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Pharmacology > ANS > Flashcards

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
Q

Effects of Epinephrine

A

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
Q

Levophed

A

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
Q

Dopamine

A

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
Q

Isoproterenol

A

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
Q

Dobutamine

A

2-10 mcg/kg/min
5mcg/kg/min = A1
Improves CO without increasing HR or BP (good for CHF)
*coronary artery vasodilator

30
Q

Ephedrine

A

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
Q

Phenylephrine

A

50-200 mcg IV or 20-50 mcg/min infusion
Increase MAP, SBP, DBP, SVR, decrease HR and CO
A1
Venoconstriction > arterial constriction

32
Q

Albuterol

A

Selective B2
Preferred choice for bronchospasm
MDI 100 mcg/puff; 2 puffs q4-6 hours; max 16-20 puffs

33
Q

Other B2 Agonists

A

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
Q

Direct acting sympathomimetics, non catecholamines

A

A1 agonists:
Midodrine, Oxymetazoline
A2 agonists:
Clonidine (partial), Dexmedextomidine (full), Methyldopa

35
Q

Indirect-acting sympathomimetics

A

Amphetamine, methamphetamine, methylphenidate (Ritalin), Cylert, ADHD meds

36
Q

Inhibitors of catecholamine storage and reuptake

A

Reserpine- vesicles don’t store norepi, 5ht, dopamine

Cocaine- prevents reuptake of catecholamines

37
Q

Alpha agonists

A

A1&raquo_space;>A2: Prazosin, terazosin, doxazosin
A2= A1: Phentolamine
A2»A1: Yohimbine, Tolazoline

38
Q

Mixed Alpha and B antagonists

A

B1=B2 > A1 > A2

Labetalol, carvedilol

39
Q

Beta Antagonists

A

B1&raquo_space;> B2: Metoprolol, atenolol, esmolol
B1= B2: Propranolol, Nadolol, Timolol
B2&raquo_space;> B1

40
Q

Phentolamine

A

Nonselective; for hypertensive emergencies
30-70 mcg/kg IV
Onset 2 minutes
Local infiltration: 2.5-5.0 mg in 10 ml

41
Q

Phenoxybenzamine

A

Binds covalentely, Alpha 1> Alpha 2

42
Q

Selective alpha 1 blocker

A

Prazosin, less reflexive tachycardia (pheochromocytoma)

43
Q

Alpha 2 blocker

A

Yohimibine, increases release of norepi from post-synaptic neuron; orthostatic hypotension and impotence

44
Q

Alpha antagonists for BPH

A

Terazosin and Tamsulosin- long active alpha 1 blocker

45
Q

Beta adrenergic receptor antagonists specificity

A

Non selective B1 and B2: Propranolol, nadalol, timolol, pindolol
Cardioselective: metoprolol, atenolol, acebutolol, betaxolol, esmolol

46
Q

Propranolol

A 
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
Q

Beta adrenergic receptor antagonists your patients might be taking?

A

Timolol- non selective treats glaucoma

Nadolol- E1/2T 20-40hrs take 1x daily

48
Q

Metoprolol

A 
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
Q

Atenolol

A

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
Q

Betaxolol

A

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
Q

Esmolol

A 
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
Q

Labetalol

A 
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
Q

Atropine

A

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
Q

IV Glycopyrrolate

A 
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
Q

Scopolamine

A

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
Q

Ipratropium

A

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
Q

Physostigmine

A

treatment for central anticholinergic syndrome

15-60 mcg/kg IV repeated as needed q1-2 hours

58
Q

Muscarinic antagonists:
Bronchodilators
Non-specific M-rec
M3 specific

A

Bronchodilators: Atrovent, Spiriva
Nonspecific M: Ditropan, Detrol (for overactive bladder)
M3: Enablex, Vesicare (overactive bladder)

Pharmacology (9 decks)

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