KH-3

Brand names: 2-diethylaminoethyl 4-aminobenzoate Hydrochloride, GeroVita, Gerovital H3, GH-3, KH-3, Procaine Hydrochloride

Usage of KH-3

Procaine has been used for decades as a local anesthetic and antiarrhythmic. The compound has several pharmacologic characteristics, including an ability to decrease membrane excitability and alter membrane ionic transmission. Procaine is hydrolyzed rapidly to inactive compounds by plasma enzymes.(Brodaty 1990)

Cholesterol

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.(Jarvik 1975)

CNS effects

Age-related cognitive impairment/dementia

Numerous studies have been conducted to evaluate the efficacy of procaine hydrochloride or commercially available mixtures of this compound for the treatment of a variety of organic diseases in aging individuals.(Orgogozo 1987)

Clinical data

A Cochrane review evaluating effects of procaine on cognitive decline and dementia identified 3 clinical trials meeting inclusion criteria; the population studied included those with dementia as well as healthy elderly participants. Pooled data from 2 studies (n=415) showed procaine had a detrimental effect in terms of adverse effects (20 of 208 patients with active treatment vs 3 of 207 with placebo; odds ratio, 7.3 [95% CI, 2.13 to 25]; P=0.002); a single small study of 12 women with dementia also suggested a detrimental effect. A positive effect on cognition was suggested in 2 older studies of healthy elderly participants; however, meta-analysis could not be performed due to use of different preparations.(Szatmári 2008)

In a placebo-controlled, double-blind study, effects of Gerovital H3 on psychologic and physiologic functions were assessed in hospitalized older patients (mean age, 73). Patients received either a 5 mL injection or placebo intramuscularly 3 times per 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. Study results indicated that Gerovital H3 had no ameliorative effect on either psychologic or physiologic functioning.(Zwerling 1975)

Results have been conflicting but generally indicate that these compounds are ineffective in the treatment of any disease. In 1977, a comprehensive review of procaine use in more than 100,000 patients found no evidence of efficacy in treatment of the aging process or common age-related conditions.(Ostfeld 1977) Further reviews have found no scientific evidence to suggest an effect of procaine on aging.(Brodaty 1990, Perls 2013)

Depression

Procaine may act as a mild inhibitor of monoamine oxidase, thereby relieving depression.(Orgogozo 1987)

Nephritis

Animal data

Based on previous animal studies demonstrating dose-dependent inhibition of the RNA-binding protein Hu antigen R (HuR) and subsequent inflammatory gene transcriptions and reactions, researchers hypothesized that treatment with KH-3 would inhibit HuR-targeted inflammatory transcripts and inflammatory reactions, thereby improving glomerulosclerosis, in a rat model of nephritis, where glomerular HuR is activated and elevated. At a dose of 50 mg/kg/day for 5 days, intraperitoneal injection of KH-3 improved markers related to renal fibrosis, including serum urea levels, urinary protein excretion, glomerular matrix accumulation lesions, renal mRNA and key modulators of matrix accumulation, and fibrotic markers in the renal cortex. Additionally, KH-3 was a well-tolerated and safe treatment.(Liu 2020)

KH-3 side effects

Reports describe heartburn, restlessness, dizziness, migraine, and SLE following treatment with KH-3.(Brodaty 1990, Szatmári 2008)

Before taking KH-3

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

How to use KH-3

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

Warnings

No data.

What other drugs will affect KH-3

KH-3 should not be coadministered with anticholinesterase agents (eg, neostigmine). Procaine may inhibit the bacteriostatic action of sulfonamides.(Brodaty 1990, McEvoy 2003)

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. Coadministration with anticholinesterase and anticholinergic agents is a potential contraindication.(McEvoy 2003)

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