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Pharm 2 > Sympatholytics, Antiarrythmics, Inotropes > Flashcards

Sympatholytics, Antiarrythmics, Inotropes Flashcards

1
Q

What are sympatholytics?

A

Typically adrenergic antagonists

Their goal is to reduce SNS stimulation, most work postsynaptically.

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2
Q

Define inotropy.

A

Contractility

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3
Q

What type of receptors are Gs receptors?

A

Stimulatory (beta-1 and beta-2 receptors)

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4
Q

What enzyme is activated by Gs receptors?

A

Adenylyl cyclase

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5
Q

What is the second messenger for Gs receptors?

A

Cyclic adenosine monophosphate (cAMP)

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6
Q

What type of receptors are Gi receptors?

A

Inhibitory (alpha-2 receptors)

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7
Q

What do Gq receptors catabolize?

A

Phospholipids

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8
Q

Which enzyme is activated by Gq receptors?

A

Phospholipase C (PLC)

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9
Q

What are the second messengers for Gq receptors?

A
  • Diacylglycerol (DAG)
  • Inositol triphosphate (IP3)
  • Protein kinase C (PKC)
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10
Q

List common types of sympatholytics.

A
  • Alpha blockers
  • Beta blockers
  • Calcium channel blockers
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11
Q

List common types of antiarrhythmics.

A
  • Beta blockers
  • Calcium channel blockers
  • Potassium channel blockers
  • Sodium channel blockers
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12
Q

What is the action of alpha blockers?

A

Interfere with ability of catecholamines (epi, NE) to stimulate an alpha response (vasoconstriction)

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13
Q

What is Phenoxybenzamine?

A

Nonselective alpha (A1, A2) blocker, noncompetitive (covalent bond)

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14
Q

What are the indications for Phenoxybenzamine?

A

Pheochromocytoma

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15
Q

How long does it take for Phenoxybenzamine to fully control hypertension?

A

Several weeks (2-10 weeks)

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16
Q

What is the half-life of Phenoxybenzamine?

A

18-24 hours

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17
Q

What is the duration of action for Phenoxybenzamine?

A

3-4 days

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18
Q

What is the oral dose range for Phenoxybenzamine?

A

0.5-1mg/kg

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19
Q

What is Phentolamine?

A

Nonselective (A1, A2) blocker, competitive

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20
Q

What are the indications for Phentolamine?

A
  • Pheochromocytoma
  • Extravasation of vasoconstrictors
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21
Q

What is the duration of action for Phentolamine?

A

10-15 minutes

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22
Q

What is the IV bolus dose for Phentolamine?

A

30-70 mcg/kg

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23
Q

What are the selective alpha blockers mentioned?

A
  • Prazosin
  • Doxazosin
  • Tamsulosin
  • Terazosin
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24
Q

What is the indication for Tamsulosin?

A

BPH

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25
Q

What is the normal function of alpha-2 stimulation?

A

Decrease in presynaptic NE release, centrally causes sedation

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26
Q

What is the effect of alpha-2 agonists?

A

Decrease the release of NE, reducing sympathetic outflow

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27
Q

What is Yohimbine?

A

Selective A2 antagonist

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28
Q

What are the side effects of Yohimbine?

A
  • Tremor
  • Tachycardia
  • Hypertension
  • Dissociation
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29
Q

What do beta blockers prevent?

A

SNS (catecholamine) action on the heart (B1) and smooth muscles of the blood vessels and airway

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30
Q

What class of antiarrhythmic are beta blockers?

A

Class 2

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31
Q

What is the action of beta blockers on cardiac action potential?

A

Action on phase 4

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32
Q

List indications for beta blockers.

A
  • Hypertension
  • Angina
  • Acute coronary syndrome/ischemia
  • Arrhythmia suppression
  • CHF
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33
Q

What should not be done prior to surgery regarding beta blockers?

A

Do not have patients stop beta blockers prior to surgery – may have rebound effect

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34
Q

What are the side effects of beta blockers?

A
  • Bradycardia
  • Asystole
  • Inhibition of gluconeogenesis (hypoglycemia)
  • Bronchoconstriction (B2 blockers)
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35
Q

What are the selective B1 blockers?

A
  • Bisoprolol
  • Esmolol
  • Atenolol
  • Metoprolol
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36
Q

What does the ratio 30:1 indicate in Metoprolol?

A

B1:B2 receptor affinity

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37
Q

What are the nonselective beta blockers?

A
  • Carvedilol
  • Propranolol
  • Labetalol
  • Nadalol
  • Sotalol
  • Timolol
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38
Q

What is the half-life of Nadalol and Pindolol?

A

20-40 hours

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39
Q

What are the long-term effects of beta blockers?

A
  • Alteration in lipoprotein and triglyceride levels
  • Related alopecia
  • Myopathy
  • Thrombocytopenia
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40
Q

What is the dose for Metoprolol IV?

A

2.5-5mg Q5min IVP

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41
Q

What is the PO dose range for Metoprolol?

A

12.5-100mg BID (50-150 mg daily ER)

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42
Q

What is the onset time for Metoprolol?

A

<1 min

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43
Q

What is the peak time for Metoprolol?

A

20 min

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44
Q

What is the duration of action for Metoprolol?

A

5-8 hours

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45
Q

What is Esmolol’s mechanism of metabolism?

A

Metabolized by plasma ester hydrolysis

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46
Q

What is the IV concentration for Esmolol?

A

10mg/mL

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47
Q

What is the dose range for Esmolol infusion?

A

50-300 mcg/kg/min infusion

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48
Q

What is Atenolol’s dose range?

A

50-200 mg/day PO

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49
Q

What is Labetalol’s A:B ratio?

A

1:3 PO and 1:7 IV

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50
Q

What is the first line treatment for pregnancy-related hypertension?

A

Labetalol

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51
Q

What is Propranolol’s lipophilicity?

A

Very lipophilic, crosses BBB

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52
Q

What is the dose range for Propranolol?

A

40-360 mg/day PO in divided doses

53
Q

What is the primary effect of Carvedilol?

A

Nonselective B1/B2 and selective A1

54
Q

What is the half-life of Carvedilol?

A

7-10 hours

55
Q

What are the signs and symptoms of beta blocker overdose?

A
  • Bradycardia
  • Dysrhythmias
  • Hypotension
  • Decreased cardiac output that can progress to cardiogenic shock
56
Q

What is the gold standard treatment for beta blocker overdose?

57
Q

How does glucagon work in beta blocker overdose?

A

Increases adenylate cyclase activity without first stimulating the beta receptor

58
Q

What is the dose range for glucagon in beta blocker overdose?

A

1 to 10 mg IV depending on severity of symptoms

59
Q

What is required for CV support in beta blocker overdose?

A

Calcium, epinephrine, pacing

60
Q

What is pheochromocytoma?

A

Adrenal medulla tumor that leads to increased Epi/NE levels

61
Q

What is the diagnostic test for pheochromocytoma?

A

Testing for catecholamine byproducts (HVA, VMA) in urine or serum

62
Q

What is the order of blockade for treating pheochromocytoma?

A

Alpha blockade must be instituted BEFORE beta blockade

63
Q

What are the classes of antiarrhythmic medications?

A
  • Na Channel Blockers
  • K Channel Blockers
  • Calcium Channel Blockers
64
Q

How are Na channel blockers classified?

A

As Moderate (A), Weak (B), or Strong (C) action on the sodium channel based on dissociation

65
Q

What do sodium channel blockers do?

A

Delay the point at which Na+ channels recover from an inactivated state, increasing the effective refractory period (ERP)

66
Q

List examples of Class A sodium channel blockers.

A
  • Quinidine
  • Procainamide
67
Q

What is an example of a Class B sodium channel blocker?

68
Q

What is an example of a Class C sodium channel blocker?

A

Flecainide

69
Q

What is the action of potassium channel blockers?

A

Alter phase 3 of the cardiac action potential by increasing action potential duration

70
Q

What is Amiodarone classified as?

A

Group 3 antiarrhythmic

71
Q

What is the IV loading dose of Amiodarone?

A

150 mg over the first 10 minutes (15 mg/min)

72
Q

What is the maintenance infusion for Amiodarone?

A

540 mg over the remaining 18 hours (0.5 mg/min)

73
Q

What is the half-life of Amiodarone?

74
Q

What risk does Amiodarone pose regarding thyroid function?

A

Can cause Amiodarone Induced Thyrotoxicosis (AIT)

75
Q

What are the potential thyroid states caused by Amiodarone?

A
  • Hyperthyroid
  • Hypothyroid
76
Q

What tests are used for diagnosing thyroid issues related to Amiodarone?

77
Q

What is the role of renin in the RAAS system?

A

Stimulates the conversion of angiotensinogen to angiotensin I

78
Q

What does ACE convert angiotensin I to?

A

Angiotensin II

79
Q

What effect does angiotensin II have on the autonomic ganglia?

A

Facilitates NE release and prevents its reuptake at nerve terminals

80
Q

List classes of medications that target renal function in hypertension.

A
  • ACE inhibitors
  • Angiotensin Receptor Blockers (ARBs)
  • Thiazide Diuretics
  • Potassium Sparing Diuretics
  • Aldosterone antagonists
81
Q

What is the suffix for ACE inhibitors?

82
Q

What is the suffix for Angiotensin Receptor Blockers (ARBs)?

83
Q

What do ACE inhibitors do?

A

Decrease conversion of angiotensin I to angiotensin II

84
Q

What is the effect of ACE inhibitors on AT1 receptors?

A

Resulting in reduced vasoconstrictor effects, aldosterone secretion, and sympathetic activation

85
Q

What is HCTZ?

A

Hydrochlorothiazide, a thiazide diuretic

86
Q

Name two Potassium Sparing Diuretics.

A
  • Triametrene
  • Amiloride
87
Q

What are Aldosterone antagonists?

A

Medications that block the effects of aldosterone, such as Spirinolactone

88
Q

What is the primary action of Angiotensin Converting Enzyme (ACE) Inhibitors?

A

Decrease conversion of angiotensin I to angiotensin II

89
Q

How do ACE inhibitors affect aldosterone secretion?

A

They inhibit aldosterone secretion

90
Q

What is a common side effect of increased bradykinin production from ACE inhibitors?

91
Q

What suffix is commonly associated with ACE inhibitors?

92
Q

What do Angiotensin Receptor Blockers (ARBs) do?

A

Block the vasoconstrictive actions of Angiotensin on the AT1 receptor

93
Q

Do ARBs inhibit the breakdown of bradykinin?

94
Q

Which trial recommended holding ACE inhibitors or ARBs before surgery?

A

POISE trial

95
Q

What is the 1st line treatment for ACEi/ARB related vasoplegia?

A

Vasopressin

96
Q

What pathway does Nitric Oxide (NO) stimulate for vasodilation?

A

cGMP Pathway

97
Q

What does Methylene Blue do in relation to Nitric Oxide?

A

Acts as a nitric oxide scavenger and vasoconstrictor

98
Q

What is the primary effect of Sodium Nitroprusside?

A

Arterial and venous dilation

99
Q

What is a significant risk of prolonged Sodium Nitroprusside administration?

A

Cyanide toxicity

100
Q

What is the elimination half-life of Nitroglycerin?

A

1-2 minutes

101
Q

What is the primary action of Adenosine?

A

Stimulates NO production and relaxes smooth muscle

102
Q

What is the mechanism of action of Digoxin?

A

Inhibits Na/K pump activity

103
Q

What are the signs of Digoxin toxicity?

A
  • Nausea
  • Heart block
  • Bradycardia
104
Q

What is the therapeutic range of Digoxin?

A

Narrow therapeutic range

105
Q

What type of medication is Milrinone?

A

Phosphodiesterase inhibitor

106
Q

What is the primary indication for Calcium Chloride?

A

Low serum calcium levels

107
Q

What is Levosimendan known as?

A

Calcium Sensitizer

108
Q

What are the common side effects of Fenoldopam?

A
  • Reflex tachycardia
  • Headache
  • Flushing
109
Q

What are the two main effects of Calcium inotrope?

A
  • Increases blood pressure
  • Inotropic activity
110
Q

What is the primary action of Phosphodiesterase Inhibitors?

A

Competitive inhibition of phosphodiesterase enzymes

111
Q

What is the main use of PDE5 inhibitors?

A

Erectile dysfunction and pulmonary hypertension

112
Q

Name a common side effect of Sodium Nitroprusside.

A

Metabolic acidosis

113
Q

What is the mechanism of action of Hydralazine?

A

Direct systemic arterial vasodilator

114
Q

What is a common effect of Nitroglycerin?

A

Reduces preload and myocardial demand

115
Q

Fill in the blank: The main smooth muscle vasodilator in normal endothelium is _______.

A

Nitric Oxide

116
Q

True or False: ARBs are used in perioperative medicine.

117
Q

What is the primary action of a D1 receptor agonist like Fenoldopam?

A

Arterial dilation through increasing levels of cAMP

118
Q

What is the duration of action for Levosimendan?

A

Depends on timing of administration

119
Q

What is the recommended treatment for cyanide toxicity from Sodium Nitroprusside?

A
  • 100% FiO2
  • NaHCO3 for acidosis
  • Sodium thiosulfate
  • Methylene blue
  • Hydroxocobalamin
120
Q

Metoprolol

A

2.5-5mg IVP q5min

121
Q

Esmolol (bolus and infusion)

A

0.5-1mg/kg

50-300mcg/kg/min

122
Q

Labetelol

A

0.1-0.5 mg/kg q5-10 min. (often 5-20mg)

123
Q

Propranolol

A

40-360mg/day PO

124
Q

Amiodarone (loading and maintenance)

A

150 mg over 10 min

360 mg over next 6 hrs

125
Q

Diltiazem (IVB and PO)

A

0.25-0.35mg/kg IV, 60-90mg PO q8h

126
Q

Nicardipine

A

5-15mg/h infusion

127
Q

Clevidipine

A

start @ 1-2mg/h (double dose q90sec until target BP) (max 32mg/h)

128
Q

Milrinone

A

0.375-0.75mcg/kg/min

Pharm 2 (2 decks)

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