The use of diuretics for the treatment of sodium retention in congesti
ve heart failure was evaluated. Particular focus was given to the alte
red renal response to diuretics in patients with heart failure and adv
erse responses to diuretic therapy. Highlighted information included h
istorical aspects of the development of diuretics, mechanisms of sodiu
m retention, the physiologic and clinical response to diuretics, and t
he altered pharmacokinetics and pharmacodynamics of diuretics in conge
stive heart failure. Despite more than 60 years of empiric diuretic us
e in heart failure, the actual database regarding the long-term effica
cy, adverse effects, and altered mortality outcome in heart failure is
relatively small. Existent pharmacokinetic and pharmacodynamic data a
re typically not collected within the context of heart failure efficac
y trials. In addition to altered electrolyte transport and total-body
electrolyte depletion, diuretics may be associated with adverse neuroh
ormonal activation. Thus, guidelines for acute and long-term therapy w
ith diuretics in heart failure remain somewhat empiric. Diuretics will
remain a mainstay for the treatment of edema in congestive heart fail
ure but must be accompanied by moderate sodium restriction. However, l
arge clinical trials of diuretics would be necessary to demonstrate th
at improved clinical efficacy with edema reduction is not offset by ad
verse effects, which include electrolyte depletion, ventricular arrhyt
hmias, and subsequent increased mortality.