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step 1 - pharm > autonomic drugs > Flashcards

autonomic drugs Flashcards

1
Q

which components of sympathetic NS are innervated by cholinergic fibers?

A

adrenal medulla

sweat glands

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2
Q

which components of PNS have nicotinic receptors?

A

somatic skeletal mm
adrenal medulla
pre-synaptic neurons of autonomic NS

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3
Q

how do nicotinic receptors work?

A

ligand-gated Na/K channels

  • Nn subtype in autonomic ganglia
  • Nm subtype in NMJ
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4
Q

how do muscarinic receptors work?

A

GPCRs

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5
Q

which autonomic receptors are Gq coupled?

A 
Quick! HAVe 1 M&M
H1
alpha1
V1
M1
M3
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6
Q

which autonomic receptors are Gi coupled?

A

I’m 2 MAD
M2
A2
D2

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7
Q

which autonomic receptors are Gs coupled?

A 
B1
B2
D1
H2
V2
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8
Q

what does Gq do?

A

activates PLC –> IP3 and DAG

  • IP3 –> increased Ca influx –> smooth mm contraction
  • DAG –> PKC activation
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9
Q

what does Gs do?

A

activates adenylyl cyclase –> cAMP increases

cAMP activates PKA –> increased Ca influx in heart, inhibition of myosin light chain kinase

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10
Q

what does Gi do?

A

inhibits adenylyl cyclase –> cAMP decreases, PKA deactivated

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11
Q

actions of alpha1?

A

Gq
vasoconstriction (skin, GI, renal, brain)
mydriasis
intestinal and bladder sphincter contraction

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12
Q

actions of alpha2?

A 
Gi
decreased sympathetic outflow
decreased insulin, lipolysis
increased platelet agg
decreased aqueous humor production
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13
Q

actions of beta1?

A

Gs
inotropy, chronotropy
increased renin release (via JG cells)
increased lipolysis

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14
Q

actions of beta2?

A 
Gs
vasodilation
bronchodilation
increased lipolysis, insulin release
uterine and ciliary mm relaxation
increased aqueous humor production
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15
Q

actions of M1?

A

parasymp - Gq

acts on CNS, enteric NS

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16
Q

actions of M2?

A

parasymp - Gi

decreases HR and atrial contraction

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17
Q

actions of M3?

A 
parasymp - Gq
increases exocrine gland secretion
increases gut peristalsis, bladder contraction
bronchoconstriction
miosis, accommodation
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18
Q

actions of D1?

A

Gs

relaxes renal vascular smooth mm

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19
Q

actions of D2?

A

Gi

brain transmitter release

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20
Q

actions of H1?

A 
Gq
increased nasal/bronchial mucus
increased vascular permeability
bronchoconstriction
pruritus
pain
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21
Q

actions of H2?

A

Gs

increased gastric acid secretion

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22
Q

actions of V1?

A

Gq

increased vasoconstriction

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23
Q

actions of V2?

A

Gs

collecting tubules - AQP insertion

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24
Q

hemocholinium MOA?

A

blocks choline entry into axon

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25
Q

vesamicol MOA?

A

blocks ACh entry into pre-synaptic vesicle

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26
Q

botox MOA?

A

blocks pre-synaptic release of ACh

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27
Q

AChE does what?

A

splits ACh into choline and acetate in synapse - terminates signal

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28
Q

metyrosine MOA?

A

blockes tyr –> DOPA conversion

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29
Q

reserpine MOA?

A

blocks dopa entry into pre-synaptic vesicles

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30
Q

bretylium, guanethidine MOA?

A

block NE release into synapse

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31
Q

amphetamine, ephedrine MOA?

A

stimulate NE release into synapse

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32
Q

cocaine, TCA, amphetamine MOA?

A

block NE reuptake into axon

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33
Q

how does NE regulate its own signal?

A

binds alpha2 receptor on pre-synaptic axon –> inhibits further release

34
Q

bethanechol?

A

uses: ileus, urinary retention

MOA: activates bowel and bladder smooth mm

** resistant to AChE

35
Q

carbachol?

A

uses: pupil constriction, glaucoma

MOA: same as ACh

36
Q

methacholine?

A

uses: asthma dx challenge

MOA: stimulates airway muscarinic rctprs

37
Q

pilocarpine?

A

uses: stimulates sweat, tears, saliva – use in open and closed angle glaucoma

MOA: contracts ciliary mm, pupillary sphincter

** resistant to AChE

38
Q

drugs for Alzheimer?

A

AChE inhibitors!

donepezil
rivastigmine
galantamine

39
Q

edrophonium?

A

used for dx of MG (historically)

very short acting AChE inhibitor

40
Q

neostigmine?

A

AChE inhibitor

uses: ileus, urinary retention, MG, postop reversal of NMJ blockade

** no CNS penetration

41
Q

physostigmine

A

AChE inhibitor

uses: anticholinergic toxicity

** crosses BBB - CNS effects

42
Q

pyridostigmine?

A

AChE inhibitor

uses: MG (long-acting).

    • increases mm strength
    • no CNS penetration
43
Q

what can you exacerbate when giving pts cholinomimetics?

A

COPD
asthma
peptic ulcers

44
Q

DUMBBELSS?

A

cholinesterase inhibitor poisoning - irreversible inhib of AChE
e.g. parathion, malathion - farmers!

** give atropine + pralidoxime (regenerates AChE if early)

45
Q

atropine, homatropine, tropicamide?

A

anticholinergic

used in eye –>
mydriasis
cycloplegia

46
Q

benztropine?

A

anticholinergic

used in PD, acute dystonia

47
Q

glycopyrrolate?

A

anticholinergic

parenteral –> preop to reduce airway secretions
oral –> drooling, peptic ulcer

48
Q

hyoscyamine, dicyclomine?

A

anitcholinergic

used in IBS (antispasmodics)

49
Q

ipratropium, tiotropium?

A

anticholinergic

used in COPD, asthma

50
Q

oxybutynin, solifenacin, tolterodine?

A

anticholinergic

used in bladder spasms, urge urinary incontinence

51
Q

scopolamine?

A

anticholinergic

used in motion sickness

52
Q

atropine toxicity?

A

hot as a hare…
can cause acute angle closure glaucoma
urinary retention in BPH
hyperthermia in infants

53
Q

jimson weed?

A

plant alkaloids –> mydriasis (atropine-like rxn)

“gardener’s pupil”

54
Q

i ate a fugu/pufferfish! what’s going to happen to me?

A 
tetrodotoxin poisoning (if improperly prepared)
binds fast voltage gated Na channels in cardiac and nerve tissue --> depol prevented
nausea, diarrhea, paresthesias, weakness, dizziness, hyporeflexia

** tx: supportive

55
Q

i ate a barracuda/snapper/moray eel! what’s going to happen to me?

A

ciguatoxin poisoning
opens Na channels –> depol
sx similar to cholinergic poisoning

    • temperature dysesthesia (cold feels hot, hot feels cold) is specific for this! WEIRD SHIT
    • tx: supportive
56
Q

i ate bonito/mackerel/mahimahi/tuna! what’s going to happen to me?

A 
scombroid poisoning (if stored at warm temp): bacterial histidine decarboxylase converts histidine --> histamine
acute burning sensation in mouth, flushing, erythema, urticaria, possible anaphylaxis

** tx: antihistmines; anti-anaphylactics as needed

57
Q

albuterol, salmeterol?

A

beta2 > beta1

albuterol = acute asthma
salmeterol = long term asthma, COPD
58
Q

dobutamine?

A

beta 1 > beta 2, alpha

use in HF, stress testing

** inotropy > chronotropy

59
Q

dopamine?

A

D1 = D2 > beta > alpha

use in unstable brady, HF, shock

** at high doses, alpha effects (inotropy, chronotropy) dominate

60
Q

epinephrine?

A

beta > alpha

use in anaphylaxis, asthma, open angle glaucoma

    • alpha effects dominate at high doses
    • stronger at beta 2 than NE
61
Q

isoproterenol?

A

beta1 = beta2

use in EP eval of tachyarrhythmias

** can worsen ischemia

62
Q

NE?

A

alpha1 > alpha2 > beta1

use in hypoT

    • decreases renal perfusion
    • weaker at beta2 vs epinephrine
63
Q

phenylephrine?

A

alpha1 > alpha2

use in hypoT, ocular procedure (causes mydriasis), rhinitis (decongestant)

64
Q

amphetamine?

A

indirect general sympathomimetic
reuptake inhibitor
releases stored catecholamines

use in narcolepsy, obesity, ADHD

65
Q

cocaine?

A

indirect general sympathomimetic
reuptake inhibitor

vasoconstriction, local anesthesia

** DON’T give BBs to cocaine users - risk of unopposed alpha1 –> extreme HTN

66
Q

ephedrine?

A

indirect general sympathomimetic
releases stored catecholamines

use for nasal decongestion, urinary incontinence, hypoT

67
Q

NE vs isoproterenol?

A

NE –> alpha1 –> increased sys and dia BP –> reflex bradycardia

isoproterenol –> beta2 –> vasodilation –> reflex (and beta1-mediated) tachycardia

68
Q

clonidine?

A

alpha2 agonist - sympatholytic!

use in HTN urgency, ADHD, tourettes

    • does not decrease renal blood flow
    • toxicity: CNS depression, brady, hypoT, resp depression, miosis
69
Q

alpha-methyldopa?

A

alpha2 agonist - sympatholytic!

use in preggos with HTN

** causes direct Coombs + hemolysis, SLE-like syndrome

70
Q

phenoxybenzamine?

A

irreversible nonselective alpha blocker
use preop in pheo

** SEs: orthostatic hypoT, reflex tachy

71
Q

phentolamine?

A

reversible nonselective alpha blocker
give to pts on MAOis who eat tyramine

** SEs: orthostatic hypoT, reflex tachy

72
Q

prazosin, terazosin, etc?

A

alpha1 selective blocker

use in BPH with urinary sx, PTSD (prazosin), HTN (NOT tamsulosin)

** SEs: 1st dose orthostasis, dizziness, HA

73
Q

mirtazapine?

A

alpha2 selective blocker

use in depression

** SEs: sedation, increased serum cholesterol, increased appetite

74
Q

what happens when you give alpha blocker to pt on epi?

A

epi –> net BP increase

alpha blockade –> net BP decrease (because of unopposed beta 2 action)

75
Q

what happens when you give alpha blocker to pt on phenylephrine?

A

phenylephrine –> net BP increase

alpha blockade –> suppression of phenylephrine effect without BP depression - no beta action

76
Q

which BBs can you give for SVT?

A

metoprolol
esmolol

** decrease AV conduction

77
Q

which BB can you give for glaucoma?

A

timolol

** decrease secretion of aqueous humor

78
Q

BB toxicity?

A

impotence
CNS - sz, sedation, sleep alterations
dyslipidemia (metoprolol)
asthma/COPD exacerbation

** AVOID in cocaine users - risk of unopposed alpha –> HTN

79
Q

which are the beta1 selective BBs?

A 
from A to M:
acebutolol
atenolol
betaxolol
esmolol
metoprolol
80
Q

which are the nonselective BBs?

A 
from N to Z
nadolol
pindolol
propranolol
timolol
81
Q

which are the nonselective alpha and beta BBs?

A

carvedilol

lavetalol

82
Q

nebivolol?

A

beta 1 blockade + beta3 stimulation –> NO synthase activation in vasculature

step 1 - pharm (13 decks)

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