Tacrolimus Extended-Release Capsule 1 mg (Tacrolimus)

Adult dose

1. Kidney transplantation Adults: The usual initial dose is 0.20 ∼ 0.30 mg/kg of body weight of tacrolimus orally once daily in the morning, followed by gradual dose reduction. The maintenance dose should be adjusted as appropriate according to symptoms, with reference to the “recommended minimum blood drug concentration.” 2. Liver transplantation Adults: The usual initial dose is 0.10 ∼ 0.20 mg/kg of body weight of tacrolimus orally once daily in the morning, followed by gradual dose reduction. The maintenance dose should be adjusted as appropriate according to symptoms, with reference to the “recommended minimum blood drug concentration.” It is recommended that this medicine be administered once daily in the morning. Take this medicine immediately after removing it from the blister. Instruct patients not to swallow the desiccant. Swallow the capsule with liquid (preferably water). This medicine is generally administered on an empty stomach, or 1 hour before a meal or 2 ∼ 3 hours after a meal, to achieve maximum absorption. If a morning dose is missed, take it as soon as possible on the same day. Do not take a double dose the next morning. When a transplant patient who has been taking a conventional tacrolimus formulation twice daily (Prograf capsules) is switched to this medicine, which is taken once daily, the total daily dose should be converted on a 1 : 1 (mg : mg) basis. This medicine should be administered in the morning. Measure the tacrolimus trough blood concentration for 2 weeks after the switch and adjust the dose as necessary to maintain similar systemic exposure. The dose may be reduced in patients with severe hepatic impairment to maintain the trough blood concentration within the recommended target range. No dose adjustment is necessary because the pharmacokinetics of tacrolimus are not affected by renal function. However, careful monitoring of renal function is recommended because of the potential nephrotoxicity of tacrolimus (including serial serum creatinine measurements, calculation of creatinine clearance, and monitoring of urine output). There is no evidence that different doses are required for men and women to achieve similar trough blood concentrations. There is no evidence that dose adjustment is necessary in older adults. Frequent measurement of trough blood concentrations is recommended during the first 2 weeks after transplantation, followed by regular monitoring during the maintenance period. Trough blood drug concentrations should be monitored when switching from a conventional tacrolimus formulation to this medicine, adjusting the dose, changing immunosuppressive therapy, or coadministering drugs that may affect whole-blood tacrolimus concentrations (see “Interactions”). The frequency of blood concentration measurements should be based on clinical need. Since tacrolimus has low clearance, it may take several days for changes in blood drug concentrations to appear after dose adjustment. In general, in clinical practice, early post-transplant trough blood concentrations were 5 ∼ 20 ng/mL in liver transplant patients and 10 ∼ 20 ng/mL in kidney and heart transplant patients. During the subsequent maintenance period, trough blood concentrations were 5 ∼ 15 ng/mL in liver, kidney, and heart transplant patients.

This medication is used to suppress the immune system to prevent the rejection of transplanted organs. However, it may lower immunity, increasing the risk of infections, and in rare cases, it may lead to cancer such as lymphoma. Patients using this medication should be under the care of an experienced physician, and regular blood tests and health condition checks are essential. It may affect kidney function, so patients with reduced kidney function should frequently check the drug concentration in the blood and adjust the dosage if necessary. Additionally, this medication can affect the nervous system, causing symptoms such as headaches, tremors, confusion, and seizures, so any abnormal symptoms should be reported immediately. Hyperkalemia and hyperglycemia can frequently occur; therefore, consistent monitoring of blood potassium and glucose levels is necessary. Caution should be exercised when using this medication with other nephrotoxic drugs, as it can put more burden on the kidneys. Avoid using potassium-sparing diuretics or certain antibiotics in combination with this medication, and it is best not to consume grapefruit juice. During pregnancy, it can affect the fetus, so consultation with a doctor is essential before use, and breastfeeding should be discontinued while on this medication. During treatment, live vaccinations should be avoided to reduce the risk of infections. It is recommended to take the medication with water on an empty stomach to enhance absorption. Special attention should be paid to the elderly or patients with impaired liver or kidney function, and regular monitoring of blood drug concentration and health status is necessary. This medication may affect driving or operating machinery, thus caution is required. It is crucial to notify healthcare providers immediately if any abnormal symptoms or discomfort occur during treatment.

Increased susceptibility to infections, potential for lymphoma, nephrotoxicity, increased serum creatinine, hyperkalemia, decreased urine output, hyperuricemia, progressive renal impairment, increased blood urea, proteinuria, tremors, 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, BK virus-associated nephropathy, JC virus-related PML, CMV infection, insulin-dependent post-transplant diabetes, pure red cell aplasia, myocardial disorders, reduced cardiac function, cardiac chamber enlargement, ventricular hypertrophy, heart failure, ventricular arrhythmias, supraventricular arrhythmias, myocardial infarction, angina, pericardial effusion, QT interval prolongation, Torsades de pointes, acute renal failure, nephrotic syndrome, thrombotic microangiopathy, pancytopenia, thrombocytopenic purpura, agranulocytosis, hemolytic anemia, intestinal obstruction, bacterial infections, viral infections, fungal infections, protozoal infections, fever, lymphadenopathy, generalized convulsions, altered consciousness, confusion, speech disturbances, hemiplegia, cerebral infarction, cerebral hemorrhage, aspiration pneumonia, worsening diabetes, hyperglycemia, pancreatitis, skin and mucous membrane syndrome, Stevens-Johnson syndrome, dyspnea, acute respiratory distress syndrome, decreased urine output, polyuria, urinary frequency, post-void residual, glucosuria, hypomagnesemia, acidosis, hypercholesterolemia, hyperphosphatemia, hypophosphatemia, hypertriglyceridemia, hyperchloremia, hypercalcemia, hypocalcemia, hyponatremia, hypokalemia, diabetes, elevated blood pressure, edema, tachycardia, palpitations, hypotension, bradycardia, ataxia, hallucinations, dysesthesia, anxiety, delirium, insomnia, paresthesia, eye twitching, limb rigidity, paralysis, drowsiness, altered consciousness, localized sensory loss, nonsensical speech, depression, agitation, sleep disturbances, despair, worry, confusion, euphoria, feelings of happiness, dreams, abnormal thoughts, loss of reflexes, emotional instability, excessive tension, lack of coordination, dystonic muscle spasms, neurological disorders, psychosis, inability to think, forgetfulness, encephalopathy, hemorrhagic stroke, muscle weakness, nerve compression, nervousness, neuralgia, flaccid paralysis, incomplete quadriplegia, postural hypotension, peripheral vascular disorders, arrhythmias, atrial fibrillation, bradycardia, cardiac tremors, cardiopulmonary failure, cardiovascular disorders, congestive heart failure, deep vein thrombosis, abnormalities in echocardiography, abnormalities in ECG QRS complex, abnormalities in ECG ST complex, cardiac dysfunction, increased heart rate, syncope, thrombosis, vasodilation, hematuria, renal failure, cystitis, dysuria, hydronephrosis, pyuria, nephrotoxic renal disease, acute renal failure, proteinuria, BK nephropathy, bladder spasms, oliguria, urgent urinary incontinence, frequent urination, urinary incontinence, urinary retention, vaginitis, acidosis, increased alkaline phosphatase, alkalosis, hyperbilirubinemia, non-healing, hyperlipidemia, hyperphosphatemia, hyperuricemia, hypocalcemia, hyponatremia, hypoproteinemia, AST increase, ALT increase, bicarbonate decrease, dehydration, hyperglycemia, hypoglycemia, increased lactate dehydrogenase, weight gain, edema, gout, hypercalcemia, hypercholesterolemia, peripheral edema, diabetes, Cushing's syndrome, coagulopathy, petechiae, hypochromic anemia, leukopenia, thrombocytopenia, erythrocytosis, decreased prothrombin, decreased plasma iron, increased hematocrit, abnormal hemoglobin, leukocytosis, arthralgia, generalized convulsions, limb spasms, myalgia, myasthenia, osteoporosis, joint disorders, painful muscle spasms, reduced mobility, asthma, bronchitis, increased cough, lung disease, pulmonary edema, pharyngitis, pneumonia, respiratory distress, rhinitis, sinusitis, voice changes, pneumothorax, dyspnea, hiccups, reduced lung function, pleural effusion, hair loss, herpes simplex, hypertrichosis, skin disorders, sweating, acne, fungal dermatitis, skin discoloration, skin ulcers, exfoliative dermatitis, shingles, benign cutaneous neoplasms, abdominal enlargement, abscess, chills, hernia, peritonitis, phototoxic reactions, allergic reactions, cellulitis, influenza-like illness, sepsis, abdominal pain, incidental injury, weakness, back pain, soft tissue infection, falls, altered sensation, temperature intolerance, ulceration, shingles, gastroesophageal reflux, reactivation of hepatitis B due to liver failure

This medication should be stored in an opaque container to protect it from light, and should be kept away from humid places. It is best stored at room temperature between 1°C and 30°C.

Appearance

A hard capsule with a white or almost white granule in the upper part and brownish-yellow in the lower part.

Package unit

50 capsules (10 capsules/PTP x 5)