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Fluoxetine (2004) ��������������������������� �������������������������������������������� ����������������������������������� ��������������������� NTP-CERHR Monograph on the Potential Human Reproductive and Developmental Effects of Fluoxetine November 2004 NIH Publication No. 05 - 4471 Table of Contents Preface .............................................................................................................................................v Introduction .................................................................................................................................... vi NTP Brief on Fluoxetine .................................................................................................................1 References ........................................................................................................................................5 Appendix I. NTP-CERHR Fluoxetine Expert Panel Preface ..............................................................................................................................I-1 Expert Panel ......................................................................................................................I-2 Appendix II. Expert Panel Report on Fluoxetine ........................................................................ II-i Table of Contents ........................................................................................................... II-iii Abbreviations ...................................................................................................................II-v List of Tables ................................................................................................................ II-viii List of Figures ................................................................................................................ II-ix Preface .............................................................................................................................II-x Chemistry, Usage and Human Exposure .........................................................................II-1 General Toxicology and Biologic Effects ......................................................................II-17 Developmental Toxicity Data .........................................................................................II-44 Reproductive Toxicity Data ..........................................................................................II-104 Summaries, Conclusions and Critical Data Needs ......................................................II-143 References ....................................................................................................................II-147 Appendix III. Public Comments on Expert Panel Report on Fluoxetine Eli Lilly and Company ................................................................................................... III-1 Lee S. Cohen ................................................................................................................ III-11 Robert L. Brent ............................................................................................................ III-14 PETA ............................................................................................................................ III-20 Terry Young .................................................................................................................. III-23 iii [This page intentionally left blank] iv Preface The National Toxicology Program (NTP) chemical is hazardous to humans. The panel established the NTP Center for the Evaluation also identifies areas of uncertainty and where of Risks to Human Reproduction (CERHR) additional data are needed. The CERHR expert in 1998. The CERHR is a publicly accessible panels use explicit guidelines to evaluate the resource for information about adverse repro- scientific literature and prepare the expert panel ductive and/or developmental health effects reports. Expert panel reports are made public associated with exposure to environmental and comments are solicited. and/or occupational chemicals. The CERHR is located at the National Institute of Environmen- Next, the CERHR prepares the NTP-CERHR tal Health Sciences (NIEHS) of the National monograph. The NTP-CERHR monograph Institutes of Health and Dr. Michael Shelby is includes the NTP brief on the chemical evalu- the director.1 ated, the expert panel report, and public com- ments on that report. The goal of the NTP brief The CERHR broadly solicits nominations of is to provide the public, as well as government chemicals for evaluation from the public and health, regulatory, and research agencies, with private sectors. The CERHR follows a formal the NTP’s interpretation of the potential for process for review and evaluation of nominated the chemical to adversely affect human repro- chemicals that includes multiple opportunities ductive health or children’s health. The NTP- for public comment. Chemicals are selected for CERHR monograph is made publicly available evaluation based upon several factors including electronically on the CERHR web site and in the following: hard copy or CD-ROM from the CERHR. • potential for human exposure from use and occurrence in the environment 1 Information about the CERHR is available on the • extent of public concern web at <http://cerhr.niehs.nih.gov> or by contact- • production volume ing the director: • extent of data from reproductive and devel- NIEHS, P.O. Box 12233, MD EC-32, opmental toxicity studies Research Triangle Park, NC 27709 919-541-3455 [phone] The CERHR convenes a scientific expert panel 919-316-4511 [fax] that meets in a public forum to review, discuss, [email protected] [email] and evaluate the scientific literature on the Information about the NTP is available on the web selected chemical. Public comment is invited at <http://ntp-server.niehs.nih.gov> or by contact- prior to and during the meeting. The expert panel ing the NTP Liaison and Scientific Review Office produces a report on the chemical’s reproductive at the NIEHS: and developmental toxicities and provides its [email protected] [email] opinion of the degree to which exposure to the 919-541-0530 [phone] v Introduction In 1999, the CERHR Core Committee, an meeting of the CERHR Fluoxetine Expert Panel advisory committee composed of representatives on March 3-5, 2004 in Alexandria, VA. from NTP member agencies, recommended fluoxetine for expert panel review. Fluoxetine This fluoxetine monograph includes the NTP (Prozac®, Sarafem™, CAS RN 54910-89-3), an brief on fluoxetine, a list of the expert panel antidepressant, is a widely prescribed drug in the members (Appendix I), the expert panel report United States. The CERHR selected fluoxetine on fluoxetine (Appendix II), and all public com- hydrochloride for evaluation because of: ments received on the expert panel report on (1) numerous reproductive and develop- fluoxetine (Appendix III). The NTP-CERHR mental studies in laboratory animals and monograph is intended to serve as a single, col- humans lective source of information on the potential (2) human exposure information for fluoxetine to adversely affect human repro- (3) changing prescription patterns duction or development. Those interested in reading this monograph may include individu- Fluoxetine hydrochloride, under the name als, members of public interest groups, and staff Sarafem™, is now being prescribed to treat of health and regulatory agencies. premenstrual dysphoric disorder, potentially increasing the number of exposures for women The NTP brief included within this monograph of childbearing age. The U.S. Food and Drug presents the NTP’s interpretation of the poten- Administration (FDA) recently approved fluox- tial for fluoxetine exposure to cause adverse re- etine for use in 7-17 year-olds thereby increasing productive or developmental effects in people. exposures of children. As part of the evaluation The brief is intended to provide clear, balanced, of fluoxetine, the CERHR convened a panel of and scientifically sound information. It is based scientific experts (Appendix I) to review, dis- on the contents of the expert panel report on cuss, and evaluate the scientific evidence on fluoxetine, public comments on that report, and the potential reproductive and developmental additional scientific information that became toxicities of the chemical. There was a public available following the expert panel meeting. vi NTP Brief on Fluoxetine NTP Brief NTP What is Fluoxetine? Fluoxetine is a pharmaceutical drug prescribed methylated metabolite, norfluoxetine, are both for a variety of psychiatric disorders, particular- therapeutically active. Fluoxetine hydrochlo- ly depression. Fluoxetine is used in the treatment ride is marketed in 10 mg, 20 mg, and 40 mg of depression, premenstrual dysphoric disorder tablets, as an oral solution of 20 mg/5 ml, and in (severe premenstrual syndrome), obsessive- a 90 mg capsule for single weekly dosage. compulsive disorder, panic disorder, and bulimia nervosa. It is also approved by the FDA to treat The annual production volume for fluoxetine is depression and obsessive-compulsive disorder in not available. However, according to the FDA, children 7-17 years old. On October 15, 2004 the in 2002, there were 1.2 billion tablets or tea- FDA issued a press release (FDA, 2004) noting spoons of fluoxetine sold to US pharmacies and that manufacturers of antidepressant medica- approximately 26.7 million prescriptions were tions, including fluoxetine, were being directed dispensed
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