CPTP 2.9 ANS 2 Flashcards

1
Q

What happens to adrenergic neurotransmitters after they are released?

A

The signal at the postjunctional effector site is rapidly terminated, because NE is either converted to inactive metabolites or is taken up by the neuron

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2
Q

Describe adrenergic receptor

A
  • Respond to epinephrine, NE and dopamine
  • Located in effector organs/ tissues of sympathetic system
  • G-protein coupled receptors
  • Slow (seconds) responses
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3
Q

Type of G-protein and its action in response to alpha 1 adrenoreceptor

A

Gq

Activates PLC

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4
Q

Type of G-protein and its action in response to alpha 2 adrenoreceptor

A

Gi

Inhibit adenylyl cyclase

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5
Q

Type of G-protein and its action in response to beta adrenoreceptors

A

Gs

Stimulate adenylyl cylase

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6
Q

What are the major effects mediated by A1 receptors?

A

PLC activated -> increased production of DAG and IP3 -> increase in calcium influx

  • vasoconstriction (major effect)
  • increased peripheral resistance
  • increased BP
  • relaxation of GI smooth muscle
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7
Q

What are the major effects mediated by A2 receptors?

A

inhibition of adenylyl cyclase -> decreased production of cAMP -> inhibition of further release of NE from the neuron

  • inhibition of NE release
  • inhibition of ACh release
  • inhibition of insulin release
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8
Q

What are the major effects mediated by B1 receptors?

A
  • increase HR (major effect)
  • increased myocardial contractility (major effect)
  • increased lipolysis
  • increased release of renin
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9
Q

What are the major effects mediated by B2 receptors?

A
  • bronchodilation (major effect)
  • vasodilation
  • decreased peripheral resistance
  • hepatic and muscle glycogeolysis
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10
Q

Which one has higher affinity to each adrenoreceptor, NE or E?

A

A1 - NE
A2 - E
B1 - NE
B2 - E

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11
Q

Name the agonists that tend to act on each adrenoreceptor

A

A1 - phenylephrine
A2 - clonidine
B1 - Dobutamine
B2 - Salbutamol

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12
Q

Therapeutic uses of sympathomimetics (adrenergic agonist)

  • cardiac arrest
  • cardiogenic shock
  • anaphylaxis
  • asthma
  • nasal decongestion
  • increase duration of action of local anaesthetic
  • premature labour
  • hypertension, migraine
A

cardiac arrest - epinephrine (IV)
cardiogenic shock - dobutamine to increase myocardial contractility
anaphylaxis - epinephrine for bronchodilation and vasodilation
asthma - salbutamol for bronchodilation
nasal decongestion - phenylephrine
increase duration of action of local anaesthetic - epinephrine
premature labour - salbutamol (B2 receptors present in wall of uterus)
hypertension, migraine - clonidine

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13
Q

Name the adrenergic antagonists that act on each adrenoreceptor

A

A1 - Phenoxybenzamine, Doxazosin
A2 - Phenoxybenzamine
B1 - Propranolol, Bisopraolol
B2 - Propranolol

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14
Q

Clinical uses of alpha adrenergic antagonist in hypertension

A

Hypertension - A1 antagonist doxazosin causes vasodilation

Phaeochromocytoma - nonselective alpha antagonist phenoxybenzamine causes irreversible blockade of adrenoreceptors

Benign prostatic hyper

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15
Q

Clinical uses of alpha adrenergic antagonist in phaeochromocytoma

A

non-selective alpha antagonist phenoxybenzamine causes irreversible blockade of adrenoreceptors

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16
Q

Clinical uses of alpha adrenergic antagonist in benign prostatic hypertrophy

A

A1 antagonists relax SM and inhibit hypertrophy

doxazosin (originally phenoxybenzamine)

17
Q

Are beta blockers competitive or noncompetitive?

A

Competitive

18
Q

What are non-selective beta blockers antagonists?

A

propranolol and timolol

19
Q

What are cardioselective beta antagonist and where do they primarily act on, B1 or B2?

A

bisoprolol and atenolol primarily block B1 receptors

20
Q

How are cardioselective B blockers used clinically?

A

Primarily used as anti-hypertensive drugs - CO and renin secretion reduced

At rest cause little change in HR, BP and CO but decrease effects of exercise

21
Q

How are nonselective B blockers used clinically?

A

Hyperthyroidism
propranolol
effective in blunting the widespread sympathetic stimulation that occurs in hyperthyroidism

Glaucoma
Timolol
reduce secretion of aqueous humor

22
Q

Use of B blockers to treat angina

A

propranolol and bisoprolol

decrease oxygen requirement of heart muscle therefore reduces chest pain on exertion

23
Q

Use of B blockers to treat MI

A

atenolol
has a protective effect on the myocardium.
Prophylactic and post MI use

24
Q

Side effects of non selective B blockers

A

fatigue
bronchoconstriction
sexual dysfunction
arrhythmias