Neuroleptic drugs

  1. first generation antipsychotic low potency(3)
    • chlorapromazine
    • prochlorapromazine
    • thioridazine
  2. neuroleptic adverse effects
    • motor, endocrine, autonomic nervous systems
    • many produce arrhythmia
  3. first gen antipsy high potency(3)
    • fluphenazine
    • haloperidol
    • pimozide
  4. 2nd gen antipsy med potency (6) (atypicals)
    • aripiprazole
    • olanzapine
    • quetiapine
    • risperidone
    • ziprasidone
  5. atypical neuroleptics adverse
    • adverse effects on motor endocrine and autonomic NS are less severe than reg neuroleptics
    • still cause cardiac and metabolic AE
  6. tourette syndrome treatment
    high potency like haldol and pimozide for motor and phonic tics who fail stnd trmt
  7. presurgical anxiety trmt
  8. intermittent poryphyria trmt
  9. tetanus adjunctive trmt
  10. anxiety associate dw/ major depression
  11. elderly dementia trmt
  12. severe behavioral probs in children trmt
  13. drug induced nausea from ca chemo trmt
  14. schizophrenia antipsychotic moa
    • postsynaptic D2 receptor blockage in limbic regions
    • decrease hallucination and delusions
  15. adverse effected areas of antipsychotics in schizo
    nigrostriatal, cortical, tuberoinfundibular
  16. nigrostriatal extrapyrimadal SE from D2 block
    • parkinsonian like syndrome w/ akathesia (restlessness) dystonia (twisting muscle contract)
    • chronic trmt- tardive dyskinesia may be permanent
  17. 4 A's negative symptoms of schizo D2 blockage, and area of brain
    • cortical dopamine system
    • alogia- speech, anhedonia- pleasure, asociality- social, avolition- motivation
  18. endocrine disruption from D2 blocking, and area
    • tuberinfundibular dop system
    • galacttorhea- ammenorrhea, infert, impotent, altered prolactin
  19. drugs that inadvertantly block muscarinic receptors
    • thioridazine
    • chlorpromazine
    • loss of visual accomodation, dry mouth, difficulty urinating and constipation
  20. drugs that inadvertantly block alpha adrenergic receptors
    • chlorpromazine
    • orthostatic hypotn, impotence and ejaculation failure
  21. drugs that inadvertantly block histamine
    • chlorpromazine
    • clozapine
    • weight gain and drowsiness
  22. drugs that inadvertantly block serotonin receptors
    • risperidone
    • clozapine
    • dopamine receptor blockade on nigrostriatal and cortical systems
  23. newer atypicals block these 2 receptors
    serotonin 5ht2a and D2 dopamine receptors
  24. when the atypical drug blocks 5ht2a receptor on the terminal of a DA neuron it...
    cause it to release more DA to overcome the added D2 bloackage
  25. example of atypical antipsychotic
    • clozapine-
    • olanzapine
    • aripiprazole
    • Quetiapine
    • Ziprasidone
    • risperidone
  26. clozapine- and SE
    • higher 5ht2a - low extrapyrimadal symptoms
    • fatal agranulocytosis- low WBZC, 1% of npts
    • strong alpha adrenergic receptor blockade- sedation, muscle relax, CV, hypotn, reflex tach, some anticholinergic effects
  27. olanzapine and SE
    • high 5ht2a affinity with low extrapyrimadal SE
    • clinical effectivenees for + and - symptoms
    • available for EX release IM Schizo pts
    • dose for acute and mixed bipolar, superior to valproate
    • low potential- moderate orthostatic, high potential for metabolic disturbances- weight gain
  28. aripiprazole and SE
    • dop system stabalizer, partial dop agonist, less SE acts as partial ag at nigrostriatal and cortical D2
    • reduces neg effects of schizo, no cardiac QT prolactin probs, acute bipolar mania and disorder, may be adjunct with lithium and valproate
    • SE- somnolence
  29. Quetiapine and se
    • potent 5ht2a antagonist. used for manic bipolar episodes and alleviate depressive episodes- NOT first line
    • weight gain, sedation, orthostatics
  30. Ziprasidone and SE
    • improve + and - schizo , also tourettes. bipolar mania, monotherapy for acute manic or mixed
    • adjunct with lithium or valproate
    • ae- minimal weight gain, QT PROlongation, CONTRAindicated in cardiac arrythmias
  31. risperidone and SE
    • for rascals- irritability and aggresion , child conditions like in autism, self injury, temper tantrums, labile mood, maintance treatment of bipolar I disorder
    • SE mod potential for weight gain and sedation, POTENT alpha adrenergic ANTagonist -orthostatic but gets better
  32. general SE of atypical AP
    • agranulocytosis - clozipine
    • weight gain/ appetitie frequent
    • hyperglycemia and DM
    • acute agitation withdrawal from EtOH or opiates, lower the seizure threshold, qt prolong TORSADES, similar risk for sudden cardiac death to typicals
    • CV and CVA w/ dementia pts- risperidone
    • mood d/o watch for suicidal ideation
  33. All first generation antipsychotics (conventional antipsychotics)
    block dopamine type 2 (D2) receptors in the limbic system and the striatum,
  34. generally atypical antipsychotics (second generation antipsychotics)
    The key advantages include reduced incidence of tardive dyskinesia, reduced movement disorder adverse events and drug-induced parkinsonism and for negative cognitive symptoms.
  35. treatment of schizophrenia and other psychotic disorders, including schizoaffective disorder and bipolar mania
    generally recommend atypical antipsychotics as first-line treatment.
Card Set
Neuroleptic drugs
Neuroleptic drugs