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Pharm > Autonomic drugs 0423FA > Flashcards

Autonomic drugs 0423FA Flashcards

1
Q

nicotinic ACh receptor

A

ligand gated Na-K channels.

subtypes: Nn and Nm

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2
Q

muscarinic ACh receptor

A

GPCR acting through second messengers.

subtypes: M1-M5

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3
Q

Gq

A

activate phospholipase C, which (though PIP2) activates protein kinase C (DAG) and increases cytosolic Ca for contraction (IP3)

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4
Q

Gs

A

activates adenylyl cyclase to increase cAMP which activates protein kinase A to increase Ca in heart and MLCK of smooth mm.

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5
Q

Gi

A

INHIBITS adenylyl cyclase, opposite of Gs

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6
Q

alpha 1 [symp]

A

Gq:
increase vasc smooth muscle contraction. increase pupillary dilator muscle contraction (mydriasis).
increase intestinal and bladder sphincter muscle contraction.

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7
Q

alpha 2 [symp]

A

Gi:
decrease symp outflow.
decrease insulin release.

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8
Q

beta 1 [symp]

A

Gs:
increase HR, contractility.
increase lipolysis.
increase renin release.

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9
Q

beta 2 [symp]

A 
Gs: 
vasodilation, bronchodilation. 
increase HR and contractility. 
increase lipolysis. 
increase insulin release. 
decrease uterine tone.
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10
Q

M1 [parasymp]

A

Gq: CNS, enteric nervous system.

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11
Q

M2 [parasymp]

A

Gi: decrease HR and contractility of atria.

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12
Q

M3 [parasymp]

A

Gq:
increase exocrine gland secretion (sweat, gastric acid).
increase gut peristalsis.
increase bladder contraction.
bronchoconstriction.
increase pupillary sphincter muscle contraction (miosis).
ciliary muscle contraction (accommodation).

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13
Q

D1 [dopamine]

A

Gs: relax renal vasc smooth muscle.

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14
Q

D2 [dopamine]

A

Gi: modulate transmitter release, esp. in brain.

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15
Q

H1 [histamine]

A 
Gq: 
increase nasal and bronchial mucus prod.
contraction of bronchioles.
pruritus. 
pain.
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16
Q

H2 [histamine]

A

Gs: increase gastric acid secretion.

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17
Q

V1 [vasopressin]

A

Gq: increase vasc smooth muscle contraction.

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18
Q

V2 [vasopressin]

A

Gs: increase water perm and reabsorp in collecting tubules of kidneys.

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19
Q

hemicholinium

A

blocks reuptake of choline into presynaptic neuron. choline is necessary for ACh synthesis.

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20
Q

vesamicol

A

blocks transport of ACh into vesicles that are supposed to fuse with membrane and release ACh.

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21
Q

botulinum toxin

A

prevent ACh release at all cholinergic terminals

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22
Q

pathway from tyrosine to NE/epi

A

tyrosine (tyrosine hydroxylase) to DOPA (DOPA decarboxylase) to dopamine (dopamine beta-hydroxylase) to NE (PNMT) to epinephrine

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23
Q

metyrosine

A

inhibits tyrosine hydroxylase

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24
Q

reserpine

A

inhibits transport of dopamine into vesicles where NE is formed

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25
Q

guanethidine

A

inhibits NE (catecholamine) release at nerve endings

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26
Q

amphetamine

A

enhances catecholamine release. inhibits reuptake.

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27
Q

what three drugs inhibit catecholamine reuptake at nerve terminal?

A
  1. amphetamine
  2. cocaine
  3. TCA
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28
Q

what factors affect NE release from symp nerve ending?

A
  1. neg feedback by NE (on alpha2 auto receptor)
  2. ACh at M2 receptor downregulates
  3. AII upregulates
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29
Q

bethanechol

A

cholinomimetic. direct agonist.
for postop and neurogenic ileus; urinary retention.
activates bowel and bladder smooth mm.
resistant to AChE.

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30
Q

carbachol

A

cholinomimetic. direct agonist.

for glaucoma, pupillary contraction, relief of IOP.

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31
Q

pilocarpine

A

cholinomimetic. direct agonist.
potent stimulator of sweat, tears, saliva.
contracts ciliary muscle of eye (open angle) and pupillary sphincter (narrow angle).
resistant to AChE.

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32
Q

methacholine

A

cholinomimetic. direct agonist.
challenge test for dx of asthma.
stimulates muscarinic receptor in airway when inhaled.

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33
Q

neostigmine

A

cholinomimetic. indirect agonist (anticholinesterase).
for postop and neurogenic ileus; urinary retention.
myasthenia gravis. reverse NMJ block.
NO CNS PENETRATION.

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34
Q

pyridostigmine

A

cholinomimetic. indirect agonist (anticholinesterase).
for myasthenia gravis (long acting, increase strength).
NO CNS PENETRATION.

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35
Q

edrophonium

A

cholinomimetic. indirect agonist (anticholinesterase).

for dx of myasthenia gravis (extremely short acting)

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36
Q

physostigmine

A

cholinomimetic. indirect agonist (anticholinesterase).
for glaucoma - DOES CROSS BBB.
for atropine overdose.

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37
Q

echothiophate

A

cholinomimetic. indirect agonist (anticholinesterase).

for glaucoma.

38
Q

donepezil

A

cholinomimetic. indirect agonist (anticholinesterase).

for alzheimer.

39
Q

what conditions can be exacerbated by cholinomimetic agents?

A

COPD, asthma, peptic ulcers

40
Q

what inhibits AChE?

A

organophosphates - parathion. component of insecticides (affects farmers).

41
Q

what are the sx of cholinesterase inhibition?

A 
DUMBBELSS
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skel mm/CNS
Lacrimation
Sweating
Salivation
42
Q

what is the antidote for organophosphate poisoning?

A

atropine + pralidoxime

43
Q

muscarinic antagonists

A

inhibit postsynaptic action of ACh.

44
Q

atropine, homatropine, tropicamide

A

muscarinic antagonists.

eye - produce mydriasis and cycloplegia (loss of accomm).

45
Q

benztropine

A

muscarinic antagonists.
CNS - parkinson disease.
“park my benz”

46
Q

scopolamine

A

muscarinic antagonists.

CNS - motion sickness.

47
Q

ipratropium

A

muscarinic antagonists.

resp - asthma, COPD.

48
Q

oxybutynin, glycopyrrolate

A

muscarinic antagonists.

GU - reduce urgency in mild cystitis. reduce bladder spasms.

49
Q

methscopolamine, pirenzepine, propantheline

A

muscarinic antagonists.

GI - peptic ulcer tx.

50
Q

atropine

A

muscarinic antagonist used for bradycardia and ophthalmic applications.

eye: increase pupil dilation, cycloplegia.
airway: decrease secretions.
stomach: decrease acid secretion.
gut: decrease motility.
bladder: decrease urgency in cystitis.

51
Q

epinephrine action

A 
direct sympathomimetic. 
a1: ++++
a2: ++++
b1: ++++
b2: ++++
D1: 0
52
Q

epinephrine use

A

anaphylaxis.
glaucoma (open angle).
asthma.
hypotension.

53
Q

norepinephrine action

A 
direct sympathomimetic. 
a1: ++++
a2: ++++
b1: ++
b2: 0
D1: 0
54
Q

NE use

A

hypotension - but decreases renal perfusion

55
Q

isoproterenol action

A 
direct sympathomimetic. 
a1: 0
a2: 0
b1: ++++
b2: ++++
D1: 0
56
Q

isoproterenol use

A

AV block (rare)

57
Q

dopamine action

A 
direct sympathomimetic. 
a1: ++++ at high dose
a2: ++++ at high dose
b1: ++++ at med dose
b2: ++ at med dose
D1: + at low dose

D1 > b > a

58
Q

dopamine use

A

shock (renal perfusion).
heart failure.
inotropic and chronotropic effects.

59
Q

dobutamine action

A 
direct sympathomimetic. 
a1: +
a2: +
b1: ++++
b2: +
D1: 0
60
Q

dobutamine use

A

heart failure.
cardiac stress testing.
inotropic and chronotropic effects.

61
Q

phenylephrine action

A 
direct sympathomimetic. 
a1: ++++
a2: ++
b1: 0
b2: 0
D1: 0
62
Q

phenylephrine use

A

ocular procedures - mydriatic effect.
hypotension - vasoconstrictive.
rhinitis - nasal decongestant.

63
Q

Metaproteronol
Albuterol
Salmeterol
Terbutaline

action

A 
direct sympathomimetic. 
a1: 0
a2: 0
b1: ++
b2: ++++
D1: 0
64
Q

Metaproteronol
Albuterol
Salmeterol
Terbutaline

use

A

Metaproteronol and Albuterol for acute asthma.
Salmeterol for long-term tx.
Terbutaline to reduce premature uterine contractions.

65
Q

ritodrine action

A 
direct sympathomimetic. 
a1: 0
a2: 0
b1: 0
b2: ++++
D1: 0
66
Q

ritodrine use

A

reduces premature uterine contractions.

67
Q

amphetamine action

A

indirect sympathomimetic.

indirect general agonist, releases stored catecholamines.

68
Q

amphetamine use

A

narcolepsy.
obesity.
ADD.

69
Q

ephedrine action

A

indirect sympathomimetic.

indirect general agonist, releases stored catecholamines.

70
Q

ephedrine use

A

nasal decongestion.
urinary incontinence.
hypotension.

71
Q

cocaine action

A

indirect general agonist.

uptake inhibitor.

72
Q

cocaine use

A

causes vasoconstriction and local anesthesia.

73
Q

sympathoplegics: clonidine, alpha-methyldopa

A

centrally acting a2-agonists. decrease central adrenergic outflow.

for HTN, esp with renal disease (no decrease in bld flow to kidney).

74
Q

nonselective alpha blockers

A

phenoxybenzamine (irreversible).

phentolamine (reversible).

75
Q

phenoxybenzamine use

A

pheochromocytoma - use drug before removing tumor since high levels of released catecholamines will not be able to overcome blockage.

tox: orthostatic hypotension, reflex tachycardia.

76
Q

phentolamine use

A

give to pts on MAO inhibitors who eat tyramine-containing food

77
Q

alpha1-selective blockers

A

-zosin: prazosin, terazosin, doxazosin

use: HTN, urinary retention in BPH.
tox: 1st dose orthostatic hypotension, dizziness, HA.

78
Q

alpha2-selective blockers

A

mirtazapine.

use: depression.
tox: sedation, increased serum chol, increased appetite.

79
Q

beta1-selective blockers

A 
b1 > b2
Acebutolol (partial agonist).
Betaxolol.
Esmolol (short acting).
Atenolol.
Metoprolol.

“A BEAM of b1-blockers”

good for pts with comorbid pulmo dz.

80
Q

nonselective beta antagonists

A 
b1 = b2
Propanolol.
Timolol.
Nadolol.
Pindolol.

Please Try Not being Picky.

81
Q

nonselective mixed alpha-beta antagonists

A

carvedilol, labetolol.

vasodilatory effects.

82
Q

partial beta agonists

A

pindolol, acebutolol.

83
Q

BB for HTN

A 
decrease CO.
decrease renin (beta block on JGA cells).
84
Q

BB for angina pectoris

A

decrease HR and contractility, resulting in decreased O2 consumption

85
Q

BB for MI

A

decrease mortality

86
Q

BB for SVT

A

[propanolol, esmolol]

decrease AV conduction velocity [class II antiarrhythmics]

87
Q

BB for CHF

A

slow progression of chronic failure

88
Q

BB for glaucoma

A

[timolol]

decrease secretion of aqueous humor

89
Q

BB toxicity

A 
impotence.
exacerbation of asthma.
hypotension.
CV: bradycardia, AV block, CHF.
CNS: sedation, sleep alterations.

*caution in diabetics

90
Q

BB antidote

A

GLUCAGON acts on GPCR to increase cAMP and Ca++ release during muscle contraction. increases HR and contractility w/in minutes.

Pharm (5 decks)

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