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Pharm Exam 2 > Lecture 14-16 - Scrogin - Adrenergics (Agonists) > Flashcards

Lecture 14-16 - Scrogin - Adrenergics (Agonists) Flashcards

1
Q

What are the direct-acting endogenous sympathomimetics?

A

NE, Epi, and dopamine

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2
Q

What is isoproterenol (ISO)

A

a synthetic catecholamine that is selective for beta receptors

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3
Q

Describe the efficacy of epi, NE, and ISO for alpha-1 receptors

A

Epi is greater than or equal to NE

Epi and NE are&raquo_space; ISO

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4
Q

Describe the efficacy of epi, NE, and ISO for alpha-2 receptors

A

Epi is greater than or equal to NE

Epi and NE are&raquo_space; ISO

*Note: this is the same for alpha 2

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5
Q

Describe the efficacy of epi, NE, and ISO for beta-2 receptors

A

Iso > Epi&raquo_space; NE

NE is a partial agonist only

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6
Q

Describe the efficacy of epi, NE, and ISO for beta-1 receptors

A

Iso > Epi = NE

NE and Epi have equal potency and efficacy

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7
Q

Adrenomimetic agonists can be broken into what 2 classes?

Define them.

A

Direct acting = acts on receptors directly

Indirect acting = promotes increase in endogenous NT in synaptic cleft (releasers or reuptake inhibitors)

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8
Q

What receptors does epi bind?

A

alpha-1 and alpha-2
beta-1 and beta-1
*depends on concentrations

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9
Q

How is epi eliminated/degraded?

A

Degraded by COMT and eliminated in urine

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10
Q

Low doses/infusion rates of epi gives binding to which receptors?

A

Beta-1 and Beta-2

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11
Q

What are the indications for low doses of epi?

A

Anaphylaxis and bronchospasm (acute asthma attack)

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12
Q

High doses/infusion rates of epi gives binding to which receptors?

A

Alpha-1

Beta-1 and Beta-2

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13
Q

What are the indications for high doses of epi?

A

Cardiac arrest and heart block

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14
Q

What is the mechanism of action for low doses of epi (*at each receptor)?

A

Beta-1 = + chronotropy and inotropy (inc HR, CO, and systolic)

Beta-2 = peripheral vasodilation, dec diastolic, and bronchodilation

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15
Q

What is the mechanism of action for high doses of epi (*at each receptor)?

A

Alpha-1 = peripheral vasoconstriction (this is the predominant effect) and dec bronchial secretions

*a1/b1/b2 give inc CO and TPR

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16
Q

What is the side effect for epi?

A

arrhythmias

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17
Q

What are the contraindications for epi?

A

Late term pregnancy

*note: this was not underlined

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18
Q

What receptors does NE bind?

A

Alpha-1 and Alpha-2
Beta-1
*has little affinity for beta-2

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19
Q

How is NE eliminated/degraded?

A

Degraded by COMT and MAO

Eliminated in urine

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20
Q

Describe the relative half life for NE and route of administration?

A

short half life

give via controlled infusion

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21
Q

What is the indication for NE?

A

Vasodilatory shock (acute HYPOtension)

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22
Q

Describe the mechanism of action for NE in relation to the receptors it binds

A

Alpha-1 = vasoconstriction, inc TPR, inc diastolic

Beta-1 = inc CO, inc systolic

Baroreflex = dec HR (dominates over chronotropy)

*also gives + chronotropy and inotropy

Inc in MAP = overall

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23
Q

What is the side effect of NE?

A

ischemia

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24
Q

What are the contraindications for NE?

A

Ischemia and pre-existing vasoconstriction (*if NE were given, it could induce gangrene)

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25
Q

What receptor does dopamine bind?

A

Dopamine-1 (D1) at low concentrations

Beta-1 and Alpha-1/Alpha-2 at higher infusion rates

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26
Q

What is the indication for dopamine?

A

Cardiogenic shock (HYPOtension due to low CO)

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27
Q

What is the mechanism of action for Dopamine at low infusion rates?

A

Activates D1 receptors = dec TPR

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28
Q

What is the mechanism of action for Dopamine at medium infusion rates?

A

Activates Beta-1 receptors = inc contractility and inc HR (inc CO)

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29
Q

What is the mechanism of action for Dopamine at high infusion rates?

A

Beta-1/Alpha-1/Alpha-2 stimulation = inc BP and inc TPR

30
Q

What are the side effects of dopamine at low infusion rates? high infusion rates?

A

Low infusion rates = HYPOtension

High infusion rates = Ischemia

31
Q

What is the contraindication for dopamine?

A

Uncorrected Tachyarrhythmia

32
Q

What are 6 direct-acting adrenergic agonists?

A
  1. Isoproterenol (ISO)
  2. Dobutamine
    3/4. Terbutaline/Albuterol
  3. Pheynlephrine
  4. Clonidine
33
Q

What are the 6 indirect acting adrenergic agonists?

A 
Amphetamine
Methamphetamine
Methylphenidate
Ephedrine
Pseudoephedrine
Tyramine
34
Q

What are the indications for ISO?

A

Bradycardia

Heart block when TPR is high

35
Q

What receptor does ISO bind?

A

It is a NON-SELECTIVE Beta-agonist

36
Q

How is ISO degraded?

A

By COMT

37
Q

What is the mechanism of action for ISO, in relation to specific receptors?

A

Beta-2 = vasodilation!, bronchodilation!, dec TPR, dec diastolic/systolic

Beta-1 = + inotropy and chronotropy (inc CO)

38
Q

What are the side effects for ISO?

A

Tachyarrhythmias

39
Q

What is the contraindication for ISO?

A

Angina with ARRHYTHMIA

40
Q

What receptor(s) does Dobutamine bind? with what affinity?

A

B1 > B2 > a

It’s a selective Beta-1 agonist

41
Q

What are the indications for Dobutamine?

A

Short term Rx for CHF (cardiac insufficiency)

Cardiogenic shock (low cardiac contractility)

42
Q

What is the mechanism of action for Dobutamine?

A

Inc CO

+ inotropy > + chronotropy (because of no/little beta-2 reflex tachy/vasodilation)

43
Q

What is the mechanism of action for high doses of Dobutamine?

A

It’ll bind Beta-2 and cause HYPOtension with reflex tachycardia

44
Q

What are the side effects for Dobutamine?

A

Hypotension (beta-2)

Arrhythmias (beta-1)

45
Q

How is Dobutamine degraded?

A

Rapidly by COMT

46
Q

What receptor(s) does Terbutaline/Albuterol bind? With what selectivity?

A

It is a Beta-2 agonist

47
Q

What are the indications for Terbutaline/Albuterol?

A

Bronchospasm (asthma, bronchitis, and emphysema)

Obstructive Airway Disease

48
Q

What does Terbutaline/Albuterol do?

A

Cause bronchodilation

Can give some Beta-1 agonist-like response (cardio effect)

49
Q

What are the side effects for Terbutaline/Albuterol?

A

Beta-1 = tachy (@ high dose)

Beta-2 = tolerance, skeletal muscle tremor, and activation of pre-synaptic cholinergic beta-2 receptors

50
Q

What receptor(s) does phenylephrine bind? Any selectivity?

A

Alpha-1 agonist

51
Q

What are the indications for Phenylephrine?

A

Paroxysmal supraventricular tachy

Mydriatic agent

Nasal decongestant

52
Q

Is Phenylephrine degraded by COMT?

A

No, because it’s not a catecholamine

53
Q

Compare the duration of action for endogenous catecholamines and phenylephrine

A

Phenylephrine has a longer duration of action

54
Q

What is the mechanism of action/effects of Phenylephrine?

A

Peripheral vasoconstriction, inc BP, activation of baroreflex, dec HR

Dilates pupil

Decreases bronchial secretions

55
Q

What is the side effect of phenylephrine?

A

HTN

56
Q

What receptoronidine does clonidine bind? Any selectivity?

A

Alpha-2 agonist

57
Q

What is the indication for clonidine

A

HTN from excess symp drive

58
Q

What is the mechanism of action for clonidine?

A

Peripheral effect = mild vasoconstriction, crosses BBB to dec symp outflow (reduce vasoconstriction an bp)

Central effect = dec BP

Overall: DEC BP

59
Q

For clonidine, dec tonic excitatory input to sympathetic cells leads to a reduction in sympathetic output to ___

A

vascular smooth muscle

60
Q

What are the side effects of Clonidine?

A

Dry mouth

Hypertensive crisis (after acute withdrawal)

61
Q

How do indirect-acting sympathomimetics increase the concentration of endogenous catecholamines?

A
  1. release of cytoplasmic catecholamines

2. blockade of re-uptake transporters

62
Q

Amphetamine-like drugs are taken up by ___ and cause ___

A

Taken up by re-uptake proteins

Cause reversal of transporter and lead to Ca2+ independent release of NT

63
Q

Do amphetamines cross the BBB?

A

Yes, this leads to high abuse potential

64
Q

What are indications of direct-acting adrenergic agonists?

A

ADD
Narcolepsy
Nasal Decongestion

65
Q

Name 2 indirect acting agonists that are used for ADHD

A

Amphetamine, Methylphenidate,

66
Q

Which indirect agonist is used for anesthesia?

A

Ephedrine

67
Q

Which indirect agonist is used for nasal decongestion?

A

Pseudoephedrine

68
Q

What is the therapeutic use of Tyramine?

A

There is none

It displaces NE

69
Q

How is Tyramine degraded?

A

By MAO

70
Q

What are the effects of indirect adrenergic agonists?

A

NE release gives peripheral vasoconstriction, + inotropy, inc conduction velocity

In the CNS it’s a stimulant and anorexic agent

71
Q

What is the side effect for indirect adrenergic agonists?

A

Tachy (beta-1)

72
Q

What is the contraindications for indirect acting adrenergic agonists?

A

Rx with MAOIs within the past 2 weeks

Pharm Exam 2 (7 decks)

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