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47 Cards in this Set
- Front
- Back
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Chlorpromazine: typical/atypical?
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typical
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Thioridazine: typ/atyp?
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typ
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trifluoperazine: typ/atyp?
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typ
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fluphenazine: typ/atyp
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typ
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thiothixene: typ/atyp
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typ
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haloperidol: typ/atyp
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typ
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clozapine: typ/atyp
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atyp
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risperidone: typ/atyp?
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atyp
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olanzapine: typ/atyp?
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atyp
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quetiapine: typ/atyp?
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atyp
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ziprasidone: typ/atyp?
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atyp
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aripiprazole: typ/atyp?
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atyp
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suppport for DA hypothesis
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most antipsych meds strongly block post-synaptic D2 receptors in CNS
Drugs that increase DA can aggravate or create psychosis de novo DA receptor density increased in untreated schizophrenics PET shows increased DA receptor density Successful tx shows change in amt fo DA metabolites |
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probs with DA hypothesis
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atypicals are not potent D2 receptor antagonists, but are effective
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absorption of antipscyhotics
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readily, but incompletely absorbed orally --> erratic/unpredictable absorption
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1st pass metabolism of antipsychotics
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high, bioavailabilty it 25-35% (haloperidol = 65%)
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lipid solubility of antipsychotics
plasma protein bindign |
very lipid soluble, readiy enters CNS, acumulates in brain, lung and other tissue
can enter fetal circulation and breast milk 92-99% bound to plasma proteins |
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metabolism of antipsychotics
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p450
metabolites produced are not impt for therapeutic action, w exceptionf of mesoridazine (metabolite of thioridazine... more active than parent compound) |
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which antipsychotics are good for rapid initiation of therapy
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fluphenazine
haloperidol |
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which antipsychotics have depot preparations
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haolperidol decanoate
fluphenazine decanoate |
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which antipsychotic has the shortest t1/2
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quetiapine
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which antipsychotic has the longest t1/2
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aripiprazole
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which are the only 2 drugs that have D4 activity
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clozapine
aripipirazole |
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other than to treat schizophrenia, what are other psych indications for antipsychotics
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used with lithium to treat mania
olanzapine can be used to treat mania, and can act as mood stabilizer in bipolar schizoaffective d/o treats toxic psychoses Tourette's psychotic sx in Alzheimer's and Parkinson's |
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which antipsychotic is used to treat Tourette's
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molindone (rarely used to treat schizo)
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What are some nonpsychiatric indications for antipsychotics?
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phenothiazines (anti-emetic, anti-pruritics, sedative)
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typical antipsychotics
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treat positive sx, not negative
provoke EPS increases PRL secretion |
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atypical antipsychotics
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treat + and - sx
decreased EPS increased PRL secretion |
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what accounts for the difference between typicals and atypicals?
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atypicals have 5HT2>D2 blockade compared with typicals
atypicas produce increased DA blockade of neurons from mesolimbic regions as compared ot nigrostriatal |
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behavioral adverse effects of antipsychotics
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pseudodepression (responds to anti-parkinsons meds)
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which drugs are most likely to cause EPS
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haloperidol
phenothiazines |
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how can neurological effects be treated
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diphenhydramine
antimuscarinics |
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what is the most unwanted adverse effect of antipsychotics
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tardive dyskinesias (mov'ts of muslces and lips... can be irreversible)
develops after several years of use (although can occur after 6 mos) |
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treatment of TD
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stop or reduce dose of med
eliminate all drugs with anti-cholinergic actions add diazepam to enhance GABAergic activity |
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drug that doesn't exacerbate TD
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clozapine
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which drug has the strongest autonomic effects? middle? weakest?
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thioridazine
clozapine and other atypicals haloperidol |
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what are the autonomic effects seen with antipsychotics
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muscarinic blockade
toxic confusional states urinary retention a-adrenergic blockade postural hypotension failure to ejaculate (esp with phenothiazines) |
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NMS
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muscle rigidity
aphoresis hyperpyrexia autonomic instability (life threatening) |
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treatment for NMS
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dantrolene
DA agonist |
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when is maximal risk for NMS to occur
how long can it last after stopping med |
within weeks
can persist for severatl days |
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which antipsychotic produces the most sedation?
least sedating? |
phenothizines
fluphenazine, haloperidol, aripiprazole |
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specific toxicities seen in thioridazine
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visual impairment (retinal deposits)
conduction defects |
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toxicity of ziprasidone
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QT prolonged
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toxicity of clozapine
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reversible agranulocytosis (1-2%)
seizures reserved for non-responders |
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which antipsychotic is fatal in OD
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thioridazine
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are typicals or atypicals more $$?
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atypicals
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which area of the brain is thought to be successful at treating, with reduced EPS sx?
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mesolimbic
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