Procaine hydrochloride (the active component of Gerovital H3)

synthetic

provenance:synthetic

first introduced:1905

regulatory status:off label

context:Procaine, a synthetic ester local anesthetic, was introduced in 1905 (marketed as Novocain) and used for decades as an injectable local anesthetic. From about 1949 to 1951 Constantin Ion Parhon and Ana Aslan in Bucharest repurposed buffered, stabilized procaine as a systemic anti-aging agent, branded Gerovital H3 (a roughly two percent procaine hydrochloride solution with benzoic acid, potassium metabisulfite, and disodium phosphate as stabilizers at about pH 3.3, procaine being the major component).

MECHANISM CLAIMED

That a course of injected (and later oral) buffered procaine systemically retards the aging process and treats the chronic diseases of later life, restoring vitality, mobility, mood, skin, and sexual function in the aged.

MECHANISM ACTUAL

Injected procaine is rapidly hydrolyzed in the body to para-aminobenzoic acid and diethylaminoethanol. The 1977 Ostfeld, Smith, and Stotsky review of the world literature (more than 100,000 treated patients) found no convincing evidence of any anti-aging or disease-treating value beyond a possible antidepressant effect, consistent with weak, reversible monoamine oxidase inhibition. Procaine remains an approved local anesthetic; its systemic anti-aging use is unapproved, and the US FDA classified the Gerovital H3 anti-aging product as an unapproved new drug and acted against its importation in 1982.

INTERVENTIONS USING IT

Gerovital H3 (procaine anti-aging therapy)

NOTES

Procaine hydrochloride is a synthetic local anesthetic introduced in 1905. Its place in this archive is as the active component of Gerovital H3, the buffered procaine preparation that Parhon and Aslan promoted from around 1949 to 1951 as a systemic treatment for aging. In the body it breaks down to para-aminobenzoic acid and diethylaminoethanol; the only systemic effect the clinical literature supports is a possible mild antidepressant action attributed to weak monoamine oxidase inhibition. The molecule remains a legitimate local anesthetic, which is why the ingredient is recorded as off-label rather than banned: it is the anti-aging use, and the specific Gerovital H3 product, that the evidence and the regulators rejected.