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50 Cards in this Set
- Front
- Back
What is the mode of administration for all anti-psychotic drugs?
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PO - erratice pattern of absorption, high 1st pass metabolism, IM produces better absorption
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What is the binding of anti-pyschotic drugs?
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most are highly PP bound, mainly to albumin = interacts with warfarin
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What is fluphenazine or haloperidol decanoate?
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long acting preparation, decanoate is a fatty acid that gets trapped in fat/muscle and releases slowly
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does the potency or efficacy vary for the different antipsychotic agents?
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potency varies 1mg/day for pimozide to 800 me/day for clorpromazine; all have similar efficacy
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what are the early onset symptoms of extrapyramidal adverse effects of antipsychotics?
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pseudoparkinsonism, acute dystonia, oculogryic crisis; they are sometimes reversible
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what causes the early sypmtoms of extrapyramidal adverse effects?
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dopamine receptor sensitization
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what can be used to treat early symptoms of extrapyramidal adverse effects?
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muscarinic blocker or anticholinergics
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what are the intermediate symptoms of extrapyramidal adverse effects?
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akathisia (motor restlessness)
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what causes the intermediate symptoms of extrapyramidal adverse effects?
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duronal tracts downstream of dopaminergic neurons in the mesolimibic system
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what are the late symptoms of extrapyramidal adverse effects?
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tardive dyskinesia, tardive dystonia, dardive akathisia; seldom reversible
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What are the ANS adverse effects of antipyschotic drugs?
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atropine like effects - especially with THIORIDAZINE
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what are the endocrine/metabolic adverse effects of anti-psychotic drugs?
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hyperlipidemia, hyperglycemia, hyperprolactinemia, weight gain, gynecomastia, amenorrhea, galactorrhea
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what causes the endocrine/metabolic adverse effects?
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dopamine receptor blockade
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what is the mechanism that causes sedation when taking anti-psychotic drugs?
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histamine receptor blockade in the CNS - PTZs are the worst!
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what are the symptoms of neuroleptic malignant syndrome?
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hyperthermia, muscular rigidity, autonomic instability, altered consciouness
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what is the treatment of neuroleptic malignant syndrome?
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dantrolene and bromocriptine (dopamine agonist) and hydration
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what are the CV adverse effects of antipsychotics?
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otherostatic hypotension - due to alpha1 blockade; prolonged QT - associated with thioridazine and ziprasodone
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which anti-psychotics are known to cause tosades?
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haloperidol, thioridazine and ziprasidone
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what are the symptoms of metabolic syndrome due to antipsychotic drugs?
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weight gain, hyperlipidemia and hyperglycemia
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which drugs are more likely to cause metabolic syndrome?
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clozapine > olanzapine > quetiapine > risperidone > ziprasidone = aripiprazole
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what is the interaction between PTZs and phenytoin
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increase or decrease in phenytoin can occur with PTZs due to PP binding and metabolism
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what is the interaction between antipsychotics and carbamazepine?
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carbamazepine induces P450 levels = decreases levels of most antipyschotics - especially haloperidol
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what is the interaction between cimetidine and antipsychotics?
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cimetidine inhibits P450 at higher doses = increases levels of most antipsychotics
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what is the interaction between aluminum antacids and antacids?
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Al antacids decrease absorption of PTZs
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what do most older and middle generation agents do to seizure activity?
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they lower the seizure threshold
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what class of antipsychotic drug is chlorpromazine?
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phenothiazine
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what class of antipsychotic drug is thioridazine?
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phenothiazine
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What class of antipsychotic drug is fluphenazine?
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phenothiazine
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what is the M.O. of PTZs?
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D2 antagonist in the mesolimibic cortex; also inhibits 5HT2 receptors
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when is chlorpromazine used?
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only in severely refractory patients due to severe side effects
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what are the adverse effects of thioridazine?
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there are fewer EPS than with most PTZs but there are cardiac adverse effects - long QT, increased incidence of delayed ejaculation and high doses causes pigmented retinopathy
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what class of antipsychotic drug is haloperidol?
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butyrophenone
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what is the M.O. of haloperidol?
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D2 antagonism with very little effect on 5HT antagoinst activity compared to PTZs
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what are the adverse side effects associated with haloperidol?
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greatest chance of EPS and neuroleptic malignant syndrome!!, but it is less likely to cause sedation and hypotension than PTZs
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what class of drug is clozapine?
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2nd generation (atypical) antipsychotic
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what class of drug is olanzapine?
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2nd generation (atypical) antipsychotic
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What class of drug is quetiapine?
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2nd generation (atypical) antipsychotic
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what class of drug is risperidone?
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2nd generation (atypical) antipsychotic
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what class of drug is ziprasidone?
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2nd generation (atypical) antipsychotic
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What class of drug is aripiprazole?
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2nd generation (atypical) antipsychotic
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What is the M.O. of the 2nd generation agents?
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5HT2a antagonist + D2 receptor antagonist - EXCEPT aripiprazole
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what are the adverse effects of clozapine?
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low EPS incidience, granulocytosis, myocarditis, marked sedation, weight gain and hyperglycermia are common
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what is the M.O. of clozapine?
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5HT2a >>> D2 antagonist
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what are the ADRs of quetiapine?
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sedation, dizziness, headache, GI upset, some incidence of weight gain - less than with risperidone or olanzapine
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what are the ADRs of olanzapine?
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HYPERLIPIDEMIA! Weight gain, hyperglycemia; lower chance of hyperprolactinemia
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what are the ADRs of risperidone?
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less sedation than with other, weight gain and cold-like rhinitis; more STIMULATORY effects - agitation, insomnia, anxiety; HIGHEST INCIDENCE OF HYPERPROLACTINEMIA!!!
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what is paliperidone?
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active metabolite of risperidone - similar ADRs and efficacy, no real advantages
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What are the ADRs of ziprasidone?
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mild sedation and prolonged QT interval BUT SELDOM causes weight gain!!
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What is the M.O. of aripiprazole?
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partial agonist (NOT ANTAGONIST) at D2 receptors and partial 5HT1a angonist; very little D antagonist effects
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What are the ADRs of aripiprazole?
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anxiety, HA, N&V and dizziness; little/no effect on weight gain, hyperprolactinemia, hyperlipidemia, hyperglycemia or EPS
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