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KH-3

Scientific Name(s): 2-diethylaminoethyl 4-aminobenzoate hydrochloride, Procaine hydrochloride
Common Name(s): GeroVita, Gerovital H3, GH-3, KH-3

Clinical Overview

Use

No credible clinical trial data exist to support the use of KH-3 or other procaine preparations in inhibiting diseases of aging or antidepressant activity. Adverse effects may limit therapeutic applications. Gerovital (KH-3) and similar products require an approved Abbreviated New Drug Application (ANDA) for legal marketing.

Dosing

There is no clinical evidence to support specific dosage recommendations for KH-3 or other procaine preparations..

Contraindications

KH-3 is contraindicated in patients with myasthenia gravis (ie, progressive muscular weakness) and systemic lupus erythematosus (theoretical risk of this condition being induced by procainamide).1, 2 KH-3 may antagonize the antibacterial effect of sulfonamides through para-aminobenzoic acid competition. Prolonged neuromuscular blockade may occur with concurrent use of KH-3 with succinylcholine. KH-3 is potentially contraindicated in patients taking anticholinesterase and anticholinergic agents.2 KH-3 is contraindicated in patients with known hypersensitivity to the drug. Furthermore, because of the lack of clinical trial data, KH-3 should not be used during pregnancy.

Pregnancy/Lactation

Information regarding safety and efficacy in pregnancy and lactation is lacking. Avoid use.

Interactions

None well documented.

Adverse Reactions

Reports have described heartburn, restlessness, dizziness, migraine, and systemic lupus erythematosus following treatment with KH-3. KH-3 is contraindicated in patients with known hypersensitivity to the drug.

Toxicology

No data.

History

Although procaine HCl is a pure synthetic drug, its use as one of the active ingredients in KH-3 is marketed by many commercial Web sites as a "natural" approach to reversing or delaying the aging process. KH-3 was developed in Germany in the 1960s and was popularized by Romanian and other Eastern European researchers.3 Gerovital (KH-3) and similar products require an approved Abbreviated New Drug Application (ANDA) for legal marketing.9

These products have been administered parenterally and orally for their effect on the overall aging process and for the treatment of cerebral atherosclerosis, progressive dementia, arthritis, hair loss, hypertension, and sexual dysfunction.

Chemistry

Preparations are based primarily on the pharmacologic effects of procaine HCl and are often marketed as mixtures of procaine, buffers (eg, benzoic acid, potassium metabisulfate), analgesics, and nutritional supplements.1 One preparation from Germany contains procaine, hematoporphyrin to aid absorption of procaine, magnesium carbonate, sodium hydrogen phosphate, potassium HCl, and other compounds. Most products contain approximately 2% procaine HCl. Studies have shown that the biotrophic treatment with Gerovital H3 has a strong influence on glucose-6-phosphate dehydrogenase with a tendency to diminish the thermolabile fractions.4

A "G.H.3." product was used in a clinical study; however, it did not contain any protamine, and instead contained a number of vitamins and minerals in combination with St. John’s wort, Ginkgo biloba, glutathione, and dimethylaminoethanol.12

Uses and Pharmacology

Procaine has been used for decades as a local anesthetic and antiarrhythmic. The compound has a number of pharmacologic characteristics, including an ability to decrease membrane excitability and alter membrane ionic transmission. Procaine is hydrolyzed rapidly to inactive compounds by plasma enzymes.1 Procaine is poorly absorbed and quickly metabolized following oral administration; therefore, it is primarily used by injection. Hematoporphyrin is added to some oral preparations and is said to inhibit intestinal hydrolysis of procaine. There is no evidence that pharmacologic levels of procaine are attained in the brain or other target organs following oral administration of KH-3 or other products.

Diseases of aging

Numerous studies also have been conducted to evaluate the efficacy of procaine HCl or commercially available mixtures of this compound for the treatment of elderly patients with a variety or organic diseases.5

Animal data

Research reveals no animal data regarding the use of KH-3 for diseases of aging.

Clinical data

The effect of Gerovital H3 on psychologic and physiologic functions was assessed on geriatric patients (mean age, 73) in a placebo-controlled, double-blind study. Patients received either a 5 mL injection or placebo IM 3 times/week for the first 6 weeks. The dose was doubled to 10 mL per injection during the second 6 weeks. Objective rating scales included interpersonal functioning, cognitive ability, psychiatric symptoms, and urine and blood chemical findings. The study results indicated that Gerovital H3 had no ameliorative effect on either psychologic or physiologic functioning.6

The results have been conflicting but generally indicate these compounds are ineffective in the treatment of any disease. As early as 1977, a comprehensive review of the use of procaine in over 100,000 patients found no evidence for its efficacy.7 Further reviews continue to find no scientific evidence to suggest an effect of procaine on aging.1, 10

CNS effects

Although controversial, some authors suggest that procaine may act as an inhibitor of monoamine oxidase, thereby relieving depression.5

Animal data

Research reveals no animal data regarding the use of KH-3 for antidepressant effects.

Clinical data

A Cochrane review of the efficacy of procaine in cognitive decline and dementia found 3 clinical trials meeting inclusion criteria. Pooled data from 2 studies (N=415) showed procaine had a detrimental effect in terms of side effects (20/208 active versus 3/207 placebo; OR 7.30; 95% confidence interval [CI] 2.13 to 25; P = 0.002). A positive effect on cognition was suggested in 2 older studies; however, a meta-analysis could not be performed due to the use of different preparations.11

Anticholesterol effects

Reports of the effect of procaine on blood cholesterol levels are inconsistent, with some studies showing a reduction in cholesterol and others showing little beneficial effect.8

Dosing

Procaine HCl is generally contraindicated in patients with known hypersensitivity to the drug or related compounds.

Pregnancy / Lactation

Because of the lack of clinical trial data, procaine HCl should not be used during pregnancy.

Interactions

The drug should not be administered to patients taking concurrent anticholinesterase medications (eg, neostigmine). Procaine may inhibit the bacteriostatic action of sulfonamides.1

Adverse Reactions

Reports have described heartburn, restlessness, dizziness, migraine, and systemic lupus erythematosus following treatment with KH-3.1, 11

Toxicology

Research reveals little or no information regarding toxicology with the use of this product.

References

1. Brodaty H. Rejuvenation with KH-3. New Ethicals J. February, 1990;11.
2. McEvoy GK, ed. AHFS Drug Administration. Bethesda, MD: American Society of Health-System Pharmacists Inc.; 2003.
3. Kent S. A look at Gerovital—the "youth" drug. Geriatrics. 1976;31:95-96,101-102.1001903
4. MacFarlane MD. Procaine HCl (Gerovital H3): a weak, reversible, fully competitive inhibitor of monoamine oxidase. Fed Proc. 1975;34:108-110.1109354
5. Orgogozo JM, Spiegel R. Critical review of clinical trials in senile dementia I. Postgrad Med J. 1987;63:237-240.2891126
6. Zwerling I, Plutchik R, Hotz M, et al. Effects of a procaine preparation (Gerovital H3) in hospitalized geriatric patients: a double-blind study. J Am Geriatr Soc. 1975;23:355-359.1097490
7. Ostfeld A, Smith CM, Stotsky BA. The systemic use of procaine in the treatment of the elderly: a review. J Am Geriatr Soc. 1977;25:1-19.12204
8. Jarvik LF, Milne JF. Gerovital-H3 —a review of the literature. Psychopharmacol Bull. 1975;11:51-53.717
9. FDA Import Alert. IA #61–01: Automatic detention for Gerovital, also known as KH3, GH3, Procaine Hydrochloride (HCL), Trofibial H3, Aslavital, Zell H3 [on-line]. Available at http://www.accessdata.fda.gov/cms_ia/importalert_163.html Published September 9, 2009. Accessed December 21, 2016.
10. Perls T. The reappearance of procaine hydrochloride (Gerovital H3) for antiaging. J Am Geriatr Soc. 2013;61(6):1024-5.23772727
11. Szatmári S, Bereczki D. Procaine treatments for cognition and dementia. Cochrane Database Syst Rev. 2008;(4):CD005993.18843698
12. Xu G, Cao Z, Shariff M, et al. Effects of G.H.3. On mental symptoms and health-related quality of life among older adults: results of a three-month follow-Up study in Shanghai, China. Nutr J. 2016;15:9.26813677

Disclaimer

This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.

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