Adrenergic Drugs Flashcards
1
Q
Epinephrine (Adrenalin)
A
Catecholamine. High affinity for Beta-2 receptors.
2
Q
Norepinephrine (Levophed)
A
Catecholamine. Less effect on Beta-2 and more effect on Beta-3.
3
Q
Isoproterenol (Isuprel)
A
Catecholamine. Equal affinity for all beta receptors.
4
Q
Phenylephrine (Neofrin; neosynephrine)
A
Alpha-1 agonist
5
Q
Pseudoephedrine (Sudafed)
A
Alpha-1 agonist
6
Q
Xylometazoline (Otrivin)
A
Alpha-1 agonist
7
Q
Oxymetazoline (Afrin)
A
Alpha-1 agonist
8
Q
Midodrine (ProAmatine)
A
Alpha-1 agonist
9
Q
Clonidine (Catapress)
A
Alpha-2 agonist
10
Q
Methyldopa (Aldomet)
A
Alpha-2 agonist
11
Q
Apraclonidine (Iopidine)
A
Alpha-2 agonist
12
Q
Dobutamine (Dobutrex)
A
Beta-1 agonist
13
Q
Albuterol (Ventolin)
A
Beta-2 agonist
14
Q
Ritodrine (Yutopar)
A
Beta-2 agonist
15
Q
Mirabegron (Myrbetriq)
A
Beta-3 agonist
16
Q
Ephedrine
A
“other” adrenergic stimulant
17
Q
Amphetamine
A
“other” adrenergic stimulant
18
Q
Methylphenidate (Ritalin)
A
“other” adrenergic stimulant
19
Q
Methamphetamine
A
“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation
20
Q
Cocaine
A
“other” adrenergic stimulant. inhibits reuptake of NE.
21
Q
Tyramine
A
“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation
22
Q
Dopamine (Intropin)
A
Dopamine agonist
23
Q
Fenoldopam (Corlopam)
A
Dopamine agonist
24
Q
VMA/HVA test
A
Measures the metabolism of NE and Epi.
25
Alpha-1 agonist effects
Vasoconstriction of peripheral vessels, nasal mucosa. Mydriasis. Contraction of the prostate and GU smooth muslce. Erection of hair (pilomotor).
26
Alpha-2 agonist effects
Act presynaptically to inhibit transmitter release. Cause aggregation of platelets and contraction of vascular smooth muscle. Decreases insulin release.
27
Beta-1 agonist effects
Increases force of contraction and AV conduction. Increases renin secretion from the kidney.
28
Beta-2 agonist effects
Relax respiratory, uterine and GI smooth muscle. Vasodilate vessels supplying skeletal muscles. Increase potassium uptake into muscle. Increase glycogenolysis and gluconeogenesis.
29
Beta-3 agonist effects
Increase lipolysis in fat cells
30
Alpha receptor effects on the heart
Increased arterial resistance in small blood vessels. Increased BP leads to baroreceptor reflex that slows the HR.
31
Alpha receptor effects on the eye
Mydriasis. No accommodation. Decreases intraocular presure.
32
Alpha receptor effects on the respiratory system
vasoconstricts the vessels in the nasal mucosa. Act as a decongestant.
33
Alpha receptor effects on the GU
Constrict the sphincters to promote continence. Promotes ejaculation.
34
Beta receptor effects on the Heart
Increased contractility and conduction through the AV node. Increases automaticity. Increased coronary and skeletal muscle blood flow (decreased diastolic BP)
35
Beta receptor effects on the eye
increased intraocular pressure.
36
Beta receptor effects on the respiratory tract
relax bronchial smooth muscle
37
Beta receptor effects GU
Relaxes the uterus
38
Beta receptor effects on metabolism
Increased renin secretion. Glycogenolysis. Increased uptake of potassium. Increased insulin secretio. Lipolysis.
39
Norepinephrine MOA
Stimulates alpha (vasoconstriction) and beta 1 receptors with little effect on beta 2. Must be injected.
40
Norepinephrine effects
Increases BP with a slight decrease in HR (vagal reflex). Atropine can inhibit the vagal reflex if given prior to NE and the HR will increase. Used rarely during severe hypotensive crisis.
41
Norepinephrine adverse side effects
Vasoconstriction at the infusion site can cause necrosis.
42
Epinephrine MOA
Must be injected. Stimulates alpha (Vasoconstriction) , beta 1 (Inotropy/chronotropy) and beta 2 (Vasodilation in skeletal muscle) receptors. Short duration of action.
43
Epinephrine effects
Increased pulse pressure. Increased BP and increased HR. Increases blood glucose and FFA concentrations. Increased renin secretion.
44
Epinephrine infused slowly
Beta 1 increases HR and contractility. Increases coronary blood flow. Alpha receptors increase systolic and diastolic BP. Beta 2 decreases diastolic pressure therefore increasing the pulse pressure. No change in mean BP shows little vagal reflex so HR is increased.
45
Epinephrine rapid infusion
Increases blood pressure with a slight increase in HR.
46
Epinephrine uses
anaphylactic shock, cardiac arrest, complete heart block, vasoconstictor to decrease diffusion of local anesthetics, glaucoma, asthma (bronchodilation).
47
Epinephrine side effects
Tremor, throbbing HA, increased BP, tachycardia, angina
48
Epinephrine contraindications
Beta blocker use. Can cause severe hypertension.
49
Epinephrine Dose dependence
Vasodilation dominates at low doses while vasoconstriction at high doses.
50
Ephedrine MOA
Stimulates alpha and beta receptors. Long duration of effect.
51
Ephedrine effects
Increases HR and BP. Causes bronchodilation.
52
Ephedrine adverse effects
hemorrhagic stroke and death due to severe hypertension.
53
Phenylephrine MOA
Alpha 1 agonist.
54
Phenylephrine effects
Vasoconstriction increases BP with a reflex decrease in HR.
55
Phenylephrine uses
Hypotensive emergency, decongestant, mydriasis.
56
Pseudophedrine uses
decongestant. Use caution in those with HTN.
57
Xylometazoline MOA
Alpha receptor stimulant
58
Xylometazoline and Oxymetazoline uses
topically as nasal sprays to decrease congestion.
59
Oxymetazoline MOA
Alpha receptor stimulant. Also acts on alpha 2 receptors and can cause hypotension is a large amount is absorbed.
60
Xylometazoline and Oxymetazoline contraindications
narrow-angle glaucoma
61
Clonidine MOA
Acts on alpha 2 receptors in the brain to decrease release of NE and overall SNS output. Used as a transdermal patch.
62
Clonidine uses
treatment of HTN, reduces addictive cravings, decreases hot flashes, used pre-anesthetically to cause sedation.
63
Clonidine adverse side effects
dry mouth, sedation, sexual dysfunction. Avoid getting the patch hot because it causes a large release of clonidine leading to hypotension. Abrupt withdrawal can cause rebound HTN.
64
Methyladopa uses
similar to clonidine.
65
Apraclonidine uses
Used in the eye to decrease intraocular pressure
66
Tizanidine uses
Less effective on lowering BP but effective at reducing muscle spasticity.
67
Isoproterenol MOA
Beta 1 and Beta 2 agonists
68
Isoproterenol effects
Increases HR and force of contraction. Causes vasodilationand decreases BP.
69
Isoproterenol uses
Cardiac arrest and complete heart block
70
Isoproterenol adverse side effects
tachycardia, palpitations and arrhythmias.
71
Dobutamine MOA
Beta 1 agonist with some effect on alpha receptors
72
Dobutamine effects
Positive inotrope that increases CO. Increases BP and HR
73
Dobutamine uses
cardiac stress tests, cardiogenic shock and CHF.
74
Albuterol MOA
Beta 2 agonist. With little effect on Beta 1 receptors.
75
Albuterol uses
asthma
76
Albuterol adverse effects
HA, tachycardia, tremor.
77
Mirabegron MOA
Beta 3 receptor agonist
78
Mirabegron uses
treatment of overactive bladder.
79
Mirabegron adverse effects
nausea, HA, HTN, diarrhea, constipation, dizziness and tachycardia.
80
Low dose dopamine MOA
D1 receptors that cause vasodilation and increases renal blood flow.
81
High dose dopamine MOA
Stimulates Beta 1 receptors and produce a positive ionotropic and chronotropic effect.
82
Dopamine uses
Cardiogenic shock
83
Dopamine adverse effects
Nausea, vomiting, tachycardia, angina, arrhythmias, HA, and peripheral vasoconstriction.
84
Fenoldopam MOA
D1 agonsit
85
Fenoldopam effects
dilation of vascular beds which decrease BP.
86
Fenoldopam uses
Treatment of a hypertensive crisis.
87
Amphetamine MOA
increases the release of NE and DA
88
Amphetamine effects
alertness, insomnia, decreased appetite, euphoria, increases motor activity.
89
Amphetamine adverse effects
Psychosis, HA, chills, pallor, arrhythmias, HTN, cerebral hemmorhage, convulsions
90
Amphetamine uses
enuresis. Causes contraction of the bladder sphincter.
91
Methamphetamine uses
Recreational drug
92
Methylphenidate uses
(ritalin) ADHD
93
Cocaine MOA
inhibits re-uptake of DA and NE.
94
Cocaine effect
Vasoconstrictor. Can cause severe HTN.
95
Cocaine adverse effects
Stroke, arrhythmias, MI, tachycardia. Long-term use can causes psychosis.
96
Tyramine MOA
Increases the release of catecholamines from the nerve terminals. Usually hydrolyzed by MOA. Those treated for depression with MOA inhibitors that ingest large amounts of tyramine can have a HTN crisis.
97
Phentolamine (Regitine)
Alpha-receptor blocker. Reversible antagonist.
98
Phenoxybenzamine (Dibenzyline)
Alpha-receptor blocker. non competitive, irreversible antagonist.
99
Prazosin (minipress)
Alpha 1 blocker. Reversible antagonist.
100
Terazosin (Hytrin)
Alpha 1 blocker. Reversible antagonist.
101
Doxazosin (cardura)
Alpha 1 blocker. Reversible antagonist.
102
Alfuzosin (Uroxatral)
Alpha 1 blocker
103
Tamsulosin (Flomax)
Alpha 1 blocker
104
Yohimbine
Alpha 2 blocker
105
Propranolol (inderal)
Beta blocker
106
Timolol (timoptic)
Beta blocker
107
Nadolol (corgard)
Beta blocker
108
Metoprolol (Lopressor)
Cardiospecific/Beta1 blocker
109
Atenolol (Tenormin)
Cardiospecific/Beta1 blocker
110
Bisoprolol (zebeta)
Cardiospecific/Beta1 blocker
111
acebutolol (sectral)
Cardiospecific/Beta1 blocker with intrinsic sympathetic activity.
112
Esmolol (brevibloc)
Cardiospecific/Beta1 blocker
113
Betaxolol (betoptic)
Cardiospecific/Beta1 blocker
114
Nebivolol (bystolic)
Cardiospecific/Beta1 blocker
115
Pindolol (visken)
beta blocker with intrinsic sympathetic activity
116
Carteolol (Cartol)
beta blocker with intrinsic sympathetic activity
117
Carvedilol (Coreg)
Combo beta and alpha blocker
118
Labetalol (Normodyne)
Combo beta and alpha blocker
119
Guanethidine (ismelin)
Affects neurotransmitter release
120
Reserpine
Affects neurotransmitter release
121
Metryrosine (demsar)
synthesis inhibitor
122
Alpha 1 blockers effects
decrease BP, orthostatic hypotension, miosis, esier to urinate, inhibit ejaculation.
123
Alpha 2 blockers effects
increased NE and insulin release.
124
Beta blockers effects
Decreased HR and contraction, decreased renin secretion, bronchoconstriction, decreased glycogenolysis and lipolysis, decreased intraocular pressure.
125
Alpha blockade effects on the heart
Lowers peripheral resistance (postural hypotension). Reflex tachycardia. Used for epinephrine reversal to block it's alpha effects and decrease BP.
126
Alpha blockade effects on the eye
Miosis
127
Alpha blockade effect on the nose
congestion due to vasoconstriction
128
Alpha blockade effect on the GU system
decreases resistance to urine flow (BPH) and inhibits ejaculation.
129
Phentolamine MOA
Competitive antagonist of alpha 1 and alpha 2 receptors.
130
Phentolamine effects
Decreases peripheral resistance with cardiac stimulation (reflex and increased NE due to alpha 2 block). Also causes gastric stimulation due to blockade of serotonin receptors.
131
Phentolamine uses
hypertensive crisis of to prevent necrosis of tissue where a vasoconstrictor has been injected.
132
Phentolamine adverse effects
tachycardia, arrhythmia, MI, Hypotension, abdominal pain, peptic ulcers.
133
Phenoxybenzamine MOA
irreversible alpha blocker that bind covalently to the receptor. Also inhibits reuptake of NE
134
Phenoxybenzamine effects
Decreases peripheral resistance.
135
Phenoxybenzamine uses
Treatment of pheochromocytoma.
136
Phenoxybenzamine adverse effects
Hypotension (if hypovolemic), postural hypotension, tachycardia, nasal congestion, inhibition of ejaculation. With Epi can cause hypotension and tachycardia.
137
Prazosin MOA
Highly selective for alpha one receptors. Well absorbed orally. Duration of action is 7-10 hours (given twice daily). Metabolized by the liver. Half life doubles in CHF (lower dose needed).
138
Prazosin effects
Decreases peripheral resistance (no increases in HR due to selectivity). Cardiac output doesn't increase. Decreases SNS outflow from the CNS. Decreases LDL/Triglycerides and increases HDL.
139
Prazosin uses
HTN, BPH.
140
Prazosin adverse effects
First does phenomenon (postural hypotension/syncope 30-90 mins after first dose). Postural hypotension, dizziness, nasal congestion, sexual dysfunction. Don't combine with drugs like viagra.
141
Terazosine MOA
Selective alpha one receptor blockade. 12 hour half life (given once daily).
142
Terazosine uses
BPH
143
Terazosine adverse effects
first dose phenomenon
144
Doxazosin MOA
Selctive alpha one receptor blockade. 20 hour half life
145
Doxazosin uses
BPH
146
Doxazosin adverse effects
first dose phenomenon
147
Tamsulosin MOA
Selective blockade for alpha 1a receptors (prostate). Half life of 5-10 hours. Metabolized by P450s.
148
Tamsulosin effects
Relaxes the prostate (alpha 1a) with little effect on BP (alpha 1b). Also relaxes the bladder sphincter.
149
Tamsulosin uses
BPH
150
Tamsulosin adverse effects
Difficulty ejaculating.
151
Alfuzosin uses
BPH
152
Alfuzosin adverse effects
dizziness
153
Yohimbine MOA
Selective alpha 2 antagonist that increases NE release
154
Yohimbine effects
Increases BP and HR. Increase in SNS may increase libido ("natural viagra").
155
Yohimbine contraindications
dangerous in men with HTN.
156
Beta blocker effect on the heart
Slows the HR and decreases contractility. Slowed AV conduction. Reduced automaticity. Decreases the oxygen demand of the heart. With chronic use BP will be lowered due to decreased CO. Renin release is reduced. Initially BP may increase due to beta 2 blockade but over time BP will be reduced.
157
Beta blocker contraindications
Pheochromocytoma without concomitant administration of an alpha blocker. Those with asthma.
158
Beta blocker effects on the respiratory system
Beta 2 blockers will cause bronchoconstriction.
159
Beta blocker effects on the eye
reduce intraocular pressure
160
Beta blocker effects on metabolism
Inhibits lipolysis (increases VLFL and decreases HDL). Decreased glycogenolysis (beta 2). Can impair the ability of type 1 diabetics recovery from hypoglycemia. Can also mask the symptoms of hypoglycemia. Should use extreme caution when prescribing beta blockers for type 1 diabetics.
161
Beta blocker use as a local anesthetic
Acebutolol, labetalol, metoprolol, pindolol, propranolol. Membrane stabilizing through blockade of sodium channels. Don't use an an anesthetic in the eye.
162
Propranolol MOA
Non-selective (beta 1 and 2) competitive antagonist.
163
Propranolol effects
Slows the HR, decreases AV conduction, decreases contractility, decreases renin release, decreases lipolysis and glycogenolysis. Can have local anesthetic effects.
164
Propranolol pharmacokinetics
Oral. Sustained release. Lipid soluble (CNS penetration). Metabolized in liver with a 3-6 hour half life.
165
Propranolol uses
Chronic use for HTN. Decreases mortality post-MI. Angina. Arrhythmias. CHF (when stable). Hyperthyroidism. Migraines. Reduces portal vein pressure in cirrhosis. Decreases tremors ("stage-fright").
166
Propranolol adverse effects
Bronchoconstriction (especially in asthmatics). Exacerbation of CHF if unstable. Bradycardia, hypotension, sedation, fatigue. Can worsen vasospastic disorders. Can mask the symptoms of hypoglycemia and hyperthyroidism. Can increase VLDL and decrease HDL. Should not be discontinued abruptly due to rebound HTN (beta receptors have been upregulated).
167
Drugs that inhibit metabolism of Propranolol
cimetidine and chlorpromazine.
168
Drugs that increase metabolism of Propranolol
barbituates, phenytoin, rifampin and smoking. Calcium channel blockers can have an additive effect.
169
Timolol uses
Glaucoma. Can be used systemically like Propranolol.
170
Timolol contraindications
asthma
171
Nadolol uses
similar to Propranolol but has a longer half life. Doesn't penetrate the CNS so less likely to cause sedation.
172
Sotalol uses
Blocks potassium channels and has class three antiarrythmic activity.
173
The beta 1 selective antagonists
Metroprolol, Atenolol and bisoprolol
174
beta 1 selective antagonists effects
Decreases HR and contractility. Does not block beta 2 receptors in the skeletal muscle vessels (better exercise tolerance) and is less likely to inhibit glycogenolysis (decreased risk of hypoglycemia).
175
beta 1 selective antagonists uses
HTN, post-MI, migraine prophylaxis.
176
beta 1 selective antagonists adverse effects
dizziness, fatigue, bradycardia and hypotension.
177
Atenolol and diabetes
Reduces the risk for type 2 diabetes.
178
beta 1 selective antagonists contraindications
Use caution in patients with COPD and asthma because the selectivity is not absolute and at high doses can effect beta 2 receptors.
179
Betaxolol MOA
selective beta 1 blocker. Less likely to cause bronchoconstriction than timolol.
180
Betaxolol uses
glaucoma
181
Nebivolol MOA
Selective beta 1 blocker that increases the release of Nitric oxide. Lowers BP without depressing LV function.
182
Nebivolol effects
Lowers BP (nitric oxide) and decreases cholesterol, triglycerides and BGL.
183
Esmolol MOA
selective beta 1 blocker with a very short duration of action (8 mins). Must be administered IV.
184
Esmolol Uses
Used when short blockade is needed or when necessary to rapidly remove the beta blocker effect.
185
Intrinsic Sympathetic activity
Means the drug is a partial agonist
186
Beta blockers with ISA uses
treatment of HTN and angina. Risk of bradycardia is lower than with other beta blockers.
187
Carteolol uses
Glaucoma
188
Beta blockers with ISA
Pindolol, carteolol, penbutolol. Acebutolol (selective Beta 1)
189
Labetalol MOA
Blocks Beta 1, Beta 2 and alpha 1 receptors.
190
Labetalol effects
Decreased BP without the compensatory increase in HR.
191
Labetalol uses
HTN emergencies
192
Carvedilol MOA
Non-selective beta blocker that also blocks alpha 1 receptors.
193
Carvedilol effects
Reduces BP without a compensatory increase in HR. Reduces the effects of free radicals on vascular smooth muscle.
194
Carvedilol uses
Decreases morbidity/mortality in CHF. Treatment of HTN.
195
Clinical uses of beta blockers
HTN, Ischemic heart disease, arrhythmias, obstructive cardiomyopathy, dissecting aortic aneurysm, hyperthyroidism, migraines.
196
Beta blockers that improve survival after an MI
Timolol, propranolol and metoprolol
197
Beta blockers that can be used in early CHF
Metoprolol, carvedilol and bisprolol.
198
Beta blockers to treat hyperthyroidism
propranolol
199
Beta blockers for migraine prophylaxis
propranolol, metoprolol and atenolol.
200
DOC for glaucoma
Prostaglandin analogues (latanoprost)
201
Beta blockers for glaucoma
Timolol, carteolol and betaxolol (beta 1 selective). Second line treatment. Decreases production of aqueous humor.
202
alpha 2 agonists for glaucoma
apraclonidine. Decreases production of aqueous humor and increases outflow.
203
Cholinergic agonist for glaucoma
Pilocarpine, carbachol, phyostigme and echothiophate. Rarely used because they effect vision.
204
Guanethidine MOA
Inhibits the release of NE. No longer used.
205
Reserpine MOA
Causes the depletion of NE, DA and serotonin by inhibitng uptake of biogenic amines.
206
Reserpine adverse effects
No longer used. Diarrhea, depression, sedation and parkinson's like symptoms.
207
Metyrosine MOA
Tyrosine analogue that blocks tyrosine hydroxylase. Decreases the amount of DA, NE and Epi.
208
Metyrosine uses
Pre-surgical treatment of pheochromocytoma.
