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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
What receptor does epinephrine interact with to relax bronchial muscle?
β2
26
What receptor does epinephrine interact with to decrease bronchial secretion and congestion within bronchial mucosa?
α1
27
What receptor does epinephrine interact with to cause muscle tremor and increase K+ uptake by skeletal muscle?
β2
28
What receptor does epinephrine interact with to enhance liver glycogenolysis and gluconeogenesis?
β2
29
What receptor does epinephrine interact with to increase renin release?
β1
30
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?
1) Reduces 2) Vasoconstrictor 3) Increases it
31
Why can't NE produce bronchodilation and vasodilation?
It does not stimulate β2
32
What effects does phenylephrine cause?
1) Vasoconstriction 2) BP elevation 3) Bradycardia
33
What effects does clonidine cause?
1) Decrease sympathetic outflow 2) Reduce BP 3) Bradycardia
34
What effects does isoproterenol cause and which beta receptor is used for each effect?
1) Increase cardiac output (β1) 2) Vasodilator, decrease arterial pressure (β2) 3) Bronchodilation (β2)
35
A (-) isomer of Dobutamine has what effect on α1 receptors? (+) isomer?
1) Agonist | 2) Antagonist
36
What effect does albuterol have?
Bronchodilation
37
Mydriasis is a sign of overdose with what drug?
Phenylephrine
38
Cocaine is an indirect adrenomimetics with what effect?
Inhibits dopamine and NE reuptake
39
Phenelzine and selegiline are indirect adrenomimetics with what effect?
Inhibit MAO
40
Amphetamines, Methylphenidate, and Tyramine are indirect adrenomimetics with what effect?
Increase dopamine and NE release while inhibiting their reuptake
41
Ephedrine is an indirect adrenomimetics with what effect?
Increase dopamine and NE release and is a direct receptor agonist
42
Why can all indirect-acting adrenomimetics except for tyramine easily penetrate the BBB?
They are lipophilic compounds
43
Indirect-acting adrenomimetics significantly affect what nervous system?
CNS
44
What is used to increase BP during Hypotensive emergencies such as hemorrhagic shock, overdose of antihypertensives, and CNS depressants?
1) NE | 2) Phenylephrine
45
What drug is used to increase BP for chronic hypotension?
Ephedrine
46
What drug is used to increase BP for cardiogenic shock?
Dobutamine
47
What drug is used for short-term use in acute heart failure?
Dobutamine
48
What class of drugs are used as a long-term treatment for hypertension?
Alpha-2 agonists
49
Phenelzine and Selegiline are used to treat?
Depression
50
What drugs are used to treat narcolepsy?
Amphetamines and methylphenidate
51
Methylphenidate is used to treat?
ADHD
52
What drugs are used to treat obesity?
Ephedrine and amphetamines
53
Albuterol is used to treat?
Bronchial asthma
54
What is used for decongestion of mucous membranes?
1) Phenylephrine | 2) Ephedrine
55
What is used to treat anaphylaxis?
Epinephrine
56
What class of drugs is used to treat glaucoma?
α2 selective agonists
57
What is used to treat stress urinary incontinence?
Ephedrine
58
Phentolamine and Phenoxybenzamine fall under what category of receptor antagonists?
Non-selective (α1 and α2) receptor antagonists
59
Prazosin, Tamsulosin, and Doxazosin fall under what category of receptor antagonists?
α1 receptor selective
60
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?
1) Phentolamine 2) Phenoxybenzamine 3) Phentolamine
61
In the cardiovascular system, Alpha antagonists have what effect on the peripheral vascular resistance and blood pressure? What effect on heart rate?
1) Decrease | 2) Tachycardia
62
In the Genitourinary system, Alpha antagonists have what effect on smooth muscle in prostate? What effect on the flow of urine?
1) Relaxation | 2) Decreased resistance
63
In the eye Alpha antagonists have what effect on the pupillary dilator muscle?
Relaxation (miosis)
64
Phentolamine, phenoxybenzamine, and metyrosine can be used to treat what tumor?
Pheochromocytoma
65
Prazosin, doxazosin (α1 selectives) are used to treat?
Chronic hypertension
66
A combination of phentolamine and a nonspecific vasodilator papaverine is used to treat?
Erectile dysfunction
67
What does Tamsulosin treat more effectively than Prazosin and doxazosin because it does not affect BP like they do?
Benign prostate hyperplasia (BPH)
68
Which α receptor subtype is the most important for mediating prostate smooth muscle contraction?
α1A
69
Labetalol and Carvedilol fall under what category of Adrenoceptor antagonists?
Mixed blockers (β- and α1 antagonist)
70
Propranolol, Pindolol, and Nadolol fall under what category of Adrenoceptor antagonists?
β1 and β2 (non-selective) blockers
71
Metoprolol, Betaxolol, Acebutolol, and Atenolol fall under what category of Adrenoceptor antagonists?
β1 selective
72
Atenolol, Nadolol, and Propranolol are under what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?
Antagonists
73
Acebutolol, Labetalol, and Pindolol are under what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?
Partial agonists
74
Betaxolol and Metoprolol are under what what specific category together in terms of their intrinsic activity of beta-blockers at the receptor?
Inverse agonists
75
What are beta blockers with ISA (Intrinsic Sympathomimetic Activity)?
Partial agonists at beta adrenergic receptors
76
What role do Beta blockers with ISA have? Why would use of this agent be useful?
1) Block sympathetic effects but not as much as antagonists | 2) Less risk for bradycardia
77
In the heart, what effect do beta-blockers have on contractility? Heart rate? It slows conduction via?
1) Negative inotropic effect 2) Negative chronotropic effect 3) AV node
78
In blood vessels, what effect do beta-blockers have on peripheral vascular resistance?
1) Initially increases | 2) Chronic use decreases
79
What effect do beta-blockers have on the Renin-angiotensin system?
Inhibit renin release
80
What effect do beta-blockers have on the respiratory system?
Increase airway resistance
81
In the eye, what effect do beta-blockers have on aqueous humor and Intraocular pressure?
Reduce both
82
What effect do beta-blockers have on lipolysis? VLDL? HDL? Glycogenolysis and gluconeogenesis in the liver?
1) Inhibit 2) Increase 3) Decrease 4) Inhibit
83
Both beta-blockers and mixed α and β blockers (labetalol, α1 and βblocker) are used to treat?
HTN
84
What reduces the frequency of anginal episodes and improve exercise tolerance?
Beta-blockers
85
What beta-blockers are used in the long term for MI?
Propranolol and Metoprolol
86
Metoprolol and carvedilol have shown in clinical trials to be effective in treating?
Heart failure
87
Betaxolol is a beta blocker without local anesthetic activity to treat?
Glaucoma
88
What beta blocker is used to treat hyperthyroidism?
Propranolol
89
If a patient is seen having adverse CNS effects such as sedation, sleep disturbances, and depression what should you switch to?
Hydrophilic drugs
90
If a patient is seen having adverse respiratory effects such as increase airway resistance, bronchospasm, and asthma attacks what should you switch to?
Beta-1 selective
91
If a patient is seen having adverse Cardiovascular effects such as depression of heart rate, cardiac contractility and excitability what should you switch to?
Partial agonist
92
If a patient is seen having adverse effects such as hypoglycemic episodes what should you switch to?
Beta-1 selective
93
Abrupt discontinuation of beta blockers can lead to?
Enhanced cardiac stimulation and arrhythmias
94
What NT is released in the SA node of the heart in response to the systemic administration of an alpha 1 adrenergic agonist drug?
ACh
95
What is the Direct-acting effect of NE? When is it utilized?
1) Activates beta-1 receptors on cardiac pacemaker cells to cause tachycardia 2) In the presence of atropine
96
What effect does propranolol have on phentolamine?
It blocks phentolamine induced tachycardia

SBL Week 1 (7 decks)

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