Autonomic Drugs Flashcards Preview

► Med 11 - USMLE 1 > Autonomic Drugs > Flashcards

Flashcards in Autonomic Drugs Deck (73):
1

Sympathetic Nervous System organs innervated by cholinergic fibers?

Sweat glands and Adrenal Medulla

2

Botulinum Toxin

Prevents release of ACh at all cholinergic terminals

3

Nicotinic ACh receptors
Description
Location?

Ligand gated Na/K channel
Autonomic ganglia and NMJ

4

α1
System
Kind of receptor?
Class
Function

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

5

α2
System
Kind of receptor?
Class
Function

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

6

β1
System
Kind of receptor?
Class
Function

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

7

β2
System
Kind of receptor?
Class
Function

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

8

M1
System
Kind of receptor?
Class
Function

Parasympathetic
GPCR
q
CNS, Enteric Nervous System

9

M2
System
Kind of receptor?
Class
Function

Parasympathetic
GPCR
i
↓ HR and atrai contractility

10

M3
System
Kind of receptor?
Class
Function

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

11

D1
Kind of receptor?
Class
Function

GPCR
s
Relaxes renal vascular smooth muscle

12

D2
Kind of receptor?
Class
Function

GPCR
i
Modulates transmitter release, esp in brain

13

H1
Kind of receptor?
Class
Function

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

14

H2
Kind of receptor?
Class
Function

GPCR
s
Gastric Acid Secretion

15

V1
Kind of receptor
Class
Function

GPCR
q
Vascular smooth muscle contraction

16

V2
Kind of receptor
Class
Function

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

17

Autonomic Receptor Mnemonic

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

18

Autonomic drugs that use IP3/DAG

"HAVe 1 M&M"
H1, α1, V1, M1, M3

19

Autonomic drugs that ↓ cAMP

"MAD2"
M2, α2, D2

20

Autonomic drugs that ↑ cAMP

Gs
"Bill Bob Doesn't Have Value"
β1, β2, D1, H2, V2

21

Hemicholinium

Blocks re-uptake of choline at ACh nerve terminal

22

Vesamicol

Blocks ACh packaging into vesicles

23

Metyrosine

Inhibits conversion of Tyrosine to DOPA

24

Reserpine

Inhibits packaging of DA into vesicles
May be turned into NE in vesicle

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