Hostname: page-component-8448b6f56d-t5pn6 Total loading time: 0 Render date: 2024-04-25T00:45:00.380Z Has data issue: false hasContentIssue false
  • English
  • Français

Clinical Pharmacology and Pharmacokinetics of Fluoxetine: A Review

Published online by Cambridge University Press:  06 August 2018

R. F. Bergstrom ,
L. Lemberger ,
N. A. Farid  and
R. L. Wolen
R. F. Bergstrom*
Affiliation:
Lilly Laboratory for Clinical Research, Eli Lilly and Company, and the Departments of Pharmacology, Medicine and Psychiatry, Indiana University School of Medicine
L. Lemberger
Affiliation:
Lilly Laboratory for Clinical Research, Eli Lilly and Company, and the Departments of Pharmacology, Medicine and Psychiatry, Indiana University School of Medicine
N. A. Farid
Affiliation:
Lilly Laboratory for Clinical Research, Eli Lilly and Company, and the Departments of Pharmacology, Medicine and Psychiatry, Indiana University School of Medicine
R. L. Wolen
Affiliation:
Lilly Laboratory for Clinical Research, Eli Lilly and Company, and the Departments of Pharmacology, Medicine and Psychiatry, Indiana University School of Medicine
*
∗Correspondence
Get access Rights & Permissions [Opens in a new window]

Extract

Drugs are discovered by a variety of approaches, which include a systematic evaluation of synthetic compounds, using extensive structure activity relationships. After a lead compound which possesses desirable pharmacological properties is found, through the exhaustive screening of a variety of compounds, a number of congeners are then synthesised and tested, using specific physiological or biochemical models of therapeutic agents. The discovery of fluoxetine involved this complex process, and led to the description in the literature of one of the first selective serotonin uptake inhibitors (Wong et al, 1974); it was subsequently tested clinically, and these studies demonstrated its effectiveness and safety as an antidepressant drug (Chouinard, 1985). This paper reviews the published information relevant to fluoxetine's pharmacology and pharmacokinetics in man.

Type
Research Article
Information
The British Journal of Psychiatry , Volume 153 , Issue S3: Progress in Antidepressant Therapy , September 1988 , pp. 47 - 50
Copyright
Copyright © 1988 The Royal College of Psychiatrists 

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

Aronoff, G. R., Bergstrom, R. F., Prottratz, S. T., Sloan, R. S., Wolen, R. L. & Lemberger, L. (1984) Fluoxetine kinetics and protein binding in normal and impaired renal function. Clinical Pharmacology and Therapeutics, 36, 138–144.CrossRefGoogle ScholarPubMed
Bergstrom, R. F., Farid, K. Z., McClurg, J. E. & Lemberger, L. (1983) The pharmacokinetics of fluoxetine in elderly subjects. Abstracts II World Conference on Clinical Pharmacology and Therapeutics, 515, 88.Google Scholar
Bergstrom, R. F., Wolen, R., Dhahir, P., Hatcher, B., Werner, N. & Lemberger, L. (1984) Effect of food on the absorption of fluoxetine in normal subjects. Abstracts of the American Pharmaceutical Association Academy of Pharmaceutical Sciences, 14, 110.Google Scholar
Bergstrom, R. F., Wolen, R., Lemberger, L., Dhahir, P. & Barrett, J. L. (1985) Fluoxetine single dose-multiple dose kinetics. Abstracts of the American Pharmaceutical Association Academy of Pharmaceutical Sciences, 15, 137.Google Scholar
Bergstrom, R. F., van Lier, R. B. L., Lemberger, L. & Tenbarge, J. L. (1986a) Absolute bioavailability of fluoxetine in beagle dogs. Abstracts of the American Pharmaceutical Association Academy of Pharmaceutical Sciences, 16, 126.Google Scholar
Bergstrom, R. F., Wolen, R. L., Lemberger, L., Tenbarge, J. L. & Masco, H. L. (1986b) Fluoxetine steady state pharmacokinetics in depressed patients. Abstracts of the American Pharmaceutical Association Academy of Pharmaceutical Sciences, 16, 125.Google Scholar
Bowsher, D. J., Rowe, H. M. & Lemberger, L. (1985) Pressor responses to tyramine and norepinephrine after subchronic administration of fluoxetine to man. Federation Proceedings, 44, 1244.Google Scholar
Chouinard, G. (1985) A double-blind controlled clinical trial of fluoxetine and amitriptyline in the treatment of outpatients with major depressive disorders. Journal of Clinical Psychiatry, 46, 32–37.Google Scholar
Farid, N. A., Bergstrom, R. F., Lemberger, L., Ziege, E. A., Tenbarge, J., Wolen, R. L. & Dhahir, P. H. (1986) Studies on the disposition of fluoxetine and radioactive isotopes. I5th CINP Congress, Puerto Rico, Collegium Internationale Neuro-Psychopharmacologium. Google Scholar
Fuller, R. W., Snoddy, H. D., Perry, K. W., Bymaster, F. P. & Wong, D. T. (1977) Importance of duration of drug action in the antagonism of p-chloroamphetamine depletion of brain serotonin - comparison of fluxotine and chlorimipramine. Biochemical Pharmacology, 29, 193–198.Google Scholar
Lemberger, L., Terman, S., Rowe, H. & Billings, R. (1976) The effect of nisoxetine (Lilly compound 94939), a potential antidepressant, on biogenic amine uptake in man. British Journal of Clinical Pharmacology, 3, 215–220.Google Scholar
Lemberger, L., Rowe, H., Carmichael, R., Horng, J., Bymaster, F. & Wong, D. (1978a) Fluoxetine, a selective serotonin uptake inhibitor. Clinical Pharmacology and Therapeutics, 23, 421–429.Google Scholar
Lemberger, L., Rowe, H., Carmichael, R., Oldham, S., Horng, J. S., Bymaster, F. P. & Wong, D. T. (1978b) Pharmacologic effects in man of a specific serotonin reuptake inhibitor. Science, 199, 436–437.Google Scholar
Lemberger, L., Rowe, H., Bergstrom, R. F., Farid, K. Z. & Enas, G. G. (1985) The effect of fluoxetine on the psychomotor performance, physiologic responses and pharmacokinetic disposition of ethanol. Clinical Pharmacology and Therapeutics, 37, 658–644.Google Scholar
Lemberger, L., Rowe, H., Bergstrom, R. F., Bosomworth, J. & Tenbarge, J. (1987) The effect of fluoxetine on the pharmacokinetics and psychomotor responses of diazepam. Clinical Pharmacology and Therapeutics, 43, 412–419.Google Scholar
Nash, J. F., Bopp, R. J., Carmichael, R. H., Farid, K. Z. & Lemberger, L. (1982) Determination of fluoxetine and norfluoxetine in plasma by gas-chromatography with electron-capture detection. Clinical Chemistry, 28, 2100–2102.CrossRefGoogle ScholarPubMed
Schenker, S., Bergstrom, R. F., Wolen, R. L. & Lemberger, L. (1988) Fluoxetine disposition and elimination in cirrhosis. Clinical Pharmacology and Therapeutics (in press).Google Scholar
Wong, D. T., Horng, J. S., Bymaster, F. P., Hauser, K. L. & Molloy, B. B. (1974) A selective inhibitor of serotonin uptake. Lilly 110140, 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine. Life Sciences, 15, 471–479.CrossRefGoogle ScholarPubMed
Submit a response

eLetters

No eLetters have been published for this article.