Pharm NMJ part II Flashcards

1
Q

what are the clinical uses of NMJ blocking drugs

A

surgical relaxation
endotracheal intubation
control of ventilation

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2
Q

how do NMJ blockers help control ventilation

A

reduce chest wall R and improve thoracic compliance
permit adequate gas exchange and prevents atelectasis in patients who have ventilatory failure
pancuronium and vecuronium most common if >24 hours

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3
Q

MOA dantrolene

A

inhibition of RYR Ca Ch blocking release of Ca from SR and so no muscle contraction

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4
Q

side effects dantrolene

A

generalized muscle weakness, sedation, and occasionally hepatitis

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5
Q

what is dantrolene used for

A

Tx for spascitiy associated with UMN disorders and management of malignant hyperthermia

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6
Q

what patients are at risk for malignant hyperthermia

A

hereditary mutations in RyR gene
permits excessive Ca release from SR under certain triggering agents
increase Ca, increase lactic acid, increase temperature

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7
Q

what do we use to reduce Ca in malignant hyperthermia

A

IV dantrolene

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8
Q

MOA botulinum toxin

A

cleaves SNARE and blcoks release of ACh by preventing vesicle exocytosis

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9
Q

what is botulinum used for

A

generalized spastic disorders, cervical dystonia and blepharospasm

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10
Q

what are direct acting cholinomimetics

A

bind and activate mAChR and nAChR

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11
Q

what are indirect acting cholinesterase inhibitors

A

inhibit AChE increasing ACh in the celft

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12
Q

where is butyrylcholinesterase made

A

liver and found inliver and plasma

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13
Q

AChE is found where

A

highly [ ] postsynaptic end plate and prevents lateral diffusion from adjacent nAChRs

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14
Q

primary target for cholinesterase inhibiting drugs

A

AChE but also block BuChE

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15
Q

3 chemical groups of cholinesterase inhibitors

A

Alcohols
Carbamic acid esters
Organophosphates

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16
Q

how does alcohol work as AChE inhibitor

A

+ charged quaternary ammonium that binds to AChE noncovalently

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17
Q

how do carbamic acid esters work like AChEI

A

quaternary and tertiary ammonium groups that bind to AChE noncovalently

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18
Q

which AChEI are carbacmic acid esters

A

neostigmine, pyridostigmine, physostigmine, carbaryl

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19
Q

what AChEI are alcohols

A

edrophonium

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20
Q

what AChEI are organophosphates

A

echothiophate, parathion and malathion, sarin, soman, tabun

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21
Q

what is a precaution with organophosphates

A

CNS toxicity since neutrally charged and lipid soluble

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22
Q

bond between organophosphates and AChE

A

covalent and irreversible

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23
Q

what is preferred administration for the AChE I with quaternary ammoniums

A

parenteral

no CNS distribution

24
Q

What are the tertiary uncharged AChE I and distribution?

A

physostigmine, donepezil, tacrin, rivastigmine, glantamine

CNS distrivution

25
what organophosphate is safe for use as insetidiced
malation
26
what is "aging" or organophosphates
phosphorylated enzyme will break one of the O-PO4 bonds of inhibitor and strenghten the bond
27
high [ ] effects of AChEI on CNS
generalized convulsions d/t neuronal hyperstimulation
28
effects of AChE I on eyes
contraction of iris | contraction of ciliary muscle
29
AChE I effects on hearat
Sympathetic and Parasympathetic parasympathetic dominates and CO decreases bradycardia
30
Tx myasthenia gravis
pyridostigmine, neostigmine and ambenonium do not cross bbb repeated dose every 2-8 hours
31
what is favored test for myasthenia gravis
ice pack test
32
Myasthenic crisis
life threatening condision defined as weakness from acquired myasthenia gravis that is severe enough to necessitate intubation
33
excessive AChE I use can lead to what
cholinergic crisis
34
Sx cholinergic crisis
muscle weakness
35
how to differentiate cholinergic crisis from myasthenic crisis
edrophonium test myasthenic crisis Sx will get better cholinergic crisis will remain unchanged
36
what AChE I are pregerred to reverse paralysis induced by NMJ blockers
neostigmine and edrophonium
37
Tx paralytic ileus, atony urinary bladder and congenital megacolon
AChE I
38
What is glaucoma
increased intraocular P
39
how do AChE I help with glaucoma
reduce intraocular P by stimulating mACHRs of ciliary body and cause contraction which facilitates outflow of aqueous humor
40
what is preferred Tx for glaucoma
topical beta blockers and PG derivatives
41
What is used to Tx dementia
donepezil, rivastigmine, glantamine and physostigmine
42
intoxication from anticholinergic Sx
cutaneous vasodilation, anhidrosis, anhydrotic hyperthermia, nonreactive mydirasis, delerium, hallucinations, reduction or elimination of desire to urinate
43
reversal of antimuscarinc toxicity
physostigmine because crosses bbb
44
what occurs if combine succinylcholine with AChE I
enhance phase I block and antagonize phase 2 block
45
effects of beta blocker with AChE I
bradycardia
46
Sx AChE intoxication
miosis, salivation, sweating, bronchial constriction, vomiting, diarrhea
47
what are the CNS involvements of AChE intoxication
confusion, ataxia, generalized convulsions, coma and respiratory paralysis
48
what causes death in AChE intoxication
respiratory failure
49
Dx AChE intoxication
measure AChE activity in RBCs and plasma
50
antidote for AChE intoxication
atropine | except is ineffective in peripheral NMJ, need cholinesterase regenerators
51
pralidoxime
cholinesterase regenerator
52
what is window frame for effective use of pralidoxime against organophosphate toxicity
before aging has occured
53
does pralidoxime cross bbb
no
54
pyridostigmine is used in military for what
prophylaxis AChE inhibitor posioning | nerve gas
55
side effects of pyridostigmine
stomach cramps, diarrhea,nausea, urination, HA, dizziness, SOB, worsening peptic ulcer, blurred vision, watery eyes