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Flashcards in Pharm- 13 Deck (50):
0

Which AA makes dopamine?

Tyr

1

Which enzyme converts Tyr --> L-DOPA?

Tyrosine hydroxylase

2

What is special about tyosine hydroxylase as far as the synthesis steps?

Its the rate-limiting step

3

What 2 substrates does tyrosine hydroxylase use to make L-DOPA from Tyr?

BH4 and O2

4

What enzyme converts L-DOPA --> Dopamine?

dopamine decarboxylase

5

What cofactor does dopa decarboxylase need?

PLP

6

Define: used to move a majority of DA back into the presynaptic cell; it’s a 12 transmembrane domain protein belongs to a family of catecholamine reuptake pumps

Dopamine Transporter (DAT)

7

True or false: Dopamine uses secondary active transport to get into the presynaptic cell.

True

8

What molecules does DA enter with into the cell throguh DAT?

Na+ and Cl-. (Na is the 1 that is made from the secondary active transport usign the Na/K ATPAase)

9

What transporter puts DA back into the synaptic vesicle?

VMAT

10

What 2 enzymes break down DA in the persynaptic terminal cytosol?

MAO and COMT

11

Which form of MAO (MAO-A or MAO-B) can degrade DA?

TRICK QUESTION LOL. Both can degrade DA.

12

Where is MAO-A expressed, brain or periphery?

GOT U AGAIN. ITS BOTH AHAHAHAHA

13

Where is MAO-B expressed, brain or periphery?

Just the brain.

14

So MAO-B inhibitors inhibit the breakdown of dopamine where?

CNS

15

What weird molecule in wine and cheese increases if you're taking an MAOi?

Tyramine

16

Where is COMT expressed?

Brain, heart, liver and kidneys

17

The breakdown of DA from COMT and MAO's break it down into which molecule?

HVA

18

Where can you test HVA to see the rate of DA breakdown?

Pee pee

19

D1- metabotropic or ionotropic

metabotropic

20

D1- Gs, Gq, or Gi?

Gs

21

D2- metabotropic or ionotropic?

metabotropic

22

D2- Gs, Gq, or Gi?

Gi

23

Which dopamine receptors are in the striatum (caudate and putamen)?

D1 and D2 (remember parkinsons???)

24

Which dopamine receptors are in the basal ganglia?

D1 and D2

25

Which dopamine receptors are in the substantia nigra?

D2 and D4

26

Which dopamine receptors are in the nucleus accumbens?

D1, D2, D3 (help with movement)

27

Which dopamine receptors are in the olfactory tubercle?

D1, D2, D3, D5

28

Which dopamine receptors are in the lactotrophs?

D2 (regulate prolactin secretion)

29

Where is the area postrema?

located in the floor of the fourth ventricle is also a target of dopamine therapies

30

What happens if you stimualte the area postrema?

VOMITING. It's a circumventricular organ.

31

Which R's can you block in the area postrema to stop nausea and vomiting?

D2

32

What area of the brain is lost in parkinsons?

Substantia nigra pars compacta

33

Approximately what % of neurons are lost in parkinsons before Sx appear?

70%

34

What % of neurons are lost in the SNpc at autopsy?

95%

35

What are the Sx to parkinsons?

Bradykinesia or slowness of movement
Rigidity and resistance to passive movement of the limbs
Impaired postural balance which predispose to falling
Characteristic tremor when limbs at rest pill rolling
Stone like facial expression and drooling

36

What drug(s) can you give to treat parkinsons?

A. Dopamine
B. Dopamine + Carbidopa
C. Poop
D. L-DOPA + Carbidopa
E. Ach + Carbidopa

D. L-DOPA + carbidopa

37

Why can't you use DA to treat parkinsons?

it doesnt cross the BBB

38

What is the fxn of carbidopa?

Doesnt allow the breakdown of L-DOPA in the periphery

39

Does carbidopa cross the BBB?

NO

40

What is levodopa used for?

Parkinsons

41

What are the adverse effects with levodopa?

skinesia, heart disease, orthostatic hypoTN, psychosis, loss of appetite, nausea, vomiting.

42

What must you give levodopa with?

Carbidopa

43

What class is levodopa for treating parkinsons?

dopamine precursor

44

What class is pramipexole and ropinerole?

Dopamine receptor agonists (D3 mainly)

45

What is pramipexole used for?

parkinsons

46

What is ropinerole used for?

Restless leg syndrome

47

What are the side effects to pramipexole and ropinirole?

dyskinesia, orthostatic hypoTN, weird CNS crap

48

What class of drugs is rasagiline or selegiline to treat parkinsons?

inhibit dopamine breakdown in the CNS (inhibit COMT or MAO)

49

What are the adverse effects to rasagiline or selegiline?

bundle branch block, GIII hemorrhage, dyskinesia, orthostatic hypoTN