Prograf

Tacrolimus

Primary immunosuppression in liver & kidney allograft recipients & rejection resistant to conventional immunosuppressive agents. Recommended to be used concomitantly w/ adrenal corticosteroids. Because of the risk of anaphylaxis, Prograf inj should be reserved for patients unable to take Prograf cap only. 0.5- & 1-mg cap: Lupus nephritis.

Primary immunosuppression in liver & kidney transplantation Adult Liver Oral 0.1-0.2 mg/kg daily in 2 divided doses, start approx 6 hr after surgery. IV Initially 0.01-0.05 mg/kg as continuous 24-hr infusion. Kidney Oral 0.15-0.3 mg/kg daily in 2 divided doses, start w/in 24 hr of surgery. IV Initially 0.05-0.1 mg/kg as continuous 24-hr infusion. Paed Liver/kidney Oral Initially 0.3 mg/kg daily in 2 divided doses. IV Liver Initially 0.05 mg/kg daily as continuous 24-hr infusion, Kidney Initially 0.1 mg/kg daily as continuous 24-hr infusion. Liver & kidney allograft rejection resistant to conventional immunosuppressive regimens Begin w/ initial dose recommended for primary immunosuppression in that particular allograft. Do not continue IV therapy for >7 days. 0.5- & 1-mg cap Lupus nephritis Adult 3 mg once daily.

Should be taken on an empty stomach: Take at least 1 hr before or 2-3 hr after meals. Avoid grapefruit juice.

Hypersensitivity to tacrolimus, other macrolides, polyoxyethylene hydrogenated castor oil or structurally-related compd.

GI disorders; risk factors for QT prolongation including patients w/ personal or family history of QT prolongation, CHF, bradyarrhythmia, electrolyte abnormalities, diagnosed or suspected congenital long QT syndrome or acquired QT prolongation; lymphoproliferative disorders & malignancies; posterior reversible encephalopathy syndrome; pure red cell aphasia. Increased risk of opportunistic infections eg, BK virus-associated nephropathy, JC virus-associated progressive multifocal leukoencephalopathy, viral hepatitis. Risk factors for CAD development associated w/ SLE. Monitor BP, ECG, neurological & visual status, fasting blood glucose levels, electrolytes (particularly K), hepatic & renal function tests, haematology parameters, coagulation values & plasma protein determinations, EBV-PCR during initial post-transplant period. Concomitant use w/ strong CYP3A4 inhibitors/inducers, nephrotoxic or neurotoxic drugs; drugs prolonging QT interval, inducing electrolyte abnormalities or increasing tacrolimus exposure. Avoid use w/ St. John's wort-containing herbal prep, ciclosporin, high K or K-sparing diuretic therapy, live vaccines. Limit exposure to sunlight & UV light. Galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption. May affect ability to drive & use machines. Renal & severe hepatic impairment. May affect male fertility. Pregnancy. Not to be used during lactation. Not recommended in childn <18 yr. 0.5- & 1-mg cap: Hypersensitivity to peanut or soya. Inj: Hypersensitivity to polyoxyethylene hydrogenated castor oil. Avoid accidental inj arterially or perivasally. Ethanol content.

Tremor, headache; diarrhoea, nausea; renal impairment; hyperglycaemic conditions, DM, hyperkalaemia; HTN; insomnia. Ischaemic coronary artery disorders, tachycardia; anaemia, leukopenia, thrombocytopenia, leukocytosis, abnormal RBC analyses; nervous system disorders; blurred vision, photophobia, eye disorders; tinnitus; dyspnoea, parenchymal lung disorders, pleural effusion, pharyngitis, cough, nasal congestion & inflammation; GI disorders; renal failure, acute renal failure, oliguria, renal tubular necrosis, toxic nephropathy, urinary abnormalities, bladder & urethral symptoms; pruritus, rash, alopecia, acne, increased sweating; arthralgia, muscle cramps, pain in extremity, back pain; metabolism & nutrition disorders; primary graft dysfunction; haemorrhage, thrombembolic & ischaemic events, peripheral vascular disorders, vascular hypotensive disorders; asthenic conditions, febrile disorders, oedema, pain & discomfort, increased blood alkaline phosphatase, increased wt, disturbed body temp perception; hepatic enzymes & function abnormalities, cholestasis, jaundice, hepatocellular damage & hepatitis, cholangitis; psychiatric disorders.

Increased blood levels w/ ketoconazole, fluconazole, itraconazole, voriconazole, erythromycin, HIV & HCV PIs, letermovir, cobicistat, nilotinib, imatinib; clotrimazole, clarithromycin, josamycin, nifedipine, nicardipine, diltiazem, verapamil, amiodarone, danazol, ethinylestradiol, omeprazole, nefazodone, Schisandra sphenanthera-containing herbal remedies; grapefruit juice; NSAIDs, oral anticoagulants, oral antidiabetics; metoclopramide, cimetidine, Mg-Al-hydroxide. Inhibited metabolism w/ bromocriptine, cortisone, dapsone, ergotamine, gestodene, lidocaine, mephenytoin, miconazole, midazolam, nilvadipine, norethindrone, quinidine, tamoxifen, troleandomycin; lansoprazole, ciclosporin. Decreased blood levels w/ rifampicin, phenytoin, St. John's wort; phenobarb; carbamazepine, metamizole, INH. Increased or decreased blood levels w/ high-dose prednisolone or methylprednisolone. Prolonged t_½ of ciclosporin. Increased blood level of phenytoin. Reduced clearance of steroid-based contraceptives. Potentially decreased clearance & increased t_½ of pentobarbital, phenazone. Increased nephrotoxic or neurotoxic effects w/ aminoglycosides, gyrase inhibitors, vancomycin, co-trimoxazole, NSAIDs, ganciclovir, aciclovir. Enhanced nephrotoxicity w/ amphotericin B & ibuprofen. Risk of hyperkalaemia w/ high K intake or K-sparing diuretics (eg, amiloride, triamterene or spironolactone). Avoid use w/ live vaccines.

Immunosuppressants

L04AD02 - tacrolimus ; Belongs to the class of calcineurin inhibitors. Used as immunosuppressants.

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