Tacrolimus is a Medicine belongs to macrolide immunosuppressant group whose information about Brand can be referenced from   Book : Martindale    Page : 2009   Edition : 37,

  ►   Brandname : Prograf, Protopic, Mustopic, PanGraf, Tacroz, Advagraf

  ►  Strength : Capsule with 0.5  mg, Capsule with 1  mg, Capsule with 5  mg, Injection with 5  mg/ml, Ointment with 0.03  %, Ointment with 0.1  %,

Reference of this Medicine for its Strength can be taken from   Book : Basic & Clinical pharmacology    Page : 999   Edition : 12,
A Route of administration in pharmacology and toxicology is the path by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration.

  ►  Route of administration : Oral, IV, Topical,
Reference :-   Book : Martindale    Page : 2007   Edition : 37,

Dosing of Medicine differ in Adult & Pediatrics ↓


Adult Dose

S.No Ailment   Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency   Additional Info
1 Liver transplantation Oral 100 200 micrograms/kg Capsule Dose: Starting about 12 hours after completion of surgery.
2 Kidney transplantation Oral 200 300 micrograms/kg Capsule Dose: Starting within 24 hours of completion of surgery.
3 Heart transplantation Oral 75 micrograms/kg Tablet Dose: After anti-body induction, and within 5 days of completion of surgery, and when the patient is stable.
4 Liver transplantation IV infusion 10 50 micrograms/kg Injection
5 Kidney transplantation IV infusion 50 100 micrograms/kg Injection
6 Heart transplantation IV infusion 10 20 micrograms/kg Injection
7 Atopic eczema Topical 0.03 0.1 % Ointment b.d.

Ref :-  Book : Martindale    Page : 2007   Edition : 37,




Pediatric Dose

S.No Ailment   Age Min   Age Max   Weight ( Kg ) Route   Dose Min   Dose Max   Unit   Dosage Form   Frequency  Additional Info  
1 Liver transplantation Oral 300 micrograms/kg Capsule
2 Kidney transplantation Oral 300 micrograms/kg Capsule
3 Heart transplantation Oral 100 300 micrograms/kg Capsule
4 Liver transplantation IV infusion 50 micrograms/kg Injection
5 Kidney transplantation IV infusion 75 100 micrograms/kg Injection
6 Heart transplantation IV infusion 30 50 micrograms/kg Injection
7 Atopic eczema 2 Year 16 Year Topical 0.03 % Ointment b.d.
8 Atopic eczema 16Year Topical 0.1 % Ointment

Ref :- Book : Martindale    Page : 2008   Edition : 37,
►  Organ Affected Nephrotoxicity – (Altered intraglomerular hemodynamics)  

Precaution :- If a Patient is using 'Tacrolimus' drug in  Generalized, Tonic-Clonic Seizures  disease, then Please Not to be given .

►  Side Effect : tremor, headache, paraesthesia, nausea, diarrhoea, hypertension, insomnia, Renal dysfunction, hyperkalaemia, Hyperglycaemia, diabetes mellitus, hyperlipidaemia, hypercholesterolaemia, hypertriglyceridaemia, anaemia, leucopenia, thrombocytopenia, gastrointestinal perforation, gastrointestinal ulceration, gastrointestinal haemorrhage, dyspnoea, parenchymal lung disorders, pleural effusion, alopecia, oedema, ascites, prolong QT interval , Cardiomyopathies, coma, Paralysis, CNS hemorrhage, Carcinogenicity,
Ref :-   Book : Martindale    Page : 2003   Edition : 37,

►  Drug Interaction : Drug interaction of Tacrolimus is with , Azole Antifungal, Calcium Channel Blockers , , Hiv Protease Inhibitors, , Macrolide antibacterials, , , Alcohol,  Bromocriptine , Cimetidine , Danazol, Metoclopramide , Carbamazapine , Nevirapine, Phenobarbital , Phenytoin , Rifampicin , Sirolimus,
Ref :-   Book : Martindale    Page : 2005   Edition : 37,


  ►    Mechanism of Drug Drug Interaction :  Increased nephrotoxicity may result if tacrolimus is given with other potentially nephrotoxic drugs: use with ciclosporin should be avoided for this reason. Similarly, concurrent use with neurotoxic drugs should be avoided. High potassium intake or potassium-sparing diuretics should also be avoided in patients receiving tacrolimus. Tacrolimus is extensively bound to plasma proteins and so has the potential to interact with other drugs that are highly protein bound. Tacrolimus is metabolised by the cytochrome P450 isoenzyme CYP3A4, and drugs that inhibit this enzyme system, such as azole antifungals, bromocriptine, calcium-channel blockers, cimetidine, some corticosteroids, ciclosporin, danazol, HIV-protease inhibitors, the NNRTI delavirdine, macrolide antibacterials, and metoclopramide, may produce increased blood concentrations of tacrolimus. The metabolism of tacrolimus may also be inhibited by grapefruit juice and they should not be taken together. Equally, inducers of this enzyme system (such as carbamazepine, nevirapine, phenobarbital, phenytoin, rifampicin, and St John’s wort) may reduce blood concentrations of tacrolimus. Sirolimus can also decrease blood concentrations of tacrolimus. Corticosteroids may increase or decrease tacrolimus concentrations. Nevirapine and the NNRTI delavirdine may also affect tacrolimus concentrations. Facial flushing or skin irritation may occur if alcohol is consumed by patients using topical tacrolimus.,
Ref :-   Book : Martindale    Page : 2005   Edition : 37,


►  Absolute Contraindication : Immunocompromised patient or those with conditions that might increase systemic absorption of tacrolimus   patients hypersensitive to macrolides   live vaccines   Tacrolimus may affect visual or neurological function   and patients so affected should not drive or operate dangerous machinery.  

►  Contraindication : renal impairment, hepatic impairment,
Ref :-   Book : Martindale    Page : 2004   Edition : 37,
  ►  Mechanism of Action :   Tacrolimus is a potent macrolide (macrolactam) immunosuppressant derived from Streptomyces tsukubaensis. Tacrolimus binds to an intracellular protein, FKBP-12, and then forms a complex with calcium, calmodulin, and calcineurin, which inhibits the activity of calcineurin. This interferes with the production of lymphokines such as interleukin-2 and inhibits T-lymphocyte activation, resulting in immunosuppression. ,
Ref :-   Book : Martindale    Page : 2007   Edition : 37,

Pathway of Dietry Product


​   ► Act.Comp / Nutrient / Food / Herb as follows :- NA


Dietry Substance Interactions


​   ► This Medicine interact with :- ST JOHNS WORT with Dietary Substance is Drug Inhibitor,

  ►  Reference :-
  • Driver, S. (2009). Stockleys Herbal Medicines Interactions. Royal pharmaceutical Society of Great Britain: Pharmaceutical press.

  •   ►  URL -- https://www.stonybrookmedicine.edu/sites/default/files/herbal_medicines_interactions-1.pdf,


    ContraIndication Dietry Substance


    ​   ► This Medicine contraindicate with :- NARINGENIN with caus interaction woth immunosuppresent ,

      ►  Reference :-
  • Eldelberg, D. The New Age of nutritional and herbal remedies. New Zealand

  •   ►  URL -- https://books.google.co.in/books?id=WZhj8EO9N3sC&pg=PA49&lpg=PA49&dq=The+New+Age+of+nutritional+and+herbal+remedies.++book&source=bl&ots=UVld-vNZL0&sig=5KwkKUUvW45p0TkfVUCtMZxnbow&hl=en&sa=X&ved=0ahUKEwiajLCNocrOAhVMto8KHfD2D-4Q6AEIMDAE#v=onepage&q=The%20,

    ►   Route of Elimination :   Biliary, Hepatic (Metabolism),
    Ref :-   Book : Martindale    Page : 2006   Edition : 37,


    ►    Plasma Half-life :   Min value :-   NA    Max value :-   NA


    ►    Peak Plasma Concentration :   Min value :-   NA    Max value :-   NA