From the Guidelines
Neoral (Cyclosporine) is a calcineurin inhibitor used as an immunosuppressant medication.
Key Characteristics
- It is available in various formulations, including Neoral, which provides improved consistency in drug delivery compared to the original Sandimmun formulation 1.
- Cyclosporine is metabolized primarily by the cytochrome P450 3A4 subtype (CYP3A4), and its use can increase or decrease the levels of other medications that are metabolized by CYP3A4, such as statins, calcium channel blockers, and warfarin 1.
- The medication has a narrow therapeutic index, and its dosage is based on trough levels of the drug, which are highly individualized 1.
Common Side Effects
- Renal toxicity and hypertension are the most significant common risks associated with Cyclosporine use 1.
- Other commonly encountered side-effects include gastrointestinal disturbances, gingival hyperplasia, hyperlipidaemia, generalized hypertrichosis, paraesthesiae, and tremor 1.
Special Considerations
- Cyclosporine can cause nephrotoxicity, and regular monitoring of its blood concentration as well as renal function is mandatory 1.
- The medication can increase vascular resistance, resulting in reduced renal blood flow, decreased clearance of endogenous creatinine, and increased serum creatinine 1.
- Cyclosporine contains ethanol and has been found in human breast milk, and a decision should be made whether to discontinue nursing or the medication based on the benefit of therapy to the patient 1.
From the FDA Drug Label
Cyclosporine capsules, USP [MODIFIED] and cyclosporine oral solution, USP [MODIFIED] are oral formulations of cyclosporine that immediately forms a microemulsion in an aqueous environment. Cyclosporine, the active principle in cyclosporine capsules [MODIFIED] and cyclosporine oral solution, USP [MODIFIED], is a cyclic polypeptide immunosuppressant agent consisting of 11 amino acids
Neoral is another name for Cyclosporine, which is a cyclic polypeptide immunosuppressant agent. It is used to prevent rejection in organ transplant patients. The main active ingredient in Neoral is Cyclosporine 2.
From the Research
Definition and Mechanism of Neoral (Cyclosporine)
- Neoral, also known as Cyclosporine, is a lipophilic cyclic polypeptide immunosuppressant that interferes with the activity of T cells chiefly via calcineurin inhibition 3.
- It produces calcium-dependent, specific, reversible inhibition of transcription of interleukin-2 and several other cytokines, most notably in T helper lymphocytes 4.
Pharmacokinetic Properties
- The original oil-based oral formulation of Cyclosporine (Sandimmun) has high intra- and interpatient pharmacokinetic variability, with poor bioavailability in many patients 3.
- Neoral, a microemulsion formulation of Cyclosporine, improves the bioavailability and pharmacokinetics of Cyclosporine, reducing inter- and intraindividual pharmacokinetic variability 5, 6.
- The microemulsion formulation provides more predictable and extensive drug absorption than the standard formulation, with faster and more extensive absorption in healthy volunteers and renal or liver transplant recipients 7.
Clinical Efficacy and Tolerability
- Neoral is at least as effective as the oil-based formulation in renal, liver, and heart transplant recipients, with trends towards decreased incidence of acute rejection in some trials 3.
- The microemulsion formulation has a safety profile comparable to that of Sandimmun, with the most common adverse events being hypertrichosis, gingival hyperplasia, and neurological and gastrointestinal effects 6, 4.
- Neoral has been evaluated in a range of disorders where immunoregulatory dysfunction is a suspected or proven aetiological factor, including psoriasis, atopic dermatitis, rheumatoid arthritis, and nephrotic syndrome 4.