Absorptive kinetics of transdermal fentanyl
Download
1 / 22

Absorptive Kinetics of Transdermal Fentanyl - PowerPoint PPT Presentation


  • 108 Views
  • Uploaded on

Absorptive Kinetics of Transdermal Fentanyl. Robert Leonard, PharmD candidate University of Florida College of Pharmacy. Overview. Rationale Barriers TTS-fentanyl Pharmacokinetics Studies of pharmacokinetic variability. Rationale. Continuous infusion Noninvasive nature

loader
I am the owner, or an agent authorized to act on behalf of the owner, of the copyrighted work described.
capcha
Download Presentation

PowerPoint Slideshow about ' Absorptive Kinetics of Transdermal Fentanyl' - nichole-lucas


An Image/Link below is provided (as is) to download presentation

Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.


- - - - - - - - - - - - - - - - - - - - - - - - - - E N D - - - - - - - - - - - - - - - - - - - - - - - - - -
Presentation Transcript
Absorptive kinetics of transdermal fentanyl

Absorptive Kinetics of Transdermal Fentanyl

Robert Leonard, PharmD candidate

University of Florida

College of Pharmacy


Overview
Overview

  • Rationale

  • Barriers

  • TTS-fentanyl

  • Pharmacokinetics

  • Studies of pharmacokinetic variability


Rationale
Rationale

  • Continuous infusion

  • Noninvasive nature

  • Special populations

    • Protracted vomiting

    • Dysphagia

  • Less frequent dosing


Barriers
Barriers

  • Epidermal microflora

  • Stratum corneum

  • Subcutaneous vasculature

  • Physicochemical properties

    • MW

    • Lipophilicity




Kinetics
Kinetics

  • Absorption

    • F = 0.92

    • Protein binding = 79 - 97%

    • Tmax = 35 hours

  • Distribution

    • Vd = 3 – 8 L/kg

  • Metabolism

    • CYP3A4

    • Major: norfentanyl

    • Minor: hydroxyfentanyl, hydroxynorfentanyl, despropionylfentanyl



Kinetics2
Kinetics

  • Elimination

    • Cl = 34.2 – 52.8L/hr

    • T1/2 = 17hrs (after removal)


Study
Study

  • Solassol I, Caumette L, Bressolle F, et al. “Inter- and intra-individual variation in transdermal fentanyl absorption in cancer pain patients.” Oncology Reports 14:1029-1036, 2005.




Absorption kinetics2
Absorption Kinetics

125 mcg/hr

175 mcg/hr

100 mcg/hr


Results
Results

  • Significant findings (P < 0.05)

    • Age: <65, 65-75, >75

      • P = 0.030

    • Primary cancer location: head and neck, GI, GU, Lung, Brest, others

      • P = 0.006

  • Findings approaching significance (P ≤ 0.06)

    • Occlusive bandage: yes, no

      • P = 0.060

    • Temperature: <38, 38-40, >40

      • P = 0.051


Limitations
Limitations

  • Indirect assay


Study1
Study

  • Ashburn MA, Ogden LL, Zhang J, et al. “The pharmacokinetics of transdermal fentanyl delivered with and without controlled heat.” The Journal of Pain 4: 291-297, 2003.




Clinical pearls
Clinical Pearls

  • Avoid cutting patches.

  • Avoid occlusive bandages.

  • Avoid heat.

  • Dose according to patient response.

  • Sustained release after removal.


References
References

Ashburn MA, Ogden LL, Zhang J, et al. “The pharmacokinetics of transdermal fentanyl delivered with and without controlled heat.” The Journal of Pain 4: 291-297, 2003.

Grond S, Radbruch L, Lehmann K. “Clinical pharmacokinetics of transdermal opioids: Focus on transdermal fentanyl.” Clinical Pharmacokinetics 38: 59-89, 2000.

Muijsers RB, Wagstaff AJ. “Transdermal fentanyl: An updated review of its pharmacological properties and therapeutic efficacy in chronic cancer pain control.” Drugs 61:2289-2307, 2001.

Solassol I, Caumette L, Bressolle F, et al. “Inter- and intra-individual variation in transdermal fentanyl absorption in cancer pain patients.” Oncology Reports 14:1029-1036, 2005.