Tacrolimus Capsule 1 Milligram (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 appropriately according to symptoms, with reference to the “recommended minimum blood concentration.” 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 appropriately according to symptoms, with reference to the “recommended minimum blood concentration.” General considerations for kidney and liver transplantation The initial doses described above are intended only as guidelines. Administration of this medicine should be based primarily on assessment of each patient’s clinical status, including rejection and tolerability, together with measurement of blood concentrations (see “Recommended minimum blood concentration” below). If clinical signs of rejection are evident, a change in the immunosuppressive treatment regimen should be considered. Recommended minimum blood concentration 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 dose. 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 trough blood concentrations should be monitored continuously. When this medicine is administered orally, the tacrolimus trough blood concentration should be measured immediately before the next dose (approximately 12 hours after the previous dose). The frequency of blood concentration measurements depends on clinical need. Because tacrolimus has a low clearance, changes in blood concentrations may take several days to appear after dose adjustment. Monitoring should be performed approximately twice weekly during the early post-transplant period and regularly during the maintenance period. Trough blood concentrations should be monitored when adjusting the dose, changing immunosuppressive therapy, or administering concomitant medications that may affect tacrolimus whole blood concentrations (see “Interactions”). According to clinical trial analyses, successful outcomes were achieved in most patients when tacrolimus trough blood concentrations were maintained below 20ng/mL. The patient’s clinical condition should be taken into account when interpreting blood concentrations. Recommended minimum blood concentrations: In clinical practice, early post-transplant trough blood concentrations were 5~20ng/mL in liver transplant recipients and 10~20ng/mL in kidney transplant recipients. During the subsequent maintenance period, trough blood concentrations were 5-15ng/mL in both liver and kidney transplant recipients. Bone marrow transplantation: Prevention of tissue graft rejection and graft-versus-host disease following bone marrow transplantation Usually, starting 1 day before transplantation, administer 0.06mg/kg of tacrolimus per dose orally twice daily. During the early post-transplant period, administer 0.06mg/kg of tacrolimus per dose orally twice daily, followed by gradual dose reduction. If treatment with this medicine 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 appropriately according to symptoms. Chronic rheumatoid arthritis The usual adult dose is 3mg of tacrolimus orally once daily after the evening meal. Regular monitoring is required in patients who develop adverse reactions. The usual dose for older adults is 1.5mg 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 orally once daily after the evening meal. In clinical trials, when the effect was deemed insufficient at 12 weeks after treatment initiation and there were no safety concerns, this medicine was administered at 4 mg/day for 4 weeks to confirm safety before increasing the dose 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 medicine was reduced to the dose that maintained the effect. Myasthenia gravis For adults, administer 3mg of tacrolimus orally once daily after a meal.

Child dose

Prevention of rejection in kidney transplantation: For children, administer 0.15mg/kg per dose orally 2 times daily. Prevention of rejection in liver transplantation: For children, administer 0.15mg/kg per dose orally 2 times daily.

As this medication is an immunosuppressant, it may increase susceptibility to infections and has the potential risk of developing malignancies such as lymphoma; therefore, it should only be used by physicians experienced in immunosuppressive therapy. This medication may affect kidney function, so patients with kidney impairment should be monitored closely, and dose adjustments or discontinuation may be necessary. Blood potassium levels may increase, so potassium concentrations should be checked frequently, and it should not be combined with potassium-sparing diuretics. It can affect the nervous system, leading to headaches, tremors, seizures, and changes in mental state, so patients should consult medical personnel immediately if these symptoms occur. Patients receiving this medication have weakened immune systems, increasing the risk of various infections, so they should be closely monitored for infection symptoms. It is crucial to regularly measure blood concentrations while taking this medication to maintain appropriate dosing. Women who are pregnant or may become pregnant must consult a doctor before taking this medication, as it can affect the fetus and should be used with caution. Children and the elderly may have decreased kidney and liver function, so dosing should be observed and adjusted carefully. This medication may interact with other drugs; patients should inform healthcare professionals of any other medications they are taking, especially when used in combination with cyclosporine, potassium-sparing diuretics, certain antibiotics, and antifungal agents. Patients should avoid consuming grapefruit juice while taking this medication and should be cautious during vaccination. In cases of overdose, renal and neurological side effects may occur, so dosage should be strictly adhered to, and patients should not increase it without a doctor's guidance. This medication is taken in capsule form; it is best absorbed when taken with water on an empty stomach. Side effects may include hypertension, diabetes, renal impairment, infections, neurological abnormalities, and gastrointestinal issues, so regular check-ups are needed. Patients should consult their doctor immediately if they experience any unusual symptoms while taking this medication.

Increased susceptibility to infection, possibility of lymphoma occurrence, increased serum creatinine, hyperkalemia, decreased urea excretion, hyperuricemia, progressive kidney function impairment, proteinuria, tremor, headache, changes in motor function, changes in mental status, changes in sensory function, seizures, coma, delirium, posterior reversible encephalopathy syndrome (PRES), convulsions, visual disturbances, hypertension, lymphoproliferative disorders (LPD), BK virus-associated nephropathy, JC virus-related PML, CMV infection, transplant rejection, insulin-dependent post-transplant diabetes, hyperglycemia, myocardial impairment, decreased cardiac function, enlargement of cardiac chambers, ventricular wall hypertrophy, heart failure, ventricular arrhythmias, atrial arrhythmias, myocardial infarction, angina, pericardial effusion, QT interval prolongation, Torsades de pointes, acute renal failure, nephrotic syndrome, thrombotic microangiopathy, hemolytic uremic syndrome, thrombotic thrombocytopenic purpura, pancytopenia, thrombocytopenic purpura, pure red cell aplasia, agranulocytosis, hemolytic anemia, bowel obstruction, bacterial infection, viral infection, fungal infection, protozoal infection, systemic infection, localized infection, chest pain, abdominal distension, gastrointestinal motility disorders, loss of appetite, diarrhea, abdominal pain, gastric ulcer, duodenal ulcer, colitis, stomatitis, nausea, vomiting, melena, hematochezia, gastrointestinal perforation, elevated amylase, abnormal liver function, jaundice, anemia, increase or decrease in platelet count, leukopenia, leukocytosis, lymphocytopenia, pruritus, hair loss, erythema, rash, tubular necrosis, hypertrophic cardiomyopathy, gynecomastia, vasodilation, decreased serum phosphate concentration, pleural effusion, ascites, asthma, fever, weight loss, flushing, general malaise, menorrhagia, myalgia, arthralgia, taste disturbances, aplastic anemia, cerebral infarction, toxic epidermal necrolysis, glaucoma, ketosis, nystagmus, mania, meningitis, cholecystitis, thrombophlebitis, thrombosis, vasculitis, sensation of a foreign body in the throat, pain, ocular pain, erythema, hyperhidrosis, polydipsia, temperature fluctuations, optic neuropathy, febrile neutropenia, insomnia, sensory abnormalities, anxiety, delirium, paresthesia, eye twitching, limb rigidity, paralysis, drowsiness, rigidity, clouding of consciousness, local sensory loss, delirium, depression, agitation, ataxia, hallucinations, insomnia, inability to think, forgetfulness, dizziness, encephalopathy, hemorrhagic stroke, monoparesis, nerve compression, irritability, neuralgia, flaccid paralysis, incomplete paralysis of limbs, hyperlexia, aphasia, visual impairment, amblyopia, tinnitus, cataract, photophobia, hearing loss, ear pain, otitis media, cholangitis, cholestatic jaundice, dyspepsia, flatulence, gastrointestinal bleeding, elevated γ-GTP, hepatitis, increased appetite, liver damage, oral candidiasis, dysphagia, esophagitis, gastritis, bowel obstruction, abnormal liver function tests, rectal disorders, duodenitis, air in the gastrointestinal tract, gastroesophageal reflux, gastrointestinal disorders, granulomatous hepatitis, esophagitis, pancreatic pseudocyst, chest pain, abnormal ECG, bleeding, hypotension, tachycardia, angina, severe vascular venous inflammation, orthostatic hypotension, peripheral vascular disorders, arrhythmia, atrial fibrillation, bradycardia, cardiac tremors, cardiac arrest, heart failure, loss of cardiac function, increased heart rate, syncope, thrombosis, vasodilation, hematuria, renal failure, cystitis, dysuria, hydronephrosis, renal tubular necrosis, nocturia, pyuria, toxic renal disease, acute renal failure, proteinuria, BK nephropathy, bladder spasms, oliguria, urge incontinence, polyuria, urinary incontinence, urinary retention, vaginitis, acidosis, increased alkaline phosphatase, alkalosis, hyperbilirubinemia, non-healing wounds, hyperlipidemia, hyperphosphatemia, hyperuricemia, hypocalcemia, hyponatremia, hypoproteinemia, elevated AST, elevated ALT, decreased bicarbonate, dehydration, hyperglycemia, hypoglycemia, increased lactate dehydrogenase, weight gain, elevated BUN, edema, gout, hypercalcemia, hypercholesterolemia, hypophosphatemia, peripheral edema, diabetes mellitus, Cushing's syndrome, coagulopathy, petechial hemorrhage, hypopigmented anemia, leukopenia, thrombocytopenia, increased erythrocytes, decreased prothrombin, decreased plasma iron, increased hematocrit, abnormal hemoglobin, leukocytosis, arthralgia, generalized convulsions, limb convulsions, myalgia, myasthenia gravis, osteoporosis, joint disorders, painful muscle cramps, reduced movement, asthma, bronchitis, increased coughing, pulmonary disease, pulmonary edema, pharyngitis, pneumonia, respiratory distress, rhinitis, sinusitis, voice changes, pneumothorax, dyspnea, hiccups, decreased lung function, pleural effusion, hair loss, herpes simplex, hypertrichosis, skin disorders, sweating, acne, fungal dermatitis, skin discoloration, skin ulcers, exfoliative dermatitis, shingles, benign skin tumors, abdominal enlargement, abscess, chills, hernia, peritonitis, photosensitive reactions, allergic reactions, cellulitis, influenza-like syndrome, sepsis, abdominal pain, accidental injuries, weakness, back pain, soft tissue infection, falls, sensation abnormalities, fever, generalized edema, intolerable temperature, ulcer, heartburn, epigastric discomfort, retinopathy, cardiac arrest, low back pain, hoarseness, cold, cytomegalovirus infection, uterine leiomyomas, cardiac arrhythmia, cardiac arrest, dysphagia

This medication may be sensitive to air and moisture, so it should be stored in a tightly sealed container. Additionally, to maintain its effectiveness, it is best stored at room temperature between 1°C and 30°C.

Appearance

A white hard capsule containing white powder

Package unit

60 capsules/box (10 capsules/PTP packaging x 6 pieces), 120 capsules/box [(10 capsules/PTP packaging x 6 pieces) * 2]