Pharm2 - Vasopressors (Spring 2012)

Front 1

Catecholamines are synthesized from what amino acid?

Back 1

Tyrosine (or if going back further, phenalanine)

Front 2

What is the rate-limiting step of catecholamine synthesis?

Back 2

Tyrosine hydroxylase

Front 3

Drugs that block tyrosine hydroxylase are sympathomimetic or sympatholytic?

Back 3

Sympatholytic

Front 4

Dopamine is synthesized from Dopa via what enzyme?

Back 4

L-amino acid decarboxylase

Front 5

Why is NE stored is vesicles?

Back 5

To prevent NT degradation via MAO enzymes in the ganglion

Front 6

NE is synthesized to Epi via what enzyme?

Back 6

Phenylethanolamine methyltransferase

Front 7

Synthesis of NE & Epi occur in what two locations?

Back 7

Sympathetic nerve terminal & adrenal medulla

Front 8

What are the five catecholamines? Which three are naturally occuring?

Back 8

Epi*
Norepi*
Dopamine*

Isoproterenol
Dobutamine

Front 9

Is ephedrine a catecholamine?

Back 9

No, it's a synthetic noncatecholamine

Front 10

What are the two enzymes that break down NTs? Where are their areas of action?

Back 10

MAO --> neuron cytoplasm
COMT --> synaptic jxn

Front 11

FYI -->
The final metabolite of NE and Epi breakdown is 3-methoxy 4-hydroxyphenylglycol

Back 11

FYI -->
The final metabolite of NE and Epi breakdown is 3-methoxy 4-hydroxyphenylglycol

Front 12

What is the NT in the preganglionic ganglia? post-ganglionic ganglia?

Back 12

Pre --> ACh
Post --> SNS is NE, PNS is ACh

Front 13

What are the preganglionic receptors? postganglionic receptors?

Back 13

Pre --> Nicotinic
Post --> SNS is Adrenergic (A,B,D), PNS is Muscarinic

Front 14

The primary NT of the SNS is...?

Back 14

Norepi
85% synthesized

Front 15

What are pre-synaptic alpha-2 receptors? Examples of pre-synaptic alpha-2 agonists are...

Back 15

Autorecetpors attached to the postganglionic presynaptic neuron; sympatholytic action via negative feedback

Clonidine & Dexmedetomidine

Front 16

Define inotrope, chronotrope, dromotrope.

(yes, i still get these mixed up!)

Back 16

Inotrope --> contraction
Chronotrope --> Heart rate
Dromotrope --> conduction velocity

Front 17

Vasoconstriction in one part of the body is met with _______ in another part of the body.

Back 17

Vasodilation

Front 18

Where are B1 receptors located? B2?

Back 18

B1 --> Heart
B2 --> everywhere else, x fat cells & kidneys

Front 19

What effect does Neosynephrine have on HR? Why?

Back 19

Reflex bradycardia
Pure alpha agonist

Front 20

What effect does Dobutamine have on vasculature? Why?

Back 20

Vasodilation & decr SVR
Pure beta agonist

Front 21

Which vasopressor is a pure alpha?

Back 21

Neosynephrine

Front 22

Which vasopressor has alpha, and some beta effects?

Back 22

Norepinephrine

Front 23

What vasopressor has both alpha & beta effect, but mostly B>A?

Back 23

Epinephrine

Front 24

Because of the strict alpha effects of Neosynephrine, this has what effect on HR? BP? Why?

Back 24

HR --> reflex bradycardia
BP --> incr

Front 25

Dopamine's clinical effect is ________ dependent. It has what receptor effects?

Back 25

Dose-dependent.
A, B, Dopa

Front 26

These vasopressors are pure beta agonist?

Back 26

Isoproterenol & Dobutamine

Front 27

Norepinephrine will (incr/decr) HR? BP? Why?

Back 27

Increase HR (beta)
Incr BP (alpha)

has both alpha & beta effects, but primarily alpha

Front 28

With Epi, you will see an (incr/decr) in HR? BP? Why?

Back 28

HR --> Incr (beta)
BP --> Decr (alpha)

Epi has both alpha & beta effects, but the beta effects outweight the alpha effects; b>a

Front 29

Dobutamine will (incr/decr) HR? BP? Why?

Back 29

HR --> Incr (beta)
BP --> Decr (beta)

Pure beta effects

Front 30

At what dose would you expect to see the beta effects of Dopamine?

Back 30

5-10mcg/kg/min

Front 31

With low-dose Dopamine, what receptors will be stimulated? What effect will you see clinically as a result?

Back 31

<5mcg/kg/min

Dopmainergic effects --> vasodilation, incr RBF, incr GFR & incr u/o

Front 32

At what dose of Dopamine would you no lose the Dopaminergic or Beta benefits of the drug?

Back 32

>15mcg/kg/min

Front 33

In a patient who is hypotensive with tachycardia, which vasopressor would you choose to use and why?

Back 33

Neosynephrine, because pure alpha effects & causes reflex bradycardia

Front 34

In a patient who is hypotensive and bradycardic, which vasopressor would you choose to use and why?

Back 34

Ephedrine, because alpha & beta effects, so will cause reflex tachycardia

Front 35

What are the unique properties of Ephedrine?

Back 35

Alpha & Beta effects
Direct & Indirect acting
Peripherally & centrally acting

Front 36

Outside of the CNS, where else are Dopamine receptors located in the body?

Back 36

Renal artery and mesenteric vessels

Front 37

Why is it therapeutic to give Dobutamine & Dopamine together? What patient population would this benefit?

Back 37

Together they provide (+) inotrope, vasodilation and (-) chronotrope effects which is ideal for patients in states of shock or heart failure.

Front 38

Stimulation of the alpha-2 receptor causes what effect(s)?

Back 38

Decr SNS outflow 2* negative feedback
Decr NE release (sympatholytic) - presynaptic stimulation
Vasoconstriction - postsynaptic stimulation
Sedation - CNS stimulation

Front 39

Stimulation of _____ receptors causes vasodilation, smooth muscle relaxation and bronchial dilation?

Back 39

Beta-2 receptors

Front 40

Stimulation of _____ receptors provide (+) inotropic and chronotropic effects.

Back 40

Beta-1 receptors

Front 41

Tocolytic drugs prevent the onset of _______. They are ____ receptor drugs. How do they work?

Back 41

Contractions
B2 agonists.

Work via increasing intracellular cAMP --> decr intracellular Ca --> hyperpolarization --> smooth muscle relaxation

Front 42

ANS of the Iris:

SNS/receptor
PNS

Back 42

SNS - mydriasis (radial muscle) - Alpha 1
PNS - Miosis (sphincter mucle)

Front 43

ANS of the Ciliary muscle:

SNS/receptor
PNS

Back 43

SNS -relaxation for far vision accommodation,
B2

PNS - contraction for near vision accommodation

Front 44

ANS of the SA:

SNS/receptor
PNS

Back 44

SNS --> Incr HR, B1
PNS --> Decr HR

Front 45

ANS of the Heart:

SNS/receptor
PNS

Back 45

SNS --> Incr HR, automaticity, conduction, contractility; B1

PNS --> Decr in HR, conduction, contractility

Front 46

ANS of the Arteries:

SNS/receptor
PNS

Back 46

SNS --> Constriction, alpha; Dilation, Beta2

PNS --> NONE

Front 47

ANS of the Salivary glands:

SNS/receptor
PNS

Back 47

SNS --> constriction & decr secretions, alpha

PNS --> dilation & incr secretions

Front 48

ANS of the Renal arteries:

SNS/receptor
PNS

Back 48

SNS --> constriction, alpha; dilation, Beta 1&2

PNS --> NONE

Front 49

ANS of the Veins:

SNS/receptor
PNS

Back 49

SNS --> Constriction, alpha
dilation, beta

PNS --> NONE

Front 50

ANS of the Lungs:

SNS/receptor
PNS

Back 50

SNS --> relaxation, B2

PNS --> constriction, Muscarinic

Front 51

ANS of the GI:

SNS/receptor
PNS

Back 51

SNS --> slows down

PNS --> speeds up

Front 52

ANS of the Bladder detrusor:

SNS/receptor
PNS

Back 52

SNS --> relaxation, B2

PNS --> contraction

Front 53

ANS of the Bladder sphincter:

SNS/receptor
PNS

Back 53

SNS --> contraction, alpha

PNS --> relaxation

Front 54

ANS of the Uterus:

SNS/receptor
PNS

Back 54

SNS --> contraction (of pregnant), alpha;
relaxation (of pregnant and non-preg), Beta-2

Front 55

ANS of the Liver:

SNS/receptor
PNS

Back 55

SNS --> glycogenolysis, gluconeogensis via alpha & beta-2

Front 56

ANS of the Pancreas:

SNS/receptor
PNS

Back 56

SNS --> decr insulin sxn, alpha2; decr insulin sxn, Beta-2

Front 57

ANS of the Adipocytes:

SNS/receptor
PNS

Back 57

SNS --> lipolysis, ALL RECEPTORS

Front 58

Alpha agonist create what effects in the eye?

Back 58

Mydriasis

Front 59

Alpha antagonists create what effect on the eye?

Back 59

Miosis

Front 60

Beta blockers have what effect on the eye? What patient population would this be appropriate for?

Back 60

decr IOP
ideal for glaucoma patients

Front 61

Cholinergic drugs have what effects on the eyeballs?

Back 61

Miosis, decr IOP

Front 62

Anticholinergics will (incr/decr) IOP? What other eyeball effects will they produce?

Back 62

Incr IOP
Cycloplegia
Mydriasis

Front 63

There will be an (incr/decr) in HR with alpha-agonists?

Back 63

Reflex bradycardia

Front 64

There will be an (incr/decr) in HR w/ alpha antagonists?

Back 64

Reflex tachycardia

Front 65

Beta-agonists will produce an (incr/decr) in HR?

Back 65

Tachycardia

Front 66

Beta-blockers will produce an (incr/decr) in HR?

Back 66

Bradycardia

Front 67

Cholinergic drugs will produce an (incr/decr) in HR?

Back 67

Bradycardia

Front 68

Anticholinergic drugs will produce an (incr/decr) in HR?

Back 68

Tachycardia

Front 69

Beta-agonist will incr/decr contractility?

Back 69

Incr contractility

Front 70

Anticholinergics will incr/decr contractility?

Back 70

Incr

Front 71

What two classes of drugs will produce vasodilation?

Back 71

Beta-agonists and alpha-antagonists

Front 72

What two classes of drugs will produce bronchoconstriction?

Back 72

beta-blockers & cholinergics

Front 73

These classes of drugs stimulate GI motility?

Back 73

Beta agonists & cholinergics

Front 74

These classes of drugs promote hyperglycemia?

Back 74

Beta-agonists and alpha-agonists

Front 75

What patient population are B-blockers most contraindicated in?

Back 75

COPD, RAD, Asthmatics, diabetics, PVD and HTN

Front 76

FYI -->
NE is reused/recycled because it is more energy efficient for the cell to reuse it then to resynthesize new NT after each use.

Back 76

FYI -->
NE is reused/recycled because it is more energy efficient for the cell to reuse it then to resynthesize new NT after each use.

Front 77

What amino acid causes an increase in NE release in conjunction w/ MAOIs or TCA use?

Back 77

Tyramine

Front 78

Inhibition of tyrosine hydroxylase is an example of which mechanism?

Back 78

inhibition of NT synthesis

Sympatholytic

Front 79

Methyldopa is an example of which mechanism?

Back 79

"False" NT synthesis/effect

Sympatholytic

Front 80

Cocaine & TCAs are drug examples of this mechanism?

Back 80

Blocking NT reuptake

Sympathomimetic

Front 81

Reserpine is an example of this mechanism?

Back 81

inhibition of vesicle synthesis

sympatholytic

Front 82

Tyramine, ephedrine & amphetamines are examples of this mechanism?

Back 82

Indirect promotion of NT exocytosis

sympathomimetic

Front 83

Bretylium and clonidine are examples of this NT action?

Back 83

Inhibition of NT release

Sympatholytic

Front 84

Noradrenaline and phenylephrine are examples of this mechanism?

Back 84

Direct acting stimulation of NT release

Sympathomimetic

Front 85

The difference between indirect and direct action of drugs is...

Back 85

direct --> receptor stimulation
indirect --> catecholamine release

Front 86

Phentolamine, propranaolol and atropine are examples of this mechanism?

Back 86

Receptor blockade

Parasympatholytic for Atropine
Phentolamine & propranolol are sympatholytic

Front 87

Neostigmine, MAOIs and Tolcapone are examples of this mechanism?

Back 87

Enzyme inhibition

Sympathomimetic

Front 88

Choline & Acetyl Co-Enzyme A are synthesized to ACh via this enzyme?

Back 88

Choline acetyltransferase

Front 89

Phosphodiesterase inhibitors are examples of this mechanism?

Back 89

interference with 2nd messenger system within cells

sympathomimetic

Front 90

Why is the inhibition of phosphodiesterase significant in NT action?

Back 90

PDE breaks down cAMP

By inhibiting cAMP degradation, catecholamines can build-up and produce a catecholamine response

Front 91

cAMP is (SNS/PNS)? cGMP?

Back 91

cAMP is SNS
cGMP is PNS

Front 92

PDE 3, 4, 7 is selective for cAMP or cGMP?

Back 92

cAMP

Front 93

PDE 1,5,6 is selective for cAMP or cGMP?

Back 93

cGMP

Front 94

What does analeptic mean?

Back 94

CNS stimulation

Front 95

What effect do atropine & glycopyrolate have of LES tone?

Back 95

Decreases LES tone

Front 96

Which AntiCh is more sedating?

Back 96

Atropine

Front 97

Which AntiCh has greater antisialogogue effects?

Back 97

Glycopyrrolate

Front 98

Which AntiCh creates cycloplegia?

Back 98

Atropine

Front 99

Which AntiCh is more effective on N/V?

Back 99

Atropine

Front 100

Which AntiCh would you administer to a pregnant woman? Why?

Back 100

Glycopyrrolate

Lipid soluble, so does not cross the BBB, therefore no fetal (or CNS) effects

Front 101

At what dose will Atropine generate complete block of the PNS?

Back 101

2mg

Front 102

At what dose of Atropine will you see cardiac slowing?

Back 102

0.5mg

Front 103

At what dose of Atropine will you see definite dryness of the mouth?

Back 103

1.0mg

Front 104

At what dose of Atropine will you see dilated pupils?

Back 104

2.0mg

Front 105

At what dose of Atropine will you see an inhibition of sweating?

Back 105

0.5mg

Front 106

At what dose of Atropine will you see difficulty speaking and/or swallowing?

Back 106

5mg

Front 107

At what dose of Atropine will you see difficulty w/ micturation, decr GI peristalsis?

Back 107

5mg

Front 108

At what dose of atropine will you see obliterated irises, hot, flushed skin, and ataxia?

Back 108

10mg

Front 109

FYI -->
Anti-Ch poisoning
Red as a beet, blind as a bat, dry as a bone, mad as a hatter, hot as a hare

Back 109

FYI -->
Anti-Ch poisoning
Red as a beet, blind as a bat, dry as a bone, mad as a hatter, hot as a hare

Front 110

Clonidine & Dex are examples of what class of drugs?

Back 110

Alpha-2 agonists

Front 111

Two examples of alpha-antagonists are...

Back 111

Droperidol & phentolamine

Front 112

Why should B-blockers be used w/ caution in DM?

Back 112

They mask the s/s of hypoglycemia