Re: Safety data on Zyprexa (olanzapine) and Symbyax (olanzapine and fluoxetine HCl capsules) Hyperglycemia, Weight Gain, and Hyperlipidemia

Similar documents
OLANZAPINE tablets USP, for oral use OLANZAPINE orally disintegrating tablets USP, for oral use Initial U.S. Approval: 1996

HIGHLIGHTS OF PRESCRIBING INFORMATION

More than We Bargained For: Metabolic Side Effects of Antipsychotic Medications

ADVERSE REACTIONS

WARNING LETTER DEPARTMENT OF HEALTH & HUMAN SERVICES TRANSMITTED BY FACSIMILE

RECENT MAJOR CHANGES Warnings and Precautions:

Olanzapine Tablets, USP Olanzapine Orally Disintegrating Tablets

ARIPIPRAZOLE tablets, for oral use Initial U.S. Approval: 2002

Maximum Dose 30. mg/day. mg/day. mg/day. mg/day. 30 mg /day. mg/day. 15 mg /day 10. mg/day. mg/day

Page 1 of RECENT MAJOR CHANGES Warnings and Precautions, Falls (5.

Clinical Policy: Olanzapine Orally Disintegrating Tablet (Zyprexa Zydis) Reference Number: CP.PMN.29 Effective Date: Last Review Date: 02.

be administered three times daily.

RECENT MAJOR CHANGES None.

Do Large Scale Studies of the Use of Antipsychotics Help Us Choose the Most Effective Treatments for Schizophrenia?

ZYPREXA RELPREVV, ZYPR-0006-USPI _ZYPR-0001-MG PRINTER VERSION 1 OF 16

Table of Contents. 1.0 Policy Statement...1

) and serotonin Type 2 (5-HT 2A

Concomitant Use of a Moderate CYP3A4 Inducer: It may be necessary to increase the dose of LATUDA (2.6, 7.1).

The PI includes important warnings and precautions. It states (in pertinent part):

Page 1 of 40. ZIPRASIDONE hydrochloride capsules, for oral use Initial U.S. Approval: 2001

Reference ID:

Elements for a Public Summary

Quetiapine Fumarate Tablets

Training Presentation

GEODON (ziprasidone HCl) capsules GEODON (ziprasidone mesylate) injection for intramuscular use Initial U.S. Approval: 2001

Metabolic Monitoring, Schizophrenia Spectrum Illnesses, & Second Generation Antipsychotics

ZYPREXA Olanzapine Tablets. ZYPREXA ZYDIS Olanzapine Orally Disintegrating Tablets. ZYPREXA IntraMuscular Olanzapine for Injection

Bipolar disorder is a recurrent and lifelong illness, with episodes

Comparison of Atypical Antipsychotics

in the formulation. (4)

Michael J. Bailey, M.D. OptumHealth Public Sector

WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS and SUICIDAL THOUGHTS AND BEHAVIORS WITH ANTIDEPRESSANT DRUGS

Abbreviated Class Review: Long-Acting Injectable Antipsychotics

Abbreviated Class Review: Long-Acting Injectable Antipsychotics

Participating Hospital Certification Form

BRAND-Name Savings May Be Waiting for You*

ARIPIPRAZOLE tablets, for oral use Initial U.S. Approval: 2002

BLONANSERIN. THERAPEUTICS Brands Lonasen see index for additional brand names

Factors. Strong CYP2D6 and CYP3A4 inhibitors

Research suggests that as many as 1 in 5 primary care patients

Kelly E. Williams, Pharm.D. PGY2 Psychiatric Pharmacy Resident April 16,2009

Study Code: Date: 27 July 2007

Your Doctor Discussion Guide

Medication Audit Checklist- Antipsychotics - Atypical

Antipsychotics in Bipolar

Concomitant Use of a Moderate CYP3A4 Inducer: It may be necessary to increase the dose of LATUDA (2.5, 7.1).

Indication Initial Dose Recommended Dose Maximum Dose mg/day 750 mg/day. Schizophrenia - Adults (2.2) daily. 25 mg twice

Bipolar disorder often coexists with other psychiatric disorders,

Pharmacy Medical Necessity Guidelines: Atypical Antipsychotic Medications. Effective: February 20, 2017

My Experience. My Words. My Treatment Journal.

Version 5.1: June ZYPADHERA Olanzapine powder & solvent for prolonged release suspension for injection

Minimising the Impact of Medication on Physical Health in Schizophrenia

In recent years, reports of diabetes, diabetic

Antipsychotic-Related Risk for Weight Gain and Metabolic Abnormalities During Development Christoph U. Correll, MD

A Treatment for Acute Manic or Mixed Episodes of Bipolar I Disorder in Adults

Bipolar Depression: A Collaborative Approach to Care

Impact of antipsychotic treatment on nonfasting triglycerides in the CATIE Schizophrenia Trial phase 1

Pharmacy Medical Necessity Guidelines: Atypical Antipsychotic Medications. Effective: December 12, 2017

Bipolar Depression Diagnosis: Confounding Factors

Recent Advances in the Antipsychotic Treatment of People with schizophrenia. Robert W. Buchanan, M.D.

Bipolar disorder is a recurrent and lifelong illness, with episodes

Polymorphic Variations in 5 HT2A, 5 HTT and DISC 1 in first episode schizophrenia patients

See Important Reminder at the end of this policy for important regulatory and legal information.

FULL PRESCRIBING INFORMATION: CONTENTS*

Cardiometabolic Risk Factors and Antipsychotic Medications Changing Prescribing Practices Promoting Wellness

RISPERIDONE Tablets, USP, for oral use. Initial U.S. Approval: 1993

Maximum Dose. 10 mg. twice daily. 10 mg. sublingually. twice daily. 10 mg. sublingually. twice daily. 10 mg. twice daily. 10 mg.

journal of medicine The new england Effectiveness of Antipsychotic Drugs in Patients with Chronic Schizophrenia abstract

UC San Francisco UC San Francisco Previously Published Works

Managing Multiple Comorbidities in Bipolar Disorder

Severe Diabetic Ketoacidosis Precipitated by an Atypical Antipsychotic Drug

Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia. Abstract

Disclosure. Speaker Bureaus. Grant Support. Pfizer Forest Norvartis. Pan American Health Organization/WHO NIA HRSA

N e w s R e l e a s e

Number needed to treat (NNT) is a measure of

RISPERDAL (risperidone)

Lurasidone: A New Antipsychotic For Schizophrenia. Objectives. Introduction. Pharmacology/Pharmacokinetics. Mechanism of Action. Mechanism of Action

Douglas Leslie, Ph.D.

N e w s R e l e a s e

Introduction. Objectives. Psychotropic Medications & Cardiometabolic Risk

EU Risk Management Plan

Objectives. Pre Discussion Question #2. Disparity in Care Demographics

FLUOXETINE HYDROCHLORIDE/OLANZAPINE

Dosing and administration information for ABILIFY MAINTENA (aripiprazole)

ASENAPINE. THERAPEUTICS Brands SAPHRIS see index for additional brand names

File NDA SE5 046/047, NDA SE5 036/037, NDA SE5 020/021

The Contribution of Abdominal Obesity and Dyslipidemia to Metabolic Syndrome in Psychiatric Patients

Antipsychotic Medications Age and Step Therapy

Maximum Dose 10 mg. twice daily. 10 mg. twice daily. 10 mg. sublingually. twice daily. 10 mg. twice daily. 10 mg. twice daily

You wrote ZYPREXA. Will your patient leave the pharmacy with something else? (cetirizine HCl) have been mistaken, one for the other, in the past.

Major depressive episodes associated with bipolar I disorder

LURASIDONE. THERAPEUTICS Brands LATUDA see index for additional brand names

STEP THERAPY CRITERIA

Bipolar disorder, a mood disorder characterized by fluctuations

ESSENTIAL SHARED CARE AGREEMENT FOR Risperidone, Olanzapine, Quetiapine, Aripiprazole, Amisulpride (South Staffordshire Only)

Bipolar disorder is characterized by fluctuations between hypomania,

Rexulti (brexpiprazole)

See Important Reminder at the end of this policy for important regulatory and legal information.

Dosing & Administration

Transcription:

www.lilly.com Eli Lilly and Company Lilly Corporate Center Indianapolis, Indiana 46285 U.S.A. Phone 317 276 2000 October 5, 2007 Re: Safety data on Zyprexa (olanzapine) and Symbyax (olanzapine and fluoxetine HCl capsules) Hyperglycemia, Weight Gain, and Hyperlipidemia Dear Health Care Professional, Eli Lilly and Company would like to inform you of important information being added to the Zyprexa (olanzapine) and Symbyax (olanzapine and fluoxetine HCl) labels. These labeling updates include new WARNINGS for Weight Gain and Hyperlipidemia and updated information in the WARNING for Hyperglycemia. These changes reflect results of recently completed pooled analyses of clinical trials in adults and adolescents as well as information from two published large studies of atypical antipsychotics, CATIE 1 and CAFE 2. The new labeling language is detailed below. Monitoring of glucose, weight, and lipids is recommended during olanzapine and olanzapine/fluoxetine combination treatment. Guidelines published by the American Diabetes Association (ADA) following the consensus development conference 3 provide recommendations for the monitoring of blood glucose, weight, and lipid levels in those treated with atypical antipsychotics. Other highlights of the updated labeling include: Abnormal or borderline glucose levels at baseline are an important risk factor for further glucose increase. While relative risk estimates are inconsistent, the association between atypical antipsychotics and increases in glucose levels appears to fall on a continuum and olanzapine appears to have a greater association than some other atypical antipsychotics. Significantly greater mean increases in total cholesterol, LDL cholesterol, and triglycerides were observed in Zyprexa-treated patients compared with placebotreated patients both with and without evidence of dyslipidemia at baseline. Labeling provides information on magnitude and distribution of weight gain over a two year period in Zyprexa-treated patients. Labeling also provides information on glucose, weight gain, and lipids from studies of Zyprexa for adolescent patients. Please note that Zyprexa and Symbyax are not approved currently for use in children and adolescents aged less than 18 years old.

2 Eli Lilly and Company remains committed to providing you with the most current product information available for the management of your patients and we will continue our ongoing research and analyses in these areas. Please refer to the full prescribing information for Zyprexa and Symbyax included with this letter. Should you have any questions or would like additional information regarding this important safety information, please contact the Lilly medical department at 1-800- Lilly-Rx or your Eli Lilly and Company sales representative. The Medical Community can further our understanding of adverse events by reporting all cases to the Agency via the MedWatch program by phone at 1-800-FDA-1088, by fax at 1-800-FDA-0178, via the MedWatch website at www.fda.gov/medwatch or by mail: MEDWATCH Food and Drug Administration 5515 Security Lane Suite 5100, HFD-001 Rockville, MD 20852 Sincerely, Tim Garnett, M.D. Vice President, Global Patient Safety Eli Lilly and Company

3 The following are the updated Hyperglycemia WARNINGS and the new Hyperlipidemia and Weight WARNINGS included in the Zyprexa label. WARNINGS: Zyprexa: The following is updated language in the WARNINGS section of the Zyprexa package insert, and will be reflected in other materials. Hyperglycemia Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with atypical antipsychotics including olanzapine. Assessment of the relationship between atypical antipsychotic use and glucose abnormalities is complicated by the possibility of an increased background risk of diabetes mellitus in patients with schizophrenia and the increasing incidence of diabetes mellitus in the general population. Given these confounders, the relationship between atypical antipsychotic use and hyperglycemia-related adverse events is not completely understood. However, epidemiological studies suggest an increased risk of treatment-emergent hyperglycemia-related adverse events in patients treated with the atypical antipsychotics. While relative risk estimates are inconsistent, the association between atypical antipsychotics and increases in glucose levels appears to fall on a continuum and olanzapine appears to have a greater association than some other atypical antipsychotics. Mean increases in blood glucose have been observed in patients treated (median exposure of 9.2 months) with olanzapine in phase I of the Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE). The mean increase of serum glucose (fasting and nonfasting samples) from baseline to the average of the two highest serum concentrations was 15.0 mg/dl. Olanzapine Monotherapy in Adults In an analysis of 5 placebo-controlled adult olanzapine monotherapy studies with treatment duration up to 12 weeks, olanzapine was associated with a greater mean change in fasting glucose levels compared to placebo (2.76 mg/dl versus 0.17 mg/dl). The difference in mean changes between olanzapine and placebo was greater in patients with evidence of glucose dysregulation at baseline (patients diagnosed with diabetes mellitus or related adverse events, patients treated with antidiabetic agents, patients with a baseline random glucose level 200 mg/dl, and/or a baseline fasting glucose level 126 mg/dl). These patients had a statistically significantly greater mean increase in HbA 1c compared to placebo. In patients with baseline normal fasting glucose levels (<100 mg/dl), 2.2% (N= 543) of those treated with olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus 3.4% (N= 293) of those treated with placebo. In patients with baseline borderline fasting glucose levels ( 100 mg/dl and <126 mg/dl), 17.4% (N=178) of those treated with

4 olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus 11.5% (N=96) of those treated with placebo. Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine have not been established in patients under the age of 18 years. In an analysis of 3 placebo-controlled olanzapine monotherapy studies of adolescent patients, including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), olanzapine was associated with a statistically significantly greater mean change in fasting glucose levels compared to placebo (2.68 mg/dl versus -2.59 mg/dl). In patients with baseline normal fasting glucose levels (<100 mg/dl), zero out of 124 (0%) of those treated with olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus 1 out of 53 (1.9%) of those treated with placebo. In patients with baseline borderline fasting glucose levels ( 100 mg/dl and <126 mg/dl), 2 out of 14 (14.3%) of those treated with olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus zero out of 13 (0%) of those treated with placebo. Physicians should consider the risks and benefits when prescribing olanzapine to patients with an established diagnosis of diabetes mellitus or having borderline increased blood glucose level (fasting 100 126 mg/dl, non-fasting 140 200 mg/dl). Patients taking olanzapine should be monitored regularly for worsening of glucose control. Patients with risk factors for diabetes mellitus (e.g., obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of anti-diabetic treatment despite discontinuation of the suspect drug. Hyperlipidemia Undesirable alterations in lipids have been observed with olanzapine use. Clinical monitoring, including baseline and follow-up lipid evaluations in patients using olanzapine, is advised. Significant, and sometimes very high (>500 mg/dl), elevations in triglyceride levels have been observed with olanzapine use. Modest mean increases in total cholesterol have also been seen with olanzapine use. Olanzapine Monotherapy in Adults In an analysis of 5 placebo-controlled olanzapine monotherapy studies with treatment duration up to 12 weeks, olanzapine-treated patients had statistically significant increases from baseline in mean fasting total cholesterol, LDL cholesterol, and triglycerides of 5.3 mg/dl, 3.0 mg/dl, and 20.8 mg/dl respectively compared to decreases from baseline in mean fasting total cholesterol, LDL cholesterol, and triglycerides of 6.1 mg/dl,

5 4.3 mg/dl, and 10.7 mg/dl for placebo-treated patients. For fasting HDL cholesterol, no statistically significant differences were observed between olanzapine-treated patients and placebo-treated patients. Mean increases in fasting lipid values (total cholesterol, LDL cholesterol, and triglycerides) were greater in patients without evidence of lipid dysregulation at baseline, where lipid dysregulation was defined as patients diagnosed with dyslipidemia or related adverse events, patients treated with lipid lowering agents, or patients with high baseline lipid levels. Table 1 shows categorical changes in fasting lipid values. Table 1. Changes in Lipids Values from Adult Placebo-Controlled Olanzapine Monotherapy Studies with Treatment Duration up to 12 Weeks Laboratory Analyte Category Change from Baseline Treatment Arm N Patients Triglycerides Increase by 50 mg/dl Olanzapine 745 39.6% a Placebo 402 26.1% Olanzapine 457 9.2% a (<150 mg/dl to 200 mg/dl) Placebo 251 4.4% Olanzapine 135 39.3% a ( 150 mg/dl and <200 mg/dl to 200 mg/dl) Placebo 65 20.0% Total Cholesterol Increase by 40 mg/dl Olanzapine 745 21.6% a Placebo 402 9.5% Olanzapine 392 2.8% (<200 mg/dl to 240 mg/dl) Placebo 207 2.4% Olanzapine 222 23.0% a ( 200 mg/dl and <240 mg/dl to 240 mg/dl) Placebo 112 12.5% Increase by 30 mg/dl Olanzapine 536 23.7% a Placebo 304 14.1% Olanzapine 154 0% LDL Cholesterol (<100 mg/dl to 160 mg/dl) Placebo 82 1.2% Olanzapine 302 10.6% ( 100 mg/dl and <160 mg/dl to 160 mg/dl) Placebo 173 8.1% a Statistically significant compared to placebo. In phase 1 of the Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE), over a median exposure of 9.2 months, the mean increase in triglycerides in patients taking olanzapine was 40.5 mg/dl. In phase 1 of CATIE, the mean increase in total cholesterol was 9.4 mg/dl. Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine have not been established in patients under the age of 18 years. In an analysis of 3 placebo-controlled olanzapine monotherapy studies of adolescent patients, including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), for fasting HDL cholesterol, no statistically significant

6 differences were observed between olanzapine-treated patients and placebo-treated patients. Table 2 shows categorical changes in fasting lipid values in adolescent patients. Table 2. Changes in Lipids Values from Adolescent Placebo-Controlled Olanzapine Monotherapy Studies Laboratory Analyte Category Change from Baseline Treatment Arm N Patients Triglycerides Increase by 50 mg/dl Olanzapine 138 37.0% a Placebo 66 15.2% Olanzapine 67 26.9% (<90 mg/dl to >130 mg/dl) Placebo 28 10.7% Olanzapine 37 59.5% ( 90 mg/dl and 130 mg/dl to >130 mg/dl) Placebo 17 35.3% Total Cholesterol Increase by 40 mg/dl Olanzapine 138 14.5% a Placebo 66 4.5% Olanzapine 87 6.9% (<170 mg/dl to 200 mg/dl) Placebo 43 2.3% Olanzapine 36 38.9% a ( 170 mg/dl and <200 mg/dl to 200 mg/dl) Placebo 13 7.7% Increase by 30 mg/dl Olanzapine 137 17.5% Placebo 63 11.1% Olanzapine 98 5.1% LDL Cholesterol (<110 mg/dl to 130 mg/dl) Placebo 44 4.5% Olanzapine 29 48.3% a ( 110 mg/dl and <130 mg/dl to 130 mg/dl) Placebo 9 0% a Statistically significant compared to placebo. Weight Gain Potential consequences of weight gain should be considered prior to starting olanzapine. Patients receiving olanzapine should receive regular monitoring of weight. Olanzapine Monotherapy in Adults In an analysis of 13 placebo-controlled olanzapine monotherapy studies, olanzapine-treated patients gained an average of 2.6 kg, which was statistically significantly different compared to an average 0.3 kg weight loss in placebo-treated patients with a median exposure of 6 weeks; 22.2% of olanzapine-treated patients gained at least 7% of their baseline weight, which was statistically significantly different compared to 3% of placebo-treated patients, with a median exposure of 8 weeks; 4.2% of olanzapine-treated patients gained at least 15% of their baseline weight, which was statistically significantly different compared to 0.3% of placebo-treated patients, with a median exposure of 12 weeks. Clinically significant weight gain was observed across all baseline Body Mass

7 Index (BMI) categories. Discontinuation due to weight gain occurred in 0.2% of olanzapine-treated patients and in zero placebo-treated patients. During long-term continuation therapy with olanzapine (238 median days of exposure), 56% of olanzapine patients met the criterion for having gained greater than 7% of their baseline weight. Average weight gain during long-term therapy was 5.4 kg. Table 3 includes data on weight gain with olanzapine pooled from 68 clinical trials. The data in each column represent data for those patients who completed treatment periods of the durations specified. Amount Gained kg (lb) Table 3. Weight Gain with Olanzapine Use 6 Weeks (N=2976) 6 Months (N=1536) 12 Months (N=778) 24 Months (N=422) 0 27 21 20 22 0-5 (0-11 lb) 57 34 25 22 5-10 (11-22 lb) 15 26 25 22 10-15 (22-33 lb) 2 12 16 18 >15 (>33 lb) 0 6 14 16 Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine have not been established in patients under the age of 18 years. In an analysis of 4 placebo-controlled olanzapine monotherapy studies of adolescent patients (ages 13 to 17 years), including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), olanzapine-treated patients gained an average of 4.6 kg, which was statistically significantly different compared to an average of 0.3 kg in placebo-treated patients, with a median exposure of 3 weeks; 40.6% of olanzapine-treated patients gained at least 7% of their baseline body weight, which was statistically significantly different compared to 9.8% of placebo-treated patients, with a median exposure of 4 weeks; 7.1% of olanzapine-treated patients gained at least 15% of their baseline weight, compared to 2.7% of placebo-treated patients, with a median exposure of 19 weeks. Clinically significant weight gain was observed across all baseline Body Mass Index (BMI) categories, but mean changes in weight were greater in adolescents with BMI categories above normal at baseline. Discontinuation due to weight gain occurred in 1% of olanzapine-treated patients, compared to zero placebo-treated patients. During long-term continuation therapy with olanzapine, 65% of olanzapine-treated patients met the criterion for having gained greater than 7% of their baseline weight. Average weight gain during long-term therapy was 7.4 kg.

8 Information for Patients: Hyperglycemia Patients should be advised of the potential risk of hyperglycemia-related adverse events. Patients should be monitored regularly for worsening of glucose control. Weight Gain Patients should be counseled that olanzapine is associated with weight gain. Patients should have their weight monitored regularly.

9 The following are the updated Hyperglycemia WARNINGS and the new Hyperlipidemia and Weight WARNINGS included in the Symbyax label. WARNINGS: Symbyax: The following is updated language in the WARNINGS section of the Symbyax package insert, and will be reflected in other materials. Hyperglycemia Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with atypical antipsychotics, including olanzapine alone, as well as olanzapine taken concomitantly with fluoxetine. Assessment of the relationship between atypical antipsychotic use and glucose abnormalities is complicated by the possibility of an increased background risk of diabetes mellitus in patients with schizophrenia and the increasing incidence of diabetes mellitus in the general population. Given these confounders, the relationship between atypical antipsychotic use and hyperglycemia-related adverse events is not completely understood. However, epidemiological studies suggest an increased risk of treatment-emergent hyperglycemia-related adverse events in patients treated with the atypical antipsychotics. While relative risk estimates are inconsistent, the association between atypical antipsychotics and increases in glucose levels appears to fall on a continuum and olanzapine appears to have a greater association than some other atypical antipsychotics. Mean increases in blood glucose have been observed in patients treated (median exposure of 9.2 months) with olanzapine in phase I of the Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE). The mean increase of serum glucose (fasting and nonfasting samples) from baseline to the average of the two highest serum concentrations was 15.0 mg/dl. In an analysis of 7 controlled clinical studies, 2 of which were placebo-controlled, with treatment duration up to 12 weeks, SYMBYAX was associated with a statistically significantly greater mean change in random glucose compared to placebo (8.65 mg/dl versus -3.86 mg/dl). In patients with baseline normal random glucose levels (<140 mg/dl), 2.3% of those treated with SYMBYAX were found to have high glucose levels ( 200 mg/dl) during SYMBYAX treatment and were statistically significantly different compared to 0.3% of those treated with placebo. In patients with baseline borderline random glucose levels ( 140 mg/dl and <200 mg/dl), 34.1% of those treated with SYMBYAX were found to have high glucose levels ( 200 mg/dl) during SYMBYAX treatment and were statistically significantly different compared to 3.6% of those treated with placebo. The difference in mean changes between SYMBYAX and placebo was greater in patients with evidence of glucose dysregulation at baseline (including those patients diagnosed with diabetes mellitus or related adverse events, patients treated with anti-diabetic agents,

10 patients with a baseline random glucose level 200 mg/dl, or a baseline fasting glucose level 126 mg/dl). These patients had a greater mean increase in HbA 1c. Controlled fasting glucose data is limited for SYMBYAX; however, in an analysis of 5 placebo-controlled olanzapine monotherapy studies with treatment duration up to 12 weeks, olanzapine was associated with a greater mean change in fasting glucose levels compared to placebo (2.76 mg/dl vs 0.17 mg/dl). Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine and olanzapine and fluoxetine in combination have not been established in patients under the age of 18 years. In an analysis of 3 placebo-controlled olanzapine monotherapy studies of adolescent patients, including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), olanzapine was associated with a statistically significantly greater mean change in fasting glucose levels compared to placebo (2.68 mg/dl versus -2.59 mg/dl). In patients with baseline normal fasting glucose levels (<100 mg/dl), zero out of 124 (0%) of those treated with olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus 1 out of 53 (1.9%) of those treated with placebo. In patients with baseline borderline fasting glucose levels ( 100 mg/dl and <126 mg/dl), 2 out of 14 (14.3%) of those treated with olanzapine were found to have high glucose levels ( 126 mg/dl) during olanzapine treatment versus zero out of 13 (0%) of those treated with placebo. Physicians should consider the risks and benefits when prescribing SYMBYAX to patients with an established diagnosis of diabetes mellitus or having borderline increased blood glucose level (fasting 100 126 mg/dl, nonfasting 140 200 mg/dl). Patients taking SYMBYAX should be monitored regularly for worsening of glucose control. Patients with risk factors for diabetes mellitus (e.g., obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of anti-diabetic treatment despite discontinuation of the suspect drug. Hyperlipidemia Undesirable alterations in lipids have been observed with SYMBYAX use. Clinical monitoring, including baseline and follow-up lipid evaluations in patients using SYMBYAX, is advised. Significant, and sometimes very high (>500 mg/dl), elevations in triglyceride levels have been observed with SYMBYAX use. Significant increases in total cholesterol have also been seen with SYMBYAX use.

11 Controlled fasting lipid data is limited for SYMBYAX. In an analysis of 7 controlled clinical studies, 2 of which were placebo-controlled, with treatment duration up to 12 weeks, SYMBYAX-treated patients had an increase from baseline in mean random total cholesterol of 12.1 mg/dl compared to a statistically significantly different increase from baseline in mean random total cholesterol of 4.8 mg/dl for olanzapine-treated patients and a decrease in mean random total cholesterol of 5.5 mg/dl for placebo-treated patients. Table 3 shows categorical changes in nonfasting lipid values. Table 3. Changes in Nonfasting Lipids Values from Controlled Clinical Studies with Treatment Duration up to 12 Weeks Laboratory Analyte Category Change from Baseline Treatment Arm N Patients Nonfasting Triglycerides Increase by 50 mg/dl OFC 174 67.8% Olanzapine 172 72.7% OFC 57 0% (<150 mg/dl to 500 mg/dl) Olanzapine 58 0% OFC 106 15.1% ( 150 mg/dl and <500 mg/dl to Olanzapine 103 8.7% 500 mg/dl) Nonfasting Total Cholesterol Increase by 40 mg/dl (<200 mg/dl to 240 mg/dl) ( 200 mg/dl and <240 mg/dl to 240 a Statistically significant compared to olanzapine. b Statistically significant compared to placebo. OFC 685 35% a,b Olanzapine 749 22.7% Placebo 390 9% OFC 256 8.2% a,b Olanzapine 279 2.9% Placebo 175 1.7% OFC 213 36.2% a,b Olanzapine 261 27.6% mg/dl) Placebo 111 9.9% Controlled fasting lipid data is limited for SYMBYAX; however, in an analysis of 5 placebo-controlled olanzapine monotherapy studies with treatment duration up to 12 weeks, olanzapine-treated patients had statistically significant increases from baseline in mean fasting total cholesterol, LDL cholesterol, and triglycerides of 5.3 mg/dl, 3.0 mg/dl, and 20.8 mg/dl respectively compared to decreases from baseline in mean fasting total cholesterol, LDL cholesterol, and triglycerides of 6.1 mg/dl, 4.3 mg/dl, and 10.7 mg/dl for placebo-treated patients. For fasting HDL cholesterol, no statistically significant differences were observed between olanzapine-treated patients and placebo-treated patients. Mean increases in fasting lipid values (total cholesterol, LDL cholesterol, and triglycerides) were greater in

12 patients without evidence of lipid dysregulation at baseline, where lipid dysregulation was defined as patients diagnosed with dyslipidemia or related adverse events, patients treated with lipid lowering agents, patients with high baseline lipid levels. Table 4 shows categorical changes in fasting lipid values. Table 4. Changes in Lipids Values from Adult Placebo-Controlled Olanzapine Monotherapy Studies with Treatment Duration up to 12 Weeks Laboratory Analyte Category Change from Baseline Treatment Arm N Patients Triglycerides Increase by 50 mg/dl Olanzapine 745 39.6% a Placebo 402 26.1% Olanzapine 457 9.2% a (<150 mg/dl to 200 mg/dl) Placebo 251 4.4% Olanzapine 135 39.3% a ( 150 mg/dl and <200 mg/dl to 200 mg/dl) Placebo 65 20.0% Total Cholesterol Increase by 40 mg/dl Olanzapine 745 21.6% a Placebo 402 9.5% Olanzapine 392 2.8% (<200 mg/dl to 240 mg/dl) Placebo 207 2.4% Olanzapine 222 23.0% a ( 200 mg/dl and <240 mg/dl to 240 mg/dl) Placebo 112 12.5% Increase by 30 mg/dl Olanzapine 536 23.7% a Placebo 304 14.1% Olanzapine 154 0% LDL Cholesterol (<100 mg/dl to 160 mg/dl) Placebo 82 1.2% Olanzapine 302 10.6% ( 100 mg/dl and <160 mg/dl to 160 mg/dl) Placebo 173 8.1% a Statistically significant compared to placebo. In phase 1 of the Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE), over a median exposure of 9.2 months, the mean increase in triglycerides in patients taking olanzapine was 40.5 mg/dl. In phase 1 of CATIE, the median increase in total cholesterol was 9.4 mg/dl. Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine and olanzapine and fluoxetine in combination have not been established in patients under the age of 18 years. In an analysis of 3 placebo-controlled olanzapine monotherapy studies of adolescent patients, including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), for fasting HDL cholesterol, no statistically significant differences were observed between olanzapine-treated patients and placebo-treated patients. Table 5 shows categorical changes in fasting lipid values in adolescent patients.

13 Table 5. Changes in Lipids Values from Adolescent Placebo-Controlled Olanzapine Monotherapy Studies Laboratory Analyte Category Change from Baseline Treatment Arm N Patients Triglycerides Increase by 50 mg/dl Olanzapine 138 37.0% a Placebo 66 15.2% Olanzapine 67 26.9% (<90 mg/dl to 130 mg/dl) Placebo 28 10.7% Olanzapine 37 59.5% ( 90 mg/dl and <130 mg/dl to 130 mg/dl) Placebo 17 35.3% Total Cholesterol Increase by 40 mg/dl Olanzapine 138 14.5% a Placebo 66 4.5% Olanzapine 87 6.9% (<170 mg/dl to 200 mg/dl) Placebo 43 2.3% Olanzapine 36 38.9% a ( 170 mg/dl and <200 mg/dl to 200 mg/dl) Placebo 13 7.7% Increase by 30 mg/dl Olanzapine 137 17.5% Placebo 63 11.1% Olanzapine 98 5.1% LDL Cholesterol (<110 mg/dl to 130 mg/dl) Placebo 44 4.5% Olanzapine 29 48.3% a ( 110 mg/dl and <130 mg/dl to 130 mg/dl) Placebo 9 0% a Statistically significant compared to placebo. Weight Gain Potential consequences of weight gain should be considered prior to starting SYMBYAX. Patients receiving SYMBYAX should receive regular monitoring of weight. In an analysis of 7 controlled clinical studies, 2 of which were placebo-controlled, the mean weight increase for SYMBYAX-treated patients was statistically significantly greater than placebo-treated (4 kg vs -0.3 kg). Twenty-two percent of SYMBYAX-treated patients gained at least 7% of their baseline weight, with a median exposure of 6 weeks. This was statistically significantly greater than in placebo-treated patients (1.8%). Approximately 3% of SYMBYAX-treated patients gained at least 15% of their baseline weight, with a median exposure of 8 weeks. This was statistically significantly greater than in placebo-treated patients (0%). Clinically significant weight gain was observed across all baseline Body Mass Index (BMI) categories. Discontinuation due to weight gain occurred in 2.5% of SYMBYAX-treated patients and zero placebo-treated patients. Table 6 includes data on weight gain with olanzapine pooled from 68 clinical trials. The data in each column represent data for those patients who completed treatment periods of the durations specified.

14 Table 6. Weight Gain with Olanzapine Use Amount Gained kg (lb) 6 Weeks (N=2976) 6 Months (N=1536) 12 Months (N=778) 24 Months (N=422) 0 27 21 20 22 0-5 (0-11 lb) 57 34 25 22 5-10 (11-22 lb) 15 26 25 22 10-15 (22-33 lb) 2 12 16 18 >15 (>33 lb) 0 6 14 16 During long-term continuation therapy with olanzapine monotherapy (238 median days of exposure), 56% of olanzapine patients met the criterion for having gained greater than 7% of their baseline weight. Average weight gain during long-term therapy was 5.4 kg. Olanzapine Monotherapy in Adolescents The safety and efficacy of olanzapine and olanzapine and fluoxetine in combination have not been established in patients under the age of 18 years. In an analysis of 4 placebo-controlled olanzapine monotherapy studies of adolescent patients (ages 13 to 17 years), including those with schizophrenia (6 weeks) or bipolar disorder (manic or mixed episodes) (3 weeks), olanzapine-treated patients gained an average of 4.6 kg, which was statistically significantly different compared to an average of 0.3 kg in placebo-treated patients, with a median exposure of 3 weeks; 40.6% of olanzapine-treated patients gained at least 7% of their baseline body weight, which was statistically significantly different compared to 9.8% of placebo-treated patients, with a median exposure of 4 weeks; 7.1% of olanzapine-treated patients gained at least 15% of their baseline weight, compared to 2.7% of placebo-treated patients, with a median exposure of 19 weeks. Clinically significant weight gain was observed across all baseline Body Mass Index (BMI) categories, but mean changes in weight were greater in adolescents with BMI categories above normal at baseline. Discontinuation due to weight gain occurred in 1% of olanzapine-treated patients, compared to zero placebo-treated patients. During long-term continuation therapy with olanzapine, 65% of olanzapine-treated patients met the criterion for having gained greater than 7% of their baseline weight. Average weight gain during long-term therapy was 7.4 kg. Information for Patients: Hyperglycemia Patients should be advised of the potential risk of hyperglycemia-related adverse events. Patients should be monitored regularly for worsening of glucose control.

15 Weight Gain Patients should be counseled that SYMBYAX is associated with weight gain. Patients should have their weight monitored regularly. References: 1. Lieberman, JA, Stroup, TS, McEvoy, JP, S. Swartz, MS, Rosenheck, RA, Perkins, DO, Keefe, RSE, Davis, SM, Davis, CE, Lebowitz, BD, Severe, J, Hsiao, JK. 2005. Effectiveness of Antipsychotic Drugs in Patients with Chronic Schizophrenia. New Engl J Med 353(12): 1209-1223. 2. McEvoy, JP, Lieberman,JA, Perkins, DO, Hamer, RM, Gu, H, Lazarus, A, Sweitzer, D, Olexy, C, Weiden, P, Strakowski, SD. 2007. Efficacy and Tolerability of Olanzapine, Quetiapine, and Risperidone in the Treatment of Early Psychosis: A Randomized, Double-Blind 52-Week Comparison. Am J Psychiatry 164:1050 1060. 3. American Diabetes Association, American Psychiatric Association, American Association of Clinical Endocrinologists, and North American Association for Study of Obesity. 2004. Consensus Development Conference on Antipsychotic Drugs and Obesity and Diabetes. Diabetes Care 27: 596-601. http://care.diabetesjournals.org/cgi/content/full/27/2/596 Zyprexa (olanzapine) is indicated for the short-term and maintenance treatment of schizophrenia. Zyprexa is also indicated as monotherapy or in combination with lithium or valproate for the shortterm treatment of acute mixed or manic episodes associated with Bipolar I Disorder and as maintenance treatment in bipolar disorder. Symbyax (olanzapine and fluoxetine HCl capsules) is indicated for treatment of depressive episodes associated with bipolar disorder.