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SRNAPharmacology I > Selective Alpha adrenergic Receptor Agonist > Flashcards

Selective Alpha adrenergic Receptor Agonist Flashcards

1
Q

Selective alpha 1 antagonists

A

competivive
reversitbel, ALL 3 subtyps (Alpha1a, alpha 1b, alpha 1d)
NO ALPHA 2 ANTAGONIST

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2
Q

Primary use of alpha 1 adrenergic

What is an alternative to Phenoxybenzamine?

A

Used for BPH

Prazosin as an ALTERNATIVE to phenoxybenxamine

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3
Q

Seleactive Alpha adrenergic receptor CV

A

Greater vasodilation at veins and arteries

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4
Q

Selective alpha 1 adrenergic found where?

A

found in bladder

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5
Q

Adverse effects

A

Orthostatic hypotension, fluid retention, vertigo, syncope and nasal congestion

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6
Q

The administration of usual doses of

A

an alpha 1 agonists such as phenylephrine may not produce the desired effect in patients , MAY HAVE TO GIVE SLIGHLY MORE MEDS

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7
Q

Selective ALPHA 1 A receptor antagonists

A

Tamsulosin, Silodosin
Both selective, competitive post synaptic alpha 1 a antagonists
Alpha 1 a : BLADDER and PROSTATIC TISSUE

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8
Q

Mechanism of action

A

Selectively inhbiti alpha 1a recepotrs found in smooth muscle in the bladder base, bladder necks, prostatic capsule

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9
Q

Beta adrenergic Receptor Antagonists

A

Bind selectively, reversibly and competitively to beta adrenergic recepotrs and INHIBIT catecholamins, and other sympathomimetics –> Decreased adenylate cyclase which decreases the concertation of cAMP

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10
Q

Beta adrenergic antagonist main pharm effect

A

Mechanism of INVERSE AGONIST

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11
Q

More drugs to compete

A

ccompetitive reversible.

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12
Q

Classification of Beta adrenergic

A 
Receptor antagonized
intrinsic sympathomimetic
difference in lipid solubility
Membrane stabilizing effects
Differences in pharmacokinetic profile.
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13
Q

Beta adrenergic receptor antagonists

A

Non selective beta or cardio selective

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14
Q

Non selective beta adrenergic agonists

A

Beta 1 and beta 2
INhibit chrono, ino, and vasodilator responses
Propanolol, nadolol,, sotalol, timolol, carvedilol, labetalol, carteolol, pinolol

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15
Q

Cardio selecte beta 1 ANTAGONISTS

A

Less likely to proDUCE BRONCHOSPASM
vASOCONSTRICITION
AND ALTER METABOLIC EFFECTS

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16
Q

It is imnt to recognize that cardioselectily is dose dependent and beta 1 selectivity is lost whe

A

higher larger doses of these agents are administered and they can inhbiti beta 2 recepots

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17
Q

It is important to recognize that cardioselectily is dose dependent and beta 1 selectivity is lost whe

A

higher larger doses of these agents are administered and they can inhbiti beta 2 recepots

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18
Q

Intrisic Sympathomimetic Activity

A

Can actually have slight AGONIST effect even though it is an antagonists

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19
Q

ISA means

But when endogenous NE is high

A

ISA means that the beta adrenergic antagonist demonstrates a PARTIAL AGONISTS effect at the beta receptor site and will partially activate the beta receptor If the concentration of endogenous NE is LOW, as in resting state.
But when endogenous NE is high, these agents will still be occupying beta receptors and the overall effect will be antagonism of NE effects

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20
Q

ISA agents cause less direct myocardial depression and result in

A

less bradycardia than agents that do not have ISA

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21
Q

Bottom line for the anesthesia providers: ISA

A

DONT USE THEM IN PATIENT UNLESS YOU HAVE TO

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22
Q

Beta adrenergic antagonists that have ISA are to be used in

A

Extreme caution with HR diseases.

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23
Q

Lipid solubility

A

Beta blocker high , mod, or high lipophilicity

High cross BB, decrease SNS outflow by antagonizing beta receptors.

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24
Q

Post op propranolol

A

Lethargy

Vivid dreams

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25
Q

The highest lipid soluble beta blocker is

A

PROPANOLOL

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26
Q

MSA (not releveant at normal doses ONLY IN

A

TOXICITY
Membrane Stabilizing activity
Can inhibit fast Na channels in the heart
Quinidine 1a antiarrythymic agents

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27
Q

MSA meds

A 
Propanolol
Acebutolol
Carvedilol
Metoproplol
Pindolol
Labetalol
Nebidolol
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28
Q

Elmination of esmolol

A

Esterases in Cytosol of RBCs

Half life 9 minutes.

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29
Q

Know nonselective or CARDIOSELECTIve agents

A

BOLD : drugs, know ISA< MSA

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30
Q

Beta blocker uses : TAPIE

A 
Essential HTN
ACS
Tachyarrythmia
Intra op HTN
Preventative to prevent negative outcomes
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31
Q

Anesthesia purpose use of Beta Blockers

A

Prevention of excessive SNS activity with
Direct laryngeal and tracheal intubation
Hypertrophic obstructive cardiomyopathies
Hyperthyroidism
Cyanotic
baroreceptor reflex
anxiety and panic attacks

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32
Q

*****PERIOPERATIVE USE OF Beta BLOCKERS

A 
Patients are 
Risk for Myocardia ischemia (or previous MI) 
Known CAD
Diabetic
LVH
Positive PRE-OP stress test
At risk for MI, from a certain surgeries

The general goal is a resting HR between 65-80 per minute
Avoid using beta adrenergic receptor antagonist that POSSES INTRINCIS sympathomimetic activity for this indication.

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33
Q

Beta Blockers MOA on NODAL ‘
_______automaticity
_________Sinus rate
__________AV nodal conduction velocity
________ Refractory period of the AV node
_________ PR interval
________ chronotrope and dromotropic effects
_________SLOPE OF PHASE 4 SPONTANEOUS DEPOLARIZATION

A

Decrease automaticity
Decrease Sinus rate
Slows AV nodal conduction velocity
Increased Refractory period of the AV node
Lengthens PR interval
Negative chronotrope and dromotropic effects
DECREASE SLOPE OF PHASE 4 SPONTANEOUS DEPOLARIZATION

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34
Q

Beta blockers MOA on Myocytes
___________ phase 2 of the fast action potential
__________ force of contraction in cardiac muscle cells
________ inotrope effects
These agent reset the baroreceptors reflex ___________

A

Decreases phase 2 of the fast action potential
Decrease force of contraction in cardiac muscle cells
Negative inotrope effects
These agent reset the baroreceptors reflex DOWNWARD

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35
Q

Beta blockers on PVR and Afterload?

A

Decrease PVR which will decrease afterload

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36
Q

Cardiac effects of Beta blockers

HR< FOC< CO, PVR, Diastolic filling, myocardial oxygen demand.

A 
Decreased HR
Decreased FOC
Decreased CO
Decreased PVR
Increase DIASTOLIC FILLING time
Decrease myocardial oxygen demand
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37
Q

No beta blockers for patients with

A

AV blocks

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38
Q

Non selective beta adrenergic agonists inhibits

A

VASODILATION of the beta agonists such as ISOPROTERENOL

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39
Q

The cardio stimulating effects of

A

CALCIUM
GLUCAGON
DIGOXIN
are not effected by beta adrenergic antagonists.

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40
Q

Non selective beta adrenergic antagnostis enehcnaeg

A

the pressor response to epinephrine since non selective beta adrenergic antagnosits prevent the beta 2 vasodilating effects of epinephrine and leave UNOPPOSED alpha 1 mediated vasocontasticn which can lead to exaggerated HTN

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41
Q

Beta adredergic receptor antagonisms

A

should only be used after adequate alpha block

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42
Q

PORTAL BLOOD FLOW EFFECTS

A

Non selective antagonists, reduce by producing splanchnic vasoconstriction thereby reducing portal blood flow .

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43
Q

Portal HTN

A

Reduces the flow, decrease the pressure

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44
Q

Portal HTN beta blocks user

A

propranolol
Nadolol
Carvedilol

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45
Q

Non-cardiac effects of beta adrenergic

A

Beta 2 agonism can lead to bronchoconstriction and increased airway resistance
uSE BETA BLOCKERS WITH bronchospactic effects

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46
Q

Metabolims of

A

Modify the metabolism of carbohydrate and lipids

Decreased with Glycogenolysis and pancreatic glucagon stimulation can occur, primarily via beta 2 blockadge.

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47
Q

Beta blockers and blood sugar

A

Type I diabetic patients : mask hypoglycemia

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48
Q

FOr anesthesia, patients with diabetes

A

ALWAYS give Beta 1 selective antagonists.

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49
Q

ALl beta blockers can interfere

A

with the counterregulartory effects of catecholamins that are secreted during hypogleycemina by blunting the pereception of tachycardia, tremor and nervousness.

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50
Q

Tachycardia is

A

an important warning sign fof HYPOGLYCMEIA is BLUNTED AND MASKED BY beta adrenergic antagnoists.

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51
Q

Beta blockers may mask

A

HYPOGLYCEMIA.

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52
Q

______Effects may occur between beta antagnoists and drugs used during anesthesia

A

Additive

53
Q

Beta Blockers contraindications (ABSOLUTE)

A 
Sinus bradycardia
2nd and 3rd degree HB
Cardiogenic shock
Decompensated HF
Sick Sinus syndrome. 
Non selective beta blockers are contraidncated in bronchial asthma/bronchospatic disease.
54
Q

Beta Blockers contraindications (ABSOLUTE)

A 
Sinus bradycardia
2nd and 3rd degree HB
Cardiogenic shock
Decompensated HF
Sick Sinus syndrome.

Non selective beta blockers are contraindicated in bronchial asthma/bronchospatic disease.
Cardio-selective beta blockers may be use in asthma and are the preferred beta blockers in these patient should be used with caution.

55
Q

Cardioselective

A

PVD, diabetes, used cardioselective

56
Q

Myocardial depression produced by INHALED or INJECTED scould be

A

Additive, with depression caused by beta blockers is usually excessive.

57
Q

****Additive cardiovascular effects with inhaled anesthetics when patients on beta blockers

A

***ENFLURANE, very high risk
INtermediatRISK e with HALOTHANE
ISOFLURANE< SEVOFLURANE< DESFLURANE low

58
Q

Avoid ketamine always

A

stimulate the SNS and promotes an increase in SVR and afterload.

59
Q

Non-dypyrimides beta blockers

A

CCB with Beta blockers, can be given with caution.

60
Q

Clinical manifestation of poisoning are dependent on:

A

ISA,
MSA
degree of beta 1 and beta 2 agonistsm

61
Q

Beta adrenergic antagonists with MSA may cause

A

QRS prolongation (quinidine like effects)

62
Q

Treatment of Beta BLOCKERS

A

IV fluids
Glucagon 2-10mg IVP followed by 5mg/hr

ATropine (DOESN’T WORK)
Calcium chloride 1-2 gm
Catecholamines

63
Q

Specific for ANESTHESIA

A

The elimination 1/2 is considered in the periop period when redosing intervals are being developed or when conversion to another beta receptor antagonists is planned
Propanolol, METOPROLOL< LABETALOL, ESMOLOL are particularly useful in anesthetic practice because they are widely available in IV formulation.

64
Q

Propanolol

A

non selective beta blocker lacks ISA
Prototype drug
IV and oral (absorbed completely) 25 % reachest systemic circulation

65
Q

There is a great inter-individual varation

A

Propanolol

66
Q

Several CYP 450 enzymes metabolism

A

Hepatic metabolism of propanolol

67
Q

Metaboism depenednet of PROPANOLOL

A

HEPATIC BLOOD FLOW

68
Q

active metabolite of propanolol

A

4-hydroxypropanolol

69
Q

Elimination t 1/propranolol

A

2-5 hours

70
Q

Propanolol is

A

Highly protein bound

No adjustments for renal dysfunction

71
Q

Propanolol ONSET OF ACTION

A

IV 0.25- 5mg IV

72
Q

Propanolol Anesthesia interaction

A

propranolol decreases the clearance of AMIDE local anesthetics by decreasing hepatic blood flow and inhibiting metabolism in the liver.
The toxicities of agens such as bupivacaine and lidocaine are increased by propranolol

73
Q

Propanolol anesthesia interaction

A

Pulmonary first pass uptake of fentanyl is substantially decreased in patients chronically treated with propranolol, as a result 2-4 times as much fentanyl

74
Q

Nadolol is a non

A

SHORT DISCUSSION

75
Q

Timolol

A

Main Beta blocker in eye gtt

76
Q

Timolol

A

Main Beta blocker in eye gtt

Side effects: Bradycardia and hypotension

77
Q

CARDIOSELECTIVE

A

Metoprolol
Selective inhibitor of beta 1 adrenergic recepotrs
LACKS ISA, and has MSA

78
Q

CARDIOSELECTIVE

Prototype

A

Metoprolol
Selective inhibitor of beta 1 adrenergic receptors, competitively block beta 1 and prevent inotropic and chronotropic responses
LACKS ISA, and has MSA (only at doses much greater than required for beta blocker)

79
Q

Metoprolol is a

A

Beta 1 selectivity of metoprolol is dose related, such that beta 1 selectivity is lost at high doses

80
Q

Metoprolol dosage form

A

IV , PO
Duration 5-8
peak IV effect : 20 minutes.
Typical IV dose of peri-operative area 1-5mg

81
Q

Metoprolol dosage form:

A 
IV , PO
Duration 5-8 (high variable)
peak IV effect : 20 minutes.
Typical IV dose of peri-operative area 1-5mg 
LOW PROTEIN BINDING
82
Q

Atenolol (TENORMIN)
comment on ISA, MSA, Lipophillix vs/ Hydrophillic

What does the administration of atenolol help?
Kidney dose adjustment?

A

TEST on boards
Cardioselective, no ISA< NO MSA, low lipophilicity, very hydrophilic.
Periop administration of atenolol in patients at risk for CAD decrease the incidence of post op MI

Prolonged effect –> only one dosing required.
Dose adjustment for kidney patients

83
Q

With metoprolol, what remains intact?

A

Bronchodilator
Vasodilator
metabolic effects of beta 2 receptors remain intact since it’s cardio selective

84
Q

With beta blockers what is lost at higher doses?

A

Beta 1 selectivity of metoprolol is dose related and beta 1 selectivity is lost at high/large doses.

85
Q

Esmolol

A

Rapid onset, short duration, no significant ISA or MSA at therapeutic dosages and is a low lipiphillic agent

86
Q

*****know ESMOLOL doses (SVT doses)

A

0.5mg/kg IV over 1 min f/b 50mcg/kg/min for 4 minutes

87
Q

If after initial 5 minute infusion your response is inadequate

A

give a 2nd 0.5mg/kg over 1 minu, then increase drip to 100mcg/kg/min max drip is 200mcg/kg/min

88
Q

For esmolol give a maximum up to

A

3 loading doses

89
Q

Loading dose always equals ______over ____min for esmolol

A

0.5/kg ; 1 min

90
Q

Intra-OP POST OP tachycardia use of Esmolol for immediate control

A

For intraop tx of tachycardia and HTN
1mg/kg bolus dose over 30 seconds f/b 150mcg/kg/min
infusion, if necessary.
Adjust the infusion rate as required up to a max of 200mcg/kg/min for tachy tx and 300mcg/kg/min for HTN tx

91
Q

Intra-OP POST OP tachycardia use of Esmolol for GRADUAL control

A

For post op tx of tachy or hypertension
500mcg/kg IV loading dose over 1 min f/b by a 4 minute infusion @ 50mcg/Kg/min
Reassess

92
Q

Esmolol onset of action is _____

A

fast 2-5 minutes

93
Q

Esmolol Duration of action

A

when infusion stop, within 10-30 minutes, effects of drugs are gone.

94
Q

Esmolol; metabolism of action via

A

ESTERASES in the CYTOSOL of RBCs

(esmolol contains ester linkage is rapidly metabolized by hydrolysis of the ester linkage, chierfly by the esterases in the cytosol of RBCs)

95
Q

Esmolol is lipid soluble?

A

NO

96
Q

Esmolol can be associated with ________ when used in labor and delivery, use with caution

A

Fetal bradycardia; uncommon

97
Q

Elimination half life of esmolol is

A

9 minutes

98
Q

Excretion of esmolol

A

73-88 % appears in urine

99
Q

Most common adverse effects of esmolol

A

Hypotension
Diaphoresis
RARERLY REPORTED WITH Esmolol: bradycardia.

100
Q

In hypovolemic patient, esmolol can

A

attenuate reflex tachycardia and increase the risk of hypotension

101
Q

Drug to drugs anesthesia Esmolol

A

a.Combining esmolol with succinylcholine, duration of succ induce neuromuscular blockade is PROLONGED
b.WIth mivacurium prolonged clinical duration and recovery index of mivacurium
ESMOLOL and propofl significant DECREASES the plasma concentration of Propofol.

102
Q

Esmolol with catecholamines

A

ESMOLOL should NOT be used to control tachycardia in the presence of vasoconstrictive and positive inotropic agents such as dopamine, epi, NE, because the danger of reducing cardiac contractility in the presence of HIGH SVR

103
Q

NEBIVOLOL (oral)

A

Highly CARDIOSLECTIVE beta 1 receptor antagonists that also have ENDOTHELIAL NO-MEDIATED VASODILATION Activity
NO ISA or MSA

104
Q

Combined ALPHA and BETA ADRENERGIC ANTAGNOISTS

A

Both beta blockers and alpha 1 antagonists

105
Q

Labetalol

A

competitive antagoistn, at alpha 1, beta 1 and beta 2
Partial agonists of B2 agonists (Vasodilation)
Affinity for 4 receptors,

106
Q

Labetalol has _____isomers

A

4

107
Q

The ration of B : Alpha 1 blocking potency is

A

3: 1 for oral
7: 1 for IV

108
Q

Labetalol is 1/10th to 1/5th as potent as phentolamine at ________ AND 1/4th to 1/3rd as potent as propranolol at blocking Beta adrenergic receptors

A

ALPHA 2

109
Q

MOA of labetalol (act on 4 receptors)

A

Alpha 1 antagonism–> relaxation of arterial SM and vasodilation causing decrease SVR and BP
Non-selective B2 blockade, decreased HR
B1 blockade decreased BP
it is a PARTIAL AGONIST at Beta 2 recepots, vasodilation

110
Q

Labetalol CV effects

CO, BP, onset, peak, Duration, can you give as continuous?

A 
CO unchanged
Hypotensive action
Onset 2-5 mns 
Peak 5-15 mns
Duration: 2-4 hours
May be given as continuous DONT DO IT
111
Q

Labetalol: pharmacokinetics

A

Undergoas extensive HEPATIC METABOLIMS
t 1/2 prolonged in the liver
Decreased blood flow decrease metabolism
Increase liver blood flow increase metabolism

112
Q

Main route of clearance is

A

Hepatic metabolism

113
Q

Pregnancy induced HTN crisis treated with

A

Labetalol

114
Q

Dose of labetalol for HTN emergencies

A

Labetalol 5-20 mg IV may be repeated EVERY 10-15 MINUTES UNTIL desired effect. GIve time to work .

115
Q

Labetalol use for treatment of

A

Pheochromocytoma also

116
Q

Adverse effects of labetalol

A

Hypotension
Orthostatic hypotension
Bronchospasm
CAUTION with CHF

117
Q

Carvedilol is a

A

competitive antagonists at alpha 1, beta 1 and beta 2

118
Q

Carvedilol

A

antioxidant
and anti-inflammatory
***FOR HF, HfREF
Has MSA< lacks ISA

119
Q

Mnemonic for drugs with MSA and list

A 
PAcMP BLCa
Propranolol
Acebutalol
Metoprolol
Pinodolol
Betaxolol
Labetalol
Carvedilol
120
Q

Mnemonic for drugs with ISA and list

A

La Pin Ace
Labetolol
Pindolol
Acebutalol

121
Q

Mnemonic for drugs with Low Lipophilicity and list

A

BetEsANadSotA

Betaxolol
Esmolol
Acebutalol
nadolol
sotalol
Atenolol
122
Q

Mnemonic for drugs with mod lipophilicity and list

A

BisMetPinTiCarLa

Bisoprolol
metoprolol
pindolol
Timolol
Carvedilol
Labetalol
123
Q

Mnemonic for drugs with High lipophilicity and list

A

Nebi - Pro

124
Q

Drugs with clearance Hepatic 1 then Renal 2

A

BetAcePinTim – Bis (Renal -> hepatic)

Betaxolol
Acebutalol
Pinodolol
Timolol
Bisoprolol
125
Q

Hepatic only clearance drugs

A 
MetNebProLa
metoprolol
Nebidolol
Propranolol
Labetalol
126
Q

Renal only clearance

A

SoCartNaAt

127
Q

Biliary 1 than hepatic only (think BH)

A

CARVEDILOL

128
Q

What is not effected by Beta adrenergic antagonism?

A

the cardio stimulating effects of CDG
Calcium
Digoxin
Glucagon.

SRNAPharmacology I (29 decks)

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