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Medical Pharmacology Exam 1 > Adrenergics II > Flashcards

Adrenergics II Flashcards

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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
What is the mechanism of action of alpha-methyldopa? What is it used to treat?
Alphamethyldopa mimics DOPA in synthetic pathway, causing synthesis of false NE (reduced efficacy) Used to treat hypertension
26
How does alphamethyldopa cause its hypotensive effects?
Stimulation of brainstem vasomotor center
27
What are 6 potential side effects associated with alpha methyl dopa?
Sedation, dizziness, sleep disturbance, impotence, dry mouth and nasal congestion
28
Why does chronic therapy with alpha methyl DOPA require close monitoring?
Chronic therapy can cause severe problems like hemolytic anemia, leukopenia, lupus and hepatitis
29
What are the 4 examples of alpha 1 selective antagonists provided? Which is least alpha 1 selective***?
Prazosin Terazosin Doxazosin Phenoxybenzamine ***
30
What is the example provided that antagonizes alpha 1 and alpha 2 equally?
Phentolamine
31
Phenoxybenzamine preferential targets which alpha receptor?
Alpha 1 over alpha 2
32
A mixed antagonist that will target both beta and alpha receptors is _. Which of the two will it bind to better?
Labetalol | Beta receptors
33
What are the three examples of beta specific antagonists provided? Which beta receptor do they preferentially bind?
Atenolol Betaxolol Metoprolol Beta 1 over beta 2
34
What are the 3 examples of antagonists drugs that bind equally to beta receptors?
Propranolol Pindolol Timolol
35
What is the mechanism of action of phenoxybenzamine (2)? How long does it act?
Non competitively and covalently binds alpha 1 receptor, blocks NE binding Covalently binds amine 1 transporter, blocks NE uptake 24 hrs
36
Phenoxybenzamine can cause hypotension and tachycardia. Why?
Takes out majority of alpha 1 receptors, leading to reflex activation of the adrenergic branch of NS
37
What are the clinical uses of phenoxybenzamine?
Pheochromocytoma (inoperable / metastatic tumor) | Severe hypertension
38
What is the example of the non-competitive alpha 1 blocker provided?
Phenoxybenzamine
39
What is the mechanism of action of prazosin?
Competitive alpha 1 blocker
40
Phenoxybenzamine and prazosin both block alpha 1 receptors. How do they compare?
Phenoxybenzamine is non-competitive | Prazosin is competitive
41
What is the use of prazosin? How long does it last?
Used for hypertension | Lasts for 12 hrs
42
What are the receptor targets of phentolamine? WHat are its effects
Competitive alpha 1 and alpha 2 receptor antagonist Vasodilation - alpha 1 Increased NE release - alpha 2
43
Phentolamine is considered a dirty drug. What other receptor subtypes will it bind (2)?
Histamine and Muscarinic receptors
44
Among Prazosin, phentolamine and phenoxybenzamine, which 2 are likely to cause tachycardia? Increased cardiac output? Postural hypotension?
Respectively... Phentolamine and phenoxybenzamine Phentolamine Phenoxybenzamine
45
What is the clinical use of phentolamine?
Pheochromocytoma induced hypertension
46
The major use of beta blockers is for the treatment of _. They are used in conjuntion with what other types of drugs?
Hypertension | Diuretics
47
4 examples provided of beta 1/2 blockers are _. Where do these drugs work (pre/post synaptic)
``` Propranolol Pindolol Timolol Nadolol Postsynaptic ```
48
Why are combined beta 1/2 blockers notable for patients with asthma?
Might block bronchiole dialation
49
Propranolol and Timolol are significant for MI because _
Can potentially prevent myocardial infarction reoccurence
50
What drug is widely used to reduce intraoccular pressure (beta blocker)?
Timolol
51
Why is nadolol different from the other combined 3 beta blocker presented?
Works for 14-24 hrs, vs 3-5 hrs for others
52
In addition to antihypertensive, what drug is also indicated for migraine, antiarrhythmia and angina pectoris?
Propranolol
53
What are the 4 beta 1 specific antagonists presented? What are their significance
``` Betaxolol Atenolol Metoprolol Esmolol Cardiac specific ```
54
Beta blockers may not always be completely specific. What group of patients have to be monitored carefully when on these drugs?
Asthma and COPD patients
55
Of the beta 1 specific drugs, which can prevent reoccurence of MI?
Metoprolol
56
Which 2 beta blockers are most likely to cause ataxia and dizziness?
Propranolol | Metoprolol
57
Which to beta blockers are least likely to cause CNS side effects?
Nadolol | Atenolol
58
What are the dangers of using beta blockers on patients with cardiac problem?
Can cause heart failure (beta 1 block reduces HR, contraction force, CO)
59
What 4 adrenergic antagonists can be used to treat urinary obstruction secondary to prostatic hyperplasia? What receptor do they target?
``` Prazosin Doxazosin Terazosin Tamsulosin Alpha 1 selective ```
60
What 3 beta blockers might prolong survival following MI?
Timolol Propranolol Metoprolol
61
What are 2 drugs used to treat pheochromocytoma preoperatively?
Phenoxybenzamine | Phentolamine

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