Neoral (cyclosporine, modified) is a critical immunosuppressive agent formulated to prevent organ rejection in transplant recipients. As a microemulsion, it offers improved and more consistent bioavailability compared to earlier formulations, allowing for more predictable blood levels and enhanced therapeutic outcomes. This advanced calcineurin inhibitor is a cornerstone of maintenance immunosuppressive therapy, trusted by transplant specialists worldwide for its efficacy in modulating T-cell activation and prolonging graft survival. Its precise pharmacokinetic profile supports individualized dosing strategies, making it an essential component in post-transplant care protocols.

Features

• Microemulsion formulation for enhanced bioavailability
• Consistent and predictable absorption profile
• Available in 25 mg and 100 mg soft gelatin capsules
• Oral solution formulation (100 mg/mL) for flexible dosing
• Calcineurin inhibitor class medication
• Requires therapeutic drug monitoring
• Brand-name version of modified cyclosporine
• Temperature-stable formulation

Benefits

• Significantly reduces risk of acute organ rejection in transplant recipients
• Provides more consistent blood levels compared to sandimmune formulation
• Allows for precise dose titration based on therapeutic drug monitoring
• Supports long-term graft survival when used as part of maintenance therapy
• Enables individualized immunosuppressive regimens
• Reduces interpatient variability in drug absorption

Common use

Neoral is primarily indicated for the prophylaxis of organ rejection in patients receiving allogeneic kidney, liver, and heart transplants. It is typically used as part of a maintenance immunosuppressive regimen, often in combination with corticosteroids and other immunosuppressive agents. The medication may also be prescribed for severe, active rheumatoid arthritis where conventional therapy has failed, and for severe, recalcitrant plaque psoriasis in adult non-immunocompromised patients. In transplant medicine, therapy is usually initiated within 24 hours before transplantation and continued postoperatively with careful monitoring of cyclosporine blood levels.

Dosage and direction

Dosage must be individualized based on patient weight, transplant type, and therapeutic drug monitoring. For kidney, liver, and heart transplantation: Initial dose is typically 8-18 mg/kg/day divided into two doses, beginning 4-12 hours prior to transplantation. Postoperative doses are adjusted based on cyclosporine blood trough levels, with maintenance doses usually ranging from 3-10 mg/kg/day. For rheumatoid arthritis: Initial dose is 2.5 mg/kg/day divided into two doses, which may be increased after 8 weeks to a maximum of 4 mg/kg/day. For psoriasis: Initial dose is 2.5 mg/kg/day divided into two doses, which may be increased after 4 weeks to a maximum of 4 mg/kg/day. Neoral should always be administered at consistent times relative to meals to maintain stable absorption.

Precautions

Patients require regular monitoring of cyclosporine blood levels, renal function, blood pressure, and liver enzymes. Blood pressure should be monitored frequently as hypertension may develop. Renal function must be assessed repeatedly as nephrotoxicity can occur. Liver function tests should be performed regularly as hepatotoxicity is possible. Patients should be monitored for signs of infection due to increased susceptibility. Regular dermatological examinations are recommended due to increased risk of skin malignancies. Lipid profiles should be monitored as hyperlipidemia may develop. Magnesium levels should be checked periodically as hypomagnesemia can occur. Patients should avoid excessive sun exposure and use protective measures due to photosensitivity risk.

Contraindications

Neoral is contraindicated in patients with hypersensitivity to cyclosporine or any component of the formulation. It should not be used with potassium-sparing diuretics in patients with hyperkalemia. Concomitant use with strong CYP3A4 inhibitors or inducers that cannot be discontinued is contraindicated. The medication is contraindicated in patients with abnormal renal function, uncontrolled hypertension, or malignancies except skin cancer. Live vaccines should not be administered during therapy. Neoral is contraindicated in patients with uncontrolled infections. The psoriasis indication is contraindicated in patients with abnormal renal function, uncontrolled hypertension, or prior PUVA or methotrexate therapy.

Possible side effects

Common adverse effects include hypertension (approximately 50% of patients), renal dysfunction (25-38%), tremor (21-55%), hirsutism (21-45%), gum hyperplasia (27%), gastrointestinal disturbances (23-44%), and headache (15-27%). Less frequent but serious side effects may include nephrotoxicity, hepatotoxicity, neurotoxicity, lymphoma and other malignancies, serious infections, thrombotic microangiopathy, and hyperkalemia. Metabolic effects may include hyperlipidemia, hypomagnesemia, and hyperuricemia. Dermatological effects can include acne and increased risk of skin malignancies. Hematological changes such as leukopenia and thrombocytopenia may occur.

Drug interaction

Neoral has numerous significant drug interactions due to CYP3A4 metabolism. Strong inhibitors of CYP3A4 (ketoconazole, itraconazole, clarithromycin) can increase cyclosporine levels. Inducers of CYP3A4 (rifampin, phenytoin, St. John’s wort) can decrease cyclosporine levels. Nephrotoxic drugs (aminoglycosides, amphotericin B, NSAIDs) may enhance renal toxicity. Potassium-sparing diuretics and potassium supplements may increase risk of hyperkalemia. Live vaccines may have reduced efficacy and increased risk of complications. Grapefruit juice may increase bioavailability and should be avoided. Statins may have increased risk of myopathy when coadministered.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. Patients should never double the dose to make up for a missed dose. If multiple doses are missed, patients should contact their healthcare provider immediately, as subtherapeutic levels may increase rejection risk. Consistency in dosing schedule is critical for maintaining therapeutic drug levels. Patients should be educated about the importance of adherence and provided with strategies to avoid missed doses.

Overdose

Cyclosporine overdose may manifest as elevated serum creatinine, hepatotoxicity, headache, nausea and vomiting, lethargy, hypertension, and tachycardia. In severe cases, overdose may lead to serious nephrotoxicity, hepatotoxicity, seizures, or coma. Management includes immediate discontinuation of Neoral, supportive care, and symptomatic treatment. Gastric lavage may be considered if ingestion was recent. Enhanced elimination through hemodialysis or hemoperfusion is not effective due to high protein binding and extensive tissue distribution. Specific monitoring of cyclosporine levels, renal and hepatic function is essential.

Storage

Neoral capsules should be stored at room temperature (15-30°C or 59-86°F) in their original container. The oral solution should be stored at room temperature and used within 2 months after opening. Both formulations should be protected from light and moisture. The medication should not be frozen. Keep out of reach of children and pets. Do not transfer capsules or solution to other containers. Unused medication should be properly disposed according to local regulations.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Neoral is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Dosage and administration must be determined by a physician based on individual patient characteristics and therapeutic drug monitoring. Patients should not adjust their dose without medical consultation. The full prescribing information should be consulted before initiating therapy. Individual results may vary, and not all side effects or interactions are listed here.

Reviews

Clinical studies demonstrate Neoral’s efficacy in transplant medicine, with one-year graft survival rates exceeding 90% in kidney transplant patients when used in combination regimens. Rheumatologists report significant improvement in rheumatoid arthritis symptoms in patients who have failed conventional DMARDs. Dermatologists note substantial clearing of psoriatic lesions in appropriate patients. However, specialists emphasize the critical importance of therapeutic drug monitoring and management of side effects. Many transplant centers consider Neoral an essential component of their immunosuppressive protocols due to its predictable pharmacokinetics and established efficacy profile.