Podcast
Questions and Answers
Which of the following drugs are classified as MAO-B inhibitors?
Which of the following drugs are classified as MAO-B inhibitors?
- Entacapone
- Selegiline (correct)
- Rasagiline (correct)
- Amantadine
Levodopa can be used alone to treat Parkinson's disease effectively.
Levodopa can be used alone to treat Parkinson's disease effectively.
False (B)
What is the primary effect of D1-like dopamine receptors?
What is the primary effect of D1-like dopamine receptors?
Excitatory effect, increasing cAMP formation
Entacapone and Tolcapone are examples of __________ inhibitors.
Entacapone and Tolcapone are examples of __________ inhibitors.
Match the drug with its corresponding function:
Match the drug with its corresponding function:
What is the effect of bromocriptine when used alone in patients with parkinsonism?
What is the effect of bromocriptine when used alone in patients with parkinsonism?
Ropinirole and pramipexole have a high affinity for D1 and nondopaminergic receptors.
Ropinirole and pramipexole have a high affinity for D1 and nondopaminergic receptors.
What is the initial dose of bromocriptine recommended for patients?
What is the initial dose of bromocriptine recommended for patients?
The combination of levodopa with a decarboxylase inhibitor is known as __________.
The combination of levodopa with a decarboxylase inhibitor is known as __________.
Match the following medications with their description:
Match the following medications with their description:
Which dopamine receptors are primarily involved in the therapeutic response to levodopa?
Which dopamine receptors are primarily involved in the therapeutic response to levodopa?
Dopamine receptors are uniformly expressed throughout the entire brain.
Dopamine receptors are uniformly expressed throughout the entire brain.
What is the effect of stimulating both excitatory D1 and inhibitory D2 receptors in the striatum?
What is the effect of stimulating both excitatory D1 and inhibitory D2 receptors in the striatum?
About ______% of administered levodopa crosses to the brain.
About ______% of administered levodopa crosses to the brain.
Match the dopamine receptor subtype to its predominant area in the brain:
Match the dopamine receptor subtype to its predominant area in the brain:
What percentage of patients experience dizziness or fainting attacks from postural hypotension when receiving antihypertensives?
What percentage of patients experience dizziness or fainting attacks from postural hypotension when receiving antihypertensives?
Tolerance to postural hypotension does not develop with continued treatment.
Tolerance to postural hypotension does not develop with continued treatment.
What is the plasma half-life (t½) of levodopa?
What is the plasma half-life (t½) of levodopa?
The enzyme that requires pyridoxal as a cofactor for levodopa metabolism is _______.
The enzyme that requires pyridoxal as a cofactor for levodopa metabolism is _______.
Match the following adverse effects of levodopa therapy with their descriptions:
Match the following adverse effects of levodopa therapy with their descriptions:
Flashcards
Levodopa
Levodopa
A drug that acts as a precursor to dopamine and is used to treat Parkinson's disease.
Dopamine Agonists
Dopamine Agonists
A class of drugs that increase dopamine levels in the brain. They are used to treat Parkinson's disease.
MAO-B Inhibitor
MAO-B Inhibitor
A type of drug that blocks the breakdown of dopamine by the enzyme MAO-B. This leads to higher dopamine levels in the brain.
COMT Inhibitor
COMT Inhibitor
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Amantadine
Amantadine
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Postural Hypotension
Postural Hypotension
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Levodopa Metabolism
Levodopa Metabolism
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Dyskinesias
Dyskinesias
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Phenothiazines, Butyrophenones, Metoclopramide
Phenothiazines, Butyrophenones, Metoclopramide
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Abnormal Movements
Abnormal Movements
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Dopamine Receptor Subtypes
Dopamine Receptor Subtypes
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D1 & D2 Receptors in Striatum
D1 & D2 Receptors in Striatum
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D1 & D2 Receptor Effects in Striatum
D1 & D2 Receptor Effects in Striatum
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D3 Receptors in Nucleus Accumbans & Hypothalamus
D3 Receptors in Nucleus Accumbans & Hypothalamus
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Peripheral Dopamine and Heart Rate
Peripheral Dopamine and Heart Rate
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Co-careldopa
Co-careldopa
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Ropinirole
Ropinirole
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Pramipexole
Pramipexole
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Study Notes
Parkinson's Disease
- Parkinsonism is an extrapyramidal motor disorder characterized by rigidity, tremors, and hypokinesia
- Secondary symptoms can include poor posture, gait issues, a mask-like face, and excessive saliva production (sialorrhoea)
- Advanced cases can lead to immobility, difficulty breathing, and susceptibility to infections or embolisms
- Parkinson's disease (PD) is a degenerative disorder primarily affecting older adults first described in 1817 by James Parkinson, it has multiple potential causes (idiopathic, arteriosclerotic, or post-encephalitic)
- Wilson's disease (hepatolenticular degeneration) also results in copper toxicity and can cause parkinsonism
- A key feature of PD is the degeneration in the substantia nigra pars compacta (SN-PC) and the nigrostriatal tract (dopaminergic)
- This results in reduced dopamine (DA) in the striatum, which controls muscle tone and coordinated movements
- Imbalance between dopaminergic (inhibitory) and cholinergic (excitatory) systems cause movement problems
- The exact cause of neuronal degeneration is unknown, but factors like oxidation of dopamine by MAO-B and aldehyde dehydrogenase, alongside free radical damage, genetic predisposition, and mitochondrial dysfunction may play a role.
- Environmental toxins can exacerbate these factors
- Synthetic toxins, such as N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), may trigger parkinsonism-like symptoms by damaging dopaminergic neurons.
Antiparkinsonian Drugs
- Levodopa is a dopamine precursor that effectively treats PD, exceeding other treatments
- Levodopa itself is inactive; it is converted to dopamine in the periphery
- Only a small percentage of levodopa reaches the brain due to the blood-brain barrier
- Levodopa is often taken with peripheral decarboxylase inhibitors (carbidopa, benserazide) to slow its peripheral metabolism and allow more to reach the brain
- Dopamine agonists (bromocriptine, ropinirole, pramipexole) stimulate dopamine receptors, offering an alternative or supplementary treatment
- Selective MAO-B inhibitors (selegiline, rasagiline) reduce dopamine breakdown in the brain, prolonging levodopa effects
- Catechol-O-methyltransferase (COMT) inhibitors (entacapone, tolcapone) block COMT, maintaining dopamine levels longer by preventing its breakdown.
- Glutamate antagonists (amantadine) may offer another approach to treating parkinsonian symptoms
Classification of Antiparkinsonian Drugs
- Drugs affecting the brain's dopaminergic system
- Dopamine Precursor: Levodopa (l-dopa)
- Peripheral Decarboxylase Inhibitors: Carbidopa, Benserazide
- Dopamine Agonists: Bromocriptine, Ropinirole, Pramipexole
- MAO-B Inhibitors: Selegiline, Rasagiline
- COMT Inhibitors: Entacapone, Tolcapone
- Drugs affecting the brain's cholinergic system
- Central Anticholinergics: Trihexyphenidyl (Benzhexol), Procyclidine, Biperiden
- Antihistaminics: Orphenadrine, Promethazine
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Description
This quiz covers key aspects of Parkinson's disease, including its characteristics, symptoms, and underlying neurobiological mechanisms. Participants will explore the differences between primary and secondary parkinsonism, as well as the role of dopamine in movement control. Test your knowledge of this complex disorder that primarily affects older adults.
