EXAM 3 Alpha-Beta adrenergic BLOCKERS

Question 1

Alpha adrenergic receptor antagonists

Answer 1

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

Question 2

2 classifications: Alpha adrenergic receptor antagonists

Answer 2

non selective antagonist

Selective antagonist

Question 3

Non-selective alpha1 and alpha 2 drugs (2)

Which one is IV / PO?

Answer 3

Phentolamine (IV)

Phenoxybenzamine (PO)

Question 4

Alpha adrenergic receptor BLOCKADE

Answer 4

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

Question 5

Most alpha 1 antagonists: BARORECEPTOR mediated reflex response

Answer 5

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)

Question 6

The action of reflexes are exaggerated when?

Answer 6

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

Question 7

Alpha 1 receptors antagonist COMBINED with sympathomimetics

Answer 7

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

Question 8

Alpha 1 receptors antagonist COMBINED with sympathomimetics

Answer 8

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

Question 9

Phenylephrine + Alpha 1 Blocks combined –>

Answer 9

Pressure response completed suppressed.

Question 10

Norepinephrine + Alpha 1 blocker combined–>

Answer 10

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

Question 11

Epinephrine and Alpha 1 blocker combined –>

Answer 11

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.

Question 12

Non CV effects of alpha adrenergic receptor antagonists

men HIGH impotence

Answer 12

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

Question 13

Non-SELECTIVE Alpha antagonists: PHENTOLAMINE

Answer 13

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

Question 14

Main effects of Phentolamine:

Answer 14

Peripheral vasodilation

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

Question 15

IV phentolamine causes

Answer 15

TACHYCARDIA

Question 16

With IV Phentolamine

Answer 16

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.

Question 17

Primarily metabolized in the

Excretion

Answer 17

Liver

Unchanged in the urine.

Question 18

Main adverse effects of PHentolamine

Answer 18

Hypotension

***TACHYCARDIA

Question 19

Extreme caution in (use of PHENTOLAMINE)

Answer 19

Coronary artery disease
MI
Tachyarrhythmias
active MI

Question 20

PHENTOLAMINE CLINICAL USES

Answer 20

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

Question 21

You should ALWAYS have in the OR for patients with PHEOCHROMOCYTOMA

Answer 21

PHENTOLAMINE

Question 22

PHENTOLAMINE for pheochromocytoma

Answer 22

Reduces huge amount of catecholamines

Question 23

PhenoxyBENZAMINE class and action

Answer 23

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

Question 24

With phenix benzamine once alpha blockade has been estamebils

Answer 24

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

Question 25

PHENOXYBENZAMIE route and duration of action.

Answer 25

Only ORAL | Long acting

Question 26

Does exactly same thing as PHENTOLAMINE

Answer 26

PHENOXYBENZAMINE

Question 27

****Most common side effects CV for phenoxybenzamine

Answer 27

* *HYPOTENSION | * **orthostatic hypotension

Question 28

PHENOXYBENZAMINE and baby

Answer 28

Does cross placenta

Question 29

Non cardiac effects

Answer 29

Same as phentolamine

Question 30

*****WARNINGS : PHENOXYBENZAMINE FDA

Answer 30

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)

Question 31

PHENOXYBENZAMINE; clinical uses for anesthesia

Answer 31

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

Question 32

NEVER, never OPERATE on

Answer 32

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

Question 33

****KNOW YOHIMBINE MECHANISM Of ACTION

Answer 33

Selective, COMPETITIVE ALPHA-2 ADRENERGIC antagonists

Question 34

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

Answer 34

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

Question 35

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

Answer 35

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

Question 36

Current selective alpha 1 adrenergic blockers

Answer 36

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

Question 37

Alpha 1 antagonists use in 2 conditions

Answer 37

HTN | BPH

Question 38

Phenoxybenzamine used in

Answer 38

Pheochromocytoma

Question 39

Antagonists of Post synaptic alpha 1 receptors results in

Answer 39

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

Question 40

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?

Answer 40

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

Question 41

Selective alpha 1 adrenergic antagonists inhibits

Answer 41

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

Question 42

Results of antagonism of alpha 1 in prostate and bladder

Answer 42

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

Question 43

Most common side effects of alpha 1 antagonists

Answer 43

Dizziness | Headache

Question 44

The first dose effect of alpha 1 antagonists is

Answer 44

orthostatic hypotension

Question 45

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

Answer 45

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

Question 46

Selective Alpha 1A Adrenergic Receptor Antagonists

Answer 46

Tamsulosin (Flomax) | Silodosin (RAPAFLOW)

Question 47

Tamsulosin and Silodosin are both

Answer 47

selective, competitive postsynaptic alpha 1 antagonists.

Question 48

Tamsulosin and silodosin

Answer 48

Improve urinary blood flow | Reduced BPH symptoms without causing peripheral vascular smooth muscle relaxation

Question 49

Tamsulosin and Silodosin side effects?

Answer 49

Headaches Dizziness Nasal congestion/rhinitis

Question 50

Beta Adrenergic Receptor Antagonists (Beta Blockers)

Answer 50

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

Question 51

Beta Antagonism leads to

Answer 51

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

Question 52

Antagonism of beta blockers is reversible meaning

Answer 52

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

Question 53

Beta blockers really act as

Answer 53

INVERSE AGONIST.

Question 54

Beta Blockers Classification properties | RID MD

Answer 54

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)

Question 55

The classification properties of beta blockers effect both :

Answer 55

relative toxicity and clinical effects.

Question 56

2 classification of beta adrenergic antagonists

Answer 56

Non-selective beta adrenergic agonists | Selective beta adrenergic agonists.

Question 57

What are the action of non selective beta adrenergic agonists?

Answer 57

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

Question 58

Cite the nonselective beta adrenergic agonists? | PNS TLCCP

Answer 58

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

Question 59

Cite the selective beta adrenergic agonists?

Answer 59

``` Metoprolol Atenolol Acebutalol Betaxolol Esmolol Bisoprolol ```

Question 60

Cardio-selective beta adrenergic

Answer 60

competitive, selective antagonists at beta-1 adrenergic

Question 61

Why are cardio-selective agents better?

Answer 61

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

Question 62

MSA means

Answer 62

Membrane Stabilizing activity