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Pharm 1 > Adrenergic > Flashcards

Adrenergic Flashcards

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
Q

beta-2 agonist mechanisms

A 
Relax bronchial smooth muscle/decrease airway resistance
Suppress leukotriene/histamine release
enhance mucociliary function
decrease microvascular permeability
inhibit phospholipase A
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26
Q

Therapeutic uses of Metaproterenol

A

long term treatment of obstructive airway disease

Acute bronchospasm

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27
Q

Selective receptor of Terbutaline

A

beta-2

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28
Q

Therapeutic uses of Terbutaline

A

long term treatment of obstructive airway disease
Acute bronchospasm
Emerngency status asthmaticus

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29
Q

Selective receptor of Albuterol

A

beta-2

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30
Q

Therapeutic uses of Albuterol

A

treat bronchospasms

delay pre-term labor

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31
Q

Therapeutic uses of Ritodrine

A

arrest premature labor

prolong pregnancy

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32
Q

Adverse effects of beta-2 agonists

A

Tremor, restlessness, anxiety
Tachycardia - pts with CAD or arrhythmias
Increased plasma glucose, lactate and FFA
Decreased K

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33
Q

Fenoldopam receptor type

A

D1

34
Q

Effects of Fenoldopam

A

renal, mesenteric, peripheral and coronary vasodilation

35
Q

Clinical use of Fenoldopam

A

Hypertensive crisis

36
Q

Isoproterenol receptor type

A

beta-1/beta-2

37
Q

Effects of isoproterenol

A

decreased TPR, increased HR, increased contractility

38
Q

Uses of Isoproterenol

A

Bradycardia, complete heart block, CHF, MI

39
Q

Effects of Dobutamine

A

increase heart rate, increase automaticity, increase contractility (TPR unaffected)

40
Q

Adverse effects of dobutamine

A

excessive increases in BP and HR
Increased ventricular response in pts with A-fib
Ventricular ectopic activity
Increased size of MI

41
Q

Uses for dobutamine

A

short term treatment of CHF and in stress tests

42
Q

Low dose IV epinephrine effects

A

Beta-1 receptors - increase PP, HR, SV, CO

Beta-2 receptors - decrease TPR (vasodilation), decrease MAP (reflex tachycardia)

43
Q

Moderate dose IV epinephrine effects

A

Similar beta-1/beta-2

alpha-1 receptors - increased TPR, increased BP

44
Q

High dose IV epinephrine effects

A

Predominantly alpha-1 - increased TPR, BP without reflex bradycardia

45
Q

Subcutaneous epinephrine effects

A

vasoconstriction

46
Q

Vascular effects of epinephrine

A

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
Q

Cardiac effects of epinephrine

A

HR increases, systole shortens, diastole remains unchanged
Positive inotropic, lusitropic, chronotropic effect
Myocardial oxygen consumption and automaticity increased

48
Q

Epinephrine reversal phenomenon

A

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
Q

Therapeutic uses of epinephrine

A

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
Q

Contradindications of epinephrine

A

pts receiving non-selective beta receptor blocking drugs - epinephrine reversal

51
Q

Adverse effects of epinpehrine

A

restlessness, headache, tremor
cerebral hemorrhage
cardiac arrhythmias
angina in pts with CAD

52
Q

Norepinephrine is a potent stimulator of

A

alpha receptors

53
Q

Cardiovascular effects of norepinephrine

A

Increased SBP, DBP, PP, coronary flow, TPR

Decreased CO, RBF, splanchnic/hepatic blood flow

54
Q

Therapeutic uses of norepinephrine

A

limited use - treatment of low BP

55
Q

Lose dose effects of dopamine

A

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
Q

Moderate dose effects of dopamine

A

Beta-1 receptor effects predominate - increase contractility, HR, SBP, PP
No effect on DBP
Increases NE release from nerve terminals

57
Q

High dose effects of dopamine

A

alpha-1 effects predominate - generalized vasoconstriction

58
Q

Contraindications of dopamine

A

patients with hypovolemia, tachycardia, hypertension, arrhythmias, MAO inhibitors/tricyclic antidepressants

59
Q

Therapeutic uses of dopamine

A

severe CHF, cardiogenic/septic shock

60
Q

Which drug indirectly releases NE and directly activates adrenoreceptors?

A

ephedrine (decongestant with mild CNS stimulation)

61
Q

Indirect acting adrenoreceptor agonists are independent of

A

Calcium

62
Q

Effects of amphetamine

A

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
Q

Effects of tyramine

A

used to synthesize NE/E via alternative pathway
susceptible to MAO; actions increased by MAO inhibition
Chiefly peripheral

64
Q

Effects of alpha-receptor antagonists

A

decreased BP, tachycardia, epinephrine reversal, miosis, nasal stuffiness, decreased resistance to urine flow

65
Q

Determining factor for reversible alpha-antagonists

A

half-life

66
Q

Determining factor for irreversible alpha-antagonists

A

rate of receptor generation

67
Q

Therapeutic uses for alpha-antagonists

A 
Pheochromocytoma
Hypertensive emergencies
Chronic hypertension
Peripheral vascular disease
Urinary obstruction
Erectile dysfunction
68
Q

Effects of phenoxybenzamine

A

irreversible alpha-1 blockade (long duration)
Also blocks H1, ACh, 5-HT receptors
Used in pheochromocytoma

69
Q

Effects of Prazosin

A

alpha-1 selective blocker
Relaxes arterial, venous, prostate smooth muscle
Used for HTN, BPH
Can cause orthostatic hypotension

70
Q

Effects of Tamsulosin

A

alpha-1a selective

used for prostate hyperplasia

71
Q

Effects of labetalol

A

alpha/beta blocker
lowers BP without increasing HR
Treatment of HTN

72
Q

Effects of beta-blockers

A

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
Q

Therapeutic uses of beta-blockers

A 
HTN
IHD
Arrhythmias
HF
Glaucoma
Hyperthyroidism
Neurologic diseases
74
Q

If a patient has chronic obstructive lung disease or asthma, what type of beta-blocker would be preferred

A

beta-1 selective blocker

75
Q

Adverse effects of beta-blockers

A 
fatigue
worsening peripheral vascular disease
worsening bronchospasms
decreased sexual functions
Increased diabetes
masking hypoglycemia
76
Q

1st generation beta-blocker

A

propranolol - non-selective beta blocker; B1=B2

77
Q

2nd generation beta-blocker

A

Metoprolol - selective beta blocker; B1»>B2

78
Q

3rd generation beta blocker

A

Labetalol - vasodilatory beta blocker; B1=B2>a1>a2

79
Q

Effects of propranolol

A

lower HR, BP, renin

used in HTN, angina pectoris, arrhythmias, migraine, hyperthyroidism

80
Q

Effects of metaprolol

A

lower HR, BP, renin

used in HTN, angina pectoris, arrythmias

Pharm 1 (6 decks)

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