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Pharm 1 > Adrenergic > Flashcards

Adrenergic Flashcards

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1
Q

Synthesis of catecholamines

A

tyrosine - dopa - dopamine - NE - E

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2
Q

RLS of catecholamine synthesis

A

tyrosine to dopa

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3
Q

RLS inhibited by

A

metyrosine

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4
Q

Catecholamine transporter

A

Vesicular monoamine transporter (VMAT)

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5
Q

VMAT inhibited by

A

reserpine

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6
Q

Reuptake transporter

A

Norepinephrine transporter (NET)

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7
Q

NET inhibited by

A

cocaine; tricyclic antidepressants

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8
Q

Metabolizer of NE

A

MAO-A

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9
Q

Metabolizer of dopamine

A

MAO-B

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10
Q

MAO is inhibited by

A

phenelzine

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11
Q

alpha-1 receptor activation

A

Eye (dilator) - contraction - mydriasis
Arterioles - contraction - increase TPR, DBP, afterload
Veins - contraction - increase VR, preload
Bladder - contraction - urinary retention
Male sex organs - vas deferens - ejaculation
Liver - increase glycogenolysis
Kidney - decrease renin release

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12
Q

alpha-2 receptor activation

A

Prejunctional nerve terminal - decrease NT release
Platelets - aggregation
Pancreas - decrease insulin secretion

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13
Q

beta-1 receptor activation

A

SA node - increase HR
AV node - increase conduction velocity
atria/ventricles - increase contractility, conduction velocity, CO, O2 consumption
His-Purkinje - automaticity and conduction velocity
Kidney - renin release

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14
Q

beta-2 receptor activation

A

Blood vessels - vasodilation - decrease TPR, DBP, afterload
Uterus - relaxation
Bronchioles - dilation
Glycogenolysis and insulin secretion

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15
Q

D1

A

Renal, mesenteric, coronary vasculature - vasodilation - increased GFR, RBF, Na excretion

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16
Q

Difference between adrenergic action and muscarinic receptor blocking drugs

A

Adrenergic - mydriasis is not accompanied by cycloplegia

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17
Q

Increased TPR associated with

A

reflex bradycardia

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18
Q

Decreased TPR associated with

A

reflex tachycardia

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19
Q

Direct acting drug responses with reserpine/guanethidine

A

Not reduced

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20
Q

Indirect acting drug responses with reserpine/guanethidine

A

Abolished

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21
Q

Mixed acting drug responses with reserpine/guanethidine

A

Reduced

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22
Q

Phenylephrine receptor type

A

alpha-1

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23
Q

Clinical use of Phenylephrine

A 
Increase BP, increase TPR
antihypotensive (hypotension, shock)
paroxysmal atrial tachycardia
nasal decongestant
mydriatic
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24
Q

alpha-2 specific agonists

A

Clonidine, methyldopa - hypertension

Apraclonidine, brimonidine - glaucoma

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25
beta-2 agonist mechanisms
``` Relax bronchial smooth muscle/decrease airway resistance Suppress leukotriene/histamine release enhance mucociliary function decrease microvascular permeability inhibit phospholipase A ```
26
Therapeutic uses of Metaproterenol
long term treatment of obstructive airway disease | Acute bronchospasm
27
Selective receptor of Terbutaline
beta-2
28
Therapeutic uses of Terbutaline
long term treatment of obstructive airway disease Acute bronchospasm Emerngency status asthmaticus
29
Selective receptor of Albuterol
beta-2
30
Therapeutic uses of Albuterol
treat bronchospasms | delay pre-term labor
31
Therapeutic uses of Ritodrine
arrest premature labor | prolong pregnancy
32
Adverse effects of beta-2 agonists
Tremor, restlessness, anxiety Tachycardia - pts with CAD or arrhythmias Increased plasma glucose, lactate and FFA Decreased K
33
Fenoldopam receptor type
D1
34
Effects of Fenoldopam
renal, mesenteric, peripheral and coronary vasodilation
35
Clinical use of Fenoldopam
Hypertensive crisis
36
Isoproterenol receptor type
beta-1/beta-2
37
Effects of isoproterenol
decreased TPR, increased HR, increased contractility
38
Uses of Isoproterenol
Bradycardia, complete heart block, CHF, MI
39
Effects of Dobutamine
increase heart rate, increase automaticity, increase contractility (TPR unaffected)
40
Adverse effects of dobutamine
excessive increases in BP and HR Increased ventricular response in pts with A-fib Ventricular ectopic activity Increased size of MI
41
Uses for dobutamine
short term treatment of CHF and in stress tests
42
Low dose IV epinephrine effects
Beta-1 receptors - increase PP, HR, SV, CO | Beta-2 receptors - decrease TPR (vasodilation), decrease MAP (reflex tachycardia)
43
Moderate dose IV epinephrine effects
Similar beta-1/beta-2 | alpha-1 receptors - increased TPR, increased BP
44
High dose IV epinephrine effects
Predominantly alpha-1 - increased TPR, BP without reflex bradycardia
45
Subcutaneous epinephrine effects
vasoconstriction
46
Vascular effects of epinephrine
Main sites - arterioles and precapillary sphincters Cutaneous blood flow reduced (hands/feet) Skeletal blood flow increased Cerebral blood flow unchanged Renal blood flow decreased; GFR unchanged Pulmonary arterial/venous pressure increased Coronary blood flow increased
47
Cardiac effects of epinephrine
HR increases, systole shortens, diastole remains unchanged Positive inotropic, lusitropic, chronotropic effect Myocardial oxygen consumption and automaticity increased
48
Epinephrine reversal phenomenon
In presence of alpha antagonist, epinephrine effect on B2 is enhanced causing vasodilation, decreased TPR and MAP In presence of beta antagonist, alpha-1 effect is enhanced leading to substantial increase in MAP
49
Therapeutic uses of epinephrine
Relieve hypersensitivity reactions Prolong anesthetics Restore cardiac rhythm in pts with cardiac arrest Relieve respiratory distress due to bronchospasm Manage post-intubation and infectious croup Stop bleeding
50
Contradindications of epinephrine
pts receiving non-selective beta receptor blocking drugs - epinephrine reversal
51
Adverse effects of epinpehrine
restlessness, headache, tremor cerebral hemorrhage cardiac arrhythmias angina in pts with CAD
52
Norepinephrine is a potent stimulator of
alpha receptors
53
Cardiovascular effects of norepinephrine
Increased SBP, DBP, PP, coronary flow, TPR | Decreased CO, RBF, splanchnic/hepatic blood flow
54
Therapeutic uses of norepinephrine
limited use - treatment of low BP
55
Lose dose effects of dopamine
Renal blood vessels - vasodilation - increase GFR, RBF and filtered Na (more Na in urine) Presynaptic D2 receptors - decrease NE release, decrease alpha-adrenergic stimulation of VSMC
56
Moderate dose effects of dopamine
Beta-1 receptor effects predominate - increase contractility, HR, SBP, PP No effect on DBP Increases NE release from nerve terminals
57
High dose effects of dopamine
alpha-1 effects predominate - generalized vasoconstriction
58
Contraindications of dopamine
patients with hypovolemia, tachycardia, hypertension, arrhythmias, MAO inhibitors/tricyclic antidepressants
59
Therapeutic uses of dopamine
severe CHF, cardiogenic/septic shock
60
Which drug indirectly releases NE and directly activates adrenoreceptors?
ephedrine (decongestant with mild CNS stimulation)
61
Indirect acting adrenoreceptor agonists are independent of
Calcium
62
Effects of amphetamine
CNS: releases amines, stimulates medullary respiratory center, stimulates cortex (prevents fatigue/sleep), treats obesity (decrease food intake) CV: activates peripheral alpha/beta; increases SBP, DBP, HR - arrhythmias may occur Bladder: increases contraction
63
Effects of tyramine
used to synthesize NE/E via alternative pathway susceptible to MAO; actions increased by MAO inhibition Chiefly peripheral
64
Effects of alpha-receptor antagonists
decreased BP, tachycardia, epinephrine reversal, miosis, nasal stuffiness, decreased resistance to urine flow
65
Determining factor for reversible alpha-antagonists
half-life
66
Determining factor for irreversible alpha-antagonists
rate of receptor generation
67
Therapeutic uses for alpha-antagonists
``` Pheochromocytoma Hypertensive emergencies Chronic hypertension Peripheral vascular disease Urinary obstruction Erectile dysfunction ```
68
Effects of phenoxybenzamine
irreversible alpha-1 blockade (long duration) Also blocks H1, ACh, 5-HT receptors Used in pheochromocytoma
69
Effects of Prazosin
alpha-1 selective blocker Relaxes arterial, venous, prostate smooth muscle Used for HTN, BPH Can cause orthostatic hypotension
70
Effects of Tamsulosin
alpha-1a selective | used for prostate hyperplasia
71
Effects of labetalol
alpha/beta blocker lowers BP without increasing HR Treatment of HTN
72
Effects of beta-blockers
CV: lower BP in pts with HTN but not NTN, suppress RAS, decrease HR, low AV conduction, decrease O2 consumption Respiratory - increase airway resistance Eye - decrease intraocular pressure Metabolic - inhibit lipolysis, decrease glucagon, increase VLDL, decrease HDL
73
Therapeutic uses of beta-blockers
``` HTN IHD Arrhythmias HF Glaucoma Hyperthyroidism Neurologic diseases ```
74
If a patient has chronic obstructive lung disease or asthma, what type of beta-blocker would be preferred
beta-1 selective blocker
75
Adverse effects of beta-blockers
``` fatigue worsening peripheral vascular disease worsening bronchospasms decreased sexual functions Increased diabetes masking hypoglycemia ```
76
1st generation beta-blocker
propranolol - non-selective beta blocker; B1=B2
77
2nd generation beta-blocker
Metoprolol - selective beta blocker; B1>>>B2
78
3rd generation beta blocker
Labetalol - vasodilatory beta blocker; B1=B2>a1>a2
79
Effects of propranolol
lower HR, BP, renin | used in HTN, angina pectoris, arrhythmias, migraine, hyperthyroidism
80
Effects of metaprolol
lower HR, BP, renin | used in HTN, angina pectoris, arrythmias

Pharm 1 (6 decks)

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