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
Q

what organophosphate is safe for use as insetidiced

A

malation

26
Q

what is “aging” or organophosphates

A

phosphorylated enzyme will break one of the O-PO4 bonds of inhibitor and strenghten the bond

27
Q

high [ ] effects of AChEI on CNS

A

generalized convulsions d/t neuronal hyperstimulation

28
Q

effects of AChE I on eyes

A

contraction of iris

contraction of ciliary muscle

29
Q

AChE I effects on hearat

A

Sympathetic and Parasympathetic
parasympathetic dominates and CO decreases
bradycardia

30
Q

Tx myasthenia gravis

A

pyridostigmine, neostigmine and ambenonium
do not cross bbb
repeated dose every 2-8 hours

31
Q

what is favored test for myasthenia gravis

A

ice pack test

32
Q

Myasthenic crisis

A

life threatening condision defined as weakness from acquired myasthenia gravis that is severe enough to necessitate intubation

33
Q

excessive AChE I use can lead to what

A

cholinergic crisis

34
Q

Sx cholinergic crisis

A

muscle weakness

35
Q

how to differentiate cholinergic crisis from myasthenic crisis

A

edrophonium test
myasthenic crisis Sx will get better
cholinergic crisis will remain unchanged

36
Q

what AChE I are pregerred to reverse paralysis induced by NMJ blockers

A

neostigmine and edrophonium

37
Q

Tx paralytic ileus, atony urinary bladder and congenital megacolon

A

AChE I

38
Q

What is glaucoma

A

increased intraocular P

39
Q

how do AChE I help with glaucoma

A

reduce intraocular P by stimulating mACHRs of ciliary body and cause contraction which facilitates outflow of aqueous humor

40
Q

what is preferred Tx for glaucoma

A

topical beta blockers and PG derivatives

41
Q

What is used to Tx dementia

A

donepezil, rivastigmine, glantamine and physostigmine

42
Q

intoxication from anticholinergic Sx

A

cutaneous vasodilation, anhidrosis, anhydrotic hyperthermia, nonreactive mydirasis, delerium, hallucinations, reduction or elimination of desire to urinate

43
Q

reversal of antimuscarinc toxicity

A

physostigmine because crosses bbb

44
Q

what occurs if combine succinylcholine with AChE I

A

enhance phase I block and antagonize phase 2 block

45
Q

effects of beta blocker with AChE I

A

bradycardia

46
Q

Sx AChE intoxication

A

miosis, salivation, sweating, bronchial constriction, vomiting, diarrhea

47
Q

what are the CNS involvements of AChE intoxication

A

confusion, ataxia, generalized convulsions, coma and respiratory paralysis

48
Q

what causes death in AChE intoxication

A

respiratory failure

49
Q

Dx AChE intoxication

A

measure AChE activity in RBCs and plasma

50
Q

antidote for AChE intoxication

A

atropine

except is ineffective in peripheral NMJ, need cholinesterase regenerators

51
Q

pralidoxime

A

cholinesterase regenerator

52
Q

what is window frame for effective use of pralidoxime against organophosphate toxicity

A

before aging has occured

53
Q

does pralidoxime cross bbb

A

no

54
Q

pyridostigmine is used in military for what

A

prophylaxis AChE inhibitor posioning

nerve gas

55
Q

side effects of pyridostigmine

A

stomach cramps, diarrhea,nausea, urination, HA, dizziness, SOB, worsening peptic ulcer, blurred vision, watery eyes