Pharmacology - Centrally acting muscle relaxants Flashcards
Baclofen
Centrally acting spasmolytic
GABAb agonist–>hyperpol and inhibition
Less sedation than diazepam
Less muscle str reduction than dantrolene
Baclofen adverse effects
Drowsiness, incr seizure in epileptics, vertigo, dizziness, psychiatric disturbance, insomnia, slurred speech, ataxia, hypotonia, muscle weakness
Carisprodol
Centrally acting spasmolytic CNS depressant Short term Schedule IV Metab by CYP2C19 Metab to meprobamate-->anxiolytic and sedative
Carisprodol adverse effects
Dizziness and drowsiness
Cyclobenzaprine
Centrally acting spasmolytic Influence alpha and gamma motor neurons Reduce tonic somatic motor activity Ineffective treating muscle spasm due to palsy or spinal cord injury Metab by CYP450
Cyclobenzaprine adverse effects
Antimuscarinic side effects
Sedation, confusion, visual hallucinations
Drowsiness, dizziness, xerostomia
Diazepam
Centrally acting spasmolytic
Benzodiazepine
Enhance GABAa–>reduce spasticity
Sedation, hypnotic effects, muscle relaxations, anxiolytic, anticonvulsant
Diazepam adverse effects
CNS depression, dependence, amnestic
Tizanidine
Centrally acting spasmolytic
Alpha2 agonist
Tizanidine adverse effects
Drowsiness, hypotension, dry mouth, asthenia/muscle weakness
Dantrolene
Non-centrally acting spasmolytic Interfere with excitation-contraction coupling Inhib RyR Ca channel Cardiac and smooth muscle unaffected Management of malignant hypertension
Dantrolene adverse effects
Muscle weakness, sedation, hepatitis
Contraind in pts with hepatitis
Botulinum toxin
Cleaves SNARE complex–>prevent ACh release
Botulinum toxin adverse effects
Focal muscle weakness, may last several months
Multiple sclerosis (MS) treatment
Glucocorticoids
Glatiramer acetate
Interferon beta 1a/1b
Mitoxantrone