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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
guanethidine
inhibits NE (catecholamine) release at nerve endings
26
amphetamine
enhances catecholamine release. inhibits reuptake.
27
what three drugs inhibit catecholamine reuptake at nerve terminal?
1. amphetamine 2. cocaine 3. TCA
28
what factors affect NE release from symp nerve ending?
1. neg feedback by NE (on alpha2 auto receptor) 2. ACh at M2 receptor downregulates 3. AII upregulates
29
bethanechol
cholinomimetic. direct agonist. for postop and neurogenic ileus; urinary retention. activates bowel and bladder smooth mm. resistant to AChE.
30
carbachol
cholinomimetic. direct agonist. | for glaucoma, pupillary contraction, relief of IOP.
31
pilocarpine
cholinomimetic. direct agonist. potent stimulator of sweat, tears, saliva. contracts ciliary muscle of eye (open angle) and pupillary sphincter (narrow angle). resistant to AChE.
32
methacholine
cholinomimetic. direct agonist. challenge test for dx of asthma. stimulates muscarinic receptor in airway when inhaled.
33
neostigmine
cholinomimetic. indirect agonist (anticholinesterase). for postop and neurogenic ileus; urinary retention. myasthenia gravis. reverse NMJ block. NO CNS PENETRATION.
34
pyridostigmine
cholinomimetic. indirect agonist (anticholinesterase). for myasthenia gravis (long acting, increase strength). NO CNS PENETRATION.
35
edrophonium
cholinomimetic. indirect agonist (anticholinesterase). | for dx of myasthenia gravis (extremely short acting)
36
physostigmine
cholinomimetic. indirect agonist (anticholinesterase). for glaucoma - DOES CROSS BBB. for atropine overdose.
37
echothiophate
cholinomimetic. indirect agonist (anticholinesterase). | for glaucoma.
38
donepezil
cholinomimetic. indirect agonist (anticholinesterase). | for alzheimer.
39
what conditions can be exacerbated by cholinomimetic agents?
COPD, asthma, peptic ulcers
40
what inhibits AChE?
organophosphates - parathion. component of insecticides (affects farmers).
41
what are the sx of cholinesterase inhibition?
``` DUMBBELSS Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skel mm/CNS Lacrimation Sweating Salivation ```
42
what is the antidote for organophosphate poisoning?
atropine + pralidoxime
43
muscarinic antagonists
inhibit postsynaptic action of ACh.
44
atropine, homatropine, tropicamide
muscarinic antagonists. | eye - produce mydriasis and cycloplegia (loss of accomm).
45
benztropine
muscarinic antagonists. CNS - parkinson disease. "park my benz"
46
scopolamine
muscarinic antagonists. | CNS - motion sickness.
47
ipratropium
muscarinic antagonists. | resp - asthma, COPD.
48
oxybutynin, glycopyrrolate
muscarinic antagonists. | GU - reduce urgency in mild cystitis. reduce bladder spasms.
49
methscopolamine, pirenzepine, propantheline
muscarinic antagonists. | GI - peptic ulcer tx.
50
atropine
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
epinephrine action
``` direct sympathomimetic. a1: ++++ a2: ++++ b1: ++++ b2: ++++ D1: 0 ```
52
epinephrine use
anaphylaxis. glaucoma (open angle). asthma. hypotension.
53
norepinephrine action
``` direct sympathomimetic. a1: ++++ a2: ++++ b1: ++ b2: 0 D1: 0 ```
54
NE use
hypotension - but decreases renal perfusion
55
isoproterenol action
``` direct sympathomimetic. a1: 0 a2: 0 b1: ++++ b2: ++++ D1: 0 ```
56
isoproterenol use
AV block (rare)
57
dopamine action
``` 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
dopamine use
shock (renal perfusion). heart failure. inotropic and chronotropic effects.
59
dobutamine action
``` direct sympathomimetic. a1: + a2: + b1: ++++ b2: + D1: 0 ```
60
dobutamine use
heart failure. cardiac stress testing. inotropic and chronotropic effects.
61
phenylephrine action
``` direct sympathomimetic. a1: ++++ a2: ++ b1: 0 b2: 0 D1: 0 ```
62
phenylephrine use
ocular procedures - mydriatic effect. hypotension - vasoconstrictive. rhinitis - nasal decongestant.
63
Metaproteronol Albuterol Salmeterol Terbutaline action
``` direct sympathomimetic. a1: 0 a2: 0 b1: ++ b2: ++++ D1: 0 ```
64
Metaproteronol Albuterol Salmeterol Terbutaline use
Metaproteronol and Albuterol for acute asthma. Salmeterol for long-term tx. Terbutaline to reduce premature uterine contractions.
65
ritodrine action
``` direct sympathomimetic. a1: 0 a2: 0 b1: 0 b2: ++++ D1: 0 ```
66
ritodrine use
reduces premature uterine contractions.
67
amphetamine action
indirect sympathomimetic. | indirect general agonist, releases stored catecholamines.
68
amphetamine use
narcolepsy. obesity. ADD.
69
ephedrine action
indirect sympathomimetic. | indirect general agonist, releases stored catecholamines.
70
ephedrine use
nasal decongestion. urinary incontinence. hypotension.
71
cocaine action
indirect general agonist. | uptake inhibitor.
72
cocaine use
causes vasoconstriction and local anesthesia.
73
sympathoplegics: clonidine, alpha-methyldopa
centrally acting a2-agonists. decrease central adrenergic outflow. for HTN, esp with renal disease (no decrease in bld flow to kidney).
74
nonselective alpha blockers
phenoxybenzamine (irreversible). | phentolamine (reversible).
75
phenoxybenzamine use
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
phentolamine use
give to pts on MAO inhibitors who eat tyramine-containing food
77
alpha1-selective blockers
-zosin: prazosin, terazosin, doxazosin use: HTN, urinary retention in BPH. tox: 1st dose orthostatic hypotension, dizziness, HA.
78
alpha2-selective blockers
mirtazapine. use: depression. tox: sedation, increased serum chol, increased appetite.
79
beta1-selective blockers
``` b1 > b2 Acebutolol (partial agonist). Betaxolol. Esmolol (short acting). Atenolol. Metoprolol. ``` "A BEAM of b1-blockers" good for pts with comorbid pulmo dz.
80
nonselective beta antagonists
``` b1 = b2 Propanolol. Timolol. Nadolol. Pindolol. ``` Please Try Not being Picky.
81
nonselective mixed alpha-beta antagonists
carvedilol, labetolol. vasodilatory effects.
82
partial beta agonists
pindolol, acebutolol.
83
BB for HTN
``` decrease CO. decrease renin (beta block on JGA cells). ```
84
BB for angina pectoris
decrease HR and contractility, resulting in decreased O2 consumption
85
BB for MI
decrease mortality
86
BB for SVT
[propanolol, esmolol] decrease AV conduction velocity [class II antiarrhythmics]
87
BB for CHF
slow progression of chronic failure
88
BB for glaucoma
[timolol] decrease secretion of aqueous humor
89
BB toxicity
``` impotence. exacerbation of asthma. hypotension. CV: bradycardia, AV block, CHF. CNS: sedation, sleep alterations. ``` *caution in diabetics
90
BB antidote
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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