In our body the immune system helps to fight against infection and reject a transplanted organ entering the body (such as liver, kidney, heart). Therefore Tacrolim 0.5mg is a immunosuppressive drug (also known as Fujimycin) which reduce the action of immune system in our body (immune system treat the new organ as invader), thereby Tacrolim 0.5mg combined with other, it will inhibit the immune system rejection of heart, liver or kidney transplant of our body.
Dr. Reddy’s Laboratories
Tacrolim 0.5mg is an immuno suppressive which is used with other medication to inhibit rejection of a Kidney, heart or liver transplant.
Tacrolim 0.5mg is indicated for reduce the inflammation associated with ulcerative colitis
Tacrolim 0.5mg is also used in treatment of eczema.
Tacrolim 0.5mg prevents the T-lymphocyte activation.
The drug binds to a protein (FKBP- 12) inside the cell and forms complex of Tacrolim 0.5mg- FKBP-12, calcium, calmodulin, and calcineurin.
The alteration of nuclear factor of activated T- cells (NF-AT), an nuclear component which initiate gene transcription for the formation of lymphokines (as interleukin-2, gamma interferon).
Finally, results prevention of T-lymphocyte activation.
Oral Slowly absorbed in the GI tract, total bioavailability 20 to 25%, highest blood plasma concentration reached after 1-3hrs.
With food: Slows down resorption and reduces bioavailability,
In the blood Tacrolim 0.5mg is mainly bound to erythrocytes, plasma 5%, plasma protein binding 98.8%.
Tacrolim 0.5mg is metabolized in liver, mainly via CYP3A and in the intestinal wall.
Tacrolim 0.5mg exerted through feces in form of its metabolites. Biological half-life 43 hrs. (healthy), liver transplation person 12hrs, for kidney transplation 16 hrs.
DOSAGE AND ADMINISTRATION
Organ Transplant in adult dose – Rejection prophylaxis :
Kidney transplant :
Initial dose: 0.03 to 0.05 mg/kg/day (IV infusion continuous) for 6 hours after transplantation.
High dose: 0.1mg/kg/day continuous IV infusion.
Tacrolim combination with azathioprine: initial dose 0.1mg/kg orally every 12hours. Initiate within 24 hours surgery.
In combination with mycophenolate: Initial dose 0.05mg/kg orally every 12hours started with 24hrs of surgery
Liver transplant :
Initial dose: 0.05 to 0.075mg/kg orally every 12hrs. Initiate not more than 6 hrs after surgery
For IV: initial dose 0.03 to 0.05 mg/kg/day as a continuous IV infusion.
Heart transplant :
Initial dose: 0.0375mg/kg/orally every 12 hrs. Initiate 6 hrs. after surgery.
For IV initial dose: 0.1mg/kg/day continuous IV infusion.
Graft versus host disease in adult :
Initial dose: 0.03mg/kg/day, initiate at least 24hrs before to stem cell infusion.
IV: initial dose 0.03mg/kg/day (continuous infusion)
To convert IV to oral then multiply total daily IV dose 4 times and administer in 2 divided oral dose /day, every 12hrs.
Pediatric dose for organ transplant – Rejection Reversal :
Liver transplant :
Initial dose: 0.075 to 0.1 mg/kg orally every 12 hrs.
IV, Initial dose: 0.03 to 0.05 mg/kg/day as continuous infusion
Graft versus host disease :
IV, initial dose 0.03 mg/kg/day (continuous IV), started at least 24 hrs. before to stem cell infusion, it used only if oral medication can be tolerated.
IF OVERDOSE OCCURS:
Tacrolim overdose may leads to passing out or breathing trouble. Call emergency medical or poison control for rapid action.
Severe side effects:
Liver and kidney problem
Increase in potassium, glucose level
Fungal infection: herpes zoster or polyoma
Carcinogenesis and mutagenesis: Non- Hodgkin’s lymphoma
Topical use common: burning or itching sensation; less common flu like symptoms, head pain.
CARE TO BE TAKEN :
Avoid Tacrolim 0.5mg, if you allergic to its own or hydrogenated castor oil, cyclosporine with the past 24 hrs. Discuss with doctor, if Tacrolim 0.5mg used for longer periods of time, it wil develop skin cancer, that weaken immune system and the possible risk.
Inform early to doctor about
Have kidney or liver disease;
Have cardiac disease, hypertension, hyperlipidemia or triglycerides (a type of fat in the blood);
a cardiac rate disorder or history of long QT syndrome;
taking heart rhythm medication; or
usage of other medications that can weaken your immune system
pregnancy, not known whether harm unborn baby
while Tacrolim 0.5mg therapy, avoid breast feed.