Adrenergic Drugs Flashcards

1
Q

MOA phenylephrine and generic name

A

Alpha agonist direct, neo-synephrine

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2
Q

MOA clonidine and generic name

A

Alpha agonist direct, catapres

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3
Q

MOA norepinephrine and generic name

A

mixed alpha and beta direct, levophed

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4
Q

MOA epinephrine and generic name

A

mixed alpha and beta direct, adrenalin

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5
Q

MOA Dobutamine and generic name

A

B agonist direct, dobutrex

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6
Q

MOA isoproterenol and generic name

A

B agonist direct, isuprel

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7
Q

MOA albuterol and generic name

A

B agonist direct, ventolin

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8
Q

MOA cocaine

A

inhibit re-uptake DA and NE, indirect

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9
Q

MOA selegiline and generic name

A

indirect inhibitors of MAO, eldepryl

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10
Q

MOA phenelzine and generic name

A

indirect inhibitor of MAO, nardil

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11
Q

MOA amphetamines

A

indirect, reverse NE and DA uptake mechanism and increase their release

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12
Q

MOA methylphenidate and generic name

A

indirect, reverse NE and Da uptake mechanism and increase their release, ritalin

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13
Q

MOA tyramine

A

indirect, reverse NE and DA uptake mechanism and increase their release

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14
Q

MOA ephedrine

A

indirect, increase release of dopamine and NE and a direct receptor agonist

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15
Q

MOA adrenergic drugs

A

modulate adrenergic transmission and primarily control the function of sympathetic nervous symptoms

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16
Q

G protein and effects for alpha1 receptor

A

Gq, increase IP3 and DAG

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17
Q

G protein and effects for alpha2 receptor

A

Gi, decrease cAMP

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18
Q

G protein and effects for B receptor

A

Gs, increase cAMP

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19
Q

G protein and effects for D1 receptor

A

Gs, increase cAMP

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20
Q

G protein and effects for D2 receptor

A

Gi, decrease cAMP

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21
Q

Full response of a1 receptor activation

A

catecholamine binding leads to activation of GPCR. PLC activated by alpha subunit, leading to production of IP3 and DAG. Results in an increase in Ca and activated protein kinase and activated PKC

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22
Q

Gs activation response

A

increase cAMP leading to increase PKA

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23
Q

How do direct acting adrenergic drugs produce their effects?

A

direct interaction with adrenergic receptors

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24
Q

How do indirect acting adrenergic drugs produce their effect?

A

increasing or reducing concentration of norepinephrine at target receptors, modulate NT concentrations in post-synaptic cleft

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25
Q

Vascular smooth muscle adrenoreceptor and action

A

alpha 1, contraction

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26
Q

Pupillary dilator muscle adrenoreceptor and action

A

alpha 1, contraction (DILATION of pupil)

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27
Q

Prostate adrenoreceptor and action

A

alpha 1, contraction

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28
Q

Heart adrenoreceptor and action

A

alpha 1, increases force of contraction

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29
Q

Neuron adrenoreceptor and action

A

alpha 2, modulates transmitter release

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30
Q

Platelets adrenoreceptor and action

A

alpha 2, aggregation

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31
Q

Adrenergic and cholinergic nerve terminals adrenoreceptor and action

A

alpha 2, inhibits transmitter release

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32
Q

Fat cells adrenoreceptor and action

A

alpha 2, inhibits lipolysis

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33
Q

Heart, juxtaglomerular cells adrenoreceptor and action

A

beta 1, increase force and rate of contraction, increases renin release

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34
Q

Respiratory, uterine adrenoreceptor and action

A

beta 2, smooth muscle relaxation

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35
Q

Skeletal muscle adrenoreceptor and action

A

beta 2, promotes potassium uptake

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36
Q

Human liver adrenoreceptor and action

A

beta 2, activates glycogenolysis and gluconeogenesis

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37
Q

Bladder adrenoreceptor and action

A

beta 3, relaxes detrussor muscle

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38
Q

Smooth muscle adrenoreceptor and action

A

D1, dilates renal blood vessels

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39
Q

Epinephrine effect on cardiac function, adrenoreceptor

A

beta 1, increases force of contraction, HR and conduction velocity at AV node

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40
Q

Epinephrine effect on vascular tone, adrenoreceptor

A

Beta 2 and alpha 1, increase systolic BP, may decrease diastolic BP and total peripheral resistance

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41
Q

adrenoreceptors in skin vessels

A

alpha 1

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42
Q

adrenoreceptors in skeletal muscle

A

alpha 1 and beta 2

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43
Q

adrenoreceptors in renal and cerebral vascular beds

A

D1 and alpha 1

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44
Q

Epinephrine effect on respiratory system, adrenoreceptor

A

beta 2: relaxes bronchial muscle

alpha 1: decreases bronchial secretions

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45
Q

Epinephrine effect on skeletal muscle, adrenoreceptor

A

Beta 2, causes muscle tremor and increases K uptake by skeletal muscle

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46
Q

Epinephrine effect on blood glucose levels, adrenoreceptor

A

beta 2, enhances liver glycogenolysis and gluconeogenesis

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47
Q

Epinephrine effect on free fatty levels in blood

A

increases free fatty levels, B1

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48
Q

Epinephrine effect on renin release

A

increases renin, B1

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49
Q

Norepinephrine effects on body, adrenoreceptors

A

a1, a2, b1; cardiac stimulant but reduces heart rate, potent vasoconstrictor, increase peripheral vascular resistance and BP

50
Q

What receptor does norepinephrine not act on that epinephrine does act on?

A

Beta 2

51
Q

Phenylephrine adrenoreceptor

A

alpha 1 and 2

52
Q

Phenylephrine action

A

effective mydriatic and decongestant; severe vasoconstriction, BP elevation, severe bradycardia

53
Q

Clonidine adrenoreceptor

A

selective alpha 2 agonist

54
Q

Clonidine action

A

central effect on presynaptic alpha 2 receptors in lower brainstem, decreases sympathetic outflow and reduces BP, bradycardia

55
Q

Isoproterenol adrenoreceptor

A

beta 1 and 2

56
Q

Isoproterenol actions

A

B1: positive inotropic and chronotropic, increases CO
B2: vasodilator, decrease arterial pressure, bronchodilation

57
Q

Dobutamine adrenoreceptor

A

selective B1

58
Q

Dobutamine action

A

positive inotropic action

59
Q

Albuterol adrenoreceptor

A

selective B2 agonist

60
Q

Albuterol action

A

bronchodilation

61
Q

Important characteristics of indirect-acting adrenomimetics

A

lipophilic, easily penetrate BBB, significant central effects

62
Q

Tyramine characteristics and effects

A

hydrophilic, does not cross BBB, metabolized by liver and causes elevation of systolic BP

63
Q

Clinical uses of norepinephrine

A

hypotensive emergencies, hemorrhagic shock, overdose of antihypertensives

64
Q

Clinical uses of phenylephrine

A

hypotensive emergencies, hemorrhagic shock, overdose antihypertensives

65
Q

Clinical uses of ephedrine

A

chronic hypotension

66
Q

Clinical uses of dobutamine

A

cardiogenic shock

67
Q

Adrenomimetic for heart failure

A

dobutamine

68
Q

adrenomimetic for hypertension

A

alpha 2 agonists

69
Q

adrenomimetic fo complete AV block and cardiac arrest

A

epinephrine and isoproterenol

70
Q

Adrenomimetic for depression

A

phenelzine and selegiline

71
Q

adrenomimetic for narcolepsy

A

amphetamines, methylphenidate

72
Q

adrenomimetic for ADHD

A

methylphenidate

73
Q

adrenomimetic for obesity

A

ephedrine and amphetamines

74
Q

adrenomimetic for bronchial asthma

A

albuterol

75
Q

adrenomimetic for decongestion of mucous membranes

A

phenylephrine, ephedrine

76
Q

adrenomimetic for anaphylaxis

A

epinephrine

77
Q

adrenomimetic for induction of mydriasis

A

phenylephrine

78
Q

adrenomimetic for glaucoma

A

alpha 2 selective agonists

79
Q

adrenomimetic for stress urinary incontinence

A

ephedrine

80
Q

CV adverse effects of adrenomimetics

A

elevated BP, increased cardiac work, sinus tachycardia and ventricular arrhythmias

81
Q

CNS toxicity AE of adrenomimetics

A

insomnia, lack of appetite, anxiety, restlessness, psychoses, convulsions and hemorrhagic stroke

82
Q

MOA phentolamine and generic name

A

non-selective alpha 1 and 2 antagonist, oraverse

83
Q

MOA phenoxybenzamine and generic name

A

non-selective alpha 1 and 2 antagonist, dibenzyline

84
Q

MOA prazosin and generic name

A

alpha 1 direct antagonist, minipress

85
Q

MOA tamsulosin and generic name

A

alpha 1 direct antagonist, flomax

86
Q

MOA Labetalol and generic name

A

Beta and a1 direct antagonist, trandate

87
Q

MOA carvedilol and generic name

A

Beta and a1 direct antagonist, Coreg

88
Q

MOA propranolol and generic name

A

B1 and B2 direct blocker, Ineral

89
Q

MOA pindolol and generic name

A

B1 and B2 direct blocker, visken

90
Q

MOA nadolol and generic name

A

B1 and B2 direct blocker, corgard

91
Q

MOA metoprolol and generic name

A

direct B1 blocker, toprol

92
Q

MOA betaxolol and generic name

A

direct B1 blocker, kerlone

93
Q

MOA acebutolol and generic name

A

direct B1 blocker, sectral

94
Q

MOA atenolol and generic name

A

direct B1 blocker, tenormin

95
Q

MOA guanethidine and generic name

A

indirect antiadrenergic, NE release inhibitor; ismelin

96
Q

MOA metyrosine and generic name

A

indirect antiadrenergic, inhibitor of tyrosine hydroxylase; demser

97
Q

Phentolamine vs. Phenoxybenzamine response to NE

A

phentolamine is a reversible competitive a antagonist that is shorter acting, phenoxybenzamine is an irreversible non-competitive a antagonist

98
Q

Alpha antagonists on CV system

A

decreased peripheral vascular resistance and BP, postural hypotension, reflex tachycardia

99
Q

Alpha antagonists on GU system

A

relaxation of smooth muscle in prostate, decreased resistance to flow of urine

100
Q

Alpha antagonists of eye

A

relaxation of pupillary dilator muscle, miosis

101
Q

Alpha antagonists used for pheochromocytoma

A

phentolamine, phenoxybenzamine, metyrosine

102
Q

Alpha antagonist used for chronic hypertension

A

prazosin and doxazosin

103
Q

Alpha antagonist used for erectile dysfunction

A

phentolamine

104
Q

Alpha antagonist used for BPH

A

Tamsulosin, relieves urinary obstruction

105
Q

AE of alpha antagonist

A

postural hypotension, nasal stuffiness, tachycardia, retention of fluid and salt, impaired ejactulation

106
Q

Beta blocker antagonists

A

atenolol, nadolol, propranolol

107
Q

Beta blocker partial agonists

A

acebutolol, labetalol, pindolol

108
Q

Beta blocker inverse agonists

A

betaxolol, metoprolol

109
Q

Beta blocker with ISA are…

A

partial agonists that produce a blunted sympathetic response, resulting in less risk for bradycardia

110
Q

B blocker effect on CV system

A

negative inotropic and chronotropic effect, slow conduction via AV node; initially increases peripheral vascular resistance but will decrease with chronic use; inhibits renin release

111
Q

B blocker effect on respiratory system

A

increase airway resistance

112
Q

B blocker effect on eye

A

reduce intraocular pressure

113
Q

B blocker effects on metabolism

A

inhibition of lipolysis, increase VLDL and decrease HDL, inhibition of glycogenolysis and gluconeogensis in liver

114
Q

B blocker used for hypertension

A

beta blockers and mixed a and B blockers are used; labetalol

115
Q

B blockers used for MI

A

propranolol and metoprolol

116
Q

Clinical uses for B blockers

A

cardiac arrhythmias, MI, angina pectoris, hypertension, heart failure, glaucoma, hyperthyroidism

117
Q

B blocker used for heart failure

A

metoprolol and carvedilol

118
Q

B blocker used for glaucoma

A

betaxolol

119
Q

B blocker used for hyperthyroidism

A

propranolol

120
Q

AE of beta blockers

A

sedation, sleep disturbances, depression, increased airway resistance, trigger bronchospasm, depressed heart rate and contractility, increase VLDL and decrease HDL, hypoglycemic episodes

121
Q

Abrupt discontinuation of B blocker therapy can cause…

A

increased responsiveness to beta receptors, enhanced cardiac stimulation and arrhythmias