Short report: the absorption of fluconazole and itraconazole under conditions of low intragastric acidity.
The study investigated the oral absorption of two antifungal agents, fluconazole and itraconazole, under conditions of low intragastric acidity. Twelve healthy male volunteers received each of 4 dosing regimens: 200 mg itraconazole alone, 200 mg itraconazole and famotidine, 100 mg fluconazole alone, and 100 mg fluconazole and famotidine. Two oral doses of 40 mg famotidine were used to induce hypochlorhydria. Serum drug concentrations were measured (by high pressure liquid chromatography) for 48 h after a single dose of each anti-fungal agent. When dosed with famotidine, there was a significant 52.9% decrease of the peak intraconazole concentration (P < 0.011), and a significant 51.1% decrease of the 48-h integrated serum intraconazole concentration (P = 0.005). Famotidine-induced hypochlorhydria did not affect the absorption of fluconazole.
Lim
S G
SG
University Department of Medicine, Royal Free Hospital School of Medicine, London, UK.
Sawyerr
A M
AM
Hudson
M
M
Sercombe
J
J
Pounder
R E
RE
D000328:Adult; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001682:Biological Availability; D015738:Famotidine / Q000494:pharmacology; D005744:Gastric Acid / Q000502:physiology*; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology*; D017964:Itraconazole; D007654:Ketoconazole / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008297:Male
D000935:Antifungal Agents; D017964:Itraconazole; D015738:Famotidine; D007654:Ketoconazole