04 CNS Review Alkana Flashcards
What is Parkinson disease pathology?
Striatal dopamine deficiency syndrome, less than 10% brain DA in basal ganglia (normally 80%)
What is Parkinson disease treatment designed to do?
Restore DA/ACh balance
What is the DOC for Parkinson Disease?
l-Dopa (plus peripheral decarboxlase inhibitor
What is the peripheral COMT inhibitor used?
Tolcapone
What is the DA potentiator used?
Amantadine
What is the DA receptor agonist used?
Bromociptine
What is the MOA-B inhibitor used?
Eldepryl
Parkinson Disease is believed to reflect destruction of what?
Dopaminergic cells in the substantia nigra
The therapeutic effects of l-dopa in PD results from increasing brain ______ and its action on ____ receptors?
Dopamine; D2
The mechanism of action of Pramipexole (Mirapex) in the treatment of PD is what?
Agonist action on D2 receptors
Classical antipsychotic medications are believed to produce their therapeutic effects by blocking what receptors?
D2
Classical antipsychotic medications are believed to produce many adverse effects by blocking what receptors?
D2
Atypical antipsychotic medications are believed to produce their therapeutic effects by blocking what receptors?
5HT2 (the thinking has shifted now to believe that its main mechanism is blocking D2)
Pseudoparkinsonism side effects from Haloperidol is most likely caused because of the blockade what receptors?
D2 receptors
What does traditional neurochemical theory propose that Schizophrenia is caused by?
Excess limbic dopaminergic (DA) function
What is the significant advantage of second generation antipsychotic agents?
Less EPS (<1% tardive dyskinesias)
What is the significant disadvantage of second generation antipsychotic agents?
Metabolic effects (weight gain; dyslipidemia, impaired glucose-insulin homeostasis)
For antipsychotic treatment, what two receptor binding may induce cascades that offset adverse effects and increase therapeutic effects?
Anticholinergic and 5HT2
The onset of therapeutic effects of atypical antidepressants corresponds best to?
Delayed autoreceptor desensitization and increase 5HT and/or NE
A primary therapeutic advantage of second generation vs. first generation antidepressants is?
Reduced affinity for mACh and adrenergic receptors (these are the receptors that cause the side effects, otherwise both generations are similar in their affinity for 5HT and NE transporters)
What happens with DA transporter blockade?
Associated with stimulant rather than antidepressant action
What are the three steps in therapeutic effect for antidepressants?
First (initial (acute): blocks reuptake of NE and/or 5HT via action on transporter protein). Second (compensatory change to offset blockade (downregulation of transmitter)). Third (delayed - autoreceptor desensitization, upregulation, increase synthesis and release of transmitter)
The anxiolytic lorazepam is thought to reduce anxiety by acting as an agonist on _____ receptors?
GABA** Slide 78
Benzodiazepines are believed to reduce the symptoms of anxiety by?
Potentiating GABAa receptors