Adrenergic Drugs Flashcards Preview

Pharmacology > Adrenergic Drugs > Flashcards

Flashcards in Adrenergic Drugs Deck (208):
1

Epinephrine (Adrenalin)

Catecholamine. High affinity for Beta-2 receptors.

2

Norepinephrine (Levophed)

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

3

Isoproterenol (Isuprel)

Catecholamine. Equal affinity for all beta receptors.

4

Phenylephrine (Neofrin; neosynephrine)

Alpha-1 agonist

5

Pseudoephedrine (Sudafed)

Alpha-1 agonist

6

Xylometazoline (Otrivin)

Alpha-1 agonist

7

Oxymetazoline (Afrin)

Alpha-1 agonist

8

Midodrine (ProAmatine)

Alpha-1 agonist

9

Clonidine (Catapress)

Alpha-2 agonist

10

Methyldopa (Aldomet)

Alpha-2 agonist

11

Apraclonidine (Iopidine)

Alpha-2 agonist

12

Dobutamine (Dobutrex)

Beta-1 agonist

13

Albuterol (Ventolin)

Beta-2 agonist

14

Ritodrine (Yutopar)

Beta-2 agonist

15

Mirabegron (Myrbetriq)

Beta-3 agonist

16

Ephedrine

"other" adrenergic stimulant

17

Amphetamine

"other" adrenergic stimulant

18

Methylphenidate (Ritalin)

"other" adrenergic stimulant

19

Methamphetamine

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

20

Cocaine

"other" adrenergic stimulant. inhibits reuptake of NE.

21

Tyramine

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

22

Dopamine (Intropin)

Dopamine agonist

23

Fenoldopam (Corlopam)

Dopamine agonist

24

VMA/HVA test

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.