Autonomic Drugs Flashcards

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
Guanethidine
Inhibits release of NE
26
Bretylium
Inhibits release of NE
27
Cocaine Re NE
Inhibit re-uptake of NE
28
TCA Re NE
Inhibit re-uptake of NE
29
Amphetamine Re NE
Inhibit re-uptake of NE
30
Presynaptic Regulation of Noradrenergic nerve terminals
NE --> α2 --/ NE release ATII --> NE release ACh --> M2 --/ NE release
31
``` Bethanechol MoA Uses Organs affected Dynamics ```
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
Carbachol MoA Uses Mnemonic
Muscarinic and Nicotinic Agonists Glaucoma, Pupillary Contraction, and Relief of Intraocular Pressure "CARBon copy of AcetylCHOLine"
33
``` Pilocarpine MoA Affects Uses Organs affected Dynamics Mnemonic ```
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
Methacholine MoA Use
Muscarinic Agonist | Asthma challenge
35
Neostigmine MoA Distribution Uses
Reversible AChE inhibitor "Neo CNS" No CNS penetration PostOp and neurogenic ileus and urinary retention, MG, Reversal of NMJ blockade PostOp
36
Pyridostigmine MoA Uses Distribution
Reversible AChE inhibitor "Rid of MG." MG (long acting) Does not penetrate CNS
37
Edrophonium MoA Uses
Reversible AChE inhibitor | Diagnosis of MG (short acting)
38
Physostigmine MoA Distribution Uses
Reversible AChE inhibitor Crosses BBB Anticholinergic toxicity "PHYso PHYxes atropine poisoning"
39
Donepezil Distribution Uses
Reversible AChE inhibitor CNS Alzheimer's Disease
40
Risk of all AChE inhibitors
Exacerbation of COPD, Asthma, Peptic Ulcer Disease
41
``` Cholinesterase Inhibitor Poisoning What is it? What causes it? Presentation Classic pt Antidote ```
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
``` Homatropine MoA Molecule like it? Organs affected? Uses ```
Muscarinic Antagonist Atropine, Tropicamide Eye Produces mydriasis and cycloplegia
43
Benztropine MoA Organs involved Use
Muscarinic Antagonist CNS "PARK my BENZ" Parkinson's Disease
44
Scopolamine MoA Organs involved Uses
Muscarinic Antagonist CNS Motion sickness
45
``` Ipratropium MoA Molecules like it Organis involved Use ```
``` Muscarinic Antagonist Tiotropium Respiratory COPD and Asthma "I PRAY i can breath again" ```
46
Oxybutynin MoA Organs involved Use
Muscarinic Antagonist GU Reduce urgency in mild cystitis and reduce bladder spasms
47
Glycopyrrolate MoA Organs involved Use
Muscarinic Antagonist GU and Respiratory Parenteral: PreOp use to reduce airway secretions Oral: Drooling, Peptic Ulcers
48
Atropine MoA Eye, Airway, Stomach, Gut, Bladder Presentation
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
Atropine Poisoning
``` Hot as a Hare Dry as a Bone Red as a Beat Blind as a Bat Mad as a Hatter ```
50
What receptors does Epi affect? | What are its uses?
α1, α2, β1, β2 (β more) | Anaphylaxis, Open Angle Glaucoma, Asthma, Hypotension
51
What receptors does NE affect? | What are its uses?
α1, α2, β1 (α more) | Hypotension (but ↓ Renal Perfusion)
52
What receptors does Isoproterenol affect? | What are its uses?
β1, β2 | Torsade de pointes, Bradyarrhythmias (but can worsen ischemia)
53
What receptors does DA affect? | What are its uses?
α1, α2, β1, β2, D1 | Shock (renal perfusion) and heart failure
54
What receptors does Dobutamine affect? | What are its uses?
α1, α2, β1, β2 (β1 way more so!) | Heart failure, Cardiac stress test
55
What receptors does Phenylephrine affect? | What are its uses?
α1 and α2 (α1 more) | Hypotension, Ocular procedures (mydriatic), Rhinitis (decongestant)
56
What receptors does Albuterol affect? Similar drugs? What are its uses?
``` β1, β2 (β2 more so) Salmeterol, Terbutaline A: acute Asthma S: long term Asthma, COPD T: reduce premature uterine contractions ```
57
Ritodrine What receptors does it affect? Uses
β2 | Reduce premature uterine contractions
58
Amphetamine MoA Uses
Release of stored Catecholamines | Narcolepsy, Obesity, ADD
59
Ephedrine MoA Uses
Release of stored Catecholamines | Nasal decongestion, Urinary incontinence, Hypotension
60
Cocaine MoA What does it lead to? Contraindications
Inhibits reuptake of catecholamines Vasoconstriction and local anesthesia β blockers contraindicated because can lead to unopposed α activation and HTN
61
NE vs Isoproterenol
NE --> ↑ in systolic and diastolic BP α mediated vasoconstriction --> ↑ MAP --> Bradycardia Isoproterenol --> β2 mediated vasodilation --> ↓ MAP and ↑ HR through β1 and reflex activity
62
Clonidine MoA Molecules similar to it? Uses
α2 agonist --> ↓ central sympathetic outflow α methyldopa HTN esp with Renal Disease
63
``` Phenoxybenzamine MoA Reversibility Uses Tox ```
α blocker Irreversible Pheochromocytoma (PreOp) Orthostatic Hypotension and reflex Tachycardia
64
Phentolamine MoA Reversibility Uses
α blocker Reversible Give to pts on MAO inhibitors who eat tyramine-containing foods
65
α1 blockers Names Uses Tox
Prazosin, Terazosin, Doxazosin, Tamsulosin HTN, Urinary retention in BPH Orthostatic Hypotension, Dizziness, Headache
66
α2 blockers Names Uses Tox
Mirtazapine Depression Sedation, ↑ Cholesterol, ↑ Appetite
67
Phenylephrine vs Epi on α blockade
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
β blockers Names Applications
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
β blockers Tox | Use with caution in...
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
β1 blockers
"A BEAM" Before M in the alphabet | Acebutolol, Betaxolol, Esmolol, Atenolol, Metoprolol
71
Non selective β blockers
"Please Try Not βeing Picky" After M in the alphabet | Propanolol, Timolol,Nadolol, Pindolol
72
α and β non selective blockers
Carvedilol, Labetalol
73
Partial β Agonists
Pindolol, Acebutolol