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PHRX 3009: drug action > 34: Drug Action on Adrenergic Receptors > Flashcards

34: Drug Action on Adrenergic Receptors Flashcards

1
Q

Explain the signaling mechanism of Chatecholamine.

A

Norepinephrine and epinephrine diffuse across the synaptic cleft –> bind to adrenergic receptors on postsynaptic membrane –> stimulate the sympathetic nervous system (SNS) –> intracellular responses.

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2
Q

Explain the different types of adrenergic receptors.

A

a-receptors:
* a1 and a2

b-receptors:
* b1, b2, and b3

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3
Q

What are the categories of adrenergic receptors based off of?

A

Based on their affinity for adrenergic agonists: norepinephrine, epinephrine, and isoprenaline.

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4
Q

Explain the difference between structures of norepinephrine, epinephrine, and isopreterenol.

A
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5
Q

What class are adrenergic receptors?

A

G protein-coupled receptors

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6
Q

What is the potency order of a1 receptor agonists?

A

NE > E&raquo_space; ISO

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7
Q

What is the potency order of a2 receptor agonists?

A

E = NE&raquo_space; ISO

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8
Q

What is the potency order of b1 receptor agonists?

A

ISO > NE > E

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9
Q

What is the potency order of b2 receptor agonists?

A

ISO > E > NE

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10
Q

What is the potency order of b3 receptor agonists?

A

ISO > NE = E

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11
Q

Explain the activation mechanisms of a1 receptors.

A
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12
Q

Explain the inhibition mechanisms of a2 receptors.

A
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13
Q

Explain the activation mechanisms of b1, b2, and b3 receptors.

A
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14
Q

Explain the tissue locations of a1 receptors.

A
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15
Q

Explain the tissue locations of a2 receptors.

A
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16
Q

Explain the tissue locations of b1 receptors.

A
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17
Q

Explain the tissue locations of b2 receptors.

A
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18
Q

Explain the tissue locations of b3 receptors.

A
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19
Q

What are the major effects from stimulation of the a1 receptor?

A

INCREASE STIMULATION of:

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20
Q

What are the major effects from stimulation of a2 receptors?

A

DECREASE STIMULATION of:

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21
Q

What are the major effects of stimulation of b1 receptors?

A

INCREASE STIMULATION of

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22
Q

What are the major effects of stimulation of b2 receptors?

A
red: decrease green: increase
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23
Q

What are the major effects of stimulation of b3 receptors?

A

INCREASE STIMULATION of

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24
Q

Explain the drug action categorizations of adrenergic agonists.

25
Name the three categories of adrenergic agonists.
* direct-acting * mixed-acting * indirect-acting
26
Name the two types of direct-acting adrenergic agonists.
Selective and non-selective
27
Name the 4 different types of indirect-acting adrenergic agonists.
* releasing agents * uptake inhibitor * MOA inhibitors * COMT inhibitors
28
Describe the diseases that can be treated by *direct-acting non-selective agonist*: epinephrine.
* heart problems: cardiac arrest, bradycardia * emergency treatment of allergic reactions by EpiPen * asthma: brochodilator * local anesthetics: prolong the action of the anesthetic agent
29
Describe the diseases that can be treated by *direct-acting non-selective agonist:* norepinephrine.
* hypotension * vasodilatory shock, such as septic shock and neurogenic shock
30
Describe the diseases that can be treated by *direct-acting non-selective agonist:* Isoprenaline.
* emergency for cardiac arrest, hypovolemic shock, septic shock * congestive heart failure * asthma
31
Describe the diseases that can be treated by *direct-acting selective a1 agonists:* phenylephrine.
Drug action: phenylephrine stimulates a1 receptor --> increase blood pressure and relieve hemorrhoids. * decongestant * hemorrhoids: prevent hemorrhoids by causing constriction of vascular smooth muscle * pupil dilation: dilation facilitates visualization of the retina * vasopressor: increase blood pressure in patients with hypotension
32
Describe the diseases that can be treated from *direct-acting selective a2 agonists:* clonidine.
drug action: stimulates a2 receptor in the brain to decrease peripheral vascular resistance and lower blood pressure. * hypertension: lower blood pressure * psychiatric disorders: stress, sleep disorders, and hyperarousal * migraine * diarrhea associated with ibs (irritable bowel syndrome)
33
Describe the diseases that can be treated from *direct-acting selective b1 agonists:* dobutamine.
drug action: stimulator of b1 receptor of the SNS to increase contractility and cardiac output. * acute heart failure * congestive heart failure by increasing cardiac output * used as a pharmacologic stress testing agent to identify coronary artery disease
34
Describe the diseases that can be treated from *direct-acting selective b2 agonists:* albuterol.
drug action: albuterol stimulates the b2 receptors on the bronchial smooth muscles to inhibit myosin phosphorylation --> lowers the intracellular concentration of Ca2+ --> less muscle contraction * allergic asthma * chronic obstructive pulmonary disease * rescue inhaler for alleviated asthma attack
35
Describe the diseases that be treated by *mixed-acting non-selective agonists:* ephedrine.
drug action: ephedrine increases release of norepinephrine from nerve endings and stimulate both a and b receptors --> raises systolic and diastolic blood pressure by vasoconstriction and cardiac stimulation. * hypotension * asthma: bronchodilation with slow action * enhancement on sleep * decrease motion sickness
36
List the common adverse effects of adrenergic agonists.
* arrhythmias * insomnia * headache * nausea * hyperactivity * tremors
37
Name the three different types of adrenergic receptor antagonists.
* a receptor antagonists * b receptor antagonists * a & b antagonists
38
Name the three types of a-receptor antagonists.
* nonselective * a1 selective * a2 selective
39
Describe the diseases that can be treated from *nonselective a receptor blocker:* phenoxybenzamine.
drug action: form permanent covalent bond with a receptors --> prevents epinephrine and norepinephrine from binding * hypertension: reduce vasoconstriction, reduce sympathetic activity, and decrease blood pressure
40
Describe the diseases that are able to be treated by *selective a1 receptor blockers:* prazosin.
drug action: selective a1 blocker, actis like an inverse agonist at a1 receptors --> induces response **opposite** of that a1 agonist. * FIRST CHOICE treatment for patients with **both** hypertension and prostatic hyperplasia
41
Explain the characteristics of adrenergic B receptor blockers.
Adrenergic b blockers act as adrenergic B receptor antagonist. * prevent the stimulation of the adrenergic receptors that are responsible for increased cardiac action * controls heart rhythm, treat angina, and reduce blood pressure.
42
Explain the three different types of B-adrenergic receptor antagonists.
1st generation nonselective 2nd generation B1-selective 3rd generation vasodilatory * nonselective * B1-selective
43
Explain the drug action mechanism of *1st generation B blockers:* propranolol.
Non-selective B-blocker and and block action of epinephrine and norepinephrine at both B1 and B2 adrenergic receptors. * propranolol is able to penetrate the BBB and exert effects in the CNS + peripheral activity.
44
Describe the diseases that can be treated from *1st generation B blockers*: propranalol
* hypertension * irregular heart rate * angina * anxiety * migraine * tremor
45
Explain the drug action mechanism of *2nd generation B blockers:* metoprolol.
Metoprolol is a selective B1 blocker * blocks the action of epinephrine and norepinephrine at B1-adrenergic receptors
46
Describe the diseases that can be treated from *2nd generation B blockers:* metoprolol.
* hypertension * tachycardia * angina * long QT syndrome * acute myocardial infarction * migraine
47
Describe the characteristics of *3rd generatino B blockers*
* Non-selective or selective * carvedilol and labetalol also have the capability to block a1 receptors * have additional vasodilating effects and are more effective in the decrease of blood pressure --> suitable for hypertension treatment
48
D. G-protein coupled receptor
49
.
B. ISO > E > NE
50
E. Decrease of cAMP and decrease of PKA
51
A. a1
52
E. None of the above is correct.
53
B. Decrease sympathetic activity by decreasing NE release from post-ganglionic neurons
54
C. a1 effect
55
.
A. NE
56
A. terozosin
57
D. Propranolol has replaced pseudoephedrin as the most common otc decongestant
58
A. B1 antagonist
59
D. metoprolol

PHRX 3009: drug action (36 decks)

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