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Pharm 3 > E1: Parkinsons > Flashcards

E1: Parkinsons Flashcards

1
Q

What are the 4 major features of Parkinson’s disease?

A
  • Bradykinesia
  • Muscular rigidity
  • resting tremor
  • Impairment of postural balance and gait
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2
Q

What is the pathophysiology behind Parkinson’s disease?

A
  • Loss of dopamine neurons in the Substantia Nigra pars compacta
  • Symptoms develop when 70-80% loss of the DA neurons
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3
Q

How does L-Dopa treat Parkinson’s?

A
  • “replacement”therapy

- Increases DA levels, dopamine does not cross the BBB, but L-Dopa does and si then converted to DA in the neuron

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4
Q

How long can L-Dopa treat the symptoms of Parkinsons?

A
  • Improvement of PD symptoms for 3-4 years, and then the effectiveness will decrease
  • Does not affect progression of disease and not effective in drug-induced Parkinsonism
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5
Q

Why Is Carbidopa often given with L-Dopa?

A

L-Dopa can be converted to DA in the periphery and Carbidopa inhibits Dopa-decarboxylase but doesn’t cross the BBB. Therefore conversion of L-Dopa to DA is inhibited in periphery but not in the brain

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6
Q

What are the side effects of L-Dopa/Carbidopa?

A
  • N/V
  • Postural hypotension, Arrhythmias, HTN
  • dyskinesias
  • Depression, anxiety, agitation (treat with atypical antipsychotics)
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7
Q

What is the “On-Off Phenomenon?”

A
  • Fluctuations in the clinical response in patients on successful L-Dopa therapy
  • “On” is improved mobility
  • “Off” is Akinesia due to falling drug levels
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8
Q

What drug can be used as a rescue during an Off phase on L-Dopa therapy?

A

Apomorphine

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9
Q

What drugs cannot be given with L-Dopa and why?

A
  • MAOI: may cause hypertensive crisis

- Pyridoxine: increases peripheral metabolism of L-Dopa thus decreases effectiveness

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10
Q

What are the contraindications of L-Dopa?

A
  • Psychosis
  • closed angle glaucoma
  • Cardiac disease
  • active peptic ulcer disease
  • malignant melanoma
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11
Q

What kind of drugs are Selegiline, Rasagiline, and Safinaminde?

A

MAOIs

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12
Q

What is the MOA of MAOIs?

A
  • Inhibits DA metabolism
  • Inhibits MAO-B in the CNA and reduces striata metabolism of DA, does not affect peripheral metabolism of DA by MAO-B

** may inhibit progression of PD by decreasing free radicals produced during DA metabolism

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13
Q

What are the Adverse effects of MAO-BIs?

A
  • Insomnia
  • Severe HTN if combined with other MAOIs
  • increase side effects of L-DOPA
  • Do NOT combined with Meperidine: can lead to stupor, rigidity, agitation, serotonin syndrome
  • Serotonin syndrome if combined with TCAs or SSRIs
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14
Q

What kind of drugs are Tolcapone and Entacapone?

A

COMT inhibitors: inhibits DA and L-Dopa metabolism

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15
Q

What is the MOA of tolcapone?

A

-Inhibits COMT in CNS and periphery, prolongs action of DA in the CNA, increases pool of L-Dopa for transport into the brain

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16
Q

What is the MOA of Entacapone?

A

-Inhibits COMT in periphery only, increases pool of L-Dopa for transport in the brain

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17
Q

What are the side effects of COMT inhibitors?

A

-Dyskinesia, confusion, nausea, hypotension, abdominal pain, sleep disturbance, and orange color to urine

18
Q

What kind of drug is Stalevo?

A

A combination of L-Dopa, Carbidopa, and Entacapone

19
Q

What is the MOA of DA receptor agonists?

A
  • Stimulates DA receptors
  • acts directly on receptors, Primarily DA D2
  • because thy act directly on receptors, they continue to be effective as the disease progresses
20
Q

What kind of drug is Bromocriptine, Ropinirole, Pramipexole, and apomorphine

A

-DA receptor agonist

21
Q

What are the side effects of Bromocriptine?

A

Vasospasm, erythromelagia

22
Q

Which drugs can be used as Monotherapy in mild PD and has a soothing response to L-Dopa in late PD?

A

Ropinirole and Pramipexole

23
Q

What is the DOC of restless leg?

A

Ropinirole, a relatively pure DA D2 agonist

24
Q

Since Apomorphine causes nausea, you should pretreat with an antiemetic. Which one should you use, and which should you avoid?

A
  • Use trimethobenzamide
  • avoid antiemetic that target the serotonin system (ondansetron) because it can cause HTN and LOC
  • Avoid antiemetics that blocks DA D2 receptors (Prochlorperazine)
25
Q

What are the side effects of DA agonists?

A
  • Anorexia, N/V
  • postural HTN, cardiac arrhythmias
  • Dyskinesia
  • mental disturbance
  • increased prolactin
26
Q

What is the MOA of Amantadine?

A
  • Increase DA neurotransmission

- may increase release of DA and may inhibit DA reuptake

27
Q

What is the use of Amantadine?

A
  • antiviral use for influenza

- used to treat early or mild cases of PD

28
Q

What are the side effects of Amantadine?

A
  • livedo reticularis: reddish blue spotting of skin

- restlessness, depression, irritability, insomnia, hallucinations, peripheral edema

29
Q

What kind of drugs are Benzotropine and Trihexyphenidyl?

A

-Muscarinic receptor antagonists that restore DA/ACh balance in the striatum

30
Q

What is the use of Benztropine and trihexyphenidyl in PD?

A
  • modest anti PD action
  • improves rigidity, tremor, and has little effect on bradykinesia
  • used in early and late stages, adjunct to DA therapy
31
Q

What is Pimavanserin?

A

an atypical antipsychotic approved for the treatment of psychosis and delusions associated with PD

32
Q

What is the MOA of Pimavanserin?

A

-Inverse agonist/antagonist for serotonin receptors, but does not affect dopamineragic, adrenergic, cholinergic, or histamine receptors

33
Q

What are the non-pharmacologic treatments of PD?

A
  • Neuroprotection with antioxidants and anti-apoptotic agents
  • Pallidotomy
  • transplants of fetal neurons or patient-derived stem cells
  • Gene therapy
  • DBS
34
Q

What is the pathophysiology behind Alzheimer’s?

A

-degeneration of cholinergic neurons

35
Q

What kind of drugs are Donepezil, rivastigmine, and Galatamine?

A

Cholinesterase inhibitors, can treat Alzheimer’s

36
Q

What is the MOA of Cholinesterase inhibitors?

A

-Inhibit metabolism of ACh, increases the amount of ACh in the nerve terminal

37
Q

How are Cholinesterase inhibitors metabolized?

A

CYP450s

38
Q

What are the common side effects of Cholinesterase inhibitors?

A

-Peripheral cholinergic side effects such as nausea, vomiting, diarrhea, cramping

39
Q

What kind of drug is Memantine?

A

-NMDA receptor antagonist that blocks pathological activation of NMDA receptors

40
Q

What is the use of Memantine?

A

-reduces excitotoxic effect of glutamate and slows degeneration, used in late stages of Alzheimer’s in combination with AChE-Is

41
Q

What are the side effects of Memantine?

A

Agitation, insomnia, urinary incontinence, diarrhea

42
Q

What are the contraindications of Memantine?

A

-Use with meperidine and Dextromethorphan

Pharm 3 (20 decks)

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