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Pharmacology > Autonomics > Flashcards

Autonomics Flashcards

1
Q

M1/M3/M5 second messenger?

A

Gq –> PLC –> DAG & IP3 –> Calcium release

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2
Q

M2/M4 second messenger?

A

Gi –> Inhibit AC –> Decreased cAMP; Kchannel –> Hyperpolarization

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3
Q

Alpha 1 second messenger?

A

Gq –> PLC –> DAG & IP3 –> Calcium release

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4
Q

Alpha 2 second messenger?

A

Gi –> inhibit AC –> Decreased cAMP; Kchannel –> Hyperpolarization

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5
Q

Use Gi as second messenger?

A

M2/M4 & Alpha 2

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6
Q

Use Gq as second messenger?

A

M1/M3/M5 & Alpha 1

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7
Q

B1/B2/B3 second messenger?

A

Gs –> Stimulate AC –> Increase cAMP

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8
Q

Bethanechol class?

A

Direct acting carbamic acid ester (direct acting muscarinic cholinomimetic)

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9
Q

Muscarine class?

A

Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)

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10
Q

Pilocarpine class?

A

Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)

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11
Q

Cevimeline class?

A

Direct acting non-ester alkaloid (direct acting muscarinic cholinomimetic)

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12
Q

Nicotine class?

A

Direct acting non-ester alkaloid (direct acting nicotinic cholinomimetic)

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13
Q

Bethanechol treats?

A

Post-op and neurogenic ileus; urinary retention (bowel & bladder smooth muscle ACh-innervated)

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14
Q

Pilocarpine treats?

A

Glaucoma (ACh activates sphincter & ciliary muscles of eye)

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15
Q

Cevimeline treats?

A

Dry mouth (Sjogren’s, post-radiation therapy) via increased salivation

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16
Q

Nicotine treats?

A

Smoking cessation via reduced cravings

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17
Q

Side effects of direct acting muscarinic cholinomimetics?

A

SLUDGE: Salivation, Lacrimation, Urination, Defecation, GI distress, Emesis

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18
Q

Direct acting muscarinic cholinomimetics?

A

Bethanechol, Muscarine, Pilocarpine, Cevimeline

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19
Q

Neostigimine class?

A

Indirect acting carbamate (AChE inhibitor)

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20
Q

Physosligmine class?

A

Indirect acting carbamate (AChE inhibitor)

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21
Q

Donepezil class?

A

Indirect acting non-ester (AChE inhibitor)

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22
Q

Edrophonium class?

A

Indirect acting non-ester alcohol (AChE inhibitor)

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23
Q

Echothiophate class?

A

Indirect acting organophosphate (AChE inhibitor)

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24
Q

Pralidoxime class?

A

Strong nucleophile and regenerates phosphorylated AChE

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25
Q

Sarin class?

A

Potent indirect acting organophosphate (AChE inhibitor)

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26
Q

Neostigmine treats?

A

Post-op and neurogenic ileus; urinary retention; myasthenia gravis; reversal of NMJ blockade

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27
Q

Neostigmine time?

A

Lasts 0.5-2 hours

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28
Q

Physostigmine treats?

A

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

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29
Q

Physostigmine time?

A

Lasts 0.5-2 hours

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30
Q

Donepezil treats?

A

Alzheimer’s (amplifies endogenous ACh in brain)

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31
Q

Edrophonium treats?

A

Myasthenia gravis (differentiating deficiency versus ACh crisis); ileus

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32
Q

Edrophonium time?

A

Lasts 5-15 minutes

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33
Q

Echothiophate treats?

A

Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)

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34
Q

Echothiophate time?

A

Lasts >100 hours

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35
Q

Pralidoxime treats?

A

Poisoning by nerve gas (also an insecticide)

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36
Q

Sarin can be used as?

A

Volatile nerve gas

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37
Q

Sarin can cause?

A

Death

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38
Q

Sarin toxicity treated how?

A

Treat with pralidoxime and atropine before aging

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39
Q

Side effects of AChE inhibitors?

A

SLUDGE + general increase in cholinergic neurotransmission; paralysis

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40
Q

Long acting AChE inhibitor?

A

Echothiophate

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41
Q

Short acting AChE inhibitors?

A

Neostigmine, Physostigmine, Edrophonium

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42
Q

Atropine class?

A

Tertiary amine antimuscarinic

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43
Q

Scopolamine class?

A

Tertiary amine antimuscarinic

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44
Q

Dicyclomine class?

A

Tertiary amine antimuscarinic

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45
Q

Tropicamide class?

A

Tertiary amine antimuscarinic

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46
Q

Tolterodine class?

A

Tertiary amine antimuscarinic

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47
Q

Benztropne class?

A

Tertiary amine antimuscarinic

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48
Q

Side effects of tertiary amine antimuscarinics?

A

General block of muscarinic functions

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49
Q

Tertiary amine antimuscarinics?

A

Atropine, Scopolamine, Dicyclomine, Tropicamide, Tolterodine, Benztropine

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50
Q

Atropine treats?

A

Mydriasis, cycloplegia

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51
Q

Scopolamine treats?

A

Prevent or reduce motion sickness

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52
Q

Dicyclomine treats?

A

Reduce transient hypermotility

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53
Q

Tropicamide treats?

A

Mydriasis, cycloplegia

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54
Q

Tolterodine treats?

A

Transient cystitis, post-op bladder spasms, incontinence

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55
Q

Benztropine treats?

A

Manifestations of Parkinson’s

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56
Q

Tertiary amine antimuscarinics that cross the BBB?

A

Scopolamine, Benztropine

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57
Q

Metabolism of scopolamine?

A

Slow

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58
Q

Metabolism of tropicamide?

A

Rapid

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59
Q

Quarternary amine antimuscarinics?

A

Ipratropium, Tiotropium

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60
Q

Ipratropium class?

A

Quarternary amine antimuscarinic

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61
Q

Tiotropium class?

A

Quarternary amine antimuscarinic

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62
Q

Which quarternary amine antimuscarinic is longer acting?

A

Tiotropium

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63
Q

Ipratropium and tiotropium treat?

A

Bronchodilation in asthma or COPD

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64
Q

Ipratropium and triotropium side effects?

A

General block of muscarinic effects

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65
Q

Ganglionic blockers?

A

Hexamethonium, Mecamylamine

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66
Q

Hexamethonium, Mecamylamine mxn?

A

Block Nn receptor and sympathetic tone

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67
Q

Hexamethonium, Mecamylamine treat?

A

Hypertenisve crisis (“Bloodless” field surgery)

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68
Q

Succinylcholine class?

A

Depolarizing blocker

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69
Q

How do depolarizing blockers work?

A

Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation

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70
Q

Succinylcholine used for?

A

Brief procedures (tracheal intubation, reset dislocated joints?

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71
Q

Side effects of succinylcholine?

A

Respiratory paralysis, disturbance of autonomic function, flaccid paralysis within minutes

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72
Q

Tubocurarine class?

A

Nondepolarizing blocker (Block Nm receptor)

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73
Q

Mivacurium class?

A

Nondepolarizing blocker (Block Nm receptor)

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74
Q

Nm blockers?

A

Tubocurarine, Mivacurium

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75
Q

Tubocurarine, Mivacurium used for?

A

Muscle relaxant for surgery w/o deep anasthesia

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76
Q

Tubocurarine, Mivacurium side effects?

A

Respiratory paralysis, disturbance of autonomic function

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77
Q

Tubocurarine time?

A

Lasts 30-60 minutes

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78
Q

Mivacurium inhibitor?

A

Rapidly hydrolyzed, short-lasting

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79
Q

Botulinum toxin A class and mxn?

A

Local paralytic: Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25

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80
Q

Botulinum tonxin A treats?

A

Reduces frown lines and wrinkles, achalasia, strabismus, oromandibular dystonia

81
Q

ANS activity in the SA node?

A

Symp accelerate B1,B2. Parasymp decelerate M2

82
Q

ANS activity in the contractility of the heart?

A

Symp increase B1,B2. Parasymp decelerate M2 (atria).

83
Q

ANS activity in the blood vessels?

A

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
Q

ANS activity in bronchiolar smooth muscle?

A

Symp relax B2. Parasymp contract M3.

85
Q

ANS activity in GI?

A

Symp relax smooth muscle contract sphictors. Parasymp contract smooth muscle relax sphinctors + secretion.

86
Q

ANS activity in GU smooth muscle?

A

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
Q

ANS activity in the eye?

A

Symp dilate relax ciliary muscle B. Parasymp constrict contract ciliary muscle M3.

88
Q

Beta 1?

A

Heart (Increase HR, Increase contraction). Kidney (Renin secretion)

89
Q

Beta 2?

A

Arterioles (Dilate). Bronchial smooth muscle (Relax). Uterus (Relax). Increase metabolic effects.

90
Q

Beta 3?

A

Increase lipolysis and thermogenesis.

91
Q

Alpha 1?

A

Arterioles (Constrict). Veins (Constrict). Uterus (Constrict).

92
Q

Alpha 2?

A

Presynaptic Nerve Endings (Inhibit NE Release and ACh release). Postsynaptic in CNS (Decreased peripheral Sympathetic Tone)

93
Q

Dopamine?

A

Renal, mesenteric, cerebral arterioles (Dilate).

94
Q

Tell me about skeletal muscle blood vessel receptors and response.

A

Alpha1 and Beta2. At physiological concentration (of epi), Beta2 predominates and vasodilation occurs. At pharmacological concentrations, Alpha2 predominates and vasoconstriction ocur.

95
Q

B1 potency?

A

ISO > Epi ~ NE > DA

96
Q

B2 potency?

A

ISO > Epi&raquo_space; NE&raquo_space; DA

97
Q

A1 potency?

A

Epi ~ NE > DA > ISO

98
Q

A2 potency?

A

CLON > Epi ~ NE&raquo_space;ISO

99
Q

Norepinephrine mxn?

A

Non-selective agonist of a1, a2, B1

100
Q

Norepinephrine for?

A

Acute hypotension

101
Q

Norepinephrine side effects?

A

HTN, Arrythmias, HAs

102
Q

Epinephrine mxn?

A

Non-selective agonist of a1, a2, B1, B2

103
Q

Epinephrine for?

A

Anaphylactic shock; combined with local anasthetic; glaucoma

104
Q

Epinephrine side effects?

A

Palpitation, arrythmias, HAs, tremors

105
Q

Amphetamine mxn?

A

Indirect acting adrenergic agonist, Increases NE release

106
Q

Amphetamine for?

A

ADHD, narcolepsy, recreation

107
Q

Amphetamine side effects?

A

HTN, insomnia, anxiety, arrythmias

108
Q

Isoproterenol mxn?

A

Nonselective agonist of B1, B2

109
Q

Isoproterenol for?

A

Shock, Heart block, Bronchodilator

110
Q

Isoproterenol side effects?

A

Palpitation, Tachyarrhythmias, HAs

111
Q

Dobutamine mxn?

A

Selective B1 agonist

112
Q

Dobutamine for?

A

Cardiac decompensation, heart block, shock

113
Q

Dobutamine side effects?

A

Tachyarrythmias, HTN

114
Q

Albuterol mxn?

A

Selective B2 agonist

115
Q

Albuterol for?

A

Mild asthma, COPD, prevent/reduce exercise-induced bronchospasm

116
Q

Albuterol timing?

A

10-15 minutes for action, 6-12 hours duration

117
Q

Albuterol side effects?

A

Tachycardia, muscle tremor, can mask progressively severe inflammation

118
Q

Terbutaline for?

A

Selective B2 agonist

119
Q

Terbutaline for?

A

Mild asthma, COPD, prevent/reduce exercise-induced bronchospasm

120
Q

Terbutaline timing?

A

10-15 minutes for action, 6-12 hours duration

121
Q

Terbutaline side effects?

A

Tachycardia, muscle tremor, can mask progressively severe inflammation

122
Q

Phenylephrine mxn?

A

Selective a1 agonist

123
Q

Phenylephrine for?

A

Postural hypotension, nasal congestion, possibly as an anorexic

124
Q

Phenylephrine side effects?

A

HTN, Reflex bradcardia

125
Q

Clonidine mxn?

A

Selective a2 agonist

126
Q

Is clonidine a prodrug?

127
Q

Can clonidine cross the BBB?

128
Q

Clonidine for?

A

Hypertension, Drug W/D, Shock

129
Q

Clonidine side effects?

A

Sedation, Retention of Na/H2O

130
Q

a-Methyldopa mxn?

A

Selective a2 agonist, Metabolite (a-methylnorepinephrine) activates CNS a2 receptors

131
Q

Is a-methyldopa a prodrug?

132
Q

Can a-methyldopa cross the BBB?

133
Q

a-Methyldopa for?

134
Q

a-Methyldopa side effects?

135
Q

Dopamine mxn?

A

Mixed acting (Indirect/Direct) agonist of D1, a1, B1. NE release

136
Q

Dopamine for?

A

Shock, renal failure, hypotension

137
Q

Dopamine side effects?

A

Vasoconstriction at high doses

138
Q

Dopamine at low dose?

A

Direct @ D1 –> dilation of renal vessels –> decrease in BP, increase in GFR/urine

139
Q

Dopamine at medium dose?

A

Direct @ B1 –> Positive inotropic effect (increased heart contraction)

140
Q

Dopamine at high dose?

A

Direct @ a1 –> Vasoconstriction

141
Q

Fenoldopam mxn?

A

Selective Dopamine agonist (D1 only)

142
Q

Fenoldopam for?

A

Increase blood flow at renal, mesenteric, cerebral arteries (HTN emergency, Anuria)

143
Q

Fenoldopam half-life?

A

10 minutes

144
Q

Phentolamine mxn?

A

Nonselective a1,a2 antagonist

145
Q

Phentolamine for?

A

Pheochromocytoma, Raynaud’s, frostbite

146
Q

Phentolamine side effects?

A

Postural hypotension, Inhibit ejaculation, Tachycardia

147
Q

Phenoxybenzamine mxn?

A

Nonselective a1,a2 antagonist (non-competitive blocker)

148
Q

Phenoxybenzamine for?

A

Pheochromocytoma, Raynaud’s, frostbite

149
Q

Phenoxybenzamine side effects?

A

Postural hypotension, inhibit ejaculation, Tachycardia

150
Q

Prazosin mxn?

A

Selective a1 antagonist

151
Q

Prazosin for?

A

Primary HTN, BPH

152
Q

Prazosin side effects?

A

Postural hypotension @ 1st dose, less side effects thatn phentolamine and phenoxybenzamine

153
Q

Terazosin mxn?

A

Selective a1 antagonist

154
Q

Terazosin for?

A

Primary HTN, BPH

155
Q

Terazosin side effects?

A

Postural hypotension @ 1st dose, less side effects thatn phentolamine and phenoxybenzamine

156
Q

Propranolol mxn?

A

1st generation nonselective B1,B2 antagonist

157
Q

Propranolol for?

A

Angina, HTN, Arrythmias

158
Q

Propranolol half-life?

159
Q

Propranolol side effects?

A

Bradycardia, Bronchoconstriction, Sexual dysfunction

160
Q

Timolol mxn?

A

1st generation nonselective B1,B2 antagonist

161
Q

Timolol for?

A

Glaucoma (Decrease secretion of aqueous humor from ciliary processes)

162
Q

Timolol side effects?

A

Bradycardia, Bronchoconstriction, Sexual dysfunction

163
Q

Timolol half life?

164
Q

Metoprolol mxn?

A

2nd generation B1 selective antagonist

165
Q

Metoprolol for?

A

HTN, Angina, Arrythmias, CHF

166
Q

Metoprolol side effects?

A

Bradycardia, Sexual dysfunction

167
Q

Metoprolol half life?

168
Q

Atenolol mxn?

A

2nd generation B1 selective antagonist

169
Q

Atenolol for?

A

HTN, Angina, Arrythmias, CHF

170
Q

Atenolol side effects?

A

Bradycardia, Sexual dysfunction

171
Q

Atenolol half life?

172
Q

Atenolol lipid soluble?

A

No, cannot access CNS

173
Q

Bisoprolol mxn?

A

2nd generation B1 selective antagonist

174
Q

Bisoprolol for?

A

HTN, Angina, Arrythmias, CHF

175
Q

Bisoprolol side effects?

A

Bradycardia, Sexual dysfunction

176
Q

Carvedilol mxn?

A

3rd generation nonselective B1, B2 antagonist

177
Q

Carvedilol for?

178
Q

Carvedilol side effets?

A

Bradycardia, fatigue

179
Q

Labetalol mxn?

A

3rd generation nonselective B1, B2 antagonist

180
Q

Labetalol for?

181
Q

Labetalol side effects?

A

Bradycardia, Fatigue

182
Q

Betaxolol mxn?

A

3rd generation selective B1 inhibitor

183
Q

Betaxolol for?

184
Q

Betaxolol side effect?

A

Bradycardia

185
Q

Cocaine mxn?

A

Prevents NE reuptake

186
Q

Cocaine for?

A

Local anasthetic, vasoconstricor

187
Q

Cocaine side effects?

A

Insomnia, anxiety, arrythmias

188
Q

Tyramine mxn?

A

Indirect acting adrenergic agonist, Increases cytoplasmic NE release (involved in exhange with NE across membrane)

189
Q

Guanethidine mxn?

A

Nerve ending blocker: False NT – Vesicles are filled with guanethidine instead of NE

190
Q

Guanethidine?

191
Q

Guanethidine side effects?

A

Many and serious – rarely used in US anymore

192
Q

Reserpine mxn?

A

Nerve ending blocker: NE is not taken into vesicles because it binds uptake transporter and stops it

193
Q

Reserpine for?

194
Q

Reserpine side effects?

A

Many and serious, including depression and suicide. Extremely cheap, but not used in the US. Used abroad.

195
Q

a-methyl-tyrosine mxn?

A

Nerve ending blocker: Inhibits tyrosine hydroxylase and decreases NE synthesis

196
Q

a-methyl-tyrosine for?

A

Inoperable pheochromocytoma

197
Q

a-methyl-tyrosine side effects?

A

Many and serious: Used only for inoperable pheochromocytoma

198
Q

Ephedrine mxn?

A

Mixed indirect/direct (B2) agonist

199
Q

Ephedrine for?

A

Anorexic, Nasal decongestion

Pharmacology (46 decks)

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