Pharmacokinetics of Sublingual Versus Oral Tacrolimus in Patients Awaiting Kidney Transplantation
Status:
Completed
Trial end date:
2009-12-01
Target enrollment:
Participant gender:
Summary
Tacrolimus (Prograf) belongs to a class of medications known as the calcineurin inhibitors.
It is a maintenance drug that is used to prevent rejection in kidney, liver, and heart
transplant recipients. Calcineurin inhibitors display high pharmacokinetic (the body's
effects on a drug) variability and necessitate use of blood tests to ensure that adequate
drug levels are present to maintain effectiveness and safety. Early after transplant or at
times when tacrolimus cannot be taken by mouth, alternative routes of administration are
sought. Although an intravenous (through the vein) product is available, it can be toxic to
the kidneys and has been associated with allergic reactions. Drug delivery via the oral
mucosa is an alternative method of systemic drug administration which offers an alternative
when oral administration is impractical (gastrointestinal dysmotility, reduced drug
absorption, intestinal failure, difficulty in swallowing, or in those with nausea or
vomiting). Administration of tacrolimus by the sublingual route may allow for direct entry
into the systemic circulation and bypasses problems associated with drug absorption and
breakdown that take place in the small intestine.