Test 1: Wk3: 3 Adrenergic Agonists and Antagonists - Salisbury Flashcards

1
Q

indirect sympathomimetic agents MOA

A

indirect acting drugs ⬆️ The availability of NE or EPI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

4 indirect acting releasing agents

A
  1. Amphetamine
    2 Methylphenidate
    3 Tyramine
    4 Ephedrine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Ephedrine can also stimulate … and …

A

alpha and Beta Receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Indirect acting Releasing Agents uses

A

ADHD

Hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

2 Indirect Acting uptake inhibitors

A

1 cocaine

2 TCA impiramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Indirect Acting uptake inhibitors uses

A

Depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Indirect Acting MAO inhibitors

A

TranyIcypromine
Phenezine
selegiline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Indirect Acting uptake inhibitors COMT inhibitors

A

Intacapone

Talcapone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Indirect Acting uptake inhibitors MAO inhibitors uses

A

Depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Avoid … w/ MOA inhibitors

A

Tyramine causes hypertensive crisis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Indirect Acting uptake inhibitors COMT inhibitors uses

A

Parkinson’s

⬆️ Levodopa

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Direct Acting sympathomimetic Drugs

A

catecholamines

Noncatecholamines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

catecholamines (5)

A
1 Dopamine
2 Isoproterenol
3 NE
4 EPI
5 Dobutamine
DINED
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Can catecholamines and noncatecholamines be given orally

A

No they’re too rapidly metabolized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Noncatecholamines (3)

A

1.phenylephrine
2 ephedrine
3 amphetamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

a 1

A

vasoconstriction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

B2

A

vasodilation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Norepinephrine Receptors

A

a1 a2 B1&raquo_space;> B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Epinepherine Receptors

A

a1 a2 B1 B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Isoproteronol Receptors

A

B1 B2&raquo_space;> a1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Norepinephrine effect on pulse rate

A

Slight decrease a1&raquo_space; B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Epinephrine effect on pulse rate

A

Slight increase, dose Dependent B2 > a1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Isoproterenol effect on pulse rate

A

Increase B2&raquo_space;> a1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

NE effect on BP

A

increase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Epi effect on BP

A

slight increase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Isoproterenol effect on BP

A

slight decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

NE effect on peripheral resistance

A

increase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Epi effect on peripheral resistance

A

slight decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Isoproterenol effect on peripheral resistance

A

decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

Low dose Epi

A

higher affinity for B2

TPR decrease

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Epi high dose

A

Epi receptor selectivity is lost
a1=B2
TPR increase and MBP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Epi reversal

A

Phenoxybenzamine

a1 and A2 block

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

adrenergic agonists MOA

A

mimic effects of SNS - sympathomimetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

adrenergic agonists exception

A

a2 receptor agonists are sympatholytic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

Epinephrine is an agonist at

A

a1, a2, B1, B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

Epi causes

A

bronchodilation - B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

Epi CV effects low dose

A

vasodilation - B2 more sensitive than a receptors

tachycardia - direct B1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Epi CV effects low dose net

A

net effect ⬆ TPR, slight ⬆ BP ⬆HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Epi CV effects high dose

A

vasoconstriction - a receptor activation dominates)
⬆ TPR ➡ ⬆ BP
direct B1 ➡ ⬆HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

Epi CV effects high dose net

A

⬆ TPR ⬆BP ⬆HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

Epi metabolic effects

A
  • hyperglycemia
  • ⬆ glycogenolysis and gluconeogenesis
  • ⬆ blood glucose
  • ⬆ free FAs in blood
  • ⬇ plasma K+
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

Epi a2 does what to insulin secretion

A

⬇⬇

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Epi B2 does what to insulin secretion

A

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

Epi a2>B2 net effect on insulin

A

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

Epi what receptor ⬆ glycogenolysis and gluconeogenesis

A

B2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

Epi — receptors in adipocytes — FFAs in blood

A

B; ⬆

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

Epi — receptors — K+ plasma concentrations

A

B2; ⬇

they increase K+ uptake thus lowering it in plasma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

Epi therapeutic uses (5)

A
1 Anaphylaxis 
2 Bronchospasm 
3 Cardiac Arrest
4 prolong action of local anesthetic 
5 glaucoma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
49
Q

Epi kinetics

A

catecholamine

not effective orally must be IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
50
Q

Epi adverse effects (4)

A

1 marked hyperglycemia
2 cardiac stimulation
3 vasoconstriction
4 CNS stimulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
51
Q

Epi vasoconstriction adverse effects

A

hypertension, slough at injection site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
52
Q

Epi CNS Stimulation Adverse Effects

A

⬆ respiration, apprehension, tremor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
53
Q

Epi contraindications

A

tachyarrhythmias, hyperthyroidism

⬆ toxicity with MAO inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
54
Q

NE is an agonists at

A

a1, a2, B1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
55
Q

NE CV effects

A

vasoconstriction ➡ ⬆TPR ➡⬆ mean BP

+- HR ➡ direct B effect + reflexes ➡ +- HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
56
Q

NE CV net effects

A

⬆ TPR ⬆ BP +- HR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
57
Q

NE therapeutic effects

A

septic and cardiogenic shock

MOA vasoconstriction + inotropic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
58
Q

NE Kinetics

A

catecholamine IV only

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
59
Q

NE adverse effects

A

cardiac - arrhythmias, angina

vasoconstriction - hypertension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
60
Q

NE Contraindications

A

tachyarrhythmias, hyperthyroidism, hypertension

⬆ toxicity with MAO Inhibitors
⬆ toxicity with cocaine and reuptake inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
61
Q

Dopamine is a direct — at —- — receptors

A

agonist, dopaminergic, D1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
62
Q

what does dopamine do

A

dilates renal, splanchnic, cerebral, and coronary vessels

Causes release of NE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
63
Q

Dopamine CV Low dose

A

D1 receptor mediated selective vasodilation of renal and splanchnic vessels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
64
Q

Dopamine CV moderate dose

A

D1 receptor mediated vasodilation ➡ ⬇ TPR

Direct and reflex B1 receptor mediated effects ➡⬆HR, ⬆ CO

+- BP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
65
Q

Dopamine CV High dose

A

a1 receptor mediated vasoconstriction > D1 mediated vasodilation ➡ ⬆ TPR

B1 receptor Cardiac Effects ➡ ⬆ HR

⬆ BP

66
Q

Dopamine protects the

A

kidney

67
Q

Dopamine therapeutic effects

A

Shock

Acute CHF

68
Q

Dopamine Shock tx MOA

A

renal vasodilation, peripheral vasoconstriction, +inotrope

69
Q

Dopamine Acute CHF tx MOA

A

renal vasodialation, +inotrope

70
Q

Dopamine Kinetics

A

catecholamine

71
Q

Dopamine Adverse Effects

A

similar to NE

cardiac - arrhythmias, angina
vasoconstriction - hypertension

72
Q

Pseudoephedrine has direct effects on

A

adrenergic receptors + release of NE

73
Q

Pseudoephedrine effects

A

vasoconstriction +- HR

from NE

74
Q

Pseudoephedrine therapeutic indications

A

Decongestant

vasoconstriction of nasal mucosa

75
Q

Pseudoephedrine adverse effects

A

hypertension

insomnia

76
Q

Dobutamine: effects

A

complex action of enantiomers on α 1 , ꞵ1 , ꞵ2 receptors

77
Q

Dobutamine Effects in pts with CHF

A

+ inotrope → ↑ CO

±HR, ±TPR, ±BP

78
Q

Dobutamine Therapeutic indications

A

acute CHF (MOA: + inotrope)

79
Q

Dobutamine

A

catecholamine (t1/2 = mins, IV only)

80
Q

Dobutamine Adverse effects

A

arrythmias, ↑ MVO2, ↑ AV nodal conduction

hypertension in some pts

81
Q

Isoproterenol agonist at

A

ꞵ1 & ꞵ2 receptors

82
Q

Isoproterenol Effects

A

bronchodilation

CV effects

83
Q

Isoproterenol CV effects

A

direct ꞵ2 effects → vasodilation (in sk musc ) → ↓TPR, ↓ BP

direct ꞵ1 + reflex ( ꞵ1) cardiac effects → ↑ HR

84
Q

Isoproterenol Net cardiac effects

A

net effect → ↓ TPR, ↓ BP, ↑ HR

85
Q

Isoproterenol Therapeutic effects

A

Reverse Bronchospasm ( β 2 effect)

cardiac arrest (MOA: + chronotrope , +

heart block (MOA: reduces block by ↑ AV

86
Q

how does Isoproterenol reverse bronchospasm

A

β 2 effect

87
Q

how does Isoproterenol help cardiac arrest

A

MOA: + chronotrope , +inotrope

88
Q

how does Isoproterenol help heart block

A

reduce block by ⬆ AV Conduction

89
Q

Isoproterenol Kinetics

A

catecholamine (not effectively orally, t1/2 = mins)

90
Q

Isoproterenol Adverse effects

A

cardiac stimulation

tremor

91
Q

Isoproterenol Contraindications/precautions

A

tachyarrhythmia

hyperthyroidism

92
Q

3 Selective

α 1 receptor agonists

A

Phenylephrine, Methoxamine, Midodrine

93
Q

Phenylephrine, Methoxamine, Midodrine Effects

A

mydriasis

vasoconstriction → ↑ TPR → ↑ BP

reflex ↓ HR

94
Q

Phenylephrine, Methoxamine, Midodrine Therapeutic uses

A

mydriatic

decongestant

prolonged action of local anesthetics

hypotension

95
Q

Phenylephrine, Methoxamine, Midodrine

Adverse effects

A

hypertension

reflex bradycardia

96
Q

Selective

α 2 receptor agonists

A

Clonidine

97
Q

Clonidine Effects

A

CNS → ↓sympathetic outflow → vasodilation → ↓ TPR → ↓ BP

little reflex ↑ HR (CNS effect → ↑ vagal tone → ±HR despite ↓ BP

98
Q

Clonidine is a

A

sympatholytic

a2 agonist

99
Q

Clonidine Therapeutic uses

A

Hypertension

drug addiction

ADHD

100
Q

how does Clonidine improve hypertension

A

⬇ sympathetic outflow from CNS

101
Q

Clonidine Adverse effects

A

hypertensive crisis upon sudden withdrawal (rebound hypertension)

sedation

sexual dysfunction

102
Q

Selective

β 2 agonists

A

β 2&raquo_space; β 1

Albuterol

103
Q

Albuterol Effects

A

bronchodilation

vasodilation → reflex ↑ HR

104
Q

Albuterol Therapeutic uses

A

reverse bronchospasm

asthma, COPD

105
Q

Albuterol Adverse effects

A

cardiac stimulation (arrhythmias, angina)

can activate β1 receptors at high doses

reflex tachycardia due to baroreceptor reflex

Tremor

106
Q

Albuterol contraindications/precautions

A

tachyarrhythmia

hyperthyroidism

107
Q

Selective

β 2 agonists Long acting

A

Salmeterol

Formoterol

Induce bronchodilation for up to 12 hours

108
Q

Adrenergic Receptor Antagonists function

A

inhibit action of endogenous
NE & Epi at receptor sites

Also inhibit actions of exogenously administered drugs that
function as adrenergic agonists
109
Q

Nonselective

α 1 & α 2 antagonists

A

Phenoxybenzamine

Phenoxybenzamine

110
Q

Phenoxybenzamine

A

non competitive block at α 1 & α 2 receptors

111
Q

Phenoxybenzamine Effects

A

vasodilation → ↓ TPR → ↓ BP

reflex ↑ HR (also blocking α 2 ↑ sympathetic outflow from CNS to
induce tachycardia)

112
Q

Phenoxybenzamine Kinetics

A

slow onset

long lasting

effective orally

113
Q

Phenoxybenzamine Therapeutic uses

A

preoperative or chronic Tx of pheochromocytoma (with β blockers)

Tx of reversible vasospastic disease

114
Q

Phenoxybenzamine Adverse effects/contraindications/precautions

A

tachycardia, arrhythmias, angina

orthostatic hypotension

sexual dysfunction

115
Q

Phentolamine function

A

Competitively blocks α 1 & α 2 receptors

116
Q

Phentolamine vs Phenoxybenzamine

A

faster onset/shorter duration of action (t1/2 = mins)

must be administered IV

117
Q

Phentolamine Therapeutic uses

A

hypertensive crisis (e.g. clonidine withdrawal)

during surgical removal of pheochromocytoma

reversible vasospastic disease (e.g. frostbite)

118
Q

Relatively selective α
1 Receptor
Antagonists

A

Doxazosin (Prazosin, Terazosine, Alfuzosin

119
Q

Doxazosin (Prazosin, Terazosine, Alfuzosin) Effects

A

arterial dilation → ↓ TPR → ↓ BP

little to no reflex ↑ HR

relaxation of the bladder sphincter and urethra

120
Q

Doxazosin (Prazosin, Terazosine, Alfuzosin) therapeutic uses

A

↑ urine flow in benign prostatic hypertrophy

hypertension

121
Q

Doxazosin (Prazosin, Terazosine, Alfuzosin)

adverse effects

A

first dose syncope → due to ↓ BP

begin therapy at night

occurs in volume depleted patients

122
Q

Tamsulosin function

A

selective inhibition of α 1A receptors may provide some selectivity for sphincter and urethra

123
Q

Tamsulosin effects

A

relax bladder sphincter

124
Q

Tamsulosin Therapeutic uses

A

↑ urine flow in benign prostate hypertrophy

125
Q

Tamsulosin Adverse effects/contraindications/precautions

A

orthostatic hypotension

126
Q

Yohimbine is a

A

(competitive antagonist that is selective for α 2 receptors)

127
Q

Yohimbine function •

In the CNS

A

→ ↑release of NE → blood pressure and heart rate

128
Q

Yohimbine effects

A

↑ motor activity and produces tremors.

129
Q

β 1 Receptor inhibition

A

heart

↓ automaticity → ↓ HR

↓ contractility

↓ conduction velocity

130
Q

β 2 Receptor inhibition

A

bronchonstriction

↓ glycogenolysis

↑ TPR

131
Q

Nonselective β Receptor Antagonists

A

Propranolol

132
Q

Propranolol MOA

A

competitive inhibition of β 1 = β 2

133
Q

Propranolol CV effects heart

A
  • ↓ automaticity → HR
  • ↓ contractility → CO
  • ↓ myocardial oxygen consumption
  • ↓ AV nodal conduction velocity
134
Q

Propranolol CV effects long term

A

↓ BP

↓ CO

↓ renin release

±TPR

135
Q

Propranolol: non

CV Effects

A

Bronchoconstriction

↓ intraocular pressure in glaucoma (↓ aqueous humor

  • ↓ lipolysis → ↓ FFA → ↑ triglycerides
  • ↓ HDL
136
Q

Propranolol Metabolic Effects

A

↓ glycogenolysis → prolong hypoglycemic event

↓ insulin release → hyperglycemia

137
Q

Propranolol Kinetcs

A

orally effective (poor availability)

Hepatic metabolism

138
Q

Propranolol Kinetcs

A

orally effective (poor availability)

Hepatic metabolism

139
Q

Propranolol Therapeutic uses (9)

A

hypertension

chronic stable angina

arrhythmias

Post MI

hyperthyroidism

pheochromocytoma

migraine prophylaxis

stage fright

essential tremors

140
Q

Propranolol Adverse Effects and Contraindications

A

slide 54

141
Q

Timolol, Nadolol

A

Similar to propranolol (competitive inhibition of β 1 = β 2)

142
Q

Timolol, Nadolol Therapeutic uses

A

similar to propranolol (hypertension, post MI)

timolol glaucoma (also levobunolol

143
Q

Cardioselective
ꞵ1 Receptor
Antagonists

A

Metoprolol, Atenolol

144
Q

Metoprolol, Atenolol function

A

inhibit ꞵ1 > ꞵ

145
Q

Metoprolol, Atenolol are Preferred over non specific ꞵblockers in pts with:

A

diabetes (especially in patients that are prone to hypoglycemic reactions)

Raynaud’s syndrome

COPD (still contraindicated in asthmatics)

146
Q

Metoprolol, Atenolol Kinetics

A

metoprolol hepatic metabolism

atenolol renal elimination

147
Q

Metoprolol, Atenolol Therapeutic uses:

A

similar to propranolol

CHF metoprolol

148
Q

Esmolol

A

Cardioselective
ꞵ1 Receptor
Antagonists

149
Q

Esmolol function

A

very short acting Cardioselective ꞵ blocker

150
Q

Esmolol kinetics

A

metabolized by red blood cell esterase

151
Q

Esmolol Therapeutic uses

A

used as antiarrhythmic (IV only)

152
Q

Mixed Action

ꞵ Blockers

A

Carvedilol, Labetalol

153
Q

Carvedilol, Labetalol function

A

non specific ꞵ block + α 1 blocker effects

antioxidant activity

154
Q

Carvedilol, Labetalol effects

A

non specific ꞵ block + α 1 blocker effects

↓ TPR

±HR, CO

↑ HDL

155
Q

Carvedilol, Labetalol Therapeutic uses

A

hypertension

CHF

156
Q

Carvedilol, Labetalol Adverse effects/contraindications/precautions

A

same as other β blockers

+ hypotension due to α1 block

157
Q

Nebivolol function

A

Cardioselective β 1 block + NO mediated vasodilation

158
Q

Nebivolol effects

A

↓ TPR

±HR, CO

159
Q

Nebivolol Therapeutic uses

A

hypertension, CHF

160
Q

Nebivolol Adverse effects/contraindications/precautions

A

same as other ꞵ blockers

+ more prominent hypotension due to NO mediated vasodilation