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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
Termination of effect of sympathomimetics Catecholamines 4
Reuptake: I (neuronal) II (extraneuronal) | MAO, COMT, lungs
26
Termination of effect | Non catecholamines: 2
MAO, urinary excretion (unchanged)
27
Alpha agonist selectivity Phenylephrine Clonidine
P: A1>A2>>>B C: A2>A1>>>B Both dont effect beta
28
Alpha and beta agonist selectivity Norepi Epi
A1=A2; B1>>>B2 | A1=A2; B1=B2
29
Beta agonist selectivity Dobutamine Isuprel
B1>B2>>>A | B1=B2>>>A
30
Bagonist selectivity | Terbutaline/albuterol
B2>B1>>>A
31
Dopamine agonist selectivity Dopamine Fenoldopam
D1=D2>>B>>A | D1>>D2
32
Epi Most potent activator of what Routes Lipid solubility, implication
Alpha receptors SQ or IV Poorly lipid soluble= little CNS effect
33
Epi Onset SQ vs IV Duration
SQ 5-10 min, IV 1-2 min | 5-10 min
34
Epi Indications 6
Bronchial asthma, acute allergic rxn, cv arrest (asystole), electromechanical dissociation, vfib unresponsive to defibrillation, gtt to increase contractility
35
Epi dosing Standard bolus for resuscitation Can start w what for less severe hypotension Need infusion when
10 mcg/kg IV 2-8 mcg/kg Single bolus dose fx dissipate after 1-5 min
36
Epi dosing | For: beta 1, beta 2, alpha and beta
1-2 mcg/min beta 2 4-5 mcg/min beta 1 10-20 mcg/min alpha and beta
37
Epi stim all ___ | Major role
Adrenoreceptors | BP regulation
38
Epi effects A1 A2
A1- vasoconstriction, inc BP, inc CVP, inc cv work | A2- negative feedback, decreases BP
39
Epi cv effects B1 B2
Increased contractility, HR, CO, inc BP | Peripheral vasodilation- decreases BP
40
Epi CV effects | A1 vs B2 targets
A1- skin, mucosa, hepatic, renal | B2- skeletal muscle
41
Epi With moderate doses, ___ tends to increase, __, ___ DBP tends to ___ ___, __ stays the same
SBP, B1, A1 | Decrease, B2, MAP
42
Epi effects in cerebral, coronary, and pulmonary vasculature
Minimal vasoconstriction of arterioles. | Inc cerebral BF even w/normal BP d/t redistribution of BF
43
Epi Ocular effects Actions of A1, A2, B1
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
Respiratory fx epi B2 A1
B2: dilate smooth muscles of bronchial tree, dec release of vasoactive mediators (histamine) in bronchial vessels A1: decongestion, reduces secretions
45
GI fx epi | A, A1, A2, B
A, B2- decreased peristalsis from smooth muscle relaxation A2- decreased gastric secretions A1- decreased sphlanchnic BF (even if BP normal)
46
``` GU epi fx Renal vasculature (receptors and effects) ```
A1- renal bf reduced even if BP stable | B1- kidney inc renin release
47
GU fx epi | Bladder (receptors and effect)
A1- contracts urethral sphincter, continence | B2- Relaxation, decreases UOP
48
GU fx epi Erectile tissue Uterus (Receptor/fx)
A1 facilitates ejaculation B2- relaxes, inhib labor
49
Metabolic fx epi A2 B2 B3
A2- inhib insulin release (opposed by B2) B2- increased liver glycogenolysis and promotes insulin release B3- Increased adipose tissue lipolysis
50
NE Hypotension dose Potent effects where
4-16 mcg/min | Alpha and beta 1
51
NE | Beta 2 effects
``` 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
Dopamine Precursor of Stim what
NE | All adrenergic receptors inc dopamine
53
Dopamine | Dosing guidelines
1-3 mcg/kg/min D1 3-10 mcg/kg/min B1 >10 mcg/kg/min alpha
54
Dopamine Increases 4 Also inc ___ why its not as useful when
Contractility, GFR, renal BF, UOP | NE, depleted catecholamine stores
55
Dopamine Synergistic w/___ to reduce ___ and improve __ __ Inhibitory at __ __, pts may have alt response to ___ Inc __ pressure
Dobutamine, afterload, CO Carotid bodies, hypoxia Intraocular
56
``` Isoproterenol __ __ and __ agonists Chemical ___ Rapid metab by ___ (need __) Pt at risk: ```
Selective B1 and B2 Pacemaker COMT (gtt) CAD
57
Isoproterenol CV effects Dose for heart block and bradydysrhythmias
Inc hr, contractility, SBP Dec SVR, DBP, MAP 1-5 mcg/min
58
Dobutamine Dose gtt CV effects
2-10 mcg/kg/min Improves CO w/o inc HR or BP (good CHF drug) Coronary artery vasodilator
59
Dobutamine Effects when: <5 mcg/kg/min >5 mcg/kg/min
<5: b1 selective, weak activity at SA node | >5: weak alpha 1 stim
60
Ephedrine Agonist where Routes
Indirect and direct at alpha and beta | PO, IM, IV
61
Ephedrine Use in anesthesia Dose
Correct hypotension, inc HR also | 10-25 mg IV, 10-50 mg IM
62
Ephedrine | Why it isn't truly a weak epi
Lasts 10x longer
63
Ephedrine | ___ with repeat dosing and implic
Tachyphylaxis (NE depletion). Occupies receptor long 1/2 life, cv compensation
64
Ephedrine | Excretion, metabolism, E 1/2
Unchanged in urine (40%) Slow metab by MAO and conjugated in liver 3 hrs
65
Phenylephrine Stim what receptor, acting Constriction
A1 primarily, mostly direct acting | Venous more than arterial
66
Phenylephrine Comparison to NE Use in anesthesia
Less potent, lasts longer | Correct BP, decreases HR
67
Phenylephrine Dose CV effects
50-200 mcg IV, 20-50 mcg./min gtt | Inc MAP, SBP, DBP, SVR. Decreases HR and CO
68
What you give if OD of: Phenylephrine Epi
Phenylephrine- vasodilator. NOT BB (A1 issue) | Epi- vasodilator/nipride, then BB after (NOT BB first)
69
B2 agonist overview Relaxes: 2 Duration of action, why
Bronchioles smooth muscle, uterine smooth muscle | Long bc different placement of hydroxyl groups on benzene ring
70
B2 agonist Routes Useful in which popn
PO, inhalation, SQ, IV | Premature labor, asthma, COPD
71
B2 agonist | SE
``` Tremor (B2 skel muscle) Reflex tachycardia (vasodilation and B2 in heart) ```
72
Albuterol Prototype for: Preferred for what
Selective B2 agonist | Bronchospasm d/t asthma
73
Albuterol MDI dosing Neb dose for life threat Can cause what
100 mcg/puff. 2 puffs q4-6h, max 16-20 puffs 15 mg/hr for 2 hrs Tachycardia and hypokalemia in large doses
74
Terbutaline Agonist where Routes, dose Indic
B2 Oral, SC (0.25 mg), IV or puffs Asthma or premature labor
75
``` Salmetrol Route Duration Sim to Receptor ```
MDI, >12h, albuterol | B2 agonist
76
Ritordine Receptors, fx Tx of Can cause what
B2, some B1 (inc hr and CO), for premature labor | Pulm edema d/t dec excretion of Na/K/water
77
What midodrine is, tx for what
Direct acting, non catecholamine, A1 agonist | For postural hypotension
78
3 drugs direct sympatho, non catechol, A1 agonist, indic
Oxymetazoline, tetrahyudrozaline, xylometazoline | Nasal and ocular decongestants
79
What clonidine is What dexmedetomidine is What methyldopa is
Colon- partial A2 selective agonist D- full A2 selective agonist M- A2 selective agonist
80
A2 selective agonists | Effects
Decreased SNS output from CNS. Decreases bp. Sedation and analgesia
81
Amphetamine Classification Effects
Indirect acting sympathomimetic Inc release of NE, 5HT, and dopamine Blocks reuptake and vesicular transport, inhib MAO
82
Methamphetamine Classification Comparison to amphetamine
Indirect acting sympathomimetic | Higher CNS effects
83
Ritalin, cylert, and amphetamine variants classification
Indirect acting sympathomimetic
84
Reserpine Classification Effects
Inhib catecholamine storage/reuptake Vesicles lose ability to store NE, 5HT, and dopamine MAO breaks down excess exc high doses. Hypotension and depression
85
Cocaine Classification Action
Inhib catecholamine storage and reuptake (NE, DA, 5HT) | Interferes w catecholamine transport

Pharmacology (19 decks)

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