Adrenergic Agonists & Antagonists Flashcards

1
Q

What is the primary clinical indication for Isoproterenol?

A

Patients with heart block

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2
Q

What ADR is associated with high doses of a Beta2 agonist?

A

Tremors due to stimulation of Beta2 receptors on skeletal muscle

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3
Q

What serious effect is associated with the abrupt discontinuance of beta blockers?

A

Heart arrhythmias

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4
Q

Dopamine is the drug of choice for the treatment of shock. Why is this?

A

Stimulates D1, beta, and alpha receptors - increases CO & BP while still maintaining adequate perfusion of important organs, such as the kidney, gut, and heart

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5
Q

What alpha1 blocker is most effective for BPH (benign prostatic hyperplasia) and not hypertension?

A

Tamsulosin

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6
Q

What drug is a Beta1 agonist?

A

Dobutamine

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7
Q

True/False. Drugs that stimulate Beta and Alpha receptors always stimulate Beta receptors first.

A

True. Beta receptors are first activated followed by alpha receptors, depending upon the drug dose. Dopamine receptors would be activated before beta receptors in a drug that stimulates all receptors.

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8
Q

A patient experiences hypertension due to a high epinephrine dose. An alpha1 blocker is administered. What is the ultimate effect on BP?

A

BP will decrease significantly and the patient will become hypotensive. This is because epinephrine also stimulates Beta receptors causing vasodilation and decreased TPR. This response is called epinephrine reversal

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9
Q

Prazosin, doxazosin, and tamsulosin are why types of drugs?

A

Selective alpha1 blockers

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10
Q

What is the MOA for beta blockers that have anesthetic effects?

A

Block Na+ channels to stabilize the cell membrane

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11
Q

What drug acts as a non-selective Beta agonist?

A

Isoproterenol

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12
Q

Alpha 2 antagonists are clinically indicated for the treatment of…?

A

Hypertension, withdrawal symptoms from opiates, tobacco, benzodiazepines

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13
Q

What catecholamine is contraindicated in patients with a sulfur allergy?

A

Isoproterenol

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14
Q

Postural hypotension is associated with blockage of what receptors?

A

Alpha1

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15
Q

What drugs belong to the non-selective beta agonists class?

A

Epinephrine & isoproterenol

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16
Q

True/False. Albuterol is used as a long-term bronchodilator for asthma treatment.

A

False. Albuterol is a short-term bronchodilator

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17
Q

Dobutamine is preferred in patients with acute heart failure. Why is this?

A

It increases CO without increasing contractility so O2 demand of the heart is not increased

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18
Q

What is the effect of Beta2 stimulation on blood vessels?

A

Vasodilation, decreased TPR, decreased BP

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19
Q

What beta-blockers can cross the BBB?

A

Propranolol & Carvedilol

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20
Q

What is the effect of NE on HR?

A

Reflex bradycardia due to increased BP and TPR

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21
Q

What is the effect of Beta2 stimulation on blood glucose?

A

Beta2 stimulation promotes glycogenolysis and increases blood glucose

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22
Q

At therapeutic doses, NE preferentially stimulates what receptors?

A

Alpha receptors more than beta receptors

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23
Q

What Beta blockers have partial agonist activity?

A

Pindolol & acebutolol

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24
Q

Stimulation of what receptor causes contraction of the bladder and promotes urine retention?

A

Alpha1

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25
Q

What adrenergic neurotransmitter is released at organs innervated by the SANS?

A

NE

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26
Q

What two drugs are mixed adrenergic agonists?

A

Ephedrine & pseudophedrine

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27
Q

What class of adrenergic drug is indicated for the treatment of an overactive bladder?

A

Beta3 agonist (Mirabegron)

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28
Q

Where are D2 receptors located?

A

CNS

29
Q

What beta-blocker can be used to treat glaucoma?

A

Nadolol - no anesthetic effects

30
Q

What drug acts on the adrenergic synapse to block NE synthesis?

A

Metyrosine

31
Q

What is the suffix for all beta blockers?

A

-olol

32
Q

Alpha1 receptors have what effects on the eye?

A

Mydriasis (pupil dilation) and increased ocular pressure

33
Q

What drug acts on the adrenergic synapse to block NE storage?

A

Reserpine

34
Q

What are the non-selective alpha-blockers?

A

Phenoxybenzamine & Phentolamine

35
Q

What drug selectively stimulates D1 receptors?

A

Fenoldopam

36
Q

What is the effect of Beta1 stimulation on the heart?

A

Increased HR, increased contraction, increased CO

37
Q

What adrenergic agonist is used to treat patients in septic shock?

A

NE to increase BP quickly

38
Q

A woman is experiencing premature labor and needs to be transferred to a facility with a NICU. What drug may be administered to inhibit uterine contractions during transportation?

A

Beta2 agonist - Terbutaline

39
Q

What is the effect of Beta2 stimulation on the lungs?

A

Bronchodilation

40
Q

What receptors are stimulated to suppress premature labor in women?

A

Beta2

41
Q

What is the difference between direct and indirect adrenergic agonists?

A

Direct agonists bind directly to the receptor. Indirect agonists indirectly increase NE at the synapse by promoting release, inhibiting reupdate, and/or inhibiting degradation

42
Q

Activation of D1 receptors has what effect on blood vessels?

A

Vasodilation

43
Q

Use of an alpha1 antagonist may have what effect on male ejaculation?

A

Inhibited ejaculation

44
Q

Nebivolol belongs to what drug class?

A

Beta1 blocker

45
Q

True/False. Epinephrine is non-selective for alpha and beta receptors.

A

True. However, since epinephrine stimulates both, beta receptors will be stimulated before alpha receptors at low doses.

46
Q

What drugs act as indirect adrenergic agonists?

A

Cocaine, TCA, amphetamines, tyramine

47
Q

What is the MOA of cocaine on the adrenergic synapse?

A

Prevents NE reuptake

48
Q

True/False. Catecholamines are used primarily in outpatient settings.

A

False. Catecholamines are extremely potent and fast acting. They must also be given via IV. As such they are used only in emergencies.

Non-catecholamines have a longer 1/2 life and are by PO administration. They are used in outpatient settings.

49
Q

What are the two classifications of direct-acting adrenergic agonists?

A

Catecholamines & Non-catecholamines

50
Q

What is the primary function of Alpha2 receptors?

A

Autoreceptors that decrease NE

51
Q

What are the short-acting Beta2 agonists?

A

Albuterol & Terbutaline

52
Q

What drug acts on the adrenergic synapse to block NE release?

A

Guanethidine

53
Q

Alpha1 receptors have what effects on blood vessels?

A

Vasoconstriction, increased TPR, increased BP

54
Q

What adrenergic receptors are always stimulatory?

A

Alpha1 & Beta1

55
Q

Alpha2 receptors are located where?

A

On pre-synaptic neurons to decrease NE

56
Q

Where are most Beta1 receptors located?

A

Heart

57
Q

What is the general effect of Isoproterenol on BP?

A

Decrease - HR & CO increase due to Beta1 stimulation, but blood vessels dilate and TPR decreases due to Beta2 stimulation

58
Q

What is the primary method in which NE is removed from the synaptic cleft?

A

Active reuptake into the pre-synaptic neuron

59
Q

What is the primary difference between Phenoxybenzamine & Phentolamine?

A

Phenoxybenzamine is long-acting and irreversible. Phentolamine is short-acting and reversible

60
Q

What adrenergic receptors are always inhibitory?

A

Alpha2 & Beta2

61
Q

This molecule is found in picked and fermented food and increases release of NE.

A

Tyramine

62
Q

Why is rebound hypertension possible with abrupt discontinuance of alpha2 agonists?

A

Alpha2 agonists decrease NE. As a result, post-synaptic neurons upregulate their receptors. When alpha2 agonists are discontinued rapidly, normal release of NE on more receptors will cause hypertension and other symptoms

63
Q

What is the MOA of amphetamines on the adrenergic synapse?

A

Increases NE release and decreases uptake

64
Q

What neurotransmitter is primarily released on Beta2 receptors?

A

Epinephrine

65
Q

True/False. Non-selective alpha agonists should never be used in the eye or nose.

A

False. They should ONLY be used in the eye and nose. Systemic use will cause severe hypertension and ADRs

66
Q

What are the clinical uses of epinephrine?

A

Anaphylactic shock, cardiac arrest, asthma attack

67
Q

What type of adrenergic receptor exists on the pre-synaptic neuron and serves as an autoreceptor to decrease NE release?

A

Alpha2 - activated when NE concentrations in the synaptic cleft are very high

68
Q

What effect do beta blockers have on blood glucose that is an important consideration in diabetic patients?

A

Can lead to hypoglycemia, but symptoms (tachycardia, tremors, etc.) may be masked