H3 Book Index:: Chapters 1-29
The many changes that procaine brings about in the sick and aged body lead, of course, to the question of
how this substance acts. Is procaine merely a catalyst? Does it combine with other substances to form some new compound? It has been suggested that procaine does not enter into the reaction at all, but merely frees certain enzymes. In spite of the efforts of many pharmacologists and biochemists, no single definitive answer has been evolved. Nor do we know why it should come closer to revitalizing old people than any other drug known, or why it should act as a psychic energizer in young people as well.
The current use of procaine, although limited, is actually a reversal of established laboratory techniques, wherein the substance under investigation must be thoroughly analyzed before it is put into use. However, strictly empirical therapy is not a new thing. Another important therapeutic agent, aspirin, has not been explored sufficiently to uncover its mechanism and mode of action.The parallel between procaine and aspirin is striking indeed. Both of these familiar drugs relieve inflammation and pain, and both reduce the crippling effects of arthritis. Aspirin, like procaine, improves the circulation of the blood. Furthermore, neither of the two drugs is habit forming.
Procaine parallels aspirin in another way that may be of considerable importance if procaine proves to be as effective against old age as Prof. Aslan claims-it is not an expensive substance to produce. While, as we have mentioned, procaine has been of value in over 150 serious diseases and lesser ailments (not to speak of its importance in geriatric practice), aspirin has been used (mostly for symptomatic treatment) against some 200 illnesses. The mystery that surrounds the impressive histories of both these substances is deepened by the fact that medical science does not know why either procaine or aspirin act the way they do. But while aspirin is an accepted drug-notwithstanding the risks its application entails, particularly gastric hemorrhages-procaine still has to fight for its recognition in this country although no undesirable side effect has become known (neither a possible allergic reaction nor its incompatibility with sulfa drugs can be classified as such).
Procaine, we may briefly repeat, is hydrolyzed in the body into two substances, para-aminobenzoip acid and diethylamino-ethanol. Both have been extensively studied but in themselves do not have all the effects procaine exerts. Para-aminobenzoic acid (PABA) was found to be necessary for normal pigmentation of hair in the rodent, maintenance of a normal fur coat in the rat, and for the multiplication of certain strains of bacteria. It is present in yeast and liver extract, and is considered a member of the Vitamin B complex. As such it has been given the name HI. But so far it has been impossible to determine PABA's exact role in the human body; we do not know whether it is necessary either for the body's nourishment or its functioning.
Diethylamino-ethanol (DAE), the other component of procaine, is believed to be more responsible for the
properties of the parent drug than PABA, but in itself does not account for the beneficial effects of procaine.
DAE, according to pharmacological textbooks, induces local anesthesia, exerts a quinidine-like action on the heart, a spasmolytic effect on smooth muscle, and also posseses analgesic and antiallergic action. In particular it has proven its therapeutic value in the treatment of
heart arrhythmies, where it is thought to be even more effective than procaine, although it must be administered intravenously in considerably higher doses. This is of no concern, however, since DAE is even less toxic than the almost nontoxic procaine.
Neither PABA nor DAE has a trophic effect on the skin, nor do they stimulate the general metabolism of
the body (leading to an increase in weight) as strongly as does procaine. For that reason it must be assumed that the procaine molecule as a whole must have a very specific effect. Whether this is vitamin-like, as Prof. AsIan believes, whether it has something to do with the production of acetylcholine in the cell structure, as other researchers surmise, or whether a direct influence on the central nervous system is involved, has not yet been proved. Perhaps it is a combination of two or more of these actions.
Rather quietly, a preparation made in Germany, was introduced in health food stores late in 1977. It's name "Omega- H3." It did not as could be inferred from the name, contain procaine, but only paraminobenzoic acid which, as we have seen, is a hydrolysis product of procaine. The distributors of Omega- H3 speak of PABA as an "improved form of procaine, which has world wide scientific recognition as a health promoting factor. . . . This led to the use of PABA in Omega-H 3, which is a vast improvement and superior in every respect to the original procaine."
We have quoted from this prospectus only to criticize the unscientific approach to consider part of a substance a "vast improvement" on the whole substance which in turn is better than the sum of its parts. Omega-H 3 may be a valuable adjunct to nutrition for it contains many vitamins and pollen extract-only an equivalent of any of the procaine preparations it is not!
G. N. Udintsev and V. B. Blank of the Leningrad Sanitary-Hygiene Medical Institute reported in 1957 on their study of the morphological changes in the blood of 150 peptic ulcer patients, before and after procaine infusions. Their results revealed that there is no toxic action of procaine on the bone marrow, and they believe that the changes in the blood produced by procaine are brought about by reflex redistribution of the blood in the body and by reflex action on the bone marrow and hemopoietic system generally.
Soviet researchers have been actively studying and reporting on the effect of procaine on the body, andthe mechanism of its action for as long as 40 years. The recent book by N. K. Gorbadei discusses applications of procaine in the treatment of peptic ulcers, and reviews the theories of the mechanism of action of procaine. After citing the theories put forth by various Soviet biochemists and physiologists as long ago as 1934, Gorbadei continues:
"On the basis of the foregoing we may conclude that no unanimity yet exists with regard to the interpretation of the mechanism of action of procaine. In the opinion of A. V. Vishnevskii, A.D. Speranskii, and N. I. Leporskii, by whatever means it is administered, in addition to its local action procaine also has a general action on the body. This general action of the drug is due to normalization of the processes of inhibition and excitation in the central nervous system.
"Our experimental and clinical findings give grounds for the assertion that when given by intra-arterial infusion, besides its action on the vascular receptor apparatus, procaine has a general action on the body as a whole, through the central nervous system. The intra-arterial infusion of procaine thus has an indirect action on the body via the neurovascular receptor apparatus and the central nervous system. The action of procaine undoubtedly depends on the initial functional state of the nervous system, and on the mode of administration. The diversity of the functional changes resulting from procaine administration, the speed of the reactions to it, and the manifestation of the effect far from the site of injection all underline the role of the general, evidently reflex, action of procaine rather than its local action. This is in agreement with the findings of Andreeva, Komarov, and Timeskov (1957), who consider that the therapeutic effect of visceral anesthesia is mainly dependent on the general neurotropic action of procaine on the body.
"Most authors thus consider that procaine acts through the nervous system. At this point, however, their views diverge. . .
"From the data in the literature and our clinical observations, there are grounds for believing that an essential role in the mechanism of the intra-arterial infusions of procaine is played by nervous reflex influences arising from the receptor apparatus of the blood vessels, as well as by humoral factors, after the entry of the procaine into the blood stream."
As was to be expected, Prof. Alsan herself, wanting to know more about the mechanism of procaine, has done extensive research at her Institute, particularly in plants and animals. This is not the place to describe the highly technical experiments which, while interesting in themselves, have not led to more than a hypothesis as to why procaine brings about the mentioned effects in human beings. Her conclusion: that procaine has a distinct vitamin like effect, but that it may also act as a biocatalyst (speeding up or slowing down certain chemical processes). It was in order to distinguish it from PABA that she proposed to call procaine H3, which is the official name of the buffered procaine she is using in the treatment of her patients.
That the vitamin like effect of procaine is the answer to the riddle may be doubted in view of the fact that, as a rule, procaine is much more successful in the treatment of old age than even extended vitamin therapy. Also the signs of "rejuvenation" appear much faster than in people largely treated with vitamins. As
explanation, if one is possible, should also be forthcoming as to why the few milligrams of PABA set free when the injected procaine hydrolyzes should be able to maintain in a patient a more youthful appearance for months, as sometimes happens after only one or a few injections of procaine.
As an aside, it is interesting to note that the coca leaves commonly chewed by Peruvians and Bolivians living on high mountains have some of the effects now ascribed to procaine. Cocaine has been derived from the coca leaves and, as we have learned, procaine was synthesized as a substitute for the toxic cocaine, which is habit forming. Strangely enough, the coca leaves do not have this effect; when coca chewers move to the cities, they usually stop using it. While digesting coca leaves, they drink and smoke little (as a matter of fact, infusions of coca capsules are being used for breaking the drinking and smoking habits without creating the danger of addiction). According to medical investigations, coca acts as a heart tonic, stimulates the contractions of the heart, thereby enriching the body with oxygen, and increases the excretion of nitrogen, chlorides, sulfates and phosphates in the urine, which may be the main reasons for the sense of well-being engendered when it is chewed. Its anesthetic effects on the palate and the mouth alleviate feelings of hunger and thirst, enabling coca chewers to walk up to fIfty miles daily without fatigue and without any intake of food. Tests made on Indians during and immediately after their coca chewing showed an increase in the metabolic rate. This rate remains high with chronic coca users, clearly showing a stimulation of the metabolism as a whole. No observations have been made as to whether coca may also have some eutrophic effects.
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H3 Book Index:: Chapters 1-29
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