2 - Neuromuscular and Ganglionic Blockers Flashcards

1
Q

Ganglionic blockers =

A

Nicotinic receptor antagonists

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2
Q

Ganglionic blockers block what reflexes?

A

Baroreceptor

Pupillary

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3
Q

____ is a ganglionic blocker for HoTN for surgery

A

Trimethaphan

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4
Q

For tourettes, smoking cessation, and severe HTN

A

Mecamylamine

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5
Q

endogenous tone of vascular smooth muscle

A

mild vasoconstriction

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6
Q

Endogenous tone of all other ANS functions

A

P>S

Mild bradycardia

blockage = tachycardia

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7
Q

Blockage of Ach transmission can occur either…

A

presyn or postsyn

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8
Q

Drugs that block nicotinic receptors on skeletal muscle have ______

They are ______

A

Quaternary amine

peripherally restricted

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9
Q

First clinically used NM blocker

A

Curare

D-tubocurarine = active alkaloid

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10
Q

What is TOF ratio

A

the response of 4th twitch relative to the first

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11
Q

TOF ratio = ____= 75% of receptors blocked

but…

A

0.25

but still near full muscular response

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12
Q

Recovery to __ needed for extubation, ___ for full recovery

A
  1. 7
  2. 9
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13
Q

____ twitch properly sedated

A

1-2

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14
Q

What level of twich can be rapidly reversed when monitoring NM blockade

A

1 twitch

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15
Q

Done redose if _____

A

no twitch

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16
Q

Sequence of paralysis by NM block

A
  1. Eye/speech
  2. DIgits
  3. Limbs
  4. Intercostals
  5. Diaphragm
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17
Q

What happens as a result of persistent depolarizaiton of the muscle fiber?

A

Makes it more resistant to further stimulation by Ach

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18
Q
  • Succinylcholine duration
  • metabolized to
  • Use?
  • CI’s?
A
  • 5-10 m
  • Metabolized to choline by BuChE
  • Used in trauma care, (intubation), electroconvulsant therapy
  • Avoid in HyperKalemia, cause of cardiac arrest
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19
Q

Binding of SUX to receptor allows ____

A

Na influx

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20
Q

Non-depolaizing NM blocker (curare-like)

A

Pancuronium (long acting, 180m)

Vecuronium + Atracurium (intermediate, 30m)

Trimethaphan (short acting i.v.)

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21
Q

Benefit of curare like NMBs

A

Easily reversible

22
Q

Reversal agents for Non-depolarizing NMB’s

A

Neostigmine (interacts with Ach)

Sugammadex (interacts with pancoronium)

23
Q

AChe degrades Ach to

A

Choline and acetate

24
Q

Enyme that makes Ach

A

ChAT

25
Q

substrates for Ach production

A

AcetylCoA + Choline

26
Q

Plasmacholinesterase =

Where?

What molecules?

A

Butyrylcholinesterase (BuChE)

In plasma

SUX, Local anesthetics (procaine)

27
Q

AChE inhibitors =

Have what groups?

Mechanism?

A
  • Carbamates
  • quaternary or tertiary amine groups
  • Temporary covalent modification to AChE

=Reversible

28
Q

Tertiry amine AchE that enters CNS?

Use?

A

Physostigmine

used for ATROPINE OD, glaucoma, Alzheimers

29
Q

Neostigmine and Pyridostygmine properties

Uses

A

Peripherally restricted, Quaternary amine

M. gravis, NMB reversal, post-op ileus, bladder distension

30
Q

Quaternary amine that’s orally available, has fewer sides and longer duration

A

Pyridostygmine

31
Q

Irreversible Covalently bonding Ach inhibitors

Length of duration

Use?

A

Organophosphates

>week in duration

Treatment for glaucoma

32
Q

Other Irrev. covalent Ach Inhibitors

A

Nerve gases = Soman/Sarin

Insecticides = Malathion (prodrug), Parathion, Diazinon

33
Q

Insecticides are _______

A

rapidly inactivated in mammals

34
Q

Antidote for ACHE poisioning

(antidote for…)

A

Pralidoxime Chloride (2-PAM)

(antidote for pesticide or nerve gas poisoning)

*should give within 2-3 hours of exposure

35
Q

Symptomatic treatment of ACHE poisioning (as opposed to antidote)

benefit of using this?

A

Atropine

fast onset

36
Q

Treatment of ACHE poisoning involves ________

A

combination of Pralidoxime + Atropine

37
Q

Symptoms of ACHEI poisoning

A

DUMBBELLS

M3 = Diarrhea, Urination, Miosis, Bronchospasms…Lacrimation, Sweating, Salivation

M2 = Bradycardia

Nm = Permanent depol of diaphragm is fatal (atropine wont help)

38
Q

ACHEI poisoning is more frequent with ______

A

farmers

39
Q

Edrophonium (Tensilon)

Binding

DoA

Use?

A

Binds non-covalently

Short acting (5-10 minutes)

Used to Dx Myasthenia Gravis

40
Q

M. gravis etiology

A

ABs block Nicotinic Ach receptors at the postsynaptic junction (NMJ)

41
Q

In M. gravis, Edrophonium improves _____

Treatment includes

A

Muscle strength

Tx = neostigmine/pyridostigmine

42
Q

Lambert Eaton Mg etiology

Treatment?

A

ABs against vg Calcium channels

Excercise improves muscle strength

Edrophonium has NO EFFECT

43
Q

Edrophonium is good at determining the difference between ___ and ___

A

Cholinergic crisis and MG

CC = no effect, small decrease in muscle strength

44
Q

CI’s to using Parasympathomimetic drugs?

A
  1. Asthma and COPD (bronchoconstrict)
  2. Coronary deficiency (lower HR)
  3. Peptic ulcer (acid secretion increased)
  4. Obstruction of UT or GIT
  5. Epilepsy (M1Rs, CNS penetrable drugs like pilocarpine)
45
Q

Parkinsons etiology

  • Reduction in ___ and____
A

Dementia with lewy bodies

  • Reduction in neocortical choline acetyltransferase (ChAT)
  • Rediuction in AchE activity in posterior regions and thalamus
46
Q

Other region implicated in Parkinson’s

A

Nucleus Basalis of Meynert

47
Q

Alzheimers = ____ of brain,

___ of sulci/____ of gyri

Improper proccessing of ___ leads to what??

A

Atrophy

wide sulci, narrow gyri

Improper processing of Beta amyloid precursor protein (b-APP) leads to toxic form that promotes apoptosis

48
Q

Toxic form of beta amyloid

A

b-A42

49
Q

Alzheimers Tx

  • MOA
  • Binding
  • but…
A

Donepezil (aricept)

  • Bind to anionic site and block ACh binding
  • Reversible, non-covalent
  • Does NOT SLOW PROGRESSION of the disease
50
Q

Rivastigmine MOA

Function

Sides

Replacement?

A

Reversible carbamate ACHEI

increases cholinergic function

Sides = Nausea, vomit, anorexia, weight loss.

Replacement = Eptastigmine

51
Q

Galamthamine MOA

From where?

May be a ____

Pharmacokinetics?

A

Reversible Competitive ACHEI

From daffodil

May be a nicotinic receptor agonist

Inhibits P450 (3A4, 2D6)

52
Q

Rivastigmine and Galanthamine caveat

A

Lost effectiveness as disease progresses