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Pharmacology Exam 5 > Skeletal Muscle Relaxants > Flashcards

Skeletal Muscle Relaxants Flashcards

1
Q

What is the clinical use of blocking drugs?

A

muscle relation for surgery and for electroshock therapy

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2
Q

What is the clinical use of anticholinesterases?

A

diagnosis and therapy of myasthenia gravis

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3
Q

Is the whole length of the muscle DIRECTLY affected by synapse activities?

A

nooooo

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4
Q

Random reminders about skeletal muscle APs

A

Ach is NT (released from vesicles), Na+ channel, all-or-none.

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5
Q

What about the Ach receptors?

A

nicotinic, ligand-gated, pentameric

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6
Q

How does Botox work?

A

inhibits release of Ach from vesicle

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7
Q

What does Acetylcholinesterase?

A

in post-synaptic receptors, stops depolarizaion by hydrolizing Ach

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8
Q

What are the 3 major conformations or states of the skeletal muscle nicotinic acetylcholine receptor?

A

resting, open, desensititized

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9
Q

Which states of the Ach receptor do the nicotinic agonists stabilize?

A

the open and desensitized

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10
Q

Which states of the Ach receptor do the competitive antagonists stabilize?

A

the resting state

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11
Q

During the desensitized state, is the Na channel open or closed? What is the purpose of this state?

A

There is still high affinity for the agonist, but the channel is closed. Purpose is protective from overstimulation

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12
Q

non-depolarizing muscle relaxants AKA…?

A

nicotinic receptor antagonists

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13
Q

What is the prototype non-depolarizing drug?

A

Vecuronium

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14
Q

What is an adverse effect of Vecuronium? Why?

A

hypotension. it is not selective for skeletal muscle nicotinic receptors and therefore also has affinity for autonomic nicotinic receptors.

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15
Q

What is Neostigmine?

A

Anticholinesterase

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16
Q

What does Neostigmine (anticholinesterase) do?

A

Reversal of Vecuronium block (there is competition between the anticholinesterase and the non-depolarizing drug)

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17
Q

What causes the adverse effect of hypotension with Vecuronium?

A

basophil histamine release, blockade of autonomic neurotransmission

18
Q

How is Vecuronium eliminated?

A

largely by biliary secretion

19
Q

What is Atracurium?

A

another non-depolarizing drug thats spontaneously breaks down at physiological pH

20
Q

depolarizing muscle relaxants AKA…?

A

Nicotinic Agonists

21
Q

What is the prototype nicotinic agonist/depolarizing blocker?

A

Succinylcholine

22
Q

What is succinylcholine?

A

essentially a stable form of Ach

23
Q

What are the two stages of SuCH block?

A

depolarizing, non-depolarizing

24
Q

What do anticholinesterases do to stage 1 SuCH block?

A

they fail to reverse stage 1 block

25
Q

What are fasciculations?

A

muscle twitches with use of depolarizing drug (succinulcholine). produce post-operative soreness

26
Q

Which stages of SuCH block are important when SuCH is used for tracheal intubation?

A

Only the first, depolarizing stage. Stage 2 block is not observed because of its slow onset

27
Q

Which stage block for tracheal intubation?

A

stage 1 (depolarizing)

28
Q

Which stage block for desensitization?

A

stage 2 (non-depolarizing)

29
Q

What are the ion channel states during stage one block (depolarizing, tracheal intubation)?

A

nicotinic receptor open, sodium channel closed (refractory)

30
Q

What are the ion channel states during stage 2 block (non-depolarizing, desensitization)?

A

nicotinic receptor closed (desensitized), sodium channel read to open

31
Q

What are some disadvantages of depolarizing blockers (4)?

A

1) muscle soreness of SuCH-induced muscle relaxation
2) inability to reverse stage 1 block with anti-ChEs
3) K+ release may be life-threatening in burn patients displaying skeletal muscle denervation hypersensitivity
4) SuCH biotransformation is abnormally slow in certain people

32
Q

Which drug can be used for treatment of malignant hyperthermia and spasticity disorders?

A

Dantrolene

33
Q

How does Dantrolene work?

A

relaxes muscle in a unique way, but inhibiting Ca ion release from skeletal muscle sarcoplasmic reticulum

34
Q

What is Myasthenia Gravis?

A

autoimmune loss of muscle nicotinic ACh receptors

35
Q

Which drugs are used to treat myasthenia gravis?

A

Neostigmine and Pyridostigmine

36
Q

How are Neostigmine and Pyridostigmine administered and what are their durations of action?

A

administered orally, intermediate durations of action

37
Q

Which drug is used for diagnosis of myasthenia gravis?

A

Edrophonium

38
Q

What else is Edrophonium used for and how?

A

adjustment of antiChE dose. If Edro produces improvement in contractility, then patient is under-medicated. if worsens contractility, over-medicated.

39
Q

What happens when the patient is under-medicated with a long-duration cholinesterase inhibitor?

A

myasthenic weakness

40
Q

What happens when the patient is over-medicated?

A

cholinergic crisis

Pharmacology Exam 5 (9 decks)

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