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Pharmacology > ANS: Sympathomimetics > Flashcards

ANS: Sympathomimetics Flashcards

1
Q

A1 actions

Vascular smooth muscle (and which)

A

Blood vessels, sphincters, bronchi

Contraction

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2
Q

A1 action
Iris
Pilomotor smooth muscle

A

Radial muscle contraction dilates pupils, mydriasis

Erects hair

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3
Q

A1 actions
Prostate and uterus
Heart

A

Contraction

Increases force of contraction but B1 more important

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4
Q

Tissues innervated by A1 6

A

Vascular smooth muscle, iris, pilomotor smooth muscle, prostate, uterus, heart

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5
Q

A2 actions
Platelets
GI tract
CNS

A

Aggregation
Relaxation (presynaptic)
Sedation and analgesia from decreased SNS outflow

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6
Q

A2 actions

Adrenergic and cholinergic presynaptic nerve terminals

A

Inhibits NT release, decreased BP and HR

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7
Q

A2 actions

Vascular smooth muscle

A

Contraction- post synaptic

Dilation- pre synaptic CNS

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8
Q

Tissues innervated by A2: 5

A

Plt, vascular smooth muscle, GI, CNS, adrenergic and cholinergic presynaptic nerve terminals

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9
Q

B1

Tissues innervated and action

A

Heart (inc force and rate of contraction)

Kidneys (stim renin release)

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10
Q

B2 action

Respiratory, uterine, vascular, GI, GU visceral smooth muscle

A

Smooth muscle relaxation

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11
Q

B2 action
Mast cells
Liver
Pancreas

A

Decreases histamine release
Glycogenolysis
Increases insulin secretion

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12
Q

B2 action

Adrenergic nerve terminals

A

Increases NE release

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13
Q

B2 Action

Skeletal muscle

A

K uptake, dilation of vascular beds, tremor, increased contraction speed

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14
Q

B3

Tissue innervated, action

A

Fat cells, lipolysis activation/thermogenesis

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15
Q

D1 tissue and action

A

Smooth muscle. Post synaptic: dilated renal, mesenteric, coronary, and cerebral blood vessels

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16
Q

D2 tissue and actions

A

Nerve endings. Pre synaptic: modulates NT release, Nausea and vomiting

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17
Q

Endogenous vs synthetic catecholamines

A

Endogenous: epi, NE, dopa
Synthetic: isoproterenol, dobutamine

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18
Q

Synthetic non catecholamines
Indirect
Direct

A

Indirect: ephedrine, mephentermine, amphetamines
Direct: phenylephrine, methoxamine

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19
Q

Selective A2 agonists

Selective B2 agonists

A

Clonidine, dexmedetomidine

Albuterol, terbutaline, ritodrine

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20
Q

SNS

Direct agonists have ___ affinities for: 4

A

Varied. A1/2, B1/2

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21
Q

SNS

Indirect agonists do what

A

Increase release of NTs

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22
Q

All sympathomimetics are __ __ ___

A

Beta phenylethylamine derivatives

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23
Q

All sympathomimetics have which side chain

What group on 3,4 carbons of benzene ring (what this is)

A

Amine NH2 side chain
Hydroxyl group, catechol (a and b receptor activity)
Why they are catecholamines

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24
Q

Sympathomimetic MOA
Activation of:
Indirect v direct

A

G protein coupled receptor
Indirect: drug inc NE release from post gang SNS nerves, activ receptor
Direct: drug binds to receptor and activ G protein itself

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25
Q

Termination of effect of sympathomimetics
Catecholamines
4

A

Reuptake: I (neuronal) II (extraneuronal)

MAO, COMT, lungs

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26
Q

Termination of effect

Non catecholamines: 2

A

MAO, urinary excretion (unchanged)

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27
Q

Alpha agonist selectivity
Phenylephrine
Clonidine

A

P: A1>A2»>B
C: A2>A1»>B
Both dont effect beta

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28
Q

Alpha and beta agonist selectivity
Norepi
Epi

A

A1=A2; B1»>B2

A1=A2; B1=B2

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29
Q

Beta agonist selectivity
Dobutamine
Isuprel

A

B1>B2»>A

B1=B2»>A

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30
Q

Bagonist selectivity

Terbutaline/albuterol

A

B2>B1»>A

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31
Q

Dopamine agonist selectivity
Dopamine
Fenoldopam

A

D1=D2»B»A

D1»D2

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32
Q

Epi
Most potent activator of what
Routes
Lipid solubility, implication

A

Alpha receptors
SQ or IV
Poorly lipid soluble= little CNS effect

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33
Q

Epi
Onset SQ vs IV
Duration

A

SQ 5-10 min, IV 1-2 min

5-10 min

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34
Q

Epi
Indications
6

A

Bronchial asthma, acute allergic rxn, cv arrest (asystole), electromechanical dissociation, vfib unresponsive to defibrillation, gtt to increase contractility

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35
Q

Epi dosing
Standard bolus for resuscitation
Can start w what for less severe hypotension
Need infusion when

A

10 mcg/kg IV
2-8 mcg/kg
Single bolus dose fx dissipate after 1-5 min

36
Q

Epi dosing

For: beta 1, beta 2, alpha and beta

A

1-2 mcg/min beta 2
4-5 mcg/min beta 1
10-20 mcg/min alpha and beta

37
Q

Epi stim all ___

Major role

A

Adrenoreceptors

BP regulation

38
Q

Epi effects
A1
A2

A

A1- vasoconstriction, inc BP, inc CVP, inc cv work

A2- negative feedback, decreases BP

39
Q

Epi cv effects
B1
B2

A

Increased contractility, HR, CO, inc BP

Peripheral vasodilation- decreases BP

40
Q

Epi CV effects

A1 vs B2 targets

A

A1- skin, mucosa, hepatic, renal

B2- skeletal muscle

41
Q

Epi
With moderate doses, ___ tends to increase, __, ___
DBP tends to ___ ___, __ stays the same

A

SBP, B1, A1

Decrease, B2, MAP

42
Q

Epi effects in cerebral, coronary, and pulmonary vasculature

A

Minimal vasoconstriction of arterioles.

Inc cerebral BF even w/normal BP d/t redistribution of BF

43
Q

Epi
Ocular effects
Actions of A1, A2, B1

A

A1- mydriasis to accommodate for distant vision
A1, A2- inc humoral outflow (reg intraocular P)
B1- Inc produc of aquous humor (reg intraocular P)

44
Q

Respiratory fx epi
B2
A1

A

B2: dilate smooth muscles of bronchial tree, dec release of vasoactive mediators (histamine) in bronchial vessels
A1: decongestion, reduces secretions

45
Q

GI fx epi

A, A1, A2, B

A

A, B2- decreased peristalsis from smooth muscle relaxation
A2- decreased gastric secretions
A1- decreased sphlanchnic BF (even if BP normal)

46
Q 
GU epi fx 
Renal vasculature (receptors and effects)
A

A1- renal bf reduced even if BP stable

B1- kidney inc renin release

47
Q

GU fx epi

Bladder (receptors and effect)

A

A1- contracts urethral sphincter, continence

B2- Relaxation, decreases UOP

48
Q

GU fx epi
Erectile tissue
Uterus
(Receptor/fx)

A

A1 facilitates ejaculation

B2- relaxes, inhib labor

49
Q

Metabolic fx epi
A2
B2
B3

A

A2- inhib insulin release (opposed by B2)
B2- increased liver glycogenolysis and promotes insulin release
B3- Increased adipose tissue lipolysis

50
Q

NE
Hypotension dose
Potent effects where

A

4-16 mcg/min

Alpha and beta 1

51
Q

NE

Beta 2 effects

A 
Minimal. Vasoconstriction skel musc, liver, kidneys, cutaneous tissue. 
Inc SBP, DBP, MAP. 
Baroreceptors activ (dec HR and RR)
Dec venous return, CO, HR (despite B1)
52
Q

Dopamine
Precursor of
Stim what

A

NE

All adrenergic receptors inc dopamine

53
Q

Dopamine

Dosing guidelines

A

1-3 mcg/kg/min D1
3-10 mcg/kg/min B1
>10 mcg/kg/min alpha

54
Q

Dopamine
Increases 4
Also inc ___ why its not as useful when

A

Contractility, GFR, renal BF, UOP

NE, depleted catecholamine stores

55
Q

Dopamine
Synergistic w/___ to reduce ___ and improve __ __
Inhibitory at __ __, pts may have alt response to ___
Inc __ pressure

A

Dobutamine, afterload, CO
Carotid bodies, hypoxia
Intraocular

56
Q 
Isoproterenol 
\_\_ \_\_ and \_\_ agonists 
Chemical \_\_\_
Rapid metab by \_\_\_ (need \_\_)
Pt at risk:
A

Selective B1 and B2
Pacemaker
COMT (gtt)
CAD

57
Q

Isoproterenol
CV effects
Dose for heart block and bradydysrhythmias

A

Inc hr, contractility, SBP
Dec SVR, DBP, MAP
1-5 mcg/min

58
Q

Dobutamine
Dose gtt
CV effects

A

2-10 mcg/kg/min
Improves CO w/o inc HR or BP (good CHF drug)
Coronary artery vasodilator

59
Q

Dobutamine
Effects when:
<5 mcg/kg/min
>5 mcg/kg/min

A

<5: b1 selective, weak activity at SA node

>5: weak alpha 1 stim

60
Q

Ephedrine
Agonist where
Routes

A

Indirect and direct at alpha and beta

PO, IM, IV

61
Q

Ephedrine
Use in anesthesia
Dose

A

Correct hypotension, inc HR also

10-25 mg IV, 10-50 mg IM

62
Q

Ephedrine

Why it isn’t truly a weak epi

A

Lasts 10x longer

63
Q

Ephedrine

___ with repeat dosing and implic

A

Tachyphylaxis (NE depletion). Occupies receptor long 1/2 life, cv compensation

64
Q

Ephedrine

Excretion, metabolism, E 1/2

A

Unchanged in urine (40%)
Slow metab by MAO and conjugated in liver
3 hrs

65
Q

Phenylephrine
Stim what receptor, acting
Constriction

A

A1 primarily, mostly direct acting

Venous more than arterial

66
Q

Phenylephrine
Comparison to NE
Use in anesthesia

A

Less potent, lasts longer

Correct BP, decreases HR

67
Q

Phenylephrine
Dose
CV effects

A

50-200 mcg IV, 20-50 mcg./min gtt

Inc MAP, SBP, DBP, SVR. Decreases HR and CO

68
Q

What you give if OD of:
Phenylephrine
Epi

A

Phenylephrine- vasodilator. NOT BB (A1 issue)

Epi- vasodilator/nipride, then BB after (NOT BB first)

69
Q

B2 agonist overview
Relaxes: 2
Duration of action, why

A

Bronchioles smooth muscle, uterine smooth muscle

Long bc different placement of hydroxyl groups on benzene ring

70
Q

B2 agonist
Routes
Useful in which popn

A

PO, inhalation, SQ, IV

Premature labor, asthma, COPD

71
Q

B2 agonist

SE

A 
Tremor (B2 skel muscle) 
Reflex tachycardia (vasodilation and B2 in heart)
72
Q

Albuterol
Prototype for:
Preferred for what

A

Selective B2 agonist

Bronchospasm d/t asthma

73
Q

Albuterol
MDI dosing
Neb dose for life threat
Can cause what

A

100 mcg/puff. 2 puffs q4-6h, max 16-20 puffs
15 mg/hr for 2 hrs
Tachycardia and hypokalemia in large doses

74
Q

Terbutaline
Agonist where
Routes, dose
Indic

A

B2
Oral, SC (0.25 mg), IV or puffs
Asthma or premature labor

75
Q 
Salmetrol 
Route 
Duration 
Sim to 
Receptor
A

MDI, >12h, albuterol

B2 agonist

76
Q

Ritordine
Receptors, fx
Tx of
Can cause what

A

B2, some B1 (inc hr and CO), for premature labor

Pulm edema d/t dec excretion of Na/K/water

77
Q

What midodrine is, tx for what

A

Direct acting, non catecholamine, A1 agonist

For postural hypotension

78
Q

3 drugs direct sympatho, non catechol, A1 agonist, indic

A

Oxymetazoline, tetrahyudrozaline, xylometazoline

Nasal and ocular decongestants

79
Q

What clonidine is
What dexmedetomidine is
What methyldopa is

A

Colon- partial A2 selective agonist
D- full A2 selective agonist
M- A2 selective agonist

80
Q

A2 selective agonists

Effects

A

Decreased SNS output from CNS. Decreases bp. Sedation and analgesia

81
Q

Amphetamine
Classification
Effects

A

Indirect acting sympathomimetic
Inc release of NE, 5HT, and dopamine
Blocks reuptake and vesicular transport, inhib MAO

82
Q

Methamphetamine
Classification
Comparison to amphetamine

A

Indirect acting sympathomimetic

Higher CNS effects

83
Q

Ritalin, cylert, and amphetamine variants classification

A

Indirect acting sympathomimetic

84
Q

Reserpine
Classification
Effects

A

Inhib catecholamine storage/reuptake
Vesicles lose ability to store NE, 5HT, and dopamine
MAO breaks down excess exc high doses.
Hypotension and depression

85
Q

Cocaine
Classification
Action

A

Inhib catecholamine storage and reuptake (NE, DA, 5HT)

Interferes w catecholamine transport

Pharmacology (19 decks)

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