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ANS: Adrenergic Antagonists Flashcards

1
Q

Selectivity

Prazosin, terazosin, doxazosin

A

A1»>A2

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2
Q

Selectivity
Phentolamine
Yohimbine, tolazoline

A

A2= A1

A2»A1

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3
Q

Selectivity

Labetolol and carvedilol

A

B1=B2>A1>A2

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4
Q

Selectivity

Metoprolol, atenolol, esmolol

A

B1»>B2

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5
Q

Selectivity
Propranolol, Nadolol, timolol
Butoxamine

A

B1=B2

B2»B1

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6
Q

A antagonists
CV effects
A1

A

Decreases PVR, lowers BP

Postural hypotension d/t failure of venous vasoconstriction on standing

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7
Q

A antagonists
A2
Cv effects

A

Inc NE release from nerves

Blocks negative feedback mechanism

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8
Q

A antagonists
GU FX
Eye/nose fx

A

Blocks in prostate and bladder cause muscle relaxation and ease micturition
Miosis, nasal congestion increased

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9
Q

Alpha antagonists

Bind __ to __ receptors, interfere w ability of ___ to cause a response

A

Selectively, alpha, catecholamines

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10
Q

Alpha antagonists
Competitive antagonists: 3
Bind covalently/hard to overcome: 1

A

Phentolamine, prazosin, yohimbine

Phenoxybenzamine

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11
Q

Phentolamine
Class
Effects

A

Nonselective alpha blocker

Vasodilation, dec BP, inc HR and CO

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12
Q

Phentolamine
Indic
Dose

A 
Htn emergencies (aut dysreflex or pheochrom) 30-70 mcg/kg IV. Onset 2 min 
Local infilt for extravasation of sympathomimetics. 2.5-5 mg in 10 ml
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13
Q

Phenoxybenzamine
Binding
Activity
Effects

A

Covalently binds
Alpha 1 > alpha 2
Dec SVR and vasodilation

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14
Q

Phenoxybenzamine
Onset, e 1/2t
Indic

A

1 hr onset (prodrug)
Long acting, 24 hrs
Preop for pts w pheochromocytoma, can be used w raynauds

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15
Q

Prazosin
Indic
Action
Less what

A

BP control in pheochromocytoma
Selective A1 blocker (minimal A2)
Less reflexive tachycardia

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16
Q

Yohimbine
Action
Indic

A

Alpha 2 selective blocker. Inc release NE from post-synaptic neuron
Orthostatic hypotension, impotence

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17
Q

Terazosin and tamulosin
Indic
Action

A

BPH. Long acting selective Alpha 1a blocker, prostatic smooth muscle relaxation

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18
Q

Beta adrenergic receptor antagonists

Do what to heart, airway, vessels

A

Prevent sympathomimetics (competitive antagonist) from provoking response. Heart (improve 02 supply and demand). Airway (can provoke bronchospasm), vasoconstriction in skel muscles and PVD symptoms increase

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19
Q

Beta adrenergic receptor antagonists

Action in juxtaglomerular cells and pancreas

A

Prevent sympathomimetic response. Dec renin release which indirectly drops BP. Decreased stim of insulin release by epi/NE at B2 then masked symptoms of hypoglycemia at B1

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20
Q

Beta adrenergic antagonist

MOA

A

Selective binding to beta receptors (inf ino/chronotropy). Competitive and reversible inhibition w/large doses of agonists (will overcome antagonist)

21
Q

Beta adrenergic agonist

Chronic use does what

A

Up regulates number of receptors

22
Q

Beta adrenergic receptor antagonist
Derivatives of what
Substitution of

A

Beta agonist isoproterenol, some sympathomimetic effects

Benzene ring

23
Q 
Beta adrenergic receptor antagonists 
Non selective (which they hit, which 4 drugs)
A

B1 and 2

Propranolol, nadalol, timolol, pindolol

24
Q

Beta adrenergic receptor antagonists
Cardioselective- which b
Which 5
Large dose does what

A

B1. Metoprolol, atenolol, acebutolol, betaxolol, esmolol

Overcomes selectivity

25
Propranolol Action Admin to what
Non selective, lacks sympathomimetic activity (true antagonist) B1=B2. Admin stepwise to goal of 55-60 BPM
26
Propranolol | Cardiac effects
Dec HR, CO, contractility. Prominent fx w/SNS and exercise. Inc PVR and coronary vascular resistance. 02 demand lowered. Na retention d/t renal response to CO drop.
27
Propranolol | Pharmacokinetics
90-95% 1st pass effect (mainly oral dose). 90-95% protein bound. Metab in liver, inc 1/2t in low hepatic BF states
28
Propranolol Dose E 1/2t Decreases clearance of
0.05 mg/kg IV or 1-10 mg, give 1 mg q5min (slow) 2-3 Hrs Amide LAs. Pulm first pass effect of fentanyl
29
Timolol Action Indic
Non selective BB. Eye gtts can drop BP and HR and inc airway resistance Tx glaucoma, dec IOP by decreasing produc of aqueous humor
30
Nadolol Action Metab E 1/2 t
Non selective BB Renal/biliary 20-40 hrs, take 1x/day
31
Metoprolol Action Selectivity
Selective beta 1 blocker Prevents ionotropy and chronotropy Dose related
32
Metoprolol First pass effect % Dose E 1/2t
60%. PO 50-400 mg. IV 1-15 mg. 3-4hrs.
33
Atenolol Action E 1/2t
Most selective B1 antagonist, least CNS effects | 6-7 hrs
34
Atenolol Metabolism, implic Useful for whom
Excreted via renal system, 1/2t inc markedly w renal disease Cardiac pts w CAD
35
Betaxolol Action E 1/2t Indic
Cardioselective B1 blocker. 11-22 hrs. | 1x/day for htn. Topical for glaucoma, less bronchospasm risk than timolol.
36
Esmolol Action DOA
Selective B1 antag. Effects HR without dec BP a lot in small doses Rapid onset and short acting
37
Esmolol Dose DOA
0.5 mg/kg IV (10-180mg IV) 50-300 mcg/kg/min gtt <15 min
38
Esmolol | In doses used it doesn't what
Occupy enough beta receptors to cause negative inotropy
39
Esmolol E 1/2t Metabolism
9 minutes** | Hydrolyzed by plasma esterases. No effects on metab of sux
40
SE BB CV PVD A/W
Dec HR/BP/contractility Exac PVD d/t blocking B2 vasodilation Bronchospasm
41
SE BB Metabolism Skel muscle
Alters carb and fat metab, masks hypoglycemia if tachycardic Distribution extracellular K, inhib K uptake into muscles
42
SE BB Local anesthetics NS GI
May decrease BP w/LA Fatigue and lethargy NVD
43
Relative contraindications to BB: 5
AV block, CV failure, reactive airway disease, DM w/o BS monitoring, hypovolemia
44
Clinical uses of BB | 5
Tx htn, angina, dec mortality post MI/in periop/preop for MI risk pts, suppresses tachyarrhythmias, prevents excessive SNS activity
45
Labetolol | Action
Selective A1 and B1 and 2 blocker. IV beta to alpha 7:1
46
Labetolol Metabolism E 1/2t
Conjugation of glucuronic acid, <5% in urine. | 5-8 hrs. Prolonged in liver disease.
47
Labetolol CV effects Max BP drop when Can cause what
Drop BP, HR, SVR, CO unaffected 5-10 min after IV admin Orthostatic hypotension, bronchospasm, heart block, CHF, bradycardia
48
Labetolol | Dose
0.1-0.5 mg/kg. Usually 5 mg at a time for mild hypertension in OR

Pharmacology (19 decks)

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