Kaplan Section 4 Chapter 1 CNS Pharm - Antipsychotic Drugs
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| Name the positive symptoms of schizophrenia | 1. thought disorders 2. delusions 3. hallucinations 4. bizarre behavior
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| Name the negative symptoms of schizophrenia | 1. amotivation 2. social withdrawal 3. flat affect 4. poverty of speech
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| What is the dopamine hypothesis for schizophrenia | excess DA in the CNS
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| drugs that activate DA receptors cause what type of sx's? | psychotic sx's
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| drugs that antagonize DA receptors cause what type of sx's? | antipsychotic actions
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| anti-psychotic drugs block 3 types of receptors -- what are they? | D2a, M (atropine-like effects), and a (postural HTN, sexual dysfxn)
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| what are neuroleptics? | antipsychotic drugs
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| what are the effects of low potency vs. high potency antipsychotic drugs? | Low potency (chlorpromazine, thioridazine) -- 100s of mg range --> cause more autonomic dysfxn. High potency (fluphenazine, haloperidol) -- 10 to 50 mg range --> cuase more extrapyramidal side fx (less autonomic dysfxn).
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| what do haloperidol, pimozide, and high-potency phenothiazines have in common? | all have most intense DA receptor block --> reversible pseudo Parkinsonism (bradykinesia, rigidity, tremor), akathisia, acute dystonic rxns
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| What is dystonia? | sustained muscle contractions cause twisting and repetitive movements or abnormal postures
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| What is akathisia? | unpleasant sensations of "inner" restlessness that manifests itself with an inability to sit still or remain motionless
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| How do you fix acute dystonias? | Some may respond to botulinum toxin
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| What antipsychotic drugs are least likely to cause extrapyramidal dysfxn? | newer drugs: clozapine, olanzapine because don't block D2a receptors. They are 5HT2 receptor antagonists (serotonin).
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| Drugs that cause extrapyramidal dysfxn also cause what? | Block DA receptors in the pituitary --> inc prolactin --> endocrine dysfxn --> gynecomastia & amenorrhea-galactorrhea
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| Chlorpromazine, thioridazine, & fluphenazine -- what class of drugs? | antipsychotics, DA receptor antagonists
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| what is risperidone? | newer antipsychotic drug that blocks 5HT2 receptors
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| Chlorpromazine | antipsychotic; prototype penothiazine; low potency
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| Thioridazine | antipsychotic; penothiazine; low potency
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| Fluphenazine | antipsychotic; penothiazine; high potency
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| Haloperidol | antipsychotic; butyrophenone; high potency
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| what receptors does clozapine block? | D2c and 5HT2
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| Why do people on clozapine have to have weekly blood tests? | the drug can cause agranulocytosis
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| Does clozapine cause extrapyramidal dysfunction? | no
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| Olanzapine | blocks 5HT2 receptors; improves negative sx's
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| Risperidone | blocks 5HT2 receptors; improves negative sx's; possible tardive dyskinesia
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| Which antipsychotic causes weight gain? | Clozapine
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| Which antipsychotic causes ocular dysfxn? | chlorpromazine
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| Which antipsychotic causes retinal deposits and cardiotoxicity (torsades - quinidine-like)? | thioridazine
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| Which antipsychotic can be given with long-acting depot forms? | haloperidol
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| Aripiprazole | Partial agonist of D2 receptor; blocks 5HT2 receptor
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| What is tardive dyskinesia? | choreoathetoid-like muscle movement associated with long-term use to DA blockers (esp haloperidol and high-potency phenothiazines)
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| Can tardive dyskinesia be reversed by stopping intake/administration of the DA blocker? | not readily
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| Should people with tardive dyskinesia be given M blockers? | no - will make the TD worse
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| Which two drugs have there been no reports of tardive dyskinesia? | Clozapine and olanzapine (5HT2 receptor blockers)
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| What is neuroleptic malignant syndrome? | life-threatening; extreme muscle rigidity, hyperthermia, CV instability, altered consciousness, enhanced sensitivity of DA receptors to blocking agents
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| How would you treat neuroleptic malignant syndrome? | bromocriptine (DA agonist) and dantrolene (muscle relaxant, treats malignant hyperthermia) + sx management
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| For which diseases would you use anti-psychotics? | schizophrenia, schizoaffective states, bipolar disorder, tourette syndrome, preoperative sedation, drug/radiation emesis, neurolept anesthesia (partially conscious)
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| How long does it take a schizophrenic patient to respond to drug therapy? | several weeks
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| What drug would you use for Tourette Syndrome? | DOC: Pimozide (intense DA receptor antagonist)
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| What drug would you use for preoperative sedation? | promethazine (minimal antipsychotic activity); H1 blocker; sedative
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| What drug would you use for drug/radiation emesis? | Proclorperazine
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| What three drugs would you use for neurolept anesthesia? | droperidol, fentanyl, nitrous oxide
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