Two medicines, procaine and its derivative Gerovital H3, have a long history of medical use: 120 years and 75 years, respectively. This chapter describes their mechanisms of action, both classical and pleiotropic. Procaine has been used as a local anesthetic and Gerovital H3 has shown several other effects that are briefly described along with some of the most recent studies that support them. The latter, sometimes together with procaine, has demonstrated antioxidant and free radical scavenger action, antiatherogenic effects, antidepressive activity, protection against deleterious effects of ionizing radiations, some positive effects in case of neoplasia, some improvement in mental symptoms. Several studies with negative results will be also presented, all of them with a critical evaluation and analysis. Many areas in the field of chronic conditions in older people are still not entirely understood.