Pharmacology - Antipsychotics
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- What causes the positive and negative signs of schizophrenia?
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Positive: hyperdopaminergic activity in the mesolimbic system
Negative: hypodopaminergic activity in the mesocortical system - How do antipsychotics (neuroleptics) work?
- they block dopamine receptors in mesolimbic and mesocortical areas (esp. D2 and D4)
- Blockade of dopamine in other areas can cause side effects. What other areas do antipsychotics affect and what side effects can occur?
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basal ganglia -> movement disorders
hypothalamus and pituitary -> increased prolactin secretion
chemoreceptor trigger zone -> inhibition of emesis - For which receptor do atypical antipsychotics have a higher affinity? What benefit does that give them?
- 5HT2; they're less likely to cause extrapyramidal symptoms
- When are antipsychotics used?
- schizophrenia, severe manic or agitated episodes, for certain drug overdoses (amphetamines), some for nausea and vomiting, intractable hiccups, and Tourette syndrome
- What causes extrapyramidal side effects? What are the features? What is the treatment?
- Cholinergic overactivity from dopamine blockade; Parkinsonian syndrome, akathisia (restlessness and increased motor activity), acute dystonic reactions, tardive dyskinesia (involuntary movements); anticholinergics (like benztropine)
- What is neuroleptic malignant syndrome? What is the treatment?
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muscular rigidity, fever, diaphoresis, myoglobinuria, metabolic acidosis; catatonia
treat with dantrolene or bromocriptine - Conventional antipsychotics include what three main groups?
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PHEnothiazines, THioxanthenes, BUtyrophenones
*PHEed THe BUrds - Phenothiazines have three groups of their own. What are they? Name some examples.
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ALiphatic: Chlorpromazine, Triflupromazine
*ACT - Low potency, Low EPS, high anticholinergic and anti-alpha-adrenergic
PiperiDine: thioridazine
*Pipe Down! thioridazine is moderate potency and has a low incidence of EPS, BUT high anticholinergic and anti-alpha-adrenergic
PiperAzine: fluphenazine, trifluoperazine, prochlorperazine
*Pipe Ap (up)! piperazine has a high potency and high EPS with lower autonomic effects - What are some examples of thioxanthenes? One of them causes a specific side effect. What is it?
- thiothixene, chlorprothixene - lenticular deposits
- What is an example of a butyrophenone? What drug should it not be used with?
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haloperidol
*High potency and High EPS
lithium (-> encephalopathy and fever) - Which symptoms of schizophrenia do conventional neuroleptics treat (+ or -)? What about atypicals?
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conv = positive
atyp = both - Name some atypical neuroleptics.
- clozapine, risperidone, olanzapine, qeutiapine, sertindole
- What are the side effects of clozapine?
- agranulocytosis, anticholinergic, sedation, orthostatic hypotension, weight gain
- What is good about clozapine?
- low EPS, may improve tardive dyskinesia, lower risk of suicide
- How is risperidone different from clozapine?
- higher EPS, less anticholinergic, less orthostatic hypotension, less weight gain
- What are the side effects of olanzapine?
- very low EPS, high sedation, anticholinergic, ortho hypo, and weight gain
- What are the side effects of qeutiapine?
- very low EPS, moderate sedation, moderate ortho hypo, low weight gain, NO anticholinergic
- What risk of sertindole led to its removal from market?
- prolongation of QT interval
- If a drug has few EPS and high other side effects, is it high potency or low potency?
- low
- What are the treatments for bipolar disorder?
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lithium
carbamazepine, valproic acid - maintenance
clonazepam - adjuvant
olanzapine