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Clinical Pharmacology 2 > Autonomic nervous system > Flashcards

Autonomic nervous system Flashcards

1
Q

What is the study of drugs that influence the ANS which controls involuntary physiological functions like heart rate, digestion, and RR?

A

autonomic pharmacology

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2
Q

What does the ANS control that drugs target?

A

cardiovascular, resp, GI, other systemic disorders

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3
Q

What does the sympathetic nervous system do to the eyes?

A

contracts radial muscle to dilate the eye (mydriasis)

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4
Q

What does the parasympathetic nervous system do to the eyes?

A

contraction of the circular muscle to constrict the eye (miosis)

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5
Q

How are nore/epi terminated?

A

reuptake, inactivated by COMT or MAO-Is

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6
Q

Review: receptors

A

sympathetic - adrenergic
parasympathetic - muscarinic, nicotinic

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7
Q

What does muscarinic M1 act on?

A

CNS neurons; sympathetic postganglionic neurons

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8
Q

What does muscarinic M2 act on?

A

myocardium, smooth muscle, CNS neurons

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9
Q

What does muscarinic M3 act on?

A

exocrine gland, vessels, CNS neurons

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10
Q

What does muscarinic M4 act on?

A

CNS neurons (cholinergic)

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11
Q

What does muscarinic M5 act on?

A

vascular endothelium, CNS neurons (cholinergic)

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12
Q

What does alpha 1 work on?

A

vascular smooth muscle (cholinergic)

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13
Q

What does alpha 2 work on?

A

presynaptic adrenergic nerve terminals (cholinergic)

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14
Q

What does beta 1 work on?

A

heart (cholinergic)

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15
Q

What does beta 2 work on?

A

vascular smooth muscle and cardiac muscle (cholinergic)

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16
Q

What does beta 3 work on?

A

lipocytes and bladder (cholinergic)

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17
Q

What are cholinergic agonists?

A

parasympathetiomimetics –> mimic effects of PNS

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18
Q

What type of drug is bethanechol, pilocarpine?

A

cholinergic agonists

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19
Q

What are cholinergic antagonists/anticholinergic drugs?

A

parasympatholytics –> block effects of PNS

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20
Q

What type of drug is atropine, scopolamine?

A

cholinergic antagonists

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21
Q

What are adrenergic agonists?

A

sympathomimetics –> mimic effect of SNS

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22
Q

What type of drugs are epinephrine, norepinephrine, albuterol?

A

adrenergic agonists

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23
Q

What are adrenergic antagonists?

A

sympatholytics –> blocking effect of SNS

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24
Q

What type of drugs are beta blockers and alpha blockers?

A

adrenergic antagonists

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25
Q

What’s the MOA of cholinergic agonists?

A

stimulate cholinergic receptors, mimicking PS effects

can be direct (at a muscarinic or nicotinic receptor)

or indirect (block metabolism of acetycholine and increase concentration)

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26
Q

What would these effects be from?
- miosis
- decreased heart rate
- bronchoconstriction/increased secretions
- increased GI motility and sphincter relaxation
- bladder wall contraction and sphincter relaxation
- increased sweat secretion?

A

cholinergic agonists

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27
Q

What are these drugs an example of?
esters -> bethanechol
alkaloids (pilocarpine, muscarine, nicotine)?

A

direct muscarinic agonists

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28
Q

What can bethanechol be used for?

A

urinary retention –> increased bladder contraction, non-obstructive post-op ileus

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29
Q

What can alkaloids be used to treat?

A

acute-angle closure glaucoma

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30
Q

What can pilocarpine and nicotine cause (separate effects)?

A

pilocarpine - stimulates salvation, used in dry mouth (xerostomia)
nicotine - stimulates nicotinic receptors, increasing HR and BP

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31
Q

What are contraindications for direct muscarinic agonists?

A

asthma, GI obstruction, PUD, pronounced bradycardia, HOTN

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32
Q

What MOA are these drugs:
- neostigmine
-pyridostigmine
-donepezil
-galantamine
-rivastigmine

A

reversible cholinesterase inhibitors (compete w Ach for a site on the enzyme)

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33
Q

What MOA are these drugs:
- malthion
- parathion
-sarin
-insecticides/nerve gas
-phosphorylate AchE and inactivate
-highly lipophilic

A

irreversible cholinesterase inhibitors (phosphorylate AchE and inactivate it)

34
Q

What are clinical uses for cholinesterase inhibitors?

A

Myasthenia gravis, Alzheimer’s disease, open angle glaucoma, reversal of neuromuscular blockade after surgery

35
Q

What are adverse effects of cholinesterase inhibitors?

A

SLUDGEM + low HR and bronchorrhea
Salivating/sweating
Lacrimation
Urination
Diarrhea
GI upset
Emesis
Miosis

36
Q

What is toxicity from cholinesterase inhibitors from?

A

organophosphate/pesticide exposure, nerve agents which can lead to AMS, coma, seizures

treat w/ atropine and pralidoxime, benzos for seizures

37
Q

What’s the MOA of cholinergic antagonists?

A

block cholinergic receptors, reducing PNS effects , competing for binding with Ach on muscarinic receptor

38
Q

What are these effects from:
- mydriasis
- high HR
- bronchodilation, less secretion
- reduced motility
- urinary retention
- decreased secretions of glands
- potentially drowsiness, hallucinations, coma?

A

cholinergic antagonists/anticholinergics

39
Q

What can you use atropine for?

A

anticholinergic = reversal agent, pre-op for drying secretions

40
Q

What can you use scopolamine for?

A

anticholinergic = motion sickness, drying secretions

41
Q

What can you use dicyclomine (bentyl) for?

A

anticholinergic = GI antispasmodic (IBS)

42
Q

What can you use oxybutynin (ditropan XL) for?

A

anticholinergic = urinary frequency, urgency, incontinence

43
Q

What can you use benztropine (cogentin) for?

A

anticholinergic = drug induced extra pyramidal symptoms; parkinsonism

44
Q

What can you use glycopyrrolate for?

A

anticholinergic = reduction of secretions (death rattle), PUD

45
Q

What can you use trihexyphenidyl for?

A

anticholinergic = drug-induced extra pyramidal symptoms; parkinsonism

46
Q

What can you use trotropium (spirivia) / ipatropium (nasal) for?

A

anticholinergic = COPD

47
Q

What anticholinergics are muscarinic antagonists?

A

atropine (increases HR) and scopolamine (used for N/V)

48
Q

What anticholinergics are nicotinic antagonists?

A

curare (muscle relaxant by blocking nicotonic receptors at neuromuscular junctions)

49
Q

What typical antipsychotics are anticholinergics?

A

haloperidol (haldol)

50
Q

What antidepressants are anticholinergics?

A

amitriptyline (TCAs)

51
Q

What are ADRs of anticholinergics?

A

ANTI-SLUDGE (opp of salivation/sweating, lacirmation, urination, defecation, GI upset, emesis, +CNS effects)
ABCDs
Agitation
Blurred vision
Constipation/confusion
Dry mouth
Stasis of urine

52
Q

What are anticholinergic contraindications?

A

untreated narrow angle glaucoma, GI obstruction or constipation, bladder obstruction, BPH

53
Q

What is characterized by psychosis/delirium, hot/flushed skin, dry mucous membranes, constipation, urinary retention, pupil dilation, inability to focus close, hyperthermia?

A

anticholinergic syndrome

reverse w/ physostigmine

54
Q

What do anticholinergic NMBs do?

A

bind to all nicotinic receptors (at junction, autonomic ganglia –> muscle relaxation)

depolarizing binds to receptor, opening channel (succinylcholine)
non depolarizing = binds to receptor does NOT open channel (rocuronium, vecuronium)

55
Q

What is the adrenergic agonists MOA?

A

stimulate adrenergic receptors
a1 = vasoconstriction, GI/urinary sphincter
a2 = lower BP/lowers sympathetic nervous system
b1=high HR and CO
b2 = bronchodilation, vasodilation, relax of bladder muscle, low GI motility

56
Q

What’s a direct alpha 1 agonist?

A

phenylephrine (decongestant) and can be used in HOTN to increase BP

57
Q

What’s a direct alpha 2 agonist?

A

clonidine for HTN

58
Q

What’s a direct beta 1 agonist?

A

dobutamine for CHF (increase contractility)

59
Q

What’s a direct beta 2 agonist?

A

albuterol for bronchodilation, asthma

60
Q

What are alpha and beta agonists?

A

epinephrine and norepinephrine for vasopressors, epi for anaphylaxis

61
Q

How do indirect acting adrenergic agonists work?

A

release previously stored norepinephrine into synapse
amphetamines + derivatives

tx ADHD and narcolepsy
CII meds
pseudophedrine also related to this

62
Q

What are ADRs of adrenergic agonists?

A

hypertension, tachycardia, increased risk for stroke/HA, arrythmia, mydriasis/photophobia

63
Q

What are contraindications for adrenergic agonists?

A

within 14 days of MAO-I
CV disease
increased IOP
BPH
seizure disorder
thyroid dysfunction

64
Q

What is the MOA of adrenergic antagonists?

A

block SNS - alpha and beta blockers

65
Q

How are central alpha 2 agonists used as adrenergic antagonists?

A

create a negative feedback loop and inhibit sympathetic output from brain and release of norepi from nerve terminals!

66
Q

What are examples of central alpha 2 agonists used as adrenergic antagonists?

A

clonidine, methyldopa, guanfacine, tizanidine

67
Q

What’s the MOA of alpha 1 blockers?

A

blockade that will produce vasodilation
more effective when it is “Firing” (i.e. when someone is standing –> postural hypotension or first dose syncope)
can also get reflex tachycardia

68
Q

What are examples of alpha-1 blockers?

A

prazosin (HTN and BPH), doxazosin, terazosin for BPH and HTN

69
Q

What are some more selective alpha-1 blockers for 1a receptor in GI tract?

A

tamsulosin = flomax (kidney stone) also for BPH
can cause lower ejaculation, or absent/retrograde

70
Q

What are clinical uses for beta blockers?

A

cardiac arrythmias (atrial fibrillation)
HTN
angina
HF
hyperthyroidism
migraines

71
Q

What are examples of cardioselective beta blockers?

A

acebutolol, atenolol, bisoprolol, esmolol, metoprolol

72
Q

What are examples of nonselective beta blockers?

A

propranolol, nadolol, penbutolol, pindolol, timolol

73
Q

What are ADRs of beta blockers?

A

decreased BP, HR, CO, fatigue, bronchoconstriction, block the effects of hypoglycemia (prevents response), heart block, ED, depression

74
Q

What type of drug is labetalol, carvedilol?

A

mixed alpha/beta blockers, used often similar to beta blockers for HTN and heart failure

labetalol for pregnancy

75
Q

What of these drugs would you use for HTN?

A

alpha blockers (prazosin)
beta blockers (atenolol)
alpha 2 agonists (clonidine)

76
Q

What of these drugs would you use for asthma/COPD?

A

beta-2 agonists (albuterol), anticholinergics (ipratropium)

77
Q

What of these drugs would you use for heart failure?

A

beta blockers (carvedilol), ACE inhibitors

78
Q

What of these drugs would you use for glaucoma?

A

muscarinic agonists (pilocarpine)

79
Q

What of these drugs would you use for motion sickness?

A

muscarinic antagonists (scopolamine)

80
Q

How can you treat parkinson’s?

A

anticholinergics (benztropine) to manage tremors and rigidity

81
Q

How can you treat alzheimers?

A

acetylcholinesterase inhibitors (donepezil) to increase Ach

82
Q

How can you treat overactive bladder?

A

anticholinergics (oxybutynin) to reduce bladder spasms

Clinical Pharmacology 2 (4 decks)

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