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Neurology 2 > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

1
Q

Alpha-1 pathway

A

Gq - PLC, IP3/DAG, Ca++/CaM, PKC, Ras, Raf, Mek, Erk

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2
Q

Beta/gamma subunit activity in Gq

A

PI-3 kinase, AKT

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3
Q

Alpha-2 pathway

A

Gi - Adenylyl cyclase inhibition, less cAMP, less PKA

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4
Q

Beta pathway

A

Gs - Adenylyl cyclase, cAMP, PKA (catalytic subunits)

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5
Q

Vascular smooth muscle

A

Alpha-1: Vasoconstriction

Beta-2: Vasodilation

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6
Q

Pupil

A

Alpha-1

Dilation

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7
Q

Hair

A

Alpha-1

Erects hair

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8
Q

Prostate

A

Alpha-1

Contraction

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9
Q

Heart

A

Alpha-1: Contraction

Beta-1: Contraction

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10
Q

Adrenergic and cholinergic nerve terminals (pre-synaptic)

A

Alpha-2: Inhibits transmitter release (auto-regulation)

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11
Q

Fat cells

A

Alpha-2: Inhibits lipid release

Beta-3: Activates lipid release

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12
Q

Smooth muscle (respiratory, uterine)

A

Beta-2: relaxation

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13
Q

Skeletal muscle

A

Beta-2: Potassium uptake

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14
Q

Liver

A

Beta-2: Glycogenolysis (activate glucose release)

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15
Q

Bladder

A

Beta-3: Relax detrusor

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16
Q

Renal blood vessels

A

D1: Dilation

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17
Q

Nerve endings

A

D2: Modulates transmitter release

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18
Q

Direct-acting adrenergic drug clases

A

Agonsts, antagonists

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19
Q

Indirect-acting adrenergic drug function

A

Altering NE at receptor location

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20
Q

Cocaine

A

Indirect agonist

Re-uptake inhibitor for DA and NE

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21
Q

Selegiline, Phenelzine

A

Indirect agonist

MAO inhibitors

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22
Q

Ephedrine

A

Mixed-acting agonist

NE release + receptor agonist

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23
Q

Amphetamines, Methylphenidate (Ritalin)

A

Indirect agonist

Reverse NE and DA uptake, increased release

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24
Q

Alpha direct agonist drugs

A

Phenylephrine
Methoxamine
Clonidine

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25
Mixed alpha/beta direct agonist drugs
NE, Epinephrine
26
Beta direct agonist drugs
Dobutamine Isoproterenol Terbutaline Albuterol
27
Dopamine direct agonist drugs
Dopamine | Fenoldopam
28
Alpha-1 > alpha-2 direct agonists
Phenylephrine | Methoxamine
29
Alpha-2 > alpha-1 direct agonists
Clonidine, methylnorepinephrine
30
NE vs Epinephrine
``` NE = Both alpha's, Beta-1 Epi = Both alpha's, both beta's ```
31
Beta-1 > beta-2 direct agonist
Dobutamine
32
Beta-2 > beta-1 direct agonists
Albuterol, terbutaline, ritodrine
33
Isoproterenol
Both beta's equal
34
Fenoldopam
D1
35
Overall effect of an adrendergic drug is based on what things?
1. Receptors expressed at a tissue 2. Receptor selectivity of drug 3. Intrinsic activity of drug 4. Compensatory reflexes 5. Tolerance and tachyphylaxis development
36
Tachyphylaxis
Sudden decrease in response to drug after administration
37
Drug tolerance
Progressively reduced response to drug over time
38
Epinephrine effects
1. Increased heart fxn (beta-1) 2. Constant arterial pressure (beta-2 + alpha-1) 3. Bronchial relaxation (beta-2) 4. Decreased bronchial secretion (alpha-1) 5. Muscle tremor and hypokalemia (beta-2) 6. Elevated blood glucose (beta-2 and alpha-2) 7. Elevated blood FA's (beta's)
39
Norepinephrine effects
NOT beta-2... 1. Increased heart fxn (beta-1) 2. Vasoconstriction --> increased BP (alpha-1)
40
NE does NOT do what?
Bronchodilation or vasodilation
41
Dopamine effects at normal dose
1. Renal, cerebral, mesenteric, coronary vasodilation (D1) | 2. Suppressed NE release (D2)
42
Dopamine effect at higher doses
3. Beta-1 activation in heart | 4. Alpha-1 vasoconstriction
43
Phenylephrine effects
Alpha-1 direct agonist... 1. Myadriasis (pupillary dilation) and decongestant 2. Severe BP elevation (vasoconstriction)
44
Phenylephrine + baroreflex
HR sharp drop following BP elevation
45
Clonidine effects
Alpha-2 direct agonist (vasomotor center of brainstem) - Decreased sympathetics (blocked NE release) a. Reduced BP (blocked NE = blocked alpha-1) b. Bradycardia (blocked NE = blocked beta-1)
46
Clonidine local application
Vasoconstriction????
47
Isoproterenol effects
Beta (both) direct agonist (inotropic, chronotropic) - Increased cardiac output (beta-1) - Decreased BP (beta-2) - Bronchodilation (beta-2)
48
Dobutamine effects
Beta-1 agonist (inotropic) | - Increased heart contractility
49
Isoproterenol vs. dobutamine
Isoproterenol = MORE chonotropic action than dobutamine
50
Dobutamine and alpha-1
Given as racemic mixture of (+) isomer and (-) isomer, which antagonize alpha-1 and agonize alpha-1, respectively. Outcome = no changed effect on alpha-1 receptors
51
Terbutaline effects
Beta-2 agonist | - Bronchodilation, uterine relaxation
52
Albuterol effects
Same as terbutaline
53
Selectivity of indirect-acting drugs
Non-selective, all receptors activated by the neurotransmitter are affected
54
Characteristics of indirect-acting agonist drugs
Lipophilic, penetrate BBB, CNS STIMULANTS
55
Function of indirect-acting agonists
Increase NE in cleft for signaling
56
Amphetamines
Increased NE in CNS... - Alerting effects - Improved attention
57
Cocaine
Inhibits transmitter re-uptake at adrenergic synapses
58
Ephedrine
Nonselective direct adrenergic agonist (like epinephrine) Indirect increased release of transmitters (like amphetamines) Mild CNS stimulant
59
Treating hypotensive emergencies How?
NE, phenylephrine, methoxamine
60
Alpha-1 and alpha-2 antagonists
Phentolamine, phenoxybenzamine
61
Alpha-1 antagonists Commonality?
Prazosin, Terazosin, Tamsulosin, Doxazosin, Alfuzosin, Silodosin ALL END IN "-OSIN"
62
Phentolamine vs. phenoxybenzamine
Both alpha1 and alpha2 antagonists... ``` Phentolamine = competitive Phenoxybenzamine = irreversible non-competitive ```
63
Alpha antagonists on CV system
Decreased BP (peripheral) Reflex tachycardia Postural hypotension
64
Alpha antagonists on GU system
Prostate relaxation | Decreased resistance to urine flow
65
Alpha antagonists on eye
Pupillary constriction (dilator relaxation)
66
Alpha-1 selective vs. non-selective alpha antagonsits
``` Alpha-1 = decreased beta activity via alpha-2 activity Both = increased beta activity (increased heart fxn) ```
67
Atenolol, Betaxolol
Beta-1 antagonist
68
Nadolol, Propranolol
Beta antagonist
69
Acebutolol
Beta-1 partial agonist
70
Labetalol
Beta and alpha-1 partial agonist
71
Penbutolol, Pindolol
Beta partial agonist
72
Carvedilol
Beta and alpha-1 inverse agonist
73
Metoprolol
Beta-1 inverse agonist
74
Beta/beta-1 partial agonists are ______
Beta blockers with ISA (intrinsic sympathomimetic activity)
75
Partial agonists produce a ______ Benefit? Used when?
Blunted sympathetic response Less risk for bradycardia, increased cholesterol, or other beta receptor blockage issues When full antagonist is not indicated (ex. lowering BP)
76
Beta-blockers on heart
Negative inotropic Negative chronotropic Block AV node (increased PR interval)
77
Beta-blockers on blood vessels
Initial rise in vascular resistance | Chronic - decrease in PVR due to heart effects
78
Beta-blockers on renal system
Inhibit renin release (decrease BP)
79
Beta-blockers on respiratory system
Increased airway resistance
80
Beta-blockers on eye
Reduced aqueous humor production --> lower intraocular pressure
81
Beta blockers on metabolism
Inhibit lypolysis Increase LDL/HDL ratio (bad) Inhibit glycogenolysis
82
Adverse effects of beta-blockers
Sedation/depression (CNS effects) Bronchospasm/asthma attack (beta-2 blockers) Hypotension Increased VLDL, decreased HDL Hypoglycemic episodes (post-prandial, DM type 1) Blunted perception of hypoglycemic episodes
83
How to fix sedation/depression from beta-blockers
Switch to more hydrophilic drug
84
How to fix bronchospasm from beta-blockers
Switch to beta-1 selective
85
How to fix heart slowing from beta-blockers
Switch to partial agonist
86
How to fix VLDL increase from beta-blockers
Switch to partial agonist
87
How to fix hypoglycemic episodes from beta-blockers
Switch to beta-1 selective
88
Abrupt discontinuation of beta-blockers Why?
Sympathetic hyper-response, heart problems Body increases NE production to try to override beta-blocker, THUS will have extra after quitting drug
89
Guanethidine Clinical use?
NE release inhibitor Chronic HTN
90
Clonidine Clinical use?
Presynaptic alpha-2 agonist Chronic HTN
91
Metyrosine Clinical use?
Tyrosine hydroxylase inhibitor (catecholamine production) Pheochromocytoma
92
MoA of Guanethidine
NE release inhibitor... Taken up by reuptake mechanism Replaces NE in vesicles Gradual depletion of NE stores

Neurology 2 (22 decks)

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