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50 Cards in this Set
- Front
- Back
what is necessary and sufficient characteristic of an effective antipsychotic drug?
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D2 blockade is a necessary and sufficient characteristic of an effective antipsychotic drug
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what is haloperidol?
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antipsychotic with D2 blocakde effect
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what pathways should be blocked to alleviate positive symptoms?
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mesolimbic (feeling)
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blockade of what pathways would aggrevate negative or cognitive symptoms?
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mesocortical (thinking)
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in what area of the brain is dompamine an inhibitor of prolactin release?
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Tuberoinfundibular (endocrine) which tract between from hypothalamus to pituitary
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which pathway, when blocked, leads to the neurological symptoms seen with a high dosage of a D2 blocking medication (antipsychotic)?
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Nigrostriatal
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Clinical response occurs at what percentage of striatal D2 receptor blocking?
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65%
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Hyperprolactinemia occurs at what percentage of striatal D2 receptor blocking?
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72%
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Neurological symptoms occur at what percentage of striatal D2 receptor blocking?
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78%
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Describe the theapuetic window for antipsychotic drugs?
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Very normal with slightly increased doses leading to first hyperprolactinemia and the neurological symptoms
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describe inmprovements from the older typical antipsychotics to the newer atypical antipsychotics?
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the newer ones are really better for + symptoms, but tend to be better for negative symptoms (because of more selectivity in D2 blockade)
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which has a higher likelyhood of causing neurological symptoms? typical or atypical antipsychotics?
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typical
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which has a higher likelyhood of causing metabolic symptoms? typical or atypical antipsychotics?
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atypical
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what is the common interaction that all atypical antipsychotics share?
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5HT2a antagonism
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why is the 5HT2a antagonist effect of atypical antipsychotics beneficial?
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it causes increased dopamine release in areas where there are serotonin receptors which can offset the D2 blockage effects of antipsyochotics in the Nigrostriatal, and Tuberoinfundibular mesocortical pathways reducing negative symptoms and alleviating other side effects (EX Neurological effects and hyperprolactinemia)
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what is the most effective drug in the drug resistant, psychotic patient?
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clozapine
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which of the antipsychotics has the weakest D2 blockade?
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clozapine
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what two behavioral changes are seen in patients who undergo therapy with clozapine?
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1. reduced suicidality
2. reduced substance abuse |
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why isnt clozapine a first line drug in the treatment of psychotic disorders?
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it has significant toxicity
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describe the unique pharmacology of aripiprazole?
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it is a partial agonist at D2 receptor thus it decreases activity of dopamine in dopamine rich areas (decreasing psychosis) and increases dopamine activity in dopamine poor areas (decreasing side effects)
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how long does it take an antipsychotic to show noticeable effects?
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weeks
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what effects to antipsychotics cause that can reduce that chronicity and severity of psychiatric disorders like schizophrenia?
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1. promote neurogenesis
2. neuroprotective/neurotropic |
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what is the best way to improve the prognosis of someone with a psychiatric disorder (EX schizophrenia)?
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Get them on antipsychotic drugs ASAP
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what is a tardive syndrome (in reference to the use of antipsychotics)
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an extra-parametal symptoms (EPS) which starts late in treatment and may not regress after treatment is stopped
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what are the 3 types of acute EPS?
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1. Dystonic reaction
2. Parkinsonism 3. Akathisia |
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which of the three types of acute EPS is described below?
is an acute-onset muscle spasm which may involve almost any muscle groups. Most notorious are those that involve back (opisthotonus) or neck (torticollis or retrocollis) muscles, extraocular muscles (oculogyric crisis), and even pharyngeal or laryngeal (which may be life-threatening) muscles Assoc. w/ young age, male sex, IM Rx |
Dystonic reaction
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what is the best treatment for a dystonic reaction?
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anticholinergic
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which of the three types of acute EPS is described below?
may include muscle rigidity, tremor, bradykinesia, drooling, mask-like facies, and flattened affect. Associated with older age, prior brain injury |
Parkinsonism reaction
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what is the DOC for a parkinsonism reaction (acute EPS) with a antipsychotic?
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Amantidine (anticholinergic)
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what acute EPS does the following describe?
is a state of motor restlessness that may be expressed subjectively (feeling unable to relax; impulsive feelings or behaviors) or objectively (fidgety or hyperactive motor behavior) is the most common acute EPS |
akathisia
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what two drug classes can be used to alleviate symptoms of Akathisia (acute EPS)?
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1. Beta-blocker
2. Anticholingergic |
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what are the three types of tardive syndromes?
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Tardive dyskinesia, akathisia, and dystonia
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what causes the formation of tardive syndromes
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D2 upregulation
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for every year of taking a typical (older generation)neuroleptic what is your risk for developing a tardive syndrome?
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4-5%
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what are the risk factors that increase the likelyhood of developing a tardive syndrome? (3)
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1. Age: elderly up to 10X risk
2. Sex: women > men (modest effect) 3. Mood disorders? Myth vs fact? Evidence base fuzzy |
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what is the greatest risk factor for developing tardive dyskinesia?
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AGE AGE AGE :)
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describe the risk per year for atypical antipsychotics in developing a tardive syndrome?
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.5-1%
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which two atypical antipsychotics have almost no risk of tardive syndrome formation?
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1. Quetiapine
2. Clozapine |
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Galactorrhea; breast swelling and tenderness; sexual inhibitions (desire, response)
are mediated by which effects of antipsychotic drugs? |
D2 blockade in the Tuberoinfundibular (endocrine) pathways
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These symptoms are most likely due to which syndrome caused by psychotic drugs?
Rigidity, hyperpyrexia, dysautonomia, mental status changes Lab: Increased CK, WBC Incidence 1-2%; mortality 5-20% |
Neuroleptic malignant syndrome
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which drugs are more likely to cause Neuroleptic malignant syndrome, first or second generation antipsychotics?
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first generation
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what are two drug therapies for Neuroleptic malignant syndrome?
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1. dantrolene - muscle relaxent
2. bromocriptine - dopaminergic |
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what is the most effective treatment for Neuroleptic malignant syndrome?
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ECT
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what is the thing that must be monitered every week when taking an antipsychotic, esp. clozapine?
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CBC
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These 4 "black box" symptoms are indicative of cardiovascular side-effects of which antipsychotic drug?
1. agranulocytosis 2. seizures 3. myocarditis 4. orthostatic hypotension/respiratory depression, esp. if coadministered a benzodiazepine |
clozapine
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which antipsychotic is particulary associated with myocarditis?
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clozapine
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why do you tell patients taking antipsychotics to be very careful when outside on a sunny summer afternoon?
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antipsychotics cause photosensitivity, but more importantly it impairs thermoregulation which can cause them to get heat stroke much faster than a normal person
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most drug interactions of antipyschotics occur because of?
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actions upon metabolic enzymes (P450)
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what are two drugs that are general inducers of antipsichotic interactions?
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1. phenytoin
2. phenobarbitol |
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what class (in regards to danger for developing fetus) are all antipsychotics?
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Class C - indicates there may be a small risk for use in pregnant women, but use anyway if benefit is large
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