Adrenergic Pharmacology Flashcards

1
Q

Precursor to catecholamines

A

Tyrosine

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2
Q

Pathway for norepinephrine

A

Tyrosine–>L DOPA–>Dopamine–>Norepinephrine

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3
Q

a2 stimulation

A

Results in negative feedback in presynaptic terminal

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4
Q

b2 receptors

A

Only stimulated by epinephrine, not NE

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5
Q

COMT

A

Metabolizes NE in synapse

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6
Q

MAO

A

Make sure that the NE mobile pool that is not recycled into vesicles is destroyed so not too much NE is released

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7
Q

Methyl Tyrosine

A

Blocks conversion of tyrosine–>L dopa and therefore decreases NE release

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8
Q

MAO inhibitors

A

Block degradation of excess NE mobile pool in presynaptic cell–can cause excess NE release

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9
Q

a1 effect on blood vessels

A

Constriction and increased BP
Arterioles: Increased TPR, increased afterload, increased diastolic BP
Veins: Increased preload and increased systolic pressure

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10
Q

a1 effect on eye

A

Dilation

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11
Q

a1 effect on kidney

A

Decreased renin release

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12
Q

a1 effect on liver

A

increased glycogenolysis

Decreased insulin

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13
Q

a1 effect on bladder

A

Increased sphincter tone and urinary retention

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14
Q

a2 effect

A

Decreased synthesis and release of NE

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15
Q

B1 effect on heart

A

Increased HR, Increased conduction velocity, increased contractility, increased SV and increased systolic pressure

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16
Q

B1 effect on kidney

A

increased renin release

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17
Q

B1 effect on ciliary body in eye

A

Increased aqueous humor

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18
Q

B2 effect on vessels

A

Vasodilation, decreased TPR and decreased diastolic pressure

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19
Q

B2 effect on bronchioles

A

Bronchodilation

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20
Q

B2 effect on uterus

A

Relaxation–can delay preterm labor

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21
Q

B2 effect on liver

A

Glycogenolysis and gluconeogenesis

Increased insulin

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22
Q

a1 agonists

A

Increase in BP with no change in pulse pressure

Does not effect HR but reflex bradycardia may occur due to increase in BP

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23
Q

Phenylephrine

A

a1 agonist
Can be used for septic shock
Use as a nasal decongestant due to vasoconstriction preventing mucus

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24
Q

a2 agonists

A

Increase negative feedback so decrease release of NE
Can help with muscle spasticity by causing muscle relaxation
Will decrease insulin so caution in diabetics

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25
Isoproterenol
Beta Agonist B1=B2 use for bradycardia and heart block (B1) and asthma (B2) Side effects: tachycardia, hypotension, flushing, headache
26
Dobutamine
B1 agonist Use for congestive heart failure management Side effects: tachycardia due to reflex from vasodilation
27
Albuterol
B2 agonist Used for acute asthma Side effects: palpitations, tremor, anxiety, restlessness
28
Terbutaline
B2 agonist | Used for premature labor
29
Salmetrerol
long acting B2 agonist, delayed onset, good for prophylaxis of asthma
30
Formoterol
Long acting b2 agonist, prompt onset, good for acute and prophylaxis
31
Norepinephrine always
Activates a1, a2, B1 Increases BP (a1 and B1 causes increased systolic BP and a1 causes slight increase in diastolic BP): increase in pulse pressure B1 causes increase in HR, however reflex bradycardia will occur due to increased BP
32
Epinephrine
Effects are dose dependent | Activates a1, a2, B1, B2
33
Low dose epi
B1 and B2 agonist | Use for anaphylactic shock
34
High dose epi
a1 and B1 primarily (looks more like NE)...B2 is masked by a1 effects Use for heart stopping
35
how to differentiate between high dose epi and NE
Need to block a1 to see if B2 becomes unmasked | Will cause hypotension if it is high dose epi
36
Effect of low dose epi on HR and BP
B1: increased HR, increased SV, increased CO B2: decreased TPR, decreased BP Increased pulse pressure and mean pressure decreases
37
Effect of medium dose epi on HR and BP
B1: increased HR, increased SV, increased CO B2: decreased TPR, decreased BP a1: increased TPR, increased BP Increased pulse pressure, mean pressure stays constant
38
Effect of high dose epi on HR and BP
B2 effect masked by a1=increased TPR and increased BP | Potential reflex bradycardia--can make ischemia worse
39
Uses of NE and epi
``` Cardiac arrest Adjunct to local anesthetic Hypotension Anaphylaxis: Epi only Asthma: Epi only ```
40
Dopamine
Can be used in shock management due to similarity to NE
41
Low dose dopamine
D1 | Vasodilation on renal, coronary, mesenteric vessels
42
Medium dose dopamine
D1 and B1 | Adds inotropic effect to D1 to preserve blood flow to heart and kidneys
43
High dose dopamine
D1, B1, a1 | a1 can help maintain BP
44
Indirect acting adrenergic receptor agonists: releasers
Displaces NE from mobile pool causing an increase in NE availability
45
Releasers can interact negatively with
MAO inhibitors and Tyramine rich food | Can cause hypertensive crisis due to too much NE
46
Examples of reuptake inhibitors of NE
Cocaine and TCAs
47
a receptor antagonists
Decrease TPR and decreases mean BP Used to fight hypertension May cause reflex tachycardia and salt/water retention
48
B1 receptor antagonists
Decreases HR, SV, and CO: good for anti-arrhythmic and decrease O2 demand and angina Decreases renin release: good for anti CHF Decreases aqueous humor production: good for anti glaucoma
49
B2 receptor antagonists
Aggregates bronchospasm in asthmatics, makes metabolic effects worse in diabetics
50
General use of beta blockers
Angina, hypertension, post MI Anti arrhythmic Glaucoma
51
Chronic use of beta blockers leads to
Upregulation and tolerance | Important to taper dose to avoid excessive CV effects
52
Additive bradycardia occurs when
Take beta blocker with calcium channel blocker | Can cause AV block
53
What can be used in Beta blocker OD
glucagon | Binds to Gs coupled receptors and reverses B blockade toxicity without interfering Beta receptor
54
1st generation beta blockers
nonselective N-Z "-olol"
55
2nd generation beta blockers
B1 selective A-M "-olol"
56
3rd generation beta blockers
Also act as vasodilators Nonselective + a1 antagonist: used in CHF Selective B1 and NO release: used in HTN
57
Clonidine
a2 agonist
58
Methyldopa
a2 agonist
59
Phentolamine
a1 blockers nonselective
60
Labetalol
A1 + b blocker
61
Amphetamines
Increase release of NE
62
Methylphenidate
Increase release of NE | Treatment of ADHD
63
Atomexetine
Increase release of NE | Treatment of ADHD
64
Modafinil
Increase release of NE | treatment of narcolepsy
65
B2 blocking effects
Bronchoconstriction, decreased aqueous humor, impotence
66
Beta blockers can decrease
Renin | Can be used for hypertension but not first line