Tacrolimus has become an important cornerstone in the prevention of rejection after kidney transplantation. However, its use has been complicated by several side effects, including chronic allograft nephropathy, diabetes mellitus, arterial hypertension, and neurotoxicity. Tacrolimus-induced neutropenia is a less recognized, but potentially harmful complication. Three patients with severe neutro...

■ Evidence summary A recent meta-analysis included 25 randomized controlled trials involving tacrolimus and pimecrolimus. This review included trials of tacrolimus and pimecrolimus in comparison with placebo, topical corticosteroids of varying strengths, and each other. They reported on both safety and efficacy. Fifteen vehiclecontrolled trials of pimecrolimus and tacrolimus were reviewed. Both...

Background: Pemphigus vulgaris is a rare autoimmune disorder characterized by cutaneous and mucosal blistering. Surprisingly, the management of oral lesions has been detailed only infrequently. As current topical therapies for oral lesions are of limited efficacy, application of calcineurin inhibitors is considered to be a potential option. The aim of this essay was to investigate the efficacy ...

Immunosuppressants require therapeutic drug monitoring because of their narrow therapeutic index and significant inter-individual variability in blood concentrations. This variability can be because of factors like drug-nutrient interactions, drug-disease interactions, renal-insufficiency, inflammation and infection, gender, age, polymorphism and liver mass. Drug monitoring is widely practiced ...

Tacrolimus was discovered in 1984 by the Fujisawa Pharmaceutical Company, based in Japan. It is structurally a macrolide, produced by Streptomyces tsukubaensis, a soil fungus originally found on Mount Tsukuba, Japan. The original research compound designation for tacrolimus was FK506, a name which is still frequently used in transplantation literature. Based on its immunomodulating properties, ...

OBJECTIVE To determine the efficacy and tolerability of topical pimecrolimus and tacrolimus compared with other treatments for atopic dermatitis. DESIGN Systematic review and meta-analysis. DATA SOURCES Electronic searches of the Cochrane Library, Medline, and Embase. STUDY SELECTION Randomised controlled trials of topical pimecrolimus or tacrolimus reporting efficacy outcomes or tolerabi...

Tacrolimus is a calcineurin inhibitor which works to induce immune suppression by preventing cytokine transcription and lymphocyte activation. Combining the immunomodulator interferon beta-1b (Betaseron) with the immunosuppressant tacrolimus (Prograf) may have the potential of additive therapeutic benefit through the complementary mechanisms of action of these two therapeutics. In this randomiz...

Specific antibody production is an important issue in crossover pharmacokinetic (PK) studies of protein-based formulations. We recently reported that intravenous co-administration of tacrolimus with multiple human interferon-alpha (h-IFN) administrations successfully suppressed the production of anti-h-IFN antibodies in rats. Since crossover PK studies are preferentially carried out using large...

The pharmacokinetics of orally administered tacrolimus were examined in six female lupus nephritis patients (mean age 43 years, range 24-55 years). Tacrolimus (3 mg) was administered after supper, and blood tacrolimus concentrations were measured just prior to dosing and 1, 2, 4, 6, 8, 12 and 24 h after administration. The maximum blood concentration (C(max)) was observed 4-8 h (mean: 6.7 h) af...

Calcineurin is a calcium- and calmodulin-dependent serine/threonine protein phosphatase, and the target of immunosuppressive agent tacrolimus (TAC). The dysfunction of calcineurin, or clinical applications of tacrolimus, have been reported to be associated with dyslipidemia. The underlying mechanisms of calcineurin and tacrolimus in lipid metabolism are largely unknown. Here, we showed that mut...