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USMLE - Pharm

Kaplan Section 4 Chapter 1 CNS Pharm - Antipsychotic Drugs

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
Created by: christinapham