Adrenergic Drugs Flashcards

1
Q

Adrenergic drugs modulate adrenergic transmission and primarily control the function of which nervous system?

A

Sympathetic nervous system

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2
Q

What are adrenomimetics or sympathomimetics drugs?

What are sympatholytics or antiadrenergic drugs?

A

1) Drugs activating adrenergic transmission

2) Drugs inhibiting adrenergic transmission

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3
Q

What do adrenomimetic drugs promote the effects of while antiadrenergic drugs prevent their effects?

A

Norepinephrine/ epinephrine / dopamine at adrenergic receptors

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4
Q

What G protein do α1 receptors use?

What effect do they have?

A

1) Gq

2) Increase IP3 and DAG

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5
Q

What G protein do α2 receptors use?

What effect do they have?

A

1) Gi

2) Decrease cAMP

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6
Q

What G protein do β1 receptors use?

What effect do they have?

A

1) Gs

2) Increase cAMP

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7
Q

What G protein do D1 (dopamine) receptors use?

What effect do they have?

A

1) Gs

2) Increase cAMP

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8
Q

What G protein do D2 receptors use?

What effect do they have?

A

1) Gi

2) Decrease cAMP

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9
Q

While Direct-acting adrenergic drugs produce their effects via direct interaction with adrenergic receptors, how do Indirect-acting adrenergic drugs produce their effects by?

A

Increasing or reducing the concentration of norepinephrine at target receptors

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10
Q

Which receptor does Phenylephrine primarily use?

A

α1

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11
Q

Which receptor does Clonidine primarily use?

A

α2

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12
Q

Which receptors does norepinephrine use?

A

1) α1 and α2

2) β1

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13
Q

Which receptors does epinephrine use?

A

1) α1 and α2

2) β1 and β2

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14
Q

Which receptor does Dobutamine primarily use?

A

β1

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15
Q

Which receptor does Isoproterenol primarily use?

A

β1 and β2

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16
Q

Which receptor does Albuterol primarily use?

A

β2

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17
Q

What effect do α1 receptors have in most vascular smooth muscle, pupillary dilator muscle, prostate and heart?

A

Contraction

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18
Q

What effect do α2 receptors have in neurons?

Platelets?

Adrenergic and cholinergic nerve terminals?

Fat cells?

A

1) Modulate transmitter release
2) Aggregation
3) Inhibit transmitter release
4) Inhibits lipolysis

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19
Q

What effect do β1 receptors have in the juxtaglomerular cells in the heart?

A

1) Increases force and rate of contraction

2) Increase renin release

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20
Q

What effect do β2 receptors have in the respiratory, uterine, and vascular smooth muscle?

Skeletal muscle?

Liver?

A

1) Promotes smooth muscle relaxation
2) Promtos potassium uptake
3) Activates glycogenolysis and gluconeogenesis

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21
Q

What effect do β3 receptors have in the bladder?

In fat cells?

A

1) Relaxes detrusor muscle

2) Activates lipolysis

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22
Q

What effect do D1 receptors have in the smooth muscles?

A

Dilates renal blood vessels

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23
Q

What receptor does epinephrine interact with to increase force of cardiac contraction, increase HR, and increase conduction velocity at AV node?

A

β1 receptors

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24
Q

What receptor does epinephrine interact with to increases systolic BP, decrease diastolic BP, and decrease total peripheral vascular resistance?

A

β2 and α1 receptors

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25
Q

What receptor does epinephrine interact with to relax bronchial muscle?

A

β2

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26
Q

What receptor does epinephrine interact with to decrease bronchial secretion and congestion within bronchial mucosa?

A

α1

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27
Q

What receptor does epinephrine interact with to cause muscle tremor and increase K+ uptake by skeletal muscle?

A

β2

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28
Q

What receptor does epinephrine interact with to enhance liver glycogenolysis and gluconeogenesis?

A

β2

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29
Q

What receptor does epinephrine interact with to increase renin release?

A

β1

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30
Q

Norepinephrine is a potent cardiac stimulate that has what effect on heart rate?

What effect does it have on blood vessels?

What effect does it have on peripheral vascular resistance and BP?

A

1) Reduces
2) Vasoconstrictor
3) Increases it

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31
Q

Why can’t NE produce bronchodilation and vasodilation?

A

It does not stimulate β2

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32
Q

What effects does phenylephrine cause?

A

1) Vasoconstriction
2) BP elevation
3) Bradycardia

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33
Q

What effects does clonidine cause?

A

1) Decrease sympathetic outflow
2) Reduce BP
3) Bradycardia

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34
Q

What effects does isoproterenol cause and which beta receptor is used for each effect?

A

1) Increase cardiac output (β1)
2) Vasodilator, decrease arterial pressure (β2)
3) Bronchodilation (β2)

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35
Q

A (-) isomer of Dobutamine has what effect on α1 receptors?

(+) isomer?

A

1) Agonist

2) Antagonist

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36
Q

What effect does albuterol have?

A

Bronchodilation

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37
Q

Mydriasis is a sign of overdose with what drug?

A

Phenylephrine

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38
Q

Cocaine is an indirect adrenomimetics with what effect?

A

Inhibits dopamine and NE reuptake

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39
Q

Phenelzine and selegiline are indirect adrenomimetics with what effect?

A

Inhibit MAO

40
Q

Amphetamines, Methylphenidate, and Tyramine are indirect adrenomimetics with what effect?

A

Increase dopamine and NE release while inhibiting their reuptake

41
Q

Ephedrine is an indirect adrenomimetics with what effect?

A

Increase dopamine and NE release and is a direct receptor agonist

42
Q

Why can all indirect-acting adrenomimetics except for tyramine easily penetrate the BBB?

A

They are lipophilic compounds

43
Q

Indirect-acting adrenomimetics significantly affect what nervous system?

A

CNS

44
Q

What is used to increase BP during Hypotensive emergencies such as hemorrhagic shock, overdose of antihypertensives, and CNS depressants?

A

1) NE

2) Phenylephrine

45
Q

What drug is used to increase BP for chronic hypotension?

A

Ephedrine

46
Q

What drug is used to increase BP for cardiogenic shock?

A

Dobutamine

47
Q

What drug is used for short-term use in acute heart failure?

A

Dobutamine

48
Q

What class of drugs are used as a long-term treatment for hypertension?

A

Alpha-2 agonists

49
Q

Phenelzine and Selegiline are used to treat?

A

Depression

50
Q

What drugs are used to treat narcolepsy?

A

Amphetamines and methylphenidate

51
Q

Methylphenidate is used to treat?

A

ADHD

52
Q

What drugs are used to treat obesity?

A

Ephedrine and amphetamines

53
Q

Albuterol is used to treat?

A

Bronchial asthma

54
Q

What is used for decongestion of mucous membranes?

A

1) Phenylephrine

2) Ephedrine

55
Q

What is used to treat anaphylaxis?

A

Epinephrine

56
Q

What class of drugs is used to treat glaucoma?

A

α2 selective agonists

57
Q

What is used to treat stress urinary incontinence?

A

Ephedrine

58
Q

Phentolamine and Phenoxybenzamine fall under what category of receptor antagonists?

A

Non-selective (α1 and α2) receptor antagonists

59
Q

Prazosin, Tamsulosin, and Doxazosin fall under what category of receptor antagonists?

A

α1 receptor selective

60
Q

Between the non-selective receptor antagonists, which one is a reversible?

Which one is longer acting?

Which one has its effect antagonized by high concentrations of alpha agonist?

A

1) Phentolamine
2) Phenoxybenzamine
3) Phentolamine

61
Q

In the cardiovascular system, Alpha antagonists have what effect on the peripheral vascular resistance and
blood pressure?

What effect on heart rate?

A

1) Decrease

2) Tachycardia

62
Q

In the Genitourinary system, Alpha antagonists have what effect on smooth muscle in prostate?

What effect on the flow of urine?

A

1) Relaxation

2) Decreased resistance

63
Q

In the eye Alpha antagonists have what effect on the pupillary dilator muscle?

A

Relaxation (miosis)

64
Q

Phentolamine, phenoxybenzamine, and metyrosine can be used to treat what tumor?

A

Pheochromocytoma

65
Q

Prazosin, doxazosin (α1 selectives) are used to treat?

A

Chronic hypertension

66
Q

A combination of phentolamine and a nonspecific vasodilator papaverine is used to treat?

A

Erectile dysfunction

67
Q

What does Tamsulosin treat more effectively than Prazosin and doxazosin because it does not affect BP like they do?

A

Benign prostate hyperplasia (BPH)

68
Q

Which α receptor subtype is the most important for mediating prostate smooth muscle contraction?

A

α1A

69
Q

Labetalol and Carvedilol fall under what category of Adrenoceptor antagonists?

A

Mixed blockers (β- and α1 antagonist)

70
Q

Propranolol, Pindolol, and Nadolol fall under what category of Adrenoceptor antagonists?

A

β1 and β2 (non-selective) blockers

71
Q

Metoprolol, Betaxolol, Acebutolol, and Atenolol fall under what category of Adrenoceptor antagonists?

A

β1 selective

72
Q

Atenolol, Nadolol, and Propranolol are under what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?

A

Antagonists

73
Q

Acebutolol, Labetalol, and Pindolol are under what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?

A

Partial agonists

74
Q

Betaxolol and Metoprolol are under what what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?

A

Inverse agonists

75
Q

What are beta blockers with ISA (Intrinsic Sympathomimetic Activity)?

A

Partial agonists at beta adrenergic receptors

76
Q

What role do Beta blockers with ISA have?

Why would use of this agent be useful?

A

1) Block sympathetic effects but not as much as antagonists

2) Less risk for bradycardia

77
Q

In the heart, what effect do beta-blockers have on contractility?

Heart rate?

It slows conduction via?

A

1) Negative inotropic effect
2) Negative chronotropic effect
3) AV node

78
Q

In blood vessels, what effect do beta-blockers have on peripheral vascular resistance?

A

1) Initially increases

2) Chronic use decreases

79
Q

What effect do beta-blockers have on the Renin-angiotensin system?

A

Inhibit renin release

80
Q

What effect do beta-blockers have on the respiratory system?

A

Increase airway resistance

81
Q

In the eye, what effect do beta-blockers have on aqueous humor and Intraocular pressure?

A

Reduce both

82
Q

What effect do beta-blockers have on lipolysis?

VLDL?

HDL?

Glycogenolysis and gluconeogenesis in the liver?

A

1) Inhibit
2) Increase
3) Decrease
4) Inhibit

83
Q

Both beta-blockers and mixed α and β blockers (labetalol, α1 and βblocker) are used to treat?

A

HTN

84
Q

What reduces the frequency of anginal episodes and improve exercise tolerance?

A

Beta-blockers

85
Q

What beta-blockers are used in the long term for MI?

A

Propranolol and Metoprolol

86
Q

Metoprolol and carvedilol have shown in clinical trials to be effective in treating?

A

Heart failure

87
Q

Betaxolol is a beta blocker without local anesthetic activity to treat?

A

Glaucoma

88
Q

What beta blocker is used to treat hyperthyroidism?

A

Propranolol

89
Q

If a patient is seen having adverse CNS effects such as sedation, sleep disturbances, and depression what should you switch to?

A

Hydrophilic drugs

90
Q

If a patient is seen having adverse respiratory effects such as increase airway resistance, bronchospasm, and asthma attacks what should you switch to?

A

Beta-1 selective

91
Q

If a patient is seen having adverse Cardiovascular effects such as depression of heart rate, cardiac contractility and excitability what should you switch to?

A

Partial agonist

92
Q

If a patient is seen having adverse effects such as hypoglycemic episodes what should you switch to?

A

Beta-1 selective

93
Q

Abrupt discontinuation of beta blockers can lead to?

A

Enhanced cardiac stimulation and arrhythmias

94
Q

What NT is released in the SA node of the heart in response to the systemic administration of an alpha 1 adrenergic agonist drug?

A

ACh

95
Q

What is the Direct-acting effect of NE?

When is it utilized?

A

1) Activates beta-1 receptors on cardiac pacemaker cells to cause tachycardia
2) In the presence of atropine

96
Q

What effect does propranolol have on phentolamine?

A

It blocks phentolamine induced tachycardia