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

Anticholinesterase/Chol.Agonist/Sugga COMP Flashcards

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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
EDROPHONIUM (Tensilon) onset (rapid intermediate or delayed)
1-2 minutes (Rapid)
26
NEOSTIGMINE onset (fast, intermediate or slow)
7-11 minutes (intermediate)
27
Pyrostigmine onset (fast, intermediate or slow)
16 minutes (delayed)
28
Duration of action of those drugs affected by __________ and ranging from _______ to ____mns
affected by rate of disappearance | 60-76 minutes
29
Renal clearance % for neostigmine? Renal clearance of Pyridostigmine and Edrophonium? Is clerance affected in renal failure?
50% 75% Yes
30
Metabolism of Neo, edro and pyridostigmine of hepatic?
Hepatic 50 % Neostigmine | 30 % of Edrophonium and pyridostigmine
31
Pharmacological response by these agents reflects_____________At__________causing_________ __________ receptors
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
32
Parasympathetic activation side effects
``` Bradycardia may lead to asystole Salivation Miosis Hyperperistalsis Bronchoconstriction ```
33
NECESSARY To give ________simultaneously with this agent?
Anticholinergic drug
34
If you give NEOSTIGMINE and Pyridostigmine then SUCC what happens to SUCCINYLCHOLINE EFFECTS? why? Which one does NOT Inhibit plasma cholinesterase activity?
- effects of SCH is prolonged because enzymes are inhibited. - Because both Neostigmine and Pyridostigmine Produced -MARKED and PROLONGED Inhibition of PLASMA CHOLINESTERASE ACTIVITY - EDROPHONIUM
35
MUSCARINIC Anticholinergic agents effects? Effects on CV attenuated by giving? What happens to patient with DENERVATED HEART such as TRANSPLANT PT? PVR and SVR?
``` Bradycardia, Escape beats, Sinus Arrest Anticholinergic ASystole ( Denervated heart--Transplant) Decrease SVR, increase PVR ```
36
GI effect of Anticholinesterases (increase ach) enhance
Gastric fluid and increase GI motility
37
ETOMIDATE and N2O increase
Chance of post op N/V
38
This agent may treat paralytic ileum or atony of bladder ____
Neostigmine.
39
What is the risk associated with giving ANTICHOLINESTERASE with patients with MYASTHENIA GRAVIS who also received NDNMB?
CHOLINERGIC CRISIS
40
MG Patients are more sensitive to ________ why? and less sensitive to __________
Non-depolarizing to block because of down-regulation of receptors. More sensitive to ANTAGONIST (NDNMB) and less sensitive to (agonist)
41
MYOTONIA with anticholinesterase agent
Share some effect of succinylcholine (can produce FASCICULATIONS and AUGMENT Twitch response
42
Use ANTICHOLINESTERASE with caution with patient that have an ABSOLUTE CONTRAINDICATIONS to Succinylcholine, those patients are patients with (4)
Myotonia Muscular dystrophies Burn patint Spinal cord transection
43
Clinical uses of the drugs
``` Antagonized NDNMB drugs Treat CNS effects of drugs Treat MG/ Glaucoma Treat paralytic ileum and atony Treat Alzheimers ```
44
Antagonize- Assist REVERSAL of NMB 3 drugs use to reverse NDNMB? How do they help ?
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
More rapid onset of action with ______ Dose of EDROPHONIUM DURATION Of ACTION are all
EDROPHONIUM 0.5 mg/kg/ IV (1mg/kg if >90% twitch depression when reversal is initiated) Similar
46
Dose of NEOSTIGMINE Neostigmine appears to be preferable when Can be given with either ______or _______why?
0.043 mg/kg/IV >90% twitch depression is to be antagonized? Atropine or Glycopyrrolate ; because of slower onset of action.
47
Dose of Pyridostigmine | What is expected with Pyridostigmine?
0.21 mg/kg/ IV | Initial TACHYCARDIA
48
When EDROPHONIUM is used, which Atropine DOSE is recommended?
7 MCG/KG.
49
LESS than the recommended ATROPINE dose CAN CAUSE _______ | The dose of atropine is about ______the dose of NEOGstimine. Initial ______Then ____
BRADYCARDIA 1/2 Tachy --> brady
50
EXCESSIVE NMB: does additional doses of anticholinesterase drugs further antagonize the block? When is ventilation indicated then?
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
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?
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
EPHODRIUM may be more effective for reversal of
ATRACURIUM
53
NEOSGTIGMINE may be more effective for reversal of
VECURONIUM
54
Hoffman eliminaton dependent
pH and temperature dependent
55
HOW TO Avoid Residual paralysis | ADUU
- 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
During anesthetics that do not enhance NMB
A minimal of TOF count of 2 should be present before administration of anticholinesterases
57
During anesthetics that DO ENHANCE NMB
A TOF count of 4 should be present before administering anti cholinesterase.
58
What should be done if recovery of TOF>0.9 is documented? why?
Neostigmine administration should be withheld. | May decrease upper airway muscle activitiy and tidal volume
59
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)
- Delay reversal - administer pharmacologic reversal - administer pharmacologic reversal - administer pharmacologic reversal consider 20mcg/kg Neogstigmine
60
``` 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 ```
- Delay reversal -administer pharmacologic reversal - administer pharmacologic reversal - administer pharmacologic reversal consider 20mcg/kg Neogstigmine NO REVERSAL recommended
61
Class of Quarternary ammonium: Example
EDROPHONIUM (no true covalent bond, so ACH can easily compete with edrophohium for binding site)
62
EDROPHonium onset
1-2 minutes
63
EDROPHONIUM duration
30-60 minutes
64
EDROPHONIUM not recommended for
DEEP BLOCK
65
NEOGSTIMINE is a
Quaternary ammonium (CANNOT ENTER CNS)
66
NEOGSTIMINE onset
7-11 minutes
67
NEOGSTIMINE duration
45-90 minutes
68
How do you mix NEO and GLYCOPYRROLATE
1mg of NEOSTIGMINE with 0.2 mg of GLYCOPYROLATE | 1cc and 1cc = total admin 2cc
69
Most commonly used reversal ______ | Used for Diagnosis of therapy for MG is
NEOGSTIMINE. | EDROPHONIUM
70
Neogstimine may cause
MAY INCREASE PONV
71
Pyridostigmine
Quarternary ammonium'
72
Only agent able to reverse CNS effect, why?
Physostigmine, crosses BBB
73
Physostigmine dose
15-60 mcg/kg IV
74
Physostigmine may reverse depression of
Reverse depression of ventilation associated with opioids but not the analgesia.
75
How to asses anticholinesterase treatment in treatment of Myasthenia Gravis
Edrophonium 1 mg IV every 1-2 minutes to assess tc if patient underdose, symptoms will improve if overdose, symptoms will worsen
76
POST op shivering you can use this agent ?
PHYSOSTIGMINE 40mcg/Kg at the conclusion of anesthesia
77
Most often POST OP used for shivering is
Meperidine
78
Overdose of anticholinesterase Muscarininc :MDS BBLR NIcotinic :
``` Acute overdose Muscarinic symptoms--> Miosis Difficulty focusing Salivating Bronchoconstiction, Bradycardia loss of bladder and rectal control ``` Skeletal muscle weakness, PARALYSIS
79
OVERDOSE of Anticholinesterase CNS effects
Confusion, ataxia, seizures
80
Treatment of anticholinesterase intoxication
Atropine 35-70mcg/kg IV every 3-10 minutes until muscarinic symptoms disappear
81
What is a ACETYLCHOLINESTERASE Reactivator?
Pralidoxime
82
What is the dose of pralidoxime (2-PAM) ?
15 mg/kg IV over 2 minutes
83
Synthetic Cholinergic Agonist are
Act as a agonists at postganglionic PNS nerves
84
Synthetic Cholinergic Agonist mimics
Ach , act as muscarinic
85
Synthetic Cholinergic Agonist 3 drugs
Methacholine (usd to diagnose asthma) Bethanechol (usd for BPH) Carbachol ( Glaucoma used)
86
Synthetic Cholinergic Agonist avoid in | PAC
Asthma CAD PUD
87
Carbachol and Bethanechol are _______
Resistant to hydrolysis of acetylcholinesterase
88
- Used as at stimulant of smooth muscle of the GI tract and urinary bladder - Use to treat NARROW ANGLE GLAUCOMA
Bethanecol | Carbachol
89
Pilocarpine
Predominant muscarinic actions DECRASE IOP OVERCOME the mydriasis produced by atropine
90
Sugammadex (Bridion)
selective relaxant binding agent designed to encapsulate the STEROIDAL NMBAs ROCURONIUM and vecuronium
91
Sugammadex forms an
inclusion complex with these NMBAs, thereby preventing their binding to nicotinic receptors at the NMJ, resulting in reversal of neuromuscular blockade.
92
Sugammadex effectiveness | Does not work with ____and______
``` Rapid and effective with BENZYLISOQUINOLINIUM (ATRA and MIVAcurium( ```
93
The reversal activity of Sugammadex is
selective for steroidal NMB agents (ROC and VEC only)
94
Shallow blocks Sugammadex ( reappearance of a 2nd twitch of the TOF)
2mg/kg
95
Deep block (1-2 post titanic count)Sugammadex dose
4mg/kg
96
Large block Sugammadex dose (For rescue) CANNOT INTUBATE< CANNOT VENTILATE
16mg/kg
97
Sugammadex WARNINGS/PRECAUTIONS Metabolism? Elimination and clearance
Limited metabolism ELIMINATED IN URINE UNCHANGED RENAL PATIENT clearance decrease, elimination half life increase. Dialysis IS NOT CONSISTENTLY EFFECTIVE
98
WARNING of SUGGAMADEX
AVOIDED IN PATIENTS with a CrCl < 30ml/min
99
Most commonly reported adverse reaction,
DYSGEUSIA (metal or bitter taste) after dose of 32mg/kg or higher Flushing, rash
100
Possibility that patients may have ______ and ______reaction, advise
Hypersensitivity and Anaphylaxis. Clinician caution.

SRNAPharmacology II (32 decks)

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