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Prograf

Prograf
Prograf is used to prevent rejection of transplanted organs.

Brand: Tacrolimus

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: June 2024
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Package Price Per pill Save Order
Prograf 5 mg
20 pills - 5 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$249.95 $12.50 $18.03 Add to cart
10 pills - 5 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$133.99 $13.40 No Add to cart
Prograf 1 mg
90 pills - 1 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$326.95 $3.63 $176.60 Add to cart
60 pills - 1 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$223.25 $3.72 $112.45 Add to cart
30 pills - 1 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$121.91 $4.06 $45.94 Add to cart
20 pills - 1 mg $89.95 $4.50 $21.95 Add to cart
10 pills - 1 mg $55.95 $5.60 No Add to cart
Prograf 0.5 mg
90 pills - 0.5 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$309.95 $3.44 $139.96 Add to cart
60 pills - 0.5 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$217.91 $3.63 $82.03 Add to cart
30 pills - 0.5 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$117.91 $3.93 $32.06 Add to cart
20 pills - 0.5 mg $86.95 $4.35 $13.03 Add to cart
10 pills - 0.5 mg $49.99 $5.00 No Add to cart

Product description

DRUG TITLE

Prograf (Tacrolimus) 

Pharmacological action 

Immunosuppressant. At the molecular level, the effects and intracellular cumulation of tacrolimus are due to binding to cytosolic protein (FKBP 12). The FKBP 12-tacrolimus complex specifically and competitively inhibits calcineurin, providing calcium-dependent blocking of T-cell signaling pathways and preventing transcription of a discrete series of lymphokine genes.


Prograf (Tacrolimus) is a highly active immunosuppressant. In in vitro and in vivo experiments tacrolimus distinctly reduced the formation of cytotoxic lymphocytes that play a key role in the transplant rejection reaction. Tacrolimus inhibits the formation of lymphokines (interleukin-2, interleukin-3, γ-interferon), T-cell activation, interleukin-2 receptor expression, and T-helper-dependent B-cell proliferation.


Pharmacokinetics

Absorption of tacrolimus is variable (absorption variability in adult patients is 6-43%). Bioavailability of Prograf (Tacrolimus) averages 20-25%. Bioavailability, as well as the rate and degree of absorption of tacrolimus are decreased when concomitant administration with food. The nature of biliary excretion does not affect absorption of the drug. The distribution of tacrolimus in the human body after IV administration is biphasic. In the systemic bloodstream, tacrolimus is well bound to erythrocytes. The ratio of tacrolimus concentrations in whole blood to plasma is about 20:1. A significant proportion of plasma tacrolimus (> 98.8%) is bound to plasma proteins (serum albumin, α1-acid glycoprotein).


Prograf (Tacrolimus) is widely distributed in the body. Vd in the equilibrium state, taking into account plasma concentrations, is about 1300 l (in healthy people). The same figure, calculated from whole blood, is on average 47.6 l.


Prograf (Tacrolimus)  has a low clearance. In healthy people, the average total clearance calculated from whole blood concentrations is 2.25 L/h. In adult patients after liver, kidney, and heart transplantation, clearance values were 4.1 L/h, 6.7 L/h, and 3.9 L/h, respectively. Low hematocrit and hypoproteinemia contribute to an increase in the unbound fraction of tacrolimus, accelerating tacrolimus clearance. Corticosteroids used in transplantation may also increase the metabolic rate and accelerate tacrolimus clearance.


The T1/2 of tacrolimus is long and variable. In healthy subjects, the average T1/2 in whole blood is approximately 43 h.


Prograf (Tacrolimus)  is actively metabolized in the liver, mainly with the participation of CYP3A4 isoenzyme. Prograf (Tacrolimus) is metabolized extensively in the intestinal wall. Several metabolites of tacrolimus have been identified. Pharmacological activity of tacrolimus is almost independent of the metabolites.


After IV and oral administration of 14C-labeled tacrolimus, the bulk of the radioactivity was detected in the feces. Approximately 2% of radioactivity was detected in the urine. In the urine and feces about 1% was detected unchanged.

Contraindications for use

For systemic and external use: pregnancy; lactation period (breast-feeding); hypersensitivity to Prograf (Tacrolimus).


For external use: genetic defects of the epidermal barrier, such as Netherton's syndrome; lamellar ichthyosis; cutaneous manifestations of "graft versus host" reaction; generalized erythroderma (due to the risk of progressive increase in systemic absorption of tacrolimus); child and adolescent age below 16 years (depending on the dosage form used).


Administration during pregnancy and lactation

Administration during pregnancy and lactation (breast-feeding) is contraindicated.


Special precautions

During the initial post-transplantation period it is necessary to perform a regular monitoring of the following parameters: BP, ECG, neurological and visual status, fasting blood glucose, electrolyte concentration (especially potassium), liver and kidney function tests, haematological parameters, coagulogram, proteinemia level. In the presence of clinically significant changes, correction of immunosuppressive therapy is necessary.


During the use of tacrolimus, prescription of herbal preparations containing Hypericum perforatum should be avoided, as well as other herbal preparations that may cause a decrease (change) in tacrolimus blood concentration and have an adverse effect on the clinical effect of tacrolimus.


Blood concentrations of tacrolimus may be significantly altered in diarrhea; careful monitoring of tacrolimus blood concentrations is necessary in case of diarrhea.


Concomitant use of cyclosporine and tacrolimus should be avoided, and caution should be exercised when treating patients who have previously received cyclosporine with tacrolimus.


Pediatric use


When used topically, Prograf (Tacrolimus)  should be used in age-appropriate dosage forms for children.


Effect on driving and operating machinery


Prograf (Tacrolimus) may cause visual and neurological impairment, especially in combination with alcohol. During the treatment period, patients should refrain from driving motor transport and working with mechanisms.

Indications of active substances of the drug Prograf (Tacrolimus) 

For systemic use: prevention and treatment of liver and kidney allograft rejection in adult patients. Treatment of allograft rejection resistant to standard immunosuppressive therapy in adult patients.


For external use: treatment of atopic dermatitis (of medium severity and severe forms) in case of insufficient response of patients to traditional methods of treatment or presence of contraindications to such methods.


Dosage regimen

The dose and frequency of use are set individually, depending on the indication, clinical situation and the dosage form used.