Pharmacokinetics of tacrolimus following topical application of tacrolimus ointment in adult and pediatric patients with moderate to severe atopic dermatitis.
OBJECTIVE
To characterize the pharmacokinetics of tacrolimus after topical application in adult and pediatric patients with moderate to severe atopic dermatitis from all clinical trials in which tacrolimus blood levels were obtained.


METHODS
Tacrolimus ointment 0.03% or 0.1% was applied twice daily. In the adult and pediatric pharmacokinetic studies, serial blood samples were obtained after single and repeated topical application. During the 12 clinical efficacy trials of tacrolimus ointment, single blood samples were obtained at various times relative to tacrolimus ointment application.


RESULTS
In the pharmacokinetic studies, 89% to 95% of tacrolimus whole blood concentration samples were less than 1 ng/mL; mean maximum concentrations ranged from 0.2 to 1.6 ng/mL and mean area under the blood concentration-time curves (0-12 hours) ranged from 1.4 to 13.1 ng x hr/mL. Likewise, in the clinical efficacy trials, the majority (85%-99%) of tacrolimus concentration samples were less than 1 ng/mL.


CONCLUSIONS
Tacrolimus ointment is associated with minimal systemic absorption and no evidence of systemic accumulation in patients with moderate to severe atopic dermatitis and extensive disease.
Krueger
Gerald G
GG
University of Utah Health Sciences Center, Salt Lake City, UT 84132, USA. Krueger@derm.med.utah.edu
Eichenfield
Lawrence
L
Goodman
J John
JJ
Krafchik
Bernice R
BR
Carlin
Christopher S
CS
Pang
Mei-Lin
ML
Croy
Richard
R
Holum
Mary Elizabeth
ME
Jaracz
Eileen
E
Sawamoto
Taiji
T
Keirns
James
J
D000293:Adolescent; D000328:Adult; D000367:Age Factors; D000368:Aged; D002648:Child; D002675:Child, Preschool; D002986:Clinical Trials as Topic; D003876:Dermatitis, Atopic / Q000188:drug therapy*; D016903:Drug Monitoring; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009823:Ointment Bases; D009824:Ointments; D010599:Pharmacokinetics; D016559:Tacrolimus / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D009823:Ointment Bases; D009824:Ointments; D016559:Tacrolimus