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Glossary of Pharmacology - Antipsychotics

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What causes the positive and negative signs of schizophrenia?
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?
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?
muscular rigidity, fever, diaphoresis, myoglobinuria, metabolic acidosis; catatonia
treat with dantrolene or bromocriptine
Conventional antipsychotics include what three main groups?
PHEnothiazines, THioxanthenes, BUtyrophenones
*PHEed THe BUrds
Phenothiazines have three groups of their own. What are they? Name some examples.
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?
haloperidol
*High potency and High EPS
lithium (-> encephalopathy and fever)
Which symptoms of schizophrenia do conventional neuroleptics treat (+ or -)? What about atypicals?
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?
lithium
carbamazepine, valproic acid - maintenance
clonazepam - adjuvant
olanzapine

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