Symphathomimetics Flashcards

1
Q

Catecholamines

A

Metabolized rapidly, not effective orally, do not penetrate CNS readily

Epi, NE, Iso, DA, Dobutamine

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2
Q

Non-catecholamines

A
Alpha agonists
Beta2 selective agonists
Amphetamines, Tyramine (Indirect acting)
Mixed acting
Methylphenidate
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3
Q

Direct actions

A

Agonists of alpha or beta receptors

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4
Q

Indirect actions

A

Release NE or block NE reuptake

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5
Q

Mixed actions

A

May release NE but also act on receptor

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6
Q

Alpha 1 adrenergic effects

A
Constrict BV - increase BP
Dilate pupils
Contract spleen
*Contract uterus
Contract bladder sphincter
Mild glycogenolysis in liver
Ejaculation
Erects hair
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7
Q

Alpha 2 adrenergic effects

A

*Inhibit insulin release
Relax GI smooth muscle

Autoreceptors inhibit release
CNS effects

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8
Q

Beta 1 adrenergic effects

A

Increase HR and CO
Stimulate Renin

Think heart

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9
Q

Beta 2 adrenergic effects

A
Relax bronchioles
*Relax uterus
Relax skeletal BV and coronary BV
Glycogenolysis and lipolysis
*Stimulate insulin and renin
Relax bladder
Relax GI smooth muscle
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10
Q

Reserpine

A

Blocks formation of NE

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11
Q

Cocaine

A

Blocks uptake of NE - increased NE in terminal (increase in BP)

Blocks uptake tyramine - decreased displacement of NE to terminal (no increase in BP)

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12
Q

Beta receptor G protein

A

Stimulates

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13
Q

Alpha receptor G protein

A

Inhibits

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14
Q

A1 and A2 catecholamine potency

A

Epi > NE > Iso

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15
Q

B2 catecholamine potency

A

Iso > Epi > NE

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16
Q

B1 catecholamine potency

A

Iso > Epi = NE

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17
Q

MAO

A

Destroys NE

Need to sequester so it isn’t destroyed

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18
Q

NE reuptake

A

Major mechanism of terminating signal

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19
Q

Dopamine effects

A

CNS neurotransmitter
D1 - increase renal blood flow
D2 - nerve endings

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20
Q

Baroreceptor response to increase BP (phenylephrine)

A

Increase firing
Increase parasympathetics at heart
Decrease sympathetics at BV

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21
Q

Baroreceptor response to decrease BP (histamine)

A

Decrease firing
Increase sympathetics at heart
Increase sympathetics at BV

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22
Q

Heart and Epi

A

Increase HR and CO

Increase work and consumption of energy

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23
Q

BV and Epi

A

Greater affinity for beta2 at low dose (vasodilate)
High dose, alpha1 dominates (vasoconstriction)

Skeletal and coronary dilate
Everything else except brain constricts

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24
Q

Smooth muscle and Epi

A

Relaxation

25
Glands and Epi
Sweaty palms Increase salivary Block insulin
26
Metabolic and Epi
Calorigenic | Tremors - K+ uptake
27
Overall Epi
Increase pulse Increase sBP Decrease dBP Overall decrease in peripheral resistance
28
Uses of Epi
``` Asthma in children Anaphylactic shock (bronchodilate, constrict, inhibit histamine) Topical hemostatic ```
29
Adverse effects of Epi
Arrhythmias Cerebral hemorrhage CNS: fear, anxiety, HA
30
Epi contraindications
``` HTN Shock Hyperthryoidism Angina Asthmatics with degenerative heart disease ```
31
NE Overall
Decrease pulse (reflex) Increase both BP Increase peripheral resistance Weak Beta2 agonist
32
NE and BV
Only alpha effect
33
NE use
Manage hypotension
34
NE side effects
Anxiety, slow forceful heart beat, HA
35
Iso overall
Increase pulse Increase sBP Decrease dBP Overall decrease in peripheral resistance More selective for beta Increase FFA
36
Iso use
Asthma Heart block Cardiogenic shock - increase CO
37
Iso side effects
Tachycardia, HA, Flushing skin | Arrhythmias, anginal pain
38
Dopamine
Low dose - stimulate DA receptors High dose - stimulate alpha1 canceling DA effect Vasodilate mesenteric and renal vascular beds
39
Dopamine use
Shock MI Chronic CHF - increase CO
40
Fenoldopam
D1 agonist - HTN
41
Bromocriptine
D2 agonist - Parkinson's disease or prolactinemia
42
Dobutamine
B1 agonist Partial agonist Used with acute MI, less incidence of arrythmias than with DA (CHF and shock as well)
43
Phenylephrine
Alpha 1 agonist Vasoconstrict with reflex bradycardia ``` Nasal decongestant Maintain BP Tachycardia Anesthetic Glaucoma ```
44
Methoxamine
Alpha 1 agonist
45
Midodrine
Alpha 1 agonist | Orthostatic hypotension
46
Mixed acting alpha 1 agonist
Mephentermine (Wyamine sulfate) | Metaraminol (Aramine) - weaker but longer than NE
47
Beta2 agonists
Selectivity dose dependent Lung > heart Not metabolized rapidly, can be taken orally
48
Albuterol
Beta 2 Treat bronchospasm SE: tremors and tachycardia most common
49
Salmeterol
Long lasting beta 2 Asthma
50
Formoterol
Long lasting beta 2 Asthma
51
Meteproterenol
Beta 2 Asthma
52
Tertbutaline
Beta 2 - Used orally Asthma, delayed deliver
53
Ritodrine
Beta 2 Asthma
54
Bitolterol
Prodrug - asthma
55
Tyramine
Displaces NE from nerve terminal - causes hypertensive crisis, MI, stroke Usually destroyed by MAO
56
Amphetamines
Inhibit NE reuptake Enter CNS Effective orally Adderall, Benzedrine, Dexedrine
57
Amphetamine poisoning treatment
Increase urine acidity
58
Ephedrine/Pseudoephedrine
Direct action on Beta receptors Indirect action increase NE Long lasting and useful orally Mild effects: CNS, heart, vascoconstriction, bronchiole relax Spinal anesthesia, decongestant, bronchospasm *can be used to make meth
59
Nasal decongestants
Alpha 1 Naphazoline Tetrahydrozoline Xylometazoline Oxymetazoline (Afrin)