Pharm Parkinson

Question 1

The effect of MPP on substantial nigra and Dopamine cells?

Answer 1

destroys them and causes parkinsonian like syndrome

Question 2

Does dopamine cross the BBB? Levadopa?

Answer 2

No and yes

Question 3

How is L-Dopa converted to dopamine?

Answer 3

decarboxylation

Question 4

L-Dopa Adverse Effects

Answer 4

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

Question 5

Role of Carbidopa?

Answer 5

prevents the metabolism of Levadopa outside of the CNS

Question 6

Akinesia

Answer 6

the wearing off of the L-dopa

Question 7

Unrelated to the Time of Dose

Answer 7

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

Question 8

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

Answer 8

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

MOA: dopamine agonist

Question 9

Dopamine Pathways

Answer 9

• nigrastriatal
• mesolimbic
• tuberoinfundibular

Question 10

Tuberoinfundibular

Answer 10

• median eminense
• neurohypophyses

Question 11

Nigrostriatal System

Answer 11

SN to Caudate/Putamen

Question 12

Mesolimbic Pathway

Answer 12

Ventral Tegmental Area/Substantia Nigra to Nucleus Accumbens

Question 13

Selegiline

Answer 13

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

Question 14

COMT Metabolism

Answer 14

Breaks L-Dopa into 3-O-Methyldopa

Question 15

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

Answer 15

Large Amino Acid Transporter

Question 16

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

Answer 16

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

Question 17

Why are COMT and MAO-B inhibitors needed?

Answer 17

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

Question 18

Rasagiline Purpose? Contraindications?

Answer 18

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)

Question 19

Entacapone Purpose? Adverse Effect?

Answer 19

COMT inhibitor, orange urine

Question 20

Tolcapone Purpose? Adverse Effects?

Answer 20

COMT inhibitor, liver hepatotoxicity

Question 21

Stalevo

Answer 21

combination of entacapone + carbidopa + L-Dopa

Question 22

Neurotransmitters for muscuranic receptors?

Answer 22

acetyl choline

Question 23

Effect of Anti-muscuranic drugs on Parkinsonian Symptoms

Answer 23

Decreases the tremors/rigidity NOT the bradykinesia

Question 24

How do dopamine and acetylcholine interact with each other?

Answer 24

Acetylcholine is intiating movement and the dopamine is inhibiting it

Question 25

5 Types of AcetylCholine Blockers

Answer 25

Benztropine (Cogentin) Diperidan (Akineton) Diphenhydramine (Benadryl) Procyclidine (Kemadrin) Trihexyphenidyl (Artane)

Question 26

Dosing for Anti-cholinergics

Answer 26

low dose and build up steady

Question 27

Adverse Side Effects of Anti-Cholinergics

Answer 27

drowsiness, mental slowness, hallucinations, arrhythmias, palpations

Question 28

Amantidine Effects? Limitations?

Answer 28

decreases **bradykinesia**, tremor, rigidity MOA in unknown Limitations - less effective than L-Dopa - treatment only lasts a few weeks

Question 29

4 Advantages of Dopamine Agonists

Answer 29

- no competition to cross BBB - fewer adverse side effects - do not require metabolism (enzymatic) - no toxic metabolites

Question 30

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

Answer 30

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

Question 31

Beta-Blockers that can't be used for tremors

Answer 31

- Metoprolol, because it is B1 selective - Betaxolol also B1 selective

Question 32

Which Beta receptor mediates tremors

Answer 32

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

Question 33

Surgical Option for Treatment Long Term tremors

Answer 33

deep thalamic stimulation implants

Question 34

Differentiate when PD and Huntington Disease Neuron Damage

Answer 34

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

Question 35

Tetrabenazine Action

Answer 35

treats Huntington's Disease inhibits vesicular monoamine transporter 2 depletes central monoamine Adverse Effects: fewer reserpine

Question 36

Tetrabenazine Action

Answer 36

treats Huntington's disease inhibits vesicular monoamine transporter 2 depletes central monoamines

Question 37

Effect of Dopamine on Huntington's Disease

Answer 37

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

Question 38

ALS Symptoms? Prognosis? Cause?

Answer 38

muscle wasting, respiratory failure in later stages 2-5 years possible disfunction in superoxidase dismutase, increased amount of free radicals in the body

Question 39

Only Drug Approved for ALS

Answer 39

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

Question 40

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

Answer 40

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

Question 41

Drugs Contraindicated for L-Dopa

Answer 41

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

Question 42

Populations that are contraindicated for L-Dopa

Answer 42

Patients with ahx of melanoma/undiagnosed skin lesions Psychotic Patients bc drugs interact with DA2 receptors angle closure glaucoma patients (increased ICP)