B-antagonist lecture Flashcards

1
Q

activation of what increases body’s readiness for strenuous activity & stress? (“fight or flight)

A

sympathetic nervous system (SNS)

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2
Q

effects of SNS activation

A

> : arterial pressure, HR, cardiac output, blood flow to muscles & heart, RR, oxygen consumption, blood glucose, glycolosis, mental activity
<: blood flow to GIT & kidneys

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3
Q

main effectors of SNS

A

norepinephrine & epinephrine

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4
Q

Norepinephrine (NE)

A

synthesized in sympathic nerve terminals & CNS as a neurotransmitter

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5
Q

epinephrine (Epi)

A

synthesized in adrenal medula (Chomaffin cells) as a hormone & in CNS (adrenergic neurons) as a neurotransmitter

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6
Q

synthesis of NE & epi starts with

A

Tyrosine

Tyr-> DOPA->domapine->NE->epi

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7
Q

what happens to the release of NE when beta 2 is stimulated?

A

increase release of NE

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8
Q

what happens to the release of NE when alpha 2 is stimulated?

A

stop release of NE

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9
Q

where are alpha 1 receptors found?

A

post synaptic

blood vessels, skin, pulmonary, kidney

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10
Q

where are alpha 2 receptors found?

A

presynaptic

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11
Q

where are Beta1 receptors found?

A

myocardium, JG cells in kidneys

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12
Q

where are beta2 receptors found?

A
smooth muscles (can be pre & post-synaptic)
SMC of arteruikes, bronchial SMC, skeletal muscle, liver, ciliary muscle of eye
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13
Q

where are beta 3 receptors found?

A

adipose tissue -> lypolysis

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14
Q

what kind of receptors are adrenoceptors(Alpha & Beta)?

A

GPCRs

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15
Q

what is alpha 1 coupled to?

A

Gq-> >inositol triphosphate, DAG & Ca

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16
Q

what is alpha 2 coupled to?

A

Gi-> < adenylyl cyclase-> < cAMP

17
Q

what are all beta coupled to?

A

Gs-> >adenylyl cyclase-> . cAMP

18
Q

alpha 1 receptors cause

A

vasoconstriction

contribute to Na reabsorption

19
Q

beta 1 receptors cause

A

chrono-dromo-iono-tropic effects

stimulate renin releaase

20
Q

beta 2 receptors cause

A

vasodilation, bronchodilation, > secretion, glycogenolysis & gluconeogenesis
in the eye-> relxation & > intraocular pressure

21
Q

1st generation beta blockers are

A

non-selctive B1 & B2 antagonists

22
Q

2nd generation beta blockers are

A

selective B1 antagonists

23
Q

3rd generation beta blockers are

A

non-selective & selective antagonists with additional effects

24
Q

beta blocker effect on normal HR or BP at rest

A

little effect; profound effect when SNS is high (HTN, stress, exercise)

25
Q

short term effect of non-selective B-blockers

A

< CO-> sympathetic activation-> > NE/Epi->activation of alpha receptors in vessels-> > PR ( B2 is blocked so no vasodilation)

26
Q

long term effect of non-selective B-blockers

A

PR returns to initial value & CO continues to lower

27
Q

reduction in BP in HTN with beta-blockers due to

A
  • reduction of cardiac output (B1)
  • inhibition of renin release from JG cells (B1)
  • from B2- < NE
  • w/ selective Beta-1-> vasodilation through B2
28
Q

beta-blockers commonly used in the treatment of

A

HTN, angina, cardiac arrhythmias, MI, glaucoma, migraine prophylaxis

29
Q

intrinsic sympathomimetic activity

A

partial agonist

some beta-blockers bind to receptors but can also slightly stimulate them

30
Q

beta-blocker structures are all derived from

A

NE & Epi structure

31
Q

main adverse cardio effects of beta-blockers

A

induce or worsen HF, induce arrhythmias in pts with AV conduction defects, worsen peripheral vascular disease, may cause sexual dysfunction

32
Q

abrupt discontinuation of beta-blockers can cuase

A

angina pectoris (myocadial ischemia) & increase risk of death

33
Q

main adverse pulmonary effects of beta-blockers

A

may worsen asthma or COPD

bronchospasm

34
Q

main adverse CNS effects

A

sedation. sleep disturbances & depression

35
Q

main adverse metabolic & endocrine effects

A

mask hypoglycemia-induced tachycardia in DM, may increase TG since lipolysis is inhibited

36
Q
  • chronotropic effect
A

decreased HR

37
Q
  • ionotropic effect
A

decreased contraction force-> decreased CO

38
Q
  • dromotropic effect
A

decreased cardiac rhythm & automaticity