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
Q

Glands and Epi

A

Sweaty palms
Increase salivary
Block insulin

26
Q

Metabolic and Epi

A

Calorigenic

Tremors - K+ uptake

27
Q

Overall Epi

A

Increase pulse
Increase sBP
Decrease dBP
Overall decrease in peripheral resistance

28
Q

Uses of Epi

A
Asthma in children
Anaphylactic shock (bronchodilate, constrict, inhibit histamine)
Topical hemostatic
29
Q

Adverse effects of Epi

A

Arrhythmias
Cerebral hemorrhage
CNS: fear, anxiety, HA

30
Q

Epi contraindications

A
HTN
Shock
Hyperthryoidism
Angina
Asthmatics with degenerative heart disease
31
Q

NE Overall

A

Decrease pulse (reflex)
Increase both BP
Increase peripheral resistance

Weak Beta2 agonist

32
Q

NE and BV

A

Only alpha effect

33
Q

NE use

A

Manage hypotension

34
Q

NE side effects

A

Anxiety, slow forceful heart beat, HA

35
Q

Iso overall

A

Increase pulse
Increase sBP
Decrease dBP
Overall decrease in peripheral resistance

More selective for beta

Increase FFA

36
Q

Iso use

A

Asthma
Heart block
Cardiogenic shock - increase CO

37
Q

Iso side effects

A

Tachycardia, HA, Flushing skin

Arrhythmias, anginal pain

38
Q

Dopamine

A

Low dose - stimulate DA receptors
High dose - stimulate alpha1 canceling DA effect

Vasodilate mesenteric and renal vascular beds

39
Q

Dopamine use

A

Shock
MI
Chronic CHF - increase CO

40
Q

Fenoldopam

A

D1 agonist - HTN

41
Q

Bromocriptine

A

D2 agonist - Parkinson’s disease or prolactinemia

42
Q

Dobutamine

A

B1 agonist
Partial agonist

Used with acute MI, less incidence of arrythmias than with DA (CHF and shock as well)

43
Q

Phenylephrine

A

Alpha 1 agonist

Vasoconstrict with reflex bradycardia

Nasal decongestant
Maintain BP
Tachycardia
Anesthetic
Glaucoma
44
Q

Methoxamine

A

Alpha 1 agonist

45
Q

Midodrine

A

Alpha 1 agonist

Orthostatic hypotension

46
Q

Mixed acting alpha 1 agonist

A

Mephentermine (Wyamine sulfate)

Metaraminol (Aramine) - weaker but longer than NE

47
Q

Beta2 agonists

A

Selectivity dose dependent
Lung > heart

Not metabolized rapidly, can be taken orally

48
Q

Albuterol

A

Beta 2
Treat bronchospasm

SE: tremors and tachycardia most common

49
Q

Salmeterol

A

Long lasting beta 2

Asthma

50
Q

Formoterol

A

Long lasting beta 2

Asthma

51
Q

Meteproterenol

A

Beta 2

Asthma

52
Q

Tertbutaline

A

Beta 2 - Used orally

Asthma, delayed deliver

53
Q

Ritodrine

A

Beta 2

Asthma

54
Q

Bitolterol

A

Prodrug - asthma

55
Q

Tyramine

A

Displaces NE from nerve terminal - causes hypertensive crisis, MI, stroke

Usually destroyed by MAO

56
Q

Amphetamines

A

Inhibit NE reuptake
Enter CNS
Effective orally

Adderall, Benzedrine, Dexedrine

57
Q

Amphetamine poisoning treatment

A

Increase urine acidity

58
Q

Ephedrine/Pseudoephedrine

A

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
Q

Nasal decongestants

A

Alpha 1

Naphazoline
Tetrahydrozoline
Xylometazoline
Oxymetazoline (Afrin)