Prograf普樂可復

Prograf

tacrolimus

Manufacturer:

Astellas

Distributor:

Firma Chun Cheong
/
DKSH
Concise Prescribing Info
Contents
Tacrolimus
Indications/Uses
Prophylaxis of transplant rejection in liver, kidney or heart allograft recipients. Treatment of allograft rejection resistant to treatment w/ other immunosuppressive medicinal products. Cap 0.5 & 1 mg: RA not adequately responsive to conventional therapies. Lupus nephritis (where the effect of steroids is insufficient or administration of steroids is difficult because of their adverse reactions).
Dosage/Direction for Use
Prophylaxis of liver transplant rejection Adult PO Initially 0.1-0.2 mg/kg/day in 2 divided doses approx 12 hr after surgery. IV Initially 0.01-0.05 mg/kg/day as a continuous 24-hr infusion. Childn PO Initially 0.3 mg/kg/day in 2 divided doses. IV Initially 0.05 mg/kg/day as a continuous 24-hr infusion. Prophylaxis of kidney transplant rejection Adult PO Initially 0.2-0.3 mg/kg/day in 2 divided doses approx 24 hr after surgery. IV Initially 0.05-0.1 mg/kg/day as a continuous 24-hr infusion. Childn PO Initially 0.3 mg/kg/day in 2 divided doses. IV 0.075-0.1 mg/kg/day as a continuous 24-hr infusion. Prophylaxis of heart transplant rejection Adult PO Initially 0.075 mg/kg/day in 2 divided doses 5 days after surgery. IV 0.01-0.02 mg/kg/day as a continuous 24-hr infusion. Childn w/o Ab induction Initially 0.03-0.05 mg/kg/day as a continuous 24-hr infusion, then PO 0.3 mg/kg/day 8-12 hr after discontinuing IV therapy. W/ Ab induction PO Initially 0.1-0.3 mg/kg/day in 2 divided doses. Treatment of allograft rejection in liver & kidney transplantation Increased Prograf doses, supplemental corticosteroid therapy & introduction of short courses of mono-/polyclonal Ab have been used to manage rejection episodes. Conversion to Prograf: Begin w/ initial oral dose recommended for primary immunosuppression. Treatment of allograft rejection in heart transplantation Increased Prograf doses, supplemental corticosteroid therapy & introduction of short courses of mono-/polyclonal Ab have been used to manage rejection episodes. Adult Conversion to Prograf: Initially 0.15 mg/kg/day in 2 divided doses. Childn Conversion to Prograf: Initially 0.2-0.3 mg/kg/day in 2 divided doses. Treatment of allograft rejection after lung transplantation PO Initially 0.1-0.15 mg/kg/day. Treatment of allograft rejection after pancreas transplantation PO Initially 0.2 mg/kg/day. Treatment of allograft rejection after intestinal transplantation PO Initially 0.3 mg/kg/day. RA PO Adult 3 mg once daily. Elderly Initially 1.5 mg once daily for 4 wk. May be increased to 3 mg once daily. Lupus nephritis (LN) PO Adult 3 mg once daily.
Administration
RA & LN: Should be taken with food: Take after dinner. Avoid grapefruit juice. Transplant: Should be taken on an empty stomach: Take at least 1 hr before or 2-3 hr after meals. Avoid grapefruit juice.
Contraindications
Hypersensitivity to tacrolimus, to any of the excipients, or other macrolides. Inj: Hypersensitivity to polyoxyethylene hydrogenated castor oil or structurally related compd.
Special Precautions
Monitor significant changes in BP, ECG, neurological & visual status, fasting blood glucose levels, electrolytes (particularly K), liver & renal function tests, haematology parameters, coagulation values & plasma protein determinations during initial post-transplant period. Reports of GI perforation. Perform extra monitoring of tacrolimus conc during episodes of diarrhoea. Reports of cardiomyopathy; monitor high-risk patients receiving substantial immunosuppression using echocardiography or ECG pre- & post-transplant (eg, initially at 3 mth & then 9-12 mth). May prolong QT interval & cause Torsades de Pointes. Reports of Epstein-Barr virus (EBV)-associated lymphoproliferative disorders. Perform EBV-VCA serology before starting treatment. Increase risk of opportunistic infections eg, BK virus-associated nephropathy & JC virus-associated progressive multifocal leukoencephalopathy. Risk of posterior reversible encephalopathy syndrome. Cases of pure red cell aplasia. Limit exposure to sunlight & UV light. Galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. Hypersensitivity to peanut or soya. Concomitant use w/ strong CYP3A4 inhibitors or inducers. Avoid concomitant use w/ St. John's wort or other herbal prep; combined administration w/ ciclosporin; high K intake or K-sparing diuretics; drugs known to have nephrotoxic or neurotoxic effects; live attenuated vaccines. May cause visual & neurological disturbances. Severe liver impairment. Pregnancy & lactation. RA: Use is limited only in patients w/ persisting symptoms despite appropriate therapies w/ NSAIDs or other antirheumatic drugs. Discontinue use if any abnormality is noted. Interstitial pneumonia may be aggravated in patients w/ RA-associated interstitial pneumonia. Use in surgery eg, artificial joint replacement. Childn. LN: Patients in acute phase w/ high disease activity. Renal disorder may be aggravated. Patients should also receive appropriate therapy for coronary diseases eg, hyperlipidemia or HTN. Long-term use. Childn.
Adverse Reactions
Transplantation: Hyperglycaemia, DM, hyperkalaemia, insomnia, tremor, headache, HTN, diarrhoea, nausea, renal impairment. RA: Abnormal renal function (increased BUN, increased creatinine), GI disorders (abdominal pain, diarrhea, nausea), impaired glucose tolerance (increased HbA1C & increased blood glucose). LN: Increased urinary β2-microglobulin, increased urinary NAG, nasopharyngitis, hyperuricemia, leukocytosis, increased creatinine, diarrhea, increased BP, hyperglycemia.
Drug Interactions
Increased tacrolimus blood levels w/ CYP3A4 inhibitors: antifungal agents eg, ketoconazole, fluconazole, itraconazole, voriconazole; erythromycin; HIV protease inhibitors eg, ritonavir, nelfinavir, saquinavir, HCV protease inhibitors eg, telaprevir, boceprevir; clotrimazole, clarithromycin, josamycin, nifedipine, nicardipine, diltiazem, verapamil, amiodarone, danazol, ethinylestradiol, omeprazole, nefazodone, herbal remedies containing extr of Schisandra sphenanthera; bromocriptine, cortisone, dapsone, ergotamine, gestodene, lidocaine, mephenytoin, miconazole, midazolam, nilvadipine, norethindrone, quinidine, tamoxifen, (triacetyl)oleandromycin; grapefruit juice; lansoprazole, ciclosporin. Increased tacrolimus blood levels w/ other active substances known to have high affinity for plasma proteins (eg, NSAIDs, oral anticoagulants, oral antidiabetics); prokinetic agents (eg, metoclopramide); cimetidine; Mg-Al hydroxide. Decreased tacrolimus blood levels w/ rifampicin, phenytoin, St. John's wort; phenobarb; maintenance doses of corticosteroids; carbamazepine, metamizole, INH. Increased or decreased tacrolimus blood levels w/ high dose prednisolone or methylprednisolone. May affect metabolism of CYP3A4 substrates. Prolonged t½ of ciclosporin. Synergistic/additive nephrotoxic effects w/ ciclosporin. Increased blood levels of phenytoin. Reduced clearance of steroid-based contraceptives. Increased toxic effects w/ medicinal products known to have nephrotoxic or neurotoxic effects (eg, aminoglycosides, gyrase inhibitors, vancomycin, cotrimoxazole, NSAIDs, ganciclovir or acyclovir). Enhanced nephrotoxicity w/ amphotericin B & ibuprofen. Increased risk of hyperkalaemia w/ high K intake or K-sparing diuretics.
ATC Classification
L04AD02 - tacrolimus ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.
Presentation/Packing
Form
Prograf cap 1 mg
Packing/Price
100's
Form
Prograf cap 5 mg
Packing/Price
50's
Form
Prograf conc for infusion 5 mg/mL
Packing/Price
10 × 1's
Form
Prograf cap 0.5 mg
Packing/Price
50's
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