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m relaxants
.
11
Medical
Graduate
12/10/2010

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Cards

Term
antispastic
Definition
specific for skeletal m, reduce spasticity that interferes w/ daily living like ms, cp, spinal cord inj

baclofen, dantrolene, bzd, tizanidine
Term
antispasmodic
Definition
relieves spasms, m relaxant, adjunct to rest, pt, relief of discomfort w/ msk d/o

cyclobenzaprine, bzd, tizanidine
Term
spasticity
Definition
inc tonic stretch reflex (1a sensory fiber --> a-motor n, inh int n), flexor m spasms punctuated w/ m weakness, often assoc w/ cp, ms, cva, involves stretch reflex arc + higher centers in cns

dmg desc pathways in spinal cord --> hyperexcitability of a-motor n

tx: red act of 1a afferent fibers and/or a-motor n
Term
bzd
Definition
enh act of gaba at gaba-a R --> open cl channel --> usu hyperpolarization (a-motor n, inh) but can depolarize (1a afferent, disrupts nt release), also anti-anxiety w/in higher cns, partly direct effect on spinal cord since works on spinal cord transection pt

diazepam most common, use to red spasticity from multiple etiologies, ae sedation
Term
baclofen
Definition
lisoresal, gaba-b R antagonist (metabotropic) on 1a afferent + motor n --> open k channel (out), close ca channel (in) --> hyperpolarization
also red pain by inh substance p

active po (rapid withdrawal --> hallucination/seizure), adjust for kidney fxn, intrathecal for sever spasticity (doesn't leak out, higher dose possible, inc qol but problem maintaining cath)
use ms (esp flexor spasm, concomitant pain), clonus, m rigidity, spinal cord inj, not helpful for cva pt or rheumatic --> skeletal m spasm

as effective as diazepam w/ less sedation, doesn't red m strength as much as dantrolene

ae teratogen, drowsiness, hypotension, gi (nausea)
Term
tizanidine
Definition
a2 agonist, congener of clonidine (less hypotensive, more cns), act presynaptic R on 1a afferent term --> dec release glu

po, onset 1.5 hr, halflife 2.5 hr, up to 6 hr, 95% first-pass

use ms/spinal inj, central/periph effect, comparable efficacy to diazepam, baclofen, dantrolene but diff ae (sedation, hypotension, dry mouth, lose strength, dizziness)

adjust for renal impair, inc lft, additive cns-dep action w/ diazepam/etoh, may inc conc phenytoin
Term
dantrolene
Definition
dantrium, periph acting, inh ca release from ryanodine channel on sr of skeletal m (not cardiac/smooth), tx (neuroleptic) malignant hyperthermia (inherited, pts can't sequester ca in sr, neuromuscular blocking agent or ga --> massive release ca --> massive contraction --> lactic acid prod, inc temp

1/3 po abs, halflife 8 hr, ae general weakness, sedation, chemical hepatitis
Term
cyclobenzaprine
Definition
use acute m spasm, inh serotonergic input to m neuron (local tissue trauma, m strain), related to tricyclic antidepressant so antimuscarinic (dry mouth, avoid in elderly or glaucoma pts), long qt (avoid in arrhythmia pts)
Term
gabapentin
Definition
ns indirectly acting gaba agonist, anti epileptic
Term
riluzole
Definition
rilutek, inh glu release (also red neuronal deg), inact v-dep na channel, use als
Term
botulinum toxin
Definition
inh ach release, local im inj for generalized spastic d/o like cp
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