Pharmacology of Neuromuscular and Ganglionic blockers Flashcards

1
Q

Ganglionic blockers description

A
  • nicotinic receptor antagonist
  • rarely used
  • block reflexes : baroreceptor, pupillary
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2
Q

Trimethaphan uses

A

hypotension for surgery

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3
Q

Mecamylamine uses

A

tourettes, smoking cessation, severe hypertension

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4
Q

Vascular smooth muscle tone with SANS and PANS

A

SANS > PANS
endogenous tone = mild vasoconstriction
blockade = vasodilation

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5
Q

All other ANS function with SANS and PANS

A

PANS > SANS
endogenous tone = mild bradycardia
blockade = tachycardia

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6
Q

Neurmomuscular blockers function

A

block acetylcholine transmission

presynaptically; decrease Ach formation/release, increase metabolism

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7
Q

Function on skeletal muscle

A

block nicotinic receptors on skeletal muscle

drugs have a quaternary ammonium = peripherally restrict

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8
Q

Use for neuromuscular blockers

A
  • surgery, orthopedic procedures, bronchoscopy, artificial respiration/intubation
  • relaxes skeletal muscle
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9
Q

Sequence of muscle paralysis by curare/neuromuscular blocker

A
  1. muscles of eye, speech
  2. fingers, toes, limbs
  3. intercostals followed by diaphragm
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10
Q

Similarity between neuromuscular blocker and GBS

A

peripheral nerve disorder
progression worsens between 1day-2wks
caused by certain bacterial or viral infections

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11
Q

Neuromuscular blockers curare vs succinylcholine

A
  • agonist nicotinic Ach receptors

- persistent depolarization makes muscle fiber resistant to further stimulation by Ach

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12
Q

Succinylcholine duration and metabolism

A
depolarizing
short duration of 5-10min
metabolized to choline by butyrylcholinesterase
slower than ACHe
choline increases BP
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13
Q

Succinylcholine time and use

A

fast onset, short duration

used in trauma for intubation and electroconvulsant therapy

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14
Q

Contraindications for succinylcholine

A

hyperkalemia and cause of cardiac arrest

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15
Q

Neuromusclar blockers curare-like vs succinylcholine

A

non-depolarizing

antagonist nicotinic ACh receptors

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16
Q

Pancuronium duration

A

long duration, >180min

17
Q

Vecuronium, Atracurium duration

A

intermediate duration, 30-40min

18
Q

Trimethaphan duration

A

short acting

19
Q

Benefits of curare like neuromuscular blockers

A

easily reversible and widely used

20
Q

Types of cholinesterases

A

Acetylcholinesterase - located in synapse, prefers Ach

Plasmacholinesterase

21
Q

Description of Plasmacholinesterase

A
- butyrylcholinesterase(BuChE)
located in plasma
BuCH > Ach
succinycholine
local anesthetics(procaine)
22
Q

Carbamates description

A
acetylcholinesterase inhibitors
quarternary or tertiary amine groups
temporary covalent modification to AChE
reversible
covalent carbamate group will dissociate in 0.5-8hrs
23
Q

Physostigmine description

A

tertiary amine
enters CNS
IM, IV, local administration
used for atropine OD; blocks CNS and nonCNS

24
Q

Physostigmine treatment for

A

Glaucoma, Alzheimer’s

25
Neostigmine and Pyridostygmine description
quartanary amine peripherally restricted IM, IV, local administration
26
Neostigimine and Pyridostygmine treatment for
Myasthenia gravid reversal of NMB postoperative ileus, bladder distention
27
Organophosphates description
irreversible, covalent binding ACHe inhibitors | long last, >week
28
Treatment of organophosphates
glaucoma, but not common
29
Dangerous organophosphates
Nerve gas: sarin, soman Insecticides: Malathion(prodrug), Parathion, Diazinon -rapidly inactivated in mammals