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50 Cards in this Set

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