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Antipsychotic Medications
Drugs that prevent the craziness!
44
Medical
Graduate
11/02/2012

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Cards

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
Less specific drugs
Term
What neurotransmitters are involved in the pathogenesis of schizophrenia?
Definition
Dopamine
Glutamate
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
GPCRs

Coupled to Gi
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
Emesis and nausea
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
Months
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
Haloperidol
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
60-80

More than 80
Term
What other receptor types do the SGAs bind to?
Definition
Serotonin reeptors
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
Relapse in psychosis
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
P450's
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
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