This article reviews the literature pertaining to the metabolism of several of the commonly used opioids, and the known activity of their metabolites. The effect of renal failure on the pharmacokinetics of these drugs and metabolites is then reviewed. Finally, the effect of renal dialysis on opioid drugs and metabolites is reviewed. Based on the review, it is recommended that morphine and codeine are avoided in renal failure/dialysis patients; hydromorphone or oxycodone are used with caution and close monitoring; and that methadone and fentanyl/sufentanil appear to be safe to use. Note is made that the "safe" drugs in renal failure are also the least dialyzable.