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SRNAPharmacology I > EXAM 3 Alpha-Beta adrenergic BLOCKERS > Flashcards

EXAM 3 Alpha-Beta adrenergic BLOCKERS Flashcards

1
Q

Alpha adrenergic receptor antagonists

A

Blocking selectively alpha adrenergic receptors and block endogenous catecholamines or other sympathomimetic from stimulating alpha

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2
Q

2 classifications: Alpha adrenergic receptor antagonists

A

non selective antagonist

Selective antagonist

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3
Q

Non-selective alpha1 and alpha 2 drugs (2)

Which one is IV / PO?

A

Phentolamine (IV)

Phenoxybenzamine (PO)

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4
Q

Alpha adrenergic receptor BLOCKADE

A

Inhibits endogenous catecholamines or sympathomimetic amine induced vasoconstriction resulting in vasodilation in arteries and veins

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5
Q

Most alpha 1 antagonists: BARORECEPTOR mediated reflex response

A

the decrease in BP pressure is opposed by baroreceptor reflexes that cause an Increase in HR (reflex tachycardia cardia and increase CO and fluid retention)

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6
Q

The action of reflexes are exaggerated when?

A

Reflexes are exaggerated if the antagonists also blocks alpha 2 receptors (the drug both alpha 1 and alpha 2 receptors) on peripheral sympathetic nerve endings, since antagonizing alpha 2 receptors leads to enhanced released of NE and increased stimulation of post synaptic beta-1 receptors in the heart and kidney

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7
Q

Alpha 1 receptors antagonist COMBINED with sympathomimetics

A

Blockade of alpha 1 receptors inhibits vasoconstriction and the increased in BP produced by the administration of sympatomimetic amines.

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8
Q

Alpha 1 receptors antagonist COMBINED with sympathomimetics

A

Blockade of alpha 1 receptors inhibits vasoconstriction and the increased in BP produced by the administration of sympathomimetic amines.

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9
Q

Phenylephrine + Alpha 1 Blocks combined –>

A

Pressure response completed suppressed.

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10
Q

Norepinephrine + Alpha 1 blocker combined–>

A

Causes maximal cardiac stimulation and pressor response is only incompletely BLOCKED because of residual stimulation of cardiac B1 receptors by NE

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11
Q

Epinephrine and Alpha 1 blocker combined –>

A

Pressor response may be transformed to vasoDEPRESSOR effects (dec BP ) because of residual stimulation of B2 receptors in the vasculature with resultant vasodilation by epinephrine.

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12
Q

Non CV effects of alpha adrenergic receptor antagonists

men HIGH impotence

A

Prevent inhibition of insulin (leading to Increase insulin levels)
Promote Increased GI motility
Prevents Ejaculation and cause IMPOTENCE

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13
Q

Non-SELECTIVE Alpha antagonists: PHENTOLAMINE

A

nonselective competitive REVERSIBLE, alpha adrenergic antagonists (post-synaptic alpha 1 and pre-synaptic alpha 2)

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14
Q

Main effects of Phentolamine:

A

Peripheral vasodilation

Decrease in systemic BP with 2 minutes last 10-15 minutes

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15
Q

IV phentolamine causes

A

TACHYCARDIA

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16
Q

With IV Phentolamine

A

Cardiac stimulation accentuated by enhanced release of NE from cardiac sympathetic nerves due to ANTAGONISM of presynaptic alpha 2 receptors which results in increase HR and Co.

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17
Q

Primarily metabolized in the

Excretion

A

Liver

Unchanged in the urine.

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18
Q

Main adverse effects of PHentolamine

A

Hypotension

***TACHYCARDIA

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19
Q

Extreme caution in (use of PHENTOLAMINE)

A

Coronary artery disease
MI
Tachyarrhythmias
active MI

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20
Q

PHENTOLAMINE CLINICAL USES

A

prevention or treatment of ACUTE HYPERTENSIVE EMERGENCIES due to pheochromocytoma and ANS HYPER-REFLEXIA.

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21
Q

You should ALWAYS have in the OR for patients with PHEOCHROMOCYTOMA

A

PHENTOLAMINE

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22
Q

PHENTOLAMINE for pheochromocytoma

A

Reduces huge amount of catecholamines

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23
Q

PhenoxyBENZAMINE class and action

A

non-selective alpha adrenergic antagonists
act by COVALENTLY to alpha 1 & alpha2 adrenergic receptors producing IRREVERSIBLE and INSURMOUNTABLE alpha receptor inhibition.

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24
Q

With phenix benzamine once alpha blockade has been estamebils

A

even massive doses of sympathomimetic are INEFFECTIVE until effect terminated by metabolism

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25
Q

PHENOXYBENZAMIE route and duration of action.

A

Only ORAL

Long acting

26
Q

Does exactly same thing as PHENTOLAMINE

A

PHENOXYBENZAMINE

27
Q

**Most common side effects CV for phenoxybenzamine

A
  • *HYPOTENSION

* **orthostatic hypotension

28
Q

PHENOXYBENZAMINE and baby

A

Does cross placenta

29
Q

Non cardiac effects

A

Same as phentolamine

30
Q

*****WARNINGS : PHENOXYBENZAMINE FDA

A

Phenoxybenzamine-induced alpha adrenergic blockade
Leave beta adrenergic receptors UNOPPOSED
Administration of agonists that stimulates both types of adrenergic receptors may, therefore, PRODUCE AN EXAGGERATED HYPOTENSIVE RESPONSE (Beta 2) and TACHYCARDIA (Beta 1)

31
Q

PHENOXYBENZAMINE; clinical uses for anesthesia

A

Pre-op TO CONTROL BP and Sweating inpatient with pheochromocytoma
start 1-3 weeks prior to surgery

32
Q

NEVER, never OPERATE on

A

A pheochromocytoma patient if they have not had adequate ALPHA BLOCKADE FIRST, if you give BETA Blockers, BP will INCREASE

33
Q

**KNOW YOHIMBINE MECHANISM Of ACTION

A

Selective, COMPETITIVE ALPHA-2 ADRENERGIC antagonists

34
Q

• Selective α1 adrenergic antagonists are _______, _______ that inhibit All 3 subtypes of postsynaptic

A

competitive , reversible antagonists that inhibit ALL 3 subtypes of postsynaptic α1 receptors (α1a & α1b & α1d).

35
Q

Does selective alpha 1 adrenergic antagonists affect the alpha 2 receptors on the NE release.

A

These agents leave intact the inhibiting effects of the α2 receptors on NE release from nerve endings

36
Q

Current selective alpha 1 adrenergic blockers

A

Prazosin (minipress)
Terazosin (Hytrin)
Doxazosin (Cardura)
Alfuzosin (Uroxatral)

37
Q

Alpha 1 antagonists use in 2 conditions

A

HTN

BPH

38
Q

Phenoxybenzamine used in

A

Pheochromocytoma

39
Q

Antagonists of Post synaptic alpha 1 receptors results in

A

Antagonism of postsynaptic α1 receptors produces vasodilation of arterioles and veins resulting in↓ SVR which ↓ afterload and ↓ blood pressure • ↓ venous return = ↓ preload, can ↓ CO (slight decrease)
• Greater vasodilation at veins when compared to arteries

40
Q

Does the decrease in SVT seen with antagonism of post synaptic alpha 1 receptors cause reflex tachycardia or increase in renin activity?
Which agents are less likely to evoke baroreceptor-mediated increase in SNS activity? Why? is there a big change in HR?

A

do not cause reflex tachycardia OR increases in renin activity
These agents are less likely than nonselective alpha blockers to evoke baroreceptor-mediated increase in SNS activity causing reflex tachycardia.
 Due to a combination of these agents decreasing preload and they do not increase the release of NE since they do not antagonize α2 receptors; this results in minimal change in HR

41
Q

Selective alpha 1 adrenergic antagonists inhibits

A

alpha 1 receptors found smooth muscle in the bladder base, bladder neck, prostatic neck, prostatic

42
Q

Results of antagonism of alpha 1 in prostate and bladder

A

smooth muscle relaxation of the prostate and bladder neck , which decreases pressure in the bladder and urethra and improves urinary flow and BPH symptoms.

43
Q

Most common side effects of alpha 1 antagonists

A

Dizziness

Headache

44
Q

The first dose effect of alpha 1 antagonists is

A

orthostatic hypotension

45
Q

the administration of usual dose of an alpha 1 agonists such as Phenylephrine may not

A

produce the desired effect in patients on a selective alpha 2 antagonist agent

46
Q

Selective Alpha 1A Adrenergic Receptor Antagonists

A

Tamsulosin (Flomax)

Silodosin (RAPAFLOW)

47
Q

Tamsulosin and Silodosin are both

A

selective, competitive postsynaptic alpha 1 antagonists.

48
Q

Tamsulosin and silodosin

A

Improve urinary blood flow

Reduced BPH symptoms without causing peripheral vascular smooth muscle relaxation

49
Q

Tamsulosin and Silodosin side effects?

A

Headaches
Dizziness
Nasal congestion/rhinitis

50
Q

Beta Adrenergic Receptor Antagonists (Beta Blockers)

A

selectively , reversibly, and competitively to beta adrenergic receptors and INHIBIT Cathecholamines or OTHER SYMPATHOMIMETICS from provoking beta responses.

51
Q

Beta Antagonism leads to

A

Decreased activation of adenylate cyclase which decreases the concentration of cyclic AMP

52
Q

Antagonism of beta blockers is reversible meaning

A

Antagonist drug may be displaced if sufficient amount of AGONIST agent is available.

53
Q

Beta blockers really act as

A

INVERSE AGONIST.

54
Q

Beta Blockers Classification properties

RID MD

A
  1. Relative affinity for beta 1 and beta 2 receptors (beta selectivity)
  2. Intrinsic sympathomimetic Activity (ISA)
  3. Difference in lipid solubility
  4. Membrane-stabilizing effects (local anesthetic activity)
  5. Differences in pharmacokinetic profile (ADME)
55
Q

The classification properties of beta blockers effect both :

A

relative toxicity and clinical effects.

56
Q

2 classification of beta adrenergic antagonists

A

Non-selective beta adrenergic agonists

Selective beta adrenergic agonists.

57
Q

What are the action of non selective beta adrenergic agonists?

A

competitive antagonists at beta 1 and beta 2 and inhibit the chronotropic, inotropic and vasodilator response to beta adrenergic stimulation proportionally

58
Q

Cite the nonselective beta adrenergic agonists?

PNS TLCCP

A 
Propanolol
Nadolol
Sotalol (also a class III anti-arrhythmic)
Timolol
Carvedilol
Labetalol
Carteolol
Pinodolol
59
Q

Cite the selective beta adrenergic agonists?

A 
Metoprolol
Atenolol
Acebutalol
Betaxolol
Esmolol 
Bisoprolol
60
Q

Cardio-selective beta adrenergic

A

competitive, selective antagonists at beta-1 adrenergic

61
Q

Why are cardio-selective agents better?

A

less likely to provoke bronchospasm, vasoconstriction, and alter metabolic effects and SAFER than non selective in patients with asthma, COPD, diabetes and peripheral artery disease

62
Q

MSA means

A

Membrane Stabilizing activity

SRNAPharmacology I (29 decks)

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