Kruse - centrally activng skeletal muscle relaxants Flashcards
Name the spasmolytic with MOA: agonist at GABAB receptors; results in hyperpolarization (due to increased K+ conductance) and inhibition of excitatory neurotransmitter release in the brain and spinal cord
baclofen
What drug is used to treat reversible spasticity associated with multiple sclerosis or spinal cord lesions with less overall loss of muscle strength than dantrolene
baclofen
AE of baclofen
drowsiness, increased seizure activity
Spasmolytic with MOA: CNS depressant, Metabolized to meprobamate, which has anxiolytic and sedative effects
carisoprodol
What are the two spasmolytics that are schedule 4 category of controlled drugs?
carisoprodol and diazepam
Use of carisoprodol
short term for MSK pain (2-3 weeks)
Use caution when administering what two drugs with CYP450 inhibitors?
- carisoprodol - metabolized by CYP2C19
- cyclobenzaprine
What drug is ineffective in treating muscle spasm due to cerebral palsy or spinal cord injury
cyclobenzaprine
What drug related to tricyclic antidepressants and may cause significant sedation, confusion, and transient visual hallucination - why these adverse effects?
cyclobenzaprine - produces antimuscarinic side effects
drowsiness, dizziness, and xerostomia - AE of ___
cyclobenzapine
What drug has MOA: promote binding of GABA (the major inhibitory neurotransmitter in the CNS) to the GABAA receptor, enhancing GABA-induced ion currents (increase frequency of channel openings); leads to increased inhibitory transmission and a reduction in spasticity
diazepam
Effect of diazepam at dose required to reduce muscle tone.
sedation
What drug is used to tx muscle spasticity and has MOA: alpha2-adrenergic agonist (chemically similar to clonidine) that decreases excitatory input to alpha motor neurons
tizanidine
Dantrolene is CI in pts with ___
hepatitis
What drug has MOA: cleaves components of the core SNARE complex involved in exocytosis, preventing the release of ACh
botulinum toxin
four drugs used for Multiple sclerosis
glucocorticoids, glatiramer acetate, IFN-B-1a/b, mitoxantrone
What drug is used to treat spasticity associated with upper motor neuron disorders (eg, spinal cord injury, stroke, cerebral palsy, or multiple sclerosis)
Dantrolene (and management of malignant hyperthermia)
What drug class has this use: a. monthly IV bolus of methylprednisolone used to treat primary or secondary progressive MS +/- immunosuppressants
Glucocorticoids
What drug has MOA: Mixture of four amino acids (L-alanine, L-glutamic acid, L-lysine, and L-tyrosine) - antigenically similar to myelin basic protein, which is an important component of the myelin sheath of nerves
Thought to induce and activate T-lymphocyte suppressor cells specific for a myelin antigen; also proposed to interfere with the antigen-presenting function of certain immune cells opposing pathogenic T-cell function
Used for…
Glatiramer acetate
used for relapsing-remitting type MS
Drug with MOA: Acts on blood-brain barrier by interfering with T-cell adhesion to the endothelium by binding VLA-4 on T cells or by inhibiting the T-cell expression of MMP
IFN-B-1a and IFN-B-1b
IFN-B-1a and IFN-B-1b treatment result in…?
in a reduction of relapses by one-third, a reduction of new MRI T2 lesions and the volume of enlarging T2 lesions, a reduction in the number and volume of Gd-enhancing lesions, and a slowing of brain atrophy
Drug with MOA: Antineoplastic agent used to treat MS, acute myeloid leukemia, and advanced, hormonerefractory prostate cancer
mitoxantrone
MOA of mitoxantrone
intercalates into DNA resulting in cross-links and strand breaks (related to anthracycline antibiotics)
