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HLSC 220 Pharmacotherapeutics for Health Professionals 💊 > Drugs for Parkinson's Disease - Ch. 24 > Flashcards

Drugs for Parkinson's Disease - Ch. 24 Flashcards

1
Q

What is Parkinson’s Disease (PD)?

A

Chronic, progressive, degenerative neurological disorder
-affects control of body movements

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2
Q

What are the motor symptoms of Parkinson’s?

A

Bradykinesia
Rigidity
Rest tremor
Postural instability
Gait disturbances
Mask-like, expressionless face
Dystonias

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3
Q

What other symptoms are associated with Parkinson’s?

A

Sleep disturbances
Depression
Psychosis
Dementia
Loss of smell
Apathy
Antonomic dysfunction (orthostatic hypotension, urinary urgency, constipation)

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4
Q

What in the brain is affected by Parkinson’s disease?

A

Dopamine-producing neurons in the brain

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5
Q

What are Parkinson’s symptoms caused by?

A

Imbalance of neurotransmitters:
Dopamine (DA)
Acetylcholine (ACh)

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6
Q

When do Parkinson’s disease symptoms occur?

A

When there is a loss of ~70-80% of dopamine neurons in the substantial nigra of the basal ganglia

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7
Q

What are treatments/interventions for PD?

A

Drugs for movement abnormalities
deep brain stimulation (drug resistant PD)
exercise
socialization

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8
Q

What is most PD drug therapy focused on?

A

DA pathway

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9
Q

What are the groups of drugs affecting DA system?

A

Direct -DA receptor agonists
Indirect -precursor, MAOI

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10
Q

What is a precursor drug for PD?

A

Levodopa-carbidopa

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11
Q

What drugs prevent DA metabolism?

A

MAOIs

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12
Q

What anticholinergic agents are used for PD?

A

Benztropine
Diphenhydramine

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13
Q

What is levodopa?

A

Precursor of dopamine

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14
Q

How does Levodopa work?

A

The BBB does not allow exogenously supplied dopamine to enter but levodopa can so it is taken up by dopaminergic terminals, converted into dopamine then released

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15
Q

What does levodopa therapy do?

A

Increases dopamine release from surviving DA neurones
Balances effects of cholinergic pathways of muscle control
Maintains functional mobility for years

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16
Q

Where is Levodopa metabolised outside the CNS?

A

Liver
GI

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17
Q

What drugs are given in combination with Levodopa?

A

Carbidopa
-benserazide as alternative

COMT inhibitors

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18
Q

What does Carbidopa prevent?

A

Prevents levodopa breakdown in periphery

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19
Q

Can carbidopa cross the BBB?

A

No

20
Q

What else can metabolise Levodopa?

A

Enzyme COMT
-Use COMT inhibitors to prevent this

21
Q

Examples of COMT inhibitors?

A

Entacapone, opicapone

22
Q

What is the “wearing-off” effect associated with Levodopa?

A

Gradual loss
-subtherapeutic levels end of dosing interval

23
Q

What is the “on-off” phenomenon associated with Levodopa?

A

Abrupt loss of drug effect even at high drug levels
lasts minutes to hours
unknown reason

24
Q

What adverse effects are associated with Levodopa?

A

Nausea and vomiting (reduced by carbidopa)
Dyskinesia (involuntary muscle movements) LOLLL
Hypotension, dysrhythmias
Psychosis; hallucinations, paranoid ideation

25
Q

What drugs prevent DA metabolism?

A

MAO-B inhibitors (inhibits DA breakdown in neurons)

26
Q

Examples of MAO-B inhibitors? MAOIs

A

Selegiline, rasagiline

27
Q

What does Amantadine do?

A

Promotes DA release from storage sites at nerve endings
Blocks reuptake of dopamine into nerve endings
Does not stimulate dopamine receptors directly
May help with levodopa dyskinesias

28
Q

What is Selegiline?

A

Irreversible MAOI that selectively inhibits MAO-B
Increases dopaminergic stimulation levels in CNS
-No cheese effect

29
Q

Why does Selegiline have no effect on NE, 5-HT breakdown

A

NE, 5-HT breakdown is done by MAO-A
Selegiline is a MAO-B inhibitor

30
Q

When is Selegiline used?

A

Milder symptoms (early in PD)

31
Q

What verse effects are associated with Selegiline?

A

Usually mild AE:
nausea, abdominal pain, dry mouth
lightheadedness, dizziness, insomnia, confusions

doses higher than 10mg/day may cause more severe AE

32
Q

What is the 1st line treatment for PD in younger pt, mild symptoms of PD?

A

Direct acting- DA receptor agonists

33
Q

What can DA receptor agonists reduce?

A

Wearing off effect of levodopa

34
Q

What is an older DA receptor agonists?

A

Bromocriptine

35
Q

What are newer DA receptor agonists?

A

Pramipexole
Ropinirole
Rotigotine (transdermal patch)

36
Q

What DA receptor agonist is administered with a pen injection?

A

Apomorphine (not an opioid)

37
Q

What are the pros of DA receptor agonists?

A

No conversion required
No dietary protein restrictions
less dyskinesias

38
Q

What are the cons of DA receptor agonists?

A

Halluciantions, postural hypotension, drowsiness
Impulse control disorders; gambling, shopping, hypersexuality

39
Q

What should clients taking Levodopa avoid?

A

High protein diets
-amino acids reduce GI absorption and transport across BBB

40
Q

Taking levodopa with what can cause hypertensive crisis?

A

non-selective MAOIs

41
Q

Levodopa may activate what?

A

Malignant melanoma

42
Q

Levodopa can darken what?

A

Urine and sweat

43
Q

What does anticholinergic therapy have greater influence on?

A

Muscle control
-Muscle tremors
-Cogwheel rigidity
-Pin-rolling movement of fingers and head bobbing while at rest

44
Q

What do anticholinergics do?

A

Block the effects of ACh

45
Q

Examples of anticholinergics?

A

Benztropine (Cogentin)
trihexyphenidyl
ethopropazine
diphenhydramine

46
Q

What else are anticholinergics used to treat (muscle related)?

A

Drug-induced extrapyramidal symptoms (EPS)

47
Q

Adverse effects associated with anticholinergics?

A

Drowsiness, confusion
Constipation, N&V
Urinary retention
Blurred vision, dilated pupils
Dry skin, fever
Dry mouth

HLSC 220 Pharmacotherapeutics for Health Professionals 💊 (31 decks)

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