THE LACK EFFECT OF FOOD ON THE BIOAVAILABILITY OF NEFAZODONE TABLETS

• Published in: Biopharmaceutics & drug disposition Vol. 17; no. 2; pp. 135 - 143
• Main Authors: Dockens, R. C., Greene, D. S., Barbhaiya, R. H.
• Format: Journal Article
• Language: English
• Published: New York John Wiley & Sons, Ltd 01.03.1996; Wiley
• Subjects: Adolescent; Adult; Antidepressive Agents, Second-Generation - pharmacokinetics; Biological and medical sciences; Biological Availability; Cross-Over Studies; Dietary Fats - pharmacology; food effects; Humans; Male; Medical sciences; nefazodone; Neuropharmacology; Pharmacology. Drug treatments; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease); Psychology. Psychoanalysis. Psychiatry; Psychopharmacology; Reference Values; Tablets; Triazoles - pharmacokinetics; Human; Serotonin; Single dose; Oral administration; Adult; Antidepressant agent; Tablet; Bioavailability; Reuptake inhibitor; Normal; Pharmacokinetics; Food drug interaction
• ISSN: 0142-2782; 1099-081X
• DOI: 10.1002/(SICI)1099-081X(199603)17:2<135::AID-BDD947>3.0.CO;2-K

The objective of this study was to assess the effect of food on the pharmacokinetics of nefazodone (NEF). A group of 24 healthy adult male volunteers received a single 200 mg dose of NEF under fasting conditions as well as 5 min after a high‐fat breakfast. There was a 1 week washout between treatments. Serial blood samples were collected for 48 h after dosing and assayed by a validated HPLC method for NEF and the metabolites hydroxynefazodone (HO‐NEF), m‐chlorophenylpiperazine (mCPP), and triazoledione (dione). The mean (SD) peak concentration (Cmax) for NEF was not affected by food and was 416 (220) ng mL−1 and 446 (271) ng mL−1 after the fed and fasted treatments, respectively. The median time to reach Cmax (Tmax ) was also unaffected by food and was 2 h for both treatments. However, the mean (SD) area under the curve (AUC) was significantly reduced by food from 1815 (1017) ng h mL−1 to 1409 (695) ng h mL−1. Although there was an 18% decrease in NEF AUC when administered with food, food had no effect on Cmax and Tmax values for NEF, HO‐NEF, mCPP or dione or AUC values for HO‐NEF, mCPP, or dione, indicating that NEF can be administered without regard to meals.