Rios A, Crofoot GE, Lenk R, Hayman A, Rosenblum M, Lopez-Berestein G; International Conference on AIDS.
Int Conf AIDS. 1992 Jul 19-24; 8: 127 (abstract no. PuB 7473).
Twelve Oaks Hospital, Houston, Texas.
OBJECTIVES: To describe the single dose safety evaluation and pharmacokinetic study of Nystatin-LF administered intravenously to patients with ARC. METHODS: Seventeen male patients received a single intravenous dose of Nystatin-LF administered at a rate of 2 mg. of Nystatin per minute. The dose levels were 0.25 mg./kg. (four patients), 0.5 mg./kg. (four patients), 0.75 mg./kg (five patients) and 1 mg./kg. of Nystatin (four patients). Serum plasma and urine samples collected after the administration of the single dose (on study day 1) were analyzed for Nystatin LF using a HPLC method. The resulting values for each patient were analyzed by non-linear regression analysis to obtained the best fit curves (RSTRIP from Micro Math Inc., Salt Lake City, UT) and pharmacokinetic parameters were obtained. RESULTS: Data from four patients were analyzed each at the 0.75 mg./kg. and the 1.0 mg./kg. dose level. The maximum achieved plasma level (CPo) at 1.0 mg./kg. was 9 + 0.6 mg./ml. The area under the curve was 1,263 + 301 mg./ml x minute. Clearance from the blood was biphasic. The t 1/2A life was 7.3 + 2.8 minute and the t 1/2B life was 42 + 16 minutes. CONCLUSIONS: No major renal, neurological, pulmonary, or cardiac toxicity was observed after the administration of a single dose of Nystatin-LF IV in patients with ARC. There were no dose/dependent changes in PKC Nystatin-LF IV between 0.75 mg./kg. dose level and 1.0 mg./kg. dose level. Using this information, phase I/II studies are being planned to define the clinical anti-HIV activity of Nystatin-LF.
Publication Types:
Keywords:
- Biomedical Research
- Chromatography, High Pressure Liquid
- Humans
- Liposomes
- Male
- Nystatin
- Protein Kinase C
- Single Person
- blood
- enzymology
- methods
- pharmacokinetics
Other ID:
UI: 102201240
From Meeting Abstracts