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Antipsychotic

Aka: Antipsychotic, Anti-Psychotic, Neuroleptic
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  1. See Also
    1. Extrapyramidal Side Effect
    2. Neuroleptic Malignant Syndrome
  2. Indications
    1. Psychosis (e.g. Schizophrenia)
  3. Efficacy: Newer low potency agents
    1. Atypicals only slightly better than high potency agents
      1. Similar efficacy in control of Psychosis
      2. Slightly less Extrapyramidal Side Effects (EPSE)
        1. Clozapine has much less EPSE, but has diabetes risk
      3. Higher weight, lipid and diabetes related conditions
      4. Compliance is similar for both types of agents
      5. Atypical Antipsychotics are much more expensive
    2. References
      1. Barry (2003) Am Fam Physician 68(5):943-4
      2. Leucht (2003) Lancet 361:1581-9
  4. Preparations: D2 Antipsychotic Agents - High Potency
    1. General: Extrapyramidal Side Effects (EPSE) with all
    2. Haloperidol (Haldol) or Haloperidol decanoate
      1. Typical dose: 10-15 mg/day
    3. Perphenazine (Trilafon)
      1. Well tolerated with similar efficacy to other agents
        1. Lieberman (2005) N Engl J Med 353:1209-23
    4. Thiothixene HCl (Navane)
      1. Typical Dose: 10 mg three times daily
      2. Maximum Dose: 60 mg per day
    5. Fluphenazine HCl (Prolixin)
      1. Typical Dose: 2.5 mg orally twice daily starting to 10-20 mg/day
      2. Maximum Dose: 40 mg orally or 100 mg IM per day
    6. Trifluoperazine (Stelazine)
  5. Preparations: D2 Antipsychotic Agents - Medium Potency
    1. Loxapine (Loxitane)
    2. Molindone (Moban)
  6. Preparations: D2 Antipsychotic Agents - Low Potency
    1. Strong Anticholinergic effects with both agents
    2. Chlorpromazine HCl (Thorazine) - not available in U.S.
      1. Anticholinergic Symptoms
      2. Alpha adrenergic blockade (Hypotension)
      3. Sedation
      4. Dosing: 400 mg/day (maximum 1000 mg/day)
    3. Thioridazine HCl (Mellaril) - not available in U.S.
      1. Anticholinergic Symptoms
      2. Alpha adrenergic blockade (Hypotension)
      3. Sedation
      4. Dosing: 200-300 mg/day (maximum 800 mg/day)
  7. Preparations: Atypical Antipsychotics (Second Generation) - Serotonin-Dopamine Antagonists
    1. Dibenzodiazepine (Clozapine, Clozaril)
      1. Typical maintenance dose: 300-600 mg/day
      2. Oldest second generation Antipsychotic (introduced in 1989)
      3. Most adverse side effect profile of second generation agents
        1. Agranulocytosis (unique to Clozapine and FDA limits prescribers due to this effect)
        2. Causes Anticholinergic effects, Sedation, Postural Hypotension, Seizures, weight gain and dyslipidemia
    2. Olanzapine (Zyprexa)
      1. Typical maintenance dose: 10-20 mg/day
    3. Quetiapine (Seroquel)
      1. Typical maintenance dose: 250-600 mg/day
    4. Risperidone (Risperdal)
      1. Typical maintenance dose: 3-6 mg/day
    5. Ziprasidone (Geodon) 40-80 mg/day
      1. Typical maintenance dose: 40-80 mg/day
    6. Aripiprazole (Abilify)
      1. Typical maintenance dose: 10-30 mg/day
  8. Adverse effects: General
    1. See Extrapyramidal Side Effect (EPSE)
      1. Especially with high potency first generation agents and Risperidone (Risperdal)
    2. Neuroleptic Malignant Syndrome
    3. Anticholinergic effects
      1. Especially with Low potency first generation agents and Clozapine (Clozaril)
    4. Sedation
      1. Especially with Low potency first generation agents, Clozapine (Clozaril), Olanzapine (Zyprexa) and Quetiapine (Seroquel)
    5. Hyperprolactinemia
      1. See Prolactin
      2. Especially with all first generation Antipsychotics and Risperidone (Risperdal)
    6. Postural Hypotension
      1. Especially with low potency first generation Antipsychotics, Clozapine (Clozaril), Quetiapine (Seroquel), and Risperidone (Risperdal)
    7. Seizures
      1. Especially with Clozapine (Clozaril)
    8. Sexual Dysfunction
      1. Especially with all first generation Antipsychotics and Risperidone (Risperdal)
    9. Ventricular arrhythmia (including Cardiac Arrest)
      1. Antipsychotic agent relative risk: 3.2
      2. Consider obtaining baseline EKG before starting therapy
      3. Consider electrolyte and Magnesium monitoring with high risk agents (e.g. Thioridazine)
      4. Avoid concurrent use of other medications prolonging QT Interval
        1. See Prolonged QT Interval due to Medication
      5. Drugs studied (from highest to lowest risk)
        1. Thioridazine (Mellaril)
        2. Ziprasidone (Geodon)
        3. Haloperidol (Haldol)
        4. Quetiapine (Seroquel)
        5. Risperidone (Risperdal)
        6. Clozapine (Clozaril)
        7. Olanzapine (Zyprexa)
      6. References
        1. Hennessy (2002) BMJ 325:1070-2
        2. Titier (2005) Drug Saf 28: 35-51
  9. Adverse Effects: Second generation agents (atypicals)
    1. Weight gain
      1. Weight gain with all second generation agents except Aripiprazole (Abilify) and Ziprasidone (Geodon)
      2. Also occurs with low potency first generation Antipsychotics (Chlorpromazine, Thioridazine)
    2. Adverse Lipid effects
      1. Serum Triglyceride increase most with Clozapine (Clozaril), Olanzapine (Zyprexa), Quetiapine (Seroquel)
      2. HDL Cholesterol decrease is variable
    3. Diabetes
      1. Highest risk with Clozapine (Clozaril) and Olanzapine (Zyprexa)
      2. Lowest risk with Ziprasidone (Geodon) and Aripiprazole (Abilify)
  10. Monitoring
    1. Precautions
      1. Clozapine has unique monitoring parameters (prescription only allowed by U.S. centers following protocol)
        1. Risk of Agranulocytosis
        2. Monitoring includes Complete Blood Count (weekly for 6 months, bimonthly for 6 months, then monthly)
    2. Medical history and Family History (including cardiovascular risks and arrhythmias)
      1. Obtain history at baseline and readdress annually
    3. Extrapyramidal Side Effects (EPSE) - all agents
      1. Screen for Tardive Dyskinesia at each visit
      2. Screen for other EPSE symptoms
      3. Educate about Neuroleptic Malignant Syndrome
    4. Obesity Monitoring (all Antipsychotics)
      1. Calculate BMI baseline, monthly for 3 months and then every 3 months thereafter
      2. Measure Waist Circumference annually
    5. Blood Pressure
      1. Obtain baseline, every 3 months and then annually
    6. Diabetes Mellitus Screening (Newer, atypical agents)
      1. Fasting Serum Glucose, 3 months and then annually
      2. Consider Hemoglobin A1C at four months after starting agent
      3. Screen for polyuria and polydipsia at each visit
    7. Hyperlipidemia (Newer, atypical agents)
      1. Lipid profile baseline and at 3 months
      2. Repeat lipids every 6 months if abnormal
        1. May decrease frequency to every 2-5 years if normal
    8. References
      1. Marder (2004) Am J Psychiatry 161: 1334-49
  11. References
    1. Gardner (2005) CMAJ 172(13): 1703-11
    2. Geddes (2000) BMJ 321:1371-6
    3. Glick (2001) Ann Intern Med 134: 47-60
    4. Haddad (2007) CNS Drugs 21(11): 911-36
    5. Lieberman (2005) N Engl J Med 353:1209-23
    6. Muench (2010) Am Fam Physician 81(5): 617-22

Antipsychotic Agents (C0040615)

Definition (NCI) A type of drug used to treat symptoms of psychosis. These include hallucinations (sights, sounds, smells, tastes, or touches that a person believes to be real but are not real), delusions (false beliefs), and dementia (loss of the ability to think, remember, learn, make decisions, and solve problems). Most antipsychotic agents block the action of certain chemicals in the nervous system.
Definition (MSH) Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.
Definition (CSP) class of drugs used to treat symptoms of schizophrenia and other psychotic behavior; includes neuroleptics.
Definition (NCI) Also known as neuroleptics, major tranquilizers, or antischizophrenics, natural or synthetic. Antipsychotic Agents relieve and control the symptoms of schizophrenic illness (hallucinations, delusions, dementia). Most antipsychotic agents interfere with various neurotransmitter functions, often blocking dopamine receptors, and induce diverse behavioral, endocrine, motor-kinetic effects. (NCI04)
Concepts Pharmacologic Substance (T121)
MSH D014150
SnomedCT 349871006, 10784006, 372482001
English Agents, Antipsychotic, Agents, Major Tranquilizing, Agents, Major Tranquillizing, Antipsychotic Agents, Major Tranquilizing Agents, Major Tranquillizing Agents, Neuroleptics, Tranquilizing Agents, Major, Tranquillizing Agents, Major, Agents, Neuroleptic, Antipsychotic Drugs, Antipsychotics, Drugs, Antipsychotic, Drugs, Neuroleptic, Major Tranquilizers, Neuroleptic Agents, Neuroleptic Drugs, Tranquilizers, Major, Anti-psychotic agent, NOS, Antipsychotic drugs, Neuroleptic drug, NOS, Antipsychotic Drug, neuroleptic, ANTIPSYCHOTICS, Neuroleptic Agent, Antischizophrenic Agent, Major Tranquilizer, neurological agents neuroleptics, antipsychotics (medication), antipsychotic tranquilizers, neuroleptics, major tranquilizers, neuroleptics (medication), antipsychotics, Antipsychotic drug (product), Antipsychotic Agent, Antipsychotic Agent [TC], Antipsychotic, [CN700] ANTIPSYCHOTICS, antipsychotic agents, antipsychotic drugs, major tranquilizer, neuroleptic drug, antipsychotic drug, neuroleptic drugs, neuroleptic agents, antipsychotics drugs, antipsychotic, neuroleptic agent, Neuroleptic drug, Neuroleptic, Anti-psychotic agent (product), Anti-psychotic agent (substance), Anti-psychotic agent, Antipsychotic agent, Antipsychotic drug, antipsychotic agent
French Anti-psychotiques, Médicaments antipsychotiques, Antipsychotiques, Agents neuroleptiques, Médicaments neuroleptiques, Agents antipsychotiques, Ataractiques, Neuroleptiques, Tranquillisants majeurs
Swedish Antipsykosmedel
Czech trankvilizéry velké, antipsychotika, neuroleptika
Spanish Antipsychotic drug, agente antisicótico, antisicótico, droga antisicótica, agente antipsicótico (producto), agente antipsicótico (sustancia), agente antipsicótico, antipsicótico, droga neuroléptica, neuroléptico, Agentes Antipsicoticos, Antipsicoticos, Medicamentos Antipsicoticos, Neurolepticos, Tranquilizantes Mayores, Antipsicóticos, Medicamentos Antipsicóticos, Agentes Antipsicóticos, Neurolépticos
Finnish Psykoosilääkkeet
Italian Tranquillanti maggiori, Agenti tranquillanti maggiori, Farmaci antipsicotici, Agenti neurolettici, Neurolettici, Farmaci neurolettici, Antipsicotici
Russian NEIROPLEGICHESKIE SREDSTVA, FENOTIAZINOVYE TRANKVILIZATORY, NEIROPLEGIKI, ANTIPSIKHOTICHESKIE SREDSTVA FENOTIAZINOVYE, TRANKVILIZATORY, PROIZVODNYE FENOTIAZINA, ANTIPSIKHOTICHESKIE SREDSTVA, BUTIROFENONOVYE TRANKVILIZATORY, TRANKVILIZATORY BOL'SHIE, NEIROLEPTICHESKIE SREDSTVA, PROIZVODNYE BUTIROFENONA, TRANKVILIZATORY, PROIZVODNYE BUTIROFENONA, ANTIPSIKHOTICHESKIE SREDSTVA BUTIROFENONOVYE, NEIROLEPTICHESKIE SREDSTVA, NEIROLEPTICHESKIE SREDSTVA, PROIZVODNYE FENOTIAZINA, NEIROLEPTIKI, АНТИПСИХОТИЧЕСКИЕ СРЕДСТВА, АНТИПСИХОТИЧЕСКИЕ СРЕДСТВА БУТИРОФЕНОНОВЫЕ, АНТИПСИХОТИЧЕСКИЕ СРЕДСТВА ФЕНОТИАЗИНОВЫЕ, БУТИРОФЕНОНОВЫЕ ТРАНКВИЛИЗАТОРЫ, НЕЙРОЛЕПТИКИ, НЕЙРОЛЕПТИЧЕСКИЕ СРЕДСТВА, НЕЙРОЛЕПТИЧЕСКИЕ СРЕДСТВА, ПРОИЗВОДНЫЕ БУТИРОФЕНОНА, НЕЙРОЛЕПТИЧЕСКИЕ СРЕДСТВА, ПРОИЗВОДНЫЕ ФЕНОТИАЗИНА, НЕЙРОПЛЕГИКИ, НЕЙРОПЛЕГИЧЕСКИЕ СРЕДСТВА, ТРАНКВИЛИЗАТОРЫ БОЛЬШИЕ, ТРАНКВИЛИЗАТОРЫ, ПРОИЗВОДНЫЕ БУТИРОФЕНОНА, ТРАНКВИЛИЗАТОРЫ, ПРОИЗВОДНЫЕ ФЕНОТИАЗИНА, ФЕНОТИАЗИНОВЫЕ ТРАНКВИЛИЗАТОРЫ
Croatian ANTIPSIHOTICI
Polish Trankwilizatory wielkie, Leki neuroleptyczne, Leki antypsychotyczne, Leki przeciwpsychotyczne, Neuroleptyki, Środki przeciwpsychotyczne
Japanese 抗精神病剤, 強トランキライザ, メジャートランキライザ, メジャートランキライザー, 抗精神病薬, 神経安定薬, 神経遮断剤, 神経遮断薬, トランキライザー-メジャー
German Antipsychotika, Neuroleptika, Tranquilizer, starke
Portuguese Agentes Antipsicóticos, Antipsicóticos, Medicamentos Antipsicóticos, Neurolépticos, Tranquilizantes Maiores, Drogas Antipsicóticas
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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