Limast

Tacrolimus

Prophylaxis of transplant rejection in adult kidney, liver or heart allograft recipients. Treatment of allograft rejection resistant to treatment w/ other immunosuppressants in adults.

Adult Liver transplant rejection prophylaxis Initially 0.1-0.2 mg/kg/day in 2 divided doses approx 12 hr after completion of surgery. Kidney transplant rejection prophylaxis Initially 0.2-0.3 mg/kg/day in 2 divided doses w/in 24 hr after completion of surgery. Heart transplant rejection prophylaxis Following Ab induction, commence at 0.075 mg/kg/day in 2 divided doses w/in 5 days after completion of surgery as soon as patient's clinical condition is stabilized. Alternatively, initially 2-4 mg/day in combination w/ mycophenolate mofetil/sirolimus & corticosteroids w/in 12 hr post-transplantation, reserved for patients w/o organ dysfunction. Lung-transplanted patients Initially 0.1-0.15 mg/kg/day. Pancreas-transplanted patient Initially 0.2 mg/kg/day. Intestinal transplantation Initially 0.3 mg/kg/day. Childn Liver, kidney transplant rejection prophylaxis Initially 0.3 mg/kg/day in 2 divided doses. Heart transplant rejection prophylaxis W/o Ab induction: Convert to oral therapy as soon as clinically practicable & 1st dose should be 0.3 mg/kg/day starting 8-12 hr after discontinuing IV therapy. Following Ab induction, start at 0.1-0.3 mg/kg/day in 2 divided doses.

Should be taken on an empty stomach: Should be taken on an empty stomach or at least 1 hr before or 2-3 hr after meal. Cap to be taken immediately following removal from the blister. Swallow whole w/ water. Avoid grapefruit juice.

Hypersensitivity to tacrolimus or other macrolides.

Inadvertent, unintentional or unsupervised switching of immediate- or PR formulations of tacrolimus is unsafe. Maintain patients on a single formulation of tacrolimus w/ the corresponding daily dosing regimen. Monitor the following parameters during the initial post-transplant period on a routine basis: BP, ECG, neurological & visual status, fasting blood glucose levels, electrolytes (particularly K), liver & renal function tests, haematology parameters, coagulation values & plasma protein determinations. Concomitant use w/ strong CYP3A4 inhibitors/inducers; St. John's wort-containing herbal prep; ciclosporin (avoid combined administration & in patients previously receiving ciclosporin); high K intake or K-sparing diuretic; nephrotoxic or neurotoxic drugs; live attenuated vaccines. Significant change in blood levels during diarrhoea episodes. Increased risk of cardiac disorders in pre-existing heart disease, corticosteroid usage, HTN, renal or hepatic dysfunction, infections, fluid overload & oedema. May prolong QT interval & cause Torsades de pointes. Combination of immunosuppressives eg, antilymphocytic Abs (basiliximab, daclizumab) given concomitantly increases risk of EBV-associated lymphoproliferative disorders. Limit exposure to sunlight & UV light. Increased risk for opportunistic infections eg, BK virus-associated nephropathy & JC virus-associated progressive multifocal leukoencephalopathy. Perform radiological procedure (eg, MRI) if patients present w/ symptoms indicating posterior reversible encephalopathy syndrome eg, headache, altered mental status, seizures, & visual disturbances. Eye disorders, sometimes progressing to vision loss. Adequately control BP & seizure, & discontinue immediately if posterior reversible encephalopathy syndrome is diagnosed. Pure red cell aplasia. Severe liver impairment. Galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. May affect ability to drive & use machines. Pregnancy. Not used during lactation.

Hyperglycaemic conditions, DM, hyperkalaemia; insomnia; tremor, headache; HTN; diarrhoea, nausea; renal impairment; abnormal LFTs. Anaemia, leukopenia, thrombocytopenia, leukocytosis, abnormal RBC analyses; hypomagnesaemia, hypophosphataemia, hypokalaemia, hypocalcaemia, hyponatraemia, fluid overload, hyperuricaemia, appetite decreased, metabolic acidoses, hyperlipidaemia, hypercholesterolaemia, hypertriglyceridaemia, other electrolyte abnormalities; anxiety symptoms, confusion & disorientation, depression, depressed mood, mood disorders & disturbances, nightmare, hallucination, mental disorders; seizures, disturbances in consciousness, paraesthesias & dysaesthesias, peripheral neuropathies, dizziness, writing impaired, nervous system disorders; vision blurred, photophobia, eye disorders; tinnitus; ischaemic coronary artery disorders, tachycardia; haemorrhage, thrombembolic & ischaemic events, peripheral vascular disorders, vascular hypotensive disorders; dyspnoea, parenchymal lung disorders, pleural effusion, pharyngitis, cough, nasal congestion & inflammations; GI inflammatory conditions, GI ulceration & perforation, GI haemorrhages, stomatitis & ulceration, ascites, vomiting, GI & abdominal pains, dyspeptic signs & symptoms, constipation, flatulence, bloating & distension, loose stools, GI signs & symptoms; cholestasis & jaundice, hepatocellular damage & hepatitis, cholangitis; pruritus, rash, alopecias, acne, increased sweating; arthralgia, muscle spasms, pain in extremity, back pain; acute renal failure, oliguria, renal tubular necrosis, toxic nephropathy, urinary abnormalities, bladder & urethral symptoms; asthenic conditions, febrile disorders, oedema, pain & discomfort, disturbed body temp perception; increased blood alkaline phosphatase, increased wt; primary graft dysfunction. Allergic & anaphylactoid reactions.

May affect metabolism & possibly increase or decrease tacrolimus blood levels w/ medicinal products or herbal remedies known to inhibit or induce CYP3A4. Increase tacrolimus blood levels w/ antifungals (eg ketoconazole, fluconazole, itraconazole voriconazole, & isavuconazole), erythromycin, HIV PIs (eg, telaprevir, boceprevir, & ombitasvir & paritaprevir w/ ritonavir combination, when used w/ & w/o dasabuvir), letermovir, nilotinib & imatinib; clotrimazole, clarithromycin, josamycin, nifedipine, nicardipine, diltiazem, verapamil, amiodarone, danazol, ethinylestradiol, omeprazole, nefazodone & Chinese herbal remedies containing Schisandra sphenanthera extr; grapefruit juice. Potentially inhibit metabolism w/ bromocriptine, cortisone, dapsone, ergotamine, gestodene, lidocaine, mephenytoin, miconazole, midazolam, nilvadipine, norethisterone, quinidine, tamoxifen, troleandomycin. Potentially inhibit CYP3A4-mediated metabolism w/ lansoprazole & ciclosporin. Possible interaction w/ products known to have high affinity for plasma proteins (eg, NSAIDs, oral anticoagulations or antidiabetics). May increase systemic exposure w/ metoclopramide, cimetidine & Mg-Al-hydroxide.

Immunosuppressants

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

Rx