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Pharmacology > ANS: Adrenergic Antagonists > Flashcards

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
Q

Propranolol
Action
Admin to what

A

Non selective, lacks sympathomimetic activity (true antagonist)
B1=B2. Admin stepwise to goal of 55-60 BPM

26
Q

Propranolol

Cardiac effects

A

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
Q

Propranolol

Pharmacokinetics

A

90-95% 1st pass effect (mainly oral dose). 90-95% protein bound. Metab in liver, inc 1/2t in low hepatic BF states

28
Q

Propranolol
Dose
E 1/2t
Decreases clearance of

A

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
Q

Timolol
Action
Indic

A

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
Q

Nadolol
Action
Metab
E 1/2 t

A

Non selective BB
Renal/biliary
20-40 hrs, take 1x/day

31
Q

Metoprolol
Action
Selectivity

A

Selective beta 1 blocker
Prevents ionotropy and chronotropy
Dose related

32
Q

Metoprolol
First pass effect %
Dose
E 1/2t

A

60%. PO 50-400 mg. IV 1-15 mg. 3-4hrs.

33
Q

Atenolol
Action
E 1/2t

A

Most selective B1 antagonist, least CNS effects

6-7 hrs

34
Q

Atenolol
Metabolism, implic
Useful for whom

A

Excreted via renal system, 1/2t inc markedly w renal disease
Cardiac pts w CAD

35
Q

Betaxolol
Action
E 1/2t
Indic

A

Cardioselective B1 blocker. 11-22 hrs.

1x/day for htn. Topical for glaucoma, less bronchospasm risk than timolol.

36
Q

Esmolol
Action
DOA

A

Selective B1 antag. Effects HR without dec BP a lot in small doses
Rapid onset and short acting

37
Q

Esmolol
Dose
DOA

A

0.5 mg/kg IV (10-180mg IV)
50-300 mcg/kg/min gtt
<15 min

38
Q

Esmolol

In doses used it doesn’t what

A

Occupy enough beta receptors to cause negative inotropy

39
Q

Esmolol
E 1/2t
Metabolism

A

9 minutes**

Hydrolyzed by plasma esterases. No effects on metab of sux

40
Q

SE BB
CV
PVD
A/W

A

Dec HR/BP/contractility
Exac PVD d/t blocking B2 vasodilation
Bronchospasm

41
Q

SE BB
Metabolism
Skel muscle

A

Alters carb and fat metab, masks hypoglycemia if tachycardic
Distribution extracellular K, inhib K uptake into muscles

42
Q

SE BB
Local anesthetics
NS
GI

A

May decrease BP w/LA
Fatigue and lethargy
NVD

43
Q

Relative contraindications to BB: 5

A

AV block, CV failure, reactive airway disease, DM w/o BS monitoring, hypovolemia

44
Q

Clinical uses of BB

5

A

Tx htn, angina, dec mortality post MI/in periop/preop for MI risk pts, suppresses tachyarrhythmias, prevents excessive SNS activity

45
Q

Labetolol

Action

A

Selective A1 and B1 and 2 blocker. IV beta to alpha 7:1

46
Q

Labetolol
Metabolism
E 1/2t

A

Conjugation of glucuronic acid, <5% in urine.

5-8 hrs. Prolonged in liver disease.

47
Q

Labetolol
CV effects
Max BP drop when
Can cause what

A

Drop BP, HR, SVR, CO unaffected
5-10 min after IV admin
Orthostatic hypotension, bronchospasm, heart block, CHF, bradycardia

48
Q

Labetolol

Dose

A

0.1-0.5 mg/kg. Usually 5 mg at a time for mild hypertension in OR

Pharmacology (19 decks)

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