Rapalobel 2 mg (Sirolimus) Tablets

Adult dose

This medicine is administered orally once daily. To minimize variability in exposure to this medicine, it should be taken consistently either with food or on an empty stomach. Do not crush, chew, or cut this medicine. General dosage for kidney transplant patients The initial dose of this medicine should be administered as soon as possible after transplantation. It is recommended that this medicine be administered 4 hours after administration of cyclosporine oral solution and/or cyclosporine capsules. Once the maintenance dose of this medicine has been adjusted, maintain that dose for at least 7~14 days before readjusting the dose based on therapeutic drug monitoring. For most patients, the following formula may be used to adjust the dose: New dose of this medicine = Current dose X (Target blood concentration / Current blood concentration) If a substantial increase in the trough blood concentration of this medicine is desired, a loading dose should also be considered in addition to the new maintenance dose: Loading dose of this medicine = 3 X (New maintenance dose - Current maintenance dose) The maximum daily dose of this medicine should not exceed 40mg. If administration of the loading dose would cause the scheduled daily dose to exceed 40mg, the loading dose should be administered over 2 days. The trough concentration of this medicine should be monitored at least 3-4 days after administration of the loading dose. Clinical trial results in patients at low or moderate immunologic risk demonstrated that taking 2mg of this medicine is clinically equivalent to administering 2mg of sirolimus oral solution; therefore, the oral solution and tablets may be substituted for one another. However, it is unknown whether the oral solution and tablets are clinically equivalent when higher doses exceeding 2mg are administered. Kidney transplant patients at low or moderate immunologic risk Combination therapy with this medicine and cyclosporine: Initially, this medicine is recommended for use in combination with cyclosporine and corticosteroids. New kidney transplant recipients should receive a loading dose 3 times the maintenance dose. For kidney transplant patients, a loading dose of 6mg/day and a maintenance dose of 2mg/day are recommended. Maintain sirolimus concentrations within the target range through therapeutic drug monitoring. Administration of this medicine after withdrawal of cyclosporine: Patients undergoing withdrawal of cyclosporine for the first time should be receiving this medicine in combination with cyclosporine. Withdrawal of cyclosporine is recommended 2~4 months after transplantation. At 2-4 months after transplantation, cyclosporine should be gradually discontinued over 4-8 weeks, and the dose of this medicine should be adjusted so that its trough concentration during the first year after transplantation is within 16-24ng/mL (chromatographic method). Thereafter, the target blood concentration of this medicine should be 12-20 ng/mL (chromatographic method). Cyclosporine inhibits the metabolism and transport of this medicine; therefore, its concentration will decrease if its dose is not increased when cyclosporine is discontinued. When cyclosporine is not administered, the dose of this medicine needs to be increased approximately 4-fold because there is no pharmacokinetic interaction (requiring approximately a 2-fold dose increase) and the need for immunosuppression increases (requiring approximately a 2-fold dose increase). Kidney transplant patients at high immunologic risk For patients at high immunologic risk, combination therapy with cyclosporine and corticosteroids is recommended for 12 months after transplantation. The safety and efficacy of administering this combination therapy for more than 1 year in patients at high immunologic risk have not been studied. Therefore, changes to immunosuppressive therapy after the first 12 months following transplantation should be considered based on the patient's clinical condition. Patients receiving this medicine in combination with cyclosporine should receive a 15mg loading dose on the day of transplantation. Starting on day 2, a maintenance dose of 5mg should be administered. Measure the trough concentration on days 5-7 of treatment and adjust subsequent doses of this medicine so that its trough blood concentration is within 10-15ng/mL (chromatographic method). The initial dose of cyclosporine should be 7mg/kg/day in divided doses, and the dose should be adjusted continuously until the target whole-blood trough concentration is reached. The target whole-blood trough concentration is 200-300ng/mL through day 14, 150-200ng/mL from day 15 to week 26, and 100-150ng/mL from week 27 to week 52. Prednisolone should be administered at a dose of at least 5mg/day. Antibody induction therapy may be used. Dosage for patients with lymphangioleiomyomatosis The initial dose of this medicine for patients with lymphangioleiomyomatosis is 2 mg daily. The whole-blood trough concentration of this medicine should be measured on days 10-20, and the dose should be adjusted to maintain the concentration within 5-15 ng/mL. For most patients, the following formula may be used to adjust the dose: New dose of this medicine=Current doseX(Target blood concentration/Current blood concentration). Once the maintenance dose of this medicine has been adjusted, maintain that dose for at least 7-14 days before readjusting the dose based on therapeutic drug monitoring. Once a stable dose has been established, therapeutic drug monitoring should be performed at least once every 3 months. For patients with hepatic impairment, a maintenance dose of approximately 2/3 of the dose for patients with normal liver function is recommended for patients with mild to moderate hepatic impairment. For patients with severe hepatic impairment, a maintenance dose of approximately 1/2 of the dose for patients with normal liver function is recommended. The loading dose does not need to be changed. No dose adjustment is required for patients with renal impairment.

Child dose

For patients aged 13 years and older who weigh less than 40kg, adjust the initial loading dose to 3mg/m2/day and the maintenance dose to 1mg/m2/day based on body surface area.

This medication suppresses immune function, which may weaken resistance to infections. Therefore, extra caution must be exercised to prevent infections while taking this medication, and medical consultation should be sought immediately if infection symptoms appear. This medication is not recommended for patients with liver or lung transplants, and there is a heightened risk of serious side effects in patients who have just received a liver transplant, thus caution is necessary. Additionally, co-administration with other immunosuppressants may increase the risks of thrombosis, transplant failure, and death, so it should be taken under medical advice. This medication can increase blood lipid levels (cholesterol, triglycerides), and regular blood tests should be conducted to monitor the condition, with appropriate treatment if necessary. Due to its potential impact on kidney function, regular kidney function tests should be conducted, and dosing adjustments or discontinuation may be necessary if kidney function worsens. While taking this medication, there is an increased risk of malignancies such as skin cancer and lymphoma; hence, it is crucial to take care of skin protection and undergo regular check-ups. Wound healing may be delayed, so care is needed with wound management after surgery, and symptoms such as fluid retention or edema may occur. This medication has interactions with certain drugs, which may alter drug concentrations if taken together; therefore, inform your healthcare provider about any other medications you are taking. Women who are pregnant or planning to become pregnant must consult with a doctor before taking this medication, as its use during pregnancy may affect the fetus. While breastfeeding, this medication may be excreted into breast milk, so breastfeeding may need to be discontinued or adjusted based on the medication use. Overdosage can lead to serious side effects, so strict adherence to prescribed dosage and administration schedule is required. This medication has not been established to be safe and effective in children, especially in those under 13 years, and caution should be exercised in its use. Elderly patients do not require special dose adjustments, but consultation with healthcare providers is recommended based on their physical condition. During the course of this medication, regular check-ups and strict adherence to medical advice are essential; report any abnormal symptoms immediately.

Thrombocytopenia, anemia, leukopenia, hemolytic uremic syndrome, neutropenia, pancytopenia, thrombotic thrombocytopenic purpura, tachycardia, pericardial effusion, abdominal pain, constipation, diarrhea, nausea, pancreatitis, stomatitis, ascites, wound healing disorders, edema, peripheral edema, fever, pain, hypersensitivity, angioedema, anaphylactic reaction, anaphylactoid reaction, pneumonia, fungal infection, viral infection, bacterial infection, herpes simplex, urinary tract infection, sepsis, pyelonephritis, cytomegalovirus infection, herpes zoster, mycobacterial infection, tuberculosis, Epstein-Barr virus infection, abnormal liver function tests, increased alanine aminotransferase, increased aspartate aminotransferase, increased serum creatinine, increased serum lactate dehydrogenase, hypokalemia, hypophosphatemia, hyperlipidemia, hypercholesterolemia, hyperglycemia, hypertriglyceridemia, fluid retention, diabetes mellitus, arthralgia, osteonecrosis, squamous cell carcinoma, basal cell carcinoma, lymphoma, malignant melanoma, post-transplant lymphoproliferative disorder, neuroendocrine carcinoma, headache, reversible posterior leukoencephalopathy syndrome, proteinuria, nephrotic syndrome, focal segmental glomerulosclerosis, menstrual disorders, amenorrhea, menorrhagia, ovarian cysts, pulmonary embolism, interstitial pneumonia, pleural effusion, epistaxis, pulmonary hemorrhage, alveolar proteinosis, rash, acne, exfoliative dermatitis, hypersensitivity vasculitis, hypertension, lymphorrhea, venous thrombosis, deep vein thrombosis, lymphedema, weakness, abdominal distension, chills, cold symptoms, hernia, malaise, atrial fibrillation, congestive heart failure, bleeding, hypervolemia, hypotension, palpitations, peripheral vascular disorder, orthostatic hypotension, syncope, vasodilation, dyspepsia, vomiting, loss of appetite, dysphagia, belching, esophagitis, gastric distension, gingival hyperplasia, intestinal obstruction, oral candidiasis, Cushing's syndrome, petechiae, leukocytosis, lymphadenopathy, erythrocytosis, hyperkalemia, weight gain, acidosis, increased BUN, increased creatine phosphokinase, dehydration, hypercalcemia, hypocalcemia, hyperphosphatemia, hypoglycemia, hypomagnesemia, hyponatremia, weight loss, arthrosis, leg cramps, myalgia, osteoporosis, stiffness, tremors, anxiety, confusion, depression, dizziness, emotional instability, muscle tension dysregulation, sensory impairment, muscle tone reduction, insomnia, neuropathy, sensory disturbance, drowsiness, shortness of breath, asthma, atelectasis, increased cough, hypoxia, pulmonary edema, fungal dermatitis, hirsutism, pruritus, skin thickening, skin ulcers, sweating, abnormal vision, cataracts, hearing loss, tinnitus, dysuria, hematuria, kidney stones, erectile dysfunction, renal colic, tubular necrosis, nocturia, oliguria, pyuria, testicular disorders, toxin nephropathy, frequent urination, urinary incontinence, urine retention, polyuria, localized reaction to surgery, stomatitis, nasopharyngitis, chest pain, upper respiratory tract infection, dizziness, myalgia, hypercholesterolemia, constipation, increased blood cholesterol, pain at the surgical site, hyperglycemia, azotemia, transplant rejection, pneumonia, intestinal obstruction, increased susceptibility to infection, fractures, agranulocytosis, abscess, cholangitis, cystitis, vesicoureteral reflux, ascites, hyperplasia of the adrenal glands, contact dermatitis, polyomavirus infection, increased plasma osmolality, worsening angina, renal artery occlusion, dental caries, ulcerative stomatitis, azoospermia, Clostridium difficile enterocolitis, liver necrosis, fascial compartment syndrome, incisional hernia, anastomotic rupture, BK virus-associated nephropathy, progressive multifocal leukoencephalopathy, acute rejection reaction, new-onset diabetes mellitus, rhabdomyolysis, anaphylaxis, angioedema, exfoliative dermatitis, hypersensitivity vasculitis

This medication should be stored in a tightly closed container to prevent exposure to air and light. Additionally, it is advisable to store it at room temperature between 20 and 25 degrees Celsius. This will help maintain the medication's efficacy for a longer period.

Appearance

Yellow or yellowish triangular film-coated tablet

Package unit

100 tablets (10 tablets/PTP x 10)