1
Q
Why use adrenergic agonist?
A
- Maintain organ perfusion
- Tx of allergic rxn
- Prolongs the effects of local anesthetics
- CP resuciation
2
Q
What are the SNS effects of adrenergic agonist at the pre junctional membrane?
A
- Interferes w/NT synthesis, storage, release, metabolism or uptake
- Stimulates NT release
3
Q
What are the SNS effects of adrenergic agonist at the post junctional membrane?
A
- Stimulates receptors
- Blocks/inhibits the NT agonist
4
Q
What is the function of direct acting adrenergic agonists?
A
- Activate adrenergic receptor directly
5
Q
Is the potency of direct acting synthetic non catecholamines less or more of less than catecholamines?
A
Less
6
Q
What is the function of indirect acting adrenergic agonists?
A
- Denervation/depletion effects
7
Q
What are the sympathetic agonists?
A
- Norepi
- Epi
- Isoproterenol
8
Q
What is the order of potency of the sympathetic agonists?
A
NE > EPI> ISO
9
Q
What are examples of selective adrenergic receptor agonists?
A
- Phenylephrine
- Clonidine
- Dobutamine
- Terbutaline
10
Q
What receptor does phenylephrine work on?
A
A1 agonist
11
Q
What is the catecholamine structure?
A
- Benzene ring with an -OH group on the 3,4 position
12
Q
What do naturally occuring catcholamines directly stimulate?
A
Adrenergic receptors
13
Q
What are the 3 naturally occurring catecholamines?
A
- Norepinephrine
- Epi
- Dopamine
14
Q
Where is NE produced?
A
- In the postganglionic neuron and adrenal medulla
15
Q
Where is Epi produced?
A
- In the adrenal medulla
16
Q
Dopamine is a _____ acting neurotransmitter?
A
- Centrally
17
Q
What % of the adrenal medulla ouput is NE? What % is Epi?
A
- NE = 20%
- Epi = 80%
18
Q
_____ is a precursor for the production of Epi and NE?
A
Dopamine
19
Q
How do synthetic catecholamines function?
A
- They mimic the effect of naturally occurring catecholamines at receptors
20
Q
Which synthetic catecholamines mimic the effect of naturally occurring catecholamines at receptors?
A
Direct acting
21
Q
What are the 2 types of synthetic non catecholamines?
A
- Direct acting
- Indirect acting
22
Q
What is an example of an indirect acting synthetic non catecholamine?
A
- Ephedrine
23
Q
What are examples of direct acting synthetic non catecholamines?
A
- Phenylephrine
- Methoxamine
24
Q
What is the prototype adrenergic agonist?
A
- Adrenaline/Epinephrine
25
Can adrenaline be given exogenously?
Yes
26
Is adrenaline/epinephrine released in response to SNS activation?
Yes
27
Where is epinephrine made?
Adrenal medulla
28
What receptors are associated with the direct acting cardiovascular effects of epinephrine?
Beta 1, Beta 2, & Alpha 1 receptors
29
What are 2 synthetic catecholemines?
- Ispoproteronolol
- Dobutamine
30
What receptors are stimulated with epi dose of 1-2 mcg/min? What is the response?
- B2 receptors in the periphery
- causes vasodilation
31
What receptors are stimulated with epi dose of 2-5 mcg/min? What is the response?
- B1 receptors in the heart
- increase contractility
32
What receptors are stimulated with epi dose of 5-10 mcg/min? What is the response?
- A1 receptors in the periphery
- causes vasoconstriction
33
1:1000 of epi is _____ mg/ml
1mg/ml
34
1:10,000 of epi is _____ mg/ml
100 mcg/ml
35
1:100,000 of epi is _____ mcg/ml
10 mcg/ml
36
What are the respiratory effects of epinephrine?
Activation of B2 receptors in the lung smooth muscle > bronchodilation
37
What are the metabolic effects of epinephrine?
Increase serum glucose
38
What are the occular effects of epinephrine?
Mydriasis
39
What are the CNS effects of epinephrine?
Restlessness
40
What effect does epinephrine have on platelets?
Causes increased aggregation
41
Does norepinephrine have a strong direct acting effect on stimulating B1 receptors?
- It has weak stimulation activity on B1
42
Does norepinephrine have a strong direct acting effect on stimulating B2 receptors?
- No, it has little B2 agonist effects
43
Does norepinephrine have a strong direct acting effect on stimulating alpha receptors?
- Yes, it is a POTENT alpha agonist
44
What are the CV effects of NE?
- intense vasoconstriction
- reduced CO
- reduced renal blood flow
- increased DBP
45
What receptors are associated with the direct acting effects of dopamine?
- Dopa 1
- B1 & 2
- A1
46
At _____er doses, you see a dopaminergic response to dopamine?
lower
47
At _____ doses, you see a beta adrenergic response to dopamine?
medium
48
At _____er doses, you see a alpha adrenergic response to dopamine?
higher
49
At what dose of dopamine do you see D1 receptor response? What is the response?
- seen at lower doses
- vasodilation
50
At what dose of dopamine do you see B1 & B2 receptor response?
medium
51
At what dose of dopamine do you see A1 receptor response? What is the response?
- seen at higher doses
- increased SVR, decreased renal blood flow, increased risk of arrhythmias, & increased BP
52
_____ is seen in high doses of dopamine as a response to increased BP?
Reflex bradycardia
53
Is isoproterenol a synthetic or naturally occurring catecholamine?
A synthetic catecholamine
54
What receptors are associated with the direct acting effects of isoproterenol?
B1 & B2
55
What are the B1 CV effects of isoproterenol?
increased HR
56
Does increasing the HR cause an increase or decrease in the myocardial O2 consumption?
Increase
57
Is isoproterenol a strong or poor inotrope?
poor
58
What are the B2 CV effects of isoproterenol?
- Skeletal muscle, renal & mesenteric vascular bed dilation
- decreases DBP
59
What are the CNS effects of isoproterenol?
Stimulation
60
What are clinical uses of Isoproterenol?
- Bronchodilator
- Decrease PVR
- Increase HR
- Inotropy/chronotropy
61
What are common side effects of Isoproterenol?
- Tachycardia
- ventricular arrythmias
- hypotension
62
Does Isoproterenol potentiate inhalation arrythmias?
Yes, it does
63
Is dobutamine a synthetic or naturally occurring catecholamine?
synthetic
64
Is dobutamine direct, indirect, or both?
Both, it is mostly direct with some indirect properties
65
What receptors are associated with the effects of dobutamine?
B1 & B2, Alpha
66
Is dobutamine a selective B1? Is it a weak B2?
Yes, it is a selective B1 and weak B2
67
Dobutamine has a dose dependent _____in CO & _____ in atrial filling pressures
Dobutamine has a dose dependent in INCREASE in CO & DECREASE in atrial filling pressures
68
Does dobutamine cause a major increase in HR & SVR? Does it increase myocardial O2 requirements?
No.
69
Does dobutamine increase or decrease SVR at low doses?
Decreases
70
Does dobutamine increase or decrease renal blood flow and CO?
Increases
71
What are common clinical uses of dobutamine?
- cardiac failure
- low cardiac output states
- used in conjunction with vasodilators
72
What are common side effects of dobutamine?
- sensitization to inhalation arrhythmias
73
Is ephedrine a synthetic non catecholemine or synthetic catecholemine?
synthetic non catecholemine
74
What is the most commonly used sympathomimetic?
Ephedrine
75
Is ephedrine a direct or indirect agonist? What percent is it?
mainly indirect, 70-80%
76
What receptors are associated with the indirect effects of ephedrine?
Non selective Beta and A1 receptors
77
What are common clinical uses of ephedrine?
- Hypotension 2/2 anesthesia
- sympathetic blockade (regional anesthesia)
- inhalation or injected anesthetic agent
78
What are the CV effects of ephedrine?
increases inotropy and dromotropy (increased conduction through AV node)
79
Which receptors causes increase in inotropy and dromotropy in ephedirne?
mainly B1 stimulation and B2 is offset by A1 in vessels
80
Does ephedrine increase or decrease fetal metabolic rate? Does it lead to acidosis or alkalosis?
Increase fetal metabolic rate and can lead to acidosis
81
What are the resp effects of ephedrine?
- stimulates respiration and bronchodilation (B2)
82
What are the metabolic effects of ephedrine?
unlike epi, does NOT produce marked hyperglycemia
83
What are the occular effects of ephedrine?
Mydriasis
84
What are the CNS effects of ephedrine?
stimulation
85
Can ephedrine cross the BBB?
Yes
86
In terms of metabolism, does ephedrine has a slow or fast inactivation & excretion? Does this shorten or prolong the effects of the drug?
Slow inactivation & excretion which prolongs the effects of the drug
87
Can tachyphylaxis occur with ephedrine?
Yes
88
Is phenyleprhine a synthetic non catecholemine or synthetic catecholemine?
A synthetic non catecholemine
89
Is phenyleprhine a direct or indirect acting agonist?
Direct acting
90
What receptors are associated with the direct effects of phenylephrine?
A1 and B receptors
91
Is the B receptor effect of phenylephrine minimal or large?
minimal
92
What is the CV effect of phenylephrine?
Increases SVR
93
What are the clinical uses of phenylephrine?
Hypotension/reduced SVR
94
What are some scenarios related to our practice where phenylephrine would be used for the hypotension/decreased SVR?
- SNS blockade post regional anesthesia
- Injected/inhaled anesthetic agents
- CPB
95
Should you rapidly increase and decrease rate of a phenylephrine infusion?
No, that can cause roller coaster effect with BP (up & down)
96
What is a potential side effect related to phenylephrine that you should be aware of?
Reflex bradycardia
97
Is methoxamine a synthetic non catecholemine or synthetic catecholemine?
synthetic non catecholemine
98
Is methoxamine a direct or indirect acting agonist?
direct acting
99
What receptors are associated with the direct effects of methoxamine?
Stimulates A1
100
What medication is the prototype pure alpha vasoconstrictor?
methoxamine
101
What is the main clinical use of methoxamine?
- arterial vasoconstriction during hypotension
102
What is a common side effect of methoxamine?
decreased renal blood flow due to the intense ARTERIAL vasoconstriction
103
Does methoxamine have a long duration of action?
Yes, up to 8hrs
104
Dexmedetomidine is _____times more selective for alpha___ receptors
Dexmedetomidine is 7-10 times more selective for alpha 2 receptors
105
What are the clinical indication for Dexmedetomidine?
- hypnotic effects
- sedation
- analgesia
106
Does dexmedetomidine increase or decrease catecholamines during anesthesia?
decreases
107
Does dexmedetomidine increase or decrease MAC?
Decreases
108
What is the most commonly used selective beta 2 agonist?
Proventil (Albuterol)
109
What are selective beta 2 agonists used to treat?
- bronchoconstriction
110
How do selective beta 2 agonist affect labor?
- stops premature labor by working as a tocolytic
111
What is tocolytic referring to when talking about selective beta 2 agonist affect?
Uterine smooth muscle relaxation
112
What are 3 examples of alpha antagonist medications?
- Phentolamine
- Phenoxybenzamine
- Prazosin
113
What condition does phentolamine treat?
Pheochromocytoma
114
What is the onset of phentolamine? Quick, slow?
Quick
115
What is the duration of phentolamine?
15-30 mins
116
Phentolamine causes _____ tachycardia?
Phentolamine causes REFLEXIVE tachycardia
117
When do you see the peak effect of Phenoxybenzamine?
1hr
118
What is the 1/2 life of Phenoxybenzamine?
24hrs
119
Is prazosin a shorter or longer acting alpha antagonist?
shorter
120
What are 4 examples of B2 blockers?
- Propranolol
- Labetolol
- Esmolol
- Metoprolol
121
How do B2 blockers work in the body?
- Oppose the effect of endogenous catecholamines at Beta receptors
122
What are the 2 classification of B2 blockers?
- Specific
- Non specific
123
Is labetolol specific or not specific to B1?
Not specific
124
What is the alpha/beta blocker ratio of labetolol?
1:7
125
What is the onset of labetolol?
2-5 mins
126
Labetolol can be redosed q ____ mins
Labetolol can be redosed q 5-10 mins
127
What is the 1/2 life of labetolol? Is it long?
>5 hrs, yes its long
128
Is esmolol specific or not specific to B1?
specific
129
What is the onset of esmolol?
1-4 mins
130
What is the duration of esmolol?
10-30 mins
131
What is the 1/2 life of esmolol?
- 9 min in adults
132
Is metoprolol specific or not specific to B1?
specific
133
What is the onset of metoprolol?
- approx 5 mins
134
What is the 1/2 life of metoprolol?
3-4 hrs
135
What are 2 examples of Phosphodiesterase Inhibitor medicaitons?
- Amrinone
- Milrinone
136
Amrinone and Milrinoine inhibit _____?
Amrinone and Milrinoine inhibit PDE 3
137
What is the clinical indication of Amrinone?
- CHF
- Ventricular dysfunction
138
Milrinone ____ myocardial contractility and causes peripheral _____ leading to an ____ CO
Milrinone INCREASES myocardial contractility and causes peripheral VASODILATION leading to an INCREASED CO
139
Should a patient stop their MAOI 2-3 wks prior to surgery?
No, they can continue until sx
140
Should you use direct or indirect acting agents in the presence of MAOIs?
Direct acting agents
141
How do TCAs/SSRIs work in the body?
- Inhibit the Uptake of NE/5HT Back Into Postganglionic Neurons.
142
Should you avoid direct or indirect acting agents in the presence of TCAs/SSRIs?
Avoid indirect acting agents
143
Anything which is a _____ to the SNS (Stress, Drugs) will potentially produce a _____ response and ______
Anything which is a STIMULANT to the SNS (Stress, Drugs) will potentially produce a HYPERTENSIVE response and ARRYTHMIAS
144
How do anticholinesterases work in the body?
- drugs which cause reversible inhibition of AChE
145
What type of bonds are associated with anticholinesterases?
Edrophonium ionic bonds
146
Which drugs will cause the formation of carbamyl esters?
- Neostigmine
- Pyridostigmine
- Physostigmine
147
What is the clincal use for anticholinesterases?
- Tx of glaucoma, decreases IOP
148
What can form after >6m of use of anticholinesterases?
Cataracts
149
What class of drugs are considered synthetic quaternary ammonium compounds?
Anti-muscarinics
150
What is an example of a synthetic quaternary ammonium compound?
glycopyrrolate
151
What are 2 examples of naturally occurring anitmuscarinic tertiary amines?
- Atropine
- Scopalamine
152
What are the clinical indication for anitmuscarinic
- preop medication
- NM blockade reversal
- prevention of reflex mediated bradycardia
153
How do antimuscarinics work in the body?
reversible bind to muscarinic receptor > inablity of ACH from to access the receptor
154
What chemical group is necessary for anitmuscarinic activity?
An ester group
155
Antimuscarinics increase or decrease _____ & ______ secretions
Antimuscarinics DECREASE BRONCHIAL & SALVIVARY secretions
156
Do Antimuscarinics have occular and cardiac effects?
Yes
157
Do Antimuscarinics have decrease or increase GI motility and urinary effects?
Decrease
158
What effect do Do Antimuscarinics have on gastric secretion of H+?
An inhibitory effect
159
What effect do Antimuscarinics have on secretions?
decrease secretions by the exocrine glands
160
What is the effect called that is related to decreased secretions by exocrine glands?
antisialagogue effect
161
In terms of secretions management, order these antimuscarinics from most effective to least: Glycopyrrolate, Scopolamine, Atropine?
Scopolamine> Glycopyrrolate> Atropine
162
Antimuscarinics block the ___2 receptor resulting in the ______ of _____ reuptake
Antimuscarinics block the M2 receptor resulting in the INHIBITION of NE reuptake
163
How do Antimuscarinics affect the P-R interval? What is the effect on A-V conduction?
- Antimuscarinics DECREASE the P-R interval
- Antimuscarinics INCREASE the A-V conduction
164
In terms of blocking the M2 receptor to inhibit NE reuptake, order these antimuscarinics from most effective to least: Glycopyrrolate, Scopolamine, Atropine
Atropine> Glycopyrrolate> Scopolamine
165
In reference to antimuscarinics, can the tertiary amines (scopalamine & atropine) cross the blood brain barrier?
Yes
166
Do antimuscarinics cause central anticholinergic delirium?
Yes
167
Which antimuscarinics cause sedation, amnesia, confusion, & hallucinations?
Naturally occurring tertiary amines - Scopalamine & atropine
168
Between scopalmaine and atropine, order them from greatest to least in regards to sedation, amnesia, confusion, & hallucinations?
Scopalamine > atropine
169
At high does what effects does atropine have?
ocular effects
170
Why is Glycopyrrolate a good choice for antimuscarinic?
Glycopyrrolate does NOT cause sedation, amnesia, confusion, & hallucinations
171
What are the ocular effects of antimuscarinics?
Mydriasis
172
What is Mydriasis?
Pupil dilation w/no accommodation
173
In terms of degree of mydriasis, order these antimuscarinics from most to least: Glycopyrrolate, Scopolamine, Atropine
Scopolamine> Atropine> Glycopyrrolate
174
What are the respiratory effects of antimuscarinics?
Relax the smooth muscle of the bronchioles
175
In terms of bronchiole relaxation, order these antimuscarinics from most to least: Glycopyrrolate, Scopolamine, Atropine
Atropine > Scopalamine = Glycopyrrolate
176
Do antimuscarinics increase or decrease GI motility, LES pressure, and gastric acid H+ secretions?
Decrease
177
Do antimuscarinics increase or decrease the tone of the bladder sphincter? Does this cause an inability or ability to void?
Antimuscarinics INCREASE bladder tone causing an INABILITY to void
178
What is an antimuscarinic overdose called?
Central anticholinergic syndrome
179
How do you treat Central anticholinergic syndrome?
Give physostigmine 15-60 mcg/kg
180
Which population is more likely to suffer from Central anticholinergic syndrome?
Elderly and peds
181
What are the symptoms of Central anticholinergic syndrome?
A range of restlessness and confusion > sedation and unconsciousness
182
How many mg of elemental calcium are in calcium chloride? What % solution is it?
- 27 mg
- 10%
183
How many mg of elemental calcium are in calcium gluconate? What % solution is it?
- 9 mg
- 10%
184
What is the clinical use of calcium?
In situations where the ionized ca 2+ is <0.8 mmol/L
185
How does calcium affect BP? Does it increase or decrease inotropy?
- Increases BP
- Increases inotropy
186
Can administration of calcium aggravate/increase cell injury? Why?
Yes, it can cause tissue injury
187
Can calcium cause tissue injury? If yes, how do you avoid this?
Yes, you can avoid tissue injury by giving it centrally.
188
What are examples of non selective direct acting adrenergic agonists?
- Isoproterenol
- epinephrine
- norepinephrine
- oxymetazoline
189
What is an example of a mixed acting adrenergic agonist?
Ephedrine
190
What are examples of indirect acting adrenergic agonists?
- Releasing agents (amphetamine, tyramine)
- Uptake inhibitors (cocaine)
- MOAIs (selegiline)
- COMT inhibitors (COMT)
