Neoral (cyclosporine, modified) is a critical immunosuppressive agent formulated to prevent organ rejection in transplant recipients. Its advanced microemulsion technology ensures more consistent and predictable drug absorption compared to conventional cyclosporine formulations, offering clinicians greater control over therapeutic outcomes. By selectively inhibiting T-cell activation, Neoral provides targeted immunosuppression while minimizing broad-spectrum immune suppression risks. It is a cornerstone therapy in solid organ transplantation and is also indicated for severe autoimmune conditions where calibrated immune modulation is essential.

Features

• Microemulsion formulation for improved bioavailability
• Consistent and predictable pharmacokinetic profile
• Available in 25 mg and 100 mg soft gelatin capsules
• Oral solution (100 mg/mL) for flexible dosing
• Branded cyclosporine with extensive clinical data
• Temperature-stable storage requirements

Benefits

• Significantly reduces risk of acute and chronic organ rejection
• Provides reliable and steady immunosuppression through enhanced absorption
• Allows for precise therapeutic drug monitoring and dose adjustments
• May reduce corticosteroid dependence in maintenance therapy
• Supports long-term graft survival in kidney, liver, and heart transplants
• Effective in managing severe rheumatoid arthritis and psoriasis when conventional therapies fail

Common use

Neoral is primarily indicated for the prophylaxis of organ rejection in patients receiving kidney, liver, and heart allogeneic transplants. It is used as part of a multidrug immunosuppressive regimen, often alongside corticosteroids and other agents. In non-transplant settings, it is approved for severe, active rheumatoid arthritis not responsive to methotrexate alone, and for severe, recalcitrant plaque psoriasis in adults. Its use requires careful patient selection and ongoing monitoring due to its narrow therapeutic index and potential for significant adverse effects.

Dosage and direction

Dosing is highly individualized and must be tailored based on transplant type, time post-transplant, therapeutic drug monitoring, and concomitant immunosuppressants. For new transplant recipients, initial oral doses typically range from 8–18 mg/kg/day, divided into two doses, administered 12 hours apart. Dosage is subsequently adjusted to achieve target cyclosporine blood trough concentrations, which vary by institution and transplant type. For autoimmune indications, starting doses are generally lower (e.g., 2.5–4 mg/kg/day for psoriasis). Neoral should be taken consistently with regard to meals to minimize absorption variability. Grapefruit and grapefruit juice must be avoided due to interaction risks.

Precautions

Patients must be under continuous medical supervision. Renal and hepatic function, blood pressure, and cyclosporine blood levels should be monitored regularly. Hyperkalemia, hyperuricemia, and hypomagnesemia may occur. Neoral increases susceptibility to infections and may exacerbate existing infections. Lymphoma and other malignancies have been reported. Blood pressure should be controlled before and during treatment. Patients should avoid excessive sun exposure due to increased photosensitivity risk. Live vaccines are contraindicated during therapy.

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, strong CYP3A4 inhibitors (e.g., ketoconazole), or inducers (e.g., rifampin) where alternatives are unavailable. Use is contraindicated in patients with abnormal renal function, uncontrolled hypertension, or malignancies, except in transplant settings where benefits outweigh risks. Concurrent use with psoralen plus ultraviolet A (PUVA) therapy is contraindicated in psoriasis patients.

Possible side effects

Common side effects include hypertension, tremor, hirsutism, hyperlipidemia, gum hyperplasia, headache, and gastrointestinal disturbances. Nephrotoxicity and hepatotoxicity are serious dose-related adverse effects. Other potential reactions include:

• Increased creatinine and reduced glomerular filtration rate
• Hyperkalemia
• Hemolytic uremic syndrome
• Seizures
• Pancreatitis
• Anaphylaxis in rare cases

Drug interaction

Neoral is a substrate of CYP3A4 and P-glycoprotein, resulting in numerous interactions. Concomitant use with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, grapefruit juice) increases cyclosporine levels and toxicity risk. Inducers (e.g., rifampin, phenytoin) may reduce efficacy. Nephrotoxic drugs like NSAIDs or aminoglycosides may enhance renal impairment. Neoral can increase concentrations of statins, digoxin, and repaglinide. Dose adjustments and close monitoring are essential when co-administering interacting drugs.

Missed dose

If a dose is missed, it should be taken as soon as possible. However, if it is nearly time for the next dose, the missed dose should be skipped. Doubling the dose is not recommended. Patients should contact their healthcare provider for guidance, especially if multiple doses are missed, as subtherapeutic levels may increase rejection risk.

Overdose

Symptoms of overdose may include severe nausea, vomiting, lethargy, hypertension, nephrotoxicity, hepatotoxicity, and seizures. Management includes immediate gastric lavage if ingestion was recent, supportive measures, and monitoring of vital signs, renal function, and cyclosporine levels. Hemodialysis is not effective due to high protein binding; charcoal hemoperfusion may be considered in severe cases.

Storage

Store at room temperature (15–30°C or 59–86°F). Keep in the original container, tightly closed, and protect from moisture and light. Do not freeze. Oral solution should be used within two months after opening. Keep out of reach of children and pets.

Disclaimer

This information is intended for healthcare professionals and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for personalized recommendations. Dosage, administration, and monitoring must be individualized under specialist supervision.

Reviews

Neoral is widely regarded among transplant specialists as a reliable and effective calcineurin inhibitor. Clinical studies consistently demonstrate its role in improving graft and patient survival. Its microemulsion formulation is praised for reducing pharmacokinetic variability. However, clinicians emphasize the necessity of vigilant therapeutic drug monitoring and management of side effects. Long-term use requires balancing efficacy with chronic nephrotoxicity risks. In autoimmune applications, it remains a valuable option for severe cases unresponsive to first-line treatments.