IngredientsGerovital H3 — also marketed as GH3, Gerovital, and other variants that may or may not be chemically identical — is a preparation developed during the 1950s and promoted by advocates as an anti-aging treatment. It is not a botanical extract or naturally occurring plant constituent; rather, Gerovital H3 (GH3) is a pharmaceutical preparation consisting of 2% procaine hydrochloride stabilized with benzoic acid, potassium metabisulfite, and disodium phosphate. Procaine, originally synthesized in 1905 as a local anesthetic known as Novocain, forms the active ingredient in this formulation.
Common synonyms for the active ingredient include: 2-diethylaminoethyl 4-aminobenzoate hydrochloride, GeroVita, Gerovital H3, GH-3, KH-3, and procaine hydrochloride.
Gerovital H3 is primarily composed of procaine hydrochloride as its active ingredient, formulated as a 2% aqueous solution for injectable administration. This local anesthetic is derived from para-aminobenzoic acid (PABA) through esterification with diethylaminoethanol, resulting in the chemical formula C₁₃H₂₀N₂O₂·HCl.
Procaine hydrochloride (novocaine) was first synthesized by the German chemist Alfred Einhorn in 1905 and was used as a local anaesthetic. Administered intravenously from 1925, it was described as effective in migraine, pain, and asthma. After 1950, it was also used for its "antiageing" effects.
The preparation includes stabilizing and preservative additives to enhance its stability and suitability for systemic use: specifically, 0.12% benzoic acid as a preservative and 0.10% potassium metabisulfite as an antioxidant stabilizer, along with 0.01% disodium phosphate to maintain a pH of approximately 3.3. Unlike plain procaine hydrochloride, which is typically used for short-term local anesthesia in dental or surgical procedures, Gerovital H3 is a buffered and stabilized formulation optimized for repeated intramuscular injections to achieve systemic distribution and prolonged bioavailability.
Some advocates acknowledge that despite the stabilizers, the procaine in Gerovital H3 breaks down rapidly into DMAE (diethylaminoethanol) and PABA (para-aminobenzoic acid), but ascribe the beneficial effects to these breakdown products.
Gerovital H3 has been produced in both injectable and oral forms. A commercially available injectable formulation consists of a 5 cc aqueous solution containing procaine hydrochloride (0.1000 gram), benzoic acid (0.0060 gram), dipotassium metabisulfite (0.0050 gram), and disodium phosphate (0.0005 gram); this specific embodiment was sold as Gerovital H3 by Rom-Amer Pharmaceuticals Ltd. The formulation may also be taken orally; the active ingredient, plus one or more additional defined components, can be placed into a capsule or tablet for ingestion.
Related trade names and preparations include Gerovital, GH3, KH3, Zell H3, and similar designations. Products known as GH3, Aslavital, Vitacel, and other variants may or may not be identical to Gerovital H3 in composition.
Ana Aslan (1897–1988) was a Romanian biologist and physician who discovered the anti-aging effects of procaine, on which she developed the formulas Gerovital H3 and Aslavital. She is considered to be a pioneer of gerontology and geriatrics in Romania. While experimenting on the effects that procaine had on arthritis, Aslan discovered other beneficial effects of this drug. She ultimately patented two cosmetic products — a hair lotion and cream under the name Gerovital H3.
Since 1945, Professor Aslan had been injecting procaine into patients with painful arthritis in order to relieve their joint pains. Many of her patients noted improving memory, less depression, more energy, and a generalised feeling of well-being. These results encouraged her to carry out additional studies to test the effects of procaine on thousands of patients. Dr. Aslan's first experiments in 1949 produced positive results. However, she discovered that the enzyme cholinesterase degraded procaine within an hour, requiring frequent injections to produce benefits.
Aslan founded the Romanian National Institute of Gerontology and Geriatrics in 1950, reportedly the first government-sponsored aging research institute in the world. She found that by adding benzoic acid as a preservative, and potassium metabisulfite as an antioxidant, the procaine molecule was stabilized, and the effects were even more dramatic than with procaine alone. She called her improved form of procaine Gerovital, or GH3.
In 1956, a paper titled "A new method for prophylaxis and treatment of aging with Novocain-eutrophic and rejuvenating effects" was published in the now-discontinued journal Therapiewoche. The author and director of the Geriatrics Institute of Bucharest, Ana Aslan, claimed phenomenal improvement in the psychic, physiological, and social functioning of 189 elderly subjects who had undergone procaine (Novocaine) therapy over a period of ten years.
From the 1950s until her death in 1988, Dr. Aslan promoted Gerovital H3 with great success. In the 1960s and 1970s, her Romanian clinic — the Parhon Institute — became a mecca for celebrities seeking treatment and an upscale tourist attraction. The New York Times referred to Gerovital's "jet-set aura," noting that Aslan had been covered in "society columns where such public figures as Nikita S. Khrushchev, Konrad Adenauer, and Ibn Saud have been listed among the multitudes said to have taken the drug."
During Gerovital's "jet-set" heyday, treatments were reportedly administered to a stellar array of celebrities and dignitaries, including John F. Kennedy, Marlene Dietrich, Kirk Douglas, and Salvador Dalí. As late as 1988, an advertisement by the Romanian National Tourist Office lauded "the picturesque and exciting cities, scenic delights, famous resorts (including Gerovital H3 treatment centers), cultural and historic treasures that await the traveler to Romania."
In communist Romania, the state sponsored the marketing of Gerovital H3. In the early 1950s, the immortality-obsessed Nicolae Ceaușescu and his wife Elena — the country's Director of Science and Technology — supported the creation of an institute to develop an immortality drug.
The main active ingredient is the well-known local anesthetic procaine hydrochloride, often referred to by the old brand name Novocaine. Procaine acts primarily by blocking sodium channels in nerve membranes to inhibit pain signal transmission, but within the specific GH3 formulation, additional systemic actions have been investigated as discussed below.
Aslan stated that "due to the effects of its main active elements, the procaine and procaine's metabolites — paraaminobenzoic acid (PABA) and diethylaminoethanol (DEAE) — Gerovital H3 belongs to pregeriatric and geriatric drugs having a eutrophic effect on the organism."
Subsequent to Aslan's investigations on the psychic effect of procaine, Pfeiffer carried out pharmacological studies on dimethylaminoethanol (DMAE) action and noticed a mental stimulation. This study placed emphasis on the relations between DMAE and acetylcholine. DMAE is reported to cross the blood-brain barrier, participating in the metabolic processes of nerve cells, fixing their protein and lipid fractions, and converting into choline and acetylcholine.
Studies have shown that both procaine and PABA act at the level of cell membrane metabolism.
Gerovital H3 also contains small amounts of benzoic acid, potassium metabisulfite, and disodium phosphate, which are said to be important in the formulation, rendering it more effective by "stabilizing" it. The stabilized formulation is notably distinct from plain procaine: pharmacokinetic studies revealed that serum procaine levels are higher after the administration of GH3 than following the administration of a procaine solution of similar concentration.
The most extensively documented and scientifically accepted mechanism for GH3 is its inhibition of monoamine oxidase. The mechanism by which Gerovital H3 produces a weak inhibition of the enzyme monoamine oxidase (MAO) was studied by several methods. Purified rat-brain mitochondrial MAO was used as the enzyme source, and reaction velocities were determined by quantitating the rate of appearance of 4-hydroxyquinoline from kynuramine. Data on dilutional studies with pre-incubated enzyme-inhibitor complexes strongly indicated that GH3 was a reversible inhibitor of MAO. Analysis of Lineweaver-Burk and Dixon plots showed that GH3 was a fully competitive inhibitor of MAO.
The relative effectiveness of Gerovital H3, commercial procaine hydrochloride (Novocain), and iproniazid as MAO inhibitors was studied by means of tests involving serotonin and kynuramine metabolism by rat-brain MAO. Gerovital H3 was a more effective MAO inhibitor than commercial procaine hydrochloride but a less effective inhibitor than iproniazid. Moreover, Gerovital H3 seemed to have a selective affinity for certain of the multiple forms of MAO.
The weak, reversible, fully competitive inhibition of MAO produced by GH3 is in marked contrast to the potent, irreversible inhibition of MAO produced by currently available agents. The mechanism by which GH3 inhibits MAO may help to explain the absence of severe adverse reactions with GH3 that are traditionally associated with irreversible MAO inhibitors in the treatment of depressive illness.
The antioxidant effects of procaine and GH3 were assessed in a human lymphoblastoid cell line to evaluate their effects using a cellular experimental model that mimics physiological targets to be protected in vivo against oxidative stress. Procaine and GH3 similarly reduced the generation of cell membrane lipoperoxides at 5 and 10 mM concentrations. However, at the lowest concentration (2.5 mM), their effects significantly differed (p < 0.0001), as GH3 was more effective in reducing the generation of membrane lipoperoxides, showing similar activity to curcumin.
Both procaine and GH3 inhibited lipid peroxidation, but procaine was more effective in inhibiting mitochondria free radicals' generation, while GH3 showed a higher antioxidant action on macrophage-induced low-density lipoprotein oxidation.
Although the main active compound in GH3 is procaine, GH3 showed a protective effect against radiation, while procaine reduced the endogenous level of DNA strand breaks — suggesting a slightly different mode of action. In a study that investigated the effects of procaine and GH3 on the formation of endogenous and X-ray-induced DNA strand breaks in peripheral blood mononuclear cells (PBMCs) isolated from young and elderly individuals, GH3 showed the strongest radioprotective effects in PBMCs from young subjects, while procaine reduced the endogenous amount of DNA strand breaks more pronouncedly in aged individuals.
Gerovital H3 and related preparations are also claimed to have the following beneficial effects: neuron regeneration, cell membrane modulation, protection against cerebral anoxia, antioxidant activity, increasing resistance to infections and toxins, antidepressant activity, increasing serum HDL-C concentrations, and decreasing triglyceride levels. They are also claimed to be thyroid inhibitors, muscle relaxants, and antihistamines. They are said to decrease plasma cortisol levels and therefore to have an anti-stress effect. However, as documented in Section 5, independent scientific review has found inadequate clinical evidence for most of these claims.
Summary: Evidence is weak and largely discredited for broad anti-aging claims.
Although studies regarding the effects of GH3 were developed within a large prophylaxis campaign and there were clinical trials involving thousands of elderly subjects, some in the medical world of the 1960s contradicted the so-claimed beneficial effects of the treatment developed by Aslan. The negative outlook and backlash were caused because, at that time, behind Gerovital was more marketing for a "miraculous anti-aging product" than indisputable scientific evidence.
In the 1970s, the National Institute on Aging commissioned a thorough evaluation of the studies and claims surrounding Gerovital H3. The conclusion of that work was that, except for a possible mild monoamine oxidase (MAO) inhibitor effect that would potentially ameliorate depression, there was no scientifically credible evidence supporting the claims that procaine is beneficial in treating age-related diseases or syndromes. A plausible explanation for why some subjects might have experienced improvements in health was that, in addition to receiving Gerovital H3, they were receiving other interventions such as exercise, stress reduction, and healthy nutrition.
A review and evaluation of the world literature on the systemic use of procaine in the treatment of the aging process and common chronic diseases of later life included data from 285 articles and books describing treatment in more than 100,000 patients over 25 years. Except for a possible antidepressant effect, there was no convincing evidence that procaine (or Gerovital, of which procaine is the major component) has any value in the treatment of disease in older patients. If procaine has an antidepressant effect, there is some likelihood that this accounts for reports of decreased complaints referable to the musculoskeletal, cardiovascular, endocrine sexual, gastrointestinal, and respiratory systems.
Summary: The most scientifically supported area — evidence is preliminary and mixed; no regulatory approval in major markets.
Gerovital H3 has a certified antidepressive effect, especially in mild and moderate depressive syndrome, attributed to its MAO-inhibitory effect. The antidepressant effect of Gerovital H3, as well as the lack of serious side effects, can be accounted for on the basis that it is a reversible and competitive MAO inhibitor.
Upon returning to the USA, Dr. Sapse contacted Dr. M.D. MacFarlane of the University of Southern California, who established a team that performed its own study. Dr. MacFarlane concluded GH3 was a short-acting, selective, fully reversible and competitive monoamine oxidase (MAO) inhibitor. Unlike other antidepressants, GH3 placed no dietary restrictions upon those taking it. Dr. Sapse decided to pursue FDA approval for GH3 as an antidepressant. Phase 1 clinical trials were successfully completed and Phase 2 trials were set to begin when media hype claiming GH3 was "the fountain of youth" alarmed the FDA, who insisted new trials prove these broader claims. Dr. Sapse protested but the FDA were unmoved and the trials ceased.
A double-blind study published in the Journal of the American Geriatrics Society (1975) by Zwerling et al. tested GH3 in hospitalized geriatric patients: the effects of Gerovital H3 (a specially stabilized form of procaine hydrochloride) on geriatric psychiatric patients were assessed in a double-blind study at Bronx State Hospital. The mean age of subjects was 73 years and the average rating for the severity of organic symptoms was "moderate." During the first six weeks, patients were each given a 5 mL injection of either Gerovital or placebo (saline) intramuscularly three times a week; this dosage was doubled to 10 mL per injection during the second six weeks. Nine Gerovital and 10 control subjects completed the first six weeks; and 6 Gerovital and 7 control subjects completed the entire 12-week study. On most measures, variability between subjects was quite large whereas differences between average scores for the two groups were usually small. The overall results of this double-blind study strongly indicated that, among these hospitalized geriatric patients with organic symptoms, Gerovital H3 had no ameliorative effect on either psychological or physiological functioning.
A randomized, placebo-controlled, double-blinded study published in 2016 in Nutrition Journal (Xu et al., Shanghai Jiaotong University) examined oral GH3 tablets: 100 eligible participants were randomly allocated into the GH3 group or the placebo group, administered either GH3 or placebo tablets and were followed up for three months. All participants were required to report their subjective feelings about quality of life, low mood, and anxiety by filling out the Self-Rating Depression Scale (SDS), Self-Rating Anxiety Scale (SAS), and a 36-item Short-Form Health Survey (SF-36 scale). Physicians evaluated related mental health indications through physical examinations at baseline and at the end of the intervention period. Participants were men and women between 50 and 89 years of age, with a median of 62.53 years. After the 12-week intervention, the scores of role-physical (RP), bodily pain (BP), general health (GH), vitality (VT), mental health (MH), health transition (HT), and mental composite score (MCS) of the GH3 group were higher than the placebo group; the scores of SDS and SAS in the GH3 group were both lower than the placebo group. The authors noted this as a preliminary positive signal warranting further investigation; the study's small sample and single-country setting are significant limitations.
Some clinical trials in the mid-to-late 1970s suggested that Gerovital H3 acts as a weak, competitive, reversible MAO inhibitor, and so may have some antidepressant value, but otherwise has a negligible effect on disease.
Summary: Cochrane review finds no credible evidence of benefit; evidence for harm may be stronger than evidence for benefit.
A glaring problem for the demonstration of any benefit associated with Gerovital H3 or similar compounds is the absence of any double-blind, placebo-controlled trials demonstrating a significant improvement in the outcomes that antiaging doctors and entrepreneurs claimed.
The Cochrane review (Malouf and Grimley Evans, 2008) concluded: "This review suggests that the evidence for detrimental effects of procaine and its preparations is stronger than the evidence for benefit in preventing and/or treating dementia or cognitive impairment." There is some evidence from older studies that procaine preparations might improve memory in persons without cognitive impairment. However, the clear evidence of side effects suggests that the risks might outweigh the benefits.
These studies were summarized in that Cochrane Review, which concluded in 2008 that there is no evidence that procaine and its preparations demonstrate a benefit in treating or preventing cognitive impairment or dementia. The reported risks of dizziness, restlessness, migraine headache, and systemic lupus erythematosus outweighed the minimal, if any, benefit.
Summary: Evidence from rigorous trials is negative.
A double-blind study of 88 rehabilitation patients suffering from back or hip disease compared Gerovital with placebo and another procaine preparation. In patients treated with Gerovital or another procaine preparation, no clinical, physiological, or psychological benefits were found in addition to the improvements following rehabilitation compared with placebo treatment. Clinical examination showed that the benefits of rehabilitation were similar in patients receiving Gerovital, another procaine preparation, and placebo.
Summary: Laboratory and in vitro evidence exists; no human clinical evidence from controlled trials.
A study investigated the effects of procaine and of a procaine-based product Gerovital H3 (GH3) on the formation of endogenous and X-ray-induced DNA strand breaks in peripheral blood mononuclear cells (PBMCs) isolated from young and elderly individuals. GH3 showed the strongest radioprotective effects in PBMCs from young subjects, while procaine reduced the endogenous amount of DNA strand breaks more pronouncedly in aged individuals. Both procaine and GH3 inhibited lipid peroxidation, but procaine was more effective in inhibiting mitochondria free radical generation, while GH3 showed a higher antioxidant action on macrophage-induced low-density lipoprotein oxidation. To the best of the authors' knowledge, there were no prior studies reporting on the effect of low doses of procaine on radiation-induced DNA damage in human cells. These findings are in vitro and ex vivo only and have not been validated in human clinical trials.
Summary: Claimed but not substantiated by rigorous independent clinical research.
Preparations containing procaine as a component have also been claimed to benefit serum HDL-C concentrations and decrease triglyceride levels, in addition to protection against cerebral anoxia. These claims are based largely on historical Romanian institutional data and have not been confirmed in independent, placebo-controlled trials of adequate methodological quality. From a review of the scientific evidence, except for a possible antidepressant effect, so far there are no data proving the alleged effects of procaine, and in view of this, the current use of this substance in the treatment of chronic diseases or as an anti-aging drug would not be justified.
In Romania, GH3 is approved by the Romanian equivalent of the FDA for use in the treatment of numerous diseases, including: (1) prevention and treatment of the aging process; (2) depression; (3) arthritis; (4) asthma; (5) gastric and duodenal ulcers; (6) osteoporosis; and many other conditions. These national approvals are not reflected in the regulatory positions of the United States, the European Union, or other major regulatory bodies.
Gerovital H3 is primarily composed of procaine hydrochloride as its active ingredient, formulated as a 2% aqueous solution for injectable administration. The injectable solution approved by the Romanian national authority specifies: commercially available Gerovital H3 (GH3) (Zentiva, Romania — approved by the National Agency of Medicines and Medical Devices according to governmental order no. 1583/2012/01) is an injectable solution containing 2% procaine hydrochloride, 0.12% benzoic acid, 0.10% potassium metabisulphite, 0.01% disodium phosphate, and pH 3.3.
In the Zwerling et al. double-blind hospitalized geriatric trial (1975): patients were each given a 5 mL injection of either Gerovital or placebo (saline) intramuscularly three times a week during the first six weeks of the study; this dosage was doubled to 10 mL per injection during the second six weeks.
In the Shanghai RCT (Xu et al., 2016): 100 eligible participants were randomly allocated into the GH3 group or the placebo group, administered either GH3 or placebo tablets and were followed up for three months. Exact tablet dosage per individual was not specified in the available abstract.
There is no clinical evidence to support specific dosage recommendations for KH3 or other procaine preparations.
Procaine does not get absorbed well when taken by mouth. It is unclear how it might work for medicinal uses when taken orally.
In the United States, the FDA bans Gerovital H3 from interstate commerce as an unapproved drug and, since 1982, has prohibited its importation. As of 2004, the FDA's 1982 automatic detention alert is still in effect and bans the import of Gerovital H3 into the U.S. as "a new drug within the meaning of 201(p), without an approved new drug application [Unapproved New Drug, Section 505(a)]."
Since September 17, 1982, the FDA has banned the importation into or distribution within the United States of Gerovital H3 (also known, according to the FDA, as KH3, GH3, and procaine hydrochloride). This order was rescinded for Gerovital Cosmetics lines not containing procaine.
Gerovital (KH3) and similar products require an approved Abbreviated New Drug Application (ANDA) for legal marketing in the United States.
In the UK, the term "Gerovital H3" was formerly considered to be a trademark registered to Gerovital Cosmetics SA, but the trademark was challenged in 2003 by Societatea Comercială "Farmec" SA and subsequently revoked.
Today, the mainstream medical view is that the preparation was seriously investigated in the 1960s and discredited, and that any promotion today is quackery.
Serious reported side effects of Gerovital injections have included low blood pressure, respiratory difficulties, and convulsions. Procaine can also cause local allergic reactions and a sensation of numbness or heat at the injection site. Allergic reactions to procaine are well-documented.
The reported risks associated with procaine preparations include dizziness, restlessness, migraine headache, and systemic lupus erythematosus.
That Gerovital H3 is a weak, reversible, competitive inhibitor of monoamine oxidase may explain the absence of adverse reactions associated with the clinical use of Gerovital H3 as compared to the severe adverse reactions that have been associated with the use of irreversible monoamine oxidase inhibitors. This pharmacological distinction is considered meaningful from a safety standpoint; however, it does not eliminate the risks associated with procaine itself.
Coadministration with anticholinesterase and anticholinergic agents is a potential contraindication. KH3/Gerovital H3 is contraindicated in patients with known hypersensitivity to the drug.
Clinical trial data are lacking to support use of KH3 or other procaine preparations for depression or age-related diseases. Adverse effects may limit therapeutic applications.
The Cochrane-affiliated review emphasizes the need for pharmacological and toxicological studies on procaine, and the need to carry out in vivo and in vitro safety trials on pharmaceutical preparations containing this substance, in order to prove or disqualify the indications for its use.
The review concluded: "This review suggests that the evidence for detrimental effects of procaine and its preparations is stronger than the evidence for benefit in preventing and/or treating dementia or cognitive impairment. There is some evidence from older studies that procaine preparations might improve memory in persons without cognitive impairment. However, the clear evidence of side effects suggests that the risks might outweigh the benefits." In the light of this, the strong marketing claims for procaine preparations should be withdrawn until trials of adequate size, duration, and quality have been conducted.
With the rise of the web, Gerovital has enjoyed a new lease of promotional life, as it is promoted by many sites with claims of its "cure-all" abilities. A few U.S.-based antiaging and longevity clinics have begun to advertise Gerovital H3 in pill form and as intravenous infusions despite the fact that the FDA banned it in 1982.
As early as 1892, the German chemist Alfred Einhorn began to model on the structural formula of cocaine in order to obtain less-addictive molecules with similar or enhanced anesthetic properties. 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 has demonstrated antioxidant and free radical scavenger action, antiatherogenic effects, antidepressive activity, protection against deleterious effects of ionizing radiations, some positive effects in cases of neoplasia, and some improvement in mental symptoms. Several studies with negative results have also been presented, all with a critical evaluation and analysis.
The weight of current peer-reviewed and regulatory evidence indicates that: (a) a weak, reversible MAO-inhibitory effect is the most pharmacologically substantiated mechanism; (b) this mechanism may produce some mild antidepressant benefit in elderly populations; (c) claims for broader anti-aging, cognitive, cardiovascular, and musculoskeletal benefits are not supported by adequately designed and independently replicated clinical trials; and (d) the regulatory bodies of the United States have banned importation and interstate distribution of the preparation as an unapproved new drug.
Health conditions that Gerovital H3 may help support.
Body systems that Gerovital H3 may help support.
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