Applied neuropharmacology

Question 1

Which neurotransmitter is unusually inactivated by extracellular breakdown? What is the other usual method to inactivate neurotransmitters?

Answer 1

acetylcholine

inactivated by uptake into glial neurons

Question 2

3 places of anatomical distribution of dopamine in the brain

Answer 2

brainstem
basal ganglia
limbic system and frontal cortex

Question 3

3 physiological functions affected by dopamine

Answer 3

reward system
vomiting
voluntary movements

Question 4

What causes Parkinson’s?

Answer 4

degeneration of DA cells in substantia nigra and DA deficiency in basal ganglia

Question 5

symptoms of parkinson’s

Answer 5

stiffness, slow, movements, tremor, change in posture

Question 6

Precursor of dopamine

Answer 6

L-Dopa, tyrosine

Question 7

Can dopamine cross the blood brain barrier?

Answer 7

No

Question 8

What type of receptors are dopaminergic and how many are there?

Answer 8

metabotropic

D1-5

Question 9

Consequence of no ionotropic dopamine receptors

Answer 9

cannot evoke fast IPSP/EPSP

Question 10

2 key enzymes in dopamine breakdown

Answer 10

MOA-B

COMT

Question 11

Examples of dopaminergic drugs

Answer 11

precursor eg levodopa

DA agonist eg ergots, non-ergots, apomorphine

Question 12

What do dopaminergic drugs do to PD symptoms?

Answer 12

improve them

Question 13

3 types of enzyme inhibitors used in PD

Answer 13

peripheral AAD inhibitor
COMT inhibitor
MOA-B inhibitor

Question 14

Peripheral AAD inhibitors effect on levodopa

Answer 14

reduce peripheral side effects

increase oral does reaching CNS

Question 15

COMT inhibitors effect on levodopa

Answer 15

decrease DA metabolism and so increase levodopa effectiveness

Question 16

Do enzyme inhibitors have an effect on synthetic dopaminergic agonists?

Answer 16

no

Question 17

3 motor features of PD dopaminergic drugs improve

Answer 17

tremor
limb rigidity
bradykinesia

Question 18

What can dopaminergic drugs worsen or cause?

Answer 18

nausea, vomiting, psychosis, impulsiveness

Question 19

What do dopaminergic drugs fail to help?

Answer 19

midline features eg balance, cognition, dysarthria

Question 20

What do dopamine antagonists improve and worsen?

Answer 20

improve - vomiting, nausea, psychosis

cause - PD

Question 21

What anti-emetics should not be used in people with PD?

Answer 21

DA antagonist

Question 22

Is the vomiting centre in medulla functionally inside or outside the blood brain barrier?

Answer 22

outside

Question 23

What DA antagonist does not cross blood brain barrier?

Answer 23

Domperidone

Question 24

What Is domperidone?

Answer 24

DA antagonist, does not cross BBB, anti-emetic, safe in PD, no antipsychotic properties, has permitted therapeutic use of apomorphine

Question 25

What drug has domperidone allowed use of? what class of drug is this?

Answer 25

apomorphine

dopaminergic agonist - strong emetic

Question 26

What may dopaminergic drugs cause? dyskinesia or parkinsonism?

Answer 26

dyskinesia

Question 27

What may DA antagonist cause? parkinsonism or dyskinesia?

Answer 27

Parkinsonism

Question 28

Long term DA antagonists used for? what do they cause and why?

Answer 28

anti-psychotics, anti dizziness

Parkinsonism - block receptor in basal ganglia