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Neuromuscular Relaxants
whole lecture
14
Medical
Graduate
08/31/2013

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Term
Curare drugs
Definition
non-depolarizing agents
Term
Pancuronium
Definition
  • half-life: 30-60min (longest of the curares)
  • MoA: non-depolarizing blockade of muscle nic recs (curare)
  • Elim: renal excretion
  • Rx: adjuvant in surgical anesthesia, abdom wall relax & orthopedic procedures
  • tox: non-analgesic, apnea
  • contras
Term
chemical antidotes of curare drugs
Definition

- cholinesterase inhibitors (neostigmine)

- muscarinic blockers (glycopyrrolate--minimizes muscarinic effects of cholinesterase inhibitors)

Term
D-turbocurarine
Definition
  • half-life: >60min
  • MoA: non-depol blockade of muscle nic receptors (curare)
  • Elim: liver and renal
  • Rxprototype (only used in lethal injection)
  • tox
  • contras
Term
Rocuronium
Definition
  • half-life: 25-60min (medium of curares)
  • MoA: non-depol blockade of muscular nic receptors (curare)
  • Elimliver
  • Rxintubation, muscle relaxation during surgery or ventillation
  • tox: apnea, non-analgesic
  • contras
Term
mivacuronium
Definition
  • half-life: 15-20min (shortest of curares)
  • MoA: non-depol blockade of muscle nic recs (curare)
  • Elimplasma cholinesterase!!
  • Rxintubation, muscle relax during surgery or vent in pts w renal failure!!
  • tox: apnea, non-anagesic
  • contras
Term
vecuronium
Definition
  • half-life: 30-45min (medium for curares)
  • MoA: non-depol blockade of muscle nic recs (curare)
  • Elim: liver, renal
  • Rx: adjuvant in surgical anesthesia, abdom wall relax & orthopedic procedures
  • tox: apnea, non-analgesic
  • contras
Term
succinylcholine
Definition
  • half-life: <8min (SHORT!!)
  • MoA: nic agonist--depolarization blockade of muscle nic receptors 
  • Elim: plasma cholinesterase--(not AchE)
  • Rx: tracheal intubation, control convulsions during ECT
  • tox: apnea, non-analgesic, muscle pain from fasciculations, can initiate malignant hyperthermia
  • contrasmalignant hyperthermia
Term
succinylcholine--phase I / antidote
Definition

phase I: depolarizing block. inactivation of volt-gated Na+ channels.

 

antidote: none (hydrolyzed in 5-10min)

--Atropine for bradycardia due to muscarinic effects

Term
succinylcholine--phase II / antidote
Definition

phase II: desensitization block (if succinylcholine left for >30min, the neuron will be desensitized even after succinylcholine dissociates)

 

antidote: cholinesterase inhibitor!

Term
baclofen
Definition
  • half-life: 
  • MoA: inhibits NT release from sk muscle sensory afferent (GABAb agonist--spasmolytic)
  • Elim
  • Rx: muscle spasticity assoc w MS or spinal cord injury
  • tox: heavy drowsiness
  • contras
Term
benzodiazepines (diazepam, clonazepam)
Definition
  • trade
  • half-life: 
  • MoA: facilitate GABA mediated pre-synaptic inhibition
  • Elim
  • Rxspasticity, MS
  • tox: sedation and drowsiness (much less than baclofen)
  • contras
Term
tizanidine
Definition
  • half-life: 
  • MoA: centrally acting a2 agonist
  • Elim
  • Rxmuscle spasticity, MS
  • tox: drowsiness, hypoTN
  • contras
Term
dantrolene
Definition
  • half-life: 
  • MoA: uncouples excitation-contraction of sk muscles (blocks ryanodine recs--blocks Ca release from SR)
  • Elim
  • Rxmuscle spasm, MALIGNANT HYPERTHERMIA
  • tox: muslce weakness, sedation
  • contras
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