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Pharmacology > Anti-Psychotics > Flashcards

Anti-Psychotics Flashcards

1
Q

What is the revised dopamine hypothesis for Schizophrenia?

A

Pxs have excess dopamine activity in the mesolimbic pathway, responsible for positive symptoms and decreased dopamine activity in the mesocortical is responsible for cognitive impairment and negative symptoms.

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2
Q

What type of symptoms are seen as easy to treat in comparison to the other type of symptoms?

A

Positive Symptoms.

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3
Q

What percent of the population is thought to have Schizophrenia?

A

1%

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4
Q

When is the peak age of incidence for Schizophrenia?

A

15-24 (females have second peak at 55-64)

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5
Q

What percent of patients have a full recovery after their first psychotic episode?

A

Less than 20%.

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6
Q

What percent of patients on anti-psychotics relapse within a given year?

A

20%

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7
Q

What percent of homeless people are thought to have schizophrenia?

A

50%

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8
Q

What is the percent chance that an identical twin would develop schizophrenia?

A

40-60% chance.

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9
Q

What are the four main dopaminergic pathways?

A
  1. Nigrostriatal Pathway. 2/3. Mesolimbic-Mesocortical pathway. 4. Tuberinfundibular Pathway
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10
Q

What is the Nigrostriatal Pathway?

A

Neurons project from substantia nigra to the striatum. Part of the extrapyramidal system.

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11
Q

What is the Mesolimbic-Mesocortical pathway?

A

Cell bodies in ventral tegmentum project to the limbic system and neocortex.

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12
Q

What is the Nigrostriatal Pathway affect on pxs. with schizophrenia?

A

None?

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13
Q

What is different in the mesolimbic pathway in patients? What is the result of this?

A

Too much dopamine. This is thought to lead to the positive sxs of schizophrenia.

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14
Q

What is different in the mesolimbic pathway in patients? What is the result of this?

A

Too much dopamine. This is thought to lead to the positive sxs of schizophrenia.

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15
Q

What is different in the mesocortical pathway in patients? What is the result of this?

A

Too little dopamine. This is thought to result in the negative sxs of schizophrenia.

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16
Q

What is different in the mesocortical pathway in patients? What is the result of this?

A

Too little dopamine. This is thought to result in the cognitive and negative sxs of schizophrenia.

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17
Q

What is the Tuberinfundibular Pathway?

A

Cell bodies in hypothalamus release dopamine into the pituitary portal circulation to inhibit prolactin secretion from the anterior pituitary.

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18
Q

Does the Tuberinfundibular Pathway work normally in pxs. with schizophrenia?

A

Yes.

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19
Q

What other NTs could be involved in schizophrenia?

A

Glutamate and Serotonin.

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20
Q

What were the first type of drugs (first generation) developed for treatment of schizophrenia?

A

Phenothiazines - originally used as a sedative.

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21
Q

What is the mechanism of action for Typical Antipsychotics?

A

Have a binding affinity to D2, but not D1. They are D2 antagonists. Thought that by doing this they can reduce positive sxs.

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22
Q

What are Typical Antipsychotics also referred to as?

A

Neuroleptics.

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23
Q

What are the side effects of Typical Anti-psychotics?

A

Movement disorders, extra-pyramidal side effects

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24
Q

What is one drug of the Phenothiazine chemical family? How potent is it?

A

Chlorpromazine (low potency).

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25
Q

What are the 2 chemical classes of Typical Antipsychotics?

A
  1. Phenothiazine. 2. Butyrophenones.
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26
Q

What is one drug of the Butyrophenone chemical class? How potent is it?

A

Haloperidol (high potency)

27
Q

In which pathway are schizophrenics thought to have too much dopamine?

A

The Mesolimbic pathway.

28
Q

What symptoms might a Typical Antipsychotics cause in the nigrostriatal pathway? Why does this happen?

A

Movement disorders (EPS). This happens because Typical Antipsychotics affect D2 receptors in all pathways.

29
Q

What symptoms might a Typical Antipsychotics cause in the mesocortical pathway?

A

It could increase the negative sxs of schizophrenia.

30
Q

What symptoms might a Typical Antipsychotics cause in the Tuberinfundibular Pathway?

A

An increase in the levels of Prolactin.

31
Q

What is acute dystonia?

A

Muscle spasms and abnormal postures.

32
Q

What causes acute dystonia?

A

Acute D2 antagonism.

33
Q

What is the time of maximal risk for acute dystonia?

A

Very early.

34
Q

What is Parkinson’s Disease? What causes it?

A

Bradykinesia, rigidity, variable tremor, shuffling gait. Caused by D2 antagonism.

35
Q

What is the time of maximal risk for Parkinson’s disease?

A

Early.

36
Q

What is Neuroleptic Malignant Syndrome? What causes it?

A

Muscle rigidity, fever, unstable blood pressure, catatonia, stupor, etc. Can be fatal. It is thought to be a severe form of EPS.

37
Q

What is the time of maximal risk for Neuroleptic Malignant Syndrome?

A

Usually early, but can occur at any time.

38
Q

What is Tardive Dyskinesia? What is it caused by?

A

Oral-facial dyskinesia, widespread choreoathetosis or dystonia. Caused by: up-regulation of or super-sensitivity of D2 receptors.

39
Q

What is the time of maximal risk for Tardive Dyskinesia?

A

Late (can continue after withdrawal of anti-psychotics).

40
Q

What is Akathisia? What is it caused by?

A

Motor restlessness. The cause is unknown.

41
Q

What is the time of maximal risk for Akathisia?

A

Early.

42
Q

How do you treat Tardive Dyskinesia?

A

Hard to treat. Important to catch early so that drugs can be changed so that DA receptors have a chance to “reset”.

43
Q

What is another name for Second Generation Anti-psychotics (SGA)?

A

Atypical Anti-psychotics.

44
Q

What is a general characteristic of Atypical Anti-psychotics?

A

They are inverse agonists (antagonist) 5HT (2A) receptors.

45
Q

What are Atypical Anti-psychotics thought to be able to treat?

A

Positive and maybe negative and cognitive sxs.

46
Q

How does Aripiprazole work?

A

It is a partial D2 agonist as well as the normal properties an Atypical Anti-psychotic has.

47
Q

How does modulating 5HT(2A) receptors help those with Schizophrenia?

A

It modulates dopamine release in several regions of the brain.

48
Q

How does modulating 5HT receptors in the nigrostriatal tract help those with Schizophrenia?

A

Serotonin action at 5HT (2A) receptors blocks dopamine release. Thus reducing EPS symptoms.

49
Q

What would happen if you block 5HT2A receptors in the mesocortical pathway?

A

Facilitates dopamine release.

50
Q

What would happen if you block 5HT2A receptors in the mesolimbic pathway?

A

It could indirectly limit dopamine release.

51
Q

What would happen if you block 5HT2A receptors in the Tuberinfundibular Pathway?

A

It may limit increases in prolactin release.

52
Q

How are Anti-psychotics metabolized? Do they experience first-pass metabolism?

A

By liver cytochrome P450 enzymes. They do experience first-pass metabolism.

53
Q

Why can anti-psychotics be active even after weeks after discontinuation?

A

Because they are highly lipid soluble and protein bound and so they can be retained for many weeks after cessation.

54
Q

Do Anti-psychotics pass the placenta? Is it toxic?

A

Yes, and little or no toxicity.

55
Q

What side effects occur if you antagonize H1 (Histamine) receptors, such as how Anti-psychotics do?

A

Weight gain, and drowsiness.

56
Q

What side effects occur if you antagonize Alpha 1 receptors, such as how Anti-psychotics do?

A

Dizziness, and Decreased blood pressure.

57
Q

What side effects occur if you antagonize M1 (Acetylcholine) receptors, such as how Anti-psychotics do?

A

Drowsiness, dry mouth, blurred vision, constipation.

58
Q

Referring to First generation Anti-psychotics which drug is better to give based on side-effects?

A

High potency ones such as Haloperidol.

59
Q

What side effects do 2nd generation Anti-psychotics have less of a chance of giving than 1st generation anti-psychotics?

A

Second generation Anti-psychotics run a lower risk of EPS and Tardive Dyskinesia.

60
Q

Can Anti-psychotics be used for all types of schizophrenia?

A

No, not catatonic form.

61
Q

What can Anti-psychotics be used to treat?

A

Bipolar, MDD, Tourette’s syndrome, schizoaffective disorders, Autism-spectrum disorders and maybe Alzheimer’s disease.

62
Q

What are two anti-psychotics given if other anti-psychotics don’t work?

A

Olanzapine and Clozapine.

63
Q

What is the efficacy of 2nd generation anti-psychotics over 1st generation anti-psychotics.

A

Their efficacy is the same, however, newer anti-psychotics have fewer side-effects.

Pharmacology (20 decks)

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