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Pharmacology > HNNS L54 - Drugs for Neurodegenerative Diseases > Flashcards

HNNS L54 - Drugs for Neurodegenerative Diseases Flashcards

1
Q

Drugs for Parkinson’s disease

A

Increasing dopamine activity in the nigrostriatal system

  • Dopamine precursors: levodopa (L-dopa) Dopamine cannot cross BBB
  • Peripheral DOPA decarboxylase inhibitors: carbidopa, benserazide
  • Dopaminergic agonists
    1. Ergot derivatives: bromocriptine, pergolide
    2. Non-ergot derivatives: ropinirole, pramipexole, rotigotine
  • MAO-B inhibitors, e.g. selegiline, rasagiline
  • COMT inhibitors, e.g. entacapone, tolcapone
  • Dopamine facilitator: amantadine

Reducing muscarinic cholinergic activity in the striatum
- Central anticholinergics, e.g. benztropine, benzhexol

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2
Q

Dopamine precursor for Parkinson’s Disease

A

Levodopa (L-dopa)
- Readily transported into CNS, converted to dopamine in brain by DOPA decarboxylase
High therapeutic index: drug of choice for symptom control esp in elderly

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3
Q

Side effects of L-dopa

A

Due to conversion of L-dopa to dopamine in the periphery

  • Nausea, vomiting
  • Arrhythmia
  • Postural (orthostatic) hypotension

Due to overstimulation of central dopamine receptors

  • Dyskinesia
  • Hallucinations
  • Restlessness
  • Confusion
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4
Q

Do not use levodopa with…

A 
-	Nonselective MAO inhibitor, e.g. phenelzine 
	Excess dopamine in periphery
	Converted into adrenaline, NA
	Life-threatening hypertensive crisis
-	Pyridoxine (Vitamin B6)
	Co-factor for the enzyme
	↑peripheral breakdown of L-dopa
-	Anti-psychotics
	Block dopamine receptors
	Cause Parkinsonian-like symptoms
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5
Q

Peripheral DOPA decarboxylase inhibitor

A

Carbidopa
Benserazide

Does NOT cross BBB

  1. Reduce metabolism of dopamine in periphery
  2. Increase availability of dopamine to CNS
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6
Q

Dopamine receptor agonists for Parkinson’s

A

Bromocriptine (Ergot, D2 agonist)

Pergolide (Ergot, D1 and D2 agonist)

Pramipexole
Ropinirole
(non-ergot, D2 agonist, 1st line for younger patients)

Rotigotine (Non-ergot, D2 agonist, transdermal patches)

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7
Q

Bromocriptine

A

Ergot dopamine D2 agoinist

Useful to delay use of L-dopa in younger patients
In conjunction with L-dopa / carbidopa
- Relieve rigidity and tremor
Minimal effects on bradykinesia

Side effects:

  • Hallucination, delirium
  • Nausea, vomiting
  • Cardiac arrhythmia, postural hypotension
  • Erythromelalgia: red, painful and swollen feet or hands
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8
Q

Pergolide

A

Ergot derivative
Dopamine agonist at D1 and D2 receptors
In combination with L-dopa / carbidopa and anticholinergics

  • Confusion
  • Hallucinations
  • Postural hypotension
  • Urinary tract infections
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9
Q

Pramipexole

A

Non-ergot dopamine agonists at D2 receptors
First line therapy in younger patients
An adjunct to L-dopa / carbidopa treatment in patients with advanced Parkinson’s disease

  • Dyskinesia
  • Insomnia / somnolence (drowsiness)
  • Dizziness
  • Postural hypotension
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10
Q

Ropinirole

A

Non-ergot dopamine agonists at D2 receptors
First line therapy in younger patients
An adjunct to L-dopa / carbidopa treatment in patients with advanced Parkinson’s disease

  • Dyskinesia
  • Insomnia / somnolence (drowsiness)
  • Dizziness
  • Postural hypotension
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11
Q

Rotigotine

A

Non-ergot dopamine D2-like receptor agonist at clinical doses
Transdermal patches when used in the treatment of Parkinson’s disease *elderly

  • Application site: hypersensitivity, skin problems e.g. redness, rashes, itching, irritation, burning sensation, etc
  • Dizzy, Headache, Nausea
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12
Q

Selegiline

A

Selective monoamine oxidase B inhibitor
Decrease metabolism of dopamine in periphery and brain
Increase dopamine levels in brain (for patients with mild parkinsonism)
Enhance effects of L-dopa / carbidopa (as an adjuvant)

High dose: hypertensive crisis
- High level of dopamine in periphery

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13
Q

Rasagiline

A

Selective monoamine oxidase B inhibitor
Decrease metabolism of dopamine in periphery and brain
Increase dopamine levels in brain (for patients with mild parkinsonism)
Enhance effects of L-dopa / carbidopa (as an adjuvant)

High dose: hypertensive crisis
- High level of dopamine in periphery

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14
Q

Entacapone

A

Catechol-O-methyl transferase (COMT) inhibitors
Block peripheral conversion of levodopa to 3-O-methyldopa
(use the same active carrier as dopamine to cross BBB)
Used only as adjuncts to L-dopa / carbidopa therapy

  • Diarrhoea
  • Postural hypotension
  • Dyskinesia
  • Sleep disorders
  • Hallucinations
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15
Q

Tolcapone

A

Catechol-O-methyl transferase (COMT) inhibitors
Block peripheral conversion of levodopa to 3-O-methyldopa
(use the same active carrier as dopamine to cross BBB)
Used only as adjuncts to L-dopa / carbidopa therapy

  • Diarrhoea
  • Postural hypotension
  • Dyskinesia
  • Sleep disorders
  • Hallucinations
  • Hepatic necrosis (for tolcapone only)
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16
Q

COMT inhibitors

A

Entacapone

Tolcapone

17
Q

Selective MAO-B inhibitor

A

Selegiline

Rasagiline

18
Q

Amantadine

A

Antiviral agent for influenza
Unknown mechanism
- Enhance release of dopamine from surviving nigral neurons
- Inhibit reuptake of dopamine at synapses
More effective than anticholinergic agents in improving bradykinesia and rigidity when used along with L-dopa / carbidopa

  • Restlessness, agitation, confusion
  • Postural hypotension
  • Peripheral edema
  • Skin rash
19
Q

Anticholinergics for Parkinson’s

A

Benztropine
Benhexol
Biperidine

Reduce cholinergic output of the striatum (inhibition to basal ganglia)
Much less efficacious than levodopa / carbidopa
As adjuvant only:
- Reduce primary symptoms e.g. tremor, rigidity and akinesia (NOT bradykinesia)
- Reduce secondary symptom e.g. drooling

(Add to L-dopa and carbidopa for control of tremor)

20
Q

Current best treatment for Parkinson’s

A

L-dopa + carbidopa / benserazide)

21
Q

To control motor fluctuations in Parkinson’s

A

COMT inhibitor / MAO-B inhibitor
+
L-dopa/carbidopa

22
Q

Huntington’s

A
  • Medications for movement disorder:
     Tetrabenazine: ‘dopamine-depleting’ to suppress chorea (involuntary jerking and writhing movement)
     Anti-psychotic drugs: haloperidol, risperidone (newer)
  • Side effect of suppressing movement
  • Medications for psychiatric disorders:
     Anti-depressants: fluoxetine (SSRI)
     Mood-stabilizing drugs: carbamazepine (treat irritability)
23
Q

Movement disorder in Hungtinton’s

A

 Tetrabenazine: ‘dopamine-depleting’ to suppress chorea (involuntary jerking and writhing movement)
 Anti-psychotic drugs: haloperidol, risperidone (newer)
- Side effect of suppressing movement

24
Q

Medications for psychiatric disorders in Huntington’s

A

 Anti-depressants: fluoxetine (SSRI)

 Mood-stabilizing drugs: carbamazepine (treat irritability)

25
Q

Tetrabenazine

A

‘dopamine-depleting’ to suppress chorea in Huntington’s(involuntary jerking and writhing movement)

26
Q

Haloperidol

A

Anti-psychotics

For movement disorders in Huntington’s

27
Q

Risperidone

A

Anti-psychotics

For movement disorders in Huntington’s

28
Q

Fluoxetine

A

SSRI

Also for psychiatric disorder in Huntington’s

29
Q

Carbamazepine

A

Mood-stabilizing for Huntington’s

30
Q

Drugs for Alzheimer’s

A

AChEI:

  • Donepezil
  • Rivastigmine (transdermal patch)
  • Galantamine

Uncompetitive NMDA receptor antagonist
- Memantine

31
Q

AChEI for Alzheimer’s

A
  • Donepezil
  • Rivastigmine (transdermal patch)
  • Galantamine

Increase the amount of ACh available by preventing its breakdown within the synaptic cleft
 improve cholinergic transmission within CNS

  • Nausea, vomiting
  • Diarrhoea, abdominal cramps
  • Anorexia (appetite and weight loss)
  • Agitation
  • Dizziness
  • Urine incontinence
32
Q

Uncompetitive NMDA receptor antagonist for Alzheimer’s

A

Memantine
Protect CNS neurons from excitotoxic effects of glutamate
(excess Mg removal  excess Ca influx  kill neurons)
Improve cognitive ability

  • Headache
  • Dizziness
  • Confusion
  • Constipation
  • Diarrhoea
33
Q

Donepezil

A

AChEI
For Alzheimer’s (All stages)

Increase the amount of ACh available by preventing its breakdown within the synaptic cleft
 improve cholinergic transmission within CNS

  • Nausea, vomiting
  • Diarrhoea, abdominal cramps
  • Anorexia (appetite and weight loss)
  • Agitation
  • Dizziness
  • Urine incontinence
34
Q

Rivastigmine

A

AChEI
For Alzheimer’s (Transdermal)

Increase the amount of ACh available by preventing its breakdown within the synaptic cleft
 improve cholinergic transmission within CNS

  • Nausea, vomiting
  • Diarrhoea, abdominal cramps
  • Anorexia (appetite and weight loss)
  • Agitation
  • Dizziness
  • Urine incontinence
35
Q

Memantine

A

For Alzheimer’s (uncompetitive NMDA receptor antagonist)

Protect CNS neurons from excitotoxic effects of glutamate
(excess Mg removal  excess Ca influx  kill neurons)
Improve cognitive ability

  • Headache
  • Dizziness
  • Confusion
  • Constipation
  • Diarrhoea

Pharmacology (10 decks)

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