Since Alfred Einhorn created the molecule in 1905, researchers have investigated its potential therapeutic uses. Initially, it was believed to be toxic or have adverse effects if it entered the general circulation. However, in 1909, Bier applied procaine intravenously to produce local anesthesia on the limbs. Since 1920, researchers have explored various ways to administer procaine, including intravenous, intra-arterial, and intramuscular ways. Several therapeutic effects have been observed, including pain, rheumatic diseases, musculoskeletal trauma, integumentary system diseases, mental and psychic effects, allergic and toxic reactions, autoimmune diseases, and cancer. Procaine’s activity on various biochemical systems, such as dopamine, norepinephrine, serotonin, and glutamate, makes it useful for studying the limbic system and emotions. After more than one hundred years of treating a wide range of conditions, systemic use of procaine has shown a strong anti-inflammatory therapeutic strategy with minimal or no side effects at moderate doses. Additionally, the systemic administration of procaine can be the basis for treating all relevant diseases in elderly people because of the wide range of geroprotective features of action. It can be administered independently of classic neural therapy. The presence of bicarbonate as an additive in the procaine infusion can extend its systemic effects. The dosage should be adjusted based on the patient’s acid-base balance and individual tolerance.