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Pharmacology > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Epinephrine (Adrenalin)

A

Catecholamine. High affinity for Beta-2 receptors.

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2
Q

Norepinephrine (Levophed)

A

Catecholamine. Less effect on Beta-2 and more effect on Beta-3.

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3
Q

Isoproterenol (Isuprel)

A

Catecholamine. Equal affinity for all beta receptors.

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4
Q

Phenylephrine (Neofrin; neosynephrine)

A

Alpha-1 agonist

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5
Q

Pseudoephedrine (Sudafed)

A

Alpha-1 agonist

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6
Q

Xylometazoline (Otrivin)

A

Alpha-1 agonist

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7
Q

Oxymetazoline (Afrin)

A

Alpha-1 agonist

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8
Q

Midodrine (ProAmatine)

A

Alpha-1 agonist

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9
Q

Clonidine (Catapress)

A

Alpha-2 agonist

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10
Q

Methyldopa (Aldomet)

A

Alpha-2 agonist

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11
Q

Apraclonidine (Iopidine)

A

Alpha-2 agonist

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12
Q

Dobutamine (Dobutrex)

A

Beta-1 agonist

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13
Q

Albuterol (Ventolin)

A

Beta-2 agonist

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14
Q

Ritodrine (Yutopar)

A

Beta-2 agonist

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15
Q

Mirabegron (Myrbetriq)

A

Beta-3 agonist

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16
Q

Ephedrine

A

“other” adrenergic stimulant

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17
Q

Amphetamine

A

“other” adrenergic stimulant

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18
Q

Methylphenidate (Ritalin)

A

“other” adrenergic stimulant

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19
Q

Methamphetamine

A

“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation

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20
Q

Cocaine

A

“other” adrenergic stimulant. inhibits reuptake of NE.

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21
Q

Tyramine

A

“other” adrenergic stimulant. Increases the release of NE from the presynaptic terminal so there must be an intact innervation

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22
Q

Dopamine (Intropin)

A

Dopamine agonist

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23
Q

Fenoldopam (Corlopam)

A

Dopamine agonist

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24
Q

VMA/HVA test

A

Measures the metabolism of NE and Epi.

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25
Q

Alpha-1 agonist effects

A

Vasoconstriction of peripheral vessels, nasal mucosa. Mydriasis. Contraction of the prostate and GU smooth muslce. Erection of hair (pilomotor).

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26
Q

Alpha-2 agonist effects

A

Act presynaptically to inhibit transmitter release. Cause aggregation of platelets and contraction of vascular smooth muscle. Decreases insulin release.

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27
Q

Beta-1 agonist effects

A

Increases force of contraction and AV conduction. Increases renin secretion from the kidney.

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28
Q

Beta-2 agonist effects

A

Relax respiratory, uterine and GI smooth muscle. Vasodilate vessels supplying skeletal muscles. Increase potassium uptake into muscle. Increase glycogenolysis and gluconeogenesis.

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29
Q

Beta-3 agonist effects

A

Increase lipolysis in fat cells

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30
Q

Alpha receptor effects on the heart

A

Increased arterial resistance in small blood vessels. Increased BP leads to baroreceptor reflex that slows the HR.

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31
Q

Alpha receptor effects on the eye

A

Mydriasis. No accommodation. Decreases intraocular presure.

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32
Q

Alpha receptor effects on the respiratory system

A

vasoconstricts the vessels in the nasal mucosa. Act as a decongestant.

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33
Q

Alpha receptor effects on the GU

A

Constrict the sphincters to promote continence. Promotes ejaculation.

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34
Q

Beta receptor effects on the Heart

A

Increased contractility and conduction through the AV node. Increases automaticity. Increased coronary and skeletal muscle blood flow (decreased diastolic BP)

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35
Q

Beta receptor effects on the eye

A

increased intraocular pressure.

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36
Q

Beta receptor effects on the respiratory tract

A

relax bronchial smooth muscle

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37
Q

Beta receptor effects GU

A

Relaxes the uterus

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38
Q

Beta receptor effects on metabolism

A

Increased renin secretion. Glycogenolysis. Increased uptake of potassium. Increased insulin secretio. Lipolysis.

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39
Q

Norepinephrine MOA

A

Stimulates alpha (vasoconstriction) and beta 1 receptors with little effect on beta 2. Must be injected.

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40
Q

Norepinephrine effects

A

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.

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41
Q

Norepinephrine adverse side effects

A

Vasoconstriction at the infusion site can cause necrosis.

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42
Q

Epinephrine MOA

A

Must be injected. Stimulates alpha (Vasoconstriction) , beta 1 (Inotropy/chronotropy) and beta 2 (Vasodilation in skeletal muscle) receptors. Short duration of action.

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43
Q

Epinephrine effects

A

Increased pulse pressure. Increased BP and increased HR. Increases blood glucose and FFA concentrations. Increased renin secretion.

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44
Q

Epinephrine infused slowly

A

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.

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45
Q

Epinephrine rapid infusion

A

Increases blood pressure with a slight increase in HR.

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46
Q

Epinephrine uses

A

anaphylactic shock, cardiac arrest, complete heart block, vasoconstictor to decrease diffusion of local anesthetics, glaucoma, asthma (bronchodilation).

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47
Q

Epinephrine side effects

A

Tremor, throbbing HA, increased BP, tachycardia, angina

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48
Q

Epinephrine contraindications

A

Beta blocker use. Can cause severe hypertension.

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49
Q

Epinephrine Dose dependence

A

Vasodilation dominates at low doses while vasoconstriction at high doses.

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50
Q

Ephedrine MOA

A

Stimulates alpha and beta receptors. Long duration of effect.

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51
Q

Ephedrine effects

A

Increases HR and BP. Causes bronchodilation.

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52
Q

Ephedrine adverse effects

A

hemorrhagic stroke and death due to severe hypertension.

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53
Q

Phenylephrine MOA

A

Alpha 1 agonist.

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54
Q

Phenylephrine effects

A

Vasoconstriction increases BP with a reflex decrease in HR.

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55
Q

Phenylephrine uses

A

Hypotensive emergency, decongestant, mydriasis.

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56
Q

Pseudophedrine uses

A

decongestant. Use caution in those with HTN.

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57
Q

Xylometazoline MOA

A

Alpha receptor stimulant

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58
Q

Xylometazoline and Oxymetazoline uses

A

topically as nasal sprays to decrease congestion.

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59
Q

Oxymetazoline MOA

A

Alpha receptor stimulant. Also acts on alpha 2 receptors and can cause hypotension is a large amount is absorbed.

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60
Q

Xylometazoline and Oxymetazoline contraindications

A

narrow-angle glaucoma

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61
Q

Clonidine MOA

A

Acts on alpha 2 receptors in the brain to decrease release of NE and overall SNS output. Used as a transdermal patch.

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62
Q

Clonidine uses

A

treatment of HTN, reduces addictive cravings, decreases hot flashes, used pre-anesthetically to cause sedation.

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63
Q

Clonidine adverse side effects

A

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.

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64
Q

Methyladopa uses

A

similar to clonidine.

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65
Q

Apraclonidine uses

A

Used in the eye to decrease intraocular pressure

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66
Q

Tizanidine uses

A

Less effective on lowering BP but effective at reducing muscle spasticity.

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67
Q

Isoproterenol MOA

A

Beta 1 and Beta 2 agonists

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68
Q

Isoproterenol effects

A

Increases HR and force of contraction. Causes vasodilationand decreases BP.

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69
Q

Isoproterenol uses

A

Cardiac arrest and complete heart block

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70
Q

Isoproterenol adverse side effects

A

tachycardia, palpitations and arrhythmias.

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71
Q

Dobutamine MOA

A

Beta 1 agonist with some effect on alpha receptors

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72
Q

Dobutamine effects

A

Positive inotrope that increases CO. Increases BP and HR

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73
Q

Dobutamine uses

A

cardiac stress tests, cardiogenic shock and CHF.

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74
Q

Albuterol MOA

A

Beta 2 agonist. With little effect on Beta 1 receptors.

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75
Q

Albuterol uses

A

asthma

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76
Q

Albuterol adverse effects

A

HA, tachycardia, tremor.

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77
Q

Mirabegron MOA

A

Beta 3 receptor agonist

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78
Q

Mirabegron uses

A

treatment of overactive bladder.

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79
Q

Mirabegron adverse effects

A

nausea, HA, HTN, diarrhea, constipation, dizziness and tachycardia.

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80
Q

Low dose dopamine MOA

A

D1 receptors that cause vasodilation and increases renal blood flow.

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81
Q

High dose dopamine MOA

A

Stimulates Beta 1 receptors and produce a positive ionotropic and chronotropic effect.

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82
Q

Dopamine uses

A

Cardiogenic shock

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83
Q

Dopamine adverse effects

A

Nausea, vomiting, tachycardia, angina, arrhythmias, HA, and peripheral vasoconstriction.

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84
Q

Fenoldopam MOA

A

D1 agonsit

85
Q

Fenoldopam effects

A

dilation of vascular beds which decrease BP.

86
Q

Fenoldopam uses

A

Treatment of a hypertensive crisis.

87
Q

Amphetamine MOA

A

increases the release of NE and DA

88
Q

Amphetamine effects

A

alertness, insomnia, decreased appetite, euphoria, increases motor activity.

89
Q

Amphetamine adverse effects

A

Psychosis, HA, chills, pallor, arrhythmias, HTN, cerebral hemmorhage, convulsions

90
Q

Amphetamine uses

A

enuresis. Causes contraction of the bladder sphincter.

91
Q

Methamphetamine uses

A

Recreational drug

92
Q

Methylphenidate uses

A

(ritalin) ADHD

93
Q

Cocaine MOA

A

inhibits re-uptake of DA and NE.

94
Q

Cocaine effect

A

Vasoconstrictor. Can cause severe HTN.

95
Q

Cocaine adverse effects

A

Stroke, arrhythmias, MI, tachycardia. Long-term use can causes psychosis.

96
Q

Tyramine MOA

A

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
Q

Phentolamine (Regitine)

A

Alpha-receptor blocker. Reversible antagonist.

98
Q

Phenoxybenzamine (Dibenzyline)

A

Alpha-receptor blocker. non competitive, irreversible antagonist.

99
Q

Prazosin (minipress)

A

Alpha 1 blocker. Reversible antagonist.

100
Q

Terazosin (Hytrin)

A

Alpha 1 blocker. Reversible antagonist.

101
Q

Doxazosin (cardura)

A

Alpha 1 blocker. Reversible antagonist.

102
Q

Alfuzosin (Uroxatral)

A

Alpha 1 blocker

103
Q

Tamsulosin (Flomax)

A

Alpha 1 blocker

104
Q

Yohimbine

A

Alpha 2 blocker

105
Q

Propranolol (inderal)

A

Beta blocker

106
Q

Timolol (timoptic)

A

Beta blocker

107
Q

Nadolol (corgard)

A

Beta blocker

108
Q

Metoprolol (Lopressor)

A

Cardiospecific/Beta1 blocker

109
Q

Atenolol (Tenormin)

A

Cardiospecific/Beta1 blocker

110
Q

Bisoprolol (zebeta)

A

Cardiospecific/Beta1 blocker

111
Q

acebutolol (sectral)

A

Cardiospecific/Beta1 blocker with intrinsic sympathetic activity.

112
Q

Esmolol (brevibloc)

A

Cardiospecific/Beta1 blocker

113
Q

Betaxolol (betoptic)

A

Cardiospecific/Beta1 blocker

114
Q

Nebivolol (bystolic)

A

Cardiospecific/Beta1 blocker

115
Q

Pindolol (visken)

A

beta blocker with intrinsic sympathetic activity

116
Q

Carteolol (Cartol)

A

beta blocker with intrinsic sympathetic activity

117
Q

Carvedilol (Coreg)

A

Combo beta and alpha blocker

118
Q

Labetalol (Normodyne)

A

Combo beta and alpha blocker

119
Q

Guanethidine (ismelin)

A

Affects neurotransmitter release

120
Q

Reserpine

A

Affects neurotransmitter release

121
Q

Metryrosine (demsar)

A

synthesis inhibitor

122
Q

Alpha 1 blockers effects

A

decrease BP, orthostatic hypotension, miosis, esier to urinate, inhibit ejaculation.

123
Q

Alpha 2 blockers effects

A

increased NE and insulin release.

124
Q

Beta blockers effects

A

Decreased HR and contraction, decreased renin secretion, bronchoconstriction, decreased glycogenolysis and lipolysis, decreased intraocular pressure.

125
Q

Alpha blockade effects on the heart

A

Lowers peripheral resistance (postural hypotension). Reflex tachycardia. Used for epinephrine reversal to block it’s alpha effects and decrease BP.

126
Q

Alpha blockade effects on the eye

A

Miosis

127
Q

Alpha blockade effect on the nose

A

congestion due to vasoconstriction

128
Q

Alpha blockade effect on the GU system

A

decreases resistance to urine flow (BPH) and inhibits ejaculation.

129
Q

Phentolamine MOA

A

Competitive antagonist of alpha 1 and alpha 2 receptors.

130
Q

Phentolamine effects

A

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
Q

Phentolamine uses

A

hypertensive crisis of to prevent necrosis of tissue where a vasoconstrictor has been injected.

132
Q

Phentolamine adverse effects

A

tachycardia, arrhythmia, MI, Hypotension, abdominal pain, peptic ulcers.

133
Q

Phenoxybenzamine MOA

A

irreversible alpha blocker that bind covalently to the receptor. Also inhibits reuptake of NE

134
Q

Phenoxybenzamine effects

A

Decreases peripheral resistance.

135
Q

Phenoxybenzamine uses

A

Treatment of pheochromocytoma.

136
Q

Phenoxybenzamine adverse effects

A

Hypotension (if hypovolemic), postural hypotension, tachycardia, nasal congestion, inhibition of ejaculation. With Epi can cause hypotension and tachycardia.

137
Q

Prazosin MOA

A

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
Q

Prazosin effects

A

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
Q

Prazosin uses

A

HTN, BPH.

140
Q

Prazosin adverse effects

A

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
Q

Terazosine MOA

A

Selective alpha one receptor blockade. 12 hour half life (given once daily).

142
Q

Terazosine uses

A

BPH

143
Q

Terazosine adverse effects

A

first dose phenomenon

144
Q

Doxazosin MOA

A

Selctive alpha one receptor blockade. 20 hour half life

145
Q

Doxazosin uses

A

BPH

146
Q

Doxazosin adverse effects

A

first dose phenomenon

147
Q

Tamsulosin MOA

A

Selective blockade for alpha 1a receptors (prostate). Half life of 5-10 hours. Metabolized by P450s.

148
Q

Tamsulosin effects

A

Relaxes the prostate (alpha 1a) with little effect on BP (alpha 1b). Also relaxes the bladder sphincter.

149
Q

Tamsulosin uses

A

BPH

150
Q

Tamsulosin adverse effects

A

Difficulty ejaculating.

151
Q

Alfuzosin uses

A

BPH

152
Q

Alfuzosin adverse effects

A

dizziness

153
Q

Yohimbine MOA

A

Selective alpha 2 antagonist that increases NE release

154
Q

Yohimbine effects

A

Increases BP and HR. Increase in SNS may increase libido (“natural viagra”).

155
Q

Yohimbine contraindications

A

dangerous in men with HTN.

156
Q

Beta blocker effect on the heart

A

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
Q

Beta blocker contraindications

A

Pheochromocytoma without concomitant administration of an alpha blocker. Those with asthma.

158
Q

Beta blocker effects on the respiratory system

A

Beta 2 blockers will cause bronchoconstriction.

159
Q

Beta blocker effects on the eye

A

reduce intraocular pressure

160
Q

Beta blocker effects on metabolism

A

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
Q

Beta blocker use as a local anesthetic

A

Acebutolol, labetalol, metoprolol, pindolol, propranolol. Membrane stabilizing through blockade of sodium channels. Don’t use an an anesthetic in the eye.

162
Q

Propranolol MOA

A

Non-selective (beta 1 and 2) competitive antagonist.

163
Q

Propranolol effects

A

Slows the HR, decreases AV conduction, decreases contractility, decreases renin release, decreases lipolysis and glycogenolysis. Can have local anesthetic effects.

164
Q

Propranolol pharmacokinetics

A

Oral. Sustained release. Lipid soluble (CNS penetration). Metabolized in liver with a 3-6 hour half life.

165
Q

Propranolol uses

A

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
Q

Propranolol adverse effects

A

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
Q

Drugs that inhibit metabolism of Propranolol

A

cimetidine and chlorpromazine.

168
Q

Drugs that increase metabolism of Propranolol

A

barbituates, phenytoin, rifampin and smoking. Calcium channel blockers can have an additive effect.

169
Q

Timolol uses

A

Glaucoma. Can be used systemically like Propranolol.

170
Q

Timolol contraindications

A

asthma

171
Q

Nadolol uses

A

similar to Propranolol but has a longer half life. Doesn’t penetrate the CNS so less likely to cause sedation.

172
Q

Sotalol uses

A

Blocks potassium channels and has class three antiarrythmic activity.

173
Q

The beta 1 selective antagonists

A

Metroprolol, Atenolol and bisoprolol

174
Q

beta 1 selective antagonists effects

A

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
Q

beta 1 selective antagonists uses

A

HTN, post-MI, migraine prophylaxis.

176
Q

beta 1 selective antagonists adverse effects

A

dizziness, fatigue, bradycardia and hypotension.

177
Q

Atenolol and diabetes

A

Reduces the risk for type 2 diabetes.

178
Q

beta 1 selective antagonists contraindications

A

Use caution in patients with COPD and asthma because the selectivity is not absolute and at high doses can effect beta 2 receptors.

179
Q

Betaxolol MOA

A

selective beta 1 blocker. Less likely to cause bronchoconstriction than timolol.

180
Q

Betaxolol uses

A

glaucoma

181
Q

Nebivolol MOA

A

Selective beta 1 blocker that increases the release of Nitric oxide. Lowers BP without depressing LV function.

182
Q

Nebivolol effects

A

Lowers BP (nitric oxide) and decreases cholesterol, triglycerides and BGL.

183
Q

Esmolol MOA

A

selective beta 1 blocker with a very short duration of action (8 mins). Must be administered IV.

184
Q

Esmolol Uses

A

Used when short blockade is needed or when necessary to rapidly remove the beta blocker effect.

185
Q

Intrinsic Sympathetic activity

A

Means the drug is a partial agonist

186
Q

Beta blockers with ISA uses

A

treatment of HTN and angina. Risk of bradycardia is lower than with other beta blockers.

187
Q

Carteolol uses

A

Glaucoma

188
Q

Beta blockers with ISA

A

Pindolol, carteolol, penbutolol. Acebutolol (selective Beta 1)

189
Q

Labetalol MOA

A

Blocks Beta 1, Beta 2 and alpha 1 receptors.

190
Q

Labetalol effects

A

Decreased BP without the compensatory increase in HR.

191
Q

Labetalol uses

A

HTN emergencies

192
Q

Carvedilol MOA

A

Non-selective beta blocker that also blocks alpha 1 receptors.

193
Q

Carvedilol effects

A

Reduces BP without a compensatory increase in HR. Reduces the effects of free radicals on vascular smooth muscle.

194
Q

Carvedilol uses

A

Decreases morbidity/mortality in CHF. Treatment of HTN.

195
Q

Clinical uses of beta blockers

A

HTN, Ischemic heart disease, arrhythmias, obstructive cardiomyopathy, dissecting aortic aneurysm, hyperthyroidism, migraines.

196
Q

Beta blockers that improve survival after an MI

A

Timolol, propranolol and metoprolol

197
Q

Beta blockers that can be used in early CHF

A

Metoprolol, carvedilol and bisprolol.

198
Q

Beta blockers to treat hyperthyroidism

A

propranolol

199
Q

Beta blockers for migraine prophylaxis

A

propranolol, metoprolol and atenolol.

200
Q

DOC for glaucoma

A

Prostaglandin analogues (latanoprost)

201
Q

Beta blockers for glaucoma

A

Timolol, carteolol and betaxolol (beta 1 selective). Second line treatment. Decreases production of aqueous humor.

202
Q

alpha 2 agonists for glaucoma

A

apraclonidine. Decreases production of aqueous humor and increases outflow.

203
Q

Cholinergic agonist for glaucoma

A

Pilocarpine, carbachol, phyostigme and echothiophate. Rarely used because they effect vision.

204
Q

Guanethidine MOA

A

Inhibits the release of NE. No longer used.

205
Q

Reserpine MOA

A

Causes the depletion of NE, DA and serotonin by inhibitng uptake of biogenic amines.

206
Q

Reserpine adverse effects

A

No longer used. Diarrhea, depression, sedation and parkinson’s like symptoms.

207
Q

Metyrosine MOA

A

Tyrosine analogue that blocks tyrosine hydroxylase. Decreases the amount of DA, NE and Epi.

208
Q

Metyrosine uses

A

Pre-surgical treatment of pheochromocytoma.

Pharmacology (24 decks)

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