Skip to main content
  • ASM
    • Antimicrobial Agents and Chemotherapy
    • Applied and Environmental Microbiology
    • Clinical Microbiology Reviews
    • Clinical and Vaccine Immunology
    • EcoSal Plus
    • Eukaryotic Cell
    • Infection and Immunity
    • Journal of Bacteriology
    • Journal of Clinical Microbiology
    • Journal of Microbiology & Biology Education
    • Journal of Virology
    • mBio
    • Microbiology and Molecular Biology Reviews
    • Microbiology Resource Announcements
    • Microbiology Spectrum
    • Molecular and Cellular Biology
    • mSphere
    • mSystems
  • Log in
  • My alerts
  • My Cart

Main menu

  • Home
  • Articles
    • Current Issue
    • Accepted Manuscripts
    • COVID-19 Special Collection
    • Archive
    • Minireviews
  • For Authors
    • Submit a Manuscript
    • Scope
    • Editorial Policy
    • Submission, Review, & Publication Processes
    • Organization and Format
    • Errata, Author Corrections, Retractions
    • Illustrations and Tables
    • Nomenclature
    • Abbreviations and Conventions
    • Publication Fees
    • Ethics Resources and Policies
  • About the Journal
    • About AAC
    • Editor in Chief
    • Editorial Board
    • For Reviewers
    • For the Media
    • For Librarians
    • For Advertisers
    • Alerts
    • AAC Podcast
    • RSS
    • FAQ
  • Subscribe
    • Members
    • Institutions
  • ASM
    • Antimicrobial Agents and Chemotherapy
    • Applied and Environmental Microbiology
    • Clinical Microbiology Reviews
    • Clinical and Vaccine Immunology
    • EcoSal Plus
    • Eukaryotic Cell
    • Infection and Immunity
    • Journal of Bacteriology
    • Journal of Clinical Microbiology
    • Journal of Microbiology & Biology Education
    • Journal of Virology
    • mBio
    • Microbiology and Molecular Biology Reviews
    • Microbiology Resource Announcements
    • Microbiology Spectrum
    • Molecular and Cellular Biology
    • mSphere
    • mSystems

User menu

  • Log in
  • My alerts
  • My Cart

Search

  • Advanced search
Antimicrobial Agents and Chemotherapy
publisher-logosite-logo

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Accepted Manuscripts
    • COVID-19 Special Collection
    • Archive
    • Minireviews
  • For Authors
    • Submit a Manuscript
    • Scope
    • Editorial Policy
    • Submission, Review, & Publication Processes
    • Organization and Format
    • Errata, Author Corrections, Retractions
    • Illustrations and Tables
    • Nomenclature
    • Abbreviations and Conventions
    • Publication Fees
    • Ethics Resources and Policies
  • About the Journal
    • About AAC
    • Editor in Chief
    • Editorial Board
    • For Reviewers
    • For the Media
    • For Librarians
    • For Advertisers
    • Alerts
    • AAC Podcast
    • RSS
    • FAQ
  • Subscribe
    • Members
    • Institutions
Pharmacology

Pharmacokinetics of Tigecycline after Single and Multiple Doses in Healthy Subjects

Gopal Muralidharan, Marlynne Micalizzi, John Speth, Donald Raible, Steven Troy
Gopal Muralidharan
Clinical Research, Wyeth Research, Collegeville, Pennsylvania
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Marlynne Micalizzi
Clinical Research, Wyeth Research, Collegeville, Pennsylvania
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
John Speth
Clinical Research, Wyeth Research, Collegeville, Pennsylvania
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Donald Raible
Clinical Research, Wyeth Research, Collegeville, Pennsylvania
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Steven Troy
Clinical Research, Wyeth Research, Collegeville, Pennsylvania
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • For correspondence: troys@wyeth.com
DOI: 10.1128/AAC.49.1.220-229.2005
  • Article
  • Figures & Data
  • Info & Metrics
  • PDF
Loading

Article Figures & Data

Figures

  • Tables
    • Open in new tab
    • Download powerpoint
    • Open in new tab
    • Download powerpoint
    • Open in new tab
    • Download powerpoint
    FIG. 1.

    Mean tigecycline concentrations in serum in the single ascending dose study in fasting subjects as 1-h infusions (A), as 1-h infusions in the 200-mg dose group (B), and as 4-h infusions (C).

  • FIG. 2.
    • Open in new tab
    • Download powerpoint
    FIG. 2.

    Tigecycline concentrations (mean plus the standard deviation) serum in multiple ascending dose study on day 1 (A) and day 10 (B).

  • FIG. 3.
    • Open in new tab
    • Download powerpoint
    FIG. 3.

    Relationship between tigecycline dose in the single ascending dose study and Cmax (A) and AUC (B).

Tables

  • Figures
  • TABLE 1.

    Tigecycline regimen description

    StudyCohortNo. active/no. placeboDosage regimenInfusion duration (h)Infusion vol (ml)Fasted or fedAntiemetic medication
    SAD16/212.5 mg1250FastedNone
    26/225 mg1250FastedNone
    36/250 mg1250FastedNone
    46/275 mg1250FastedNone
    56/2100 mg1250FastedNone
    66/2200 mg1250FastedNone
    76/2200 mg4250FastedNone
    86/2200 mg1250FedNone
    96/2300 mg1250FedNone
    106/2300 mg4250FedNone
    116/2200 mg1250FastedOndansetron
    MAD16/225 mg q12h1250FedNone
    26/250 mg q12h1250FedNone
    36/2100 mg q12h1250FedNone
    46/275 mg q12h1250FedNone
    VVIR16/3100 mg + 50 mg q12h1100FedNone
    27/3100 mg + 50 mg q12h0.5100FedNone
    36/3100 mg + 50 mg q12h1250FedNone
  • TABLE 2.

    Mean pharmacokinetic parameters (%CV) of tigecycline after various single i.v. doses in SAD study

    ParameterMean valuea (% CV) after:P
    1-h infusion (group no., tigecycline [mg], fasting or fed)4-h infusion (group no., tigecycline [mg], fasting or fed)
    1, 12.5 fasting2, 25, fasting3, 50, fasting4, 75, fasting5, 100, fasting6, 200, fasting8, 200, fed11, 200, fastingb9, 300, fed7, 200, fasting10, 300, fed
    C max (ng/ml)108.5 (10)252 (25)383 (17)566 (14)911 (29)1,643 (18)1,528 (22)2,189 (30)2,817 (17)680 (22)960 (10)0.001
    AUC (ng h/ml)753 (68)2,255 (45)2,558 (21)3,658 (27)6,396 (10)12,426 (23)11,719 (19)14,462 (17)17,856 (10)14,237 (22)16,732 (16)0.06
    CL (l/h/kg)0.29 (67)0.20 (50)0.28 (14)0.29 (16)0.20 (13)0.25 (22)0.22 (12)0.20 (19)0.25 (11)0.24 (11)0.26 (13)0.27
    V ss (l/kg)2.8* (34)6.4* (20)6.4* (31)7.5* (10)8.6 (18)11 (25)13 (18)12 (43)12 (20)14 (11)12 (24)0.001
    t 1/2 (h)11* (84)32* (64)18* (21)21* (25)38 (14)42 (28)54 (28)53 (20)46 (13)58 (14)42 (23)0.001
    CLR (l/h)NDNDNDND2.6 (26)3 (50)2.2 (22)1.8 (24)2.7 (23)NA2 (28)0.13
    fe (%)2.1 (113)6.5 (39)1.9 (72)8 (37)11 (25)12 (31)7.8 (25)8.5 (38)10.4 (22)NA8 (39)0.001
    • ↵ a ND, could not be determined accurately because of low concentrations in urine and serum; NA, not available. Values marked with an asterisk may not be reliably estimated due to the limit of quantification.

    • ↵ b Received ondansetron.

  • TABLE 3.

    Mean pharmacokinetic parameters of tigecycline after various i.v. doses infused over a 1-h period q12h in the MAD study

    Tigecycline dose group (mg)Mean Value (%CV) at:
    Day 1Day 10a
    Cmax (ng/ml)AUC0-τ (ng h/ml)Cmax (ng/ml)AUCss (ng h/ml)t1/2 (h)CL (l/h/kg)Vss (l/kg)
    25261 (14)796 (8)324 (17)1,482 (18)49.3 (72)0.20 (17)8.6 (23)
    50487 (17)1,440 (14)621 (15)3,069 (12)36.9 (32)0.20 (9)7.2 (7)
    100816 (15)2,389 (13)1,173 (15)4,980 (19)66.5 (34)0.24 (20)9.1 (32)
    • ↵ a Day 10 values for the 100-mg tigecycline dose group are actually day 9 values.

  • TABLE 4.

    Trough concentrations of tigecycline among various dose groups after multiple doses of tigecycline given as a 1-h infusion in the MAD study

    DayMean (% cv) concn (ng/ml)a at:P
    25 mg50 mg100 mg
    786 (28)153 (13)214 (13)0.07
    881 (34)195 (15)255 (16)0.12
    983 (28)204 (17)257 (17)0.06
    1087 (26)145 (16)NA0.23
    • ↵ a For comparison among dose groups, concentrations were dose normalized to the 100-mg dose before statistical analysis. For the 25-, 50-, and 100-mg dose groups, the P values were 0.98, 0.01, and 0.37, respectively. NA, not available.

PreviousNext
Back to top
Download PDF
Citation Tools
Pharmacokinetics of Tigecycline after Single and Multiple Doses in Healthy Subjects
Gopal Muralidharan, Marlynne Micalizzi, John Speth, Donald Raible, Steven Troy
Antimicrobial Agents and Chemotherapy Dec 2004, 49 (1) 220-229; DOI: 10.1128/AAC.49.1.220-229.2005

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Print

Alerts
Sign In to Email Alerts with your Email Address
Email

Thank you for sharing this Antimicrobial Agents and Chemotherapy article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Pharmacokinetics of Tigecycline after Single and Multiple Doses in Healthy Subjects
(Your Name) has forwarded a page to you from Antimicrobial Agents and Chemotherapy
(Your Name) thought you would be interested in this article in Antimicrobial Agents and Chemotherapy.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Share
Pharmacokinetics of Tigecycline after Single and Multiple Doses in Healthy Subjects
Gopal Muralidharan, Marlynne Micalizzi, John Speth, Donald Raible, Steven Troy
Antimicrobial Agents and Chemotherapy Dec 2004, 49 (1) 220-229; DOI: 10.1128/AAC.49.1.220-229.2005
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Top
  • Article
    • ABSTRACT
    • MATERIALS AND METHODS
    • RESULTS
    • DISCUSSION
    • ACKNOWLEDGMENTS
    • FOOTNOTES
    • REFERENCES
  • Figures & Data
  • Info & Metrics
  • PDF

KEYWORDS

Anti-Bacterial Agents
minocycline

Related Articles

Cited By...

About

  • About AAC
  • Editor in Chief
  • Editorial Board
  • Policies
  • For Reviewers
  • For the Media
  • For Librarians
  • For Advertisers
  • Alerts
  • AAC Podcast
  • RSS
  • FAQ
  • Permissions
  • Journal Announcements

Authors

  • ASM Author Center
  • Submit a Manuscript
  • Article Types
  • Ethics
  • Contact Us

Follow #AACJournal

@ASMicrobiology

       

ASM Journals

ASM journals are the most prominent publications in the field, delivering up-to-date and authoritative coverage of both basic and clinical microbiology.

About ASM | Contact Us | Press Room

 

ASM is a member of

Scientific Society Publisher Alliance

 

American Society for Microbiology
1752 N St. NW
Washington, DC 20036
Phone: (202) 737-3600

Copyright © 2021 American Society for Microbiology | Privacy Policy | Website feedback

Print ISSN: 0066-4804; Online ISSN: 1098-6596