Neurodegenerative Disease Flashcards
Riluzole
ALS; complex pre and post synaptic mechanism: inhibits GLU release, inhibits NMDA and kainite GLU receptors; inhibits fast Na+ channels (slight effect to slow disease progression 2-3 months)
Edaravone
ALS; mechanism unclear, no benefit advanced cases, may slow in early disease, IV dosing
Baclofen
GABAb agnoist - acts in spinal cord inhibit motoneurons (palliative ALS); skeletal muscle relaxant
Tizansidine
alpha2 agonist; CNS to decrease muscle tone palliative ALS also skeletal muscle relaxant
Dextromethorphan
Pseudobulbar affect in ALS; complex MOA: agnoist at sigma receptor, weak inhibition of 5-HT transporter; allosteric inhibition of NMDA
Quinidine
reduced dextromethorphan metablism so acts longer (by CYP2D6)
L-DOPA/Carbidopa
LDOPA DA precursor enters CNS via AA transporter (neutral), enters DA neurons, converted to DA by DOPA decarboxylase (nausea, vomiting); Carbidopa does not penetrate CNS, keeps L DOPA from converting to DA in periphery
DA Receptor Agonists
Parkinson’s less motor recovery and more side effects than L DOPA but less risk of dyskinesias (nausea, vomiting, psychiatric rxns, postural hypotension)
Bromocriptine
obsolete ergot DA receptor agonist
Pramipexole
renal clearance; non ergot DA receptor agonist also approved for sudden restless leg syndrome. D2 agonists can impair impulse control, lead to excessive gambling, shopping, food intake, sexual activity etc
Ropinirole
hepatic clearance; non ergot DA receptor agonists; can impair impulse control
Rotigitine
24 hr transdermal patch DA receptor agonist
apomorphine
non ergot DA receptor agonist injected s.c. rapid but temp relief of off akinesia episodes; nausea common
trimethobenzamide
pretreat nausea of apomorphine, antiemetic
MAO-B inhibitors
minor effects for Parkinson’s alone but enhance L DOPA effects
Selegiline
MAO B inhibitor; metabolites include methaphetamine and amphetamine - insomnia anxiety. minor effects for Parkinson’s alone but enhance L DOPA effects