Autonomic Pharmacology Flashcards

1
Q

AA origin of NE, epi

A

tyrosine –> L-DOPA –> DA –> NE –> Epi

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2
Q

AA origin of 5-HT

A

tryptophan

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3
Q

AA origin of histamine

A

histidine

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4
Q

AA origin of NO

A

arginine

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5
Q

1st order neuron of ANS uses ____ on _____ receptor.

A

ACh, Nn

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6
Q

2nd order neurons of ANS in PSNS use _____ on _____ receptor.

A

ACh, M

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7
Q

2nd order neurons of ANS in SNS use _____ on ______ receptors.

A
  • ACh, M (sweat glands)
  • NE, a/B (most)
  • DA, D1 (kidneys)
  • epi from adrenal medulla acting diffusely
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8
Q

NMJ uses ____ on ____ receptors.

A

ACh, Nm

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9
Q

Removal of ACh from the synapse occurs by:

A

AChesterase, acetate (diffuses away) + choline (recycled)

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10
Q

NE degraded by ____ vs epi degraded by:

A

reuptake, MAO/COMT (epi is more processed so requires more enzyme for uptake)

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11
Q

GPCR receptor types

A
  • a1 - Gq
  • a2 - Gi
  • B1 - Gs
  • B2 - Gs
  • M1 - Gq
  • M2 - Gi
  • M3 - Gq
  • D1 - Gs
  • D2 - Gi
  • H1 - Gq
  • H2 - Gs
  • V1 - Gq
  • V2 - Gs

“qiss and qiq til you’re siq of sqs”

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12
Q

a1 receptor roles:

A
  • Gq
  • vasoconstriction
  • mydriasis
  • intestinal/bladder sphincter contraction
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13
Q

a2 receptor roles:

A
  • Gi
  • decreased SNS
  • decreased insulin release from B cells and lipolysis from adipocytes
  • decreased production of aqueous humor
  • increased platelet aggregation
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14
Q

B1 receptor roles:

A
  • Gs
  • increase in heart rate and contractility
  • increase in renin release from in cells
  • increased lipolysis
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15
Q

B2 receptor roles:

A
  • Gs
  • vasodilation
  • bronchodilation
  • increased lipolysis and insulin release from B cells
  • decreased uterine/bladder tone
  • ciliary muscle relaxation (opposite of accommodation)
  • increased aqueous humor production
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16
Q

M2 receptor roles:

A
  • Gi
  • decreased heart rate and contractility
  • relaxation of internal sphincter
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17
Q

M3 receptor roles:

A
  • Gq
  • increased exocrine gland secretions
  • increased gut peristalsis
  • bladder contraction
  • bronchoconstriction
  • miosis
  • accommodation (contraction of ciliary muscle)
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18
Q

D1 receptor roles:

A
  • Gs

- relaxes renal vascular smooth muscle

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19
Q

H1 receptor roles:

A
  • Gq
  • increased nasal/bronchial mucus production
  • increased vascular permeability
  • contraction of bronchioles
  • pruritus
  • pain
  • constricts the venules causing edema
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20
Q

H2 receptor roles:

A
  • Gs

- gastric acid secretion

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21
Q

V1 receptor roles:

A
  • Gq

- vascular smooth muscle contraction

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22
Q

V2 receptor roles:

A
  • Gs

- increased H2O permeability and reabsorption in collectube duct of nephron via AQ2 channels

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23
Q

bethanechol

A
  • cholinergic agonist resistant to AChesterase

- postop ileus, neurogenic ileus, urinary retention, xerostomia

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24
Q

carbachol

A
  • cholinergic agonist resistant to AChesterase

- causes miosis and decrease in IOP

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25
Q

methacholine

A
  • cholinergic agonist with very short t 1/2

- dx of asthma

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26
Q

pilocarpine

A
  • cholinergic agonist resistant to AChesterase
  • stimulates sweat, tears, saliva and treats open and closed angle glaucoma

“cry, drool, and sweat on my pillow”

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27
Q

galantamine, rivastigmine, donepezil

A

AChesterase inh specific to CNS used to boost ACh for memory consolidation in Alzheimer dz

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28
Q

edrophonium

A

AChesterase inh used to test for myasthenia gravis

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29
Q

neostigmine

A

AChesterase inh used for ileus, urinary retention, reversal of NMJ blockade

“NeO CNS penetration”

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30
Q

physostigmine

A

AChesterase inh that can cross BBB and thus used to treat anticholinergic toxicity

“phyxes atropine OD”

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31
Q

pyridostigmine

A

AChesterase inh. used for myasthenia gravis

“get RID of myasthenia gravis”

32
Q

organophosphate

A
  • irreversible AChesterase inh
  • DUMBBELSS - diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of NMJ, lacrimation, sweating, salivation
  • also nausea and vomiting
33
Q

atropine

A

muscarinic antagonist, eye/heart

34
Q

benztropine

A

muscarinic antagonist, CNS (Parkinson’s)

35
Q

glycopyrrolate

A

muscarinic antagonist, GI/resp

36
Q

-tropium

A

muscarinic antagonist, bronchi (bronchodilation)

37
Q

oxybutynin

A

muscarinic antagonist, GI (overactive bladder)

38
Q

scopolamine

A

muscarinic antagonist, motion sickness

39
Q

succinylcholine

A
  • depolarizing Nm antagonist –> paralysis

- very short half life

40
Q

“-cur-“ drugs

A
  • non-depolarizing Nm antagonist –> paralysis

- long half life –> need AChesterase inh + muscarinic antagonist to bring them off after surgery

41
Q

malignant hyperthermia

A
  • AD genetic disorder
  • hyperthermia + hyperkalemia in response to inhaled anesthetics and succinylcholine releasing Ca 2+ from sarcoplasmic reticulum which activates ATPase to produce heat
  • treat with dantrolene (prevents Ca 2+ release from sarcoplasmic reticulum)
42
Q

-terol drugs

A

B2 > B1 agonists (works in smaller, more peripheral airways)

43
Q

dobutamine

A

B1 > B2 agonist used for HF and cardiac stress testing as well as cardiogenic shock

44
Q

dopamine

A

D > B > a agonist depending on dose used to preserve blood flow to kidneys and vital organs during shock

45
Q

epinephrine

A
  • B1,2 > a1,2 agonist used for anaphylaxis and asthma
  • increase in SBP (a1) but decrease in DBP (B2) so MAP remains the same –> used with local anesthetics for vasoconstriction since it won’t raise BP
46
Q

isoproterenol

A
  • B1,2 agonist

- SBP only slightly increases, but DBP drops significantly so MAP decreases

47
Q

norepinephrine

A
  • a1 > a2 > B1 agonist used for hypotension
  • SBP increased significantly, DBP unchanged so MAP increases
  • can cause reflex bradycardia
48
Q

phenylephrine

A
  • a1 > a2 agonist

- used for hypotension, rhinitis (decongestant), priapism

49
Q

amphetamine (Adderall)

A
  • displaces NE/DA in vessicles
  • partial adrenergic agonist
  • blocks catecholamine re-uptake transporters
  • used for narcolepsy and ADHD
50
Q

cocaine

A
  • inhibits DRTs causing vasoconstriction

- never give B blockers if cocaine use is suspected (unopposed a1)

51
Q

ephedrine

A
  • displaces NE in vessicles
  • partial adrenergic agonist
  • used for nasal congestion, urinary incontinence, hypotension
52
Q

ritodrine

A

B2 agonist used to relax uterus and prevent premature delivery

53
Q

methylphenidate (Ritalin)

A
  • DRT, NERT in RAS

- first-line ADHD treatment

54
Q

What should people on MAO inhibitors avoid?

A

consuming tyramine (in fermented foods/beverages)

55
Q

NE will casue reflex ____.

A

bradycardia

56
Q

isoproterenol will cause reflex ____.

A

tachycardia

57
Q

clonidine, guanfacine

A
  • a2 agonist that reduces SNS output
  • used to treat hypertensive urgency, ADHD, Tourette
  • rebound HTN if taken off too quickly
58
Q

a-methyldopa

A
  • a2 agonist that reduces SNS output

- treats HTN in pregnancy

59
Q

phenoxybenzamine

A
  • irreversible a1/a2 antagonist

- used before pheochromocytoma surgery

60
Q

phentolamine

A
  • reversible a1/a2 antagonist

- given to patients on MAO inhibitors who eat tyramine-containing foods

61
Q

-azosin drugs, tamsulosin

A
  • a1 antagonist

- urinary retention due to BPH, PTSD, HTN

62
Q

mirtazapine

A
  • a2 antagonist

- used for depression

63
Q

-olol drugs

A
  • B blockers

- angina pectoris, MI, SVT, HTN, CHF, glaucoma

64
Q

acebutolol, atenolol, betaxolol, bisoprolol, emolol, metoprolol are ____ antagonists.

A

B1 selective (A –> M)

65
Q

Avoid ____ in cocaine users.

A

B blockers –> unopposed a1 action and HTN

66
Q

carvedilol, labetalol

A

a and B antagonists - great for HTN!!

67
Q

homatropine

A

muscarinic antagonist - eye

68
Q

tropicamide

A

muscarinic antagonist - eye

69
Q

trihexyphenidyl

A

muscarinic antagonist - CNS (acute dystonia)

70
Q

hyoscyamine

A

muscarinic antagonist - GI (prevents spasm in IBS)

71
Q

dicyclomine

A

muscarinic antagonist - GI (prevents spasm in IBS)

72
Q

solifenacin

A

muscarinic antagonist - bladder (reduces urge incontinence)

73
Q

tolterodine

A

muscarinic antagonist - bladder (reduces urge incontinence)

74
Q

BB used for SVT

A

metoprolol, esmolol

75
Q

BB used for HF

A

metoprolol, bisoprolol, carvedilol

76
Q

BB used for glaucoma

A

timolol

77
Q

BB used for variceal ppx

A

propanolol