Antipsychotics Flashcards

1
Q

Define psychosis and appreciate schizophrenia as one common form of psychosis

A

Psychosis: means delusions and/or psychotic hallucinations

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2
Q

List the major positive and negative symptoms of schizophrenia

A

+auditory hallucinations
+delusions
+disorganized speech
+disorganized behavior

  • flat effect
  • social withdrawal
  • lack of motivation
  • lack of speech/thought
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3
Q

Briefly describe the dopamine hypothesis of psychosis

A

All current antipsychotic drugs block DA neurotransmission

Drugs that release DA from terminals and DA agonists can cause psychotic symptoms

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4
Q

Compare/contrast first and second generation antipsychotics regarding their affinity for D2 and 5-HT2A receptors

A

1st generation =
D2 antagonists

2nd generation =
D2 + 5HT2A antagonists
(Some efficacy against negative symptoms)

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5
Q

Describe MOA and clinical use of:

Haloperidol

A

D2 antagonist

Indication: clearly effective for positive symptoms

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6
Q

Describe MOA and clinical use of:

Trifluperazine

A

D2 antagonist

Indication: clearly effective for positive symptoms

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7
Q

Describe MOA and clinical use of:

Fluphenazine

A

D2 antagonist

Indication: clearly effective for positive symptoms

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8
Q

Describe MOA and clinical use of:

Chlorpromazine

A

D2 antagonist

Indication: clearly effective for positive symptoms

(Low potency 1st gen.)

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9
Q

Describe MOA and clinical use of:

Thioridazine

A

D2 antagonist

Indication: clearly effective for positive symptoms

(Low potency 1st gen)

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10
Q

Describe MOA and clinical use of:

Clozapine

A

D2 antagonist

5HT2A antagonist

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11
Q

Describe MOA and clinical use of:

Quetiapine

A

D2 antagonist

5HT2A antagonist

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12
Q

Describe MOA and clinical use of:

Olanzapine

A

D2 antagonist

5HT2A antagonist

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13
Q

Describe MOA and clinical use of:

Aripriprazole

A

PARTIAL D2 agonist

5HT2A antagonist

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14
Q

Describe MOA and clinical use of:

Risperidone

A

D2 antagonist

5HT2A antagonist

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15
Q

Describe MOA and clinical use of:

Ziprasidone

A

D2 antagonist

5HT2A antagonist

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16
Q

Describe major AEs of:

Haloperidol

A

EPS (acute and chronic)

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17
Q

Describe major AEs of:

Trifluperazine

A

EPS (acute and chronic)

18
Q

Describe major AEs of:

Fluphenazine

A

EPS (acute and chronic)

19
Q

Describe major AEs of:

Chlorpromazine

A

EPS (acute and chronic)

20
Q

Describe major AEs of:

Thioridazine

A

EPS (acute and chronic)

21
Q

Describe major AEs of:

Clozapine

A

Agranulocytosis
(No neutrophils)

Seizures

Salivation

22
Q

Describe major AEs of:

Quetiapine

A

Less AE than other 2nd generation antipsychotics

23
Q

Describe major AEs of:

Olanzapine

A

Most problematic for weight gain and metabolic changes

24
Q

Describe major AEs of:

Aripiprazole

A

Less AE than other 2nd generation antipsychotics

25
Q

Describe major AEs of:

Risperidone

A

WORSE than other 2nd generation antipsychotics in terms of increasing prolactin secretion and causing EPS

26
Q

Describe major AEs of:

Ziprasidone

A

Causes QT prolongation

27
Q

What are the first generation (aka typical) antipsychotics?

A

Haloperidol
Trifluperazine

Fluphenazine
Chlorpromazine

Thioridazine

28
Q

What are second generation (aka atypical) antipsychotics?

A

Clozapine
Quetiapine

Olanzapine
Aripiprazole

Risperidone
Ziprasidone

29
Q

Compare and contrast positive/negative symptoms regarding their responsiveness to antipsychotic drugs

A

Most treat positive

Clozapine works against negative symptoms

30
Q

Define one major location of 5-HT2A R’s and correlate drugs with an affinity for these receptors with the incidence of extrapyramidal side effects

A

Nigrostriatal pathway

2nd generation antipsychotics will help decrease EPS

31
Q

Briefly define bipolar disease

A

Symptoms of major depression and mania/hypomania

Bipolar I = more mania
+extreme mood swings, very euphoric then very depressed

Bipolar II = recurrent depressive episodes + hypomanic episodes
+less extreme on positive side, still very sad

32
Q

List three classes of drugs (inc. examples) used for tx of bipolar disease

A

Lithium = 1st line

Antiseizure drugs
+valproic acid
+carbamazepine
+lamotrigine

2nd gen antipsychotics 
\+ziprasidone
\+olanzapine
\+risperidone
\+aripiprazole
\+quetiapine
33
Q

For lithium, describe clinical uses and major side effects and contraindications

A

Indications:
bipolar disease

AEs = “L..M..N..O..P”

  • movement problems - tremor
  • nephrogenic DI
  • hypOthyroidism
  • Pregnancy NO!
  • N/V
  • kidney dysfunction

CI

  • pregnancy
  • renal disease
  • thyroid dysfunction
34
Q

What are AEs of 1st generation antipsychotics?

From D2 receptor blockade

A
Extrapyramidal Sx's (EPS)
Acute =
-dystonia
-akathisia
-Parkinsonian syndrome

Late EPS = tardive dyskinesia

Neuroleptic malignant syndrome (rare)

Hyperprolactinemia

35
Q

How do you treat acute extrapyramidal symptoms from 1st generation antipsychotics?

A

Dec. dose

Change to a 2nd gen.

Administer muscarinic receptor antagonist = trihexyphenidyl

Change to a lower potency antipsychotic

36
Q

What are differences amongst 1st generation antipsychotics and their potencies?

A

Low potency = more blockade of H1, M, alpha1

High potency = more extrapyramidal effects

37
Q

What are AEs of 1st generation antipsychotics?

Due to M, alpha1 and H1 blockade

A

M blockade =
Anticholinergic: dry mouth, blurred vision, urinary retention, constipation

alpha1 blockade = orthostatic hypotension

H1 blockade = sedation, inc. weight and appetite

38
Q

What is the MOA of second generation antipsychotics?

A

D2 receptor blockade

5HT2A receptor blockade

39
Q

What are indications for 2nd generation antipsychotics?

A

Schizophrenia - more effective against negative symptoms compared to 1st gen. Antipsychotics

40
Q

What are AEs of 2nd generation antipsychotics?

A

Dec. risk of EPS

Can cause metabolic syndrome

41
Q

What are the high potency first generation antipsychotics?

A

“Try to Fly High”

Trifluperazine
Fluphenazine
Haloperidol