(by James South, MA)

Gerovital (GH3) is the grandmother of modern anti-aging drugs. Since it was first introduced to the western world in the early 1950’s by its inventor, Rumanian gerontologist Dr. Ana Aslan. GH3 has been the subject of both intense marketing hype and glamor, as well as heated scientific controversy.

The marketing hype has been in part fueled by the glamor attached to GH3’s many famous users. Celebrity columnists reported regulars at Dr. Aslan’s Rumanian clinic during the 1950’s and 1960’s, such as German Chancellor Konrad Adenaner, Winston Churchill, Bob Hope, Cary Grant, Marilyn Monroe, Jack Benny and Prince Rainer, among other “glitterati”. The scientific controversy surrounding GH3 has stemmed in part through confusion and disagreement regarding both the chemical identity of GH3 as well as its mechanism of action.

 

GH3 – PROCAINE AND STABILIZERS

Dr. Aslan defined GH3 as procaine (the famous dental anaesthetic) stabilized with small amounts of benzoic acid, potassium metabisulfate and disodium phosphate. Yet the various scientific detractors of GH3, none of whom had any clinical experience using GH3, claimed that the “stabilizers” were irrelevant and unnecessary.

On that basis, they performed various small scale, short term experiments using procaine alone, which, (surprise!) failed to confirm Aslan’s GH3 rejuvenation effects, and then they claimed that this proved Aslan’s thousands of patient years of clinical experience and multi faceted success using GH3 to be fraud, delusion, quackery or mere placebo effect generated through the attention received by lonely and bored “oldsters” during Aslan’s GH3 treatments.

It should be noted that this is a standard method used by the medical establishment to “refute” claims they consider heresy. For example, during the 1970’s Linus Pauling and Dr. Ewan Cameron had many clinical successes treating cancer with mega-doses of vitamin C. Based on their clinical experience, they noted that the therapy only worked reliably on patients whose immune system had not been damaged by Chemotherapy or radiation therapy. The (infamous Mayo Clinic then ran trials using mega dose C with cancer patients all of whom had received Chemo and or X-ray treatment and found (surprise!) the “Pauling method” (which they did not follow) didn’t work.

In the 1970’s the (infamous Sloan Kettering Cancer Hospital ran trials to test the cancer remedy Laetrile, significantly deviating from the carefully documented and published protocols followed by clinicians successful with Laetrile, and (surprise!) found Laetrile “didn’t work”. Also recently a trial by detractors of the Candida yeast syndrome using only the anti fungal drug Nystatin failed to find patient benefit while (surprise!) totally ignoring the need to accompany the drug with a low sugar diet (to starve the yeast) as is routinely done by doctors successfully treating Candida patients.

 

GH3 AND KH3 – WHAT’S THE DIFFERENCE?

Indirect support for Aslan’s claim that procaine requires stabilizers for clinical efficacy ironically was provided through research on the German drug “knock off” of GH3-KH3.

KH3 is procaine at one half the dose of GH3, stabilized with a tiny amount of hematoporphyrin (HP). HP is simply hemoglobin minus its protein and iron.

Studies with KH3 carried out in 1979 by D. Hegner at the Munich Institute for Pharmacology, Toxicology and Pharmacy and by L. Tirri at the Chemistry Department, University of Nevada in Las Vegas, did in fact find the HP to be a successful stabilizer of procaine, making it more effective.

 

THE REAL McCOYS!

The stability issue derives in part from the fact that under some conditions procaine hydrolyzes in solution into diethylaminoethanol (DHEA – a close cousin of DMAE) and the “B vitamin” para-aminobenzoic acid (PABA). It has been claimed by both supports and opponents of GH3 that it is these two constituents that (allegedly) provide the “benefit” of GH3. Because DEAE is so similar to DMAE, and may even be metabolized into it in the body, there have been many “pseudo GH3’s” sold in health food stores which are nothing but physical mixtures of DMAE and PABA. Yet GH3/KH3 have been shown to have similar properties possessed by neither DMAE or PABA.

One of the most important benefits of GH3 may derive from its role as a weak, reversible monoamine oxidase inhibitor (MAOI). MAO is an enzyme in the brain that increases substantially with age. MAO’s degrade key brain neurotransmitters, especially noradrenalin (AKA – norepinephrine), dopamine and serotonin.

As a consequence, brain levels of these neurotransmitters tend to diminish with age, with concomitant loss of key brain functions (memory, attention span, drive, hormone regulation etc.) and an increase in depression.

 

GH3 – REVERSIBLE MAOI

In the late 1960’s famed University of California gerontologist Dr. Joseph Hrachovac reported that GH3 could significantly lower brain MAO activity. And M.D. MacFarlane reported in the prestigious journal Federation Proceedings in 1975 that GH3 was a “weak, reversible, fully competitive inhibitor of MAO.”

GH3’s ability to serve as a weak, reversible MAOI is extremely important. The original pharmaceutical antidepressants were MAOIs, but they soon fell into disuse due to serious, even lethal side effects. These pharmaceutical MAOIs were strong, irreversible MAOIs. As a consequence they could lead to the phenomenon called the “cheese effect,” whereby consuming certain foods and beverages rich in the amino acid derivative thyramine, while taking prescription MAOIs could lead to severe high blood pressure crises, even fatal strokes. Because GH3/KH3 are weak, reversible MAOIs, they do not exhibit this dangerous side effect.

 

GH3 – THE CLINICAL TRIALS AND ANTI-AGING USES

Several clinical studies published in the journal Psychosonmatics in 1974 verified the clinical effectiveness of GH3 as an anti-depressant. W.K. Zung of Duke University reported GH3 to be more effective than the standard anti-depressant Imipramine, while Cohen and Ditman reported that most patients receiving GH3 “felt a greater sense of well being and relaxation, slept better at night and many obtained some relief from depression and the discomforts of chronic inflammation or degenerative disease.” And researchers M.R. Hall and colleagues noted in the journal Age and Aging in 1983, based on a trial with 247 healthy elderly subjects taking KH3 over 2 years, that “the results of this trial suggest that KH3 is an active substance…earlier work on procaine claimed that it improved recall, increased psychomotor activity and muscle strength in the elderly. We were surprised to substantiate these finding.

It should be noted that by increasing brain serotonin, a MAOI would improve sleep; by increasing brain noradrenalin a MAOI would increase memory and attention; and a MAOI induced increase in dopamine would increase psychomotor activity and muscle strength.

Another report from Vienna in 1970, a 5 month trial of KH3 in 120 people with an additional 112 receiving placebo, found that the KH3 group had a better memory for numbers, felt more alert and had superb concentration and hand – eye coordination, according to W. Czerwenka in the Vienna Medical Weekly Journal.

Other GH3/KH3 benefits reported in journals over the years include stabilizing brain cell membranes in ways that reverse “normal” age related membrane deterioration; increasing general intracellular metabolic rate, especially in muscle cells; and increasing intra cellular DNA levels necessary for optimal regeneration and repair of age induced cellular “wear and tear”.

 

GH3 – THE ULTIMATE YET UNKNOWN BENEFITS?!

Yet what may turn out to be the most important anti-aging benefit of GH3/KH3, as well as the root of its diverse clinical benefits ranging from decreasing hypertension, to improving memory, to reducing insomnia, to minimize stress, fatigue, depression and wrinkles; is generally unknown, even to many of GH3’s most ardent supporters!

I first learned of this important function of GH3 in 1984, from an obscure paper by Alfred Sapse in the generally ignored journal Medical Hypotheses: Stress, Cortisol, Interferon and Stress Diseases.

In this landmark 14 page paper with 62 references, Sapse made the case that cortisol, the “state of siege” hormone secreted by the adrenal glands, could all by itself cause a host of the common mental and physical problems related to stress, aging and degenerative disease.

In more recent years, the central role of cortisol in promoting degenerative disease and aging has been expounded by Dilman and Dean in their magnum opus The Neuroendocrine Theory of Aging and Degenerative Disease and world famous stress researcher Robert Sapolsky in his scientific papers and the book Why Zebras Don’t Get Ulcers; and most recently as a key theme of the 1997 book Brain Longevity by D.S. Khalsa (Warner Books).

Over a lifetime cortisol damages the brain, muscle, bone, skin and the immune system. A key regulatory center of the brain, the hippocampus, may gradually lose 20% of its cells due to its unique sensitivity to cortisol damage.

The hippocampus, a mid brain structure strategically seated above the hypothalamus/pituitary gland and below the cerebral cortex, plays a crucial role in cognition, attention, memory, emotional stability and sensory integration. It also plays a major role in regulating the hypothalamic – pituitary axis, which in turn regulates the entire endocrine (glandular) system of the human body.

The hippocampus is ravenged in Alzheimer’s dementia and is damaged to a lessor extent in “normal” aging. Ironically, it has been discovered that as the hippocampus is more and more damaged through a lifetime of stress induced cortisol secretion, the hippocampus loses its ability to regulate cortisol secretion. This in turn allows ever higher average cortisol levels, leading to a vicious spiral of ever less hippocampal cortisol control and ever more elevated chronic cortisol levels. Anything which safely and effectively protects the structure, function, health and stability of the hippocampus is at the core of promoting a healthy and vibrant middle and old age.

To my knowledge it was Sapse in his 1984 paper who first compiled a list of substances which protect our bodies and brains from the ravages of stress induced cortisol excess. His short list included Dilantin (Phenytoin), vitamin C, salicylates (aspirin, although copper salicylate is a better form in small [2-3 mg copper] doses), and Gerovital, GH3!

In his chapter on GH3, in Mind Food and Smart Pills, Ross Pelton lists a host of ailments, problems and diseases claimed to be cured or helped by GH3. Over half of Pelton’s list, including senility, wrinkling skin, stress, depression, fatigue, poor memory, hypertension, sexual impotence (loss of desire), insomnia, heart disease, hormonal deficiencies (cortisol opposes, for example many of the benefits of insulin, testosterone, growth hormone and thymic hormones), Alzheimer’s disease and headache, are among the many ill effects of excess cortisol cited by Sapse.

Thus, the confusion and scepticism of many researchers as to how simple procaine, even if it is an effective MAOI, could lead to such a broad and seemingly unrelated host of benefits for body and mind, is now resolved. It is through GH3/KH3’s antagonism of the broad spectrum degenerative effects of stress induced chronic cortisol excess, so common in the modern world, that GH3/KH3 can claim to be not just the original but also still one of the most important anti-aging drugs. And this is why it’s one of the cornerstones of my personal anti-aging program.

 

GH3 – THE DOSE AND CAUTIONS

The traditional program for GH3 is to take one GH3 (or two KH3) once or twice daily on an empty stomach. Those who find it too stimulating should use a lesser dose and/or not take it later than early afternoon. Due to its MAOI effect, GH3/KH3 energizing tendency may make it necessary to take a periodic “holiday” from use, the original protocol was 5 days off each month.

GH3/KH3 may also amplify the stimulating effect of other “neuro-energizers” which increase dopamine and/or noradrenalin activity, such as deprenyl, L-dopa, modafinil (adrafinil), Hydergine or DLPA/phenylalanine/tyrosine. It is especially important to take periodic GH3 breaks if you are using such “neuro-energizers.”

Those known or suspected to be procaine allergic should avoid GH3/KH3. People with cortisol deficiency problems or who are using medically prescribed cortisol or prednisone therapy should use GH3/KH3 cautiously if at all. Those using psychiatric drugs, such as tranquilizers, anti-epileptics, anti-depressants etc., should also be wary of using GH3/KH3.

 

GH3 – TMI COMMENTS

It has been the experience of TMI that two major factors are involved when choosing a GH3/KH3 supplement and this is borne out with another of James South’s excellent articles.

Firstly, use only those supplements made with real procaine, either original-formula Gerovital H3 with 100 mgs of procaine per tablet, or the KH3 capsules made by Schwarzhaupt of Germany. (Ask for our specialty order form for current prices of true KH3 from Schwarzhaupt).

Secondly, don’t expect instant results, both GH3 and KH3 are best when utilized over a few months and certainly several weeks. We consider GH3/KH3 to be an excellent long term use anti-aging product, the cost effectiveness and long term usage of GH3/KH3 means that its ease of accessibility is wide-spread.

Accept no substitutes for Original-Formula GH3 with procaine. No matter what the hype, there is no way to create the effects of procaine by combining DMAE and PABA or whatever they try. Use the Original; use TMI’s GH3.