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BMS 615 Cardiovascular > Test 1: Wk3: 3 Adrenergic Agonists and Antagonists - Salisbury > Flashcards

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

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2
Q

4 indirect acting releasing agents

A
  1. Amphetamine
    2 Methylphenidate
    3 Tyramine
    4 Ephedrine
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3
Q

Ephedrine can also stimulate … and …

A

alpha and Beta Receptors

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4
Q

Indirect acting Releasing Agents uses

A

ADHD

Hypotension

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5
Q

2 Indirect Acting uptake inhibitors

A

1 cocaine

2 TCA impiramine

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6
Q

Indirect Acting uptake inhibitors uses

A

Depression

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7
Q

Indirect Acting MAO inhibitors

A

TranyIcypromine
Phenezine
selegiline

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8
Q

Indirect Acting uptake inhibitors COMT inhibitors

A

Intacapone

Talcapone

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9
Q

Indirect Acting uptake inhibitors MAO inhibitors uses

A

Depression

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10
Q

Avoid … w/ MOA inhibitors

A

Tyramine causes hypertensive crisis

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11
Q

Indirect Acting uptake inhibitors COMT inhibitors uses

A

Parkinson’s

⬆️ Levodopa

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12
Q

Direct Acting sympathomimetic Drugs

A

catecholamines

Noncatecholamines

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13
Q

catecholamines (5)

A 
1 Dopamine
2 Isoproterenol
3 NE
4 EPI
5 Dobutamine
DINED
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14
Q

Can catecholamines and noncatecholamines be given orally

A

No they’re too rapidly metabolized

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15
Q

Noncatecholamines (3)

A

1.phenylephrine
2 ephedrine
3 amphetamine

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16
Q

a 1

A

vasoconstriction

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17
Q

B2

A

vasodilation

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18
Q

Norepinephrine Receptors

A

a1 a2 B1&raquo_space;> B2

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19
Q

Epinepherine Receptors

A

a1 a2 B1 B2

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20
Q

Isoproteronol Receptors

A

B1 B2&raquo_space;> a1

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21
Q

Norepinephrine effect on pulse rate

A

Slight decrease a1&raquo_space; B2

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22
Q

Epinephrine effect on pulse rate

A

Slight increase, dose Dependent B2 > a1

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23
Q

Isoproterenol effect on pulse rate

A

Increase B2&raquo_space;> a1

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24
Q

NE effect on BP

A

increase

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25
Epi effect on BP
slight increase
26
Isoproterenol effect on BP
slight decrease
27
NE effect on peripheral resistance
increase
28
Epi effect on peripheral resistance
slight decrease
29
Isoproterenol effect on peripheral resistance
decrease
30
Low dose Epi
higher affinity for B2 | TPR decrease
31
Epi high dose
Epi receptor selectivity is lost a1=B2 TPR increase and MBP
32
Epi reversal
Phenoxybenzamine | a1 and A2 block
33
adrenergic agonists MOA
mimic effects of SNS - sympathomimetic
34
adrenergic agonists exception
a2 receptor agonists are sympatholytic
35
Epinephrine is an agonist at
a1, a2, B1, B2
36
Epi causes
bronchodilation - B2
37
Epi CV effects low dose
vasodilation - B2 more sensitive than a receptors | tachycardia - direct B1
38
Epi CV effects low dose net
net effect ⬆ TPR, slight ⬆ BP ⬆HR
39
Epi CV effects high dose
vasoconstriction - a receptor activation dominates) ⬆ TPR ➡ ⬆ BP direct B1 ➡ ⬆HR
40
Epi CV effects high dose net
⬆ TPR ⬆BP ⬆HR
41
Epi metabolic effects
- hyperglycemia - ⬆ glycogenolysis and gluconeogenesis - ⬆ blood glucose - ⬆ free FAs in blood - ⬇ plasma K+
42
Epi a2 does what to insulin secretion
⬇⬇
43
Epi B2 does what to insulin secretion
⬆
44
Epi a2>B2 net effect on insulin
⬆
45
Epi what receptor ⬆ glycogenolysis and gluconeogenesis
B2
46
Epi --- receptors in adipocytes --- FFAs in blood
B; ⬆
47
Epi --- receptors --- K+ plasma concentrations
B2; ⬇ | they increase K+ uptake thus lowering it in plasma
48
Epi therapeutic uses (5)
``` 1 Anaphylaxis 2 Bronchospasm 3 Cardiac Arrest 4 prolong action of local anesthetic 5 glaucoma ```
49
Epi kinetics
catecholamine | not effective orally must be IV
50
Epi adverse effects (4)
1 marked hyperglycemia 2 cardiac stimulation 3 vasoconstriction 4 CNS stimulation
51
Epi vasoconstriction adverse effects
hypertension, slough at injection site
52
Epi CNS Stimulation Adverse Effects
⬆ respiration, apprehension, tremor
53
Epi contraindications
tachyarrhythmias, hyperthyroidism | ⬆ toxicity with MAO inhibitors
54
NE is an agonists at
a1, a2, B1
55
NE CV effects
vasoconstriction ➡ ⬆TPR ➡⬆ mean BP +- HR ➡ direct B effect + reflexes ➡ +- HR
56
NE CV net effects
⬆ TPR ⬆ BP +- HR
57
NE therapeutic effects
septic and cardiogenic shock MOA vasoconstriction + inotropic
58
NE Kinetics
catecholamine IV only
59
NE adverse effects
cardiac - arrhythmias, angina | vasoconstriction - hypertension
60
NE Contraindications
tachyarrhythmias, hyperthyroidism, hypertension ⬆ toxicity with MAO Inhibitors ⬆ toxicity with cocaine and reuptake inhibitors
61
Dopamine is a direct --- at ---- --- receptors
agonist, dopaminergic, D1
62
what does dopamine do
dilates renal, splanchnic, cerebral, and coronary vessels | Causes release of NE
63
Dopamine CV Low dose
D1 receptor mediated selective vasodilation of renal and splanchnic vessels
64
Dopamine CV moderate dose
D1 receptor mediated vasodilation ➡ ⬇ TPR Direct and reflex B1 receptor mediated effects ➡⬆HR, ⬆ CO +- BP
65
Dopamine CV High dose
a1 receptor mediated vasoconstriction > D1 mediated vasodilation ➡ ⬆ TPR B1 receptor Cardiac Effects ➡ ⬆ HR ⬆ BP
66
Dopamine protects the
kidney
67
Dopamine therapeutic effects
Shock Acute CHF
68
Dopamine Shock tx MOA
renal vasodilation, peripheral vasoconstriction, +inotrope
69
Dopamine Acute CHF tx MOA
renal vasodialation, +inotrope
70
Dopamine Kinetics
catecholamine
71
Dopamine Adverse Effects
similar to NE cardiac - arrhythmias, angina vasoconstriction - hypertension
72
Pseudoephedrine has direct effects on
adrenergic receptors + release of NE
73
Pseudoephedrine effects
vasoconstriction +- HR from NE
74
Pseudoephedrine therapeutic indications
Decongestant vasoconstriction of nasal mucosa
75
Pseudoephedrine adverse effects
hypertension insomnia
76
Dobutamine: effects
complex action of enantiomers on α 1 , ꞵ1 , ꞵ2 receptors
77
Dobutamine Effects in pts with CHF
+ inotrope → ↑ CO ±HR, ±TPR, ±BP
78
Dobutamine Therapeutic indications
acute CHF (MOA: + inotrope)
79
Dobutamine
catecholamine (t1/2 = mins, IV only)
80
Dobutamine Adverse effects
arrythmias, ↑ MVO2, ↑ AV nodal conduction hypertension in some pts
81
Isoproterenol agonist at
ꞵ1 & ꞵ2 receptors
82
Isoproterenol Effects
bronchodilation CV effects
83
Isoproterenol CV effects
direct ꞵ2 effects → vasodilation (in sk musc ) → ↓TPR, ↓ BP direct ꞵ1 + reflex ( ꞵ1) cardiac effects → ↑ HR
84
Isoproterenol Net cardiac effects
net effect → ↓ TPR, ↓ BP, ↑ HR
85
Isoproterenol Therapeutic effects
Reverse Bronchospasm ( β 2 effect) cardiac arrest (MOA: + chronotrope , + heart block (MOA: reduces block by ↑ AV
86
how does Isoproterenol reverse bronchospasm
β 2 effect
87
how does Isoproterenol help cardiac arrest
MOA: + chronotrope , +inotrope
88
how does Isoproterenol help heart block
reduce block by ⬆ AV Conduction
89
Isoproterenol Kinetics
catecholamine (not effectively orally, t1/2 = mins)
90
Isoproterenol Adverse effects
cardiac stimulation tremor
91
Isoproterenol Contraindications/precautions
tachyarrhythmia hyperthyroidism
92
3 Selective | α 1 receptor agonists
Phenylephrine, Methoxamine, Midodrine
93
Phenylephrine, Methoxamine, Midodrine Effects
mydriasis vasoconstriction → ↑ TPR → ↑ BP reflex ↓ HR
94
Phenylephrine, Methoxamine, Midodrine Therapeutic uses
mydriatic decongestant prolonged action of local anesthetics hypotension
95
Phenylephrine, Methoxamine, Midodrine | Adverse effects
hypertension reflex bradycardia
96
Selective | α 2 receptor agonists
Clonidine
97
Clonidine Effects
CNS → ↓sympathetic outflow → vasodilation → ↓ TPR → ↓ BP little reflex ↑ HR (CNS effect → ↑ vagal tone → ±HR despite ↓ BP
98
Clonidine is a
sympatholytic a2 agonist
99
Clonidine Therapeutic uses
Hypertension drug addiction ADHD
100
how does Clonidine improve hypertension
⬇ sympathetic outflow from CNS
101
Clonidine Adverse effects
hypertensive crisis upon sudden withdrawal (rebound hypertension) sedation sexual dysfunction
102
Selective | β 2 agonists
β 2 >> β 1 Albuterol
103
Albuterol Effects
bronchodilation vasodilation → reflex ↑ HR
104
Albuterol Therapeutic uses
reverse bronchospasm asthma, COPD
105
Albuterol Adverse effects
cardiac stimulation (arrhythmias, angina) can activate β1 receptors at high doses reflex tachycardia due to baroreceptor reflex Tremor
106
Albuterol contraindications/precautions
tachyarrhythmia hyperthyroidism
107
Selective | β 2 agonists Long acting
Salmeterol Formoterol Induce bronchodilation for up to 12 hours
108
Adrenergic Receptor Antagonists function
inhibit action of endogenous NE & Epi at receptor sites ``` Also inhibit actions of exogenously administered drugs that function as adrenergic agonists ```
109
Nonselective | α 1 & α 2 antagonists
Phenoxybenzamine Phenoxybenzamine
110
Phenoxybenzamine
non competitive block at α 1 & α 2 receptors
111
Phenoxybenzamine Effects
vasodilation → ↓ TPR → ↓ BP reflex ↑ HR (also blocking α 2 ↑ sympathetic outflow from CNS to induce tachycardia)
112
Phenoxybenzamine Kinetics
slow onset long lasting effective orally
113
Phenoxybenzamine Therapeutic uses
preoperative or chronic Tx of pheochromocytoma (with β blockers) Tx of reversible vasospastic disease
114
Phenoxybenzamine Adverse effects/contraindications/precautions
tachycardia, arrhythmias, angina orthostatic hypotension sexual dysfunction
115
Phentolamine function
Competitively blocks α 1 & α 2 receptors
116
Phentolamine vs Phenoxybenzamine
faster onset/shorter duration of action (t1/2 = mins) must be administered IV
117
Phentolamine Therapeutic uses
hypertensive crisis (e.g. clonidine withdrawal) during surgical removal of pheochromocytoma reversible vasospastic disease (e.g. frostbite)
118
Relatively selective α 1 Receptor Antagonists
Doxazosin (Prazosin, Terazosine, Alfuzosin
119
Doxazosin (Prazosin, Terazosine, Alfuzosin) Effects
arterial dilation → ↓ TPR → ↓ BP little to no reflex ↑ HR relaxation of the bladder sphincter and urethra
120
Doxazosin (Prazosin, Terazosine, Alfuzosin) therapeutic uses
↑ urine flow in benign prostatic hypertrophy hypertension
121
Doxazosin (Prazosin, Terazosine, Alfuzosin) | adverse effects
first dose syncope → due to ↓ BP begin therapy at night occurs in volume depleted patients
122
Tamsulosin function
selective inhibition of α 1A receptors may provide some selectivity for sphincter and urethra
123
Tamsulosin effects
relax bladder sphincter
124
Tamsulosin Therapeutic uses
↑ urine flow in benign prostate hypertrophy
125
Tamsulosin Adverse effects/contraindications/precautions
orthostatic hypotension
126
Yohimbine is a
(competitive antagonist that is selective for α 2 receptors)
127
Yohimbine function • | In the CNS
→ ↑release of NE → blood pressure and heart rate
128
Yohimbine effects
↑ motor activity and produces tremors.
129
β 1 Receptor inhibition
heart ↓ automaticity → ↓ HR ↓ contractility ↓ conduction velocity
130
β 2 Receptor inhibition
bronchonstriction ↓ glycogenolysis ↑ TPR
131
Nonselective β Receptor Antagonists
Propranolol
132
Propranolol MOA
competitive inhibition of β 1 = β 2
133
Propranolol CV effects heart
* ↓ automaticity → HR * ↓ contractility → CO * ↓ myocardial oxygen consumption * ↓ AV nodal conduction velocity
134
Propranolol CV effects long term
↓ BP ↓ CO ↓ renin release ±TPR
135
Propranolol: non | CV Effects
Bronchoconstriction ↓ intraocular pressure in glaucoma (↓ aqueous humor * ↓ lipolysis → ↓ FFA → ↑ triglycerides * ↓ HDL
136
Propranolol Metabolic Effects
↓ glycogenolysis → prolong hypoglycemic event ↓ insulin release → hyperglycemia
137
Propranolol Kinetcs
orally effective (poor availability) Hepatic metabolism
138
Propranolol Kinetcs
orally effective (poor availability) Hepatic metabolism
139
Propranolol Therapeutic uses (9)
hypertension chronic stable angina arrhythmias Post MI hyperthyroidism pheochromocytoma migraine prophylaxis stage fright essential tremors
140
Propranolol Adverse Effects and Contraindications
slide 54
141
Timolol, Nadolol
Similar to propranolol (competitive inhibition of β 1 = β 2)
142
Timolol, Nadolol Therapeutic uses
similar to propranolol (hypertension, post MI) timolol glaucoma (also levobunolol
143
Cardioselective ꞵ1 Receptor Antagonists
Metoprolol, Atenolol
144
Metoprolol, Atenolol function
inhibit ꞵ1 > ꞵ
145
Metoprolol, Atenolol are Preferred over non specific ꞵblockers in pts with:
diabetes (especially in patients that are prone to hypoglycemic reactions) Raynaud’s syndrome COPD (still contraindicated in asthmatics)
146
Metoprolol, Atenolol Kinetics
metoprolol hepatic metabolism atenolol renal elimination
147
Metoprolol, Atenolol Therapeutic uses:
similar to propranolol CHF metoprolol
148
Esmolol
Cardioselective ꞵ1 Receptor Antagonists
149
Esmolol function
very short acting Cardioselective ꞵ blocker
150
Esmolol kinetics
metabolized by red blood cell esterase
151
Esmolol Therapeutic uses
used as antiarrhythmic (IV only)
152
Mixed Action | ꞵ Blockers
Carvedilol, Labetalol
153
Carvedilol, Labetalol function
non specific ꞵ block + α 1 blocker effects antioxidant activity
154
Carvedilol, Labetalol effects
non specific ꞵ block + α 1 blocker effects ↓ TPR ±HR, CO ↑ HDL
155
Carvedilol, Labetalol Therapeutic uses
hypertension CHF
156
Carvedilol, Labetalol Adverse effects/contraindications/precautions
same as other β blockers + hypotension due to α1 block
157
Nebivolol function
Cardioselective β 1 block + NO mediated vasodilation
158
Nebivolol effects
↓ TPR ±HR, CO
159
Nebivolol Therapeutic uses
hypertension, CHF
160
Nebivolol Adverse effects/contraindications/precautions
same as other ꞵ blockers + more prominent hypotension due to NO mediated vasodilation

BMS 615 Cardiovascular (49 decks)

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