Autonomic Drugs Flashcards

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1
Q

Sympathetic Nervous System organs innervated by cholinergic fibers?

A

Sweat glands and Adrenal Medulla

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2
Q

Botulinum Toxin

A

Prevents release of ACh at all cholinergic terminals

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3
Q

Nicotinic ACh receptors
Description
Location?

A

Ligand gated Na/K channel

Autonomic ganglia and NMJ

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4
Q
α1
System 
Kind of receptor?
Class
Function
A

Sympathetic
GPCR
q
Vascular SM contraction, Pupillary dilator muscle contraction (mydriasis), Intestinal and Bladder Sphincter muscle contraction

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5
Q
α2
System 
Kind of receptor?
Class
Function
A

Sympathetic
GPCR
i
↓ sympathetic outflow, ↓ insulin release, ↓ lipolysis, ↑ platelet aggregation

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6
Q
β1
System 
Kind of receptor?
Class
Function
A

Sympathetic
GPCR
s
↑ HR, contractility, rennin release, lipolysis

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7
Q
β2
System 
Kind of receptor?
Class
Function
A

Sympathetic
GPCR
s
Vasodilation, Bronchodilation, ↓ Uterine Tone (tocolysis)
↑ HR, contractility, lipolysis, insulin release
Ciliary Muscle Relaxation and ↑ Aqueous Humor production

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8
Q
M1
System 
Kind of receptor?
Class
Function
A

Parasympathetic
GPCR
q
CNS, Enteric Nervous System

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9
Q
M2
System 
Kind of receptor?
Class
Function
A

Parasympathetic
GPCR
i
↓ HR and atrai contractility

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10
Q
M3
System 
Kind of receptor?
Class
Function
A

Parasympathetic
q
GPCR
Exocrine gland secretion, gut peristalsis, bladder contraction, Bronchoconstriction, Pupillary sphincter muscle contraction (Miosis), Ciliary muscle contraction (accommodation)

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11
Q

D1
Kind of receptor?
Class
Function

A

GPCR
s
Relaxes renal vascular smooth muscle

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12
Q

D2
Kind of receptor?
Class
Function

A

GPCR
i
Modulates transmitter release, esp in brain

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13
Q

H1
Kind of receptor?
Class
Function

A

GPCR
q
Nasal and Bronchial mucus production, contraction of bronchioles, pruritus, pain

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14
Q

H2
Kind of receptor?
Class
Function

A

GPCR
s
Gastric Acid Secretion

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15
Q

V1
Kind of receptor
Class
Function

A

GPCR
q
Vascular smooth muscle contraction

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16
Q

V2
Kind of receptor
Class
Function

A

GPCR
s
↑ water permeability and reabsorption in collecting tubule of kidneys

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17
Q

Autonomic Receptor Mnemonic

A
QISS and QIQ until you're SIQ of SQS
α1, α2, β1, β2
M1, M2, M3
D1, D2
H1, H2
V1, V2
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18
Q

Autonomic drugs that use IP3/DAG

A

“HAVe 1 M&M”

H1, α1, V1, M1, M3

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19
Q

Autonomic drugs that ↓ cAMP

A

“MAD2”

M2, α2, D2

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20
Q

Autonomic drugs that ↑ cAMP

A

Gs
“Bill Bob Doesn’t Have Value”
β1, β2, D1, H2, V2

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21
Q

Hemicholinium

A

Blocks re-uptake of choline at ACh nerve terminal

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22
Q

Vesamicol

A

Blocks ACh packaging into vesicles

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23
Q

Metyrosine

A

Inhibits conversion of Tyrosine to DOPA

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24
Q

Reserpine

A

Inhibits packaging of DA into vesicles

May be turned into NE in vesicle

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25
Q

Guanethidine

A

Inhibits release of NE

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26
Q

Bretylium

A

Inhibits release of NE

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27
Q

Cocaine Re NE

A

Inhibit re-uptake of NE

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28
Q

TCA Re NE

A

Inhibit re-uptake of NE

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29
Q

Amphetamine Re NE

A

Inhibit re-uptake of NE

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30
Q

Presynaptic Regulation of Noradrenergic nerve terminals

A

NE –> α2 –/ NE release
ATII –> NE release
ACh –> M2 –/ NE release

31
Q
Bethanechol
MoA
Uses 
Organs affected 
Dynamics
A

Muscarinic agonist
PostOp ileus, Neurogenic ileus, Urinary retention
“Bethany Call me if you want to activate your Bowels or Bladder”
Activates Bowel and Bladder smooth muscle
Resistent to AChE

32
Q

Carbachol
MoA
Uses
Mnemonic

A

Muscarinic and Nicotinic Agonists
Glaucoma, Pupillary Contraction, and Relief of Intraocular Pressure
“CARBon copy of AcetylCHOLine”

33
Q
Pilocarpine 
MoA
Affects 
Uses 
Organs affected 
Dynamics 
Mnemonic
A

Muscarinic Agonist
Stimulator of sweat, tear, and salivary glands
Open and closed angle glaucoma
Contracts ciliary muscles of eye (closed angle glaucoma), Pupillary sphincter (closed angle glaucoma)
Resistant to AChE
“You Cry, Drool, and Sweat on your PILOw”

34
Q

Methacholine
MoA
Use

A

Muscarinic Agonist

Asthma challenge

35
Q

Neostigmine
MoA
Distribution
Uses

A

Reversible AChE inhibitor
“Neo CNS” No CNS penetration
PostOp and neurogenic ileus and urinary retention, MG, Reversal of NMJ blockade PostOp

36
Q

Pyridostigmine
MoA
Uses
Distribution

A

Reversible AChE inhibitor
“Rid of MG.” MG (long acting)
Does not penetrate CNS

37
Q

Edrophonium
MoA
Uses

A

Reversible AChE inhibitor

Diagnosis of MG (short acting)

38
Q

Physostigmine
MoA
Distribution
Uses

A

Reversible AChE inhibitor
Crosses BBB
Anticholinergic toxicity
“PHYso PHYxes atropine poisoning”

39
Q

Donepezil
Distribution
Uses

A

Reversible AChE inhibitor
CNS
Alzheimer’s Disease

40
Q

Risk of all AChE inhibitors

A

Exacerbation of COPD, Asthma, Peptic Ulcer Disease

41
Q
Cholinesterase Inhibitor Poisoning 
What is it?
What causes it?
Presentation 
Classic pt
Antidote
A

Irreversible AChE inhibition
Organophosphates like Parathion
“DUMBBELSS”
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation (of skeletal muscle and CNS), Lacrimation, Sweating, Salivation
Farmer working with insecticides
Atropine + Pralidoxime (regenerates active AChE)

42
Q
Homatropine 
MoA
Molecule like it?
Organs affected?
Uses
A

Muscarinic Antagonist
Atropine, Tropicamide
Eye
Produces mydriasis and cycloplegia

43
Q

Benztropine
MoA
Organs involved
Use

A

Muscarinic Antagonist
CNS
“PARK my BENZ”
Parkinson’s Disease

44
Q

Scopolamine
MoA
Organs involved
Uses

A

Muscarinic Antagonist
CNS
Motion sickness

45
Q
Ipratropium 
MoA
Molecules like it
Organis involved 
Use
A
Muscarinic Antagonist 
Tiotropium 
Respiratory 
COPD and Asthma 
"I PRAY i can breath again"
46
Q

Oxybutynin
MoA
Organs involved
Use

A

Muscarinic Antagonist
GU
Reduce urgency in mild cystitis and reduce bladder spasms

47
Q

Glycopyrrolate
MoA
Organs involved
Use

A

Muscarinic Antagonist
GU and Respiratory
Parenteral: PreOp use to reduce airway secretions
Oral: Drooling, Peptic Ulcers

48
Q

Atropine
MoA
Eye, Airway, Stomach, Gut, Bladder
Presentation

A

Muscarinic Antagonist
↑ pupil dilation, cycloplegia (acute angle glaucoma in elderly)
↓ airway secretions, ↓ stomach acids, ↓ gut motility (constipation), ↓ bladder urgency
Blocks DUMBBeLSS (excitation mediated by nicotinic receptors)

49
Q

Atropine Poisoning

A
Hot as a Hare
Dry as a Bone
Red as a Beat
Blind as a Bat
Mad as a Hatter
50
Q

What receptors does Epi affect?

What are its uses?

A

α1, α2, β1, β2 (β more)

Anaphylaxis, Open Angle Glaucoma, Asthma, Hypotension

51
Q

What receptors does NE affect?

What are its uses?

A

α1, α2, β1 (α more)

Hypotension (but ↓ Renal Perfusion)

52
Q

What receptors does Isoproterenol affect?

What are its uses?

A

β1, β2

Torsade de pointes, Bradyarrhythmias (but can worsen ischemia)

53
Q

What receptors does DA affect?

What are its uses?

A

α1, α2, β1, β2, D1

Shock (renal perfusion) and heart failure

54
Q

What receptors does Dobutamine affect?

What are its uses?

A

α1, α2, β1, β2 (β1 way more so!)

Heart failure, Cardiac stress test

55
Q

What receptors does Phenylephrine affect?

What are its uses?

A

α1 and α2 (α1 more)

Hypotension, Ocular procedures (mydriatic), Rhinitis (decongestant)

56
Q

What receptors does Albuterol affect?
Similar drugs?
What are its uses?

A
β1, β2 (β2 more so)
Salmeterol, Terbutaline 
A: acute Asthma
S: long term Asthma, COPD
T: reduce premature uterine contractions
57
Q

Ritodrine
What receptors does it affect?
Uses

A

β2

Reduce premature uterine contractions

58
Q

Amphetamine
MoA
Uses

A

Release of stored Catecholamines

Narcolepsy, Obesity, ADD

59
Q

Ephedrine
MoA
Uses

A

Release of stored Catecholamines

Nasal decongestion, Urinary incontinence, Hypotension

60
Q

Cocaine
MoA
What does it lead to?
Contraindications

A

Inhibits reuptake of catecholamines
Vasoconstriction and local anesthesia
β blockers contraindicated because can lead to unopposed α activation and HTN

61
Q

NE vs Isoproterenol

A

NE –> ↑ in systolic and diastolic BP
α mediated vasoconstriction –> ↑ MAP –> Bradycardia
Isoproterenol –> β2 mediated vasodilation –> ↓ MAP and ↑ HR through β1 and reflex activity

62
Q

Clonidine
MoA
Molecules similar to it?
Uses

A

α2 agonist –> ↓ central sympathetic outflow
α methyldopa
HTN esp with Renal Disease

63
Q
Phenoxybenzamine 
MoA
Reversibility 
Uses 
Tox
A

α blocker
Irreversible
Pheochromocytoma (PreOp)
Orthostatic Hypotension and reflex Tachycardia

64
Q

Phentolamine
MoA
Reversibility
Uses

A

α blocker
Reversible
Give to pts on MAO inhibitors who eat tyramine-containing foods

65
Q

α1 blockers
Names
Uses
Tox

A

Prazosin, Terazosin, Doxazosin, Tamsulosin
HTN, Urinary retention in BPH
Orthostatic Hypotension, Dizziness, Headache

66
Q

α2 blockers
Names
Uses
Tox

A

Mirtazapine
Depression
Sedation, ↑ Cholesterol, ↑ Appetite

67
Q

Phenylephrine vs Epi on α blockade

A

Epi will cause net decrease in BP because of actions on β

PE will cause a reversal to baseline because it is pure α

68
Q

β blockers
Names
Applications

A

Acebutolol, Betaxolol, Esmolol, Atenolol, Metolol, Propanolol, Timolol, Pindolol, Labetalol
Angina Pectoris, MI, SVT (M and E ↓ conduction velocity), HTN (renin), CHF, Glaucoma (T ↓ secretion of aqueous humor)

69
Q

β blockers Tox

Use with caution in…

A

Bradycardia (AV block and CHF), Bronchoconstriction, Claudication, Lipids, Vivid dreams (seizures, sedation), Impotence, Masks hypoglycemia
Use with caution in diabetics, ↓ insulin release
Use with caution in diabetics

70
Q

β1 blockers

A

“A BEAM” Before M in the alphabet

Acebutolol, Betaxolol, Esmolol, Atenolol, Metoprolol

71
Q

Non selective β blockers

A

“Please Try Not βeing Picky” After M in the alphabet

Propanolol, Timolol,Nadolol, Pindolol

72
Q

α and β non selective blockers

A

Carvedilol, Labetalol

73
Q

Partial β Agonists

A

Pindolol, Acebutolol