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47 Cards in this Set
- Front
- Back
drug that was major factor to significant increase in discharge of mental patients?
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chlorpromazine
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prototype phenothiazine?
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chlorpromazine
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differences between high to low potency phenothiazines?
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high potency have high incidence of extrapyramidal side effects but lower incidence of anticholinergic and antiadrenergic side effects conpared with low-potency phenothiazine; have roughly the same therapeutic efficacy
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CNS effects of phenothiazines?
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sedation, calming effect;
anti-emetic; impairment of temp regulating system; neuroendocrine effects (hyperprolactinemia); decreased seizure threshold |
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which class of phenothiazines are ANS effects most often seen?
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low potency
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ANS effects of phenothiazines?
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block M receptors;
block α receptors |
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phenothiazines mechanism of action?
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inhibit DA neurotransmission in CNS by blocking postsynaptic receptor sites in the limbic system
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phenothiazine side effects?
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orthostatic hypotension;
obstructive jaundice; blood dyscrasias; extrapyramidal reactions |
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extrapyramidal reactions associated with phenothiazines?
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parkinsonian syndrome;
akasthisia; neuroleptic malignant syndrome; dystonias; tardive dyskinesia |
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neuroleptic malignant syndrome?
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typically after IM dose of haloperidol;
onset in 30 mins, symptoms may persis 3-4 weeks; muscle rigidity, hyperthermia |
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chlorpromazine?
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less potent phenothiazine
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thioridazine?
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potent phenothiazine
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fluphenazine?
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more potent phenothiazine
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dystonias?
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appears late with chronic, long term treatment with phenothiazines;
prolonged abnormal contractions of the neck, tongue, and mouth muscles |
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tardive dyskinesia?
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after month or years of phenothiazine therapy;
rhythmic, involuntary movements of tongue, lip smaking, abnormal postures and involuntary limb movements; exacerbated by rapid withdrawal of drug; symptoms may persist long after withdrawal |
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phenothiazine drug interactions?
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potentiates anticholinergics;
potentiates other CNS depressants; potentiates adrenergic blocking antihypertensives |
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other antipsychotic drugs?
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haloperidol
molindone thiothixene (chemically distinct from phenothiazines but have similar therapeutic and side effect profiles) |
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haloperidol?
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resembles high potency phenothiazines;
high incidence of EP side effects; few ANS side effects |
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molindone?
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antipsychotic;
high incidence of EP side effects; possible antidepressant activity |
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thiothixene?
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resembles low potency phenothiazines
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atypical antipsychotic mechanism of action?
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greater occupancy at 5-HT receptors relative to D2 receptors;
selectively block DA receptors on mesolimbic neurons rather than nigrostriatal neurons |
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atypicals main advantage over phenothiazines?
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low incidence of EP side effects
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phenothiazines are generally more effect for which symptoms of schizophrenia?
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positive symptoms
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main side effect of clozapine?
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agranulocytosis
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clozapine (clozaril)?
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atypical antipsychotic
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clozapine mechanism?
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weak blocker of D1 and D2 receptors;
5-HT receptor; α1 receptor (relatively weak); M receptor (relatively weak); H1 receptor (relatively weak) |
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side effects of clozapine?
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sedation, hypotension, tachycardia, fever, increased salivation, dizziness, weight gain;
more prominent with dose escalation |
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olanzipine (zyprexa)?
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atypical antipsychotic;
also approved for use in mania |
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olanzipine mechanism?
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similar to clozapine without wbc problems;
higher affinity for D2; lower affinity for 5-HT2; blocks Ach |
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respiridone (risperdol)?
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atypical antipsychotic;
recommended in first episode of schizophrenia where negative symptoms predominate |
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which atypical antipsychotic produces agranulocytosis?
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clozapine
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contraindications for respiridone?
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arteriosclerotic cardiovascular disease
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which atypical antipsychotic is contraindicated in ateriosclerotic cardiovascular disease?
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respiridone
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respiridone mechanism?
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potent blocker of D2 receptors and 5-HT2 receptors
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quetiapine (seroquel)?
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atypical antipsychotic;
monotherapy for bipolar mania |
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major side effect of quetiapine?
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marked somnolence
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quetiapine mechanism?
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potent 5-HT2 antagonist;
moderate D2 antagonism; (also 5-HT1, D1, H1,α1, α2 antagonist) |
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ziprasidone (geodon)?
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atypical antipsychotic
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major side effect of ziprasidone?
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fatal cardiac arrythmias
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which atypical antipsychotic is associated with fatal cardiac arrythmias?
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ziprasidone
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aripirazole (abilify)?
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atypical antipsychotic
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theories for mechanism of schizophrenia?
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DA overstimulation;
hypofunctional NMDA receptor |
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antipsychotic therapeutic indications?
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schizophrenia;
bipolar with psychotic features; Tourettes; disturbed behavior in dementia; antiemetic; preoperatively for neuroleptic anesthesia |
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glycine and schizophrenia?
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coagonist with glu at NMDA;
large doses reported to improve negative symptoms |
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d-cycloserine?
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glycine partial agonist for stimulation of NMDA
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evidence supporting hypofunctional NMDA receptor theory?
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blockade induces schizophrenia symptoms;
SNPs in subset of schizophrenics results in reduced glu binding |
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future directions for antipsychotic therapy?
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NMDA superagonists;
gly transporter inhibitors |