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Flashcards in Pharm 5 Lecture Deck (79)
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1

What is the main sympathetic nervous system neurotransmitter?

Norepinephrine

2

What is released from the adrenal medulla (when stimulated by SNS) as a HORMONE?

Epinephrine

3

Catecholamines

hormones made by the adrenal glands, release when a person is under physical or emotional stress, high potency, quick duration, does not penetrate BBB, easily broken down, can't be taken orally

4

What are some examples of catecholamines?

Norepinephrine (Noradrenaline)
Epinephrine (adrenaline)
Dopamine
Dobutamine

5

What are the 6 steps of adrenergic neurotransmission?

1. Synthesis of norepi
2. uptake into storage vessicles
3. release of neurotransmitter
4. binding to receptor
5. removal of norepi
6. metabolism

6

What is the rate-limiting step of the synthesis of norepinephrine?

Hydroxylation of tyrosine into DOPA (dihyro-Phenoxyalanine)

7

What is the main precursor to epinephrine?

Dopamine

8

When is dopamine converted to norepinephrine?

Inside the vessicle; where it is protected from degradation

9

What inhibits transport of dopamine into the vessicle?

Reserpine

10

What causes fusion of the vesicle containing norepi with the cell membrane in a process known as exocytosis?

Influx of calcium causes the fusion

11

What blocks the release of the vesicle containing norepi?

Guanethidine and bretylium

12

What prevents reuptake of norepinephrine?

Cocaine and imipramine

13

What metabolizes norepineprhine?

Methylated by Catecol-O-methyl transferase (COMT)
Oxidized by Monoamine oxidase (MAO)

14

DOPA

dihydro-Phenoxyalanine

15

How does DOPA --> Dopamine?

Dopa is decarboxylated

16

Isoproteronol

A direct acting synthetic catecholamine

17

Alpha Adrenoceptors in order of affinity

Highest Affinity: Epinephrine
Norepinephrine
Lowest: Isoproterenol

18

Beta Adrenoceptors in order of affinity

Highest affinity: Isoproterenol
Epinephrine
Lowest: Norepinephrine

19

What are the names of the dopaminergic receptors?

D1, D2, D3, D4, D5

20

A1 receptors have a relatively high affinity for....

Norepinephrine

21

A2 receptors have a high affinity for....

Clonidine (Catapres), an antihypertensive drug

22

What does alpha 1 innervate?

Smooth muscle of most non-cardiac origin

23

What are the effects of stimulating alpha 1?

vasoconstriction; increased bp
mydriasis (dilation of pupils)
increased bladder tone
increased tension in prostate

24

What are the effects of stimulating alpha 2?

Creates negative feedback loops (prejunctional nerve terminals)
Some GI and digestive effects

25

Where are alpha 2 receptors located?

Prejunctional nerve terminals

26

Why would we stimulate alpha 2?

Increasingly used in human cardiovascular surgery as a sedative as part of multi-modal anesthesia

27

What are some advantages to stimulating alpha 2 during srugery?

Modulates DPB-induced inflammatory responses better than glucocorticoids (such as a cortisol)

Sympatholytic effects help ameliorate unwanted CV reflexes post-op

less respiratory depression postop than other options

28

What is the one alpha 2 drug used in humans?

Dexmedetomidine (precedex)

29

What has affinity for Beta 1 receptors?

Equal affinity for norepinephrine and epinephrine (both less than isoproterenol)

30

What has affinity for Beta 2 receptors?

More affinity for epinephrine than norepinephrine
Both again, have more affinity than isoproterenol