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CPR- my cards > Autonomic NS Drugs > Flashcards

Autonomic NS Drugs Flashcards

1
Q

Nicotinic ACh receptors

A

Na+/K+ channels
N(n) - autonomic ganglia
N(m) - neuromuscular juctions

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2
Q

Muscarinic ACh receptors

A

G protein coupled receptors that act through 2nd messengers

M1, M2, M3, M4, M5

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3
Q

affinities of alpha-1 and alpha-2 receptors

A

EPI >= NE&raquo_space;> I

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4
Q

Alpha-1 receptor:

A

G(q) protein coupled receptor:

  • activates phospholipase C, increases IP3, mobilizes intracellular stores of Ca
  • increases diacylglycerol (DAG)
  • activates PKC
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5
Q

Alpha-2 receptors:

A

G(i) coupled receptor:
- activate guanine nucleotide inhibitors, inhibit adenylyl cyclase, decrease cAMP levels, lower PKA, lower intracellular Ca/increased myosin light-chain kinase (smooth muscle relaxation)

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6
Q

beta-1 receptor:

A

G(s) coupled receptor:
- stimulates adenylate cyclase activity, increased cAMP, increased PKA, increased intracellular Ca/decreased myosin light-chain kinase (smooth muscle)
OPENS L-TYPE Ca CHANNELS

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7
Q

beta-2 receptor

A

G(s) coupled receptor:
- stimulates adenylyl cyclase, increase cAMP, increase PKA, increased Ca/decreased myosin light chain kinase (smooth muscle)

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8
Q

Location of alpha-1 receptors and function

A
  • blood vessels: vasoconstriction
  • GI tract/urinary sphincters: contraction
  • radial muscles of iris: contraction (mydriasis-dilation)
  • liver: gluconeogenesis, glycogenolysis
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9
Q

Locations and functions of Alpha-2 receptors

A
  • presynaptic neuron: inhibit NE release
  • postsynaptic neuron: inhibit NE uptake
  • pancreas: decrease insulin release
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10
Q

Location and function of Beta-1 receptors

A 
Heart: 
- increase conduction velocity (heart rate)
- increase automaticity
- increase contractility
- increase renin release
Kidney: increase renin secretion
Fat: lipolysis
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11
Q

Location and function of Beta-2 receptors

A 
Blood vessels: vasodilation
Bronchioles: dilation
GI tract/bladder: decrease motility
Uterus: relaxation
Liver: gluconeogenesis, glycogenolysis
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12
Q

Epinephrine selectivity for adrenergic receptors

A 
STIMULATES ALL ADRENERGIC RECEPTORS
alpha-1
alpha-2
beta-1
beta-2
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13
Q

Isoproterenol selectivity for adrenergic receptors

A

BETA MOSTLY
beta-1
beta-2
(very little effect on alpha-1/alpha-2)

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14
Q

Norepinephrine selectivity for adrenergic receptors

A

alpha-1
alpha-2
beta-1
NO EFFECT ON BETA-2

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15
Q

Dopamine selectivity for adrenergic receptors

A

low dose: D1
med dose: Beta-1
high dose: alpha-1 receptors

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16
Q

Epinephrine effects on heart

A

(Beta-1): increase automaticity, conduction velocity, HR, contractile force, cardiac ouput (CO), O2 consumption

  • accelerates phase 4 diastolic depolarization in Purkinje fibers, activates latent pacemaker cells (may cause arrhythmias)
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17
Q

EPI effects on peripheral resistance

A

(alpha-1): increases cutaneous, mesenteric, renal vascular resistance

low EPI: (beta-2) decreases skeletal muscle resistance
high EPI: (alpha-1) increases skeletal muscle resistance

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18
Q

Vagal escape

A

When increased parasympathetic stimulation (vagus nerve) is overcome by sympathetic release of NE on heart. Results in increased HR

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19
Q

NE effects on the heart

A

chronotropic- increase HR
ionotropic- increase contractility
increase conduction speed in AV node (shorter P-R interval)

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20
Q

Effects of ACh on the cardiovascular system (4)

A

1) vasodilation
2) decrease HR (negative chronotropy)
3) decrease conduction velocity through SA and AV nodes (negative dromotropy)
4) decrease force of contraction (negative ionotropy)

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21
Q

Effect of M3 receptor stimulation

A

Muscarinic receoptors on endothelial cells
- respond to ACh
- produce NO –> guanylate cyclase activity increases –> more cGMP produced
END RESULT: smooth muscle relaxation/vasodilation

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22
Q

Effect of M2 receptor stimulation

A

decrease in HR (often overridden by baroreceptor reflex)

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23
Q

Baroreceptor Reflex

A

drop in BP at carotid sinus stimulates sympathetic release of NE

  • alpha-1: vasoconstriction
  • beta-1: increase HR
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24
Q

Effects of carotid occlusion

A

Decreased BP sensed at carotid sinus:

  • stimulates sympathetic NE release, decreases parasympathetic vagal stimulation
  • HR and BP increase
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25
Q

What does hexamethonium do?

A

Antagonist of ACh at preganglionic synapse

affects nACHRn > nACHRm

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26
Q

Atropine

A

Competitive inhibitor of ACh at all M receptors (blocks Parasympathetic relaxation)

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27
Q

Cholinergic Drugs are:

A

Paraympathomimetic Drugs
(mimic effects of ACh)
- act on Muscarinic receptors
ex: Bethanechol, carbachol, pilocarpine

28
Q

Anticholinergic Drugs are:

A

Parasympatholytic/Antimuscarinic Drugs

antagonists of ACh

29
Q

Muscarinic receptors:

  • are activated by what?
  • are blocked by what?
A

Activated: ACh, Muscarine

Blocked: Atropine, Scopolamine

30
Q

Where are M1 receptors found?

What do they do?

A

sympathetic postganglionic neurons, and CNS neurons
- G(q) coupled receptor: activates PLC, increases IP3, DAG
(IP3–> increased release of Ca++ from ER/SR)
(DAG –> activates PKC –> increased influx of extracelluar Ca++)

31
Q

M2 receptors

  • where are they?
  • what do they do?
A

presynaptic: cardiac and smooth muscle

- G(i/o) coupled receptor: inhibit adenylyl cyclase (decreased cAMP), open K+ channels (promote hyperpolarization)

32
Q

M3 receptors

  • where are they?
  • what do they do?
A

exocrine glands, blood vessel endothelium, smooth muscle and ganglia
- G(q) coupled receptor: activates PLC, increases IP3, DAG
- endothelial cells: activates NOS –> NO diffuses to smooth muscle –> activates guanyl cyclase –> increased cGMP –> muscle relaxation
(IP3–> increased release of Ca++ from ER/SR)
(DAG –> activates PKC –> increased influx of extracelluar Ca++)

33
Q

M4 receptors

  • where are they?
  • what do they do?
A

Post ganglionic nerve terminals in brain
- work like M2 receptors
(inhibit adenylyl cyclase, increase K+ channels)

34
Q

M5 receptors

  • where are they?
  • what do they do?
A

dopamine neurons in brain
- like M1/M3
(activate PLC –> IP3, DAG)

35
Q

Choline ester cholinergic agonists

A

Bethanechol

  • ACh (hydrolyzed too quickly by AChesterase to be used clinically)
  • Carbachol (not used clinically)
  • Metacholine (not used clinically)
36
Q

Bethanechol

A
  • slowly hydrolyed
  • specific to muscarinic receptors (agonist)
  • treatment for post-op urinary retention, abdominal distension, gastric atony (increase GI motility, decrease sphincter tone)
37
Q

Natural Alkaloid cholinergic agonists

A

Pilocarpine

-Muscarine (not used clinically)

38
Q

Pilocarpine

A

Muscarinic receptor agonist

  • treat glaucoma: decreases intraoccular pressure
  • treat Sjogren syndrome: increase salivary secretion
39
Q

Effect of M receptors on heart

A

Decrease HR, but resulting decrease in BP may produce reflex increase in HR by sympathetic system

40
Q

Effect of M receptors on blood vessels

A

M3: decrease tone in arterioles and small blood vessels (due to NO)
- decrease BP

41
Q

Effect of M receptors on smooth muscle (other than blood vessels)

A

increase tone

increase contraction

42
Q

Effect of M receptors on Exocrine glands

A

increased salivation, mucous secretion

43
Q

Effect of M receptors on GI tract

A

increase tone, contractions, peristalsis

44
Q

Effect of M receptors on bronchioles

A

Bronchoconstriction

45
Q

Effect of M receptors on bladder

A

decreased bladder capacity

46
Q

Tertiary Amine Anticholinergics

  • what do they do?
  • list some examples
A

inhibit action of PNS and muscarinic agonists on end receptors
EFFECT CNS

  • *atropine**
  • scopolamine
  • homatropine
  • benztropine
  • oxybutynin, tolterodine
  • pirenzipine
47
Q

Atropine

A

Competitive antagonist to Muscarinic receptor

- long half-life

48
Q

Scopalamine uses

A

motion sickness

sedation

49
Q

Homatropine uses

A

ophthamolagy: mydriasis and cycloplegia

- reduces smooth muscle tone

50
Q

benztropine uses

A

Parkinson disease

51
Q

pirenzipine uses

A

M1 selective: reduce secretions

  • antidepressant
  • reduces stomach acid (peptic ulcers)
52
Q

oxybutynin uses

A

urinary incontinence

53
Q

Quaternary amine Anticholinergic Drugs

  • what do they do?
  • list some examples
A

inhibit action of PNS and muscarinic agonists on end receptors
DO NOT ENTER CNS
- ipratropium, tiotropium
- glycopyrrolate

54
Q

Ipratropium uses

A

asthma

- reduce bronchoconstriction

55
Q

Tiotropium uses

A

asthma (M1, M3 selective), longer duration of action than Ipratropium
- reduce bronchoconstriction

56
Q

Glycopyrrolate uses

A

Pre-anasthetic

57
Q

Atropine sensitivities in the body

A

lowest dose: secretory < eye and heart < GI/urinary motility < GI secretion < CNS: highest dose

58
Q

Symptoms of Atropine toxicity

A
  • elevated temperature
  • dry skin, eyes
  • hallucinations/delirium
  • mydriasis, cycloplegia
  • tachycardia
59
Q

Dopamine selectivity for adrenergic receptors

A

D 1
D 2
Beta-1
(Alpha receptors only at high concentrations)

60
Q

Receptors located on blood vessels

A

Alpha-1: skin/systemic, constriction
Beta-2: skeletal muscle/liver, dilation
D-1: kidney/mesentary, dilation

61
Q

Receptors of the GI tract

A

Alpha-1: sphincters, contraction

Beta-2: tract, relaxation

62
Q

How do alpha-1 receptors instigate contraction?

A

G(q) coupled receptor: increase phospholipase C, increases IP3, increases Ca++ release from SR = CONTRACTION

63
Q

How do alpha-2 receptors instigate relaxation?

A

G(i) coupled receptor: decrease adenylyl cyclase activity, opens K+channels, promotes hyperpolarization = RELAXATION

G(o) coupled receptor: closes Ca++ channels, less able to contract = RELAXATION

64
Q

How do beta-1 receptors instigate contraction?

A

G(s) coupled receptor: increase adenylyl cyclase activity, increase opening of L-type Ca++, more Ca++ release from SR = CONTRACTION

65
Q

How does beta-2 receptor instigate relaxation?

A

G(s) coupled receptor: increased adenylyl cyclase activity, increased cAMP, more PKA, phosphatase activated, dephosphorylation leads actin and myosin to slide apart

CPR- my cards (4 decks)

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