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Risperidone – Binding Profile

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1 Risperidone – Binding Profile
5HT2A/D2 antagonist (high affinity for D2 receptors) a 1 antagonist a 2 antagonist Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

2 Risperidone – Prescribing Facts
Dosage range: 2 – 8 mg/day for acute psychosis and bipolar disorder mg /day for children and elderly patients 25-50 mg IM every two weeks Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambrigde University Press; 2011

3 Risperidone – Prescribing Facts
Dosage forms: Tablets: 0.25mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg, 6 mg. Orally disintegrating tablets: 0,5 mg , 2 mg Liquid: 1 mg/ml, 30 ml bottle LAI: Risperidone microspheres for IM use. 25 mg, 37.5 mg, 50 mg Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambridge University Press; 2011

4 Risperidone – Clinical Profile
Approved for use in children and adolescents: Schizophrenia, ages 13 and older Acute mania/mixed mania, ages 10 and older Autism related irritability in children, ages 5 -16 LAI approved for maintenance treatment of bipolar 1 disorder Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambridge University Press; 2011

5 Risperidone – Clinical Profile
Weight gain: intermediate risk. Lower risk than olanzapine and clozapine Higher risk than aripiprazole and ziprasidone EPS risk is dose dependent. A PET study found that risperidone occupies 75-80% of striatal D2 receptors at a dose of 6mg/day. Prolactin elevation is a risk. Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

6 Paliperidone Metabolite of risperidone: 9-hydroxyl-risperidone
Available as LAI: paliperidone palmitate

7 Paliperidone– Binding Profile
5HT2A/D2 antagonist a 1 antagonist a 2 antagonist Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

8 Paliperidone- Prescribing Facts
Dosage range: 6 mg/day (up to 12 mg/day) Dosage forms: Extended release tablets: 3 mg, 6 mg, 9 mg LAI - Paliperidone palmitate: 39 mg, 78 mg, 117 mg, 156 mg, 234 mg. INVEGA [package insert]. Accessed at : November 2012

9 Paliperidone - Clinical Profile
First antipsychotic to be approved for schizoaffective disorder. Paliperidone and risperidone are the two SGAs associated with hyperprolactinemia.

10 Quetiapine – Binding Profile
5HT2A/D2 antagonist 5HT1A partial agonist H1 antagonist a 1 antagonist Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

11 Quetiapine – Prescribing Facts
Dosage range: mg/day for schizophrenia and bipolar mania 300 mg / day for bipolar depression Dosage forms: Tablets: 25 mg, 50 mg, 100 mg, 200 mg, 300 mg, 400 mg XR tablets: 200 mg, 300 mg, 400 mg Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambrigde University Press; 2011

12 Quetiapine – Clinical Profile
Approved for: Bipolar maintenance Bipolar depression Acute mania/mixed states Adjunctive treatment of MDD Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambrigde University Press; 2011

13 Quetiapine – Clinical Profile
Adverse effects: Most common adverse effects: somnolence and dizziness. Orthostatic hypotension About 7% of patients Syncope is a possibility with rapid titration Weight gain: intermediate risk EPS: low risk Used in patients with Parkinson’s disease and Lewy body dementia Schatzberg, AF., Cole, JO, and DeBattista, C. Manual of Clinical Psychopharmacology. 7th ed.American Psychiatric Publishing, 2010.

14 Ziprasidone - Binding Profile
5HT2A/D2 antagonist 5HT1A partial agonist 5HT1D antagonist 5HT2C antagonist Low affinity for H1, M1 and a 1 receptors Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

15 Ziprasidone – Prescribing Facts
Dosage range: Schizophrenia: 40 – 200 mg/day Bipolar disorder: mg/day Maximum daily IM dose: 40 mg Dosage forms: Capsules: 20 mg, 40 mg 60 mg, 80 mg Injection: 20 mg/mL Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambrigde University Press; 2011

16 Ziprasidone – Clinical Profile
Associated with QT prolongation: Not dose dependent Careful with: Patients with CV conditions: uncompensated heart failure, cardiac arrhythmias Hypokalemia Hypomagnesemia Bradycardia Use of medications that prolong the QT interval Janicak, P G., Marder S R., and. Pavuluri M N. Principles and Practice of Psychopharmacotherapy. 5th ed. Philadelphia: Lippincott Williams & Wilkins, 2010.

17 Ziprasidone – Clinical Profile
Very low risk of inducing weight gain Patients who are overweight or have metabolic disturbances Dose dependent sedation Janicak, P G., Marder S R., and. Pavuluri M N. Principles and Practice of Psychopharmacotherapy. 5th ed. Philadelphia: Lippincott Williams & Wilkins, 2010.

18 Aripiprazole – Binding Profile
Partial D2/D3 agonist (pre and postsynaptic receptors) 5HT2A antagonist 5HT1A partial agonist Modest affinity for H1, M1 and a 1 receptors Tasman, A; Lieberman, J; Key, J; Maj, M. Psychiatry. 3rd ed. John Wiley & Sons, 2008 Schatzberg, AF, Nemeroff, CB. The American Psychiatric Publishing Textbook of Psychopharmacology. 4th ed.American Psychiatric Publishing, 2009

19 Aripiprazole – Prescribing Facts
Dosage range: 15-30 mg/day Dosage forms: Tablets: 2 mg, 5 mg, 10 mg, 15 mg, 20 mg, 30 mg Orally disintegrating tablets: 10 mg, 15 mg Oral solution: 1mg/ml Injection: 9.75 mg/1.3 ml Stahl, S M. The Prescriber's Guide. 4thd ed. New York: Cambrigde University Press; 2011

20 Aripiprazole – Clinical Profile
Approved as adjunctive treatment for MDD Low risk of causing weight gain Akathisia is a possibility


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