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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.

A
25
Q

Name the three categories of adrenergic agonists.

A
  • direct-acting
  • mixed-acting
  • indirect-acting
26
Q

Name the two types of direct-acting adrenergic agonists.

A

Selective and non-selective

27
Q

Name the 4 different types of indirect-acting adrenergic agonists.

A
  • releasing agents
  • uptake inhibitor
  • MOA inhibitors
  • COMT inhibitors
28
Q

Describe the diseases that can be treated by direct-acting non-selective agonist: epinephrine.

A
  • heart problems: cardiac arrest, bradycardia
  • emergency treatment of allergic reactions by EpiPen
  • asthma: brochodilator
  • local anesthetics: prolong the action of the anesthetic agent
29
Q

Describe the diseases that can be treated by direct-acting non-selective agonist: norepinephrine.

A
  • hypotension
  • vasodilatory shock, such as septic shock and neurogenic shock
30
Q

Describe the diseases that can be treated by direct-acting non-selective agonist: Isoprenaline.

A
  • emergency for cardiac arrest, hypovolemic shock, septic shock
  • congestive heart failure
  • asthma
31
Q

Describe the diseases that can be treated by direct-acting selective a1 agonists: phenylephrine.

A

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
Q

Describe the diseases that can be treated from direct-acting selective a2 agonists: clonidine.

A

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
Q

Describe the diseases that can be treated from direct-acting selective b1 agonists: dobutamine.

A

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
Q

Describe the diseases that can be treated from direct-acting selective b2 agonists: albuterol.

A

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
Q

Describe the diseases that be treated by mixed-acting non-selective agonists: ephedrine.

A

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
Q

List the common adverse effects of adrenergic agonists.

A
  • arrhythmias
  • insomnia
  • headache
  • nausea
  • hyperactivity
  • tremors
37
Q

Name the three different types of adrenergic receptor antagonists.

A
  • a receptor antagonists
  • b receptor antagonists
  • a & b antagonists
38
Q

Name the three types of a-receptor antagonists.

A
  • nonselective
  • a1 selective
  • a2 selective
39
Q

Describe the diseases that can be treated from nonselective a receptor blocker: phenoxybenzamine.

A

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
Q

Describe the diseases that are able to be treated by selective a1 receptor blockers: prazosin.

A

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
Q

Explain the characteristics of adrenergic B receptor blockers.

A

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
Q

Explain the three different types of B-adrenergic receptor antagonists.

A

1st generation nonselective
2nd generation B1-selective
3rd generation vasodilatory
* nonselective
* B1-selective

43
Q

Explain the drug action mechanism of 1st generation B blockers: propranolol.

A

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
Q

Describe the diseases that can be treated from 1st generation B blockers: propranalol

A
  • hypertension
  • irregular heart rate
  • angina
  • anxiety
  • migraine
  • tremor
45
Q

Explain the drug action mechanism of 2nd generation B blockers: metoprolol.

A

Metoprolol is a selective B1 blocker
* blocks the action of epinephrine and norepinephrine at B1-adrenergic receptors

46
Q

Describe the diseases that can be treated from 2nd generation B blockers: metoprolol.

A
  • hypertension
  • tachycardia
  • angina
  • long QT syndrome
  • acute myocardial infarction
  • migraine
47
Q

Describe the characteristics of 3rd generatino B blockers

A
  • 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
Q
A

D. G-protein coupled receptor

49
Q

.

A

B. ISO > E > NE

50
Q
A

E. Decrease of cAMP and decrease of PKA

51
Q
A

A. a1

52
Q
A

E. None of the above is correct.

53
Q
A

B. Decrease sympathetic activity by decreasing NE release from post-ganglionic neurons

54
Q
A

C. a1 effect

55
Q

.

A

A. NE

56
Q
A

A. terozosin

57
Q
A

D. Propranolol has replaced pseudoephedrin as the most common otc decongestant

58
Q
A

A. B1 antagonist

59
Q
A

D. metoprolol

PHRX 3009: drug action (36 decks)

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