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26 Cards in this Set
- Front
- Back
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Local Anesthetic MOA
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Block voltage-dependent NA+ channels--> decreases influx of Na+--> inhibits depolarization & blocks conduction of Action potential
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Size and myelination
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Small>large
myelinated>unmyelinated? |
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non-Topical local anesthetics
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Procaine
Bupivacaine |
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Only local anesthetic that doesn't vasodilate
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Cocaine!
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Cocaine's other mechanisms
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Blocks reuptake of NE
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Lidocaine SE
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Seizures
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The Amide local anethestics
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Bupivacaine
Lidocaine *have 2 "I"s* |
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Esters
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Tetracaine
Procaine Benzocaine Cocaine |
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Class of the "CURONIUM"
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Non-depolarizing NM blocker
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Tubocurarine Class
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Non-depolarizing NM blocker
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How does AChE inhibitor affect Nondepolarizing Muscle relaxants
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Reversed by AChE inhibitors
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Aside from being a NM blocker, what other actions does Tubocurarine have that the CURONIUMs don't?
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Weak blocker of ANS ganglia
Histamine release |
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MOA of Nondepolarizing Muscle relaxants
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Prevents action of ACh at skeletal muscle end plate. "Competative"
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What does AChE inhibitor do to Depolarizing NM blocker
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Doesn't affect it!
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Succinylcholine SE
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Malignant Hyperthermia
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What do Succinylcholine and Tubocurarine have in common?
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Both have histamine release and work on the ANS
T >>S for histamine Tubocurarine BLOCKS ANS Succinylcholine STIMULATES ANS!!! |
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Class of Succinylcholine
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Depolarizing NM blocker
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Succinylcholine MOA
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Acts like Nicotinic Agonist & depolarizes NM endplate--> continuous causes muscle relaxation & paralysis
Also stim ANS ganglia & cardiac M receptors |
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Centrally Acting Muscle Relaxants
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Baclofen
Diazepam (benzo) |
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Direct Acting Muscle Relaxant
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Dantrolene
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Baclofen MOA
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Spinal cord GABA-B agonist at both pre & post synaptic receptors--> hyperpolarization
Pre: decreases Ca2+ influx, decreases release of glutamic acid Post: facilitates inhibition by GABA |
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Diazepam SE
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Resp acidosis
Flumazenil reverses CNS toxicity |
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Diazepam MOA
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Facilitates GABA mediated presynaptic inhibition via GABA-A!!!!--> gating of Cl- channel--> hyperpolarizes
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Dantrolene MOA
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Binds to RyR1 channel on Sacroplasmic reticulum in skeletal muscle by decreasing release of activator CA2+ from SR
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What is an important use of muscle relaxants?
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Needed especially for tracheal intubation and ventilation (emergency)
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The only Agonist at nicotinic end plate in Muscle relaxants
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Succinylcholine!!
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