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61 Cards in this Set
- Front
- Back
What are the major chemical subgroups of the older antipsychotics?
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phenothiazines (chlorpromazine, thioridazine, fluphenazine)
thiozanthenes (thiothizene) butyrophenones (haloperidol) |
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What are newer "second-generation" antipsychotic drugs?
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Heterocyclic structure including clozapine, loxapine, olanzapine, risperidone, quetiapine, ziprasidone, and aripiprazole
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Which antipsychotic drugs have parenteral forms that are used for rapid initiation and depot therapy?
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fluphenazine and haloperidol
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What are the 3 main reasons excess dopamine is thought to cause schizophrenia?
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1. Many antipsy drugs block D2
2. dopamine agonist drug exacerbate schizophrenia 3. increased dopamine receptors in schizophrenia patient |
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Which receptor do the older antipsychotic drugs work on? What is the negative side effect?
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1. D2 repector
2. blocking can cause extrapyramidal dysfunction due to D2 found at caudate putamen, nucleus accumbens, cerebral cortex, and hypothalamus |
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Which receptors does Clozapine act on?
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D4 and 5-HT2 receptor-blocking action
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Which receptors does atypical drugs (Olanzapine, quetiapine, and risperidone) act on?
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5-HT2A mainly and some D2
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Which receptors does Ziprasidone act on?
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ANTAGONIST at D2, 5-HT2A and 5-HT1D,
AGONIST 5-HT1A |
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Which receptors does Aripiprazole act on?
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partial agonist at D2 and 5-HT1A receptor,
strong ANTAGONIST 5-HT2A |
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With the exception of _____, all antipsychotic drugs block H1 receptor to some degree.
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HALOPERIDOL
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Which dopaminergic tract regulates mentation and mood?
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mesocortical-mesolimbic
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Which dopaminergic tract regulates extrapyramidal function?
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nigrostriatal pathway
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Which dopaminergic tract regulates control of prolactin release?
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tuberoinfundibular pathways
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Which dopaminergic tract regulates emesis?
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chemoreceptor trigger zone
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______ dopamine receptor blockade presumably underlies antipsychotic effects
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mesocortical-mesolimbic
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What are the positive symptoms of schizophrenia?
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hyperactivity, bizarre ideation, hallucinations, and delusions
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____ is effective in some schizophrenic patients resistant to treatment with other anytipsychotics drugs?
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Clozapine
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Newer atypical drugs are reported to improve some of the negative symptoms of schizophrenia, including ___, ___, and ___
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emotional blunting, social withdrawal and lack of motivation
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Which two antipsychotic drugs are used for maintence of bipolar disorder?
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olanzapine and aripiprazole
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____ is used mainly for Tourette's syndrome and rarely used in schizophrenia
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Molindone
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With the exception of ___, most phenothizines have antiemetic actions
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thioridazine
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Which phenothiazine is solely used for antiemetic actions?
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prochlorperazine
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____ blockade, most often present in short side-chain phenothiazines, provide the basis for their use as antipruritics and sedatives and contribute to antiemetic effects?
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H1 receptor blockade
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Extrapyramidal side effects most common with which antipsychotics?
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haloperidol and piperazine side-chain phenothiazines (fluphenazine and trifluoperazine)
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Neurologic dysfunctions akathisia and dystonias from antipsychotics can be treated with what 2 agents?
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diphenhydamine or muscarinic blocking agents
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What antipsychotic toxicity could be IRREVERSIBLE?
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Tardive dyskinesias - choreaoathetoid movements of the muscles of the lips and buccal cavity
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Treating extrapyramidal effects with antimuscarinic drugs may cause what side effect?
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INCREASE tardive dyskinesia
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How does increasing the neuroleptic dosage affect tardive dyskinesias?
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TEMPORARILY decrease suggesting tardive dyskinesia may be caused by dopamine receptor sensitization
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Which antipsychotic drug has the STRONGEST autonomic effect? WEAKEST?
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Strongest- Thioridazine
Weakest- Haloperidol |
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___ and most the atypical drugs have intermediate autonomic effects?
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Clozapine
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Which two antipsychotics drugs do NOT have atropine side effects?
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ziprasidone and aripiprazole
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Which antipsychotics have the most atropine (dry mouth, constipation, urinary retention, and visual problems) side effects?
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Thiordiazine and phenothiazines with aliphatic side chains (chlorpromazine)
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Which antipsychotics are known to cause postural hypotension caused by A-blockade
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older antipsychotics such especially phenothiazines
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Which antipsychotics can cause orthostatic hypotension?
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atypical drugs
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Failure to ejaculate is common in men treated with ___
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phenothiazines
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What are the main endrocrine and metabolic side effects of antipsychotics?
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hyperprolactinemia, gynecomastia, the amenorrhea-galactorrhea syndrome and infertility
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Which antipsychotic has prominent elevated prolactin side effect?
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Resperidone
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Significant weight gain and hyperglycemia due to a diabetogenic action occur with several of the atypical agents, especially ___ and _____
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clozapine and olanzapine
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Which two antipsychotic drugs has little or no tendency to cause hyperglycemia, hyperprolactinemia, or weight gain?
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Aripiprazole and ziprasidone
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Drugs used to treat malignant hyperthermic syndrome of antipsychotic drugs?
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dantrolene, diazepam, and dopamine agonist
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What is the most sedating antipsychotic drug?
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phenothiazines especially CHLORPROMAZINE
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Which two of the older antipsychotics are least sedating?
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fluphenazine and haloperidol
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Which newer antipsychotic is least sedating?
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aripiprazole
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Visual impairment caused by retinal deposits has occurred with ___, at high does, this drug may also cause severe conduction defects in the heart resulting in fatal ventricular arrhythmias
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thioridazine
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Most atypicals, especially ___, prolong QT interval of the ECG; the underlying myocardial effect may lead to cardiac arrhythias (torsades)
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Ziprasidone
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____ causes small but important (1-2%) incidence of agranulocytosis and at high doses has caused seizures
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Clozapine
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Most neuroleptics lower the convulsive threshold and may cause seizures which are treated with ___ and ___
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diazepan or phenytoin
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Target therapeutic plasma concentration for Lithium is ___
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0.8-1.2 mEq/L and for maintenance 0.4-0.7 mEq/L
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What drugs can cause a increase of Lithium in the blood to toxic levels?
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Thiazides, NSAIDS, ACEIs, loop diuretics and also Dehydration
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___ and ___ increase the renal clearance of lithium
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Caffeine and theophylline
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MoA of Lithium
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inhibits inositol monophosphatase, rate limiting enzyme for generation of IP3 and DAG in 2nd messenger amine neurotransmission
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____ continues to be the standard treatment of bipolar disorder
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Lithium carbonate
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Acute mania can be treated with what 3 drugs?
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Lithium, valproic acid and olanzapine
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What drugs are required for the initiation of bipolar treatment?
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Antipsychotics and/or benzodiazepines due to slow onset of lithium and valproic acid
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Other then lithium, what drugs can be used in the maintenance of bipolar disorder?
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Aripiprazole and olanzapine, as well as anticonvulsants carbamazepine and lamotrigine
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Adverse neurologic effects of lithium include ___, ___, __ and ____. ___ enlargement may also occur
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tremor, sedation, ataxia and aphasia. Thyroid
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____ kidney problem occurs commonly at therapeutic lithium levels
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Reversible nephrogenic diabetes insipidus
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What skin problems can occur with lithium therapy?
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Edema and acneiform skin eruptions
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What side effect is ALWAYS present with lithium therapy?
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Leukocytosis
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The use of Lithium during pregnancy is thought to increase the incidence of ____
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congenital cardiac anomalies (Ebstein's anomaly)
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Can nursing mothers use Lithium?
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NO, should even stop 24-48 hours before delivery
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