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Miscellaneous Drugs during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Tacrolimus is a macrolide immunosuppressant, used to prevent solid organ rejection after transplantation (Scott et al., 2003). Tacrolimus decreases T-cell production through binding to an immunophilin, FK506 binding protein (FKBP), inhibiting calcineurin phosphatase. This inhibits downstream calcium-dependent events, such as interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, inhibiting T-cell production. Several small case series or case reports of the use of tacrolimus during pregnancies of transplant patients are published (Jain et al., 1993; Laifer et al., 1994; Yoshimura et al., 1996). No birth defects or adverse pregnancy outcomes were reported, except for slightly reduced birth weight and transient immunocompromise.
Urinary Tract Disease
Published in Vincenzo Berghella, Maternal-Fetal Evidence Based Guidelines, 2022
Pregnancy in KT are considered high risk and should be followed by an integrated multidisciplinary team including a transplant physician, nephrologist, diabetologist, and a maternal-fetal medicine specialist. Knowledge of what immunosuppressive agents can be used in pregnant KT patients, in order to avoid teratogenic medications. Azathioprine and steroids are the most often employed and best known drugs. Tacrolimus and cyclosporine are also frequently used in pregnancy. Mycophenolate mofetil is to be avoided as teratogenic, while only few studies have considered the use of m-Tor inhibitors, Rituximab, and Simulect in pregnancy, whose use is also discouraged (Table 17.9). Levels of calcineurin inhibitors (i.e cyclosporine, tacrolimus) should be checked monthly (consider twice monthly in the first and second trimester), to adjust doses when levels decrease [41, 42].
Tacrolimus
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Tacrolimus is a macrolide immunosuppressive drug obtained from the fermentation broth of a Japanese soil sample that contained the bacterium Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12 protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus is used orally after allogenic organ transplantation for immunosuppression to reduce the risk of organ rejection. It is also widely utilized topically for the treatment of atopic dermatitis, severe refractory uveitis after bone marrow transplantation, and vitiligo (1).
Systemic Immunosuppression in Cornea and Ocular Surface Disorders: A Ready Reckoner for Ophthalmologists
Published in Seminars in Ophthalmology, 2022
Tacrolimus is a T cell inhibitor, that acts by a mechanism similar to cyclosporine.66,67 Topical tacrolimus is available in concentrations of 0.005%, 0.03%, and 0.1% while oral tacrolimus is administered in a dose for 0.05−0.1 mg/kg/day (2–12 mg/day) in two divided doses. The whole blood level of tacrolimus should be maintained between 1 and 12 µg/L, to avoid toxicity. 68 There is no consensus on duration of treatment, and therapy can last from anywhere between 6 to 18 months.68–70 Side effects reported with use of oral tacrolimus include hypertension, renal toxicity, gastrointestinal intolerance, paresthesia, pancreatitis, and lymphopenia.68,70 Monitoring for tacrolimus toxicity is similar to that of cyclosporine, with the addition of initial weekly measurement of CBC, blood glucose, liver enzymes, bilirubin, electrolytes (calcium, magnesium, and phosphate), and a lipid profile, the frequency of which may be reduced to monthly after stabilization of the dose.4
Topical tacrolimus for the treatment of external eye inflammation in children
Published in Expert Review of Ophthalmology, 2022
Bernales Andrea, Berger Osvaldo, Hamada Samer
Tacrolimus was prescribed bilateral for 18 pediatric patients in the study period. Six patients were excluded (five due to loss of follow up, and one did not need to use tacrolimus), in total 12 patients (11 males and 1 female) were included. Clinical improvement was achieved in 11 patients (92%) and only in 1 patient with VKC who used tacrolimus for 12 months, there was no clinical improvement (Table 2). Total mean clinical score decreased from 4.5 to 0.6 (P = 0.0002) after treatment. Table 3 shows scores per individual sign. Mean onset of response was seen 3.8 weeks after treatment initiation. There was a significant reduction in the score for conjunctival hyperemia, papillary reaction, and corneal signs.
Efficacy and safety of tacrolimus in patients with rheumatoid arthritis – A systematic review and meta-analysis
Published in Modern Rheumatology, 2021
Yuko Kaneko, Yutaka Kawahito, Masayo Kojima, Takeo Nakayama, Shintaro Hirata, Mitsumasa Kishimoto, Hirahito Endo, Yohei Seto, Hiromu Ito, Keiichiro Nishida, Isao Matsushita, Toshihisa Kojima, Naoyuki Kamatani, Kiichiro Tsutani, Ataru Igarashi, Mieko Hasegawa, Nobuyuki Miyasaka, Hisashi Yamanaka
The efficacy and safety of tacrolimus were enhanced with increasing doses in all studies; however, the efficacy was less dose-dependent than safety. These findings were consistently observed in the efficacy and safety of 5mg/day tacrolimus. This could be ascribed to the relationship between the tacrolimus blood concentrations and the effects of the drug. While clinical studies on renal transplant have shown the close correlation between tacrolimus blood concentrations and adverse events, especially showing that a ≥ 10 ng/mL dose of tacrolimus is relevant to a higher incidence of adverse events [20], the median or mean concentrations of tacrolimus of 2–3 ng/mL could be effective in at least a part of patients with RA [14,21]. Unfortunately, little has been reported about blood tacrolimus concentrations in the studies identified in our search. In the trial of tacrolimus versus mizoribine by Kawai et al., a tacrolimus concentration of >10 ng/mL was found in approximately one-tenth of patients treated with 3 mg/day tacrolimus [16]; however, the associations of tacrolimus concentration with the efficacy of the drug remained unclear. The relationship between tacrolimus doses and concentrations were reported in a single-center cohort study in Japan, which showed mean tacrolimus concentrations of 3.0, 4.3, and 8.3 ng/mL for doses of 1, 2, and 3 mg/day, respectively [22].