Tacrobel Capsule 0.25 mg (Tacrolimus Hydrate)

Adult dose

Suppression of rejection in kidney transplantation Usually, the initial dose for adults is 0.10~0.15mg/kg of tacrolimus per dose, administered orally twice daily, followed by gradual dose reduction. The maintenance dose should be adjusted as appropriate according to symptoms, with reference to the “recommended whole blood trough concentrations.” Suppression of rejection in liver transplantation Usually, the initial dose for adults is 0.05~0.10mg/kg of tacrolimus per dose, administered orally twice daily, followed by gradual dose reduction. The maintenance dose should be adjusted as appropriate according to symptoms, with reference to the “recommended whole blood trough concentrations.” General considerations for kidney and liver transplantation The initial doses presented above are intended only as guidelines. Administration of this drug should be based primarily on clinical assessment of rejection and tolerability in each patient, together with measurement of blood concentrations (see “Recommended whole blood trough concentrations” below). If clinical symptoms of rejection are evident, a change in the immunosuppressive treatment regimen should be considered. Recommended whole blood trough concentrations in kidney and liver transplantation (whole blood trough level) Several immunoassay methods, including semi-automated microparticle enzyme immunoassay (MEIA), are available for monitoring tacrolimus whole blood concentrations (whole blood level) to optimize the dosage. Comparisons between blood concentrations reported in the literature and those measured in clinical practice must be made with detailed knowledge of the assay method used. In current clinical practice, whole blood concentrations are monitored using immunoassay methods. Tacrolimus whole blood trough concentrations must be monitored continuously. When this drug is administered orally, the tacrolimus whole blood trough concentration should be measured immediately before the next dose (approximately 12 hours after the previous dose). The frequency of blood concentration measurements should be based on clinical need. Because tacrolimus has a low clearance, changes in blood concentrations may take several days to appear after dosage adjustment. Monitoring should be performed approximately twice a week during the early post-transplant period and regularly during the maintenance period. Trough concentrations should be monitored when the dosage is adjusted, immunosuppressive therapy is changed, or the drug is coadministered with medicines that may affect tacrolimus whole blood concentrations (see “Interactions”). According to clinical trial analyses, successful outcomes were achieved in most patients when tacrolimus whole blood trough concentrations were maintained below 20ng/mL. The patient's clinical condition should be taken into account when interpreting blood concentrations. Recommended whole blood trough concentrations: In clinical practice, early post-transplant trough concentrations were 5~20ng/mL in liver transplant patients and 10~20ng/mL in kidney transplant patients. Thereafter, during the maintenance period, trough concentrations were 5-15ng/mL in both liver and kidney transplant patients. Bone marrow transplantation: Prevention of graft rejection and graft-versus-host disease following bone marrow transplantation Usually, 0.06mg/kg of tacrolimus per dose is administered orally twice daily starting 1 day before transplantation. During the early post-transplant period, 0.06mg/kg of tacrolimus per dose is administered orally twice daily, followed by gradual dose reduction. If treatment with this drug is initiated after the onset of graft-versus-host disease, the usual dose is 0.15mg/kg of tacrolimus per dose, administered orally twice daily. The dose should also be adjusted as appropriate according to symptoms. Because absorption of this product after oral administration is variable and differs among patients, blood concentrations should be measured according to the patient's condition, and the dose adjusted with reference to the trough level, to prevent adverse effects when blood concentrations are high and rejection or graft-versus-host disease when blood concentrations are low. Blood concentrations should be measured frequently, particularly immediately after transplantation or initiation of treatment. Also, use caution because adverse effects are more likely to recur when the trough concentration remains above 20ng/mL for a prolonged period. Chronic rheumatoid arthritis The usual adult dose is 3mg of tacrolimus administered orally once daily after the evening meal. Regular monitoring is required in patients who develop adverse reactions. The usual dose for elderly patients is 1.5mg administered orally once daily after the evening meal, and may be increased to 3mg depending on symptoms. Lupus nephritis The usual adult dose is 3mg of tacrolimus administered orally once daily after the evening meal. In clinical trials, when the effect was considered insufficient 12 weeks after treatment initiation and there were no safety concerns, this drug was administered at 4 mg/day for 4 weeks to confirm safety, and then increased to up to 5 mg/day. If adverse reactions occurred, the dose was appropriately reduced by 0.5 mg or 1 mg, taking the patient's condition into account. When an adequate effect on lupus nephritis was achieved, this drug was reduced to a dose that maintained the effect. Myasthenia gravis For adults, 3mg of tacrolimus is administered orally once daily after a meal.

Child dose

Suppression of rejection in kidney transplantation: Children are administered 0.15mg/kg per dose orally twice daily. Suppression of rejection in liver transplantation: Children are administered 0.15mg/kg per dose orally twice daily.

This drug suppresses the immune system, making it easier for infections to occur and increasing the possibility of malignant tumors such as lymphomas. Patients using this drug require thorough observation by an experienced physician and appropriate medical facilities. It may affect kidney function, so regular kidney function tests are necessary for those with renal impairment or potential kidney toxicity. Since potassium levels in the blood may increase, it should not be used with potassium-sparing diuretics, and blood potassium concentrations should be monitored frequently. Neurological side effects such as tremors, headaches, seizures, coma, and confusion may occur; if these symptoms develop, the physician should be consulted immediately. This drug can induce or worsen hypertension and diabetes; therefore, regular monitoring of blood pressure and glucose levels is essential. It may be harmful to the fetus during pregnancy, so women of childbearing age should take appropriate contraceptive measures, and the drug should be administered cautiously to pregnant women. This drug may interact with various medications, so patients on other drugs must inform their physician or pharmacist. There is an increased risk of infection while taking this drug, so any signs of infection should be reported immediately to medical personnel. While on this medication, regular blood tests and other necessary tests should be conducted to check for adverse reactions. Take this drug at the same time, regardless of meals, and consult a physician immediately if side effects occur. Extra caution is needed when administering this drug to children or the elderly, and dosage adjustments and monitoring of their condition are essential.

Increased susceptibility to infections, potential for lymphoma development, renal function impairment, increased serum creatinine, hyperkalemia, decreased urea excretion, hyperuricemia, progressive renal dysfunction, proteinuria, tremors, headache, changes in motor function, changes in mental status, changes in sensory function, seizures, coma, delirium, posterior reversible encephalopathy syndrome (PRES), headache, changes in mental status, seizures, visual impairment, hypertension, lymphoma, malignant tumors, BK virus-associated nephropathy, JC virus-related progressive multifocal leukoencephalopathy (PML), CMV infection, insulin-dependent post-transplant diabetes mellitus (PTDM), hyperglycemia, cardiac dysfunction, decreased heart function, cardiac chamber enlargement, ventricular wall hypertrophy, heart failure, ventricular arrhythmia, supraventricular arrhythmia, myocardial infarction, angina, pericardial effusion, QT prolongation, Torsades de pointes, acute renal failure, nephrotic syndrome, thrombotic microangiopathy, hemolytic uremic syndrome, thrombotic thrombocytopenic purpura, pancytopenia, thrombocytopenic purpura, pure red cell aplasia (PRCA), agranulocytosis, hemolytic anemia, intestinal obstruction, bacterial infections, viral infections, fungal infections, parasitic infections, fever, lymphadenopathy, generalized seizures, altered consciousness, confusion, speech disturbances, hemiplegia, cerebral infarction, cerebral hemorrhage, pneumonitis, worsening diabetes, pancreatitis, skin and mucous membrane syndrome (Stevens-Johnson syndrome), respiratory distress, acute respiratory distress syndrome, myasthenic crisis, elevated blood pressure, edema, tachycardia, palpitations, lowered blood pressure, bradycardia, ataxia, hallucinations, insomnia, paresthesia, eye twitching, hypertonia, paralysis, drowsiness, confusion of consciousness, localized sensory loss, delirium, depression, agitation, chest pain, abdominal bloating, gastrointestinal motility disturbance, loss of appetite, diarrhea, abdominal pain, gastric ulcer, duodenal ulcer, colitis, stomatitis, nausea, vomiting, melena, hematochezia, gastrointestinal perforation, elevated amylase, abnormal liver function tests (AST, ALT, ALP, LDH, γ-GTP increase), jaundice, anemia, increased or decreased platelet count, leukopenia, leukocytosis, lymphopenia, pruritus, hair loss, erythema, rash, tubular necrosis, hypertrophic cardiomyopathy, gynecomastia, vasodilation, decreased serum phosphate levels, pleural effusion, ascites, asthma, weight loss, flushing, generalized weakness, menorrhagia, myalgia, arthralgia, taste disturbances, aplastic anemia, cerebral infarction, toxic epidermal necrolysis (Lyell's syndrome), glaucoma, ketosis, nystagmus, mania, meningitis, hyperviscosity, thrombophlebitis, thrombosis, vasculitis, foreign body sensation in the throat, pain, eye pain, erythema, excessive sweating, thirst, temperature changes, optic nerve disease, febrile neutropenia, tremors, diarrhea, hypertension, nausea, headache, renal dysfunction, insomnia, sensory abnormalities, dizziness, dyspepsia, chest pain, hematuria, urinary tract infection, edema, frequent urination, arthralgia, increased cough, rash, pruritus, sleep disturbances, agitation, worry, confusion, depression, euphoria, dreams, abnormal thoughts, drowsiness, loss of reflexes, emotional instability, excessive tension, imbalance, hypertensive crises, neural disorders, psychosis, impaired cognition, amnesia, encephalopathy, hemorrhagic stroke, paresis of the limbs, nerve compression, nervousness, neuralgia, flaccid paralysis, incomplete limb paralysis, acquired disability, aphasia, visual impairment, amblyopia, tinnitus, cataract, photophobia, hearing loss, ear pain, otitis media, cholangitis, cholestasis jaundice, gastrointestinal bleeding, hepatitis, increased appetite, liver damage, oral moniliasis, dysphagia, gastritis, intestinal obstruction, abnormal liver function tests, rectal disorders, duodenitis, air in the gastrointestinal tract, gastroesophageal reflux, granulomatous hepatitis, esophagitis, pancreatic pseudocysts, chest pain, abnormal ECG, hemorrhage, hypotension, angina, severe vascular inflammatory disease, orthostatic hypotension, peripheral vascular disorders, arrhythmia, atrial fibrillation, slow pulse, cardiac tremors, cardiopulmonary failure, cardiac dysfunction, increased heart rate, syncope, thrombosis, vasodilation, hematuria, cystitis, dysuria, hydronephrosis, pyuria, toxic renal disease, acute renal failure, proteinuria, BK nephropathy, bladder spasms, oliguria, urgency urinary incontinence, urinary incontinence, urinary retention, vaginitis, acidosis, increased alkaline phosphatase, alkalosis, hyperbilirubinemia, non-healing conditions, hyperlipidemia, hyperphosphatemia, hyperuricemia, hypocalcemia, hyponatremia, hypoalbuminemia, elevated AST, elevated ALT, decreased bicarbonate, dehydration, hyperglycemia, hypoglycemia, increased lactate dehydrogenase, weight gain, edema, gout, hypercalcemia, hypercholesterolemia, peripheral edema, Cushing's syndrome, coagulopathy, petechial hemorrhage, hypochromic anemia, leukopenia, thrombocytopenia, erythrocytosis, decreased prothrombin, decreased plasma iron, increased hematocrit, abnormal hemoglobin, leukocytosis, joint disease, painful muscle cramps, decreased movement, asthma, bronchitis, lung disease, pulmonary edema, pharyngitis, pneumonia, respiratory distress, rhinitis, sinusitis, voice changes, pneumothorax, hiccups, reduced lung function, hair loss, herpes simplex, hirsutism, skin diseases, sweating, acne, fungal dermatitis, skin discoloration, skin ulcers, exfoliative dermatitis, shingles, benign skin tumors, abdominal distension, abscesses, chills, hernia, peritonitis, photosensitivity reactions, allergic reactions, cell inflammation, influenza-like symptoms, sepsis, incidental injuries, back pain, soft tissue infection, falls, abnormal sensations, inability to tolerate temperature, ulcers, heartburn, discomfort in the epigastrium, retinopathy, cardiac arrest, low back pain, hoarseness, cold.

This drug may be sensitive to air or moisture, so it must be stored in a tightly sealed container. It is best to keep it at room temperature, between 1°C and 30°C. This helps maintain the efficacy and safety of the drug.

Appearance

A hard capsule with a white upper part and a pale yellow lower part containing white or off-white powder.

Package unit

50 capsules (10 capsules/PTP × 5)