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24 Cards in this Set
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Used in ICU to induce muscle paralysis
Interfere with transmission at NMJ Lack CNS activity Mainly used as adjuncts during general anesthesia |
Neuromuscular Blockers
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Reduce spasticity
Used to treat chronic pain and fibromyalgic conditions |
Spasmolytics
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non-depolarizing NM blockers block action of ? at Nm receptors
depolarizing blockers block by using an ? |
ACh
agonist (succinyl choline) |
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Both nondepolarizing and depolarizing have 2 ?
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quaternary nitrogens
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depolarizing NM have ? structure similar to ?
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linear ; ACh
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Non depol. NM blockers conceal double ACh structures in ?
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a ring system
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All steriodal muscle relaxants are metabolized to ?
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3, 17 hydroxy products
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Intermediate acting
Hepatic and spontaneous degradation (laudanosine, long half life, crosses bbb, may cause seizures) Causes transient hypotension (histamine release) |
Atracurium (generic, Tracrium):
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Potent isomer of atracurium
Produces less laudanosine and is less likely to release histamine Has replaced atracurium |
Cisatracurium (Nimbex):
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Shortest acting (duration 15 min)
Rapidly inactivated by plasma cholinesterases (liver disease patients or genetic deficiency of cholinesterase, renal impairment) Onset is slower than succinylcholine, histamine release |
Mivacurium (Mivacron):
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Short duration of action (5-10 min)
Highly metabolized by cholinesterases (plasma, liver) Metabolite (succinylmonocholine) is rapidly degraded Plasma esterases (prolonged duration in patients with abnormal variant of cholinesterase) |
Succinylcholine (generic, Anectine)
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measure of the ability of the patient to metabolize succinylcholine
Normally, dibucaine inhibits normal enzyme activity by 80% and abnormal enzyme by 20% |
dibucaine number
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act competitive antagonists at the nicotinic muscle receptors at the NMJ
Effect of neostigmine, edrophonium, and pyridostigmine In larger doses, can block the pore Can also block prejunctional sodium channels |
Non Depolarizing blockers
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succinlycholine, are agonists on the Nm receptors, stimulate rec at low conc, block the pore at high conc
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depolarizing blockers
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Depolarization, prolonged flickering, unresponsive to stimuli
Flaccid paralysis Augmented by ChEI which phase I or II? |
phase I
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Membrane repolarization
Similar to nondepolarizing block Reversible by ChEI Which phase I or II? |
phase II
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Adverse affects of depolarizing blockade
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hyperkalemia, increased intraocular pressure, increased intragastric pressure, muscle pain
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Submitted for FDA approval as a reversal drug
Rapidly inactivates steroidal NMN blockers by forming an inactive complex |
Sugammadex
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antagonize NM blockade by nondepolarizing blockers
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ChEI (Neostigmine, pyridostigmine)
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Mechanism
Used in patients with almost any type of muscle spasm spasmolytic |
Diazepam (Valium)
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GABAB agonist
Reduce release of Excitatory nt in brain, spinal cord Reduce pain, inhibit release of substance P Start at 15 mg dose 2x daily Increase as tolerated to 100 Adverse effects: Drowsiness Increased seizures in epileptic patients |
Baclofen (Lioresal)
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spasmolytic
a2 agonist Both pre and postsynaptic inhibition in spinal cord Inhibits nociceptive transmission in spinal cord dorsal horn Adverse effects: Drowsiness, hypotension, dry mouth, asthenia |
Tizanidine (Zanaflex):
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Progabide (GABAA and GABAB agonist)
Glycine, inhibitory neurotransmission spasmolytic |
gabapentin (neurontin)
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Blocks excitation-contraction coupling
Doses start at 25 mg daily, may increase up to 100 mg daily Used in malignant hyperthermia (1 mg/kg IV) spasmolytic |
dantrolene
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