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STEP1 > ANS Drugs > Flashcards

ANS Drugs Flashcards

1
Q

What happens when a nicotinic receptor is activated?

A

there is an influx of positive ions, which depolarize the cell

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2
Q

Describe the distribution, second messenger system, and effects of M1, M2, and M3 receptors.

A
  • M1 are coupled to Gq and can be found in the CNS
  • M2 are coupled to Gi and can be found in the SA node, AV node, and atria to reduce heart rate, AV conduction velocity, and atrial inotropy
  • M3 are coupled to Gq and can be found in glands and smooth muscle where they mediate smooth muscle relaxation and gland activation
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3
Q

What effect does a low dose of IV cholinomimetic have? What is this effect dependent on?

A
  • the cholinomimetic will active M3 receptors on endothelial cells, triggering release of NO, which causes smooth muscle relaxation and vasodilation
  • this effect, then, is dependent on the presence of an intact endothelium
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4
Q

What is bethanochol?

A

a muscarinic agonist

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5
Q

What is pilocarpine?

A

a muscarinic agonist

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6
Q

What is varenicline?

A

a nicotinic agonist used for smoking cessation

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7
Q

What is carbachol?

A

a muscarinic and nicotinic agonist

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8
Q

What is methacholine?

A

a muscarinic agonist used as a “challenge” to test for asthma

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9
Q

What drugs end in the suffix “-stigmine”?

A

acetylcholinesterase inhibitors

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10
Q

What is the preferred treatment for myasthenia gravis?

A

pyridostigmine or neostigmine, long-acting acetylcholinesterase inhibitors that don’t penetrate the CNS

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11
Q

Describe the tensilon test.

A
  • a test used to determine whether an individual with myasthenia gravis is being over or under treated
  • when edrophonium is given, systems should improve if under treated and worsen if over treated
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12
Q

Why cholinesterase inhibitors don’t penetrate the CNS? Which do penetrate the CNS?

A
  • the quaternary amines neostigmine, pyridostigmine, and edrophonium don’t enter the CNS
  • the tertiary amines like physostigmine do
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13
Q

What is the mechanism of action of the curare drugs?

A

they are non-depolarizing NMJ blockers that directly inhibit nicotinic activity at the skeletal muscle end plate

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14
Q

What is succinylcholine used for?

A

it is a depolarizing NMJ blocker

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15
Q

How does succinylcholine compare to tubocurarine?

A

succinylcholine is a depolarizing NMJ blocker whereas tubocurarine is a non-depolarizing blocker, thus succinylcholine may cause an initial period of fasciculations and muscle soreness and can’t be readily reversed by acetylcholinesterase inhibitors

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16
Q

What is the preferred treatment for atropine poisoning?

A

physostigmine because it is an acetylcholinesterase inhibitor that penetrates the CNS

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17
Q

What are organophosphates?

A

acetylcholinesterase inhibitors that demonstrate aging

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18
Q

How is insecticide or organophosphate poisoning treated?

A
  • pralidoxime is used to regenerate acetylcholinesterase in the periphery but doesn’t penetrate the CNS
  • atropine is used to control the CNS effects
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19
Q

Name three acetylcholinesterase inhibitors used to treat Alzheimer’s disease.

A
  • galantamine
  • donepezil
  • rivastigmine
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20
Q

What is atropine?

A

a muscarinic antagonist

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21
Q

Which two plants are known to contain natural atropine?

A
  • atropa belladona (aka deadly nightshade)

- datura stramonium (aka jimsonweed)

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22
Q

What is scopolamine and it’s primary use?

A

a muscarinic antagonist used primarily for the treatment of motion sickness as a transdermal patch

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23
Q

What are ipratropium and tiotropium?

A

inhaled M3 antagonist used to reduce pulmonary secretions and bronchodilation in those with COPD

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24
Q

What are oxybutinin and tolterodine?

A

M3 antagonist with selectivity for receptors in the bladder and thus used to treat urgency incontinence

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25
Q

What are benztropine and trihexyphenidyl?

A

M1 antagonists used to treat the tremor and rigidity of Parkinson’s or the EPS effects of anti-psychotic medications

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26
Q

Describe the effects of activating a1 receptors, including the receptor cascade involved.

A
  • a1 receptor activation triggers a Gq cascade
  • this results in arterial and venous constriction
  • as well as mydriasis and sphincter contraction
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27
Q

Describe the effects of activating a2 receptors, including the receptor cascade involved.

A
  • a2 receptors are linked to a Gi cascade on presynaptic cells
  • activation inhibits insulin release, lipolysis and fat mobilization, and aqueous humor production
  • activation also inhibits neurotransmitter release
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28
Q

What is the effect of brimonidine?

A

it is an a2 receptor agonist used to reduce aqueous humor production for the treatment of chronic open angle glaucoma

29
Q

Describe the effects of activating B1 receptors, including the receptor cascade involved.

A
  • B1 receptors are linked to a Gs cascade
  • they are located on cardiac myocytes and JGA cells
  • activation leads to an increased heart rate, improved inotropy, and renin release
30
Q

Describe the effects of activating B2 receptors, including the receptor cascade involved.

A
  • B2 receptors are linked to a Gs cascade
  • activation leads to bronchodilation and vasodilation in the lungs and skeletal muscle as well as coronary dilation
  • activation also has many metabolic effects, stimulating gluconeogenesis, release of insulin, and lipolysis and fat mobilization
  • B2 receptor stimulation also induces greater aqueous humor production
31
Q

What is phenylephrine?

A

an a1 agonist, it is used as a nasal decongestant and can also be used to induce mydriasis

32
Q

What is the effect of phenylephrine, an a1 agonist, on a pressure curve?

A
  • because it constricts arteries and veins, it causes an increase in systolic, diastolic, and mean arterial pressure
  • it will, however, also induce a reflex bradycardia
33
Q

What is the selectivity of norepinephrine?

A

it has significant alpha activity and some B1 activity

34
Q

What is the effect of norepinephrine on a pressure curve?

A
  • it’s alpha activity causes arterial and venous constriction, raising systolic and diastolic pressure
  • it’s beta1 activity increases inotropy, widening pulse pressure
  • it induces a reflex bradycardia but increases systolic, diastolic, and mean arterial pressure
35
Q

What is the selectivity of dobutamine?

A

it has primarily beta1 activity and some beta2 activity

36
Q

Describe the effect of dobutamine on a pressure curve.

A
  • it has primarily beta1 activity but some beta2 activity
  • beta1 activity increases heart rate and inotropy, increasing systolic arterial pressure and widening pulse pressure
  • beta2 activity causes vasodilation and a drop in diastolic pressure
  • together, the mean arterial pressure remains relatively unchanged although the pulse pressure is widened
37
Q

What are the preferred treatments for distributive or hypovolemic shock and cardiogenic shock?

A
  • distributive or hypovolemic shock: a1 agonists

- cardiogenic: B1 agonists

38
Q

B2 agonists are useful in the treatment of what?

A

bronchoconstriction

39
Q

Describe the selectivity of isoproterenol.

A

it has equal B1 and B2 activity

40
Q

What is the effect of isoproterenol on a pressure curve?

A
  • it has equal B1 and B2 activity
  • in this case, the vasodilation caused by B2 outweighs the increase in heart rate and inotropy elicited by B1
  • the result is a drop in diastolic pressure, a drop in MAP, a widened pulse pressure, and relatively unchanged systolic pressure
41
Q

What is terbutaline?

A

a selective B2 agonist used to stop premature uterine contractions by relaxing smooth muscle

42
Q

What is ritodrine?

A

a selective B2 agonist used to stop premature uterine contractions by relaxing smooth muscle

43
Q

Describe the selectivity of epinephrine and it’s effect on a pressure curve.

A
  • at low dose, it has greater beta activity and at higher dose it has greater alpha activity
  • typically, it causes a rise in systolic pressure, a small drop in diastolic pressure
  • thus, it increases MAP and widens pulse pressure
44
Q

What is metyrosine?

A

a drug that blocks conversion of tyrosine to L-dopa and thus has a sympatholytic activity

45
Q

What is reserpine?

A

a drug that blocks the VMAT and packaging of catecholamines into synaptic vesicles, thus is has a sympatholytic activity

46
Q

What is atomoxetine?

A

an NET antagonist that maintains high synaptic levels of NE and is used to treat ADHD

47
Q

Describe the mechanism of action and effects of cocaine.

A
  • it blocks NET and DAT, keeping catecholamines in the synaptic cleft
  • in doing so it causes mydriasis, tachycardia, hypertension, and CNS arousal
  • long-term use is associated with atrophy of the nasal mucosa and septal perforation because it is vasoconstrictive
  • it’s vasoconstrictive activity can also lead to MI and angina
48
Q

Why should beta blockers never be used in those with cocaine in their system?

A

because it leads to unopposed alpha1 activity and hypertension

49
Q

How do amphetamines work?

A

they displace catecholamines from synaptic vesicles, releasing them into the synaptic cleft

50
Q

What is modafinil?

A

a stimulant used to treat narcolepsy

51
Q

What vascular effects do D1 receptors mediate?

A

activation of D1 with an agent like fenoldopam leads to widespread vasodilation which uniquely includes the renal vasculature and can be used in hypertensive emergency

52
Q

Dopamine agonists have what sympathetic activity?

A
  • at low dose, D1 agonists bind D1 receptors and cause widespread vasodilation including in the renal and coronary vasculature
  • at higher dose, they begin activating B1 receptors and stimulate the heart
  • at even higher doses, they being activating a1 receptors and have a vasopressor effect
53
Q

What is clonidine?

A
  • a centrally-acting a2 agonist
  • reduces sympathetic tone
  • useful in the treatment of hypertensive urgency, ADHD, and tourette’s syndrome
54
Q

What is a-methyldopa?

A
  • a centrally-acting a2 agonist
  • reduces sympathetic tone
  • useful in the treatment of gestational hypertension
  • may cause a lupus-like syndrome
55
Q

What is tizanidine?

A

an a2 agonist that is useful as a muscle relaxant

56
Q

What is phentolamine?

A
  • a reversible a1 and a2 antagonist
  • used in the treatment of cocaine-, tyramine-, and pheochromocytoma-induced hypertensive crisis
  • may cause orthostatic hypotension with reflex tachycardia
57
Q

What is phenoxybenzamine?

A
  • an irreversible a1 and a2 antagonist
  • used in the treatment of cocaine-, tyramine-, and pheochromocytoma-induced hypertensive crisis
  • may cause orthostatic hypotension with reflex tachycardia
58
Q

Which drugs end in the suffix “-osin”?

A

alpha1 antagonists (“o” for opera and “sin” for singer - phantom of the alpha)

59
Q

What is prazosin?

A
  • an alpha1 antagonist
  • used in the treatment of hypertension and PTSD
  • may cause orthostatic hypotension with reflex tachycardia
60
Q

What is mirtazapine?

A
  • an alpha2 agonist
  • used to treat depression because it disinhibits presynaptic neurons and increases release of norepinephrine and serotonin
61
Q

What is carvedilol?

A

a nonselective beta blocker that also has alpha1 antagonist activity

62
Q

What is labetolol?

A

a nonselective beta blocker that also has alpha1 antagonist activity

63
Q

Name two beta blockers with a1 antagonist activity as well.

A

carvedilol and labetolol

64
Q

Name five B1-selective blockers.

A

those that are in the first half of the alphabet (A-BEAM)

  • atenolol
  • betaxolol
  • esmolol
  • acebutolol
  • metoprolol
65
Q

Name two beta blockers with partial agonist activity.

A

acebutolol and pindolol

66
Q

How is beta-blocker over dose treated?

A

glucagon

67
Q

What are the clinical uses for beta-blockers.

A
  • treatment of hypertension and hypertensive crisis
  • treatment of MI, reducing mortality
  • management of chronic heart failure
  • treatment of arrhythmias
  • treatment of hypertrophic obstructive cardiomyopathy
  • treatment of thyroid storm
  • migraine prophylaxis
  • treatment of essential tremor
68
Q

What is labetolol?

A
  • a non-selective beta blocker with alpha1 antagonist effects
  • used for the treatment of gestational hypertension
  • available IV for the treatment of hypertensive crisis and aortic dissection
69
Q

Beta-blockers can exacerbate which two pre-existing conditions?

A

chronic pulmonary disease (COPD or asthma) and heart block

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