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NUH Viva Preparations (Pharmacotherapy, Pharmacology) > Antipsychotics > Flashcards

Antipsychotics Flashcards

Schizophrenia

1
Q

What are the drug classes for Schizophrenia and their MOA?

A

Dopamine Receptor Antagonist
1. Typical Antipsychotic (D2)
2. Atypical Antipsychotic (D2, 5HT2A)
3. Benzodiazepines (GABA)

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2
Q

What are the goals of therapy for Schizophrenia?

A

Acute Stabilization
1. Reduce harm to self or others
2. Reduce symptoms

Stabilization and Maintenance
1. Relapse prevention
2. Adherence
3. QOL

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3
Q

What is the role of antipsychotics?

A

Calm down disturbed patients (Short-term tranquilizing effect without losing consciousness)

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4
Q

What are the 4 dopaminergic pathways in the brain?

A
  1. Mesolimbic (Reward): Positive Sx
  2. Mesocortical (Cognition): Negative Sx
  3. Nigrostriatal (Motor): EPSE
  4. Tuberoinfundibular (Milk): Prolactin
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5
Q

What are the postulated effects related to the neurotransmitters?

A
  1. D2: Positive Sx, EPSE, Prolactin
  2. 5HT2A: Negative Sx
  3. H1: Sedation, weight gain
  4. Alpha: Lightheadedness
  5. M1: Dry mouth, constipation, urinary retention
  6. IKr: QTc prolongation
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6
Q

What are the postulated effects related to different serotonin types?

A

5HT1A: Anxiety reduction
5HT2A: Depression reduction
5HT2C: Weight gain, appetite
5HT3: Nausea, vomiting

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7
Q

What is the criteria for adequate trial of antipsychotic in schizophrenia?

A

Optimal dose + 2 to 6 weeks duration

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8
Q

What is the criteria for treatment resistant schizophrenia?

A

Failed 2 or more adequate trials of antipsychotics (including at least one SGA)

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9
Q

What are the treatment options and dosing for acute agitation (psychiatric emergency) if the patient is compliant to medicine?

A

Either of these options:
(A) Oral Lorazepam 1 – 2mg

(B) Oral Antipsychotic:
- Haloperidol 2 – 5mg tablet/solution with pre-treatment ECG

  • Risperidone 1–2mg tablet/ODT/solution
  • Quetiapine 50-100mg Tablet/IR
  • Olanzapine 5 – 10mg Tablet/ODT
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10
Q

What are the treatment options and dosing for acute agitation (psychiatric emergency) if the patient is NOT compliant to medicine?

A

Either of these options:

(a) IM Lorazepam 1 – 2mg

(b) IM Olanzapine 5-10mg; 2nd dose ≥2h after 1st dose; 3rd dose ≥4 h after 2nd dose.

(c) IM Aripiprazole 9.75mg

(d) IM Haloperidol 2.5 – 10mg, with pre-treatment ECG

(e) IM Promethazine 25-50mg

(f) (a) + (d)

(g) (d) + (e)

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11
Q

Why is it that IM Olanzapine and IM Lorazepam must not be given within 1h of each other?

A

Risk of cardiorespiratory fatality

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12
Q

Compare IM Aripiprazole with IM Olanzapine. Why will I choose one over another?

A

IM Aripiprazole less hypotensive than IM Olanzapine option

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13
Q

What can be used for catatonia during psychiatric emergency?

A

PO/IM Lorazepam 1-2 mg

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14
Q

Which antipsychotics can be consolidated as once-daily dosing and why?

A

Chlorpromazine, Sulpiride; Amisulpride, Clozapine, Quetiapine

Long half-life. Need to consider the risk of hypotension and seizures when consolidating doses!

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15
Q

What is the course of treatment response to antipsychotics?

A

Early Improvement

Week 1: Agitation, aggression and hostility reduced

Week 2-4: Paranoia, hallucinations reduced, thought organization

Late Improvement

Week 6-12: Delusions reduced, negative symptoms improve

Month 3-6: Cognitive symptoms improve (with SGA)

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16
Q

List the four types of EPSE and in layman terms

A

Dystonia: Muscle spasm and stiffness in the face, neck, back

Pseudo-parkinsonism: Uncontrollable shaking of limbs

Akathisia: Restlessness and need to keep moving constantly

Tardive dyskinesia: Smacking lips, moving of jaws and tongue

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17
Q

List the treatment and prophylaxis options for Dystonia EPSE

A

Benztropine 1-2 mg (Max: 6 mg/day)
- Initial: IM (once)
- Subsequent: PO BD to TDS

OR

Diphenhydramine 25-50 mg (Max: 300 mg/day)
- Initial: IM (once)
- Subsequent: PO q4-12h

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18
Q

List the treatment and prophylaxis options for Pseudo-parkinsonism EPSE

A

Trihexyphenidyl 1 mg/day (Range PO 5-15 mg/day)

19
Q

List the treatment and prophylaxis options for Akathisia EPSE

A

PO Clonazepam 0.5 mg/day; increase daily dose based on response and tolerability by 0.5 mg every 5 days up to 4 mg/day in 2 divided doses

PO Propranolol 10 mg BD (Max: 120 mg/day)

20
Q

List the treatment and prophylaxis options for Tardive Dyskinesia EPSE

A

None. Discontinue any anticholinergics, reduce the dose of antipsychotics

21
Q

List of Typical Antipsychotics (D2 Neuroleptics) in NUH

A
  1. Haloperidol (0.5 mg green, 1.5 mg white, 5 mg pink)
  2. Chlorpromazine HCL (Largo, White tablet)
  3. Trifluoperazine (Stilizan, Blue tablet)
  4. Sulpiride (Devodil, White tablet)
22
Q

Haloperidol: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations
- 1.5 mg, 5 mg Tablet
- 2 mg/mL Oral Solution
- 5 mg/mL Injection

Max dosing varies per indication.

Usual Dose Range:
PO 3-5 mg BD (5-15 mg/day)
IM 2-10 mg per dose

Absolute max dosing: 100 mg/day, but doses >30 mg/day are in general not recommended

23
Q

Chlorpromazine: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations:
- 25 mg, 100 mg Tablet
- 50 mg IJ* EX

Max dosing varies per indication.

Usual Dose Range:
PO 25 mg BD (50-400 mg/day)

Absolute Max dosing: 800 mg/day

24
Q

Trifluoperazine HCL: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation: 5 mg Tablet

Usual Dose Range: 2-20 mg

Max dosing: 40 mg/day

25
Q

Sulpiride: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation: 200 mg Tablet

Depends on +/- Sx
Higher dose for +: 800 mg/day
Lower dose for -: 200 mg/day

Max dosing: 2400 mg/day

26
Q

List of Atypical Antipsychotics (D2 and 5HT2 Neuroleptic)

A

More metabolic side effects
1. Quetiapine
2. Olanzapine
3. Clozapine

Less metabolic side effects
1. Risperidone (Eperon)
2. Paliperidone (Metabolite of risperidone) (Invega)
3. Aripiprazole
4. Brexpiprazole
5. Amisulpride

27
Q

Quetiapine: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation:
- IR Tab: 25mg, 100mg, 200mg
- XR Tab: 50mg, 200mg, 300mg

Usual Dose Range: 150-500 mg

Max dosing varies for indications.

Absolute max dosing: 800 mg/day

28
Q

Olanzapine: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations:
- 10 mg Orodispersible Tablet
- 5 mg, 10 mg Tablet

Usual Dose Range: 5-20 mg

Max: 20 mg/day

29
Q

Risperidone: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations:
- 1mg, 2mg Tablet
- 1mg/mL Oral Solution

Usual Dose Range: 2-6 mg

Max: 16 mg

30
Q

Paliperidone: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations:
- ER Tab: 3mg, 6mg, 9mg
- PR Injection: 50 mg to 525 mg

Max: 12 mg/day
Initial: 6 mg/day
Usual Dose Range: 3-12 mg
CrCL < 80 mL/min require dose adjustment (80% urinary excretion)

31
Q

Aripiprazole: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation
- 5 mg, 10 mg, 15 mg Tablet
- 400 mg Injection

Max: 30 mg
Initial: 10 mg/day
Usual Dose Range: 10-30 mg

32
Q

Brexpiprazole: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulations: 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg Tablet (Rexulti)

Max: 4 mg
Initial: 1 mg/day for 4 days
Usual Dose Range: 2-4 mg
CrCL < 60 mL/min: 2 mg/day

33
Q

Amisulpride: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation: 200 mg Tablet

Max: 1200 mg
Negative Sx: 50-300 mg/day
Usual Dose Range: 50-800 mg

34
Q

Clozapine: Formulations available, usual dose range for schizophrenia and max dosing?

A

Formulation: 25 mg, 100 mg Tablets

12.5 mg ON then BD (Day 1), 25-50 mg ON (Day 2)
Usual Range: 300-450 mg
Max: 900 mg/day

35
Q

What is clozapine indicated for?

A

Treatment resistant schizophrenia after 2 adequate trials of different antipsychotics for 6 to 8 weeks, at least one is second-generation.

Dementia-related agitation and psychosis (severe/refractory)

Suicidal schizophrenia or schizoaffective disorder

Parkinson-related psychosis

Treatment-resistant bipolar

36
Q

When can you initiate clozapine therapy?

A

TWC > 3.5 X 10^9/L (3500)
ANC > 1.5 X 10^9/L (1500)

37
Q

How frequent do you need to monitor blood count for clozapine?

A

Every week for the first 18 weeks.

After 18 weeks, monitor monthly

38
Q

What do you do for clozapine monitoring if WBC = 3.0 to 3.5 X 10^9/L OR WBC drops by 3.0 X 10^9/L AND ANC > 1.5 X 10^9/L?

A

Repeat WBC count 2x/week until WBC > 3.5 X 10^9/L

39
Q

What do you do for clozapine monitoring if WBC = 2.0 to 3.0 X 10^9/L OR ANC = 1.0 to 1.5 X 10^9/L?

A
  • Stop Clozapine
  • Check WBC daily and monitor for signs of infections
  • Resume Clozapine only if no infection is present and once WBC is > 3.0 X 10^9/L
40
Q

What do you do for clozapine monitoring if WBC < 2.0 X 10^9/L OR
ANC < 1.0 X 10^9/L?

A
  • Stop Clozapine
  • Refer to hematologist and consider isolation
  • Never start Clozapine again
41
Q

What other indications can antipsychotics be used for besides schizophrenia?

A

Antiemetic in palliative care

Motor tics and adjunctive treatment in choreas and Tourette’s syndrome

Intractable hiccups

Irritability associated with Autistic Disorder

42
Q

Describe the clinical presentation of hyperprolactinemia

A

Changes in menstrual cycle in females (irregular or stopping of menstrual periods) and/or

Abnormal breast swelling, soreness or secretion (in both men and women)

43
Q
A

NUH Viva Preparations (Pharmacotherapy, Pharmacology) (7 decks)

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