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Nurs 575 Anesthesia Pharmacology > Sympathomimetic drugs (week 10) > Flashcards

Sympathomimetic drugs (week 10) Flashcards

Week 10 (103 cards)

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1
Q

Where is Epinephrine synthesized, stored, & released?

A

Adrenal Medulla

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2
Q

Natural functions of Epinephrine?

A
  • Regulates contracility
  • HR
  • Vascular/Bronchial smooth muscle tone
  • Glandular Secretions
  • Metabolic processes: glycogenolysis & Lipolysis
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3
Q

What receptors does Epinephrine work on?

A
  • a-adrenergic receptors
  • B1and B2 adrenergic receptors
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4
Q

What issues does epinephrine have with oral adminstration

A

Not effective

  • rapidly metabolized in GI/Liver
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5
Q

Epinephrine is (Water or Lipid) soluble and what does this property account for?

A

Water-soluble

  • It’s poor lipid solubility = lack of CNS effects

Prevents entrance to CNS

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6
Q

Clinical uses of Epinephrine?

A
  • Anaphylaxis
  • Severe Asthma/Bronchospasm
  • Cardiopulmonary resuscitation
  • Inc. myocardial contractility & vascular resistance
  • Prolong LA duration of action
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7
Q

Which catecholamine has the most significant effects on metabolism? What effects are these?

A

Epinephrine

  • Glycogenolysis & inhibition of insulin secretion
  • Hyperglycemia
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8
Q

How is coagulation affected by Epinephrine?

A

It is accelerated (hypercoaguable)

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9
Q

A patient is hypercoaguable during the intra & post-operative state, what could this reflect?

A

Epinephrine release due to the stress of surgery

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10
Q

Epinephrine dosing in Adults
(Cardiac Arrest/Infusion/Bolus)

A
  • Cardiac Arrest: 1mg q3-5 min
  • Infusion: 1-16 mcg/min or 0.1-1mcg/kg/min
  • Bolus: 5-10mcg
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11
Q

Epinephrine dosing in Pediatrics
(Cardiac Arrest/Infusion/Bolus)

A
  • Cardiac Arrest: 0.01mg/kg q3-5 min
  • Infusion: 0.1-1mcg/kg/min
  • Bolus: 1-2mcg
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12
Q

Where is Norepinephrine systhesized & stored?

A

Post-ganglionic sympathetic nerve endings

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13
Q

When is norepinephrine released?

A

SNS stimulation

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14
Q

What receptors does Norepinephrine activate?

A
  • B1-adrenergic agonist
  • a1-adrenergic agonist
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15
Q

Norepinephrine is the first line agent to treat what?

A

Refractory HoTN in severe sepsis

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16
Q

Primary utility of Norepi?

A

Potent vasoconstrictor to increase SVR/MAP

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17
Q

Benefits of Norepi in severely HoTN septic pts?

A

Increases:

  • Sphlancnic blood flow
  • UOP
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18
Q

Primary S/E of Norepi?

A

Excessive vasoconstriction may lead to:
* End-organ hypoperfusion & ischemia
* Decreased Renal, sphlancnic, peripheal vascular bed blood flow

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19
Q

Norepi Adult dosing?
(Bolus/Infusion)

A

Bolus: 8-16 mcg
Infusion: 0.02-1mcg/kg/min

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20
Q

Norepi Pediatric dosing?
(Infusion)

A

Infusion: 0.05-2mcg/kg/min

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21
Q

What is Dopamine?

A

Endogenous catecholamine

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22
Q

Function of Dopamine (generally)

A
  • Regulates cardiac, vascular, & endocrine function
  • Important neurotransmitter in the CNS/PNS
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23
Q

Hemodynamic effects of Dopamine?

A

Increases CO by increasing SV
* via B1 adrenergic agonism

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24
Q

Why must Dopamine be a continuous infusion?

A

Rapid half-life of 1-2 min

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25
Hemodynamic effects of Dopamine
* Increase HR * Increase CO * Increase SBP * Increase UOP after CPBP or w/ CHF
26
Unique properties of Dopamine
Simultaneously Increase: * CO * Renal blood flow * UOP * GFR * Na+ excretion
27
Between Dobutamine, epinephrine, & Dopamine which drug is associated with sinus tachycardia/ventricular arrhythmias the most?
Dopamine | Dose related
28
Dopamine dosing for Adults/Pediatrics? (Infusion)
Adults/Pediatric infusion: 2-20mcg/kg/min
29
What is the most potent sympathomimetic? How much more than Epi/Norepi?
**Isoproterenol** * 2-3x Epi * 100x Norepi
30
What receptors does Isoproternol interact with? Effects?
* B1-agonist in the heart -> Increase CO * B2-agonist in Skeletal muscle -> Decrease MAP
31
Why doesn't HR decrease w/ Isoproterenol?
Baroreceptor mediated reflex doesn't occur because MAP doesn't increase
32
Clinical use of Isoproterenol
**Increases HR** before PPM or TPM insertion
33
Dosing/use of Isoproterenol (Infusion)
Infusion: 1-5mcg/min to increase HR 2/2 heart block
34
What is Dobutamine
Synthetic catecholamine derived from Isoproterenol
35
What receptors does Dobutamine interact with? Effects?
* Potent B1: **Increased Myocardial contractility & SA/AV node automaticity** * B1 and a1: myocardial contractility @ higher doses * Weak B2: peripheral vasodilation
36
Clinical uses of Dobutamine
* Inc. CO in CHF or weaning from bypass * Combined with vasodilators to improve CO w/ increased SVR
37
Adverse effects of Dobutamine?
**Occurence of Tachyarrhythmias** * especially in HF or pts with pre-existing arrhythmias
38
Dosing/Half-life of Dobutamine
Infusion: 2-10 mcg/kg/min Half-life: 2 min | That's why infusion only, like dopamine/isoprotereno
39
What drugs are catecholamines?
* Epi * Norepi * Dopamine
40
What drugs are synthetic catecholamines?
* Isoproterenol * Dobutamine
41
What drugs are synthetic non-catecholamines?
* Ephedrine * Phenylephrine
42
Description of Ephderine
Direct & indirect sympathomimetic
43
Direct & Indirect effects of Ephedrine?
* Direct: stimulates a and B-adrenergic receptors * Indirect: Release of endogenous Norepi
44
Unique benefit to Ephedrine and why does it occur?
**Prolonged Duration** (10-60 min vs. 5-10 min of Epi) * Slow inactivation/excretion
45
Clinical use of Ephedrine
* Increase SBP in SNS blockade 2/2 regional anesthesia or IV/inhaled anesthetics * Maternal HoTn **AND** bradycardia post-spinal/epidural
46
Adult Ephedrine dosing
5-10mg IV
47
CV effects of Ephedrine? Primary mechanism?
Increase in: * SBP/DBP * HR * CO Myocardial contractility via B1 receptors
48
You give a second bump of that Ephedrine, but it had less of an effect, why?
**Tachyphylaxis** * B1-receptor inhibition * Occurs with many sympathomimetics
49
Mechanism of Phenylephrine?
* Primarily direct a1-adrenergic stimulation * small indirect release of Norepi
50
True/False: Phenylephrine causes increases in SBP by arterial constriction
False: venoconstriction
51
Dosing of Phenylephrine (Bolus/Infusion)
Bolus: 50-200 mcg IV Infusion: 20-50mcg/min
52
Clinical uses of Phenylephrine
* Treat SNS blockade by regional anesthetics * Treat vasodilation 2/2 IV/Inhaled anesthetics * Primary tx for Maternal HoTN 2/2 neuraxial block
53
What effects do B2-selective adrenergic agonists have on tissues?
* Relax bronchiole & uterine smooth muscle * Generally lack B1effects on heart
54
Concentration per puff of Albuterol, Metaproterenol & Terbutaline?
* Albuterol - 90 mcg/puff * Metaproterenol - 200 mcg/puff * Terbutaline - 200 mcg/puff
55
B2 Selectivity of Albuterol, Metaproterenol & Terbutaline?
* Albuterol - High * Metaproterenol - Moderate * Terbutaline - High
56
Clinical uses of B2-adrenergic agonists?
* Preferred Tx of acute asthma & exercise induced asthma * **Given to stop premature uterine contractions (tocolytic)**
57
With optimal technique, where are B2 agonists delivered, and how much?
* 12% makes it to the lungs * Other 88% goes to Mouth, pharynx, larynx
58
Describe the optimal technique steps for Metered dose inhaler
* Discharge inhaler while taking a slow deep breath over 5-6 seconds * Hold breath @ full inspiration (IRV am'i'rite) for 10 seconds
59
When delivering a metered dose inhaler via ETT, what should you know?
**Decreases 50-70% amount of drug reaching the trachea**
60
Side effects of systemic absorption of B2-agonists?
* Tremor * Inc. HR (less so with selective) * **Hyperglycemia** * **Hypokalemia & hypomagnesemia** * Transient desaturation (relaxation of Hypoxic pulmonary vasoconstriction)
61
Albuterol dosing & Timing
* Two puffs 1 to 5 min apart * Q4-6hrs * No more than 16-20 puffs/day
62
What effect would volatile anesthetics and albuterol have on bronchomotor tone?
**Effects are additive**
63
Dosing & effects for Terbutaline
0.25mg SubQ Effects similar to Epi but longer
64
MoA of PDEi
Exert competitive inhibitory effect on phosphodiasterase enzymes
65
Unique benefit of PDE3is?
Benefits pts who would benefit from inotropy & vasodilation
66
What is Milrinone a derivative of and how does it compare?
**Amrinone** 30x the inotropic effect & less side-effect
67
Milrinone dosing (Bolus/Infusion)
* Bolus: 50mcg/kg over 10 min * Infusion: 0.375-0.75 mcg/kg/min
68
Clinical uses of Milrinone
* LV dysfunction * Wean from CPBP * CHF pts w/ B1 downregulation * P. HTN * Vasodilation & dec. SVR > dobutamine | CPBP = cardiopulmonary bypass
69
Does Milrinone cause more or less tachycardia than dobutamine?
Less
70
S/E of Milrinone
**Rapid administration ->** * HoTN * AV nodal enhancement -> arrhythmias
71
Calcium (gluconate or chloride) may be used to treat what situations?
**Myocardial depression** caused by * Volatile anesthetics * Transfusion of citrated blood * Termination of CPBP
72
Normal plasma iCal and what % is it of total plasma calcium?
* 1-1.26mmol/L (2-2.5 mEq/L or 4-5mg/dL) * 45% of total plasma
73
Side-effects from an a-Adrenergic  receptor blockade?
* Orthostatic HoTN * Reflex Tachycardia (baroreceptor) * Impotence (unfortunate)
74
Which drugs are competitive a-antagonists?
* Phentolamine * Prazosin * Yohimbine
75
MoA & Clinical uses of Phentolamine
Non-selective a-receptor blockade * Acute HTN * Manipulation/removal pheochromocytoma * Sympathomimetic extravasation (infiltrate phentolamine @ the site)
76
Most beneficial clinical response to a-antagonist
Diseases w/ large cutaneous vasoconstriction * Raynauds disease
77
What is Prazosin?
Selective post-synaptic a1-antagonist
78
Benefits of Prazosin's selectivity?
**Less likely to evoke reflex tachycardia (Baroreceptor)** * via leaving the inhibitory a2 activity on NE release
79
What effect does acutely holding B-adrenergic antagonists pre-operatively do?
* **Upregulation of B receptors w/ chronic B blockade** * **Causes SNS Hyperactivity to surgical stimulus** | So don't hold them
80
What is the principle difference in pharmacokinetics between B-blockers?
Elimination half-life * 10 min for esmolol * Up to hours for others
81
Description & effects of Metoprolol?
**Selective B1-adrenergic antagonist** prevents * Inotropy * Chronotropy * Leaves B2 receptors intact
82
What happens if you give a FAT dose of metoprolol?
Becomes non-selective
83
Description & forms of Esmolol
**Rapid onset & short acting B1-adrenergic antagonist** IV only
84
Dosing of Esmolol
0.5-1.5mg/kg IV over 60 seconds w/ 50-300 mcg/kg/min infusion
85
What is important to know about Esmolol's metabolism?
**Plasma esterase's responsible for hydrolysis are distinct from plasma cholinesterase** * Succinylcholine duration not prolonged
86
Principle contraindication for B-receptor antagonists?
Pre-exisiting AV heart block or cardiac failure not caused by Tachycardia
87
Signs of B-blocker related excess myocardial depression?
* Bradycardia * Low CO * HoTN * Cardiogenic shock
88
Treatment for B-blocker related myocardial depression?
* Atripine first * Isoproterenol continuous infusion if atropine unsuccessful * Glucagon 1-10mg IV bolus, 5mg/hr infusion * Transvenous pacemaker
89
Concern with B-antagonists and airways?
Non-selective B-blockers increase airway resistance 2/2 bronchoconstriction due to B2-blockade
90
How do non-selective B-blockers interfere with hypoglycemia recognition?
* Interfere w/ glycogenolysis caused by Epi in response to hypoglycemia * Blunt hypoglycemia related tachycardia * non-selective not recommended for DM @ risk of hypoglycemia
91
Coadministration of B-blockers with volatile anesthetics has minimal myocardial depressant effects. What is the exception to this?
**Timolol** Severe bradycardia in presence of inhaled anesthetics
92
Which B-antagonists have the least effect on the CNS?
**Atenolol & Nadolol** Less lipid soluble than other B-antagonists-> less CNS effects
93
What class of drugs are recommended for pts at risk of myocardial ischemia during high-risk surgery? What kind of pts considered high risk?
**B-adrenergic antagonists** * CAD * Positive preop stress test * DM w/ insulin * LV hypertrophy High risk surgeries Vascular thoracic Intraperitoneal Anticipated large blood loss
94
Dosing for Metoprolol IV?
5 mg IV
95
Dosing for Atenolol IV?
5-10mg
96
Dosing for propanolol IV?
1-10mg IV
97
What are Propanolol & Esmolol are effective at controlling
* Ventricular rate in Afib/Flutter * Atrial dysrhytmias post-cardiac surgery
98
What drugs are a- and B- receptor antagonists?
Labetalol & Carvedilol
99
B to alpha potency ratio for Labetalol?
* 3:1 Oral * 7:1 IV
100
CV effects of Labetalol
* Decrease SVR via a1 blockade * No reflex tachycardia due to B blockade * CO unchanged
101
Dosing of Labetalol
0.1-0.5mg/kg IV
102
S/E of Labetalol
* Orthostatic HoTN * Bronchospasm * Fluid retention w/ long term therapy- combine with diuretic
103
Why are B-blockers ideal for laryngoscopy/intubation?
**Prevent Excessive SNS activity** Attenuate HR & BP

Nurs 575 Anesthesia Pharmacology (18 decks)

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