Anti- Psychotic
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| besides schizophrenia and related disorders, what two things are some antipsychotics prescribed for | 1) "manic" phase of bipolar disorder; 2) anti-emetics
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| what are the three groups of schizophrenia symptoms | 1) positive; 2) negative; 3) cognitive
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| what are the four general findings that implicate dopamine and dopamine receptors in schizophrenia | 1efficacy of drugs corresponds to affinity for drug at dopamine receptors 2drugs that increase dopamine levels can precipitate psychotic sx 3DA-R density in post-mortem tissue is higher in schizophrenic people 4) PET scans show increased dopamine R
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| how many dopamine receptor types are there, and what is their structure like | five types, all are G-protein coupled receptors
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| what are the two classes of DA receptors, and which class stimulates / inhibits | two classes: D1 like (stimulatory); D2 like (inhibitory)
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| what are the D1-like and D2-like receptors | D1-like: D1 and D5; D-2-like: D2, D3, and D4
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| what second messenger pathway do dopamine receptors act on | cAMP --> PKA
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| what typical antipsychotics must we know (2) | 1) haloperidol; 2) chlorpromazine
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| what atypical antipsychotics must we know (5) | 1) clozapine; 2) risperidone; 3) olanzapine; 4) quetiapine; 5) ziprasidone
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| what are atypical antipsychotics effective at doing, and for what purpose are they less effective | very potent at relieving positive symptoms of schizophrenia, but much less effective at relieving the negative symptoms
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| what serious type of side effects do they commonly cause | extrapyramidal disturbances
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| what disease are these symptoms like, and what are three extrapyramidal symptoms mentioned | Parkinson-like symptoms: 1) tremor; 2) dystonia; 3) tardive dyskinesia
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| what is usually the limiting factor for typical antipsychotic therapy | intolerable levels of tardive dyskinesia
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| what is tardive dyskinesia, and where in the body does it occur (2) | tics, especially in: 1) face; 2) neck muscles
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| what is particularly devastating about some cases of extrapyramidal effects | irreversible
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| what is potency for alleviating positive symptoms proportional to (specific) | drug's affinity for D2-type dopamine receptors
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| what else is proportional to this | propensity to cause extrapyramidal disturbances
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| what are two advantages of atypical antipsychotics | 1) less extrapyramidal disturbances; 2) may have efficacy in treating negative symptoms (as well as alleviating positive symptoms)
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| how does affinity to D2 receptors compare to typical agents | lower
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| what may the lower incidence of extrapyramidal side effects be due to actions on (2 and/or) | 1) 5HT receptors' 2) muscarinic acetylcholine receptors
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| what autonomic adverse effects are listed (list) | loss of accomodatoin, dry mouth, constipation, difficulty urinating, orthostatic hypotension, impotence, failure to ejaculate
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| what CNS adverse effects are listed (list) | Parkinson's syndrome, akathisia (inner restlessness), dystonias (movement disorder), tardive dyskinesia, toxic-confusional state
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| what endocrine effects can occur (3) | 1) amenorrhea-galactorrhea; 2) infertility; 3) impotence
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| what adverse effect occurs, particularly in atypical antipsychotics | weight gain
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| what adverse effect occurs most in typical antipsychotics, and what may it be due to | sedation - may be due to action on histamine receptors
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| what can happen to mood from antipsychotics | blunt affect, lack of pleasure, dysphoria
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| do they cause nausea | no, they actually have antiemetic actions
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| what is perhaps the most serious adverse effect (and rarest) of antipsychotic medications | neuroleptic malignant syndrome
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| what is the classic triad of symptoms in neuroleptic malignant syndrome | 1) rigidity; 2) fever; 3) cognitive changes
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| when do symptoms usually begin (90% of the time) for neuroleptic malignant syndrome | within two weeks of starting treatment
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| how can muscle rigidity be detected (laboratory test) | increased creatine phosphokinase levels
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| what other symptoms frequently occur (over 50%) in neuroleptic malignant syndrome (4) | 1) EEG slowing (50%); 2) tachypnea (78%); 3) diaphoresis (60%); 4) labile blood pressure (54%)
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| what is the course of symptoms (how do they progress, when do they peak, and how long can they last (range)) | they progress rapidly, peak within three days, and can last from hours to 5 or 6 weeks
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| what factors put one at risk for NMS (3 - test question bold) | 1) YOUNG AGE [FOR MALES]; 2) dehydration; 3) hyponatremia
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| what is critical to treatment of neuroleptic malignant syndrome | early diagnosis
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| what drug is most likely to cause neuroleptic malignant syndrome | haloperidol
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| what supportive measures should be taken (3) | 1) respiration; 2) hydration; 3) cooling
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| what test should be done, and why | arterial gas sampling to determine if metabolic acidosis is a concern (alkalizing agents may be indicated)
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| what change should be initiated in antipsychotic treatment | discontinue
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| what drugs should the patient be given (2 and/or) | 1) dantrolene; 2) bromocriptine
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| in what manner are these drugs often given in combination (mode of administration of each, and which is maintained longer) | dantrolene: IV; bromocriptine: oral - dantrolene can be discontinued and bromocriptine maintained
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| how long should treatment continue | at least ten days
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| how much time should pass before antipsychotic treatment is initiated again, and what drug should be used | clinician should not reintroduce antipsychotic medications for at least two weeks, and a different antipsychotic should be tried
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| what was chloropromazine developed as | an antiemetic
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| what led to its decline in favor of other atypical antipsychotics | severe extrapyramidal side effects
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| what is chlorpromazine still commonly used for, and why | because of its powerful sedative side effects, it is commonly used to tranquilize non-compliant patients in emergency situations
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| is chlorpromazine a viable treatment option for any psychotic symptoms | yes - it works for positive symptoms and it is relatively cheap
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| how potent is haloperidol compared to chlorpromazine as an antipsychotic | far more potent (about 50X)
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| what is it the most common antipsychotic associated with | neuroletpic malignant syndrome
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| what other adverse effect(s) does it cause more commonly than chlorpromazine, and why | extrapyramidal effects (due to high affinity for D2 receptors)
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| what else is different about the range of side effects caused by haloperidol compared to chlorpromazine, and why | narrower range of side effects (dry mouth, constipation, hypotension, weight gain, etc.) - less affinity for some non-D2 receptors
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| what three receptors was haloperidol mentioned to have low affinity for | 1) cholinergic; 2) seritonergic; 3) histaminergic
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| what was clozapine, the first atypical antipsychotic, recently approved for (additional use) | schizophrenic patients at risk for suicide
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| what drug's effectiveness is it equal to in relieving positive symptoms | chlorporomazine
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| what other symptoms is it effective against | negative symptoms
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| what other major advantage does it have over typicals | very few extrapyramidal side effects
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| what is the limiting factor for prescribing clozapine (serious adverse effect) and what % of patients experience this | agranulocytosis (can be fatal) in 1-2% of patients
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| what four new, atypical antipsychotics must we know | 1) olanzipine; 2) quetiapine; 3) risperidone; 4) ziprasidone
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| what % of new prescriptions for schizophrenia and related disorders were made up by these drugs | 90%
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| what is the main reason these are desirable alternatives to typicals | lower incidence of extrapyramidal adverse effects
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| which of these agents were mentioned to still cause some degree of extrapyramidal side effects (2 specifically mentioned) | 1) olanzapine; 2) risperidone
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| what adverse effect do all of these agents, with one exception, cause, and what is the exception | all of these agents, with the exception of ziprasidone, cause considerable weight gain
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| how consistent is patient responsiveness to these agents | highly variable
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| what is one major factor restricting the use of atypicals compared to typicals | atypicals are far more expensive - typicals may still provide the most cost-effective treatment for some patients
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| why is compliance to these medications very low (4) | 1) initial sedative effects; 2) blockade of reward circuit; 3) weight gain; 4) many sufferers do not believe they are ill
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| what is sometimes done to improve compliance | intramuscular depots
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| what process may a physician have to use to find the best drug and dose, and why | trial and error - patients respond very differently
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| why is close monitoring of dosage essential | adverse effects
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| what effects of other agents can most antipsychotics potentiate | CNS depressant effects of other agents
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| what reason was mentioned for this | many antipsychotics inhibit CYP2D6, which is important for metabolizing many alagesic,s anesthetics, and sedatives
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| what drug in particular are schizophrenics at greater risk for abusing | nicotine
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| what other abused drugs were mentioned to exacerbate symptoms and/or reduce symptoms of antipsychotics (3) | 1) PCP; 2) cocaine; 3) meth
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| how effective are drugs at treating schizophrenia | not effective alone
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| what additional things are important (2) | 1) supportive (family) environment; 2) sufficient stimulation
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