Muscle Relaxants (Kruse) Flashcards
What are the nondepolarizing, Isoquinoline derivative, neuromuscular blocking drugs? (5)
-curium: (except for one)
1) Atracurium
2) Cisatracurium
3) Doxacurium
4) Mivacurium
5) Tubocurarine
What are the nondepolarizing, steroid derivative, neuromuscular blocking drugs? (4)
-curonium:
1) Pancuronium
2) Pipercuronium
3) Rocuronium
4) Vecuronium
What are the depolarizing neuromuscular blocking drugs?
Succinylcholine
What are the acetylcholinesterase inhibitors? (7)
1) Ambenonium
2) Donepezil
3) Echothiophate
4) Edrophonium
5) Galantamine
6) -Stigmine: Neostigmine, Physostigmine, Pyridostigmine, and Rivastigmine
7) Tacrine
What are the antimuscarinic compounds? (2)
1) Atropine
2) Glycopyrrolate
What is the cholinesterase reactivator?
Pralidoxime
What are the centrally acting spasmolytics (muscle relaxants)? (5)
1) Baclofen
2) Carisoprodol
3) Cyclobenzaprine
4) Diazepam
5) Tizanidine
What are the non-centrally acting spasmolytics? (2)
1) Dantrolene
2) Botulinum toxin
What are the immunologic drugs for MS? (5)
1) Glucocorticoids
2) Glatiramer acetate
3) Interferon beta 1a and 1b
4) Mitoxantrone
The following drugs make up what drug class?
1) Atracurium
2) Cisatracurium
3) Doxacurium
4) Mivacurium
5) Tubocurarine
Nondepolarizing, isoquinoline derivative, neuromuscular blocking drugs
The following drugs make up what drug class?
1) Pancuronium
2) Pipercuronium
3) Rocuronium
4) Vecuronium
Nondepolarizing, steroid derivative, neuromuscular blocking drugs
Succinylcholine makes up what drug class?
Depolarizing neuromuscular blocking drugs
The following drugs make up what drug class?
1) Ambenonium
2) Donepezil
3) Echothiophate
4) Edrophonium
5) Galantamine
6) -Stigmine: Neostigmine, Physostigmine, Pyridostigmine, and Rivastigmine
7) Tacrine
Acetylcholinesterase inhibitors
The following drugs make up what drug class?
1) Atropine
2) Glycopyrrolate
Antimuscarinic compounds
Pralidoxime makes up what drug class?
Cholinesterase reactivators
The following drugs make up what drug class?
1) Baclofen
2) Carisoprodol
3) Cyclobenzaprine
4) Diazepam
5) Tizanidine
Centrally acting spasmolytics (muscle relaxants)
The following drugs make up what drug class?
1) Dantrolene
2) Botulinum toxin
Non-centrally acting spasmolytics
The following drugs make up what drug class?
1) Glucocorticoids
2) Glatiramer acetate
3) Interferon beta 1a and 1b
4) Mitoxantrone
Immunologic drugs for MS
Neuromuscular blockers interfere with transmission at the neuromuscular end plate and lack?
CNS activity
Neuromuscular blockers are used as adjuncts during?
Anesthesia
What are the effects on consciousness or pain threshold with neuromuscular blockers?
No known effects
Spasmolytic agents are often called?
Centrally acting muscle relaxants
Spasmolytic agents are used to reduce spasticity in a variety of conditions by acting on?
CNS
What is the nondepolarizing blockade mechanism of neuromuscular blocking drugs?
What is the prototype?
1) Prevents access of ACh to its receptor and blocks depolarization
2) d-tubocurarine
What is the depolarizing blockade mechanism of neuromuscular blocking drugs?
What is the prototype?
1) Neuromuscular blockade due to excess of a depolarizing agonist
2) Succinylcholine
Why are Vecuronium, Rocuronium, Cisatracurium, and Atracurium commonly used in a clinical setting?
Allows tight control over paralysis due to an intermediate duration of action
What are some adverse effects of the neuromuscular blocking drugs?
1) Long acting
2) Hypotension and tachycardia with large doses
3) Histamine release
What are used to reverse NMJ blockade?
What are often administered with these drugs to minimize effects at mAChRs?
1) Cholinesterase inhibitors
2) Anticholinergic agents
What is the duration of action for succinylcholine?
What is this due to?
1) Ultra-short
2) Rapid hydrolysis and inactivation by butyrylcholinesterase and pseudocholinesterase
What are the MOA for succinylcholine?
1) Phase 1 depolarizing block
2) Phase 2 desensitizing block
In regards to the Phase 1 block of succinylcholine effects:
The effects are similar to ACh but?
The depolarized membranes remain depolarized and?
Flaccid paralysis results due to?
1) It produces a longer effect at the NMJ
2) Unresponsive to subsequent impulses
3) Lack of repolarization
In regards to the Phase 2 block of succinylcholine effects:
Continued exposure to succinylcholine causes?
nAChR behaves as if in a?
What happens to the receptor?
1) Initial end plate depolarization to decrease and the membrane becomes repolarized
2) Prolonged closed state
3) Desensitization
Which phase in the depolarizing block of succinylcholine is antagonized by cholinesterase inhibitors?
Phase 2
What are the clinical uses of neuromuscular blocking drugs?
1) Surgical relaxation
2) Tracheal intubation
3) Control of ventilation
4) Treatment of convulsions
The drugs of choice for rapid sequence intubation are those that act quickly such as?
Succinylcholine
The drugs of choice used as adjuncts to general anesthesia for muscle relaxation are those that are of longer duration such as?
Pancuronium
Acetylcholinesterase (AChE) inhibitors in this topic are used to?
Reverse pharmacologic paralysis
The centrally acting spasmolytic agent Baclofen has what MOA?
What effect does this have?
1) GABA(B) agonist
2) Inhibition of excitatory neurotransmitter release
The centrally acting spasmolytic agent Diazepam has what MOA?
What effect does this have?
1) Enhance GABA(A) receptor activity in the presence of GABA
2) CNS depression
The centrally acting spasmolytic agent Tizanidine has what MOA?
What effect does this have?
1) alpha2 agonist
2) CNS depression
The non-centrally acting spasmolytic agent Dantrolene has what MOA?
What effect does this have?
1) Inhibition of ryanodine receptors
2) Blocks the release of Ca2+
The non-centrally acting spasmolytic agent Botulinum toxin has what MOA?
What effect does this have?
1) Cleaves the VAMP and blocks fusion to presynaptic membrane
2) Inhibits ACh release
