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
[Cholinergic drugs] | Reversal of nondepolarizing neuromuscular block
Neostigmine
26
[Cholinergic drugs] | treatment of glaucoma
[PLE-TSU] Physostigmine, Pilocarpine - trabecular meshwork Latanoprost - schlemm Epinephrine - uveoscleral vein
27
[Cholinergic drugs] | diagnosis of bronchial hyperreactivity (direct acting M agonist, M3)
methacoline
28
[Cholinergic drugs] | treatment of Alzheimer disease (Acetylcholinesterase inhibitor)
Donepezil | Rivastigmine (patch)
29
How does EDROPHONIUM differentiate myasthenic crisis from cholinergic crisis?
EDROPHONIUM IMPROVES muscle strength in myasthenic crisis WEAKENS muscle strength in cholinergic crisis
30
Small cell cancer may present with a myasthenia-like paraneoplastic syndrome. What is this condition called?
Lambert-Eaton Syndrome
31
What are the signs and symptoms of organophosphate poisoning?
``` DUMBBELSS diarrhea urination miosis bronchospasm bradycardia excitation (skeletal muscle and CNS) & Emesis lacrimation sweating salivation ```
32
[Cholinergic Antagonists] | induction of mydriasis(innervation of radial muscles) and cycloplegia (loss of accommodation)
tropicamide
33
[Cholinergic Antagonists] | Parkinsons disease
Biperiden
34
[Cholinergic Antagonists] | Sinus bradycardia
atropine
35
[Cholinergic Antagonists] | Chronic obstructive pulmonary disease(COPD)
Ipratropium
36
[Cholinergic Antagonists] | Motion sickness, sea sickness
Scopolamine
37
[Cholinergic Antagonists] | Gastrointestinal spasms
hyoscyamine, HNBB (Hyoscine N-butylbromide) | "glycopyrrolate"
38
[Cholinergic Antagonists] | treatment for organophosphate poisoning/ nerve gas poisoning
Pralidoxime + Atropine
39
Muscarinic Antagonists for Parkinson Disease
"Try to Park your Benz, beep here." TRIhexyphenidyl BENZtropine BIPeriden
40
Why is Ipratropium the preferred bronchodilator in patients with comorbid COPD and heart disease?
Ipratropium is less likely to cause tachycardia and cardiac arrhythmia
41
What are the signs of atropine toxicity?
``` HOT as a hare DRY as a bone RED as a beet BLIND as a bat MAD as a hatter ```
42
Contraindications to muscarinic blockers
cautious use in infants, acute angle-closure glaucoma, benign prostatic hyperplasia
43
[Adrenergic Agonists] | drug of choice for anaphylactic shock, adjunct to local anesthesia, cardiac arrest, croup
epinephrine
44
[Adrenergic Agonists] | acute CHF, cardiac stress testing
dobutamine
45
[Adrenergic Agonists] | acute CHF, shock (cardiogenic, septic)
dopamine
46
[Adrenergic Agonists] Alpha> Beta receptor affinity uses: neurogenic shock SE: reflex bradycardia (baroreceptor mechanism to achieve hemostasis)
norepinephrine
47
[Adrenergic Agonists] | nasal congestion, mydriasis without cycloplegia
phenylephrine antidote: phentolamine
48
[Adrenergic Agonists] | SE: rebound hypertension on discontinuation
clonidine antidote: phentolamine
49
[Adrenergic Agonists] | SE: hemolytic anemia (positive Coombs test)
methyldopa
50
[Adrenergic Agonists] bronchial asthma, COPD acute asthma attack DOC
salbutamol
51
[Adrenergic Agonists] | tocolysis for preterm labor
terbutaline ritodrine isoxuprine
52
Direct NON-SELECTIVE Adrenergics/Sympathomimetics
``` "DINE" Dopamine Isoproterenol Norepinephrine Epinephrine ```
53
Epinephrine MOA
Epinephrine MOA A1: vasoconstriction, increase BP B1: increase HR, conduction and contractility B2: bronchodilation - can cross placenta (may cause fetal anoxia)
54
Norepinephrine MOA
Norepinephrine MOA A1: vasoconstriction, increase BP B1: increase HR, conduction and contractility
55
Dopamine MOA
Dopamine MOA A1: vasoconstriction, increase BP B1: increase HR, conduction and contractility D1: vasoDilation in splanchnic and renal blood vessels
56
Isoproterenol MOA
non selective beta adrenergic receptors activator B1: increase HR, conduction and contractility B2: bronchodilation uses: asthma
57
Direct ALPHA 1 Adrenergics/Sympathomimetics drugs
``` Phenylephrine pseudophedrine oxymetazoline tetrahydrozoline midrodine naphazoline xylometazoline ```
58
Direct ALPHA 1 Adrenergics/Sympathomimetics MOA
``` 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
Direct ALPHA 2 Adrenergics/Sympathomimetics drugs
"CAM" Clonidine Apraclonidine (+ brimonidine) Methyldopa (+guanfacine, guanabenz, dexmedetomidine, tizanidine)
60
Direct ALPHA 2 Adrenergics/Sympathomimetics: CLONIDINE MOA
Direct ALPHA 2 Adrenergics/Sympathomimetics: CLONIDINE MOA: A2: decrease central sympathetic outlfow *treat rebound HPN with phentolamine
61
Direct ALPHA 2 Adrenergics/Sympathomimetics: METHYLDOPA, guanfacine, guanabenz, dexmedetomidine, tizanidine MOA
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
Direct ALPHA 2 Adrenergics/Sympathomimetics: APRACLONIDINE, Brimonidine MOA
Direct ALPHA 2 Adrenergics/Sympathomimetics: APRACLONIDINE, Brimonidine MOA: decrease secretion of aqueous humor uses: glaucoma
63
Direct BETA 1 Adrenergics/Sympathomimetics drug
Direct BETA 1 Adrenergics/Sympathomimetics drug dobutamine
64
Direct BETA 2 Adrenergics/Sympathomimetics drug
Direct BETA 2 Adrenergics/Sympathomimetics drug ``` salbutamol albuterol terbutaline isoxuprine ritodrine ```
65
Direct BETA 2 Adrenergics/Sympathomimetics salbutamol, albuterol, terbutaline, isoxuprine, ritodrine MOA
Direct BETA 2 Adrenergics/Sympathomimetics salbutamol, albuterol, terbutaline, isoxuprine, ritodrine MOA: B2: bronchodilation uses: salbutamol- acute asthma attack DOC
66
used as vasodilator in Reynaud's phenomenon; may cause maternal pulmonary edema
isoxuprine
67
most common SE of B2 agonists
muscle tremor, palpitations
68
Indirect adrenergics/sympathomimetics (releasers)
Phenylpropanolamine
69
Indirect adrenergics/sympathomimetics (releasers): Phenylpropanolamine MOA
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
[Dose dependent action of dopamine] | vasodilation in the splanchnic and renal vascular beds via D1 receptors
low dose (1-5 mcg/kg/min)
71
[Dose dependent action of dopamine] | increased renal blood flow and urine output
low dose (1-5 mcg/kg/min)
72
[Dose dependent action of dopamine] | increased renal blood flow, heart rate, cardiac contractility, and cardiac output via B1 receptors
medium dose (5-15 mcg/kg/min)
73
[Dose dependent action of dopamine] | vasoconstriction and increased blood pressure via alpha receptors
high dose (>15 mcg/kg/min)
74
[Adrenergic Antagonist] | preoperative treatment if pheochromocytoma
phenoxybenzamine (non-selective, irreversible)
75
[Adrenergic Antagonist] | treatment of rebound hypertension
phentolamine tolazoline (non-selective, reversible)
76
[Adrenergic Antagonist] benign prostatic hyperplasia SE: first dose orthostatic hypotension
``` "-osin" prazosin doxazosin terazosin tamsulosin silodosin alfuzosin ```
77
[Adrenergic Antagonist] | most selective for prostatic smooth muscle
tamsulosin
78
[Adrenergic Antagonist] | not indicated in females for treatment of hypertension
``` Alpha 1 selective adrenergic antagonists "-osin" doxazosin tamsulosin silodosin alduzosin ```
79
[Adrenergic Antagonist] - used for angina prophylaxis, hyperthyroidism - masks hypOglycemia in diabetics SE: bronchospasm, erectile dysfunction
``` nonselective beta adrenergic antagonists (L-Z except Carvedilol and Carteolol) propranolol pindolol timolol labetalol carvedilol nadolol levobunolol metipranolol carteolol ```
80
[Adrenergic Antagonist] | combined alpha and beta blockade (may be used in pheochromocytoma)
"CL" carvedilol labetalol
81
[Adrenergic Antagonist] adverse effects: IUGR, small placenta and congenital abnormalities have been reported with use, but no adequate and well-contracted studies conducted
Propranolol
82
[Adrenergic Antagonist] | used as ophthalmic drops for glaucoma
metipranolol
83
[Adrenergic Antagonist] | has longest half-life
"NAsa DOLO" | Nadolol
84
Beta blockers with intrinsic sympathomimetic (partial agonist) activity
"ISA PA! isa pa! isa pang chicken joy" | Intrinsic sympathomimetic activity = Pindolol, Acebutolol
85
[Adrenergic Antagonist] | Beta 1 selectivity
``` beta 1 selectivity: (A-K except Metoprolol and Nebivolol) atenolol betaxolol esmolol acebutol metoprolol alprenolol nebivolol bisoprolol "NBEAM" ```
86
Beta 1 adrenergic antagonist (beta 1 blocker) with shortest half-life
"Esmall-LOL" | esmolol
87
Beta 1 adrenergic antagonist (beta 1 blocker) that may also be used as ophthalmic solution for glaucoma
betaxolol
88
use of this cardioselective beta blocker during pregnancy has been shown to lower birthweights and impair fetal growth
atenolol
89
nonselective beta blocker used to treat glaucoma
timolol | -lack local anesthetic effect
90
What drugs are used to control blood pressure in pheochromocytoma?
phenoxybenzamine phentolamine labetalol
91
what is the pharmacologic advantage of alpha 1 selectivity?
reflex tachycardia is less common and less severe
92
non selective adrenergic antagonist
propranolol, timolol
93
beta1 selective adrenergic antagonist
acebutolol, betaxolol, esmolol, atenolol, metoprolol
94
[adrenergic antagonist] | partial agonist
pindolol, acebutolol
95
[adrenergic antagonist] | lacking local anesthetic
timolol
96
[adrenergic antagonist] | low lipid solubility
atenolol
97
[adrenergic antagonist] | shortest-acting
esmolol
98
[adrenergic antagonist] | longest-acting
nadolol
99
[adrenergic antagonist] | combined alpha and beta blockade
carvedilol, labetalol
100
a nonselective beta AGONIST
isoproterenol