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For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration depends on how long the plasma concentration remains above Cmin.Two primary factors influence this duration: dose size and the rate of drug removal from the action site. Both depend on the drug's redistribution to poorly perfused tissues and elimination processes. A larger dose promotes rapid onset and prolongs the effect's duration.Consider a...
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Related Experiment Video

Updated: May 15, 2026

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
08:38

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Published on: November 8, 2015

Sublingual tacrolimus: a pharmacokinetic evaluation pilot study.

Demetra Tsapepas1, Stuart Saal, Steven Benkert

  • 1NewYork-Presbyterian Hospital, Columbia University Medical Center, New York, New York 10032, USA. det9021@nyp.org

Pharmacotherapy
|January 12, 2013
PubMed
Summary

This study compared sublingual and oral tacrolimus pharmacokinetics. A 1:1 oral-to-sublingual dose conversion may be suitable with clotrimazole, but a 2:1 conversion might be needed without interacting drugs.

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Area of Science:

  • Pharmacology
  • Transplantation Medicine
  • Clinical Pharmacy

Background:

  • Tacrolimus is a key immunosuppressant in organ transplantation.
  • Drug interactions, particularly at the intestinal level, can significantly alter tacrolimus pharmacokinetics.
  • Understanding dose conversions between administration routes is crucial for patient management.

Purpose of the Study:

  • To compare the pharmacokinetic parameters of sublingual versus oral tacrolimus.
  • To evaluate these parameters in the presence and absence of intestinal drug interactions.
  • To inform appropriate tacrolimus dosing strategies.

Main Methods:

  • A prospective, randomized, open-label, parallel-group pilot study.
  • Five adult patients with end-stage renal disease awaiting kidney transplantation participated.
  • Patients received both sublingual and oral tacrolimus, with and without interacting drugs (clotrimazole or nystatin).

Main Results:

  • Area under the concentration-time curve (AUC) varied between administration routes and interacting drug conditions.
  • Sublingual tacrolimus generally showed a higher average maximum concentration (Cmax) than oral administration.
  • Specific AUC ranges differed significantly between the clotrimazole and nystatin groups.

Conclusions:

  • Individualized evaluation of oral-to-sublingual tacrolimus dose conversion is recommended.
  • A 1:1 dose conversion may be appropriate when co-administering with clotrimazole.
  • A 2:1 oral-to-sublingual conversion might be necessary in the absence of interacting drugs.