinson's treatment?

The phenomenon where fluctuations in levodopa's plasma concentration cause periods of normal movement (on) alternating with periods of Parkinson's symptoms (off).

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How does levodopa affect the pupils?

Stimulates α1-receptors on the radial muscle of the eye, causing dilation of the pupils (mydriasis) in high doses; contraindicated in patients with narrow-angle glaucoma.

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How does protein intake affect levodopa absorption?

Levodopa's absorption from the small intestine is reduced by the presence of protein in the diet.

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What is the mechanism of action of levodopa?

Levodopa is converted to dopamine, a neurotransmitter that is deficient in Parkinson's disease.

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How does levodopa cross the blood-brain barrier?

Levodopa is transported into the brain via active amino acid transport, competing with other amino acids.

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How does vitamin B6 affect levodopa's efficacy?

Vitamin B6 enhances the peripheral conversion of levodopa to dopamine, reducing the effectiveness of levodopa in reaching the brain.

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Why are non-selective MAO inhibitors problematic with levodopa?

Non-selective MAO inhibitors can increase dopamine levels, potentially leading to dangerous interactions with levodopa.

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What are MAOB inhibitors?

MAOB inhibitors are a type of medication used to treat Parkinson's disease. They work by specifically inhibiting the enzyme MAOB, which breaks down dopamine in the brain. This leads to increased dopamine levels, which helps to alleviate the symptoms of Parkinson's disease.

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What is Rasagiline?

Rasagiline is a medication used to treat Parkinson's disease. It is a highly potent and selective inhibitor of MAOB, meaning it effectively blocks the enzyme that breaks down dopamine in the brain. It can be used on its own or in combination with other medications.

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What is Amantadine?

Amantadine is a medication used to treat Parkinson's disease. It works by increasing dopamine release and decreasing its reuptake in the brain. It is less effective than L-dopa and its effects diminish over time.

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What are anticholinergic drugs?

Anticholinergic drugs are a type of medication used to treat Parkinson's disease. They work by blocking the action of acetylcholine, a neurotransmitter that contributes to the symptoms of Parkinson's disease.

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Give examples of anticholinergic drugs used to treat Parkinson's disease.

Benztropine, Trihexyphenidyl, procyclidine, and Biperiden are examples of anticholinergic drugs used to treat Parkinson's disease. They are used as adjunctive therapy, meaning they are used in combination with other medications.

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Peripheral dopa decarboxylase inhibitors

Drugs that inhibit the conversion of levodopa (L-dopa) to dopamine in the periphery, increasing the amount of L-dopa reaching the brain. They help to reduce the side effects associated with peripheral dopamine.

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COMT inhibitors

Drugs that block the enzyme Catechol-O-Methyl Transferase (COMT), preventing the breakdown of L-dopa. They help to increase L-dopa's effectiveness and reduce the dosage required.

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Dyskinesia

Involuntary, abnormal movements that develop in patients taking L-dopa therapy for Parkinson's disease. Usually appear after 4-10 years of treatment due to the overstimulation of dopamine receptors in the brain.

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Central side effects of L-dopa

Neurological side effects of L-dopa therapy, including delusions, hallucinations, psychosis, mood changes, anxiety, and depression. Resulting from the increased dopamine levels in the brain's mesolimbic and mesocortical pathways.

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Nausea, vomiting, and anorexia due to L-dopa

A common side effect of L-dopa therapy affecting the CTZ (Chemoreceptor trigger zone) in the medulla, causing nausea, vomiting, and loss of appetite.

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Domperidone

A medication used to counteract the nausea and vomiting caused by L-dopa. It acts as a D2 receptor blocker but only peripherally, without entering the brain.

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Tachycardia, arrhythmia, and postural hypotension

Peripheral side effect of L-dopa therapy, causing increased heart rate (tachycardia) and irregular heartbeat (arrhythmia). Also contributes to postural hypotension due to dopamine's vasodilatory properties.

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Tolcapone

A potent COMT inhibitor used to treat Parkinson's disease. It is effective in managing symptoms and reducing L-dopa dosage but carries a risk of hepatotoxicity (liver damage).

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What are dopamine receptor agonists and how do they work?

Dopamine receptor agonists stimulate D2 receptors in the striatum, mimicking the effects of dopamine. They are particularly effective in patients who haven't responded well to levodopa, offering advantages like longer duration of action and no dependence on presynaptic conversion to dopamine.

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When are dopamine receptor agonists used in Parkinson's disease?

Dopamine receptor agonists are initially considered for patients with mild Parkinson's Disease (PD) and a younger age of onset. They can also be used as adjuncts to levodopa in patients with severe motor fluctuations. Additionally, they can decrease the dose of L-dopa in advanced PD.

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What are the common side effects of dopamine receptor agonists?

Dopamine receptor agonists can cause nausea, vomiting, confusion, psychomotor excitation, and hallucinations. However, they can cause more severe psychiatric complications compared to levodopa alone, as they directly affect the brain's dopamine system.

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What are the specific risks associated with bromocriptine?

Bromocriptine, an ergotamine derivative, is a dopamine receptor agonist that can worsen peripheral vascular disease due to its vasoconstrictive properties. It can also cause serious cardiac problems in patients with a history of myocardial infarction.

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How is apomorphine used in Parkinson's Disease treatment?

Apomorphine, a non-ergot dopamine receptor agonist, is used as an injection primarily during 'off' periods of L-dopa treatment, helping to reduce the 'frozen' sensation and improve movement. Due to its high risk of nausea, it's usually preceded by an antiemetic.

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What are the different forms and uses of non-ergot dopamine receptor agonists?

Pramipexole and ropinirole are taken orally, while rotigotine is a transdermal patch that can be applied once daily. These non-ergot dopamine receptor agonists are alternatives to bromocriptine with a lower risk of vascular and cardiovascular complications.

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How does Deprenyl affect dopamine levels?

Deprenyl (Selegiline) is an irreversible MAOB inhibitor, specifically targeting MAOB (monoamine oxidase type B) in the brain. It increases dopamine levels by inhibiting its breakdown, and also acts as a free radical scavenger protecting brain cells.

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How is Deprenyl used in treating Parkinson's Disease?

Deprenyl can be used as a single drug in early or mild PD or in combination with L-dopa. It can also help improve motor function in patients experiencing 'wearing off' and 'on-off' phenomena associated with levodopa.

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Study Notes

Drugs Affecting the Central Nervous System

  • Neurodegenerative diseases involve neuronal damage in specific brain areas.
  • Neuronal damage is caused by excitotoxicity (excess glutamate acting on NMDA receptors), stroke, head trauma, oxidative stress (free radicals like OH), and apoptosis (programmed cell death).
  • Neurodegenerative diseases like Parkinson's, Alzheimer's, Huntington's, and Multiple sclerosis are challenging to treat due to the inability of CNS neurons to regenerate once damaged. Treatment focuses on symptom management rather than disease progression.

Antiparkinsonian Drugs

  • Dopamine (DA) is a precursor to norepinephrine and a neurotransmitter in major dopaminergic pathways (nigrostriatal, mesolimbic-mesocortical, tuberoinfundibular, and chemoreceptor trigger zone).
  • The nigrostriatal pathway regulates movement (kinesis).
  • The mesolimbic-mesocortical pathway regulates cognitive functions and sensory perceptions.
  • The tuberoinfundibular pathway regulates prolactin.
  • Dopamine pathways in the brain's substantia nigra are damaged in Parkinson's disease.

Parkinson's Disease

  • Parkinson's Disease (PD) is a progressive neurological disorder affecting muscle movement, characterized by four cardinal motor features: bradykinesia (slow movement), rigidity, resting tremor, and abnormal posture/gait (shuffling gait).
  • Non-motor symptoms include depression, dementia, and sleep disturbances.
  • PD most commonly affects individuals over 65.
  • The etiology involves a balance imbalance between inhibitory dopaminergic (DA) neurons and excitatory cholinergic (Ach) neurons.

Classification of Parkinson's Disease

  • Primary (Idiopathic) PD: Degeneration of greater than 80% of DA neurons, often linked to oxidative stress and aging.
  • Secondary (Atypical) PD has multiple causes: Vascular Parkinsonism caused by multiple small strokes affecting movement control areas, Post-Traumatic Parkinsonism (repeated head injuries), Toxin-induced Parkinsonism (exposure to certain toxins), Infectious Parkinsonism (brain infections), and Drug-induced Parkinsonism (use of dopamine blockers, such as antipsychotics).

Treatment for Parkinson's Disease

  • The goal of treatment is to increase DA and decrease Ach.

  • Dopaminergic drugs and anticholinergic drugs are used.

    • Dopamine receptor agonists also help.
    • Levodopa (L-dopa), a dopamine precursor, is the most commonly used treatment.
    • Large doses of Levodopa are needed, but most is converted to dopamine in the periphery and not the brain causing unwanted effects.
    • Carbidopa is added to levodopa to decrease peripheral conversion.
    • Entacapone and Tolcapone are COMT inhibitors that increase the availability of levodopa to the CNS.
  • Anticholinergic drugs (Benztropine, Trihexyphenidyl, procyclidine,) reduce Ach effects, but primarily treat tremor and rigidity.

Adverse Effects of Levodopa

  • Central adverse effects include dyskinesias (involuntary movements) potentially occurring within 4-10 years after treatment start due to dopamine receptor overstimulation.
  • Central adverse effects also include psychosis (delusions, hallucinations, mood changes, anxiety). Low doses of certain atypical antipsychotics can be helpful in this instance.
  • Peripheral effects can include nausea, vomiting, postural hypotension, and brown saliva, sweat, and urine, due to higher levels of dopamine in the body. Wearing-off phenomenon (end-of-dose deterioration) occurs because symptomatic improvement from a levodopa dose wears off between doses. This can be mitigated through more frequent administrations, sustained release formulations or combination treatments.
  • High protein foods decrease L-dopa absorption. L-dopa absorption can improved by taking it 30 minutes before a meal.
  • Fluctuations in plasma concentrations of levodopa create "on-off" periods, where the symptoms return. This can be mitigated through adjustments to medication dosing or by adding other medications.
  • Levodopa interacts with other drugs including vitamin B6,MAOIs and antipsychotics.
  • Amantadine is an antiviral that also increases dopamine release and is used as an adjunct to levodopa.

Dopamine Receptor Agonists

  • Dopamine receptor agonists stimulate dopamine receptors, and their use is effective in patients who do not respond to levodopa as they reduce motor fluctuations and dyskinesias. These may be less effective than levodopa alone, but are better tolerated in the long term.
  • Bromocriptine is an ergot-derived dopamine receptor agonist. A serious side effect is worsening of peripherial vascular disease from alpha receptor and serotonin receptor stimulation..
  • Non-ergot drugs (Apomorphine,Pramipexole, Ropinirole and Rotigotine) have slightly different side effect profiles and usages, and are usually taken orally or by patch.

MAO-B Inhibitors (Selegiline and Rasagiline)

  • These drugs inhibit MAO-B; a critical enzyme for dopamine metabolism. They have a free radical scavenging effect, preserving DA neurons in brain tissue and increasing L-dopa effects, thus reducing the dosage required.
  • Selegiline can be metabolized to amphetamine or methamphetamine, which can cause insomnia or anxiety.
  • Rasagiline does not have this side effect. It is more potent and can be used in early stages of Parkinson's.

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Test your knowledge on the mechanisms and side effects of key medications in Parkinson's disease treatment. This quiz covers Amantadine, anticholinergics, and Rasagiline, focusing on their efficacy and associated risks. Perfect for students and professionals in medical and health fields.

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