{"id":4391,"date":"2025-03-31T18:12:06","date_gmt":"2025-03-31T18:12:06","guid":{"rendered":"https:\/\/kidneydiseaseclinic.net\/kdc\/tacrolimus-txt\/"},"modified":"2025-03-31T18:12:06","modified_gmt":"2025-03-31T18:12:06","slug":"tacrolimus-txt","status":"publish","type":"post","link":"https:\/\/kidneydiseaseclinic.net\/kdc\/tacrolimus-txt\/","title":{"rendered":"Tacrolimus.txt"},"content":{"rendered":"

CLINICAL USE <\/H3>
\nImmunosuppressive agent:Prophylaxis and treatment of acute rejection in liver, heart and kidney transplantationTreatment of moderate to severe atopic eczema

DOSE IN NORMAL RENAL FUNCTION <\/H3>Oral:Liver transplantation: 100\u2013200 mcg\/kg\/day in 2 divided dosesKidney transplantation: 150\u2013300 mcg\/kg\/ day in 2 divided dosesHeart transplantation: 75 mcg\/kg\/day in 2 divided dosesIV:Liver transplantation: 10\u201350 mcg\/kg as a continuous 24 hour infusion, starting 6 hours post surgeryKidney transplantation: 50\u2013100 mcg\/kg as a continuous 24 hour infusion, starting within 24 hours of surgeryHeart transplantation:
  • 10 to 20 &nbsp &nbsp : mcg\/kg as a continuous 24 hour infusion

    PHARMACOKINETICS <\/H3>
  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :822<\/li>\n
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>98<\/li>\n
  • %Excreted unchanged in urine &nbsp &nbsp : <1<\/li>\n

  • Volume of distribution (L\/kg) &nbsp &nbsp &nbsp :1300 litres<\/li>\n

  • half-life \u2013 normal\/ESRD (hrs)&nbsp &nbsp &nbsp :12\u201316\/Probably unchanged

    DOSE IN RENAL IMPAIRMENT <\/H3>

    GFR (mL\/MIN)<\/H4>
  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES <\/H3>
  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function<\/p>\n
  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in normal renal function
  • HDF\/high flux &nbsp :Unknown dialysability. Dose as in normal renal function
  • CAV\/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS <\/H3>Potentially hazardous interactions with other drugs\n
  • Ciclosporin: may increase the half-life of ciclosporin and exacerbate any toxic effects. The two should not be prescribed concomitantly. Care should be taken when converting from ciclosporin to tacrolimusTacrolimus levels increased by: atazanavir, basiliximab, bromocriptine, caspofungin, chloramphenicol, cimetidine, cortisone, danazol, dapsone, diltiazem, ergotamine, ethinyloestradiol, gestodene, grapefruit juice, imidazole and triazole antifungals, lidocaine, felodipine, lansoprazole, possibly levofloxacin, macrolides, midazolam, nelfinavir, nicardipine, nifedipine, omeprazole, pantoprazole, quinidine, quinupristin\/dalfopristin, ritonavir, saquinavir, tamoxifen, telithromycin, theophylline, verapamil and voriconazoleTacrolimus levels decreased by: carbamazepine, caspofungin, isoniazid, phenobarbital, phenytoin (phenytoin levels possibly increased), rifampicin and St John\u2019s wortIncreased nephrotoxicity with: aciclovir, aminoglycosides, amphotericin, co-trimoxazole, ganciclovir, NSAIDs and vancomycin
    Increased risk of hyperkalaemia with: potassium-sparing-diuretics and potassium salts\n
  • Clotrimazole: more than doubles the bioavailability of tacrolimus (US-based researchers report that concomitant clotrimazole substantially increases the relative oral bioavailability of tacrolimus in renal transplant recipients.

    ADMINISTRATION <\/H3>

    Reconstition<\/H4>\u2013

    Route <\/H4>IV, oral, topical

    Rate of Administration <\/H4>Continuous infusion over 24 hours

    Comments<\/H4>Dilute in glucose 5% or sodium chloride 0.9% to a concentration of 4\u2013100 micrograms\/mL, i.e. 5 mg in 50\u20131000 mL
    Incompatible with PVC.
    Add to either glucose 5% in polyethylene or glass containers or to sodium chloride 0.9% in polyethylene containersContains polyethoxylated castor oil which has been associated with anaphylaxis

    OTHER INFORMATION <\/H4>When converting from oral to IV, give one fifth of the total daily dose over 24 hours and monitor levels
    Also available as a 0.03% and 0.1% ointment for eczema and anal Crohn\u2019s diseaseApproximate whole blood ranges: Initially: liver: 5\u201310 ng\/mL, renal: \u20148\u201315 ng\/mL . Maintenance: 5\u201315 ng\/mL \u2014.
    \n","protected":false},"excerpt":{"rendered":"

    CLINICAL USE Immunosuppressive agent:Prophylaxis and treatment of acute rejection in<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"","ping_status":"","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[1],"tags":[7],"class_list":["post-4391","post","type-post","status-publish","format-standard","hentry","category-blog","tag-post-by-auto-php"],"_links":{"self":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/4391","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/comments?post=4391"}],"version-history":[{"count":0,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/posts\/4391\/revisions"}],"wp:attachment":[{"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/media?parent=4391"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/categories?post=4391"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/kidneydiseaseclinic.net\/kdc\/wp-json\/wp\/v2\/tags?post=4391"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}