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SRNAPharmacology II > Anticholinesterase/Chol.Agonist/Sugga COMP > Flashcards

Anticholinesterase/Chol.Agonist/Sugga COMP Flashcards

1
Q

Anticholinesterase Drugs

A

facilitate speed of recovery from skeletal muscle effects produced by NDNMBS

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2
Q

Anticholinesterase drugs are:

A

Edrophonium
Neostigmine
Pyridostigmine

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3
Q

What is the drug that crosses the BBB and is use to produce nonspecific antagonism of the CNS effects or certain drugs and iS NOT IONIZED?

A

PHYSOSTIGMINE

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4
Q

Anticholinesterase drugs use to treat 3 conditions

A

Myasthenia Gravis
Glaucoma
Alzheimer’s

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5
Q

Exelon patch is

A

Neogstimine, may interact with REVERSAL agent (like giving more of a drug)

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6
Q

MOA of anticholinesterases

A

Enzyme inhibition –> Inhibits acetylcholinesterase

Presynaptic effects and direct effects @ NMJ

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7
Q

Anticholinesterase role

A

Rapid hydrolysis of acetylcholine

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8
Q

ACH compete for

A

receptor sites

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9
Q

What is the most efficient enzymes in the body why?

A

Anticholinesterase; One mol hydrolyzes 300000 ate molecules

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10
Q

Neostigmine and pyridostigmine MOA

A

inhibit breakdown of ACH by acting as a substrate for acetylcholinesterase and altering its structure making it LESS EFFECTIVE

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11
Q

Edrophonium MOA ? Long or short acting?

A

Short acting

works by forming a reversible electrostatic attachment to acetylcholinesterase

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12
Q

What is Edrophonium reversal always given with

A

ATROPINE, because of the very fast onset of action, need faster onset of action anticholinergic.

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13
Q

Anticholinesterase drugs are classified according to the mechanism by which they inhibit the activity of cholinesterase. Which ANTICHOLINESTERASE work by IRREVERSIBLE ACTIVATION?
REVERSIBLE ?

A

Organophosphates
Formation of carbamyl esters
Electrostatic binding

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14
Q

Are anticholinesterase drugs lipid soluble?

What happens when acetylcholinesterase is carbamylated?

A

very lipid soluble

carbamylated acetylcholinesterase cannot Hydrolyze Ach

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15
Q

Poisons resemble what kinds of blockade

A

Depolarizing Blockade

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16
Q

Clinical uses of Edrophonium (3)

A

Antagonissm of NDNMS
Diagnosis of assess therapy for Myasthenia Gravis
Evaluated presence of mixed block associated with Such

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17
Q

What are the Anticholinesterase Drugs that work by Formation of carbamyl Esters?

A

Physostigmine
Neostigmine
Pyridostigmine

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18
Q

MOA of Anticholinesterase Drugs that work by Formation of carbamyl Esters? Half life of_____

A

produces reversible inhibition of acetylcholinesterase by formation of carbamyl esters complex
half life of complex 30 mins

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19
Q

How does the Organophophase anticholinesterase work?

What is the Organophosphate poisoning antidote?

A

Form a stable inactive complex that does not undergo Hydrolysis
ATROPINE

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20
Q

After bolus concentration, the plasma concentration of EDROPHONIUM, NEOGSTIMINE, and PYRIDOSTIGMINE peak and decrease ________

A

5-10 mins

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21
Q

What should be given along with Neogstigmine?

A

Glycopyrrolate

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22
Q

Anticholinesterase clearance has much longer half life of these patients?

A

Renal disease

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23
Q

Quarternary compounds are:
Lipid solubility is? What happens at physiologic pH?
Can it penetrate lipid membrane of the GIT and CNS?
What does QUARTERNARY Means?

A

Pyridostigmine, Edrophonium, Neogstimine (PEN)
POOR Lipid soluble, ionized at physiological pH
NO
Nitrogen bonded to 4 molecules
Can’t be used for toxicity

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24
Q

TERTIARY AMINE compounds are
Lipid solubility is? What happens at physiologic pH?
Can it penetrate lipid membrane of the GIT and CNS?
What does TERTIARY Means?
Use to treat anticholinergic agent ?

A

PHYSOSTIGMINE, Antilirium and ORGANOPHOSPHATES
LIPID SOLUBLE, Nonionized at physiologic pH
Penetrate GIT and Crosses BBB
Nitrogen bonded to 3 molecules
USE To treat ANTICHOLINERGIC AGENTS

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25
Q

EDROPHONIUM (Tensilon) onset (rapid intermediate or delayed)

A

1-2 minutes (Rapid)

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26
Q

NEOSTIGMINE onset (fast, intermediate or slow)

A

7-11 minutes (intermediate)

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27
Q

Pyrostigmine onset (fast, intermediate or slow)

A

16 minutes (delayed)

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28
Q

Duration of action of those drugs affected by __________ and ranging from _______ to ____mns

A

affected by rate of disappearance

60-76 minutes

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29
Q

Renal clearance % for neostigmine?
Renal clearance of Pyridostigmine and Edrophonium?
Is clerance affected in renal failure?

A

50%
75%
Yes

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30
Q

Metabolism of Neo, edro and pyridostigmine of hepatic?

A

Hepatic 50 % Neostigmine

30 % of Edrophonium and pyridostigmine

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31
Q

Pharmacological response by these agents reflects_____________At__________causing_________
__________ receptors

A

Accumulation of ach at muscarinic POST synaptic parasympathetic activation; Severe BRADYCARDIA
NICOTINIC
POST synaptic Skeletal Muscle Increased strength desired
Pre synaptic : Inhibition of release of ACH undesired, increased weakness

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32
Q

Parasympathetic activation side effects

A 
Bradycardia may lead to asystole
Salivation
Miosis
Hyperperistalsis
Bronchoconstriction
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33
Q

NECESSARY To give ________simultaneously with this agent?

A

Anticholinergic drug

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34
Q

If you give NEOSTIGMINE and Pyridostigmine then SUCC what happens to SUCCINYLCHOLINE EFFECTS? why?
Which one does NOT Inhibit plasma cholinesterase activity?

A
  • effects of SCH is prolonged because enzymes are inhibited.
  • Because both Neostigmine and Pyridostigmine Produced -MARKED and PROLONGED Inhibition of PLASMA CHOLINESTERASE ACTIVITY
  • EDROPHONIUM
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35
Q

MUSCARINIC Anticholinergic agents effects?
Effects on CV attenuated by giving?
What happens to patient with DENERVATED HEART such as TRANSPLANT PT?
PVR and SVR?

A 
Bradycardia, Escape beats, 
Sinus Arrest
Anticholinergic
ASystole ( Denervated heart--Transplant) 
Decrease SVR, increase PVR
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36
Q

GI effect of Anticholinesterases (increase ach) enhance

A

Gastric fluid and increase GI motility

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37
Q

ETOMIDATE and N2O increase

A

Chance of post op N/V

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38
Q

This agent may treat paralytic ileum or atony of bladder ____

A

Neostigmine.

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39
Q

What is the risk associated with giving ANTICHOLINESTERASE with patients with MYASTHENIA GRAVIS who also received NDNMB?

A

CHOLINERGIC CRISIS

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40
Q

MG Patients are more sensitive to ________ why? and less sensitive to __________

A

Non-depolarizing to block because of down-regulation of receptors. More sensitive to ANTAGONIST (NDNMB) and less sensitive to (agonist)

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41
Q

MYOTONIA with anticholinesterase agent

A

Share some effect of succinylcholine (can produce FASCICULATIONS and AUGMENT Twitch response

42
Q

Use ANTICHOLINESTERASE with caution with patient that have an ABSOLUTE CONTRAINDICATIONS to Succinylcholine, those patients are patients with (4)

A

Myotonia
Muscular dystrophies
Burn patint
Spinal cord transection

43
Q

Clinical uses of the drugs

A 
Antagonized NDNMB drugs
Treat CNS effects of drugs
Treat MG/ Glaucoma
Treat paralytic ileum and atony
Treat Alzheimers
44
Q

Antagonize- Assist REVERSAL of NMB
3 drugs use to reverse NDNMB?
How do they help ?

A

Edrophonium, Neostigmine, and pyridostigmine used to reverse NDNMB
Increase amount of ACH at the nicotinic receptors which is the result of giving these drugs increases the changes of 2 Ach molecule binding to the alpha subunits of the nicotinic receptors.

45
Q

More rapid onset of action with ______
Dose of EDROPHONIUM
DURATION Of ACTION are all

A

EDROPHONIUM
0.5 mg/kg/ IV (1mg/kg if >90% twitch depression when reversal is initiated)
Similar

46
Q

Dose of NEOSTIGMINE
Neostigmine appears to be preferable when
Can be given with either ______or _______why?

A

0.043 mg/kg/IV
>90% twitch depression is to be antagonized?
Atropine or Glycopyrrolate ; because of slower onset of action.

47
Q

Dose of Pyridostigmine

What is expected with Pyridostigmine?

A

0.21 mg/kg/ IV

Initial TACHYCARDIA

48
Q

When EDROPHONIUM is used, which Atropine DOSE is recommended?

A

7 MCG/KG.

49
Q

LESS than the recommended ATROPINE dose CAN CAUSE _______

The dose of atropine is about ______the dose of NEOGstimine. Initial ______Then ____

A

BRADYCARDIA
1/2
Tachy –> brady

50
Q

EXCESSIVE NMB: does additional doses of anticholinesterase drugs further antagonize the block?
When is ventilation indicated then?

A

Once maximally inhibited acetylcholine , giving additional anticholinesteras drugs does not further antagonize the block.
When there is persistent NMB despite large doses of anticholinesterase drugs (NEO >70mcg/kg) , ventilate until NMB wears off , use sedation.

51
Q

Events that influence reversal
EDROPHONIUM Vs NEO which is more EFFECTIVE in reversing deep NMB produced by continous infusion of Atracurium, Vecuronium and Pancuronium?

Inhibited antagonism by ARHH?

A
  1. Intensity of block at time of reversal agent administration
    NEO More effectivee; EDROPHONIUM less effective than NEO in reversing deep NMB produced by continous infusion of Atracurium, Vecuronium and Pancuronium.

Inhibited antagonism by ARHH

  • Aminoglycosides
  • Hyperthermia
  • Resp acidosis associated with PaCO2> 50
  • Hypokalemia and Metabolic acidosis.
52
Q

EPHODRIUM may be more effective for reversal of

A

ATRACURIUM

53
Q

NEOSGTIGMINE may be more effective for reversal of

A

VECURONIUM

54
Q

Hoffman eliminaton dependent

A

pH and temperature dependent

55
Q

HOW TO Avoid Residual paralysis

ADUU

A
  • Avoid long acting (PANCURONIUM)
  • use INTERMEDIATE ACTING
  • USE QUANTITATIVE ObJECTiVE TESTS (TOF <0.9 last twitch)
  • DO NOT use clinical tests *Head life, jaw clenching (unreliable)
56
Q

During anesthetics that do not enhance NMB

A

A minimal of TOF count of 2 should be present before administration of anticholinesterases

57
Q

During anesthetics that DO ENHANCE NMB

A

A TOF count of 4 should be present before administering anti cholinesterase.

58
Q

What should be done if recovery of TOF>0.9 is documented? why?

A

Neostigmine administration should be withheld.

May decrease upper airway muscle activitiy and tidal volume

59
Q

Peripheral Nerve Stimulator (subjective) assessment TOF count of 1 or no TOF response_______
TOF count 2 or 3 ________
TOF with fade (TOF <0.4) _________
TOF no evidence of fade (TOF >0.4)

A
  • Delay reversal
  • administer pharmacologic reversal
  • administer pharmacologic reversal
  • administer pharmacologic reversal consider 20mcg/kg Neogstigmine
60
Q 
Quantitative EVOKED response monitor 
TOF count of 1 or no TOF response\_\_\_\_\_\_\_
TOF count 2 or 3 \_\_\_\_\_\_\_\_
TOF less than <0.4
TOF = 0.40 to .90) \_\_\_\_\_\_\_\_\_
TOF >0.90
A
  • Delay reversal
    -administer pharmacologic reversal
  • administer pharmacologic reversal
  • administer pharmacologic reversal consider 20mcg/kg Neogstigmine
    NO REVERSAL recommended
61
Q

Class of Quarternary ammonium: Example

A

EDROPHONIUM (no true covalent bond, so ACH can easily compete with edrophohium for binding site)

62
Q

EDROPHonium onset

A

1-2 minutes

63
Q

EDROPHONIUM duration

A

30-60 minutes

64
Q

EDROPHONIUM not recommended for

A

DEEP BLOCK

65
Q

NEOGSTIMINE is a

A

Quaternary ammonium (CANNOT ENTER CNS)

66
Q

NEOGSTIMINE onset

A

7-11 minutes

67
Q

NEOGSTIMINE duration

A

45-90 minutes

68
Q

How do you mix NEO and GLYCOPYRROLATE

A

1mg of NEOSTIGMINE with 0.2 mg of GLYCOPYROLATE

1cc and 1cc = total admin 2cc

69
Q

Most commonly used reversal ______

Used for Diagnosis of therapy for MG is

A

NEOGSTIMINE.

EDROPHONIUM

70
Q

Neogstimine may cause

A

MAY INCREASE PONV

71
Q

Pyridostigmine

A

Quarternary ammonium’

72
Q

Only agent able to reverse CNS effect, why?

A

Physostigmine, crosses BBB

73
Q

Physostigmine dose

A

15-60 mcg/kg IV

74
Q

Physostigmine may reverse depression of

A

Reverse depression of ventilation associated with opioids but not the analgesia.

75
Q

How to asses anticholinesterase treatment in treatment of Myasthenia Gravis

A

Edrophonium 1 mg IV every 1-2 minutes to assess tc
if patient underdose, symptoms will improve
if overdose, symptoms will worsen

76
Q

POST op shivering you can use this agent ?

A

PHYSOSTIGMINE 40mcg/Kg at the conclusion of anesthesia

77
Q

Most often POST OP used for shivering is

A

Meperidine

78
Q

Overdose of anticholinesterase
Muscarininc :MDS BBLR
NIcotinic :

A 
Acute overdose 
Muscarinic symptoms--> 
Miosis
Difficulty focusing
Salivating
Bronchoconstiction, 
Bradycardia
loss of bladder and rectal control

Skeletal muscle weakness, PARALYSIS

79
Q

OVERDOSE of Anticholinesterase CNS effects

A

Confusion, ataxia, seizures

80
Q

Treatment of anticholinesterase intoxication

A

Atropine 35-70mcg/kg IV every 3-10 minutes until muscarinic symptoms disappear

81
Q

What is a ACETYLCHOLINESTERASE Reactivator?

A

Pralidoxime

82
Q

What is the dose of pralidoxime (2-PAM) ?

A

15 mg/kg IV over 2 minutes

83
Q

Synthetic Cholinergic Agonist are

A

Act as a agonists at postganglionic PNS nerves

84
Q

Synthetic Cholinergic Agonist mimics

A

Ach , act as muscarinic

85
Q

Synthetic Cholinergic Agonist 3 drugs

A

Methacholine (usd to diagnose asthma)
Bethanechol (usd for BPH)
Carbachol ( Glaucoma used)

86
Q

Synthetic Cholinergic Agonist avoid in

PAC

A

Asthma
CAD
PUD

87
Q

Carbachol and Bethanechol are _______

A

Resistant to hydrolysis of acetylcholinesterase

88
Q
  • Used as at stimulant of smooth muscle of the GI tract and urinary bladder
  • Use to treat NARROW ANGLE GLAUCOMA
A

Bethanecol

Carbachol

89
Q

Pilocarpine

A

Predominant muscarinic actions
DECRASE IOP
OVERCOME the mydriasis produced by atropine

90
Q

Sugammadex (Bridion)

A

selective relaxant binding agent designed to encapsulate the STEROIDAL NMBAs ROCURONIUM and vecuronium

91
Q

Sugammadex forms an

A

inclusion complex with these NMBAs, thereby preventing their binding to nicotinic receptors at the NMJ, resulting in reversal of neuromuscular blockade.

92
Q

Sugammadex effectiveness

Does not work with ____and______

A 
Rapid and effective
with BENZYLISOQUINOLINIUM (ATRA and MIVAcurium(
93
Q

The reversal activity of Sugammadex is

A

selective for steroidal NMB agents (ROC and VEC only)

94
Q

Shallow blocks Sugammadex ( reappearance of a 2nd twitch of the TOF)

A

2mg/kg

95
Q

Deep block (1-2 post titanic count)Sugammadex dose

A

4mg/kg

96
Q

Large block Sugammadex dose (For rescue) CANNOT INTUBATE< CANNOT VENTILATE

A

16mg/kg

97
Q

Sugammadex WARNINGS/PRECAUTIONS
Metabolism?
Elimination and clearance

A

Limited metabolism
ELIMINATED IN URINE UNCHANGED
RENAL PATIENT clearance decrease, elimination half life increase.
Dialysis IS NOT CONSISTENTLY EFFECTIVE

98
Q

WARNING of SUGGAMADEX

A

AVOIDED IN PATIENTS with a CrCl < 30ml/min

99
Q

Most commonly reported adverse reaction,

A

DYSGEUSIA (metal or bitter taste) after dose of 32mg/kg or higher
Flushing, rash

100
Q

Possibility that patients may have ______ and ______reaction, advise

A

Hypersensitivity and Anaphylaxis. Clinician caution.

SRNAPharmacology II (32 decks)

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