Main indication in lupus:

Tacrolimus (a calcineurin inhibitor) has no approval in systemic lupus, but some experts recognize its effectiveness in lupus with renal involvement, particularly in combination with Mycophenolate Mofétil.

Dosing:

Usually 0.10 to 0.30 mg/kg/day in 2 daily doses, one hour before or two hours after meals. There is an extended-release form that allows only one intake per day (0.5 mg, 1 mg, 2 mg or 5 mg capsules).

Main adverse reactions:

- Nephrotoxicity

- Neurotoxicity: tremors, headaches, paresthesia, agitation, anxiety, insomnia...

- Hyperglycemia or even diabetes

- Cardiac disorders, digestive disorders, arthralgia, skin rash, anemia, leukopenia or thrombocytopenia, elevation of transaminases...

Contraindications: known hypersensitivity to macrolides, live vaccines.

In case of pregnancy: the use of Tacrolimus is possible in case of pregnancy. There is no alternative; breastfeeding is not recommended.

Drug interaction:

Some products that may interact with tacrolimus: aluminum/magnesium antacid, cyclosporine, sirolimus, temsirolimus, ziprasidone, amiloride, spironolactone, cimetidine, danazol, nefazodone, ethinyl estradiol, methylprednisolone, St. John's wort, azole antifungals (such as itraconazole, voriconazole), HIV and HCV protease inhibitors (such as nelfinavir, ritonavir, boceprevir, telaprevir), rifamycins (such as rifampin, rifabutin), certain anti-seizure drugs (such as phenobarbital, phenytoin).

Monitoring:

- Tacrolimus may cause a condition that affects the heart rhythm (QT prolongation). An initial EKG is recommended.

- Blood count, creatinine, transaminases, alkaline phosphatases, gamma GT, uricemia, blood glucose regularly

- Blood dosage of the drug: Tacrolimus is prescribed in autoimmune diseases with a residual concentration target on whole blood of around 6 to 8 ng/ml.