Adrenergic Drugs Flashcards
1
Q
MOA phenylephrine and generic name
A
Alpha agonist direct, neo-synephrine
2
Q
MOA clonidine and generic name
A
Alpha agonist direct, catapres
3
Q
MOA norepinephrine and generic name
A
mixed alpha and beta direct, levophed
4
Q
MOA epinephrine and generic name
A
mixed alpha and beta direct, adrenalin
5
Q
MOA Dobutamine and generic name
A
B agonist direct, dobutrex
6
Q
MOA isoproterenol and generic name
A
B agonist direct, isuprel
7
Q
MOA albuterol and generic name
A
B agonist direct, ventolin
8
Q
MOA cocaine
A
inhibit re-uptake DA and NE, indirect
9
Q
MOA selegiline and generic name
A
indirect inhibitors of MAO, eldepryl
10
Q
MOA phenelzine and generic name
A
indirect inhibitor of MAO, nardil
11
Q
MOA amphetamines
A
indirect, reverse NE and DA uptake mechanism and increase their release
12
Q
MOA methylphenidate and generic name
A
indirect, reverse NE and Da uptake mechanism and increase their release, ritalin
13
Q
MOA tyramine
A
indirect, reverse NE and DA uptake mechanism and increase their release
14
Q
MOA ephedrine
A
indirect, increase release of dopamine and NE and a direct receptor agonist
15
Q
MOA adrenergic drugs
A
modulate adrenergic transmission and primarily control the function of sympathetic nervous symptoms
16
Q
G protein and effects for alpha1 receptor
A
Gq, increase IP3 and DAG
17
Q
G protein and effects for alpha2 receptor
A
Gi, decrease cAMP
18
Q
G protein and effects for B receptor
A
Gs, increase cAMP
19
Q
G protein and effects for D1 receptor
A
Gs, increase cAMP
20
Q
G protein and effects for D2 receptor
A
Gi, decrease cAMP
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
22
Q
Gs activation response
A
increase cAMP leading to increase PKA
23
Q
How do direct acting adrenergic drugs produce their effects?
A
direct interaction with adrenergic receptors
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
25
Vascular smooth muscle adrenoreceptor and action
alpha 1, contraction
26
Pupillary dilator muscle adrenoreceptor and action
alpha 1, contraction (DILATION of pupil)
27
Prostate adrenoreceptor and action
alpha 1, contraction
28
Heart adrenoreceptor and action
alpha 1, increases force of contraction
29
Neuron adrenoreceptor and action
alpha 2, modulates transmitter release
30
Platelets adrenoreceptor and action
alpha 2, aggregation
31
Adrenergic and cholinergic nerve terminals adrenoreceptor and action
alpha 2, inhibits transmitter release
32
Fat cells adrenoreceptor and action
alpha 2, inhibits lipolysis
33
Heart, juxtaglomerular cells adrenoreceptor and action
beta 1, increase force and rate of contraction, increases renin release
34
Respiratory, uterine adrenoreceptor and action
beta 2, smooth muscle relaxation
35
Skeletal muscle adrenoreceptor and action
beta 2, promotes potassium uptake
36
Human liver adrenoreceptor and action
beta 2, activates glycogenolysis and gluconeogenesis
37
Bladder adrenoreceptor and action
beta 3, relaxes detrussor muscle
38
Smooth muscle adrenoreceptor and action
D1, dilates renal blood vessels
39
Epinephrine effect on cardiac function, adrenoreceptor
beta 1, increases force of contraction, HR and conduction velocity at AV node
40
Epinephrine effect on vascular tone, adrenoreceptor
Beta 2 and alpha 1, increase systolic BP, may decrease diastolic BP and total peripheral resistance
41
adrenoreceptors in skin vessels
alpha 1
42
adrenoreceptors in skeletal muscle
alpha 1 and beta 2
43
adrenoreceptors in renal and cerebral vascular beds
D1 and alpha 1
44
Epinephrine effect on respiratory system, adrenoreceptor
beta 2: relaxes bronchial muscle
| alpha 1: decreases bronchial secretions
45
Epinephrine effect on skeletal muscle, adrenoreceptor
Beta 2, causes muscle tremor and increases K uptake by skeletal muscle
46
Epinephrine effect on blood glucose levels, adrenoreceptor
beta 2, enhances liver glycogenolysis and gluconeogenesis
47
Epinephrine effect on free fatty levels in blood
increases free fatty levels, B1
48
Epinephrine effect on renin release
increases renin, B1
49
Norepinephrine effects on body, adrenoreceptors
a1, a2, b1; cardiac stimulant but reduces heart rate, potent vasoconstrictor, increase peripheral vascular resistance and BP
50
What receptor does norepinephrine not act on that epinephrine does act on?
Beta 2
51
Phenylephrine adrenoreceptor
alpha 1 and 2
52
Phenylephrine action
effective mydriatic and decongestant; severe vasoconstriction, BP elevation, severe bradycardia
53
Clonidine adrenoreceptor
selective alpha 2 agonist
54
Clonidine action
central effect on presynaptic alpha 2 receptors in lower brainstem, decreases sympathetic outflow and reduces BP, bradycardia
55
Isoproterenol adrenoreceptor
beta 1 and 2
56
Isoproterenol actions
B1: positive inotropic and chronotropic, increases CO
B2: vasodilator, decrease arterial pressure, bronchodilation
57
Dobutamine adrenoreceptor
selective B1
58
Dobutamine action
positive inotropic action
59
Albuterol adrenoreceptor
selective B2 agonist
60
Albuterol action
bronchodilation
61
Important characteristics of indirect-acting adrenomimetics
lipophilic, easily penetrate BBB, significant central effects
62
Tyramine characteristics and effects
hydrophilic, does not cross BBB, metabolized by liver and causes elevation of systolic BP
63
Clinical uses of norepinephrine
hypotensive emergencies, hemorrhagic shock, overdose of antihypertensives
64
Clinical uses of phenylephrine
hypotensive emergencies, hemorrhagic shock, overdose antihypertensives
65
Clinical uses of ephedrine
chronic hypotension
66
Clinical uses of dobutamine
cardiogenic shock
67
Adrenomimetic for heart failure
dobutamine
68
adrenomimetic for hypertension
alpha 2 agonists
69
adrenomimetic fo complete AV block and cardiac arrest
epinephrine and isoproterenol
70
Adrenomimetic for depression
phenelzine and selegiline
71
adrenomimetic for narcolepsy
amphetamines, methylphenidate
72
adrenomimetic for ADHD
methylphenidate
73
adrenomimetic for obesity
ephedrine and amphetamines
74
adrenomimetic for bronchial asthma
albuterol
75
adrenomimetic for decongestion of mucous membranes
phenylephrine, ephedrine
76
adrenomimetic for anaphylaxis
epinephrine
77
adrenomimetic for induction of mydriasis
phenylephrine
78
adrenomimetic for glaucoma
alpha 2 selective agonists
79
adrenomimetic for stress urinary incontinence
ephedrine
80
CV adverse effects of adrenomimetics
elevated BP, increased cardiac work, sinus tachycardia and ventricular arrhythmias
81
CNS toxicity AE of adrenomimetics
insomnia, lack of appetite, anxiety, restlessness, psychoses, convulsions and hemorrhagic stroke
82
MOA phentolamine and generic name
non-selective alpha 1 and 2 antagonist, oraverse
83
MOA phenoxybenzamine and generic name
non-selective alpha 1 and 2 antagonist, dibenzyline
84
MOA prazosin and generic name
alpha 1 direct antagonist, minipress
85
MOA tamsulosin and generic name
alpha 1 direct antagonist, flomax
86
MOA Labetalol and generic name
Beta and a1 direct antagonist, trandate
87
MOA carvedilol and generic name
Beta and a1 direct antagonist, Coreg
88
MOA propranolol and generic name
B1 and B2 direct blocker, Ineral
89
MOA pindolol and generic name
B1 and B2 direct blocker, visken
90
MOA nadolol and generic name
B1 and B2 direct blocker, corgard
91
MOA metoprolol and generic name
direct B1 blocker, toprol
92
MOA betaxolol and generic name
direct B1 blocker, kerlone
93
MOA acebutolol and generic name
direct B1 blocker, sectral
94
MOA atenolol and generic name
direct B1 blocker, tenormin
95
MOA guanethidine and generic name
indirect antiadrenergic, NE release inhibitor; ismelin
96
MOA metyrosine and generic name
indirect antiadrenergic, inhibitor of tyrosine hydroxylase; demser
97
Phentolamine vs. Phenoxybenzamine response to NE
phentolamine is a reversible competitive a antagonist that is shorter acting, phenoxybenzamine is an irreversible non-competitive a antagonist
98
Alpha antagonists on CV system
decreased peripheral vascular resistance and BP, postural hypotension, reflex tachycardia
99
Alpha antagonists on GU system
relaxation of smooth muscle in prostate, decreased resistance to flow of urine
100
Alpha antagonists of eye
relaxation of pupillary dilator muscle, miosis
101
Alpha antagonists used for pheochromocytoma
phentolamine, phenoxybenzamine, metyrosine
102
Alpha antagonist used for chronic hypertension
prazosin and doxazosin
103
Alpha antagonist used for erectile dysfunction
phentolamine
104
Alpha antagonist used for BPH
Tamsulosin, relieves urinary obstruction
105
AE of alpha antagonist
postural hypotension, nasal stuffiness, tachycardia, retention of fluid and salt, impaired ejactulation
106
Beta blocker antagonists
atenolol, nadolol, propranolol
107
Beta blocker partial agonists
acebutolol, labetalol, pindolol
108
Beta blocker inverse agonists
betaxolol, metoprolol
109
Beta blocker with ISA are...
partial agonists that produce a blunted sympathetic response, resulting in less risk for bradycardia
110
B blocker effect on CV system
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
B blocker effect on respiratory system
increase airway resistance
112
B blocker effect on eye
reduce intraocular pressure
113
B blocker effects on metabolism
inhibition of lipolysis, increase VLDL and decrease HDL, inhibition of glycogenolysis and gluconeogensis in liver
114
B blocker used for hypertension
beta blockers and mixed a and B blockers are used; labetalol
115
B blockers used for MI
propranolol and metoprolol
116
Clinical uses for B blockers
cardiac arrhythmias, MI, angina pectoris, hypertension, heart failure, glaucoma, hyperthyroidism
117
B blocker used for heart failure
metoprolol and carvedilol
118
B blocker used for glaucoma
betaxolol
119
B blocker used for hyperthyroidism
propranolol
120
AE of beta blockers
sedation, sleep disturbances, depression, increased airway resistance, trigger bronchospasm, depressed heart rate and contractility, increase VLDL and decrease HDL, hypoglycemic episodes
121
Abrupt discontinuation of B blocker therapy can cause...
increased responsiveness to beta receptors, enhanced cardiac stimulation and arrhythmias
