Neurodegenerative diseases Flashcards
(44 cards)
Drug classes in treatment for Alzheimees
- Cholinesterase Inhibitors
- NMDA receptor Antagonist
Cholinesterase inhibitors
- Donepezil (Aricept)
- Rivastigmine (Exelon)
- Galantamine (Razadylne)
NMDA receptor antagonist
Memantine (Namenda)
Mechanism of action for cholinesterase inhibitors
- Prevents action of acetylcholinesterase
- this increases acetlycholine in the synapse
Nausea
Bronchospasm
Cholinesterase inhibitors
Headache, Dizziness, Diarrhea
Cholineaterase inhibitors
and
NMDA receptor antagonists
- sedation
- fatigue
- hypertension
- rash
- weight gain
- urinary frequency
- anemia
NMDA receptor antagonists- Memantine
Memantine (Namenda) mechanism of action
- Block leaky channels to reduce calcium induced excitotoxicity
- Block leaky channels to reduce background noise and make signals relatively stronger
- Blocks the pathalogical activation of NMDA receptors
What is drug therapy for parkinsons aimed at
increasing dopamine or decreasing Acetylcholine to balance the two
Three mechanisms of action of dopiminergic agents
- increase amounts of dopamine in th Striatum
- incresed delivery or decreased degredation of dopamine
- Mimic the effects of dopamine - dopamine agonists
what is the mechanism of action of anticholonergic agents
Prevent cholonergic inhibition of dopamine release
First line of therapy for Parkinsons
Levadopa
80% of paitines show improvement, and 20% Regain normal function with levadopa therapy, but what else is very improtant about this therapy
Its effects wer off over time (2-3 years) likely due to advanced neuro degeneration
Levadopa mechanism of action
levadopa is converted to dopamine increasing dopamine in the striatum
Levadopa is converted to ____________providing dopamine in the striatum, this happens in the _________________. Levadopa is only needed in the _________ and large amounts of levadopa in the __________ causes problems. This is why Levadopa is dosed with ___________ a ________________ and ___________a ___________ which causes sthe same amount of Levadopa to reach the brain with a ____________ dose. ___________ is added when ________________ wanes.
- dopamine
- periphery and the brain.
- brain
- periphery
- Carbadopa a peripheral decarboxylase inhibitor
- Entacopne a COMT inhibitor
- smaller
- Entacapone
- Levadopa/Carbadopa
Acute side effects of Levadopa
Disappear after a few week s and include nausea, anorexia and hypotension
Sede effects of Levadopa
- involutary movements
- on-off effects (hypokinesia and improvements)
- Psychosis - schizophrinia like symptoms with excess domamine
Adverse drug interaction with Levadopa
MAO Inhibitors- will cause an overload of dopamine and NE
Levadopa when given alone is degraded by
Mosty decarboxylases and a little by COMT causing ittle to get to the brain
When levadopa is given with a DDC inhipibitor (Decarboylase inhibitor) ____________.
Dopamine is still broken down by COMT and not as much gets to the brain
Optimization of levadopa happens when
Levadopa is given with a DDC inhibitor and a COMT inhibitor - this allows for the most amount of the drug to get to the brain
Dopamine agonists
Pramipexole and Ropinirole
Highly selective for D2/D3 receptors
Pramipexole and Ropinirole
may cuase halucinations and compulsive behaviors
Pramipexole and Ropinirole