Central Dopaminergic Signaling Agents

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  1. dopamine acts as a
    • CNS neurotransmitter
    • controlling emotion, movement and reward mechanism
  2. dopamine is classified as a
    catecholamine neurotransmitter
  3. tyrosine → blood brain barrier → dopaminergic neurons ↺ dihydroxyphenylalamine (DOPA) by enzyme tyrosine hydroxylase ↺ dopamine
  4. type of family receptor that stimulates the formation of cAMP and phosphatidyl inositol hydrolysis
    D1 family
  5. type of receptor that inhibits cAMP synthesis
    D2 family
  6. is the primary mechanism by which dopamine is removed from the synaptic cleft
    dopamine transporter
  7. dopamine metabolism occurs through enzymatic action via
    MAO or COMT
  8. dopamine is metabolized by
    • intraneuronal MAO A and by glial
    • astrocyte cells by MAO A and MAO B
  9. dopamine can be converted to (2)
    • DOPAC dihydrocyphenylacetic acid
    • HVA homovanilic acid
    • human (HVA then DOPAC)
  10. 4 major pathways of neurotransmission of dopamine
    • nigrostriatal
    • mesocortical
    • mesolimbic
    • tuberohypophyseal
  11. pathway of dopamine that involves the production of movement
    (75% dopamine in the brain)
  12. - pathway of dopamine that involves in motivation and emotional response
    - essential to the normal cognitive function of the prefrontal cortex
  13. pathway of dopamine that involves with pleasure and reward behavior
  14. pathway of dopamine that involves in the regulation of prolactin
  15. is a progressive neurogenerative illness characterized by tremor, muscular rigidity, bradykinesia and postural imbalance
  16. factors affecting parkinson
    • aging process
    • oxidative stress
    • environmental chemicals
    • genetic aspects
  17. this combination can result in a sustantial increase in dopamine delivery to the CNS with a decrease in peripheral side effects and prevents decarboxylation of levodopa outside the CNS
    levodopa, carbidopa
  18. is indicated for the tx of idiophatic, postencephalitic and symptomatic parkinsonism
    levodopa USP
  19. are utilized to prolong the plasma half life of levodopa or block the striatal metabolism of dopamine
    MAO B inhibitor
  20. when administered with levodopa, it allows for a reduction in the daily dosage and improves the wearing off effect of levodopa
    selegiline hydrochloride USP
  21. 5 times more potent than selegiline
    rasagiline mesylate
  22. 2 types of derivative of dopamine agonists
    ergot and non ergot
  23. the combination of levo/carbidopa with it permits the reduction of the dose of levodopa making the side effects lessen resulting in more continuous stimulation of dopamine receptors
    bromocriptine mesylate USP (parlodel)
  24. tx of hyperprolactinemic disorders either idiopathic or caused by pituitary adenomas
    cabergoline (dostinex)
  25. indicated for the acute, intermittent tx of hypomobility, "off" episodes associated with advanced Parkinson disease
    apomorphine HCl (apokyn)
  26. is indicated for symptomatic tx of moderate to severe idiopathic restless legs syndrome
    pramipexole diHCl (mirapex)
  27. tx of early stage parkinson
    rotigotine (neupro)
  28. indicated as an adjunct to levo/carbidopa to treat patients with idiopathic parkinson disease who experience the signs and symptoms of end of dose wearing off
    entacapone (comtan)
  29. is characterized by delusion, abdnormal behaviors, hallucinations, and thought disorder
  30. an antipsychotic drug for tx of symptomatic relief of nausea vomiting hiccups and porphyria
    chlorpromazine HCl USP (thorazine)
  31. an antipsychotic drug for the tx of schizo px who fail to respond to tx with other APD
    thioridazine HCl USP (mellaril)
  32. an antipsychotic drug for the use in the management of the manifestations of psychotic disorders and for control of severe nausea and vomiting in adults
    perphenazine USP 
  33. an antipsychotic drug for mgmt of schizo and short term tx of nonpsychotic anxiety
    trifluoperazine HCl USP (Stelazine)
  34. an antipsychotic drug for long term tx of psychosis and for px who are noncompliant with their drug tx
    haloperidol USP (Haldol)
  35. an antipsychotic drug for tx of long term maintenance in schizo, psychoses 
    haloperidol decanoate
  36. a critical antipsychotic drug for px with Gilles de la Tourette disorder who cannot tolerate haloperidol
    pimozide USP
  37. shown to provide a greater reduction in both + and - symptoms of schizo
    atypical antipsychotic drug
  38. atypical antipsychotic drug for acute mania associated with bipolar disorder
  39. atypical antipsychotic drug tx of irritability in autistic children and adolescents
    risperidone (risperidal)
  40. is hypothesized to be an effective neurprotectant
    coenzyme Q10
Card Set:
Central Dopaminergic Signaling Agents
2015-02-03 19:49:55

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