Ch 27: Skeletal Muscle Relaxants Flashcards
neuromuscular blockers
can get muscle relaxation w/out deep depression
effects of neuromuscular blockers
- 1st cause muscle weakness, then flaccid & unexcitable
- larger muscles more resistant & recover quicker (diaphragm last)
act as:
depolarizing agents
non-depolarizing agents
depolarizing agents
- can cause arrhythmia (stimulates mus. & Nic receptors of heart… decrease inotropicity & chronotropicity)
- Succinylchlorine: paralysis takes 1 minute
non-depolarizing agents
- can cause hypotension (hist. release; give w/ antihistamine)
- Vecuronium, doxacurium
Spasmolytics
can reduce spasticity & spasms
Spasticity
abnormal stretch reflex, especially. w/ rapid lengthening of muscle: appears mostly due to “higher centers” (upper motor neuron lesion)
Spasms
afferents from damaged muscle tissue excites outflow from alpha motor neurons
Centrally acting agents
Diazepam
Baclofen
Tizanidine
Direct acting agents
Dantrolene sodium (Dantrium) Botulinum toxin (botox)
Diazepam
facilitates GABA-a activity
- causes sedation (problem)
- useful w/ spasms/spasticity (acts in the cord)
- causes sedation, hangover, tolerance
Baclofen
primary agent for spasticity
(beta-chlorophenyl- GABA)
- activates GABA in cord & increases K+ conductance (hyperpolarization)
- inhibits alpha motor activity
- given orally or intrathecal to subarachnoid space near affected area (can have problems w/ delivery system {pump, catheter} & tolerance)
Side effects of Baclofen
initial drowiness
fatigue
headache
Tizanidine
alpha 2 adrenergic agonist
- reinforce pre- and post-synaptic inhibition in cord
side effects of Tizanidine
drowsiness
hypotension
dry mouth
(studies show equal efficacy as diazepam, baclofen & dantrolene in several types of spasticity)
Dantrolene sodium (Dantrium)
primary use for MS
- inhibits calcium release from SR in “excited” muscle cells
- block receptor site on SR that opens the channels that calcium exits (ryanodine site)
side effects of Dantrolene sodium (Dantrium)
generalized muscle weakness
drowsiness
dizziness
- severe hepatotoxicity