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29 Cards in this Set

  • Front
  • Back
What does Acetylcholine breakdown to when it binds in the post synaptic groove? What was is it broken down by
Acetyl Acid and Choline. Broken Down by acetylcholinesterase.
What are the three major conformations or states of the skeletal muscle nicotinic acetylcholine receptor?
resting, open and desensitized.
Nicotinic agonists stabilize which 2 states of the receptor?
the open and desensitized states
Competitive antagonists stabilize what what state of the receptor
Resting state
What are the 2 clinical uses of neuromuscular drugs
provide muscle relaxation for surgery, 2) Anticholinesterases are used for dx and tx of myasthenia gravis
What is the name of the prototype NON depolarizing muscle relaxants (nicotinic receptor antagonist)
Vecuronium. This drug sits on receptor and doesn't allow it to respond to ACH
How does neostigmine work?
It blocks Acetylcholinesterase. Neostigmine binds to the anionic site of cholinesterase. The drug blocks the active site of acetylcholinesterase so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are too few acetylcholine receptors so with the acetylcholinesterase blocked, acetylcholine can bind to the few receptors and trigger a muscular contraction.
What is the adverse effects of non depolarizing muscle relaxants?
Hypotension
How does your body get rid of vecuronium?
Biliary secretion. Polar drugs are usually secreted in bile, it takes long for its effects and is eliminated slowly.
How does your body get rid of Atracurium?
Breaks down at physiological pH. This drug is non polar and works faster. It is chemically unstable. its spontaneously cleaved. doesn't have to be excreted, it breaks down by itself.
This drug is used for tracheal intubation
Succinylcholine
What is the ion channel state with the nicotinic receptor and sodium channel receptors during Tracheal Intubation?
nicotinic is open, sodium channel is closed (refractory)
what is the ion channel state with nicotinic and sodium channel receptors during Desensitization (pg 361?)
Nicotinic receptor is closed and sodium channel is open.
Is succinylcholine fast or slow acting and how many minutes does it stay. what then chews it up?
fast acting, stays 2-5 minutes. Plasma cholinesterase chews it up.
What are 4 disadvantages of depolarizing blockers?
1) Muscle soreness of succinylcholine-induced muscle relaxation
2) Inability to reverse stage 1 block with anti ChEs. 3) Potassium release may be life threatening in burn patients displaying skeletal muscle denervation hypersensitivity.4) Succinylcholine biotransformation is abnormally slow in certain people.
With the muscle relaxants Nicotinic agonists, there is continuous depolarization/fasiculations. Spontaneous contractions. Thin later with Anti-ChE further relaxation is taking place
True
True or False: Depolarization muscle relaxation meds can not be reversed by Anti CHE
True
This drug blocks the release of calcium from internal stores
Dantrolene
This drug is used for malignant hyperthermia and spasticity disorders
Dantrolene.
This drug relaxes muscle in a unique way, by inhibiting Ca+ ion release from skeletal muscle sarcoplasmic reticulum
Dantrolene
The Molecular Basis of this disease is the autoimmune loss of muscle nicotinic ACh receptors
Myasthenia Gravis. Antibodies that bind to nicotinic receptors which degrades them and disappears, and makes the muscles weak.
These 3 drugs are given for myasthenia gravis
neostigmine, pyridostigmine, edrophonium
These 2 myasthenia Gravis drugs are administered orally and display intermediate durations of action
neostigmine and pyridostigmine (anti-cholinesterases)
This myasthenia gravis drug is used for diagnosis of MG and for adjustment of AntiChE dose regime
Edrophonium (anti-cholinesterases)
True or False: With increasing Anti-ChE, you can start with Maysthemic weakness, then began to have optimal contractility, but then have cholinergic crisis.
True. You have cholinergic crisis due to decreased contractility because of desensitization (Resembling the 2nd stage of SuCC) Patient over medicates with esterase inhibitor and needs to decrease dosage or decrease frequency..(Myasthenic weakness occurs when the patient is undermedicated with a long duration cholinesterase inhibitor, where as cholinergic crisis occurs when the patient is over medicated.
True or False. A Major advantage of using a non depolarizing muscle relaxant acting upon the neuromuscular nicotonic receptor is because of the rapid reversibility with an acetylcholinesterase agonist.
False. A Major advantage of using a non depolarizing muscle relaxant acting upon the neuromuscular nicotonic receptor is because of the rapid reversibility with an acetylcholinesterase INHIBITOR
You do not use this drug if a surgical patient has suffered extensive skeletal muscle trauma several days to weeks earlier
Succinylcholine (depolarizing muscle relaxant/nicotinic agonist)
When a patient with myasthenia gravis is under medicated with an anticholinesterase, injection of a small dose of edrophonium will cause:
transient increase in muscle contractility.
With this drug: There is possible systolic arrest in post trauma patients with denervation hypersensitivity, clearance rate varies. This drug also can't be reversed by anti-ChE
Succinylcholine