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