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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Prograf

$39.23120 capsules/1 mg
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Tacrolimus volume of distribution

* 2.6 2.1 L/kg (pediatric liver transplant patients) * 1.07 0.20 L/kg (patients with renal impairment, 0.02 mg/kg/4 hr dose, IV) * 3.1 1.6 L/kg (Mild Hepatic Impairment, 0.02 mg/kg/4 hr dose, IV) * 3.7 4.7 L/kg (Mild Hepatic Impairment, 7.7 mg dose, PO) * 3.9 1.0 L/kg (Severe hepatic impairment, 0.02 mg/kg/4 hr dose, IV) * 3.1 3.4 L/kg (Severe hepatic impairment, 8 mg dose, PO)

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What is Tacrolimus

Tacrolimus (also FK-506 or Fujimycin) is an immunosuppressive drug whose main use is after organ transplant to reduce the activity of the patient’s immune system and so the risk of organ rejection. It is also used in a topical preparation in the treatment of severe atopic dermatitis, severe refractory uveitis after bone marrow transplants, and the skin condition vitiligo. It was discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. Tacrolimus is chemically known as a macrolide. It reduces peptidyl-prolyl isomerase activity by binding to the immunophilin FKBP-12 (FK506 binding protein) creating a new complex. This FKBP12-FK506 complex interacts with and inhibits calcineurin thus inhibiting both T-lymphocyte signal transduction and IL-2 transcription.

Tacrolimus mechanism of action

The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte activation by first binding to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This prevents the dephosphorylation and translocation of nuclear factor of activated T-cells (NF-AT), a nuclear component thought to initiate gene transcription for the formation of lymphokines. Tacrolimus also inhibits the transcription for genes which encode IL-3, IL-4, IL-5, GM-CSF, and TNF-, all of which are involved in the early stages of T-cell activation. Additionally, tacrolimus has been shown to inhibit the release of pre-formed mediators from skin mast cells and basophils, and to downregulate the expression of FceRI on Langerhans cells.

Dosage forms of Tacrolimus

Capsule (extended release)oral0.5 mg
Capsule (extended release)oral1 mg
Capsule (extended release)oral3 mg

Prescription Generics


International Brands



Anhydrous tacrolimus Tacrolimus anhydrous


Accord Healthcare Inc

CAS number






Affected organisms

Humans and other mammals

Indication of Tacrolimus

For use after allogenic organ transplant to reduce the activity of the patient’s immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart, small bowel, pancreas, lung, trachea, skin, cornea, and limb transplants. It has also been used in a topical preparation in the treatment of severe atopic dermatitis.

Toxicity of Tacrolimus

Side effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion. LDsub50/sub=134-194 mg/kg (rat).

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