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Pharma Review > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

1
Q

A1 Receptor (location, action, preferred substrate)

A

location: smooth muscle
action: vasoconstriction
preferred substrate: Epi> NE

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2
Q

A2 Receptor (location, action, preferred substrate)

A

location: nerve terminals
action: inhibits release of neurotransmitters
preferred substrate: Epi> NE

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3
Q

B1 Receptor (location, action, preferred substrate)

A

location: heart
action: increase rate and contractility
preferred substrate: isoproterenol>Epi>NE

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4
Q

B2 Receptor (location, action, preferred substrate)

A

location: respiratory smooth muscles; uterus
action: broncho/vasodilation, uterine relaxation
preferred substrate: isoproterenol>Epi>NE

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5
Q

B3 Receptor (location)

A

location: brown fat

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6
Q

D1 Receptor (location, action, preferred substrate)

A

location: splanchnic and renal vessels
action: vasodilation of renal blood vessels
preferred substrate: dopamine

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7
Q

D2 Receptor (location, action, preferred substrate)

A

location: nerve terminals of CNS
action: regulates neurotransmitters
preferred substrate: dopamine

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8
Q

M1 Receptor (location, action, preferred substrate)

A

location: CNS
action: stimulation
preferred substrate: ACH

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9
Q

M2 Receptor (location, action, preferred substrate)

A

location: heart
action: decrease HR
preferred substrate: ACH

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10
Q

M3 Receptor (location, action, preferred substrate)

A

location: smooth muscle: GI, GU, Pulmo, Eye
action: gut peristalsis, bladder contraction, bronchoconstriction, pupil constriction
preferred substrate: isoproterenol>Epi>NE

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11
Q

Cholinergic inhibitors steps: synthesis

A

hemicholinium

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12
Q

Cholinergic inhibitors steps: storage

A

vesamicol

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13
Q

Cholinergic inhibitors steps: release

A

botulinum

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14
Q

Cholinergic inhibitors steps: termination (metabolism)

A

neostigmine

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15
Q

Cholinergic inhibitors steps: termination (reuptake)

A

none

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16
Q

Adrenergic inhibitors steps: synthesis

A

metyrosine

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17
Q

Adrenergic inhibitors steps: storage

A

reserpine

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18
Q

Adrenergic inhibitors steps: release

A

guanethidine

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19
Q

Adrenergic inhibitors steps: termination (metabolism)

A

MAOIs, COMTIs

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20
Q

Adrenergic inhibitors steps: termination (reuptake)

A

Cocaine, TCAs

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21
Q

[Cholinergic drugs]
bowel and bladder atony
MOA: direct acting M agonist, M2-M3

A

Bethanecol
“B= Bethanecol = bowel and bladder atony”
(carbacol for glaucoma)

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22
Q

[Cholinergic drugs]
Sjorgen syndrome (xerostomia, xerophthalmia and rheumatoid arthritis)
MOA: direct acting M agonist, M1 M2 M3
“cry, drool, sweat on your pillow”

A

Pilocarpine

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23
Q

[Cholinergic drugs]
diagnosis of myasthenia gravis, differentiation of myastenic and cholinergic crisis (indirect acting cholinomimetic)
“tensilon test”

A

Edrophonium

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24
Q

[Cholinergic drugs]

treatment of myasthenia gravis

A

Pyridostigmine

“-stigmine”

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25
Q

[Cholinergic drugs]

Reversal of nondepolarizing neuromuscular block

A

Neostigmine

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26
Q

[Cholinergic drugs]

treatment of glaucoma

A

[PLE-TSU]
Physostigmine, Pilocarpine - trabecular meshwork
Latanoprost - schlemm
Epinephrine - uveoscleral vein

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27
Q

[Cholinergic drugs]

diagnosis of bronchial hyperreactivity (direct acting M agonist, M3)

A

methacoline

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28
Q

[Cholinergic drugs]

treatment of Alzheimer disease (Acetylcholinesterase inhibitor)

A

Donepezil

Rivastigmine (patch)

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29
Q

How does EDROPHONIUM differentiate myasthenic crisis from cholinergic crisis?

A

EDROPHONIUM
IMPROVES muscle strength in myasthenic crisis
WEAKENS muscle strength in cholinergic crisis

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30
Q

Small cell cancer may present with a myasthenia-like paraneoplastic syndrome. What is this condition called?

A

Lambert-Eaton Syndrome

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31
Q

What are the signs and symptoms of organophosphate poisoning?

A 
DUMBBELSS
diarrhea
urination
miosis
bronchospasm
bradycardia
excitation (skeletal muscle and CNS) & Emesis
lacrimation
sweating
salivation
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32
Q

[Cholinergic Antagonists]

induction of mydriasis(innervation of radial muscles) and cycloplegia (loss of accommodation)

A

tropicamide

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33
Q

[Cholinergic Antagonists]

Parkinsons disease

A

Biperiden

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34
Q

[Cholinergic Antagonists]

Sinus bradycardia

A

atropine

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35
Q

[Cholinergic Antagonists]

Chronic obstructive pulmonary disease(COPD)

A

Ipratropium

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36
Q

[Cholinergic Antagonists]

Motion sickness, sea sickness

A

Scopolamine

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37
Q

[Cholinergic Antagonists]

Gastrointestinal spasms

A

hyoscyamine, HNBB (Hyoscine N-butylbromide)

“glycopyrrolate”

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38
Q

[Cholinergic Antagonists]

treatment for organophosphate poisoning/ nerve gas poisoning

A

Pralidoxime + Atropine

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39
Q

Muscarinic Antagonists for Parkinson Disease

A

“Try to Park your Benz, beep here.”
TRIhexyphenidyl
BENZtropine
BIPeriden

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40
Q

Why is Ipratropium the preferred bronchodilator in patients with comorbid COPD and heart disease?

A

Ipratropium is less likely to cause tachycardia and cardiac arrhythmia

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41
Q

What are the signs of atropine toxicity?

A 
HOT as a hare
DRY as a bone
RED as a beet
BLIND as a bat
MAD as a hatter
42
Q

Contraindications to muscarinic blockers

A

cautious use in infants,
acute angle-closure glaucoma,
benign prostatic hyperplasia

43
Q

[Adrenergic Agonists]

drug of choice for anaphylactic shock, adjunct to local anesthesia, cardiac arrest, croup

A

epinephrine

44
Q

[Adrenergic Agonists]

acute CHF, cardiac stress testing

A

dobutamine

45
Q

[Adrenergic Agonists]

acute CHF, shock (cardiogenic, septic)

A

dopamine

46
Q

[Adrenergic Agonists]
Alpha> Beta receptor affinity

uses: neurogenic shock
SE: reflex bradycardia (baroreceptor mechanism to achieve hemostasis)

A

norepinephrine

47
Q

[Adrenergic Agonists]

nasal congestion, mydriasis without cycloplegia

A

phenylephrine

antidote: phentolamine

48
Q

[Adrenergic Agonists]

SE: rebound hypertension on discontinuation

A

clonidine

antidote: phentolamine

49
Q

[Adrenergic Agonists]

SE: hemolytic anemia (positive Coombs test)

A

methyldopa

50
Q

[Adrenergic Agonists]
bronchial asthma, COPD

acute asthma attack DOC

A

salbutamol

51
Q

[Adrenergic Agonists]

tocolysis for preterm labor

A

terbutaline
ritodrine
isoxuprine

52
Q

Direct NON-SELECTIVE Adrenergics/Sympathomimetics

A 
"DINE"
Dopamine
Isoproterenol
Norepinephrine
Epinephrine
53
Q

Epinephrine MOA

A

Epinephrine MOA

A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility
B2: bronchodilation

  • can cross placenta (may cause fetal anoxia)
54
Q

Norepinephrine MOA

A

Norepinephrine MOA

A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility

55
Q

Dopamine MOA

A

Dopamine MOA

A1: vasoconstriction, increase BP
B1: increase HR, conduction and contractility
D1: vasoDilation in splanchnic and renal blood vessels

56
Q

Isoproterenol MOA

A

non selective beta adrenergic receptors activator
B1: increase HR, conduction and contractility
B2: bronchodilation

uses: asthma

57
Q

Direct ALPHA 1 Adrenergics/Sympathomimetics drugs

A 
Phenylephrine
pseudophedrine
oxymetazoline
tetrahydrozoline
midrodine
naphazoline
xylometazoline
58
Q

Direct ALPHA 1 Adrenergics/Sympathomimetics MOA

A 
Phenylephrine
pseudophedrine
oxymetazoline
tetrahydrozoline
midrodine
naphazoline
xylometazoline

MOA:
A1: vasoconstriction, increase BP

SE: rebound nasal congestion (rhinitis medicamentosa)

  • avoid PSEUDOEPHEDRINE in 1st term, may cause gastroschisis
  • Phentolamine - DOC for A1 agonist overdose
59
Q

Direct ALPHA 2 Adrenergics/Sympathomimetics drugs

A

“CAM”
Clonidine
Apraclonidine (+ brimonidine)
Methyldopa (+guanfacine, guanabenz, dexmedetomidine, tizanidine)

60
Q

Direct ALPHA 2 Adrenergics/Sympathomimetics:
CLONIDINE
MOA

A

Direct ALPHA 2 Adrenergics/Sympathomimetics:
CLONIDINE

MOA:
A2: decrease central sympathetic outlfow

*treat rebound HPN with phentolamine

61
Q

Direct ALPHA 2 Adrenergics/Sympathomimetics:
METHYLDOPA, guanfacine, guanabenz, dexmedetomidine, tizanidine
MOA

A

Direct ALPHA 2 Adrenergics/Sympathomimetics:
METHYLDOPA, guanfacine, guanabenz, dexmedetomidine, tizanidine

MOA:
A2: decrease central sympathetic outlfow

uses: preeclampsia, GHPN,
dexmedetomidine- used for conscious sedation
tizanidine- used for muscle relaxant

SE: sedation, hemolytic anemia, (+) coomb’s test

62
Q

Direct ALPHA 2 Adrenergics/Sympathomimetics:
APRACLONIDINE, Brimonidine
MOA

A

Direct ALPHA 2 Adrenergics/Sympathomimetics:
APRACLONIDINE, Brimonidine

MOA: decrease secretion of aqueous humor
uses: glaucoma

63
Q

Direct BETA 1 Adrenergics/Sympathomimetics drug

A

Direct BETA 1 Adrenergics/Sympathomimetics drug

dobutamine

64
Q

Direct BETA 2 Adrenergics/Sympathomimetics drug

A

Direct BETA 2 Adrenergics/Sympathomimetics drug

salbutamol
albuterol
terbutaline
isoxuprine
ritodrine
65
Q

Direct BETA 2 Adrenergics/Sympathomimetics
salbutamol, albuterol, terbutaline, isoxuprine, ritodrine
MOA

A

Direct BETA 2 Adrenergics/Sympathomimetics
salbutamol, albuterol, terbutaline, isoxuprine, ritodrine

MOA:
B2: bronchodilation

uses:
salbutamol- acute asthma attack DOC

66
Q

used as vasodilator in Reynaud’s phenomenon; may cause maternal pulmonary edema

A

isoxuprine

67
Q

most common SE of B2 agonists

A

muscle tremor, palpitations

68
Q

Indirect adrenergics/sympathomimetics (releasers)

A

Phenylpropanolamine

69
Q

Indirect adrenergics/sympathomimetics (releasers): Phenylpropanolamine MOA

A

Indirect adrenergics/sympathomimetics (releasers): Phenylpropanolamine

MOA: act mainly by causing release of NE, but also has direct agonist activity at some adrenergic receptors; activates A and B adrenergic receptors in respi mucosa

uses: nasal vasoconstrictor, appetite suppressant
* may precipitate hemorrhagic stroke especially in women

70
Q

[Dose dependent action of dopamine]

vasodilation in the splanchnic and renal vascular beds via D1 receptors

A

low dose (1-5 mcg/kg/min)

71
Q

[Dose dependent action of dopamine]

increased renal blood flow and urine output

A

low dose (1-5 mcg/kg/min)

72
Q

[Dose dependent action of dopamine]

increased renal blood flow, heart rate, cardiac contractility, and cardiac output via B1 receptors

A

medium dose (5-15 mcg/kg/min)

73
Q

[Dose dependent action of dopamine]

vasoconstriction and increased blood pressure via alpha receptors

A

high dose (>15 mcg/kg/min)

74
Q

[Adrenergic Antagonist]

preoperative treatment if pheochromocytoma

A

phenoxybenzamine (non-selective, irreversible)

75
Q

[Adrenergic Antagonist]

treatment of rebound hypertension

A

phentolamine
tolazoline
(non-selective, reversible)

76
Q

[Adrenergic Antagonist]
benign prostatic hyperplasia
SE: first dose orthostatic hypotension

A 
"-osin"
prazosin
doxazosin
terazosin
tamsulosin
silodosin
alfuzosin
77
Q

[Adrenergic Antagonist]

most selective for prostatic smooth muscle

A

tamsulosin

78
Q

[Adrenergic Antagonist]

not indicated in females for treatment of hypertension

A 
Alpha 1 selective adrenergic antagonists
"-osin"
doxazosin
tamsulosin
silodosin
alduzosin
79
Q

[Adrenergic Antagonist]

  • used for angina prophylaxis, hyperthyroidism
  • masks hypOglycemia in diabetics

SE: bronchospasm, erectile dysfunction

A 
nonselective beta adrenergic antagonists
(L-Z except Carvedilol and Carteolol)
propranolol
pindolol
timolol
labetalol
carvedilol
nadolol
levobunolol
metipranolol
carteolol
80
Q

[Adrenergic Antagonist]

combined alpha and beta blockade (may be used in pheochromocytoma)

A

“CL”
carvedilol
labetalol

81
Q

[Adrenergic Antagonist]
adverse effects: IUGR, small placenta and congenital abnormalities have been reported with use, but no adequate and well-contracted studies conducted

A

Propranolol

82
Q

[Adrenergic Antagonist]

used as ophthalmic drops for glaucoma

A

metipranolol

83
Q

[Adrenergic Antagonist]

has longest half-life

A

“NAsa DOLO”

Nadolol

84
Q

Beta blockers with intrinsic sympathomimetic (partial agonist) activity

A

“ISA PA! isa pa! isa pang chicken joy”

Intrinsic sympathomimetic activity = Pindolol, Acebutolol

85
Q

[Adrenergic Antagonist]

Beta 1 selectivity

A 
beta 1 selectivity:
(A-K except Metoprolol and Nebivolol)
atenolol
betaxolol
esmolol
acebutol
metoprolol
alprenolol
nebivolol
bisoprolol
"NBEAM"
86
Q

Beta 1 adrenergic antagonist (beta 1 blocker) with shortest half-life

A

“Esmall-LOL”

esmolol

87
Q

Beta 1 adrenergic antagonist (beta 1 blocker) that may also be used as ophthalmic solution for glaucoma

A

betaxolol

88
Q

use of this cardioselective beta blocker during pregnancy has been shown to lower birthweights and impair fetal growth

A

atenolol

89
Q

nonselective beta blocker used to treat glaucoma

A

timolol

-lack local anesthetic effect

90
Q

What drugs are used to control blood pressure in pheochromocytoma?

A

phenoxybenzamine
phentolamine
labetalol

91
Q

what is the pharmacologic advantage of alpha 1 selectivity?

A

reflex tachycardia is less common and less severe

92
Q

non selective adrenergic antagonist

A

propranolol, timolol

93
Q

beta1 selective adrenergic antagonist

A

acebutolol, betaxolol, esmolol, atenolol, metoprolol

94
Q

[adrenergic antagonist]

partial agonist

A

pindolol, acebutolol

95
Q

[adrenergic antagonist]

lacking local anesthetic

A

timolol

96
Q

[adrenergic antagonist]

low lipid solubility

A

atenolol

97
Q

[adrenergic antagonist]

shortest-acting

A

esmolol

98
Q

[adrenergic antagonist]

longest-acting

A

nadolol

99
Q

[adrenergic antagonist]

combined alpha and beta blockade

A

carvedilol, labetalol

100
Q

a nonselective beta AGONIST

A

isoproterenol

Pharma Review (15 decks)

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