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Atypical Antipsychotic Pharmacology

Atypical Antipsychotic Pharmacology. Stephanie Nichols, Pharm.D., BCPS, BCPP Associate Professor of Pharmacy Practice NicholsS@Husson.edu. Using Receptor Binding Profiles to Predict Adverse Effects. Objectives. Recognize atypical antipsychotics by brand and generic name

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Atypical Antipsychotic Pharmacology

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  1. Atypical Antipsychotic Pharmacology Stephanie Nichols, Pharm.D., BCPS, BCPP Associate Professor of Pharmacy Practice NicholsS@Husson.edu Using Receptor Binding Profiles to Predict Adverse Effects

  2. Objectives • Recognize atypical antipsychotics by brand and generic name • Understand how key pharmacological properties of antipsychotics translate into side effects • Compare and contrast the pharmacology of the atypical antipsychotics • Predict which antipsychotics may be more, or less, desirable in various patient scenarios

  3. 1950 1960 1970 1980 1990 2000 2010 FDA Approval of Antipsychotics Thioridazine Perphenazine Aripiprazole Trifluoperazine Risperidone Mesoridazine Iloperidone Chlorpromazine Pimozide Clozapine Asenapine Quetiapine Haloperidol Droperidol Ziprasidone Prochlorperazine Lurasidone Fluphenazine Paliperidone Loxapine Olanzapine Thiothixene Stephanie Nichols, PharmD BCPS BCPP 2014

  4. What defines an Antipsychotic? • Dopamine2 post synaptic antagonism • Reduce DA in the mesolimbic tract • Nucleus accumbens • Positive Symptoms • EPS

  5. Antagonism Partial Agonism

  6. Mesolimbic – VTA to NA, HC, amygdala Mesocortical – VTA to PFC Nigrostriatal – SN to BG Tuberoinfundibular – Hypothalamus to Pituitary Gland http://psychopharmacologyinstitute.com/antipsychotics-videos/dopamine-pathways-antipsychotics-pharmacology/

  7. What defines an Atypical Antipsychotic? • Serotonin2a post-synaptic antagonism • 5HT2a puts the brakes on DA in PFC • Disinhibiting the inhibitor – increased mesocortical DA • ? Improved negative and cognitive symptoms • Reduced EPS – at what cost?

  8. Typicals vs. Atypicals

  9. Recognize atypical antipsychotics by brand and generic name

  10. Atypical Antipsychotics in the US Generic Availability Brand Name Only Aripiprazole (Abilify) Paliperidone (Invega) Iloperidone (Fanapt) Asenapine (Saphris) Lurasidone (Latuda) • Clozapine (Clozaril) • Olanzapine (Zyprexa) • Quetiapine (Seroquel) • Risperidone (Risperdal) • Ziprasidone (Geodon)

  11. Understand how key pharmacological properties of antipsychotics translate into side effects

  12. Receptor Antagonism & Clinical Effect

  13. Compare and contrast the pharmacology of the atypical antipsychotics

  14. Addressing Negative Symptoms in Schizophrenia. CPNP University 2013

  15. NIMH Psychoactive Drug Screening Program (PDSP) Ki Database: http://pdsp.med.unc.edu/pdsp.php

  16. What do you think? • Based upon Quetiapine’s binding profile, which of the following adverse effects is most likely to occur? • Parkinsonism • Antimuscarinic Effects • Sedation

  17. ↑ BDNF

  18. 5HT2c and H1 Metabolic Changes • Dyslipidemia and hypertriglyceridemia • pancreatitis • Hyperglycemia and insulin resistance • diabetic ketoacidosis • Increased body weight • Increased adiposity

  19. Quetiapine Metabolic Effects • Even low dose (<200mg/day) quetiapine causes significant weight gain and increase in BMI after 52 weeks Cates ME et al. Metabolic Consequences of Using Low Dose Quetiapine for Insomnia in Psychiatric Patients. Community Ment Health J. 2009;45:251-4.

  20. Olanzapine in Healthy Volunteers • 10mg nightly x3 days Albaugh VL, Singareddy R, Mauger D, Lynch CJ (2011) A Double Blind, Placebo-Controlled, Randomized Crossover Study of the Acute Metabolic Effects of Olanzapine in Healthy Volunteers. PLoS ONE 6(8): e22662.

  21. 15 healthy subjects given 10mg po olanzapine or placebo (self-control) • Results: • decrease in glucose effectiveness, free fatty acids, and serum cortisol • increase in fasting glucose and prolactin After a single dose!! Hahn MK. et al. J Clin Psychopharmacol 2013; 33(6):740-6.

  22. Newer Agents: Metabolic Profiles CNS Drugs 2012. 26(9):733-59.

  23. * Partial 5HT2cAgonist Data from: Nguyen CT et al. Prim Care Comp CNS Disord 2012;12(5).

  24. Metabolic Changes • iloperidone • quetiapine • risperidone

  25. Weight Gain / Metabolic Effects

  26. Extra Pyramidal Symptoms (EPS) • Dystonia • Parkinsonism • Tardive Dyskinesia _______________________________________________ • Akathisia

  27. Parkinsonism

  28. Akathisia • ziprasidone • lurasidone • asenapine • aripiprazole Poyurovsky M. BJP 2010;196:89-91.

  29. Decreased EPS

  30. D2 Hyperprolactinemia • Gynecomastia • Amenorrhea • Breast tenderness • Sexual dysfunction • Galactorrhea

  31. Hyperprolactinemia Peuskens J et al. CNS Drugs 2014. PMID 24677189

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