Antipsychotic Medications
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Questions and Answers

What is the approved age range for Zyprexa (olanzapine) in the treatment of schizophrenia?

  • 13 and over (correct)
  • 18 and over
  • 20 and over
  • 10 and over

    • What is the typical dosage range for Lybalvi (olanzapine/samidorphan)?

  • 50-800 mg (correct)
  • 100-1000 mg
  • 5-10 mg
  • 10-20 mg

    • What is a common side effect associated with Zyprexa (olanzapine)?

  • Headache
  • Insomnia
  • Sedation (correct)
  • Anxiety

    • What is the approved indication for Saphris (Asenapine) in patients 10 and up?

    <p>Treatment of mania</p> Signup and view all the answers

    What is the formulation of Lybalvi (olanzapine/samidorphan) that has a 6-8 hour half-life?

    <p>IR formulation</p> Signup and view all the answers

    What is a unique instruction for patients taking the SL formulation of Saphris (Asenapine)?

    <p>Do not eat or drink for 10 minutes after administration</p> Signup and view all the answers

    What is the maximum daily dosage of Haldol (haloperidol)?

    <p>100mg</p> Signup and view all the answers

    Which of the following is NOT an FDA-approved indication for Haldol (haloperidol)?

    <p>Hypertension</p> Signup and view all the answers

    What is a rare but serious side effect of antipsychotic medications like Haldol (haloperidol)?

    <p>Neuroleptic malignant syndrome</p> Signup and view all the answers

    Which of the following antipsychotic medications is NOT available in the U.S.?

    <p>Flupenthixol</p> Signup and view all the answers

    What is the typical daily dosage range for Thorazine (chlorpromazine)?

    <p>200-800mg</p> Signup and view all the answers

    Which of the following is a contraindication for Haldol (haloperidol)?

    <p>Parkinson's disease</p> Signup and view all the answers

    What is the bioavailability of the medication if the instructions are not followed?

    <p>28%</p> Signup and view all the answers

    What is the starting dose for children to decrease the risk of dystonia?

    <p>5 mg SL BID</p> Signup and view all the answers

    What is the FDA-approved age range for Risperdal in treating schizophrenia?

    <p>Ages 13 and up</p> Signup and view all the answers

    What is the common side effect of Risperdal, even at low doses?

    <p>Elevation of prolactin</p> Signup and view all the answers

    What is the dosing range for Invega in schizophrenia?

    <p>6-12 mg</p> Signup and view all the answers

    What is the unique characteristic of Invega's elimination?

    <p>Eliminated via urinary excretion</p> Signup and view all the answers

    What is the FDA warning issued for Geodon in 2014?

    <p>DRESS</p> Signup and view all the answers

    What is the requirement for taking Invega Sustenna?

    <p>Take with a small meal or around 500 kcal</p> Signup and view all the answers

    What is the primary mechanism of action of Caplyta (lumeteperone)?

    <p>Serotonin-dopamine antagonist</p> Signup and view all the answers

    Which of the following medications is FDA approved for hallucinations and delusions related to Parkinson's disease?

    <p>Nuplazid (pimavanserin)</p> Signup and view all the answers

    What is the typical dosing range for the treatment of schizophrenia with the medication mentioned in the content?

    <p>1.5-6 mg</p> Signup and view all the answers

    Which medication has a high affinity for D3, D2, 5HT2b, and 5HT1a receptors?

    <p>One of the medications mentioned in the content</p> Signup and view all the answers

    What is a common side effect associated with Nuplazid (pimavanserin)?

    <p>Peripheral edema</p> Signup and view all the answers

    Which medication is a dopamine partial agonist?

    <p>One of the medications mentioned in the content</p> Signup and view all the answers

    What is a contraindication for the use of Fanapt?

    <p>History of QTc prolongation</p> Signup and view all the answers

    What is the typical dosing range for Fanapt?

    <p>12-24 mg in divided doses</p> Signup and view all the answers

    What is a side effect of Latuda that can be minimized by taking it with a meal?

    <p>Decreased absorption</p> Signup and view all the answers

    What is a receptor that Latuda has moderate affinity for, which may benefit mood and cognitive impairment?

    <p>5HT7</p> Signup and view all the answers

    Which of the following is a characteristic of Latuda that differentiates it from other antipsychotics?

    <p>No known issues with QTc prolongation</p> Signup and view all the answers

    What is the age range for which Fanapt is FDA approved for bipolar depression?

    <p>Ages 10 and up</p> Signup and view all the answers

    What is the main mechanism of action of typical antipsychotics?

    <p>Blockade of D2 receptors in the mesolimbic dopamine pathway</p> Signup and view all the answers

    What is a common side effect associated with the blockade of Histamine H1 receptors?

    <p>Weight gain and sedation</p> Signup and view all the answers

    What is a long-acting injectable with a dosing schedule of 12 weeks?

    <p>Invega Trinza</p> Signup and view all the answers

    What is a metabolic side effect associated with antipsychotic medications?

    <p>Dyslipidemia</p> Signup and view all the answers

    What is the main target of typical antipsychotics in the treatment of psychosis?

    <p>Positive symptoms of psychosis</p> Signup and view all the answers

    What is a side effect associated with the blockade of α1-adrenergic receptors?

    <p>Orthostatic Hypotension</p> Signup and view all the answers

    What is a characteristic of typical antipsychotics?

    <p>They are also known as classical or conventional antipsychotics</p> Signup and view all the answers

    What is the effect of blockade of D2 receptors in all areas of the brain?

    <p>Multitude of side effects</p> Signup and view all the answers

    Blocking 5HT2a receptors theoretically prevents the release of which neurotransmitter?

    <p>Glutamate</p> Signup and view all the answers

    Which of the following antipsychotics is considered the gold standard for efficacy in schizophrenia?

    <p>Clozapine</p> Signup and view all the answers

    Which of the following antipsychotics has a high metabolic risk?

    <p>Clozapine</p> Signup and view all the answers

    Prior to initiating antipsychotic therapy, which of the following laboratory tests should be performed?

    <p>All of the above</p> Signup and view all the answers

    Which of the following antipsychotics is FDA-approved for reducing the risk of suicide in schizophrenia and schizoaffective disorder?

    <p>Clozapine</p> Signup and view all the answers

    Which of the following side effects is associated with Clozapine?

    <p>All of the above</p> Signup and view all the answers

    Which of the following antipsychotics has a low metabolic risk?

    <p>Ziprasidone</p> Signup and view all the answers

    What is the primary reason Clozapine is not a first-line treatment choice for schizophrenia?

    <p>Unfavorable side effect profile</p> Signup and view all the answers

    What is the primary mechanism of action of Caplyta (lumeteperone)?

    <p>Dopamine partial agonist</p> Signup and view all the answers

    Which medication has a high affinity for D3, D2, 5HT2b, and 5HT1a receptors?

    <p>Caplyta (lumeteperone)</p> Signup and view all the answers

    What is the typical dosing range for the treatment of schizophrenia with Latuda?

    <p>1.5-6 mg</p> Signup and view all the answers

    Which medication is FDA approved for hallucinations and delusions related to Parkinson's disease?

    <p>Nuplazid (pimavanserin)</p> Signup and view all the answers

    What is a common side effect associated with Nuplazid (pimavanserin)?

    <p>Peripheral edema</p> Signup and view all the answers

    What is the dosing range for Caplyta (lumeteperone) in the treatment of schizophrenia?

    <p>1.5-6 mg</p> Signup and view all the answers

    What is the primary mechanism of action of Nuplazid (pimavanserin)?

    <p>Serotonin 2a/2c agonist/inverse agonist</p> Signup and view all the answers

    Which medication has a warning for QTc prolongation?

    <p>Nuplazid (pimavanserin)</p> Signup and view all the answers

    What is the primary reason for taking Invega with food?

    <p>To double bioavailability and increase absorption</p> Signup and view all the answers

    What is the typical dosage range for Risperdal in the treatment of psychosis or mania?

    <p>2-8 mg</p> Signup and view all the answers

    What is the common side effect associated with Risperdal, even at low doses?

    <p>Elevation of prolactin</p> Signup and view all the answers

    What is the FDA-approved indication for Risperdal in children with autism?

    <p>Irritability</p> Signup and view all the answers

    What is the unique characteristic of Geodon's side effect profile?

    <p>Associated with a rare but serious skin condition</p> Signup and view all the answers

    What is the typical dosage range for Invega Sustenna in schizophrenia?

    <p>80-160 mg</p> Signup and view all the answers

    What is the half-life of Invega Sustenna?

    <p>7 hours</p> Signup and view all the answers

    What is the benefit of taking Invega Sustenna over Risperdal?

    <p>Less sedation</p> Signup and view all the answers

    What is the dosage range for Abilify in treating ASD?

    <p>5-15 mg</p> Signup and view all the answers

    What is a unique characteristic of Abilify?

    <p>D2 dopamine receptor partial agonist</p> Signup and view all the answers

    What is the half-life of Abilify?

    <p>75 hours</p> Signup and view all the answers

    What is a potential side effect of Abilify?

    <p>Impulse control issues</p> Signup and view all the answers

    What is the FDA-approved indication for Abilify in pediatric patients?

    <p>All of the above</p> Signup and view all the answers

    What is the mechanism of action of Abilify?

    <p>Dopamine receptor partial agonist</p> Signup and view all the answers

    What is the dosage range for the medication with a half-life of 91 hours?

    <p>2-4 mg</p> Signup and view all the answers

    What is a common side effect of the medication with a half-life of 91 hours?

    <p>Akathisia</p> Signup and view all the answers

    Study Notes

    Antipsychotics

    Typical Antipsychotics

    • Chlorpromazine (Thorazine): indicated for psychosis, Tourette's, schizophrenia; 1-40mg dosage; available in PO tablet, liquid, IM, IV, and deaconate formulations
    • Mesoridazine (Serentil): typical antipsychotic
    • Thioridazine (Mellaril): typical antipsychotic
    • Loxapine (Loxitane): mid-potency antipsychotic
    • Fluphenazine (Prolixin): mid-potency antipsychotic
    • Haloperidol (Haldol): mid-potency antipsychotic; 1-40mg dosage; available in PO tablet, liquid, IM, IV, and deaconate formulations
    • Perphenazine (Trilafon): mid-potency antipsychotic
    • Pimozide (Orap): mid-potency antipsychotic
    • Thiothixene (Navane): mid-potency antipsychotic
    • Trifluoperazine (Stelazine): mid-potency antipsychotic

    Atypical Antipsychotics

    • Olanzapine (Zyprexa): FDA-approved for treatment of schizophrenia and mania in ages 13 and over; 10-20mg dosage; available in ODT, IM, and LAI formulations
    • Asenapine (Saphris): FDA-approved for treatment of mania in ages 10 and up, schizophrenia, and bipolar maintenance; 10-20mg dosage; available in transdermal and SL formulations
    • Risperidone (Risperdal): FDA-approved for schizophrenia, mania, irritability r/t autism, and bipolar maintenance; 2-8mg dosage; available in tablet, liquid, ODT, and LAI formulations
    • Paliperidone (Invega): FDA-approved for management of schizophrenia in ages 12 and older; 6-12mg dosage; available in LAI formulation
    • Ziprasidone (Geodon): DRESS FDA warning issued in 2014; 40-80mg dosage; available in IM formulation
    • Iloperidone (Fanapt): FDA-approved for bipolar depression and schizophrenia; 12-24mg dosage; available in divided doses
    • Lurasidone (Latuda): FDA-approved for bipolar depression, schizophrenia, and mania; must be taken with a small meal; 1.5-6mg dosage
    • Lumeteperone (Caplyta): FDA-approved for schizophrenia; 42mg once-daily dosage; available in capsule formulation
    • Pimavanserin (Nuplazid): FDA-approved for hallucinations and delusions r/t Parkinson's; 34mg daily dosage; available in capsule and tablet formulations

    Antipsychotics

    • Antipsychotics can cause side effects such as weight gain and sedation due to blockade of Histamine H1 receptors.
    • Blockade of α1-adrenergic receptors can lead to Orthostatic Hypotension and Drowsiness.
    • Metabolic side effects include weight gain, Dyslipidemia, Diabetes/Insulin resistance, and Hypertension.

    Long-Acting Injectables (LAI)

    • Dosing schedules for LAI:
      • Invega Sustenna: 4 weeks
      • Invega Trinzia: 12 weeks
      • Abilify Maintena: 4 weeks
      • Aristada: 4, 6, or 8 weeks
      • Risperdal Consta: 2 weeks
      • Risperdal Perseris: 4 weeks
      • Haldol Decanoate: 4 weeks
      • Prolixin Decanoate: 2 weeks

    Typical Antipsychotics

    • Also known as classical, conventional, or first-generation antipsychotics.
    • Discovered in the 1950s, with therapeutic effects due to blockade of D2 receptors in the mesolimbic dopamine pathway.
    • Mainly target positive symptoms of psychosis.
    • Unfortunately, Typical antipsychotics block D2 receptors in all areas of the brain, leading to a multitude of side effects.

    Atypical Antipsychotics

    • Aripiprazole (Abilify)
    • Asenapine (Saphris)
    • Brexpiprazole (Rexulti)
    • Cariprazine (Vraylar)
    • Clozapine (Clozaril)
    • Illoperidone (Fanapt)
    • Lurasidone (Latuda)
    • Olanzapine (Zyprexa)
    • Paliperidone (Invega)
    • Quetiapine (Seroquel)
    • Risperidone (Risperdal)
    • Ziprasidone (Geodon)
    • Lumateperone (Caplyta)

    Metabolic Risk

    • High risk: Clozapine (Clozaril), Olanzapine (Zyprexa)
    • Moderate risk: Risperidone (Risperdal), Paliperidone (Invega), Quetiapine (Seroquel), Iloperidone (Fanapt)
    • Low risk: Ziprasidone (Geodon), Lurasidone (Latuda), Aripiprazole (Abilify), Asenapine (Saphris), Cariprazine (Vraylar)

    Labs & Monitoring

    • Prior to initiation:
      • Weight/BMI/Waist circumference
      • EKG
      • CMP
      • CBC with diff
      • Fasting Lipid Panel
      • Blood pressure
    • Monitoring:
      • BMI quarterly
      • Blood pressure, Lipids, and Glucose within 3 months, and then every 6 months
      • Prolactin as needed
      • CBC with diff as needed
      • Abnormal Involuntary Movement Scale periodically

    Clozapine (Clozaril)

    • First antipsychotic to be recognized as atypical
    • Gold standard for efficacy in schizophrenia
    • Only antipsychotic to demonstrate increased efficacy compared to other antipsychotics
    • Only antipsychotic to be FDA approved for reducing the risk of suicide in schizophrenia and schizoaffective disorder
    • Not a first-line treatment choice, usually reserved for treatment-resistant schizophrenia, due to unfavorable side effect profile
    • May be very sedating
    • Associated with excessive salivation, myocarditis

    Risperdal (Risperidone)

    • FDA approved for:
      • Schizophrenia ages 13 and up
      • Mania ages 10 and up
      • Irritability r/t Autism ages 5 and up
      • Bipolar maintenance
    • Dosage: 2-8 mg for psychosis or mania; 0.5-2 mg for agitation in children
    • Comes in tablet, liquid, ODT, and LAI formulations (Consta and Perseris)
    • More typical at high doses, may be more likely to cause EPS
    • Weight gain and sedation are common
    • Common elevation of prolactin even at low doses

    Invega (Paliperidone)

    • Dosing: 6-12 mg; Sustained released, once a day dosing
    • FDA approved for management of schizophrenia ages 12 and older
    • The active metabolite of Risperdal
    • Is not hepatically metabolized, eliminated via urinary excretion
    • Possibly better tolerated, with less sedation, EPS, and orthostasis
    • Comes in LAI form Invega Sustenna
    • Dosing range of 80-160 mg in BMD, up to 200 mg in schizophrenia
    • Comes in IM formulation

    Geodon (Ziprasidone)

    • DRESS (Drug Reaction with Eosinophilia) FDA warning issued in 2014
    • Rare but serious skin condition
    • Rash that may spread to other parts of the body, causing fever, swollen lymph nodes, swollen face, inflammation of organs, an increase in white blood cells, and death
    • Symptoms often develop 11-30 days after initiation of treatment
    • Dosage range: 5-15 mg for ASD, 15-30 mg for Schizophrenia/mania, 2-10 mg for depression
    • Comes in Tablet, ODT, Oral solution, and 2 LAI formulations (Maintena and Aristada)
    • Half-life of 75 hours
    • Low level of EPS (except Akathisia), dyslipidemia, elevation of triglycerides, or insulin resistance, and weight gain

    Abilify (Aripiprazole)

    • D2 dopamine receptor partial agonist
    • Theoretically reduces dopamine output when dopamine concentrations are high, improving positive symptoms
    • Theoretically increases dopamine output when dopamine concentrations are low, improving cognition and negative symptoms
    • Has 5HT1a partial agonist actions, may contribute to antidepressant actions
    • Lacks D1, anticholinergic, and antihistamine properties
    • May not deliver sufficient antipsychotic efficacy in difficult to treat patients
    • No issues with hyperprolactinemia, and may even reverse hyperprolactinemia
    • Reports of issues with impulse control including compulsive gambling, shopping, binge eating, and sexual activity

    Caplyta (Lumateperone)

    • FDA approved for schizophrenia, launched Q1 2020
    • Dosed at 42 mg once a day with food
    • Most common side effects are sedation and dry mouth
    • Serotonin-dopamine antagonist
    • Blocks serotonin 2a receptors, post-synaptic D2 receptors
    • Affinity for serotonin reuptake pump
    • Interactions at a myriad of other neurotransmitter receptors may contribute to efficacy
    • Moderate binding affinity for D1 and D4 receptors

    Nuplazid (Pimavanserin)

    • A serotonin 2a/2c agonist/inverse agonist
    • Inverse agonist and antagonist activity at 5HT2a receptors, and to a lesser extent 5HT2c receptors
    • FDA approved for hallucinations and delusions r/t Parkinson's
    • Dosing of 34 mg per day (comes in a 34 mg capsule and 10 mg tablet)
    • Warning for QTc prolongation
    • Common SEs are Peripheral edema, nausea, and confusion
    • Should not worsen motor symptoms of Parkinson's

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