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Pharma Recall - Pharmacology > Ch 15 - Drugs Used to Treat CNS Degenerative Disorders - DONE > Flashcards

Ch 15 - Drugs Used to Treat CNS Degenerative Disorders - DONE Flashcards

1
Q

What is Parkinson´s disease?

A

A movement disorder that has the four following characteristics:

  1. Resting tremors
  2. Muscle rigidity
  3. Bradykinesia
  4. Abnormal posture and gait
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2
Q

What is the pathophysiology of Parkinson’s disease?

A
  • The disorder is thought to occur because of a loss of dopamine in the nigrostriatal pathway.
  • The loss of dopamine disrupts the delicate balance between cholinergic and dopaminergic systems within the stratum and basal ganglia.
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3
Q

What are the pharmacological treatment options for Parkinson´s disease?

A
  1. Dopamine agonists
  2. MAO inhibitors
  3. Amantadine
  4. Antimuscarinic agents
  5. Catechol-O- Methyltransferase (COMT)
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4
Q

Give examples of Dopamine agonists:

A
  • levodopa/carbidopa
  • bromocriptine
  • pergolide
  • pramipexole
  • ropinirole
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5
Q

Give examples of MAO inhibitor:

A

selegiline

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6
Q

Give examples of Catechol-O- Methyltransferase (COMT):

A
  • entacapone

- tolcapone

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7
Q

Can we use drugs to cure Parkinson´s disease?

A

Nope. They neither revers or arrest the disease. And they can offer temporary relief.

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8
Q

What is the treatment strategy for Parkinson´s disease?

A
  • The ultimate goal is to reestablishing the balance between dopamine and acetylcholine in the brain.
  • This can be accomplished by either:
    1. increasing dopamine int he nigrostriatal system
      2. reducing the cholinergic output of the stratum
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9
Q

What is Levodopa?

A
  • metabolic precursor of dopamine

- first-line drug for the treatment of Parkinson´s disease

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10
Q

What is the advantages in using a precursor dopamine?

Levodopa

A

Dopamine itself does not cross the blood-brain barrier. However, Levodopa is transported to the brain and subsequently converted to dopamine in the basal ganglia.

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11
Q

What are the disadvantages of using Levodopa alone?

A

Large doses of Levodopa is required if used alone because this drug is decarboxylated in the periphery to dopamine

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12
Q

What is Levodopa usually used in the combination with?

A

another drug, such as Carbidopa

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13
Q

What are the pharmacokinetics of Levodopa?

A

Levodopa is absorbed well in the GI tract.
However, if it is ingested with high protein meals, its transport across the blood-brain barrier is impaired because of competition from neutral amino acids.

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14
Q

What is the on-off phenomenon?

Levodopa

A

Because Levodopa has an extremely short half-life, plasma levels may drop suddenly.

This may cause sudden immobility, tremors, and cramps.

These rapid changes are called the on-off phenomenon.

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15
Q

**What drugs should NOT be given with Levodopa?

page 113. read for more

A
  • nonselective monoamide oxidase inhibitors
  • pyridoxine
  • antipsychotics
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16
Q

Levodopa AE:

A
  • Nausea, vomiting, arrythmias, and postural hypotention: due to the conversion of Levodopa to dopamine in the periphery
  • Dyskinesia, hallucinations, restlessness, and confusion: due to overstimulation of central dopamine receptors
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17
Q

What is Carbidopa?

A

A dopamine decarboxylase inhibitor that does not cross the blood-brain barrier.

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18
Q

Why do we use Carbidopa?

A

When administered with Levodopa, Carbidopa reduces the metabolism of dopamine in the periphery and therefore increases the availability of dopamine in the CNS.

  • With the use of Carbidopa we need less Levodopa.
  • Carbidopa also reduces the side effects of Levodopa, such as nausea and vomiting
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19
Q

What is the efficacy of levodopa/Carbidopa (Sinemet) treatment?

A
  • The treatment efficacy declines as the disease progresses. This occurs because Levodopa requires some healthy dopaminergic neurons to be effective
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20
Q

What is Bromocriptine?

A
  • Bromocriptine is an ergotamine derivative that acts as a dopamine receptor agonist at D2 receptors.
  • It is a second-line drug after Levodopa.
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21
Q

What is the therapeutic use of Bromocriptine?

A

Bromocriptine is used in conjunction with Levodopa. It may allow reduction in the maintenance dosage of Levodopa and therefore reduce the occurrance if side effects associated with long-term Levodopa use.

22
Q

How is Bromocriptine when used alone?

A

Bromocriptine has very little effect on parkinsonian symptoms when used alone

  • however when used in conjunction with Levodopa, it helps relieve rigidity and tremor. It has minimal effects on bradykinesia.
23
Q

What is the adverse effects of Bromocriptine?

A
  • Hallucinations and delurium occure more often with Bromocriptine than with Levodopa
  • Nausea and vomiting
  • Cardiac arrythmia, postural hypotention
  • Erythromelagia; a condition characterized by red, painful, and swollen feet or hands
24
Q

What, other than Parkinson´s disease, is Bromocriptine used for?

A

hyperprolactinemia!

25
Q

How does Peroglide work?

A
  • Like Bromocriptine, it is an ergot derivative

- it is a dopamine agonist at both D1 and D2 receptors

26
Q

What role does Peroglide hav in the treatment of Parkinson´s disease?

A

It is usually used in combination with levodopa and anticholinergic drugs

27
Q

Peroglide AE:

A
  • Confusion
  • Hallucination
  • Orthostatic hypotension
  • UTIs
28
Q

How do the Pramipexole and Ropinirole work?

A
  • Pramipexole and Ropinirole are non-ergot agonists at dopamine (D2) receptors.
  • They can be used as first-line therapy or as an adjunct to levodopa treatment
29
Q

How do the Pramipexole and Ropinirole differ from Bromocriptine and Pergolide?

A
  • Unlike Bromocriptine and Pergolide, they can be initiated at therapeutic levels quickly rather than by a slowing increase,
  • Pramipexole and Ropinirole also cause fewer GI side effects
30
Q

What are the side effects that should be monitored when using Pramipexole and Ropinirole?

A
  • dyskinesia
  • insomnia or somnolence
  • dizziness
  • orthostatic hypotension
31
Q

How are the Pramipexole and Ropinirole eliminated?

A

Pramipexole and Ropinirole are excreted through the kidneys.

- Ropinirole is much more extensively metabolized than pramipexole

32
Q

What is the mechanism of action of Selegiline?

A

Selegiline selectively inhibits monoamine oxidase B (MAO-B), which metabolizes dopamine.

MAO-A, however, is not affected unless extremely high doses of Selegiline is given.

33
Q

What is the therapeutic use of Selegiline?

A

Because it decreses the metabolism of dopamine periphery, Selegiline, increases dopamine levels in the brain.

The effects of levodopa are enchanced when it is used in conjunction with Selegiline; however, there is a threat of hypertensive crisis when this drug is administered in high dosages.

34
Q

What is the classification of Amantadine?

A

Amantadine is an antiviral agent used to treat influenza

35
Q

What is the mechanism of action of Amantadine?

A

The exact mechanism of action is unknown.

Amantadine appear to either enhance the release of dopamine from surviving nigral neurons or inhibit the reuptake of dopamine at synapses.

36
Q

What is the therapeutic use of Amantadine?

A

Amantadine may improve bradykinesia, tremor, and rigidity when used along with Levodopa.
It is usually only effective for a few weeks but seems to be more effective with anticholinergic agents.

37
Q

What are the toxic effects of Amantadine?

A
  • Restlessness, agitation, confusion
  • Orthostatic hypotesion
  • Peripheral edema
  • Livedo reticularis (skin rash)
38
Q

Name three examples of Anticholinergic agents:

A
  • The three most commonly used anticholinergic drugs are:
    1. Benztropine
    2. Biperiden
    3. Trihexiphenidyl
39
Q

Why do people use anticholinergic agens?

A

These drugs help reduce the cholinergic output of the striatum.
Again, this is another method to restore balance between dopamine and acetylcholine with nigrostratal system.

40
Q

What is the therapeutic efficacy of anticholinergic agents?

A

These drugs are less efficacious than levodopa.

  • They are commonly used adjuvantly in parkinsonian therapy.
  • They primarily help reduce tremor, rigidity, and akinesia - Secondary symptoms like drooling are also reduced.
41
Q

What are the AE of anticholinergic agents:

A

The following are cause by decreased parasympathetic response:

  • sedation
  • urinary retention
  • dry mouth
  • constipation
  • mental confusion
42
Q

What is drug-induced parkinsonism?

A

Parkinsonian symptoms can be caused by potent antipsychotic agents such as haloperidol because they block dopamine receptors

43
Q

What is the treatment of drug-induced parkinsonism?

A
  • lower the drug levels
  • change the drug to a less potent one
  • use an anticholinergic agent
44
Q

Define Huntington´s disease:

A

A genetic disorder due to a single defect on chromosome 4

45
Q

What are the the symptoms of Huntington´s disease?

A

Individuals who have the disease display dementia and/or chorea

46
Q

What is the pathophysiology of Huntington´s disease?

A

This disease is thought to occur because of excessive dopaminergic activity and diminished γ-aminobutyric acid (GABA) functions in the basal ganglia (caudate and putamen)

47
Q

What is the treatment of Huntington´s disease?

A

Dopamine blockers such as haloperidol or tetrabenazine are used to treat Huntington´s disease

48
Q

What is Tourette´s syndrome?

A

A disease characterized by abnormal tics and facial movement

49
Q

What is the treatment of Tourette´s syndrome?

A
  • Clonidine

- Haloperidol has also been used

50
Q

Define Wilson´s disease:

A

Wilson´s disease is a genetic disorder of copper metabolism.

- Excess copper is deposited in the liver, brain, and other tissues.

51
Q

What is the treatment of Wilson´s disease?

A

A copper chelating agent known as Penicillamine

Pharma Recall - Pharmacology (14 decks)

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