Antipsychotics

Typical Antipsychotics

Butyrphenones

  • Haloperidol (Halodol®)
    • Available doses: 0.5 mg, 1 mg, 2 mg, 5 mg, 10 mg, 20 mg
    • Usual dose: 5 mg to 15 mg PO or IM
  • Droperidol (Inapsine®)
    • Available doses: 2.5 mg/ml
    • Usual dose: 2.5 mg to 10 mg IM

Dibenzoxazepines

  • Loxapine (Loxitane®)
    • Available doses: 4 mg, 10 mg, 25 mg, 50 mg
    • Usual dose:  45 mg, 90 mg

Dihydrindolones

  • Molindone (Moban®)
    • Available doses: 5 mg, 10 mg, 25 mg, 50 mg
    • Usual dose: 30 mg to 60 mg po

Phenothiazines

  • Chlorpromazine (Thorazine®)
    • Available doses: 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 100 mg/ml
    • Usual dose: 300 mg to 600 mg
  • Fluphenazine (Prolixin®)
    • Available doses: 1 mg, 2.5 mg, 5 mg, 10 mg
    • Usual dose: 5 mg to 15 mg
  • Perphenazine (Trilafon®)
    • Available doses: 2 mg, 4 mg, 8 mg, 16 mg, 16 mg/ml
    • Usual dose: 32 mg to 64 mg
  • Trifluoperazine (Stelazine®)
    • Available doses: 1 mg, 2 mg, 5 mg, 10 mg
    • Usual dose: 15 mg to 30 mg
  • Mesoridazine (Serentil®)
    • Available doses: 10 mg, 25 mg, 50 mg, 100 mg
    • Usual dose: 150 mg to 300 mg
  • Thioridazine (Mellaril®)
    • Available doses: 10 mg, 15 mg, 25 mg, 50 mg, 100 mg
    • Usual dose: 300 mg to 600 mg

Diphenylbutylpiperidine

  • Pimozide (Orap®)
    • Available doses: 1 mg, 2 mg
    • Usual dose:2 mg to 6 mg

Thioxanthenes

  • Thiothixene (Navane®)
    • Available doses: 1 mg, 2 mg, 5 mg, 10 mg, 20 mg, 5 mg/ml
    • Usual dose: 15 mg to 30 mg

Atypical Antipsychotics

  • Are used for the treatment of:
    • Schizophrenia
    • Schizophrenia-related disorders
    • Bipolar disorders
    • Delusional disorders
    • Agitation
    • OCD
    • Tourette’s syndrome
    • Amphetamine abuse

Indication

  • Are used for the treatment of:
    • Schizophrenia
    • Schizophrenia-related disorders
    • Bipolar disorders
    • Delusional disorders
    • Agitation
    • OCD
    • Tourette’s syndrome
    • Amphetamine abuse

Types of antipsychotics

Typical (conventional, first generation):

  • Haloperidol (Haldol)
    • Preparations:
      • Pills
      • Liquid
      • Injection
  • Droperidole
    • Preparations:
      • Pills
      • Liquid
      • Injection
  • Loxapine
  • Molindone
  • Chlorpromazine (Thorazine)
  • Perphenazine
  • Fluphenazine
  • Trifluoperazine:
  • Mesoridazine
  • Thioridazine
  • Pimozide
  • Thiothixene

Atypical (second generation):

  • Benefits:
    • Lower EPS
    • Superior efficacy
    • Prevent negative symptoms of schizophrenia
    • Less likely to produce hyperprolactinemia
  • Adverse effects:
    • Atypical antipsychotic medications can cause major weight gain and changes in a person’s metabolism.
    • This may increase a person’s risk of getting diabetes and high cholesterol.1
    • A person’s weight, glucose levels, and lipid levels should be monitored regularly by a doctor while taking an atypical antipsychotic medication.
  • Examples:
    • Clozapine (Clozaril):
      • Is the last choice
      • It is a very effective medication that treats psychotic symptoms, hallucinations,
      • But clozapine can sometimes cause a serious problem called agranulocytosis, which is a loss of the white blood cells that help a person fight infection.
      • clozapine is potentially helpful for people who do not respond to other antipsychotic medications.
    • Risperidone (Risperdal)
    • Olanzapine (Zyprexa)
    • Quetiapine (Seroquel)
    • Ziprasidone (Geodon)
    • Aripiprazole (Abilify)
    • Paliperidone (Invega).

Side effects

General:

  • Dizziness when changing positions
  • Dry mouth
  • Constipation
  • Weight gain

Ocular:

  • Blurred vision
  • Pigmentary changes in the lens

Cardiac:

  • Rapid heartbeat
  • Hypotension
  • QT prolongation
  • Agranulocytosis

Skin:

  • Sensitivity to the sun
  • Skin rashes

CNS:

  • Lowered seizure threshold
  • Sedation
  • Drowsiness
  • Suppressed temperature regulation

Endocrine:

  • Menstrual problems for women
  • Hyperprolactinemia
  • DM

Extrapyramidal:

  • Acute Dystonic Reaction:
    • Pathophysiology:
      • Occurs within hours to days of initiation of treatment
      • Uncontrollable spasm of muscles of neck, back, tongue, or lateral eye
      • Laryngeal involvement causes stridor
    • Treatment:
      • Anticholinergics
        • Benztropine 1-2 mg po bid
        • Diphenhydramine 25-50 mg po tid
        • Trihexyphenidyl 5-10 mg po bid
      • Beta-blockers:
        • Propranolol 20 mg po tid
  • Parkinsonism syndrome:
    • Pathophysiology:
      • Less dopamine than acetylcholine in Basal Ganglia
      • Gradual onset
    • Symptoms:
      • Masked face
      • Cogwheel rigidity
      • Slowed movements
      • Drooling
      • Small handwriting
      • Pill-rolling tremor
    • Treatment:
      • Anticholinergics
        • Benztropine 1-2 mg po bid
        • Diphenhydramine 25-50 mg po tid
        • Trihexyphenidyl 5-10 mg po bid
      • Dopaminergic agent:
        • Amantadine (elderly) 100 mg po bid
  • Akathisia
    • Symptoms:
      • Restlessness in the lower extremities
      • Inability to site still
    • Treatment:
      • Switch to atypical antipsychotics
      • Add B-blocker or
      • Decrease dose
  • Tardive dyskinesia
    • Symptoms:
      • Involuntary choreoathetoid movements of face, trunk, or extremities
      • Clozapine has low risk of minor risk of TD
    • Treatment:
      • Discontinue medication
      • No Tx
  • Neuroleptic malignant syndrome
    • Pthophysiology:
    • Symptoms:
      • Marked muscle rigidity
      • Fever
      • Increased WBC
      • Increased CK > 300 U/mL
      • Delirium
    • Treatment:
      • Danterolene 4-8 mg/kg/day
      • Bromocriptine 1.25-2.5 mg BID

Response to antipsychotics

  • People respond in different ways to antipsychotic medications, and no one can tell beforehand how a person will respond. Sometimes a person needs to try several medications before finding the right one.
  • Symptoms of schizophrenia, such as feeling agitated and having hallucinations, usually go away within days. Symptoms like delusions usually go away within a few weeks. After about six weeks, many people will see a lot of improvement.
  • Some people may have a relapse—their symptoms come back or get worse. Usually, relapses happen when people stop taking their medication, or when they only take it sometimes.
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