Term
What is the main mechanism of antipsychotic activity in antipsychotic drugs? |
|
Definition
Reducing dopaminergic activity via the blocking of D2 dopamine receptors |
|
|
Term
What kinds of drugs have more motor side effects? |
|
Definition
Drugs that have a high specificity for D2Rs have more extrapyramidal (motor) side effects than less specific |
|
|
Term
What kinds of drugs have more motor and autonomic side effects? |
|
Definition
|
|
Term
What neurotransmitters are involved in the pathogenesis of schizophrenia? |
|
Definition
|
|
Term
What ennzyme is responsible for the breakdown of dopamine? |
|
Definition
MAO Catecholamine-O-methyltransferase |
|
|
Term
What transporters does cocaine interact with in the brain? What does it do? |
|
Definition
D2 transporters on postsynaptic cels
Blocks dopamine reuptake |
|
|
Term
What transporters does amphetamine act on in the brain? What does it do? |
|
Definition
D2 transporters on post-synaptic cells
Causes cocaine to go o |
|
|
Term
What type of a receptor is the D2 receptor family? |
|
Definition
|
|
Term
Overall, what is the activity of D2 receptor family? |
|
Definition
Decreased cAMP Increased K conductance Decreased C conductance
Overall, hyperpolarizes the cell |
|
|
Term
What is the function of the ventral tegmentum in dopamine neuroanatomy? |
|
Definition
Involved in the mesolimbic, mesocortical system
It's a part of the reward system pathway |
|
|
Term
What is the function of the mesocortical pathway? |
|
Definition
Cognition
Thoughts and actions orchestrating with internal goals |
|
|
Term
What is the function of the mesolimbic pathway? |
|
Definition
Complex reward-oriented behavior |
|
|
Term
What is the function of the negrostriatal pathway? |
|
Definition
Motor planning, habit formation, memory
Degenerates in parkinson's |
|
|
Term
What is the function of the tuboinfundibular pathway? |
|
Definition
Tonic inhibition of prolactin release
Increase growth hormone release |
|
|
Term
What is the function of the chemoreceptor trigger zone? |
|
Definition
|
|
Term
What symptoms of schizophrenia are antipsychotics effective at treating? |
|
Definition
Positive symptoms
NOT THE NEGATIVE ONES! |
|
|
Term
How is glutamate involved in the pathogenesis of schizophrenia? |
|
Definition
Decreased activity (which is to say, less excitement)going into the limbic region |
|
|
Term
What is the effect of reducing glutamate on psychosis? |
|
Definition
Makes the psychosis worse |
|
|
Term
What is the treatment for reduced glutaminergic activity in the brain in schizophrenia? |
|
Definition
Give an NMDA (channel for glutamate) agonist |
|
|
Term
How long does it take for the antipsychotic drugs to start working? |
|
Definition
|
|
Term
What is the typical way that you'll prescribe medications for schizophrenia? |
|
Definition
First: 'atypical' antipsychotics Second: conventional, old-line drugs Last: Clozapine |
|
|
Term
What are some of the 'atypical" antipsychotic drugs? When do you prescribe them? |
|
Definition
Olanzapine Apripiprazole Risperidone |
|
|
Term
What is an example of a conventional old-line drugs used for antipsychosis? |
|
Definition
|
|
Term
Why is clozapine prescribed last when giving antipsychotic drugs? |
|
Definition
It has the most severe side effects |
|
|
Term
What makes an antipsychotic drug more porent? |
|
Definition
How well it binds to the D2 receptors |
|
|
Term
What kinds of receptors does chlorpromazine bind to? |
|
Definition
H1 receptors: it's a sedative Alpha adrenergic: it causes hypotension D2 |
|
|
Term
If something binds specifically to D2 receptors, what kinds of side effects result? |
|
Definition
Lots of extrapyramidal problems |
|
|
Term
What is the specificity of haloperidol to D2Rs? |
|
Definition
VERY HIGH.
LOTS OF EXTTRAPYRAMIDAL SYMPTOMS |
|
|
Term
What are the unique properties of aripiprazole? |
|
Definition
Partial dopamine agnoist!
You're still allowing some activity, but you're stopping there from being too many effects |
|
|
Term
What is one large difference between the fist and second generation antipsychotic drugs? |
|
Definition
First generation have much fewer extrapyramidal symptoms |
|
|
Term
What is the ideal receptor occupancy for the antipsychotic drugs? When do you start to get extrapyramidal symptoms? |
|
Definition
|
|
Term
What other receptor types do the SGAs bind to? |
|
Definition
|
|
Term
What kinds of tolerance do or don't develop in antipsychotic drugs? |
|
Definition
Sedative effects are tolerated No tolerance to: prolactin, antipsychotic effect |
|
|
Term
What is the effect of rapidly discontinuing antipsychotic drugs? |
|
Definition
|
|
Term
What is the dosing of antipsychotic drugs? |
|
Definition
One pill/day
There's a half-life of 6-40 hours |
|
|
Term
What enzymes metabolize the antipsychotic drugs? |
|
Definition
|
|
Term
What are the drugs interteractions of the antipsychotic drugs? |
|
Definition
They're CNS depressants, so the effects potentiate
Block effects of DOPA agonists |
|
|
Term
What are the endocrine side-effects of the antipsychotic drugs? |
|
Definition
amenorrhea Galactorrhea Infertility Impotence |
|
|
Term
What are some of the metabolic side effects of the antipsychotic drugs? |
|
Definition
Weight gain High lipids High glucose Diabetes |
|
|
Term
What are some of the ANS side effects of antipsychotic drugs? |
|
Definition
Muscarinic cholinergic blockade: -Loss of accomodation -Dry mouth -Difficulty urinating -Constipation
Alpha-adrenergic receptor blockade -Orthostatic hypotension -Impotence -Failure to ejaculate |
|
|
Term
What kinds of antipsychotic drugs cause the most severe side effects? |
|
Definition
Olanzapine Clozapine Chlorpromazine |
|
|
Term
How are extrapyramidal side effects manifest? |
|
Definition
Acute dystonia Akathisia Parkinsonism Tardive dyskinesia |
|
|
Term
What are the co-agonists of the NMDA receptor? What is their use? |
|
Definition
Glycine D-serine
Antipsychotic |
|
|
Term
What are blockers of the NMDA channel? How do they block it? |
|
Definition
Phencyclidine Ketamine
Noncompetitive antagonists |
|
|