KH-3

Scientific Name(s):Procaine HCl, 2-diethylaminoethyl 4-aminobenzoate hydrochloride

Common Name(s): KH-3 , Gerovital H3 , GH-3 , GeroVita

Uses

Without much supporting clinical trial data, KH-3 has been credited with inhibiting diseases of aging and may have antidepressant activity.

Dosing

There is no clinical evidence to support specific dosage recommendations for KH-3. Although not supported by clinical trial data, dosage regimens marketed by commercial Web sites include: (a) 100 to 200 mg capsule daily by mouth; (b) 100 to 200 mg capsule daily by mouth for 1 month, then no drug for 1 week, then repeat the cycle.

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

Published reports have described heartburn, migraine, and systemic lupus erythematosus. 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 Procaine-containing products are available over-the-counter and by mail order in the US and parts of Europe.

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

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 Of 8 studies published prior to 1980, 6 found no effect. 1

Antidepressant activity

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

One study found slight mood improvement in depressed elderly patients. 1 Although a slight antidepressant activity was considered possible in 1 study, 7 it was suggested this may have accounted for the occasional reports of improvement in complaints related to the musculoskeletal, cardiovascular, and GI symptoms.

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

Dosage

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, migraine, and systemic lupus erythematosus following treatment with KH-3. No adverse events have been reported in other studies. 1

Toxicology

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

Bibliography

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.
4. MacFarlane MD. Procaine HCl ( Gerovital H3 ): a weak, reversible, fully competitive inhibitor of monoamine oxidase. Fed Proc . 1975;34:108-110.
5. Orgogozo JM, Spiegel R. Critical review of clinical trials in senile dementia I. Postgrad Med J . 1987;63:237-240.
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.
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.
8. Jarvik LF, Milne JF. Gerovital-H3 —a review of the literature. Psychopharmacol Bull . 1975;11:51-53.

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