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ODR
Pharm Muscle Relaxers
20
Pharmacology
Graduate
12/12/2010

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Cards

Term
define spasticity
Definition
hyperexcitability of alpha motor neurons
increase in tonic stretch reflex
increase in flexor muscle spasm
muscle weakness
input from higher centers in CNS
Term
When are antispasmodic drugs used?
Definition
when NSAIDs are ineffective
Term
What are the functions of the GABA receptors on the Ia afferent fibers?
Definition
GABA A: Cl- efflux disrupts Na & Ca channel activation and inhibits NT release
GABA B: decreases CA influx and inhibits presynaptic release of NT
Term
What are the functions of the GABA and A2 receptors on the Ia afferent fibers?
Definition
GABA A: Cl- efflux disrupts Na & Ca channel activation and inhibits NT release
GABA B: decreases CA influx and inhibits presynaptic release of NT
A2: decreased glutamate release
Term
What are the functions of the GABA and alpha-2 receptors at the alpha motor neuron?
Definition
GABA A: Cl influx hyperpolarizes and stabilizes the membrane
GABA B: K+ conductance is increased, so the membrane is hyperpolarized
A2: inhibition
Term
Baclofen MOA and uses
Definition
antispastic
GABA B agonist
po/intrathecal
used for MS, clonus, muscle rigidity, SC disease, may decrease muscle strength
Term
What are the AE of baclofen?
Definition
drowsiness
hypotension
GI problems (nausea)
teratogenic?
withdrawal from po: hallucinations, seizures
Term
dantrolene MOA and uses
Definition
antispastic
peripherally acting, decreases Ca release from SR via ryanodine receptors
used for malignant HT, neuroleptic malignant syndrome
Term
Which drugs are purely antispastic?
Definition
baclofen and dantrolene
Term
What are the AEs of dantrolene?
Definition
hepatitis, general muscle weakness, sedation
Term
Which drugs are antispastic and antispasmodic?
Definition
benzodiazepenes (diazepam) and tizanadine
Term
benzodiazepenes (diazepam)
Definition
allosteric modulation of GABA-A in CNS & SC
if patient has a central lesion you need a larger dose but that will cause sedation
Term
What are the adverse effects of benzodiazepenes?
Definition
sedation
abuse potential
Term
Tizanadine
Definition
short acting A2 agonist
PO
Used for MS & SCIs
Term
What are the AE of Tizanadine?
Definition
dry mouth, sedation, dizziness, hypotension, increased liver enzyomes (aminotransferase)
Term
cyclobenzaprine
Definition
unclear MOA (may decrease excitatory drive to MNs)
used for acute muscle spasms & local pain associted with them
Term
What are the AEs of cyclobenzaprine?
Definition
anticholinergic effects
prolongs QT interval (avoid in patients w/heart problems)
Term
What drug is used to treat malignant HT?
Definition
dantrolene
Term
Which drugs have antispasmodic activity? antispastic?
Definition
antispasmodic: cyclobenzaprine, tizanadine, benzodiazepene
antispastic: baclofen, dantrolene, benzos, tizanadine
Term
which drug can cause a prolonged QT interval?
Definition
cyclobenzaprine
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