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GH3: Procaine Hydrochloride

by Conrad S Myers Ph.D.(more info)

listed in ageing, originally published in issue 31 - August 1998

As we age an inevitable decline in our physical and mental health occurs. We all fear these debilitating aspects to ageing and strive to avoid them through controlled diet, exercise and taking of nutritional supplements. Many beneficial supplements are already commonly used with more constantly appearing, but beneficial supplements exist which seem to be forgotten.

A highly beneficial supplement for people of any age, but especially those of middle-age and older, has existed for nearly 50 years. Largely unknown it has become neglected and left to gather dust in nutritional archives. This supplement is called GH3.

My interest in GH3 began over three years ago, when I read a book called "The Fountain of Youth." It was fascinating and made remarkable claims for a nutrient of which neither I, nor anyone I asked, had heard. Though not a medical or health professional, I decided to discover more about GH3. This research has proved enlightening and the following passages provide a summary of just part of my discoveries about GH3.

The development of GH3

Procaine Hydrochloride, the active ingredient of GH3, was first synthesised in 1905, by biochemist Dr Alfred Einhorn as a local anaesthetic. It is still used by dentists, especially in the USA where it is known as Novocain.

Despite reports of beneficial side-effects in patients given procaine, research into therapeutic uses did not begin until the 1920s. Papers soon appeared in medical journals indicating direct injection, into joints and muscles, could benefit people suffering from a range of ailments.[1] Having read this research Dr Ana Aslan, director of The Romanian National Institute of Gerontology and Geriatrics, decided to investigate.

Dr Aslan's first experiments in 1949, produced positive results. However, she discovered the enzyme cholinesterase degraded procaine within an hour requiring frequent injections to produce benefits.[2]

Having decided to improve procaine for therapeutic use, in 1951 the product of this research was perfected and named Gerovital H3 (GH3).[3] Adding stabilising agents meant the anaesthetic properties of procaine were removed and allowed GH3 to remain stable for at least six hours.[4]

Immediate experiments began and in 1954 preliminary results were published in The Journal of The Romanian Academy of Science. Dr Aslan presented her findings at the Karlsruhe Therapy Congress in 1956, asserting GH3 was an important discovery for treating degenerative ailments. This conclusion was initially rejected. After further research, Dr Aslan returned to Karlsruhe in 1957 and her revised work received a warm response.

Regardless of this research, health professionals remained sceptical of the claims for GH3. A denouncement was published in the Journal of The American Medical Association, 1963,[5] concluding GH3 was harmless but of little use.

This contradicted research from Europe. A team from the Chicago Medical Institute for Medical Research attempted to resolve this dispute in 1965. Their investigation accounted for negative results due to investigators failing to use GH3. This was emphasised by results the Chicago team obtained using GH3, fully supporting the claims of Dr Aslan.[6]

Despite thousands of studies into GH3 having been conducted, the vast majority of them supporting Dr Aslan's initial claims, only those demonstrating a low efficacy have received publicity. Past Romanian governments have not helped, rarely allowing GH3 to be exported and not making more information available. The result has been continued poor press for GH3 leading to its neglect.

What GH3 is and how it works

Procaine hydrochloride, the main active ingredient of GH3, is created by combining two, water soluble B-vitamins: para-amino benzoic acid (PABA) and diethylaminoethanol (DEAE). Both are found within the body and are important for good health.

Though PABA and DEAE can be taken separately, they are not readily absorbed since both carry an electrical charge. When combined into a procaine molecule, PABA and DEAE become ionised and are readily absorbed by the body.[7]

The basic ingredients of a GH3 formulation are, in descending order; procaine hydrochloride, ascorbic acid, citric acid, benzoic acid, potassium metabisulphite and disodium phosphate. All substances in GH3, other than procaine hydrochloride, are primarily employed as buffering and stabilising agents, though benefits have been attributed to them.

Interviews with biochemists and laboratory pharmacists have stressed the GH3 formula and correct formulation are essential for it to have any beneficial effect.

Adding three organic acids with procaine hydrochloride creates a complex. This reputedly protects the procaine from premature hydrolysis, by raising the pH level to a mildly acidic 3.3.[8] Inclusion of organic acids enables the procaine molecule to cross cell membranes,[9] which it cannot otherwise do.

Once across the cell membrane, the procaine molecule hydrolyses back into PABA and DEAE where they appear to nourish cells from within.[10] The functions performed are no different from those already attributed to these vitamins. It is the ability to enter cells which appears to allow PABA and DEAE to provide greater benefits than usually experienced.

The stabilising agents, once released from the complex, also perform important functions at the cellular level. During formulation, benzoic acid reacts with other stabilising agents to create a harmless substance which acts as an antioxidant.[11] Potassium metabisulphite separates into its constituents; the metabisulphite enters the bloodstream and acts as a cleansing agent; while potassium is used to produce neurotransmitters for the brain and central nervous system.[12]

The metabolic pathways of GH3 - chart

Medical research on GH3

The most famous study of GH3, by Dr Aslan, began in 1956. It involved over 15,000 Romanians, of varying ages, health status and employment types, selected from 144 clinics throughout Romania.

Only half received GH3, but all were given extensive medical attention, including vitamin injections. Within two years, results showed all receiving GH3 suffered significantly fewer episodes of illness, regardless of age or initial health status. It was also found many previously suffering health problems had these conditions either stabilised or improved.

The results impressed the Romanian government who funded administration of GH3 to all persons of working age.

In 1970 Dr Alfred Sapse renewed interest in GH3. While serving his internship in Romania, Dr Sapse met those treated by Dr Aslan, and was able to study the research documents.

When asked why he decided to revive interest in GH3, Dr Sapse, referring to Dr Aslan's patients, replied "Their ailments were either gone or greatly regressed, at least to the point where they did not bother these old people. I know what I saw… it was incredible."[13]

Upon returning to the USA, Dr Sapse contacted Dr M D MacFarlane of the University of Southern California, who established a team which performed its own study. Dr MacFarlane concluded GH3 was a short-acting, selective, fully reversible and competitive monoamine oxidase (MAO) inhibitor.[14] Unlike other anti-depressants GH3 placed no dietary restrictions upon those taking it.

Dr Sapse decided to pursue FDA approval for GH3 as an anti-depressant. Phase 1 clinical trials were successfully completed and Phase 2 trials set to begin when media hype, claiming GH3 was "the fountain of youth", alarmed the FDA who insisted new trials prove these claims. Dr Sapse protested but the FDA were unmoved and the trials ceased.

The work was not wasted, inspiring further investigation into GH3 as an anti-depressant. Dr Yau of Ohio Mental Health and Mental Retardation Centre, Cleveland, found GH3 had four major actions as an anti-depressant,[15] supporting and expanding on the findings of Dr MacFarlane.

GH3 proved to be a weak, reversible and competitive MAO inhibitor; it operates as an anti-depressant by regulating MAO levels; MAO regulation only occurs in the brain; finally, GH3 is selective when inhibiting the oxidative deanimation of other important brain monoamines such as serotonin.[16]

At Duke University Medical Centre, USA Dr Zung conducted a double-blind study on patients aged between 61 and 77.[17] A control group received a saline solution; while test cases were given either GH3 or Imipramine.

In his conclusions Dr Zung stated "…using the Clinical Global Impression and Zung Self Depression Scales, the change scores obtained from calculating pre-treatment and post-treatment differences showed GH3 to be superior to Imipramine, since the GH3/placebo differences were significantly different, while the Imipramine/placebo differences were not."[18]

Further support for GH3 as a treatment for mental disorders was provided by Dr L. Bucci of Rockland State Hospital, New York and Dr J.C. Saunders of Columbia University College of Physicians and Surgeons, who demonstrated the positive effects of GH3 administered to aged and psychotic patients.[19]

The research of Dr Marangoni, Chief of Medicine, Flower Hospital, New York is worth noting. Dr Marangoni found both procaine therapy and GH3 highly effective in treating paroxysmal supraventricular tachycardia, anterial fibrillation and complete heart block.[20]

Dr P. Luth of the Municipal Hospital Offenbach/Main, Germany has conducted extensive research using GH3 over many years. By directly injecting GH3 into geriatric patients, Dr Luth has noted the dramatic change in appearance and behaviour of those he has treated. Dramatic improvements in skin conditions, sleep patterns, blood pressure and heart arrhythmia have proved common in those receiving GH3.[21]

The claims for GH3

GH3 is regarded as a nutritional supplement with implied medicinal value. It has never gained approval as a medicine, but is officially listed in the Merck Index as Vitamin H3.[22]

As a nutrient the action of GH3 cannot be predicted for everyone. This general nature of operation is emphasised by GH3 functioning at the cellular level, with benefits being subtle and occurring over extended periods. Some people experience almost immediate benefits, but others may have to take GH3 for a year or more for any gain.

Despite these factors, clinical trials have established the following as benefits of GH3:
– GH3 is a potent anti-depressant and brain tonic
– GH3 can arrest or reverse the symptoms of ageing including hair loss and greying, and the wrinkling and hardening of skin.[23]

Dr Aslan never claimed GH3 could extend life, though she believed it capable of extending quality of life. The ability to restore hair and skin to a former youthful state is significant and can prove important to an individual. Of greater importance is GH3's ability to improve mental functioning and general well-being of anyone at any age, most significantly after age 45.

It is known levels of MAO increase within the brain from the age of 45, though it can occur earlier due to poor health. Excess MAO can cause depression and impair higher mental functions. By removing excess MAO, GH3 reduces the chance of depression developing. A healthy and correctly functioning endocrine system is important for maintaining bodily health. The prevention of excess MAO from interfering with the production and operation of important hormones and neurotransmitters, which occurs as people age, enables the body to maintain its own good health.

GH3 is recognised as a pro-vitamin, stimulating the body to produce vitamins, besides directly providing the B-vitamins PABA and DEAE. Use of GH3 stimulates production of vitamin K, folic acid, choline, acetylcholine and thiamine. This pro-vitamin action is important as people age, assisting their body's in a vital activity for health maintenance it may not otherwise perform effectively.

Conclusion

GH3 is not the "fountain of youth" but the data I have unearthed, both medical research and personal experiences, would suggest it is a supplement that has been unfairly ignored.

The basics of GH3 are simple, probably too simple for many to believe the affect many credit it with. Surely two well known B-vitamins, already available and widely used, cannot produce such startling results simply by being combined? There is strong clinical evidence to suggest the answer to this question is "yes."

Perhaps the biggest factor operating against GH3 is its history. Originally developed by a medical doctor as a therapeutic treatment and subjected to clinical medical trials, GH3 has been more accurately re-designated a nutritional supplement with medicinal benefits. Unfortunately, this has resulted in GH3 falling between the medical and nutritional camps, with neither readily accepting it.

It has been my intention to present a balanced account of GH3. Hopefully, this has been achieved by presenting the facts, for readers to become informed and draw their own conclusions.

Case Studies

Comments from people currently using GH3 are informative when wishing to assess its effect. The three people I quote below are of different ages and have varying health status.

Andy is aged 24 and has suffered from ME for the past 4 years. He was gradually going blind, "white blind" as he described it, though his eyesight has improved. It has been his decision to spend long periods each day in bed, but Andy says "this has enabled me to do some things during the day."

For the past 3 years Andy has taken GH3 and believes it has been of benefit, though he does not regard it as a cure for his ME. "I do believe GH3 is a very good anti-depressant and has helped keep me cheerful" said Andy and added "it seems to have a major effect as a psycho-stimulant. Only 20 minutes after taking GH3, I can feel the blood flowing to the brain. It's like pins and needles in my head. This is a very clear and positive reaction."

Mrs Worsted has been taking GH3 for a number of years. The effect she believes it has had for her and her family, who now all take GH3, may not seem amazing but have made them happier people.

After only a few months of taking it, her husband's Naturopath commented to him "You look younger than when I saw you two months ago." Mrs Worsted says, "my family, including myself and my husband, are all feeling benefits in various ways such as sleeping better, depression lifted, skin looking smoother and younger and generally feeling better all round."

Mike is 57 and runs a successful health and nutrition shop. He only discovered GH3 when he started stocking it in December 1997. Mike decided to try it and experienced a remarkable change.

"For a month I had had a pain down my left side, some kind of muscle tension. An osteopath/chiropractor I had seen suggested exercise, but this only made the pain worse. I could not even tie my shoe-laces." said Mike, but after only 3 days of taking GH3 Mike found the pain was going.

"I did not immediately put it down to the GH3" he says "especially since I was not taking the full recommended dose. Then I went to the full dose and within a week not only had the pain gone in my side, but a pain I had suffered for 18 months in my neck was completely gone."

Mike now takes GH3 only 2 or 3 times a week but still feels benefits. "My energy levels are up and I am more cheerful. I am a definite convert," he says.

References

1. Longbrook, Michael; The Development Uses & Future Of Gerovital H3, For Physicians, A Summary Into The Nutrient Qualities Of Procaine; page 1.
2. Longbrook, Michael; ibid; pages 1 – 2.
3. Mann, J A; Harbor Publishing, 1980; Secrets Of Life Extension; Chapter 10.
4. Mann, J A; ibid; Chapter 10.
5. Mann, J A; ibid; Chapter 10.
6. Longbrook, Michael; ibid; page 3.
7. Longbrook, Michael; ibid; pages 3 – 4.
8. Hoffer, Abram & Walker, Morton; 1980; Nutrients To Age Without Senility; Chapter 10.
9. Longbrook, Michael; ibid;
10. Longbrook, Michael; ibid; page 4.
11. Hoffer, A & Walker, M; ibid; Chapter 10.
12. MacFarlane, M D; Journal Of The American Geriatric Society 22:8, 1974; Procaine (Gerovital H3) therapy: Mechanism Of Inhibition Of Monoamine Oxidase.
13. MacFarlane, MD; ibid.
14. Yau, T M; Theoretical Aspects Of Ageing, New York, Academic Press Inc., 1974.
15. Yau, T M; ibid.
16. Zung, W W K; Gianturco, D; Pfeiffer, E; et al; Psychopharmocology Bulletin, 2(12), April, 1976; Treatment of Depression in the Aged With Gerovital H3: Clinical Efficacy & Neurophysiological Effects; pages 50 – 51.
17. Zunge, W W K, et al; ibid.
18. Hoffer, A & Walker, M; ibid; Chapter 10.
19. Hoffer, A & Walker, M; ibid; Chapter 10.
20. Kent, S; Geriatrics, 31(12): December 1976; A Look At Gerovital – The "Youth" Drug; pages 101 – 102.
21. Hoffer, A & Walker, M; ibid; Chapter 10.
22. Longbrook, M; ibid.
23. Kent, S; ibid.

Further Reading

Leslie Kenton; The New Ultra Health; Chapter 17.
Herbert Bailey; GH3 – Will It Keep You Young Longer?; Bantam Books, NewYork. This book is now out of print, but is the finest book on GH3 and worth trying to find.
Dr Mitchell Kurk & Dr Morton Walker; Prescription For Long Life; Avery Publishing Group, USA. It is available from selected health shops and nutritional suppliers in the UK.

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About Conrad S Myers Ph.D.

Conrad S. Myers is a freelance writer and researcher. He has a degree in Sociology, specialising in health and society, global health issues and epidemiology, and a Ph.D. in Religion and Science. For more than three years he has conducted private research into all aspects of GH3, including its history and usage. For further details regarding GH3, or any other aspect of his work, Conrad Myers can be contacted by telephone on 01705 340177 or by e-mail at cmyers@clara.net.co.uk

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