CNS Flashcards
glutamate antagonists
memantine
Memantine MOA
binds NDMA receptor with higher affinity than Mg → inhibits Ca2+
uses of Memantine
Alzheimer’s and Ischemic stroke
GABA agonists
muscimol
MOA of GABA agonists
bind GABA receptor induces hyperpolarization
uses of GABA agonists
epilepsy
GABA antagonists
Bicuculine
Picrotoxin
GABA antagonists MOA
blocks inhibitory action of GABA
uses of GABA antagonists
convulsants
AchE inhibitors
Tacrine
Donepezil
Rivastigmine
Galantamine
MOA of AchE inhibitors
inhibits breakdown of Ach
uses of AchE inhibitors
Alzheimer’s (minimal benefit)
COMT inhibitors
Tolcapone
Entacapone
MOA of COMT inhibitors
inhibits extracellular dopamine degradation
uses of COMT inhibitors
2nd line drug, not sufficient alone
GABA up-regulators
barbiturates
benzodiazepines
MOA of GABA up-regulator
Increase: GABA receptor function, burst opening of GABA channels, Cl- influx into the cell to enhance inhibitory synaptic transmission
uses of GABA up regulators
Seizures, status epilepticus, sleep disorders (insomnia), pre- operative sedation
dopamine precursor
L-dopa (Levodopa)
uses of dopamine L-dopa
Less effective as the disease progresses and more dopamine receptors are lost
Small, frequent doses are best
Pair with Carbidopa to block dopamine uptake in the periphery
MOA of L-dopa
Converted by decarboxylase to dopamine
5-HT can also convert
Absorbed in small intestine via transporters for aromatic amino acids
how can dyskinesia be lessened?
Amantadine also deep brain sleep
side effects of L-dopa
nausea, vomiting, sedation, hallucinations, nightmare, confusion, behavioral changes (impulse control disorders)
Orthostatic hypotension (bc of activation of vascular DA receptors)
front line drug for parkinson’s
L-dopa
Ropinirole
Pramipexole
dopamine receptor (D2) agonists
ropinirole
pramipexole
MOA of D2 receptor agonists
Full D2 agonists Longer duration than L-dopa (8-24hrs)
what class of drug is more effect for treating Parkinson’s?
dopamine precursor first then D2 agonists
anticholinergic drugs
biperiden
benzotropine
procylidine
trihexypehnidyl
MOA of anticholinergics
Blocks muscarinic Ach receptors Restore balance between dopamine and Ach in basal ganglia
MAO-B inhibitors
selegiline
rasagiline
MOA of MAO-B
Inhibits intracellular dopamine degradation
glutamate receptors (NMRA-R) blocker
amantadine
uses of Amantadine
aids in reducing L-dopa induced dyskinesia
MOA of glutamate receptors blockers
block dopamine uptake or stimulates release