Pharmacokinetics of oral cyclosporine (Neoral) in heart transplant recipients during the immediate period after surgery

• Published in: Transplant international 2002-12, Vol.15 (12), p.649
• Main Authors: Banner, Nicholas R, David, Olivier J, Leaver, Neil, Davis, Julie, Breen, Jane, Johnston, Atholl, Yacoub, Magdi H
• Format: Article
• Language: English
• ISSN: 0934-0874; 1432-2277
• DOI: 10.1007/s00147-002-0491-0

Neoral cyclosporine has better absorption characteristics than the original Sandimmun formulation. This has allowed Neoral to be administered orally in circumstances where Sandimmun had been ineffective, including the postoperative phase of liver transplantation. Sampling strategies, such as the measurement of drug concentration 2 h after oral administration, have been used in a variety of settings to estimate systemic exposure to Neoral (measured as the area under the blood concentration curve (AUC) of the drug) in blood. We conducted a pilot study to determine whether Neoral could be administered orally immediately after heart transplantation and to determine which pharmacokinetic parameters reflect systemic drug exposure in this setting. Eight male patients (mean age 50 years) undergoing a first heart transplant were studied. Neoral was administered orally before surgery and at 12-h intervals via a nasogastric tube after surgery. Twelve-hour pharmacokinetic profiles were obtained on postoperative days 1, 3 and 5. Cyclosporine concentrations were measured with the Dade Behring Emit assay, which is specific for the parent drug. Drug concentrations were dose-normalised and drug exposure was measured by the AUC. Drug exposure following administration (AUC0-12) was low on day 1 but increased by 99% between postoperative day 1 and day 5 (P