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70 True/False questions

  1. Positive SymptomsFeelings or behaviors that are not usually present

          

  2. What is the basic MOA of typical antipsychotics?Blocking (antagonism) of D2 receptors in the brain

          

  3. What was the first atypical antipsychotic?Blocking (antagonism) of D2 receptors in the brain

          

  4. Cognitive symptomsDisorganization and cognitive impairment

          

  5. Cl substitution on the 2 position of chlorpromazine causes the active conformer to...the Z isomer (because it is able to superimpose of dpoamine where as the E isomer can not)

          

  6. T/F: Thiordazine has high anticholinergic activityAntihelminthics

          

  7. T/F: Atypical antipsychotics do not have as much affinity for D1 receptors, making them better for EPS symptoms.Partial agonists

          

  8. Which drugs can be considered 3rd generation antipsychotics?- Benzazepines
    - Benzisoxazole and Benzisothiazoles
    - Other/ Miscellaneous

          

  9. Affective symptomsFeelings or behaviors that are not usually present

          

  10. If a phenothiazine has a 2 carbon side chain, why type of activity will it have?Antihistamine

          

  11. What are the 2 methods of haloperidol metabolism?1. Reduction --> Oxidative deamination
    2. Oxidative deamination --> Reduction

          

  12. What is responsible for the extrapyramidal symptoms of typical antipsychotics?- Blocking D1 receptors

          

  13. Examples of positive symptoms- Hallucinations
    - Delusions
    - Disturbances in thought

          

  14. Thioridazine is a ______ of phenothiazineInverse agonist

          

  15. The 4-arylpiperidine moiety is ____ for fluoro-butyrophenones.Essential for activity

          

  16. Why was clozapine withdrawn from the market in 1975?Have not responded to other antipsychotic medications
    (Note: it was approved by FDA in 1989 with BBW requiring regular WBC count)

          

  17. Which modes of metabolism of a phenothiazine will result in active metabolites?1. Aryl hydroxylation
    2. N-dealkylation

          

  18. Dopamine HypothesisLack of feelings or behaviors that are usually present

          

  19. How can activity of the phenothiazines be decreased?1. Substitution at position 1
    2. Substitution at position 4
    3. Branching at the beta carbon of the side chain by phenyl or polar group

          

  20. The neurotoxic effect of haloperidol is similar to _____, which is a precursor for ____.Essential for activity

          

  21. What are the classes of atypical (2nd generation) antipsychotics?Blocking (antagonism) of D2 receptors in the brain

          

  22. Benzisoxazoles and benzisothiazoles combine the structural features of ____ and ____.1. Tricyclic ring system
    2. Electron withdrawing group at "X" (position 2 carbon)
    3. Sulphur at position 5 has receptor binding function
    4. 3 carbon side chain between N10 and N of amino acid.
    (4 carbon side chain= antitussive, and 2 carbon side chain= Antihistamine)

          

  23. There is a neurotransmitter imbalance especially in ____ and ____ in schizophrenic patients.Dopamine
    Glutamine

          

  24. The esterified decanoate ester of haloperidol gives is _____ duration of action.Long (1/month IM injection)

          

  25. Haloperidol has less _____ side effects, but more _____ side effects.Sedative
    EPS

          

  26. Introduction of a piperidine or piperazine at the end of the side chain of a phenothiazine will...Piperazines > dialkylamino > piperidines

          

  27. Aripiprazole's only active metabolite is _____, which is formed via ____ (mode of metabolism).Dehydroaripiprazole
    Dehydration

          

  28. ____ and ____ metabolism of aripiprazole are possible, but rare.Aryl hydroxylation
    Oxidative deamination

          

  29. Which isomer of thioxanthenes is the active one?Dibenzoxepinopyrrole

          

  30. The "X" electron withdrawing group of tfriflupromazine is ___.-CF3

          

  31. Haloperidol's 4-OH groups is esterified into ______.Decanoate ester

          

  32. _____ is the most potent phenothiazine available as lipid soluble esters for depot IM injection1. Aryl hydroxylation
    2. N-dealkylation

          

  33. _____ is the only 1st generation typical antipsychotic approved for use in the USA.Blocking (antagonism) of D2 receptors in the brain

          

  34. Who coined the term schizophrenia?Schizophrenia results from increased dopaminergic neurotransmission

          

  35. T/F: Hyperprolactinemia is a side effect associated with typical antipsychotics?Blocking (antagonism) of D2 receptors in the brain

          

  36. Fluoro-butyrophenones block D2 receptors so they have EPS symptoms, but are relatively _____.Non-sedating

          

  37. What are the metabolic pathways for ziprasidone?1. N-dealkylation and S-oxidation --> S-oxidation
    2. Aldehyde reductase --> S-methylation

          

  38. Thioxanthenes are _____ analogues of phenothiazines.Ring
    (Bio-esters?)

          

  39. Antipsychotic hypotensive side effects of different substitutions on alkyl nitrogen of phenothiazinedialkylamino = piperidines > piperazines

          

  40. Risperidone and Paliperidone are ___ and ____ antagonists.Muscarinic (M)

          

  41. Antipsychotic sedation effects of different substitutions on alkyl nitrogen of phenothiazinePiperazines > Piperidines > Dialkylamino

          

  42. What are the 3 general modes of metabolism for phenothiazines?Chlorpromazine

          

  43. The 4-aromatic ring on piperidine moiety of fluoro-butyrophenones is ____Assits activity

          

  44. Which substituents of a phenothiazine are essential for its activity?- Oxidation of the sulphur

          

  45. If a phenothiazine has a 4 carbon side chain, what type of activity will it have?Antihistamine

          

  46. Thiordazine has ___ (more or less) EPS side effects than phenothiazine?More

          

  47. Haloperidol acts as an _____ of dopamineInverse agonist

          

  48. Examples of negative symptoms- Hallucinations
    - Delusions
    - Disturbances in thought

          

  49. How will p-Fluoro substitution of fluoro-butyrophenones affect activity?Enhances activity

          

  50. Which modes of metabolism of a phenothiazine will result in an inactive metabolite?1. Aryl hydroxylation
    2. N-dealkylation

          

  51. Increasing activity for potential electron withdrawing groups for substituent X on the 2 position carbon of phenthiazinesCF3 > SO2CF3 > SCF3 > SOCH3 > SCH3 > Cl > CH3 > H

          

  52. What is the general MOA of atypical antipsychotics?Clozapine

          

  53. What is the prototype of the phenothiazines?Dibenzoxepinopyrrole

          

  54. What is the pharmacophore of asenapine?Dibenzoxepinopyrrole

          

  55. Fluphenazine enanthate and Fluphenazine decanoate are _____ phenothiazines.Ring
    (Bio-esters?)

          

  56. Antipsychotic activity of different substitutions on alkyl nitrogen of phenothiazinepiperidine analog

          

  57. What is the dosing schedule for Plaiperidone Palmitate?1/month IM injection

          

  58. Classes of Typical Antipsychotics (1st generation antipsychotics)- Phenothiazines
    - Thioxanthenes
    - Butyrophenones

          

  59. Asenapine has little affinity for ____ receptors.Muscarinic (M)

          

  60. Antipsychotic EPS symptoms of different substitutions on alkyl nitrogen of phenothiazinePiperazines > dialkylamino > piperidines

          

  61. Phenothiazines were first used as....Antihelminthics

          

  62. Triflupromazine has _____ (more or less) EPS side effects compared to chlorpromazine?Less

          

  63. How will -OH substitution of fluoro-butyrophenones affect activity?Enhances activity

          

  64. Today, clozapine is only used in patients who...True

          

  65. Smoking will _____ CYP1A2, which will ____ the therapeutic effect of clozapine.Induce
    Decrease

          

  66. 3rd generation antipsychotics tend to be ______ (MOA) at D2 receptors.Partial agonists

          

  67. What is responsible for the antiemetic effect of typical antipsychotics?- Antagonism in the CTZ in the brainstem

          

  68. The attachment of 4th carbon to a tertiary cyclic amine is _____ for fluoro-butyrophenones.Long (1/month IM injection)

          

  69. Negative symptomsLack of feelings or behaviors that are usually present

          

  70. T/F: Asenapine has no EPS side effects?- Hallucinations
    - Delusions
    - Disturbances in thought