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ANS Flashcards

1
Q

Endogenous catecholamines

A

Epinephrine
Norepinephrine
Dopamine

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2
Q

Synthetic catecholamines

A

Isoproterenol

Dobutamine

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3
Q

Synthetic non-catecholamines

A

Indirect acting: Ephedrine, mephentermine, amphetamines

Direct acting: Phenylephrine, Methoxamine

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4
Q

Selective Alpha 2 agonists

A

Clonidine, dexmedetomidine

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5
Q

Selective Beta 2 adrengergic agonists

A

Albuterol, Terbutaline, Ritodrine

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6
Q

All sympathomimetics are ___ ____ derivatives

A

Beta-phenylethylamine derivatives
Amine group (NH2) side chain
Hydroxy group on the 3,4 carbons of benzine ring (catechol)
*this allows COMPT to metabolize them

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7
Q

Termination of effect of sympathomimetics

A 
Catecholamines: 
Reuptake- uptake 1 is neuronal reuptake; uptake II is extraneuronal uptake
MAO
COMPT
LUNGS

Non-Catecholamines: MAO
Urinary excretion (unchanged)
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8
Q

Receptor agonist: Phenylephrine

A

a1 > a2»>b

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9
Q

Receptor agonist: Clonidine

A

a2 >a1&raquo_space;> b

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10
Q

Receptor agonist: Norepinephrine

A

a1=a2; b1»> b2

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11
Q

Receptor agonist: Epinephrine

A

a1=a2; b1= b2

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12
Q

Receptor agonist: Dobutamine

A

b1>b2&raquo_space;>a

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13
Q

Receptor agonist: Isoproterenol

A

b1=b2&raquo_space;>a

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14
Q

Receptor agonist: Terbutaline/Albuterol

A

b2»b1»>a

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15
Q

Receptor agonist: Dopamine

A

D1=D2» b»a

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16
Q

Receptor agonist: Fenoldopam

A

D1» D2

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17
Q

GCPR and effects: Alpha 1

A

Gaq= increased Ca= constriction

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18
Q

GCPR and effects: Alpha 2

A

Gai= decreased CAMP= constriction

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19
Q

GCPR and effects: Betas

A

Gas- adenylate cyclase= increase CAMP= DILATION and increased contractility and HR

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20
Q

Where are B1 found?

A

Heart- Increase force and rate of contraction

Kidneys- stimulate renin release

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21
Q

Where are B2 found?

A

Bronchioles, uterine, vascular, GI, GU- smooth muscle relaxation
Mast cells- Decrease histamine
Skeletal muscles- increase K uptake, dilation, tremor
Liver- glycogenolysis
Pancreas- increase insulin secretion
Adrenergic nerve terminals- increase NE release

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22
Q

Where are A2 found?

A 
Platelets- aggregation
Adrenergive presynaptic- inhibits transmitter release (decrease BP and HR)
Vascular smooth muscle- contraction
GI- relaxation
CNS- sedation and analgesia
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23
Q

Where are Alpha 1 found?

A 
Vascular smooth muscle- contraction
iris- contraction (dilates- mydrasis)
Pilomotor- erects hair
Prostate and uterus- contraction
Heart- Increase force of contraction
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24
Q

Epinephrine

A 
1-2 mcg/min= B2
4-5 mcg/min= B1
10-20 mcg/min= alpha and beta
Onset: 1-2 min IV (5-10 min SQ)
Duration: 5-10 min
*with moderate dosing, SBP increases-B1, A1; DBP decrease- B2; Map stays the same.
25
Effects of Epinephrine
Constricts cerebral, coronary, pulmonary. a1- mydriasis; a1,a2- increase humoral outflow; B1 increase aqueous humor; B2 decreased released of histamine, a1- decongestion; *A1 DECREASED RENAL BLOOD FLOW, B1 INCREASED RENIN RELEASE; a1- contraction of urethral sphincter, B2- relaxtion decreases urinary output. B2- relaxation- inhibits labor. B2- glycogenolysis
26
Levophed
Hypotension 4-16 mcg/min Potent alpha and beta-1 effects (minimal B2) Increased SBP, DBP, MAP (decreased HR baroreceptor response0 Decreased venous return, CO, HR (despite B1 effects)
27
Dopamine
1-3 mcg/kg/min= Dopamine 1 3-10 mcg/kg/min- Beta 1 >10 mcg/kg/min- alpha Synergistic with dobutamine to reduce afterload and improve CO (used in heart failure)
28
Isoproterenol
Equal B1 and B2; increases HR and contractility with decreased SVR. Inc SBP, decreased DBP, decreased MAP. 1-5 mcg/min for heart block and bradydysrythmias *rapid COMPT, need infusion
29
Dobutamine
2-10 mcg/kg/min 5mcg/kg/min = A1 Improves CO without increasing HR or BP (good for CHF) *coronary artery vasodilator
30
Ephedrine
Indirect and direct at alpha and beta 10-25 mg; 10-50 mg IM *excreted unchanged in the urine (40%) slowly metabolized by MAO
31
Phenylephrine
50-200 mcg IV or 20-50 mcg/min infusion Increase MAP, SBP, DBP, SVR, decrease HR and CO A1 Venoconstriction > arterial constriction
32
Albuterol
Selective B2 Preferred choice for bronchospasm MDI 100 mcg/puff; 2 puffs q4-6 hours; max 16-20 puffs
33
Other B2 Agonists
Albuterol Terbutaline- oral, SC or puffs or IV. (for asthma or premature labor) Salmeterol- doa >12 hours Ritordine- treatment of premature labor (some B1 effects can increase HR and CO, can cause pulmonary edema)
34
Direct acting sympathomimetics, non catecholamines
A1 agonists: Midodrine, Oxymetazoline A2 agonists: Clonidine (partial), Dexmedextomidine (full), Methyldopa
35
Indirect-acting sympathomimetics
Amphetamine, methamphetamine, methylphenidate (Ritalin), Cylert, ADHD meds
36
Inhibitors of catecholamine storage and reuptake
Reserpine- vesicles don't store norepi, 5ht, dopamine | Cocaine- prevents reuptake of catecholamines
37
Alpha agonists
A1 >>>A2: Prazosin, terazosin, doxazosin A2= A1: Phentolamine A2>>A1: Yohimbine, Tolazoline
38
Mixed Alpha and B antagonists
B1=B2 > A1 > A2 | Labetalol, carvedilol
39
Beta Antagonists
B1 >>> B2: Metoprolol, atenolol, esmolol B1= B2: Propranolol, Nadolol, Timolol B2 >>> B1
40
Phentolamine
Nonselective; for hypertensive emergencies 30-70 mcg/kg IV Onset 2 minutes Local infiltration: 2.5-5.0 mg in 10 ml
41
Phenoxybenzamine
Binds covalentely, Alpha 1> Alpha 2
42
Selective alpha 1 blocker
Prazosin, less reflexive tachycardia (pheochromocytoma)
43
Alpha 2 blocker
Yohimibine, increases release of norepi from post-synaptic neuron; orthostatic hypotension and impotence
44
Alpha antagonists for BPH
Terazosin and Tamsulosin- long active alpha 1 blocker
45
Beta adrenergic receptor antagonists specificity
Non selective B1 and B2: Propranolol, nadalol, timolol, pindolol Cardioselective: metoprolol, atenolol, acebutolol, betaxolol, esmolol
46
Propranolol
``` Non- selective. 90-95% first pass. 0.05mg/kg IV or 1-10 mg 90-95% protein bound Metabolized in liver. E1/2T 2-3 hours Decreased clearance of amide LA Decreases pulmonary first pass effect of fentanyl ```
47
Beta adrenergic receptor antagonists your patients might be taking?
Timolol- non selective treats glaucoma | Nadolol- E1/2T 20-40hrs take 1x daily
48
Metoprolol
``` Selective beta 1 blocker. Prevents ionotropy and chronotropy 60% first pass effect PO: 50-400 mg IV: 1-15 mg E1/2t 3-4 hours ```
49
Atenolol
Most selective beta 1 antagonist E1/2T: 6-7 hrs Not metabolized in liver, lengthened in renal disease Useful in cardiac patients with CAD
50
Betaxolol
Cardioselective B1 E1/2 is 11-22 hrs single dose daily for HTN, topical for glaucoma, good choice for asthmatics, less bronchospasm than timolol
51
Esmolol
``` Selective B1, rapid, short acting 0.5 mg/kg IV (10-180 IV) DOA <15 mins E1/2T 9 minutes, rapidly hydrolyzed by plasma esterases (no effect on sux metabolism) Affects HR without decreasing BP ```
52
Labetalol
``` Combined Alpha and Beta. Beta to Alpha: 7:1 E1/2T 58 hours, prolonged in liver disease Max drop seen in BP 5-10 min after Dose 0.1-0.5 mg/kg *5mg at a time in OR ```
53
Atropine
0.2-0.4 mg IV (preop) 0.4-1.0 mg IV (bradycardia) 2mg in 5ml NS via neb (bronchodilation) Onset 1 minute DOA: 30-60 min E1/2T 1.25 hours 80% unchanged via urine
54
IV Glycopyrrolate
``` 0.1-0.2 mg IV (pre-op and bradycardia) Onset of 2-3 mins DOA: 30-60mins E1/2T: 1.25 hours 80% unchanged via urine ```
55
Scopolamine
0.3-0.5 or 5mcg/kg IM (preop) 1.5 transdermal (5mcg/hr x72 hours for nausea) extensively metabolized with 1% excreted in urine
56
Ipratropium
MDI- 40-80 mcg 2 puffs 0.25-0.5 via nebulizer onset 30-90 minutes Consider in asthmatics, COPD, smokers prior to airway instrumentation
57
Physostigmine
treatment for central anticholinergic syndrome | 15-60 mcg/kg IV repeated as needed q1-2 hours
58
Muscarinic antagonists: Bronchodilators Non-specific M-rec M3 specific
Bronchodilators: Atrovent, Spiriva Nonspecific M: Ditropan, Detrol (for overactive bladder) M3: Enablex, Vesicare (overactive bladder)

Pharmacology (9 decks)

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