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Medical Pharmacology Exam 1 > Adrenergics II > Flashcards

Adrenergics II Flashcards

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USMLE® Step 1 flashcards
1
Q

Reduction is SA node pace and decreasing cardiac contractility is accomplished by modulating which type of receptor?

A

Muscarinic (M2)

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2
Q

What is the effect of cholinergic stimulation to the SA node? AV node?

A

SA - Decrease HR

AV - Decrease conduction velocity, increase refractory period

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3
Q

What is the effect of cholinergic stimulation to the Atria? Ventricles?

A

Atria - Decreased contractile strength

Ventricle - Small decrease in contractile strength

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4
Q

The major effects of the sympathetic NS on the heart are accomplished via what adrenergic receptor?

A

Beta 1 (mainly)

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5
Q

What is the effect of sympathetic NS stim on the eye? Parasymp?

A

Symp - mydriasis

Parasymp - Miosis

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6
Q

What is the exception to the rule where the sympathetic NS causes glandular secretion?

A

Sweat glands - cholinergic post-ganglionic sympathetic neurons

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7
Q

Stimulation of what receptor will Lead to blood vessel constriction in cardiac and skeletal muscle? What about dilation?

A

Constriction - Alpha 1

Dilation - Beta 2

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8
Q

Stimulation of what receptor will Lead to blood vessel constriction in the skin and GI tract?

A

Alpha 1

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9
Q

Symp or parasymp; which is responsible for erection? ejaculation?

A

Erection - parasymp

Ejaculation - symp

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10
Q

Increased glycogenolysis in liver and skeletal muscle, and increased insulin secretion occurs because of stimulation of what type of adrenergic receptor?

A

Beta 2

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11
Q

Sympathetic NS mediated increased lypolysis is accomplished via stimulation of what receptors (2)?

A

Beta 1 and beta 3

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12
Q

What are the 2 adrenergic type receptors found on presynaptic sites?

A

Alpha 2 and DA 2

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13
Q

Drugs stimulating the adrenergic system will likely treat _, while drugs inhibiting it will likely treat _ [hypo/hypertension]

A

Stimulate - hypotension

Inhibit - hypertension

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14
Q

Clonidine, guanabenz and alpha-methyldopa are all examples of _. They are used to promote _

A

Alpha 2 receptor agonists

Hypotension

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15
Q

What are six side effects associated with alpha 2 receptor agonists?

A

sedation, xerostomia,
anorexia, fluid retention,
vivid dreams & CNS
stimulation

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16
Q

What is the target of bromocriptine? What is the clinical use?

A

DA 2 receptor agonist

Treatment of Parkinson’s with CNS effects

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17
Q

What are 2 expected side effects of D2 receptor agonists (bromocriptine)? What is the location of the receptors that mediate its side effects?

A

Postural hypotension
Cardiac arrhythmia
Peripheral NS - desired targets in CNS

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18
Q

What is the mechanism of action of reserpine? How does it get into the presynaptic terminal?

A

Reduces biogenic amines stored in vesicles / released

Enters in presynaptic terminal via amine 1 transporter AKA Norepinephrine Transporter

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19
Q

What are the biogenic amines that can be affected by reserpine?

A

Epi, DA, NE, serotonin

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20
Q

What are 3 expected CNS side effects of reserpine?

A

Sedation
Depression
Parkinsonian symptoms

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21
Q

What is the side effect of reserpine on GI function?

A

Increased motility, ulcers

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22
Q

What is the mechanism by which guanethidine functions? What are the indications?

A

Stabilizes membranes, depletes vesicles containing NE

Severely elevated arterial pressures

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23
Q

What is the expected effect of cocaine and tricyclic antidepressants on guanethidine function? How does guanethidine enter the presynaptic terminal?

A

Cocaine and TCAs block transport of NE back into the synapse, therefore antagonize guanethidine function
Enters synapse via amine 1 transporter (AKA NET)

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24
Q

What is the effect of chronic guanethidine use? How does it affect epinephine and DA? What are the CNS side effects?

A

Chronic use deplete NE
No effects on epi and DA
No CNS effects, doesn’t cross BBB

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25
Q

What is the mechanism of action of alpha-methyldopa? What is it used to treat?

A

Alphamethyldopa mimics DOPA in synthetic pathway, causing synthesis of false NE (reduced efficacy)
Used to treat hypertension

26
Q

How does alphamethyldopa cause its hypotensive effects?

A

Stimulation of brainstem vasomotor center

27
Q

What are 6 potential side effects associated with alpha methyl dopa?

A

Sedation, dizziness, sleep disturbance, impotence, dry mouth and nasal congestion

28
Q

Why does chronic therapy with alpha methyl DOPA require close monitoring?

A

Chronic therapy can cause severe problems like hemolytic anemia, leukopenia, lupus and hepatitis

29
Q

What are the 4 examples of alpha 1 selective antagonists provided? Which is least alpha 1 selective***?

A

Prazosin
Terazosin
Doxazosin
Phenoxybenzamine ***

30
Q

What is the example provided that antagonizes alpha 1 and alpha 2 equally?

A

Phentolamine

31
Q

Phenoxybenzamine preferential targets which alpha receptor?

A

Alpha 1 over alpha 2

32
Q

A mixed antagonist that will target both beta and alpha receptors is _. Which of the two will it bind to better?

A

Labetalol

Beta receptors

33
Q

What are the three examples of beta specific antagonists provided? Which beta receptor do they preferentially bind?

A

Atenolol
Betaxolol
Metoprolol
Beta 1 over beta 2

34
Q

What are the 3 examples of antagonists drugs that bind equally to beta receptors?

A

Propranolol
Pindolol
Timolol

35
Q

What is the mechanism of action of phenoxybenzamine (2)? How long does it act?

A

Non competitively and covalently binds alpha 1 receptor, blocks NE binding
Covalently binds amine 1 transporter, blocks NE uptake
24 hrs

36
Q

Phenoxybenzamine can cause hypotension and tachycardia. Why?

A

Takes out majority of alpha 1 receptors, leading to reflex activation of the adrenergic branch of NS

37
Q

What are the clinical uses of phenoxybenzamine?

A

Pheochromocytoma (inoperable / metastatic tumor)

Severe hypertension

38
Q

What is the example of the non-competitive alpha 1 blocker provided?

A

Phenoxybenzamine

39
Q

What is the mechanism of action of prazosin?

A

Competitive alpha 1 blocker

40
Q

Phenoxybenzamine and prazosin both block alpha 1 receptors. How do they compare?

A

Phenoxybenzamine is non-competitive

Prazosin is competitive

41
Q

What is the use of prazosin? How long does it last?

A

Used for hypertension

Lasts for 12 hrs

42
Q

What are the receptor targets of phentolamine? WHat are its effects

A

Competitive alpha 1 and alpha 2 receptor antagonist
Vasodilation - alpha 1
Increased NE release - alpha 2

43
Q

Phentolamine is considered a dirty drug. What other receptor subtypes will it bind (2)?

A

Histamine and Muscarinic receptors

44
Q

Among Prazosin, phentolamine and phenoxybenzamine, which 2 are likely to cause tachycardia? Increased cardiac output? Postural hypotension?

A

Respectively…
Phentolamine and phenoxybenzamine
Phentolamine
Phenoxybenzamine

45
Q

What is the clinical use of phentolamine?

A

Pheochromocytoma induced hypertension

46
Q

The major use of beta blockers is for the treatment of _. They are used in conjuntion with what other types of drugs?

A

Hypertension

Diuretics

47
Q

4 examples provided of beta 1/2 blockers are _. Where do these drugs work (pre/post synaptic)

A 
Propranolol
Pindolol
Timolol
Nadolol
Postsynaptic
48
Q

Why are combined beta 1/2 blockers notable for patients with asthma?

A

Might block bronchiole dialation

49
Q

Propranolol and Timolol are significant for MI because _

A

Can potentially prevent myocardial infarction reoccurence

50
Q

What drug is widely used to reduce intraoccular pressure (beta blocker)?

A

Timolol

51
Q

Why is nadolol different from the other combined 3 beta blocker presented?

A

Works for 14-24 hrs, vs 3-5 hrs for others

52
Q

In addition to antihypertensive, what drug is also indicated for migraine, antiarrhythmia and angina pectoris?

A

Propranolol

53
Q

What are the 4 beta 1 specific antagonists presented? What are their significance

A 
Betaxolol
Atenolol
Metoprolol
Esmolol
Cardiac specific
54
Q

Beta blockers may not always be completely specific. What group of patients have to be monitored carefully when on these drugs?

A

Asthma and COPD patients

55
Q

Of the beta 1 specific drugs, which can prevent reoccurence of MI?

A

Metoprolol

56
Q

Which 2 beta blockers are most likely to cause ataxia and dizziness?

A

Propranolol

Metoprolol

57
Q

Which to beta blockers are least likely to cause CNS side effects?

A

Nadolol

Atenolol

58
Q

What are the dangers of using beta blockers on patients with cardiac problem?

A

Can cause heart failure (beta 1 block reduces HR, contraction force, CO)

59
Q

What 4 adrenergic antagonists can be used to treat urinary obstruction secondary to prostatic hyperplasia? What receptor do they target?

A 
Prazosin
Doxazosin
Terazosin
Tamsulosin
Alpha 1 selective
60
Q

What 3 beta blockers might prolong survival following MI?

A

Timolol
Propranolol
Metoprolol

61
Q

What are 2 drugs used to treat pheochromocytoma preoperatively?

A

Phenoxybenzamine

Phentolamine

Medical Pharmacology Exam 1 (15 decks)

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