Pharm Parkinson Flashcards

1
Q

The effect of MPP on substantial nigra and Dopamine cells?

A

destroys them and causes parkinsonian like syndrome

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2
Q

Does dopamine cross the BBB? Levadopa?

A

No and yes

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3
Q

How is L-Dopa converted to dopamine?

A

decarboxylation

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4
Q

L-Dopa Adverse Effects

A

dyskinesia in 80% of patients choreoathetosis: in distal limbs and face

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5
Q

Role of Carbidopa?

A

prevents the metabolism of Levadopa outside of the CNS

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6
Q

Akinesia

A

the wearing off of the L-dopa

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7
Q

Unrelated to the Time of Dose

A

On/Off Phenomena Off: akinesa On: increased mobility but it is dyskinesia

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8
Q

How can off periods be treated? MOA? What is given with it?

A

Apomorphine, antiemetics(trimethobenzamide) with a side effect is nausea and vomiting

MOA: dopamine agonist

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9
Q

Dopamine Pathways

A
  • nigrastriatal
  • mesolimbic
  • tuberoinfundibular
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10
Q

Tuberoinfundibular

A
  • median eminense
  • neurohypophyses
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11
Q

Nigrostriatal System

A

SN to Caudate/Putamen

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12
Q

Mesolimbic Pathway

A

Ventral Tegmental Area/Substantia Nigra to Nucleus Accumbens

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13
Q

Selegiline

A

irreversible MAO-B inhibitor

can cause stimulatory effect (shoudl be given in morning or lunch)

can be used in early symptoms however, used as adjunctive treatment in later stages

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14
Q

COMT Metabolism

A

Breaks L-Dopa into 3-O-Methyldopa

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15
Q

What receptor do 3-O-Methyldopa and L-Dopa compete for?

A

Large Amino Acid Transporter

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16
Q

How is L-Dopa reuptake affected by increased levels of 3OMD?

A

decreases, because the 3OMD and the L-Dopa are competing for the large amino acid transporter

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17
Q

Why are COMT and MAO-B inhibitors needed?

A

to reduce the amount of L-Dopa that is metabolized and therefore lower doses can be used

18
Q

Rasagiline Purpose? Contraindications?

A

more potent MAO-B inhibtor

can be a neuroprotectant in animal studies

can be in monotherapy or adjunctive therapy(i.e. seligiline)

contraidicated: Meperidine + SSRI (serotonin syndrome)

19
Q

Entacapone Purpose? Adverse Effect?

A

COMT inhibitor, orange urine

20
Q

Tolcapone Purpose? Adverse Effects?

A

COMT inhibitor, liver hepatotoxicity

21
Q

Stalevo

A

combination of entacapone + carbidopa + L-Dopa

22
Q

Neurotransmitters for muscuranic receptors?

A

acetyl choline

23
Q

Effect of Anti-muscuranic drugs on Parkinsonian Symptoms

A

Decreases the tremors/rigidity NOT the bradykinesia

24
Q

How do dopamine and acetylcholine interact with each other?

A

Acetylcholine is intiating movement and the dopamine is inhibiting it

25
Q

5 Types of AcetylCholine Blockers

A

Benztropine (Cogentin)

Diperidan (Akineton)

Diphenhydramine (Benadryl)

Procyclidine (Kemadrin)

Trihexyphenidyl (Artane)

26
Q

Dosing for Anti-cholinergics

A

low dose and build up steady

27
Q

Adverse Side Effects of Anti-Cholinergics

A

drowsiness, mental slowness, hallucinations, arrhythmias, palpations

28
Q

Amantidine Effects? Limitations?

A

decreases bradykinesia, tremor, rigidity

MOA in unknown

Limitations

  • less effective than L-Dopa
  • treatment only lasts a few weeks
29
Q

4 Advantages of Dopamine Agonists

A
  • no competition to cross BBB
  • fewer adverse side effects
  • do not require metabolism (enzymatic)
  • no toxic metabolites
30
Q

Beta-Blocker that can be used for Tremor? What population is at risk with use?

A

Propranolol, acts on B1 and B2 receptors, be cautious when giving to heart and asthma patients

31
Q

Beta-Blockers that can’t be used for tremors

A
  • Metoprolol, because it is B1 selective
  • Betaxolol also B1 selective
32
Q

Which Beta receptor mediates tremors

A

B2, that’s why the B1 receptor blockers are ineffective

33
Q

Surgical Option for Treatment Long Term tremors

A

deep thalamic stimulation implants

34
Q

Differentiate when PD and Huntington Disease Neuron Damage

A

PD dopaminergic cells in SN, Huntington’s: possible glutamate toxicity, cortical volume loss (caudate nucleus), medium sized GABA neurons in Basal Ganglia

35
Q

Tetrabenazine Action

A

treats Huntington’s Disease

inhibits vesicular monoamine transporter 2

depletes central monoamine

Adverse Effects: fewer reserpine

36
Q

Tetrabenazine Action

A

treats Huntington’s disease

inhibits vesicular monoamine transporter 2

depletes central monoamines

37
Q

Effect of Dopamine on Huntington’s Disease

A

dopamine levels cause choreoform movement, therefore decreases dopamine levels is beneficial to the patient

38
Q

ALS Symptoms? Prognosis? Cause?

A

muscle wasting, respiratory failure in later stages

2-5 years

possible disfunction in superoxidase dismutase, increased amount of free radicals in the body

39
Q

Only Drug Approved for ALS

A

Riluzole: protects neurons from damage from the toxic effects of glutamate by inhibiting glutamate signaling

40
Q

Dosing Regimen for Sinemet? Dose? TImes a day? Adjusting?

A

L-Dopa (100mg) + Carbidopa (25 mg)

Increasing the dosage increases the side effects, if a greater therapeutic effect is needed supplement the meds with dopamine agonists and COMT/MAO Inhibitors

3 times a day

41
Q

Drugs Contraindicated for L-Dopa

A

Anti-psychotics that interact with DA2 receptor, therefore they work against each other

Haloperidol/fluphenazine

42
Q

Populations that are contraindicated for L-Dopa

A

Patients with ahx of melanoma/undiagnosed skin lesions

Psychotic Patients bc drugs interact with DA2 receptors

angle closure glaucoma patients (increased ICP)