6 Autonomic Pharmacology Flashcards

1
Q

What are the general effects of sympathetic stimulation on the CVS through different receptors?

A

B1 - increased heart rate and contractility
regulation of renin release
B2 - some vasodilation
A1 + 2 - vasoconstriction

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2
Q

What does beta adrenoreceptor activation do to the heart?

A

+ chronotropic
+ inotropic
increased automaticity
lusitropic effect

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3
Q

What is a + chronotropic effect?

A

increased HR

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4
Q

What is a + inotropic effect?

A

increased contractility rate

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5
Q

What is the lusitropic effect?

A

fast relaxation and recovery

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6
Q

What intracellular pathways are associated with B1 activation?

A
increased Ca2+ entry
increased Ca2+ sensitivity
increased SR Ca2+ uptake
increased I(K) for faster repolarisation
increased Na+ / K+ ATPase activity
increased I(f)
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7
Q

What is the significance of an increased I(f) during B1 activation?

A

+ chronotropy

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8
Q

What is the significance of increased SR Ca2+ uptake?

A

lucitropic effect

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9
Q

Name 2 clinical agonists of B1

A

Adrenaline

Dobutamine

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10
Q

What is adrenaline used for?

A

asystole
anaphylaxis

when injected locally, causes vasoconstriction (commonly used with Lidocaine)

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11
Q

What is Dobutamine used for?

A

used to treat cardiogenic shock

usually only seen in ICU

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12
Q

What is the classical a1 adrenorecptor intracellular pathway?

A

IP3 mediated Ca2+ from SR

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13
Q

Name 2 a1 agonists used clinically

A

phenylephrine

midodrine

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14
Q

What is phenylephrine used for?

A

vasoconstrictant, nasal decongestant

is in Sudafed

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15
Q

What is midodrine used for?

A

venoconstriction (keeps up total peripheral resistance so blood is shunted centrally)

used for postural hypotension

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16
Q

What is postural hypotension treated with?

A

midodrine (venoconstriction)

fludocortisone (steroid, increases circulating volume)

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17
Q

What is Droxidopa?

A

prodrug for NAd

used for short term treatment of postural hypotension in autonomic failure

18
Q

Name 2 a2 agonists

A

Clonidine

Brimonidine

19
Q

What does Clonidine do?

A

alpha-2 agonist

centrally acting antihypertensives
decreases sympathetic drive

20
Q

What does Brimonidine do?

A

direct ranscutaneous vasoconstriction

for Rosacea

21
Q

Name 5 adrenoreceptor antagonists used clinically

A
Doxazosin (a1)
Beta Blockers
     propranalol (1, 2)
     metoprolol (1)
     atenolol (1)
Carvedilol (mixed)
22
Q

What does Doxazosin do?

What is it used for?

A

a1 antagonist
vasodilation

treats hypertension and Raynaud’s syndrome

23
Q

What is Raynaud’s syndrome?

A

limits circulation particularly in the hands and feet

24
Q

What 4 main things do beta blockers do?

A
  • chronotropy
  • inotropy
  • automaticity

anti-platelet aggregation

25
Q

What are beta blockers used to treat?

A

angina
heart failure
cardiac arrhythmias
hypertension

26
Q

What does Carvedilol do?

A
mixed B and A antagonist
inhibits cardiac K+ chanel, leading to a class III antiarrhythmic action

used for heart failure

27
Q

What is the implication of using Carvedilol to treat HF?

A

beat blockers themselves decrease cardiac workload
many with heart failure also have hypertension
so blocking alpha receptors peripherally, can cause BP to decrease

28
Q

What problem is associated with decreased cadiac output by beta blockers?

A

may lead to a ‘resetting of baroreceptors’

29
Q

What are the 3 effects of parasympathetic innervation of the heart?

A

Vagal rhythm
Negative chronotropy through SAN
Slow AVN conduction

little effect on myocardial contractility

30
Q

What is the intracellular mechanism associated with M2 receptors?

A

G(i), inhibits adenyl cyclase

31
Q

Name a muscarinic antagonist

A

atropine

32
Q

What effects does atropine have on the body?

A
decreased secretions
bronchodilation
constipation
urinary retention
pupillary dilation
confusion / hallucination
33
Q

According to the BNF, when is atropine used?

A

to reverse bradycardia

  • following MI w/ hypotension
  • XS beta blocker use
  • intra-operatively
34
Q

In what 2 ways can noradrenaline be taken in?

A

neuronal

non-neuronal

35
Q

What is neuronal uptake of NAd mediated by?

A

Noradrenaline Transporter

36
Q

Name 2 NAT blockers

A
cocaine
tricylic antidepressants (like imipramine)
37
Q

Name 2 monoamine oxidase inhibitors

A

phenelzine

iprozinad

38
Q

What is the MOA of Methyldopa?

A

DOPA decarboxylase inhibition

converted by dopamine beta hydroxylase to alpha methylnorepinephrine, an a2 agonist, dropping central sympathetic drive

39
Q

What is methyldopa used for?

A

treatment of hypertension in pregnancy

40
Q

Name 3 indirectly acting sympathomimetic amines

A

tyramine
ephedrine
emphetamine
(substrates for NAd transporter blocker)

41
Q

Where would you find tyramine?

A

cheese