Autonomics Flashcards
1
Q
M1/M3/M5 second messenger?
A
Gq –> PLC –> DAG & IP3 –> Calcium release
2
Q
M2/M4 second messenger?
A
Gi –> Inhibit AC –> Decreased cAMP; Kchannel –> Hyperpolarization
3
Q
Alpha 1 second messenger?
A
Gq –> PLC –> DAG & IP3 –> Calcium release
4
Q
Alpha 2 second messenger?
A
Gi –> inhibit AC –> Decreased cAMP; Kchannel –> Hyperpolarization
5
Q
Use Gi as second messenger?
A
M2/M4 & Alpha 2
6
Q
Use Gq as second messenger?
A
M1/M3/M5 & Alpha 1
7
Q
B1/B2/B3 second messenger?
A
Gs –> Stimulate AC –> Increase cAMP
8
Q
Bethanechol class?
A
Direct acting carbamic acid ester (direct acting muscarinic cholinomimetic)
9
Q
Muscarine class?
A
Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)
10
Q
Pilocarpine class?
A
Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)
11
Q
Cevimeline class?
A
Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)
12
Q
Nicotine class?
A
Direct acting non-ester alkaloid (direct acting nicotinic cholinomimetic)
13
Q
Bethanechol treats?
A
Post-op and neurogenic ileus; urinary retention (bowel & bladder smooth muscle ACh-innervated)
14
Q
Pilocarpine treats?
A
Glaucoma (ACh activates sphincter & ciliary muscles of eye)
15
Q
Cevimeline treats?
A
Dry mouth (Sjogren’s, post-radiation therapy) via increased salivation
16
Q
Nicotine treats?
A
Smoking cessation via reduced cravings
17
Q
Side effects of direct acting muscarinic cholinomimetics?
A
SLUDGE: Salivation, Lacrimation, Urination, Defecation, GI distress, Emesis
18
Q
Direct acting muscarinic cholinomimetics?
A
Bethanechol, Muscarine, Pilocarpine, Cevimeline
19
Q
Neostigimine class?
A
Indirect acting carbamate (AChE inhibitor)
20
Q
Physosligmine class?
A
Indirect acting carbamate (AChE inhibitor)
21
Q
Donepezil class?
A
Indirect acting non-ester (AChE inhibitor)
22
Q
Edrophonium class?
A
Indirect acting non-ester alcohol (AChE inhibitor)
23
Q
Echothiophate class?
A
Indirect acting organophosphate (AChE inhibitor)
24
Q
Pralidoxime class?
A
Strong nucleophile and regenerates phosphorylated AChE
25
Sarin class?
Potent indirect acting organophosphate (AChE inhibitor)
26
Neostigmine treats?
Post-op and neurogenic ileus; urinary retention; myasthenia gravis; reversal of NMJ blockade
27
Neostigmine time?
Lasts 0.5-2 hours
28
Physostigmine treats?
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
29
Physostigmine time?
Lasts 0.5-2 hours
30
Donepezil treats?
Alzheimer's (amplifies endogenous ACh in brain)
31
Edrophonium treats?
Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus
32
Edrophonium time?
Lasts 5-15 minutes
33
Echothiophate treats?
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
34
Echothiophate time?
Lasts >100 hours
35
Pralidoxime treats?
Poisoning by nerve gas (also an insecticide)
36
Sarin can be used as?
Volatile nerve gas
37
Sarin can cause?
Death
38
Sarin toxicity treated how?
Treat with pralidoxime and atropine before aging
39
Side effects of AChE inhibitors?
SLUDGE + general increase in cholinergic neurotransmission; paralysis
40
Long acting AChE inhibitor?
Echothiophate
41
Short acting AChE inhibitors?
Neostigmine, Physostigmine, Edrophonium
42
Atropine class?
Tertiary amine antimuscarinic
43
Scopolamine class?
Tertiary amine antimuscarinic
44
Dicyclomine class?
Tertiary amine antimuscarinic
45
Tropicamide class?
Tertiary amine antimuscarinic
46
Tolterodine class?
Tertiary amine antimuscarinic
47
Benztropne class?
Tertiary amine antimuscarinic
48
Side effects of tertiary amine antimuscarinics?
General block of muscarinic functions
49
Tertiary amine antimuscarinics?
Atropine, Scopolamine, Dicyclomine, Tropicamide, Tolterodine, Benztropine
50
Atropine treats?
Mydriasis, cycloplegia
51
Scopolamine treats?
Prevent or reduce motion sickness
52
Dicyclomine treats?
Reduce transient hypermotility
53
Tropicamide treats?
Mydriasis, cycloplegia
54
Tolterodine treats?
Transient cystitis, post-op bladder spasms, incontinence
55
Benztropine treats?
Manifestations of Parkinson's
56
Tertiary amine antimuscarinics that cross the BBB?
Scopolamine, Benztropine
57
Metabolism of scopolamine?
Slow
58
Metabolism of tropicamide?
Rapid
59
Quarternary amine antimuscarinics?
Ipratropium, Tiotropium
60
Ipratropium class?
Quarternary amine antimuscarinic
61
Tiotropium class?
Quarternary amine antimuscarinic
62
Which quarternary amine antimuscarinic is longer acting?
Tiotropium
63
Ipratropium and tiotropium treat?
Bronchodilation in asthma or COPD
64
Ipratropium and triotropium side effects?
General block of muscarinic effects
65
Ganglionic blockers?
Hexamethonium, Mecamylamine
66
Hexamethonium, Mecamylamine mxn?
Block Nn receptor and sympathetic tone
67
Hexamethonium, Mecamylamine treat?
Hypertenisve crisis ("Bloodless" field surgery)
68
Succinylcholine class?
Depolarizing blocker
69
How do depolarizing blockers work?
Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation
70
Succinylcholine used for?
Brief procedures (tracheal intubation, reset dislocated joints?
71
Side effects of succinylcholine?
Respiratory paralysis, disturbance of autonomic function, flaccid paralysis within minutes
72
Tubocurarine class?
Nondepolarizing blocker (Block Nm receptor)
73
Mivacurium class?
Nondepolarizing blocker (Block Nm receptor)
74
Nm blockers?
Tubocurarine, Mivacurium
75
Tubocurarine, Mivacurium used for?
Muscle relaxant for surgery w/o deep anasthesia
76
Tubocurarine, Mivacurium side effects?
Respiratory paralysis, disturbance of autonomic function
77
Tubocurarine time?
Lasts 30-60 minutes
78
Mivacurium inhibitor?
Rapidly hydrolyzed, short-lasting
79
Botulinum toxin A class and mxn?
Local paralytic: Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
80
Botulinum tonxin A treats?
Reduces frown lines and wrinkles, achalasia, strabismus, oromandibular dystonia
81
ANS activity in the SA node?
Symp accelerate B1,B2. Parasymp decelerate M2
82
ANS activity in the contractility of the heart?
Symp increase B1,B2. Parasymp decelerate M2 (atria).
83
ANS activity in the blood vessels?
Symp contract skin vessels alpha. Symp relax skeletal muscle vessels B2. Parasymp release EDRF relax vessels M3 (not innervated and responds only to circulating muscarinic agonists)
84
ANS activity in bronchiolar smooth muscle?
Symp relax B2. Parasymp contract M3.
85
ANS activity in GI?
Symp relax smooth muscle contract sphictors. Parasymp contract smooth muscle relax sphinctors + secretion.
86
ANS activity in GU smooth muscle?
Symp relax bladder wall B2, contract sphinctor a1. Parasymp contract bladder wall M3, relax sphinctor M3. Symp relax uterus B2, contract uterus a. Parasymp contract uterus M3.
87
ANS activity in the eye?
Symp dilate relax ciliary muscle B. Parasymp constrict contract ciliary muscle M3.
88
Beta 1?
Heart (Increase HR, Increase contraction). Kidney (Renin secretion)
89
Beta 2?
Arterioles (Dilate). Bronchial smooth muscle (Relax). Uterus (Relax). Increase metabolic effects.
90
Beta 3?
Increase lipolysis and thermogenesis.
91
Alpha 1?
Arterioles (Constrict). Veins (Constrict). Uterus (Constrict).
92
Alpha 2?
Presynaptic Nerve Endings (Inhibit NE Release and ACh release). Postsynaptic in CNS (Decreased peripheral Sympathetic Tone)
93
Dopamine?
Renal, mesenteric, cerebral arterioles (Dilate).
94
Tell me about skeletal muscle blood vessel receptors and response.
Alpha1 and Beta2. At physiological concentration (of epi), Beta2 predominates and vasodilation occurs. At pharmacological concentrations, Alpha2 predominates and vasoconstriction ocur.
95
B1 potency?
ISO > Epi ~ NE > DA
96
B2 potency?
ISO > Epi >> NE >> DA
97
A1 potency?
Epi ~ NE > DA > ISO
98
A2 potency?
CLON > Epi ~ NE >>ISO
99
Norepinephrine mxn?
Non-selective agonist of a1, a2, B1
100
Norepinephrine for?
Acute hypotension
101
Norepinephrine side effects?
HTN, Arrythmias, HAs
102
Epinephrine mxn?
Non-selective agonist of a1, a2, B1, B2
103
Epinephrine for?
Anaphylactic shock; combined with local anasthetic; glaucoma
104
Epinephrine side effects?
Palpitation, arrythmias, HAs, tremors
105
Amphetamine mxn?
Indirect acting adrenergic agonist, Increases NE release
106
Amphetamine for?
ADHD, narcolepsy, recreation
107
Amphetamine side effects?
HTN, insomnia, anxiety, arrythmias
108
Isoproterenol mxn?
Nonselective agonist of B1, B2
109
Isoproterenol for?
Shock, Heart block, Bronchodilator
110
Isoproterenol side effects?
Palpitation, Tachyarrhythmias, HAs
111
Dobutamine mxn?
Selective B1 agonist
112
Dobutamine for?
Cardiac decompensation, heart block, shock
113
Dobutamine side effects?
Tachyarrythmias, HTN
114
Albuterol mxn?
Selective B2 agonist
115
Albuterol for?
Mild asthma, COPD, prevent/reduce exercise-induced bronchospasm
116
Albuterol timing?
10-15 minutes for action, 6-12 hours duration
117
Albuterol side effects?
Tachycardia, muscle tremor, can mask progressively severe inflammation
118
Terbutaline for?
Selective B2 agonist
119
Terbutaline for?
Mild asthma, COPD, prevent/reduce exercise-induced bronchospasm
120
Terbutaline timing?
10-15 minutes for action, 6-12 hours duration
121
Terbutaline side effects?
Tachycardia, muscle tremor, can mask progressively severe inflammation
122
Phenylephrine mxn?
Selective a1 agonist
123
Phenylephrine for?
Postural hypotension, nasal congestion, possibly as an anorexic
124
Phenylephrine side effects?
HTN, Reflex bradcardia
125
Clonidine mxn?
Selective a2 agonist
126
Is clonidine a prodrug?
No
127
Can clonidine cross the BBB?
Yes
128
Clonidine for?
Hypertension, Drug W/D, Shock
129
Clonidine side effects?
Sedation, Retention of Na/H2O
130
a-Methyldopa mxn?
Selective a2 agonist, Metabolite (a-methylnorepinephrine) activates CNS a2 receptors
131
Is a-methyldopa a prodrug?
Yes
132
Can a-methyldopa cross the BBB?
Yes
133
a-Methyldopa for?
HTN
134
a-Methyldopa side effects?
Sedation
135
Dopamine mxn?
Mixed acting (Indirect/Direct) agonist of D1, a1, B1. NE release
136
Dopamine for?
Shock, renal failure, hypotension
137
Dopamine side effects?
Vasoconstriction at high doses
138
Dopamine at low dose?
Direct @ D1 --> dilation of renal vessels --> decrease in BP, increase in GFR/urine
139
Dopamine at medium dose?
Direct @ B1 --> Positive inotropic effect (increased heart contraction)
140
Dopamine at high dose?
Direct @ a1 --> Vasoconstriction
141
Fenoldopam mxn?
Selective Dopamine agonist (D1 only)
142
Fenoldopam for?
Increase blood flow at renal, mesenteric, cerebral arteries (HTN emergency, Anuria)
143
Fenoldopam half-life?
10 minutes
144
Phentolamine mxn?
Nonselective a1,a2 antagonist
145
Phentolamine for?
Pheochromocytoma, Raynaud's, frostbite
146
Phentolamine side effects?
Postural hypotension, Inhibit ejaculation, Tachycardia
147
Phenoxybenzamine mxn?
Nonselective a1,a2 antagonist (non-competitive blocker)
148
Phenoxybenzamine for?
Pheochromocytoma, Raynaud's, frostbite
149
Phenoxybenzamine side effects?
Postural hypotension, inhibit ejaculation, Tachycardia
150
Prazosin mxn?
Selective a1 antagonist
151
Prazosin for?
Primary HTN, BPH
152
Prazosin side effects?
Postural hypotension @ 1st dose, less side effects thatn phentolamine and phenoxybenzamine
153
Terazosin mxn?
Selective a1 antagonist
154
Terazosin for?
Primary HTN, BPH
155
Terazosin side effects?
Postural hypotension @ 1st dose, less side effects thatn phentolamine and phenoxybenzamine
156
Propranolol mxn?
1st generation nonselective B1,B2 antagonist
157
Propranolol for?
Angina, HTN, Arrythmias
158
Propranolol half-life?
4 hours
159
Propranolol side effects?
Bradycardia, Bronchoconstriction, Sexual dysfunction
160
Timolol mxn?
1st generation nonselective B1,B2 antagonist
161
Timolol for?
Glaucoma (Decrease secretion of aqueous humor from ciliary processes)
162
Timolol side effects?
Bradycardia, Bronchoconstriction, Sexual dysfunction
163
Timolol half life?
4 hours
164
Metoprolol mxn?
2nd generation B1 selective antagonist
165
Metoprolol for?
HTN, Angina, Arrythmias, CHF
166
Metoprolol side effects?
Bradycardia, Sexual dysfunction
167
Metoprolol half life?
4 hours
168
Atenolol mxn?
2nd generation B1 selective antagonist
169
Atenolol for?
HTN, Angina, Arrythmias, CHF
170
Atenolol side effects?
Bradycardia, Sexual dysfunction
171
Atenolol half life?
6-8 hours
172
Atenolol lipid soluble?
No, cannot access CNS
173
Bisoprolol mxn?
2nd generation B1 selective antagonist
174
Bisoprolol for?
HTN, Angina, Arrythmias, CHF
175
Bisoprolol side effects?
Bradycardia, Sexual dysfunction
176
Carvedilol mxn?
3rd generation nonselective B1, B2 antagonist
177
Carvedilol for?
CHF, HTN
178
Carvedilol side effets?
Bradycardia, fatigue
179
Labetalol mxn?
3rd generation nonselective B1, B2 antagonist
180
Labetalol for?
CHF, HTN
181
Labetalol side effects?
Bradycardia, Fatigue
182
Betaxolol mxn?
3rd generation selective B1 inhibitor
183
Betaxolol for?
HTN, CHF
184
Betaxolol side effect?
Bradycardia
185
Cocaine mxn?
Prevents NE reuptake
186
Cocaine for?
Local anasthetic, vasoconstricor
187
Cocaine side effects?
Insomnia, anxiety, arrythmias
188
Tyramine mxn?
Indirect acting adrenergic agonist, Increases cytoplasmic NE release (involved in exhange with NE across membrane)
189
Guanethidine mxn?
Nerve ending blocker: False NT -- Vesicles are filled with guanethidine instead of NE
190
Guanethidine?
AntiHTN
191
Guanethidine side effects?
Many and serious -- rarely used in US anymore
192
Reserpine mxn?
Nerve ending blocker: NE is not taken into vesicles because it binds uptake transporter and stops it
193
Reserpine for?
AntiHTN
194
Reserpine side effects?
Many and serious, including depression and suicide. Extremely cheap, but not used in the US. Used abroad.
195
a-methyl-tyrosine mxn?
Nerve ending blocker: Inhibits tyrosine hydroxylase and decreases NE synthesis
196
a-methyl-tyrosine for?
Inoperable pheochromocytoma
197
a-methyl-tyrosine side effects?
Many and serious: Used only for inoperable pheochromocytoma
198
Ephedrine mxn?
Mixed indirect/direct (B2) agonist
199
Ephedrine for?
Anorexic, Nasal decongestion
