PMID- 11255279
OWN - NLM
STAT- MEDLINE
DCOM- 20010802
LR  - 20131121
IS  - 0390-6078 (Print)
IS  - 0390-6078 (Linking)
VI  - 86
IP  - 3
DP  - 2001 Mar
TI  - Pharmacokinetic study of the new cyclosporine-A formulation (Neoral) in adult 
      allogeneic bone marrow transplant recipients.
PG  - 311-5
AB  - BACKGROUND AND OBJECTIVES: A major problem encountered during oral cyclosporin-A 
      (CsA) administration to prevent acute graft-versus-host-disease (GVHD) after 
      allogeneic bone marrow transplantation (allo-BMT) is its irregular 
      pharmacokinetics. The aim of this study was to evaluate the pharmacokinetics of 
      Neoral, a new water-free microemulsion formulation of CsA. DESIGN AND METHODS: 
      Eighteen patients aged over 18 were enrolled into the study. When able to eat 
      normally after allo-BMT, patients received CsA orally and after 4 days a 12-hour 
      CsA pharmacokinetic profile was constructed. Three patients received Sandimmune 
      10 mg/kg/day, 5 patients received Neoral 7.5 mg/kg/day and 10 patients Neoral 5 
      mg/kg/day. CsA concentration was analyzed on whole blood by high-performance 
      liquid chromatography (HPLC). RESULTS: Neoral showed concentration-time profiles 
      characterized by a smooth and faster rise to the Cmax value compared to that 
      produced by Sandimmune. The comparison between pharmacokinetic parameters 
      obtained in patients receiving Neoral 5 mg/kg/day or 7.5 mg/kg/day showed a 
      proportional increase of the AUC (4776+/-1084 vs. 7746+/-2006 ng/mL h) and C(max) 
      (1027+/-203 vs. 1514+/-231 ng/mL). In all patients to whom 7.5 mg/kg/day of 
      Neoral were given, C(trough) levels were always above the threshold of 200 ng/mL. 
      INTERPRETATION AND CONCLUSIONS: Our data suggest that oral administration of 
      Neoral 7.5 mg/kg/day early after allo-BMT may represent an appropriate dose 
      resulting in adequate CsA C(trough) levels without significant renal toxicity.
FAU - Dotti, G
AU  - Dotti G
AD  - Divisione di Ematologia, Ospedali Riuniti di Bergamo, and Istituto di Ricerche 
      Farmacologiche Mario Negri Bergamo, Italy.
FAU - Gaspari, F
AU  - Gaspari F
FAU - Caruso, R
AU  - Caruso R
FAU - Perico, N
AU  - Perico N
FAU - Remuzzi, G
AU  - Remuzzi G
FAU - Barbui, T
AU  - Barbui T
FAU - Rambaldi, A
AU  - Rambaldi A
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Italy
TA  - Haematologica
JT  - Haematologica
JID - 0417435
RN  - 0 (Immunosuppressive Agents)
RN  - 83HN0GTJ6D (Cyclosporine)
SB  - IM
MH  - Adult
MH  - Aged
MH  - Area Under Curve
MH  - *Bone Marrow Transplantation
MH  - Cyclosporine/*pharmacokinetics
MH  - Female
MH  - Graft vs Host Disease/drug therapy/prevention & control
MH  - Hematologic Neoplasms/therapy
MH  - Humans
MH  - Immunosuppressive Agents/*pharmacokinetics
MH  - Male
MH  - Middle Aged
MH  - Transplantation, Homologous
EDAT- 2001/03/20 10:00
MHDA- 2001/08/03 10:01
CRDT- 2001/03/20 10:00
PHST- 2001/03/20 10:00 [pubmed]
PHST- 2001/08/03 10:01 [medline]
PHST- 2001/03/20 10:00 [entrez]
PST - ppublish
SO  - Haematologica. 2001 Mar;86(3):311-5.