Adjuncts 1: catecholamines, noncatecholamines, beta blockers, CCBs, alpha blockers, vasodilators, antiarrythmics Flashcards

Question

Dobutamine: metabolism

Answer 1

COMT and MAO in blood, liver, kidneys, GI tract | Metabolites excreted in urine

Answer 2

``` Dyspnea Tachycardia, SVT Thrombocytopenia and platelet inhibition Phlebitis Down regulation of beta receptors after 3 days of tx = tolerance ``` Fever, headache, nausea Paresthesia TOXICITY = anorexia, NV, tremor, head, SOB, angina, chest pain, anxiety

Answer 3

Hypersensitivity Hypovolemia CAD without CHF Caution in pregnancy

Answer 4

Start at 0.5-1mcg/kg/min; titrate every few minutes to 2-20mcg/kg/min Max dose 40mcg/kg/min

Answer 5

Endogenous catecholamine | Alpha, beta adrenergic, and dopaminergic receptor agonist

Answer 6

Low doses – agonize dopaminergic 1 receptors in coronary, renal, and mesenteric vascular smooth muscle cells to stimulate G-CP, AC, cAMP Medium doses – agonize beta 1 adrenergic receptors in cardiac myocytes to increase contractility = +inotrope = ↑CO and HR High doses – agonize alpha1 in GU, GI, heart, liver and vascular smooth muscle

Answer 7

Rapid onset

Answer 8

MAO and COMT Beta hydroxylated to norepinephrine, then methylated to epinephrine in liver and plasma Eliminated in urine

Answer 9

``` Limb ischemia if extravasated Tachycardia, angina, palpitations Dyspnea Increased IOP Hyperglycemia ``` Headache, N/V

Answer 10

``` Right heart failure d/t increase pulm art pressure MAOIs Sulfa allergy V-fib Pheochromocytoma Cocaine use (exaggerated response) ```

Answer 11

0.5 to 2mcg/kg/min low dose 2-5mcg/kg/min medium dose >10mcg/kg/min large dose

Answer 12

Exogenous antidiuretic peptide and vasopressor

Answer 13

Stimulates V1 receptors on vascular smooth muscle, glomerular mesangial cells, and vasa recta causing potent vasoconstriction Stimulates V2 receptors on basolateral cell membrane of renal collecting ducts to ↑ water reabsorption and constricts glomerular efferent arteriole to maintain GFR

Answer 14

``` Onset = nasal 1hr DOA = nasal 3-8hrs ```

Answer 15

Metabolized by tissue peptidases Rapid oral inactivation by trypsin E1/2t 10-20min

Answer 16

``` Coronary artery vasospasm, angina, MI Vasoconstriction and HTN Increased peristalsis, N/V, and abd pain Decreased PLTs Tremor, headache, fever, diaphoresis ```

Answer 17

Hypersensitivity | Caution w/ NSAIDs, carbamazepine (inc AVP effect)

Answer 18

Refractory cardiac arrest: 40 units IV push Esophageal varicies: 20 units over 5 mins Hemorrhagic/septic shock: 0.04 units/min DI: 100-200mU/hr IV

Answer 19

Synthetic non-catecholamine Indirect alpha 1 and beta 2 agonist Direct beta 1 agonist

Answer 20

Indirectly: increases NE release from post ganglionic SNS nerve, activating receptors Directly: binds to receptors and activates G protein, activates or intracellular enzyme adenylate cyclase to cAMP and phospholipase C

Answer 21

Rapid onset DOA 1 hr E1/2 t 3hrs

Answer 22

COMT, though inefficiently; 40% unchanged in the urine

Answer 23

``` Tachyphylaxis Arrhythmias HTN MI CNS stim ```

Answer 24

``` Hypersensitivity Severe HTN Arrhythmias CHF Glaucoma MAOIs Cocaine use (be cautious) ```

Answer 25

5-25 mg IV

Answer 26

Synthetic non-catecholamine | Selective alpha 1 adrenergic agonist

Answer 27

Binding to alpha1 receptor causes direct stimulation of g-protein coupled receptor, increases adenylate cyclase, and cAMP, leading to an influx of calcium on systemic VENOUS vascular smooth muscle and vasoconstriction

Answer 28

Reflex bradycardia Hypertension and decreased CO d/t increased afterload Decreased renal, splanchnic, cutaneous blood flow Decreased UO Metabolic acidosis Anxiety, HA, nervousness, weakness, paresthesia Rebound nasal congestion

Answer 29

``` Hypersensitivity Glaucoma Severe HTN and tachycardia Arrythmias Caution in elderly, heart blocks, HTN, bradycardia ```

Answer 30

50-200mcg IV bolus Q5mins 20-180mcg/min to start with maintenance at 10-60mcg/min

Answer 31

Selective beta 1 adrenergic antagonist

Answer 32

Reversibly binds to beta 1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, and cAMP Slows SA rate and conduction through the AV node and decreases contractility, reducing cardiac O2 demand

Answer 33

``` Onset: 30-60 sec DOA = 10-15mins E1/2t = 9 mins High Vd 55% PB ```

Answer 34

Plasma esterases and excretion in the urine

Answer 35

``` Severe bradycardia Hypotension Heart block CHF and pulmonary edema POI d/t propylene glycol ``` Syncope/dizziness Headache

Answer 36

``` Hypersensitivity CHF Concurrent CCB (= complete heart block) Sick sinus syndrome Severe hypotension HR dependent Asthma and COPD (in high doses) Pregnancy ```

Answer 37

5-10mg IV Q3-5mins to total dose of 80mg | 300-500mcg/kg/min

Answer 38

Beta 1, beta 2, alpha1 adrenergic antagonist

Answer 39

Reversibly binds to beta1, beta2, alpha1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, cAMP. Slows SA node rate (beta 1), slows conduction through the AV node (beta 1), decreases contractility (beta 1), and causes peripheral, cerebral, and coronary vasodilation (alpha 1)

Answer 40

``` Onset = 3-5 mins Peak effect 5-10mins (redose 5-10mins) E1/2t = 5-8hrs Vd 7L/kg 50% PB ```

Answer 41

Hepatic microsomal enzymes | Eliminated in urine 50% - fecal 50%

Answer 42

``` Bronchospasm* Fluid retention* Hypoglycemia* Severe bradycardia Hypotension Heart block ``` Syncope/dizziness Headache

Answer 43

``` Hypersensitivity Asthma/COPD Severe CHF Concurrent CCB use (= complete heart block) Severe hypotension or bradycardia Sick sinus syndrome ```

Answer 44

5-10mg IV Q5-10mins up to 300mg total

Answer 45

Selective beta 1 adrenergic antagonist

Answer 46

Reversibly binds to beta 1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, and cAMP Slows SA rate and conduction through the AV node and decreases contractility, reducing cardiac O2 demand

Answer 47

Onset Rapid E1/2 life = 3-7hrs 12% PB

Answer 48

Hepatic metabolism | Renal excretion

Answer 49

``` Bradycardia Cardiac failure/asystole Dyspnea Heart block Peripheral edema Arterial insufficiency ```

Answer 50

``` Hypersensitivity Sick sinus syndrome Concurrent CCB use (= complete heart block) Asthma and COPD (in high doses) HR dependent pts ```

Answer 51

1.25-5mg IV Q2-5mins to max of 15mg

Answer 52

Beta 1 and beta 2 adrenergic antagonist

Answer 53

Reversibly binds to beta 1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, and cAMP. Slows SA rate and conduction through the AV node and decreases contractility, reducing cardiac O2 demand. Causes peripheral, cerebral, and coronary vasodilation.

Answer 54

Vd 4L/kg 90%PB E1/2t = 4hrs

Answer 55

1st pass effect & pulmonary uptake Active metabolite: hydroxypropanolol Excreted in the urine

Answer 56

``` Bronchospasm* Hypoglycemia* Severe bradycardia Severe hypotension Heart block Rebound tachycardia with rapid withdrawal ``` Syncope/dizziness

Answer 57

``` Hypersensitivity Asthma/COPD Heart block Concurrent CCB (= complete heart block) PVD DM Pregnancy ```

Answer 58

0.25-0.5mg IV titrate to 1mg/min IV

Answer 59

Dihydropyridine calcium channel antagonist

Answer 60

Competitive binds to calcium channels in vascular smooth muscle to maintain them in the INACTIVATED CLOSED STATE, preventing the influx of calcium through slow L-type voltage gated Ca++ channels , preventing the contraction of vascular smooth muscle cells

Answer 61

Onset 1-3 mins Peak 1-3 hrs E1/2t = 3-7 hrs 90% PB

Answer 62

Hepatic CYP450 metabolism | Renal excretion

Answer 63

Reflex tachycardia Hypotension MI d/t decreased afterload Skeletal muscle weakness Flushing Vertigo HA

Answer 64

Hypersensitivity Heart failure Hypotension Concomitant with grapefruit juice

Answer 65

5-15mcg/kg

Answer 66

Non-dihydropyridine calcium channel antagonist | Class IV antiarrythmic

Answer 67

Competitively binds to calcium channels in cardiac muscle tissues to maintain them in the INACTIVATED CLOSED STATE, preventing the influx of calcium through slow L-type voltage gated Ca++ channels in cardiac muscle cells. Primarily inotropic/chronotropic effects, not blood pressure.

Answer 68

CYP 450 enzymes Active metabolite: norverapamil 70% unchanged in urine

Answer 69

Heart failure Peripheral edema Increased K+ with blood products Gingival hyperplasia Dizziness

Answer 70

``` Hypersensitivity Renal failure Wide QRS V-tach Heart failure WPW, SSS, bradycardia, or heart block (conduction abnormalities) ```

Answer 71

2.5-5mg IV over 2 mins Then 5-10mg in 15 to 30 mins as needed Max 20mg

Answer 72

Benzothiazipine antiarrythmic

Answer 73

Competitively binds to calcium channels in cardiac muscle tissues, and ARTERIOLAR vascular smooth muscle tissue maintaining them in INACTIVATE CLOSED STATE, preventing the influx of calcium through slow L-type voltage gated Ca++ channels and preventing the contraction of both vascular smooth muscle and cardiac muscle cells.

Answer 74

1st pass effect | CYP450 and 30% unchanged in the urine

Answer 75

Bradycardia AV block Heart failure Edema HA, flushing Dizziness/syncope

Answer 76

Hypersensitivity

Answer 77

SVT 0.25mg/kg over 2 mins + 0.35mg/kg prn Pheo 3-10mcg/kg/min

Answer 78

Potentiates NMB Decreases anesthetic reqs Use w/ BBs can cause heart block

Answer 79

Decreases anesthetic reqs | Use w/ BBs can cause heart block

Answer 80

Potentiates NMB | Use w/ BBs can cause heart block

Answer 81

Long acting, non-selective alpha adrenergic receptor antagonist

Answer 82

Irreversibly binds to the alpha 1 and alpha 2 adrenergic receptors preventing the binding of NE, Epi, and other alpha agonists, preventing the stimulation of G-coupled proteins, adenylate cyclase, and cAMP. Blocks alpha mediated vasoconstriction. It also antagonizes Ach, Histamine, 5HT

Answer 83

Slow onset – Prodrug 60mins to peak E1/2t 24 hrs

Answer 84

Hepatic metabolism | Renal and biliary excretion

Answer 85

``` Reflex tachycardia Hypotension Seizures Palpitations Sedation with chronic use (alpha 2) Hypoglycemia ``` Flushing/syncope Impotence Nasal stuffiness Dry mouth

Answer 86

Hypersensitivity Hypotension Hypovolemia

Answer 87

10mg BID up to total 120mg/day oral – started 2-3 weeks pre op

Answer 88

Short acting, non-selective alpha adrenergic receptor antagonist

Answer 89

Competitively but REVERSIBLY binds to alpha 1 and alpha 2 adrenergic receptors, preventing the binding of NE, Epi, and other alpha agonists, preventing the stimulation of G-coupled proteins, adenylate cyclase, and cAMP. Blocks alpha mediated vasoconstriction.

Answer 90

Onset =2-5 mins DOA = 10-15 mins E1/2L = 19 mins

Answer 91

Hepatic metabolism | 10% excreted unchanged in urine

Answer 92

``` Tachycardia – reflexive Severe hypotension Arrhythmias MI Hypoglycemia ``` ``` Dizziness Flushing Impotence Nasal stuffiness Abd cramps ```

Answer 93

``` Hypersensitivity CAD, MI Pregnant moms Renal impairment PUD ```

Answer 94

30-70 mcg/kg IV to decrease BP from transient stimulation Max 20mg Extravasation = 10mg injected into affected site.

Answer 95

Selective alpha 1 adrenergic antagonist

Answer 96

Competitively binds to alpha 1 adrenergic receptors preventing the stimulation of G-coupled proteins, adenylate cyclase, and cAMP causing vasodilation of arterial and venous vasculature. Leaves the inhibiting effect of alpha 2 activity on NE release intact = less likely to have reflex tachycardia

Answer 97

Peak 3 hrs | E1/2 t = 3-4 hrs

Answer 98

Hepatic metabolism, elimination via bile and feces NON RENALLY!!

Answer 99

``` Hypotension Fluid retention Anticholinergic effects N/V Palpitations Drug-induced lupus Hepatotoxicty ``` ``` Flushing/dizziness Syncope HA Dry mouth Nasal congestion ```

Answer 100

Hypersensitivity BB use (refractory hypotension) Pregnant

Answer 101

Additive effects with diuretics/other BP meds

Answer 102

1mg PO at bedtime (max daily 20mg in divided doses)

Answer 103

Selective alpha 2 adrenergic antagonist

Answer 104

Inhibits sympathetic outflow from the medulla = decreased HR and contractility and vasomotor tone. Enhance antinociceptive state by inhibiting release of spinal substance P. Inhibit central thermoregulatory control to decrease vasoconstriction and shivering. Also affects the function of K+ channels in the CNS = making cell hyperpolarized = decreased anesthetic requirements

Answer 105

``` Onset 30-60mins Peak 60-9mins DOA 8 hrs PO E1/2t 9-12hrs 30% PB 2L/kg ```

Answer 106

50% metabolized in liver, 50% excreted unchanged

Answer 107

``` Bradycardia Heart failure Hepatotoxicity Sedation Postural hypotension Rebound hypertension with abrupt withdrawal Sodium and water retention ``` Dry mouth Skin rash Impotence

Answer 108

Pregnant women Prior to surgery Hypersensitivity

Answer 109

0.2mg-0.3mg/day Epidural and SAB = 150-450mcg

Answer 110

Direct acting vasodilator

Answer 111

Activates guanylate cyclase which leads to membrane hyperpolarization, K+ channel activation, inhibition of calcium release from SR in vascular smooth muscle. Can trigger reflexive tachycardia.

Answer 112

``` IV onset 5-20mins Peak 15-20mins E1/2t = 4 hrs (4x in renal dz) E1/2L = 100hrs d/t strong binding to smooth muscle 90% PB ```

Answer 113

Metabolized in the liver with extensive first pass effect

Answer 114

Anemias, hepatotoxicity Increased ICP, head ache, fever, chills, anxiety, disorientation, depression and coma RA, lupus like syndrome, cramps, weakness, tremors, neuritis Tachycardia, angina, orthostatic hypotension, dizziness, palpitations, Nasal congenstion, dyspnea Anorexia, NV, diarrhea, constipation, ileus Impotence, difficult micturition

Answer 115

Hypersensitivity Dissecting aortic aneurysm CAD Mitral valve rheumatic heart disease Prolonged onset should be considered before redosing

Answer 116

2.5 - 20 mg IV Q4hrs

Answer 117

Organic nitrate and venodilator

Answer 118

Generates Nitric Oxide to stimulate production of cGMP to cause peripheral and smooth muscle vasodilation. Increased venous capacitance decreases the preload to the right side of the heart = decreased right and left end diastolic pressure = decreased myocardial demand.

Answer 119

``` Reflex tachycardia Tachypnea Increase in ICP with decreased intracranial compliance Increased bleeding time Dizziness, lightheadedness, syncope N/V ```

Answer 120

``` Hypertrophic obstructive cardiomyopathy Severe aortic stenosis Hypotension, shock or MI with low left ventricular filling pressures Increased ICP Glaucoma Severe anemaia Cardiac tamponade Restrictive cardiomyopathy or pericarditis ```

Answer 121

Metabolism results in nitrate metabolite capable of producing methemoglobin by oxidation of ferrous ion in hgb

Answer 122

5-200mcg/min IV

Answer 123

Phosphodiesterase inhibitor vasodilator

Answer 124

Selectively inhibits phosphodiesterase III which is a heart specific enzyme responsible for degradation of cAMP, which increases calcium and thus increases contractility and inotropic effects. Increased cAMP also works in vascular smooth muscle to cause vasodilation and decrease peripheral vascular resistance. This all increases cardiac output.

Answer 125

``` Onset 5-15mins Peak after 5 mins E1/2time = 2.5hrs Vd = 0.4L/kg 70% PB ```

Answer 126

80% unchanged in the urine

Answer 127

``` Cardiac dysrhythmias, ventricular arrhythmias, and supraventricular arrhythmias Hypotension Angina Headaches Hypokalemia, tremor, thrombocytopenia ```

Answer 128

Hypersensitivity | Acute MI

Answer 129

50mcg/kg IV over 10mins + 0.375mcg/kg/min maintenance infusion

Answer 130

Antiarrythmic, endogenous nucleoside consisting of adenine and pentose sugar

Answer 131

Adenosine acts on adenosine A1 receptors in the cardiac conduction system that are linked to acetylcholine activated G-coupled potassium channels (Kach). This leads to slowing of cardiac conduction tissue, slowing SA node conduction, and a delay in AV node conduction.

Answer 132

E1/2 life = 10 sec; immediate onset, must be IV pushed very fast

Answer 133

Intracellular enzyme metabolism. No hepatic/renal involvement.

Answer 134

``` Headache, dizziness, parasthesia Palpitations, chest pain Hypotension Dyspnea Chest pressure Numbness ```

Answer 135

``` Hypersensitivity 2nd or 3rd degree heart block SSS without pacer Bronchospastic and restrictive lung disease (not effective in afib, aflutter, VT) ```

Answer 136

SVT: 6mg IV, if not effective give 12mg, if not effective give 18mg Controlled hypotension: 220mcg/kg/min

Answer 137

Class III antiarrhythmic (with Class I, II, IV effects) Benzofurane derivative containing iodine Atrial and ventricular dysrhythmic

Answer 138

Alters lipid membrane where ion channels are located, particularly the K+ channels responsible for repolarizations Also blocks Na+ and Ca++ channels, as well as alpha/beta receptors

Answer 139

``` Onset – IV is rapid Vd 66L/kg 96% PB E1/2t = 29days Duration after d/c therapy = 7-50days ```

Answer 140

CYP450 microsomal enzymes with biliary excretion | Active metabolite: DEA

Answer 141

Hypotension Bradycardia AV block, prolonged QTc and VT, torsades, Decreased response to catecholamines Pulm fibrosis, alveolar pneumonitis, ARDS (2% of pts) Hyper/hypothyroidism, photosensitivity

Answer 142

Hypersensitivity Cardiogenic shock, bradycardia, 2nd or 3rd degree heart block Pregnancy

Answer 143

Inhibits CYP450 enzymes = increased conc of warfarin, procainamide, digoxin Fentanyl = cardiac arrest, bradycardia, hypotension

Answer 144

A-flutter, Stable VT/SVT: 150mg IV over 10 mins, 1 mg/min over next 6 hrs, then 0.5 mg/min over next 18hrs Pulseless VT/VF: 300mg IVP, then 150mg IVP, then gtt

Answer 145

Antiarrythmic | Cardiac glycoside

Answer 146

Directly inhibits Na+/K+/ATPase pump, which increases Na+ in cardiac myocytes, which decreases Ca++ outflow by Na+/Ca++ pump, which increases available calcium for cardiac muscle contractions. Also decreases sympathetic tone and increases vagal tone to slow conduction through SA and AV nodes

Answer 147

``` Onset = 5-30mins IV Peak 1-5 hrs E1/2life = 30-48hrs Vd 7L/kg 25% PB ```

Answer 148

Hepatic metabolism | 50% excreted by kidneys unchanged.

Answer 149

EKG changes: prolonged PR interval, ST depression, T wave changes Dysrhythmias Heart block Blurred vision NV, diarrhea, headache, fatigue

Answer 150

Vfib, v-tach, heart block IHSS Renal impairment (decrease dose) Hypokalemia, hypomagnesemia or hypercalcemia can lead to toxicity

Answer 151

Loading dose = 0.75-1.5mg PO or 0.5-1.0mg IV Maint dose = 0.125-0.5mg PO or 0.25mg IV Therapeutic level 0.5-2.0ng/mL