Elevated aluminum concentrations have been implicated in several disea
se states in the elderly. We examined the effects of sucralfate, a bas
ic aluminum salt of sucrose sulfate, and ranitidine, administered indi
vidually and in combination, on plasma and urine aluminum concentratio
ns in the elderly in a prospective, randomized, three-arm crossover st
udy. Subjects were 20 healthy volunteers over age 65 years, with no cl
inically significant comorbidities or recent use of aluminum-containin
g drugs or histamine (H)(2)-antagonists. The three regimens were ranit
idine 300 mg at bedtime, sucralfate 1 g 4 times/day, and ranitidine 30
0 mg at bedtime plus sucralfate 1 g 4 times/day, administered for 4 we
eks, with a washout period of at least 1 week between regimens. Plasma
and urine aluminum concentrations were measured on days 0, 1, 7, 14,
and 28 of each regimen. After 28 days, mean plasma aluminum concentrat
ions were significantly higher in subjects receiving sucralfate alone
(8.5 +/- 1.8 mu g/L) and sucralfate plus ranitidine (5.1 +/- 1.3 mu g/
L) compared with those receiving ranitidine alone (2.4 +/- 0.7 mu g/L)
. Urine aluminum concentrations were significantly higher in subjects
receiving sucralfate alone (133.2 +/- 32.8 mu g/g creatinine) and sucr
alfate plus ranitidine (148.1 +/- 51.9 mu g/g creatinine) compared wit
h those receiving ranitidine alone (11.0 +/- 3.7 mu g/g creatinine). T
here was no significant difference in plasma or urine aluminum concent
rations between subjects who received sucralfate alone versus those wh
o received sucralfate plus ranitidine. Sucralfate 4 g/day in elderly s
ubjects produces a significant increase in both plasma and urine alumi
num concentrations, compared with ranitidine 300 mg/day. This increase
most likely is secondary to gastrointestinal absorption of aluminum i
n the sucralfate formulation. The clinical relevance of this increase
requires further evaluation.