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Laetrile

THE ROBERT CATHEY RESEARCH SOURCE
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[Note, the following paper by Dr. Krebs, can also be found along with other important details about the story of Laetrile and metabolic therapy in Maureen Salaman's book: Nutrition, The Cancer Answer, Statford Publishing, 1259 El Camino Real, Suite 1500, Menlo Park, California 94025.]
The Extraction, Identification and Packaging of Therapeutically Effective Amygdalin
Extracted from a compendium of papers written by Dr. E. T. Krebs, Jr. co-discoverer and developer of Laetrile-amygdalin, for the John Beard Memorial Foundation
THE INFORMATION CONTAINED HEREIN IS OF VITAL IMPORTANCE TO ALL MEDICAL PERSONNEL WHO WISH TO OBTAIN THE FULL CLINICAL POTENTIAL OF AMYGDALIN THERAPY

"Words can conduce to a better knowledge of the subject; they cannot always enforce a standard of excellence in the implementation of such knowledge" Dr. E. T. Krebs, Jr., D. Sc. May 7, 1979

The Prevention and Control of Chronic Metabolic Disease Has Always Been Accomplished by Means Common to Man's Biologic Experience.

Without becoming involved in the unitarian or trophoblastic thesis, suffice it to say cancer is a dietary deficiency disease involving a specific deficiency, at a cellular level, of pancreatic enzymes and vitamin B 17 (with associated A and C and other vitamin, mineral and trace element deficiencies.)

Just as nothing foreign to biological experience has ever prevented or cured any chronic metabolic disease, the prevention

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or cure of the disease has always involved supplying the deficient factor, either water or oil soluble, in the same molecular form as obtained from man's normal surrounding biological environment.

Within a theoretical context (the unitarian or trophoblastic theses of cancer) which we need not consider here, Dr. E. T. Krebs, Sr. and myself deduced the relevance of amygdalin (vitamin B 17) *as it occurs in nature* to the possible prophylaxis, palliation and therapy of cancer in man and animal.

Pursuant to this deduction, we prepared pure amygdalin in the Krebs' laboratories in the 1940's, did comparative toxicity studies, found it non-toxic in doses appropriate to human and animal needs, and then proceeded to study the material clinically.

From the first, those of us involved in the clinical tests were aware that the *amygdalin molecule occurring in nature*, and common to human biologic experience in hundreds of edible seeds and plants, is unstable during and after extraction from its natural source. The slight variations in extracting procedure cause many of the amygdalin molecules to change to a form unknown to nature. These are known as isomers(1). Such a conformation is called neo-amygdalin. A mixture of natural amygdalin molecules and neo- amygdalin molecules is called isoamygdalin. This unnatural iso-amygdalin which is the result of poor extraction technique, caused unpredictable, often severe, reactions in our patients.

All of our successful therapeutic studies were conducted using only pure natural amygdalin.

With no exceptions, all theory and successful practice in amygdalin therapy is based upon the clinical use of pure natural amygdalin.

Scientific Facts Cannot Be Written to Suit Expediency

There are today individuals, manufacturers, and purveyors who label their iso-amygdalin products amygdalin contrary to all of the recognized specifications for the natural vitamin substance
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(1) Isomer one of two or more distinct compounds which possess the same molecular formula, each molecule containing the identical atoms of each element but in a different arrangement. [page 2]


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which is the only true amygdalin. Whether they do this for commercial or political purposes, they certainly cannot justify such fallacy on any rational basis. This scientific heresy and commercial fraud, for it can be called no less, has resulted in tremendously reducing the effectiveness of amygdalin therapy.

Amygdalin is as Defined in the Merck Index and All Scientific Compendia. Any Other Specification is Not Amygdalin.

The identity of amygdalin has been known, with an increasing degree of sophistication, for over 150 years. Its identity over this span of time has not changed. It is defined and explicated in terms of optical activity, molecular weight, chemical composition, and other means of identification in literally hundreds of compendia, papers, encyclopedias and the like in virtually every country of the world.

At one time or another, it has been official in the great pharmacopoeias of the world. Its qualities and identity are irrevocably established. Any compound that is labelled amygdalin should represent but one thing - amygdalin. To the extent that any compound so labelled deviates from what the world accepts as amygdalin, that compound is properly described by all vigilant regulatory agencies as adulterated. Adulterated foods and drugs are subject to confiscation, and their purveyors to prosecution.

Only the Natural Laevo Amygdalin Has Proven Therapeutic Value.

The slightest deviation of compound from that standard which normally identifies it may spell very far reaching physiological and/or pharmacological consequences. I give you a photocopy of page 341 of Paul Karrer's "Organic Chemistry" (Elsevier Publishing Co., Inc., N.Y. 1950). Look at the simplistic structure of D-Glucose. Compare it with that of D-Galactose and compare both to D-Mannose. Glucose is chemically identical with D- Glucose, except that on the 4th carbon atom the hydroxy group in one compound is disposed as the mirror image of the other. Then [page 3]


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in Mannose on the second carbon atom the hydroxy is on the left compared to that on the right for D-Glucose. (Table A) [NB:Table not scanned yet.rsc]

But what difference does it make-medically at least? In relieving hypoglycemic symptoms, galactose, for example, is very much less effective than D-Glucose while mannose, for reasons not fully known, is just about as effective as D-Glucose in relieving such symptoms. Reliance upon D-Galactose in the place of D-Glucose-even if you called the former an iso-glucose or a neo-glucose---could allow the patient to die from unabated hyperinsulinism. (Herring, P.T., J.C. Irvine, and J.J.R. MacLeod --- The efficiency of various sugars and their derivatives in relieving the symptoms caused by insulin in mice. *Biochem J 18*:1023, 1924).

In amygdalin the disaccharide gentiobiose is stereochemically quite stable; therefore, we are presently not specially concerned with that moiety except in its attachment to the asymmetric carbon atom of mandelonitrile. I refer you to the enclosed structure of amygdalin from page 12 of McIlroy's "Plant Glycosides". Please note that in the flow-sheet of synthesis the end product is described as "l-rotatory amygdalin identical with natural amygdalin" (Table B). Note also that the stereoisomeric "unnatural form---non-amygdalin" is separated from the "natural" form by crystallization.

It Has Been Contended that the So-Called Amygdalin Preparations in International Commerce Are Not Actually Amygdalin. This Contention is Correct Because for the Greater Part They Are Iso-amygdalin.

Iso-amygdalin was first prepared by the action of alkali on amygdalin by Walker ( 1903, 1909). Iso-amygdalin is accidentally produced through less than efficient or careful extraction processes for amygdalin.

Put very simply, so called iso-amygdalin is approximately 50 percent amygdalin and 50 percent non-amygdalin (neoamygdalin). It does not follow from this that iso-amygdalin is only 50 percent less therapeutically effective than amygdalin. Our laboratory and clinical experience suggest a far greater loss. [page 4]


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Iso-amygdalin is Less Than 50 Percent as Therapeutically Effective As Amygdalin.

Clinically, the results obtained from amygdalin therapy have deteriorated over the years as the quality and methods of production and packaging have become progressively abominable until therapeutic efficiency is today less than one third that of the lyophilized Laetrile produced by Krebs and Delmar Laboratories.

The reduction in clinical efficiency is the direct responsibility of manufacturers who either out of concern for profit, or lack of concern for the product, have provided inadequate extraction facilities and personnel, the result is spoiled production which they package and label as amygdalin.

The Necessity to Maintain The Natural Configuration for Clinical Effectiveness is not Unique to Amygdalin.

We know no instance in biology or medicine in which an "unnatural isomer" can be accorded equivalence with a natural one.

Consider thyroxine, L-thyroxine is the physiologically active stereo-isomer. In the case of epinephrine, which is laevo-rotatory to polarized light, we find the dextro-rotatory isomer has only about one-twelfth the action of the natural or laevo compound. There are the closely related Synephrins: while Synepherin rotates polarized light to the right: Neosynephrin rotates it to the left. The latter compound is much more active and has generally replaced Synephrine.

Atropine is a racemic (2) hyoscyamine; that is, it consists of equal parts of laevohyoscyamine and dextrohyoscyamine; the action of atropine is practically that of its laevohyoscyamine half. In plants, atropine does not itself exist; the laevo-hyoscyamine is racemized in extraction. Shades of iso-amygdalin! The ester of atropine and mandelic acid is known as homoatropine. Laevo isomers, both of them.
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(2) A racemic mixture is a 50/50 mixture of laevo and dextro rotary forms of a compound, i.e. mirror images of each other. The term is sometimes used to refer to a simple mixture of isomers.

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Nowhere in Living or Biological Systems is There an Equal Tolerance for Natural and Unnatural Isomers. The Unnatural Mixtures are Always at Least 50 Percent Inferior to Pure Preparations of the Natural Isomer.

*Iso-amygdalin is not amygdalin*. It is spoiled amygdalin. It is therapeutically as unsound as racemized epinephrine, racemized thyroxine, racemized Synephrine, racemized hyoscyamine, or the like. In the case of atropine the "equal part" of dextrohyoscyamine is physiologically dead or inert. But suppose it were more than this? Suppose that it inhibited the laevohyoscyamine half?

In the case of unnatural forms of amygdalin (iso-amygdalin or neo-amygdalin) used for antineoplastic effect how do we know that the unnatural isomer does not render the natural one inert? Is it not entirely possible that neo-amygdalin (3) acts as an anti-vitamin destroying or inhibiting the metabolic pathway of natural amygdalin? At the very worst; could neo-amygdalin, in common with many products modern man ingests that are not included in his biological experience, actually be carcinogenic or promote metastasis? Until the answers to these questions are known it is prudent to avoid all but natural amygdalin.

Sooner or later some regulatory authority will correctly accuse distributors of iso-amygdalin of "watering the milk": charging for amygdalin and supplying about 50 percent of it as the inferior isomer. In all of organic nature there is simply no such thing as the natural isomer of an optically active compound having the same physiological characteristics as the unnatural form.

Of All the Seventeen or More Water or Oil Soluble Vitamins, There is No Such Thing as a Deviance From the Naturally Occurring Structure Proving Anything More Than Unsatisfactory or Inert.

We are going to be called, as I have been in the past, to go to a blackboard to write out the entire structural formula of amygdalin in explicit detail down to the identification of the isomer. If any manufacturer or purveyor is going to fool with any structural deviation from actual amygdalin then he has the scientific and regulatory responsibility of specifically identifying the "unnatural
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(3)Neo-amygdalin is the pure isomer to which many natural amygdalin molecules are converted during inexpert extraction. Iso-amygdalin is an equilibrium mixture of approximately 46% natural amygdalin molecules and 54% neo-amygdalin molecules.

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molecule": being able to draw its total structure on a blackboard and being able to defend the identity of that structure with what carries the same identification in a commercial dosage form.

When I personally produced amygdalin I was able to demonstrate its conformity with the molecules as it occurred in the seeds or kernels from which it was extracted. Of course, I had the prior assistance of literally hundreds of chemists all over the world who for a century had exhausted all of the chemical and physical or optical properties of amygdalin in giving it as hard a definition as that for pure gold, any other element, or for water and dextrose.

Recall epinephrine (Adrenalin) where the natural form is twelve times more active than the unnatural form? An "iso-epinephrine" would be, approximately, a 40 percent (or greater) fraud on the purchaser.

Like amygdalin, extraction techniques for epinephrine may result in iso-epinephrine, as they do in the case of amygdalin for iso-amygdalin. Because of imperfect or sloppy extraction techniques one is left with two possible options when faced with such accident of extraction. One is to take the "iso" mixture and separate through crystallization one isomer from the other, and then prepare the natural isomer for packaging. This becomes relatively costly because the loss in recovering the pure natural isomer is about 60 percent more than stopping with the "iso form". If one stops with the iso form and goes ahead and packages it, the economic cost is about 70 percent less, the cost in human health and life may be incalculable.

To Mislabel Iso-Amygdalin as Amygdalin is Scientifically, Medically, and Morally Indefensible.

I would be tempted to greater tolerance, at this stage of our development, were it not for the fact that almost 20 years ago I produced pure amygdalin in kilogram quantities that measured up to all official standards working with equipment (short of

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lyophilization) that cost us less than $12,000.
We were really purists about it all---just as Parke Davis is with Adrenalin. When an accident of extraction occurred we simply ran the product down the sewer. Unquestionably this had much to do with the fact that our "therapeutic index" was about 80 percent higher than it is with deviant material on the market today---even when implemented by "metabolic therapy".

Packaging of Injectable Amygdalin is as Important as Extraction.

Even carefully extracted amygdalin is extremely unstable when placed in solution for storage or shipment. The slightest variances in temperature or pH will cause many of the molecules to change to the same unnatural configuration obtained by poor extraction procedure with the same attendant reduction in therapeutic efficacy. Amygdalin in solution of indefinite age is extremely unpredictable and should be avoided.

All Injectable Laetrile Amygdalin Must Be Lyophilized (Freeze Dried) Anything Else is Simply Not Laetrile--Amygdalin.

Freeze drying (lyophilizing) is the only presently available method of preserving the natural laevo amygdalin to be used parenterally for an indefinite period.

Historically no dosage unit of parenteral Laetrile amygdalin has ever been legitimately dispensed unlyophilized. Any vial or ampules containing an aqueous solution labelled amygdalin has by its very nature been mislabelled and should bear the label iso-amygdalin from which its lessened therapeutic efficacy could be deduced.

Three Grams of Amygdalin Can Not Be Dissolved, Much Less Shipped, in a 10 cc Ampule.

Currently the labelled three gram vial, or ampule, of amygdalin has become the standard unit for injection. These vials and ampules, each with a lOcc capacity, are an anathema to those individuals knowledgeable in stereochemistry and the technical specifications of amygdalin.

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By specification one gram of amygdalin will dissolve in not less than 12 ml. (lOcc) of water at room temperature. One is therefore led to the obvious conclusion that a lOcc vial, labelled to contain 3 grams of amygdalin, either contains much less than three grams or contains iso-amygdalin, which is far more soluble in water than natural amygdalin. Either conclusion means that the label of 3 grams amygdalin is fraudulent, and the clinical activity of the vial, if any, is far less than should be expected.
Lyophilization Makes Minimum Size Injections Possible.

The only exception to the chemical axiom of amygdalin solubility: 1 gram will dissolve in not less than 12 ml. of water at room temperature, is a special form of lyophilization. Lyophilization (freeze drying) of amygdalin will create a crystalline structure which is capable of being reconstituted in a much smaller amount of sterile water. The advantage of lyophilized amygdalin, for parenteral use, is obvious when one considers that it requires 36 ml. of water to dissolve 3 grams of amygdalin for injection. Three grams of lyophilized amygdalin can be reconstituted and injected in a far more reasonable and practical quantity.

It should be remembered that once in solution the lyophilized amygdalin will reassume the unstable characteristics of the amygdalin molecule and should therefore be injected as shortly after being put in solution as possible.

I Hope All This Has Been Helpful. Words Can Conduce To A Better Knowledge Of The Subject: They Cannot Always Enforce A Standard of Excellence in the Implementation of Such Knowledge.

It may be asked why we have not spoken out more strongly against the mislabelled, adulterated under-strength, products currently in commerce while the therapeutic index of success with amygdalin has continually decreased! F.D.A. regulation has made extraction of amygdalin in the U.S.A. illegal. The only manufacturing available has been on foreign soil and until now these sources have been woefully inadequate, but even these

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sub-potent products have given superior results to the cut, burn, and poison protocols of established medical practice.
In A Practical World We Must Often Accept Expedient Relief of Human Distress As Better Than No Relief At All. At the Same Time We Cannot Diminish the Energy With Whice We Strive Toward the Ideal Means of Relief.

As new sources become available clinicians will be careful to ascertain that the amygdalin proffered to them is natural amygdalin with the molecular structure found in man's normal surrounding biological environment.(4) Doctors will not be fooled by products that are presented in powdered or lyophilized form but are still composed of unnatural iso-amygdalin. It is only the natural amygdalin that we can be sure has antineoplastic effect.
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(4) Doctors should demand a certificate of analysis from a certified laboratory. Optical rotation is a negative test only and is not acceptable by the National Cancer Institute, the F.D.A. or any technically knowledgeable laboratory as an index of pure natural laevo amygdalin. Optical rotation can be too easily altered by the addition, accidentally or on purpose, of such compounds as free glucose. The most accurate test to determine pure natural amygdalin is H.P.L.C. and 13C-NMR (according to Thomas Cairns et al., John K. Howie, and D.T. Sawyer, U.S. Food and Drug administration, Los Angeles, California 90015 and Dept. of Chemistry, University of California Riverside, California 92521.


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Disclaimer.
This Web page was written and made by Roger Cathey, Research Associate of the ROBERT CATHEY RESEARCH SOURCE.
All pages Copyright © 1996 R.S.Cathey, except where specified otherwise.

What Is The Laetrile Therapy
Metabolism is the total function of our body. In order for our body to function properly, all its attributes (physical, mental, and spiritual) must work in harmony. Total care is the goal of the Metabolic Therapy, has several elements that are utilized in order to provide our human organism the best environment to combat the disease and regain health. The Metabolic Therapy, our primary nontoxic cancer treatment, is based on the use of laetrile, digestive enzymes, immuno-stimulants, mega-doses of vitamins and minerals, spiritual, nutritional, and psychological support. The metabolic Therapy is not complete without its chief anti-tumor agent.

Laetrile (B-17) is a natural chemotherapeutic agent found in over 1,200 plants, particularly in the seeds of common fruits such as apricots, peaches, plums, and apples.

It is a diglucocide with a cyanide radical that is highly"bio-accessible". This means that it penetrates through the cellular membrane reaching high intracellular concentrations easily. The cyanide radical is what preoccupies most scientists, but it has been proved that Laetrile (B-17) is completely nontoxic. Our own experience with hundreds of patients give us complete confidence that there is no danger. The normal cells in our organism contain an enzyme called Rodhenase which "neutralizes" the laetrile.

This enzyme does not allow the laetrile to release the cyanide. In this way, laetrile only serves as a glucose to healthy cells providing energy. Malignant cells do not contain this enzyme. In the absence of Rodhenase, the laetrile is activated liberating the cyanide radical inside the malignant cell causing its destruction. This is the way God creates things:
only cancerous cells are destroyed but normal ones are not affected.

As the laetrile attacks unhealthy cells, it transforms into silicate which is much like aspirin. It contributes greatly to pain control. Though it has limitations in certain cancers, it is extremely effective in the most common tumors such as Carcinoma of the Lung, Breast, Prostate, Colon, and Lymphomas .

A highly publicized clinical trial conducted by the National Cancer Institute (NCI) in 1981, tried unsuccessfully to prove that Laetrile was ineffective and toxic. Today, Laetrile occupies a position on the "front lines" of Alternative Cancer Therapies. We have found Laetrile to be effective on people that have active cancer; but that is not its only function. For prevention of cancer and the maintenance of remission there is nothing as effective as Laetrile. Its non-toxicity permits its use indefinitely in the prevention of relapses and the prevention of metastases. Surgery, Radiation, and Chemotherapy can only be administered for a limited time, afterwards patient are left without any protection.

There is no doubt that the struggle against cancer is the greatest challenge that medical science has ever faced. There is no other disease to which more money is devoted, or to which scientists dedicate more hours of study. The magnitude of the cancer problem may be demonstrated by a few statistics. One of three Americans will develop Cancer during their lifetime, and one out of four will die from it. This year, over 989,200 people will die from cancer in the USA .

Cancer is increasing in all age categories. Lifestyle, nutrition, food additives, pesticides, ultraviolet radiation and a variety of other environmental factors are directly implicated. With certain exceptions, cancer appears to be a man-made disease and is therefore a preventable disease. It is now apparent that cancer may be caused by an almost limitless variety of physical, chemical and biological agents. Although it is true that surgery an radiotherapy are capable of curing some patients with localized tumors and that chemotherapy has achieved cures in some malignant tumors, the general mortality rate from cancer is increasing. Many patients cannot be exposed to chemotherapy, surgery or radiotherapy because of the undesirable effects over their poor physical condition resulting from cancer.

All this justifies, and even makes imperative, the search for new substances with anti-tumoral effects and ideally with little or no toxicity in therapeutic dosages. In the last 15 years, several herbs and hormonal substances have been discovered with such characteristics. Therefore, many patients who formerly could not be benefited or alleviated medicinally may not be exposed to useful anti-neoplastic treatments. Nature provides an arsenal to destroy tumors or at least to neutralize their growth.

The leading natural therapy is Amygdalin, better known as Laetrile, a product made with the purest amygdalin, obtained from apricot kernels (bitter almonds), through an exclusive extraction process.

What Is The Nature Of Cancer?

In order to intelligently discuss any form of therapy, it is essential to know something about the nature of the disease. Cancer has been defined as a cellular tumor, the natural course of which is fatal. Another term for cancer is a malignant neoplasm . Neoplasm refers to a progressive uncontrolled new growth of tissue.

The term tumor may be correctly applied to any neoplasm, benign or malignant. A benign tumor is one that lacks the ability to invade other tissues and does not spread or metastasize , and for the most part can be surgically removed. A malignant tumor or cancer is characterized by it's ability to invade tissue, metastasize, the cells are less differentiated (a process known as anaplasia , in which the tumor cells do not resemble those of the parent tissue), and ultimately results in the death of the victim. The term metastasis refers to the transfer or spread of the cancer from one organ or part to another not directly connected with it. Thus, tumor cells may originate in one part of the body ( primary tumor ) and suddenly appear in some other organ or distant part of the body ( secondary tumor ).

Metastases are a significant factor in bringing about the death of the patient. There are over 100 different clinical types of cancers which are frequently divided into the two broad categories of carcinomas and sarcomas . Carcinomas are malignant new growths of epithelial cells and may involve the breasts, digestive tract, uterus, skin, etc. Sarcomas are malignant new growths of connective tissue and involve such organs as bone, muscle, nerves, lymph glands, etc. Hodgkin's disease and melanomas are a type of sarcoma. In general, tumors are classified according to the cell type involved, and occasionally they are of the mixed type containing both epithelial and connective elements. The leukemias are another type of malignancy that involves a progressive proliferation of the blood forming organs of the body. Leukemia is sometimes referred to as cancer of the blood.

The typing and grading of malignant tumors becomes very complicated and goes far beyond the intent of this publication. In order to explain some of the more basic elements of carcinogenesis, it is necessary to deal with some of the fundamental of cell structure and function. The major subdivisions of a cell include the nucleus and the surrounding cytoplasm . The nucleus is the primary control center of the cell. Chromosomes are a structure in the nucleus comprised of a linear thread of a nucleic acid known as deoxyribonucleic acid (DNA) . Chromosomes appear as elongated threadlike bodies in the nucleus and are clearly visible only when the cell is undergoing division. The chromosomes are comprised of nucleic acid and protein. The nucleic acid DNA transmits genetic information. The chromosomes also bear the basic units of heredity called genes .

The genes determine the characteristics of the cells, and act as control units in the metabolic activities of the cell. Genes therefore serve as code units which determine most of the enzymatic and other biochemical activities within the cell. It is through the genes that this basic metabolic data is passed on from one generation of cells to the next. The cytoplasm surrounding the nucleus of the cell contains a complex network of membranes known as the endoplasmic reticulum . This reticulum is lined on its outer surface by small particles called ribosomes . The ribosomes contain large concentrations of a nucleic acid known as ribonucleic acid (RNA).

These ribosomes are directly concerned with protein synthesis. RNA also occurs in the nucleus of the cell. It is now known that RNA is synthesized in the nucleus of the cell and migrates to the cytoplasm. The DNA acts as a template or pattern for the synthesis of RNA, which in turn acts as a biochemical messenger between the DNA of the nucleus and the metabolic machinery of the cytoplasm. Thus, RNA appears to exert a controlling influence over the entire metabolic activities of the cell. Any alteration in the DNA mechanism is going to affect the RNA messenger and thereby alter the metabolic changes in the cell. In case of cancer, the regulatory mechanism that governs cell division is obviously affected and the cells begin to rapidly proliferate and gradually lose their differentiation.

There are numerous theories that have been proposed as to the cause of cancer. It is now apparent that cancer may be caused by an almost limitless variety of physical, chemical and biological agents. However, it is becoming increasingly apparent that regardless of the precipitating factor, somewhere along the progression of biochemical events, the basic DNA-RNA mechanism is involved. If this vital genetic machinery is damaged, cancer may be the end result. It would appear that if the cause of cancer is due to an alteration of the normal metabolism of the cell, then the correction of the problem would be by means of a Metabolic approach, which is basically the subject of this web page.

Amygdalin ( Laetrile ) History and Actions

Amygdalin is a herbal constituent derived from the kernels of various fruits of the Genus Prunus (synonym amygdalus) , which includes the plum, prune, cherry, peach and apricot. It is among the most ancient herbal products used against cancer. Apricot kernels have been in medical use since the days of Pen T'sao (great Chinese Herbalist), in the year 2800 B.C., in ancient China. Also, the great Persian master of pharmacy, medicine and natural sciences, Avicenna (980-1037) recommended the use of apricot bitter almond oil in the treatment of tumors of the spleen, uterus, stomach and liver. Amygdalin is one of the first and best known cyanogenic glycosides. The systematized study of amygdalin did not really begin until the first half of the past century when crystalline amygdalin was isolated in 1830 by two French chemists, Robiquet and Boutron. Now known as Prunus Amygdalus, of the rose family Rosaceae, amygdalin is hence appropriately named after the scientific name of the bitter almond. The chemical structure of amygdalin is well established as laevo-D-mandelonitrile-B-D-glucoside-6-B-D-glucoside; essentially, it is a diglucoside with a cyanide radical. Laetrile is a decomposition product resulting from the hydrolysis of amygdalin. Neither amygdalin nor laetrile contain free cyanide. Laetrile formula is laevo-D-mandelonitrile-B-glucoronide. The term laetrile was first proposed by Ernest T. Krebs, Jr. in 1949.

The word is derived from the contraction of the chemical term LAE vo-mandeloni TRILE . Krebs also designated laetrile as vitamin B17 . Krebs contended that amygdalin is essential to human health. The Amygdalin Therapy The amygdalin (laetrile) therapy utilizes the cyanogenic glycoside amygdalin, or one of it's byproducts, together with a broad-based nutritional program Metabolic Therapy for the control of cancer. Krebs, Jr. and his research group found that amygdalin has it's powerful cancer killer capabilities because it contains cyanide that destroys cancer cells. Not all cyanide compounds are poisonous, humans constantly eat produce with cyanide, about 1,200 kinds of foods have it. Detoxification of cyanide can take place in all tissues of the body, but principally in the liver. The dosage levels and toxicity of amygdalin (laetrile) in laboratory animals and humans is well established and documented. No evidence of acute or accumulative toxicity was observed in any animals giving doses in excess of 100 times the maximum intravenous dose usually given in humans.

These findings coincide with that mentioned by Otto Jacobsen in 1887, Davidson in 1944 and Dr. Dean Burk ( National Cancer Institute) in 1968: "Amygdalin is impressively nontoxic from the pharmacological point of view", and "non-hydrolyzed amygdalin is less toxic than glucose". The oral toxicity of amygdalin was found to be 39 to 44 times greater than the intramuscular route, and more toxic than intravenous route (parentenal route). Amygdalin is less tolerable by oral administration because of the hydrolysis of amygdalin by the gastric juices. On the other hand, amygdalin, in dosages of 20-40/mg/kg orally (for a 200 lb human this would translate to 16 - 500mg laetrile/B17 tablets, daily), used in humans, is 10 to 20 times less than the minimum toxic dosage in dogs. The biological half life of amygdalin is only 80 minutes. Over 80% of the amygdalin administered is excreted from the body in 4 hours. The usual metabolic approach to amygdalin (laetrile) therapy is to provide the patient with adequate nutritional support, with relatively nontoxic high doses of vitamins and minerals, and other active natural substances.
Amygdalin (laetrile) has been administered in dosages of up to 70 grams (70,000 miligrams-mg) per day in adult humans by combined oral and parentenal routes without adverse effects.

Amygdalin's Action Mechanisms (Krebs Hypothesis)

The most widespread theory ("cyanide theory") on the action of amygdalin was propounded by Ernest Krebs, Jr. in the seventies. Krebs hypothesis: The resulting end products of the hydrolysis of amygdalin are the hydrocyanic acid (HCN) and benzaldehyde. In order to produce these products B-glucuronidase is required. It has been demonstrated that this enzyme is present in cancerous tissue, about 1,000 to 3,600 times higher than in normal tissue. Rhodanase is an enzyme found in the liver cell and is known to be concerned with the conversion of toxic hydrocyanic acid to thiocyanate, a harmless substance. Rhodanase is part of the normal detoxification process of the body. However, it was found that normal cells contain a relatively high concentration of rhodanase and low concentration of B-gluco-ronidase, whereas cancerous cells are high in available B-glucoronidase and low in available rhodanase.

Thus, the normal cellular protective mechanism is decreased in tumor cells and they become more sensitive to the effects of the cyanide ion. The HCN would tend to depress the enzyme functions of the cancer cell and thereby destroy it. Since normal cells contain large quantities of rhodanase and relatively low quantities of available B-glucoronidase, the available rhodanase would detoxify the cyanide ion (CN-), forming the non-toxic thiocyanate. Then according to Ernest Krebs amygdalin's toxic effect is against the cancerous cell and not the host.

The Effectiveness Of Amygdalin (laetrile) In Cancer

Ever since the days of Louis Pasteur (1822-1895) and Paul Ehrlich (1854-1915), cancer victims have hoped for the "wonder vaccine" or the "magic bullet". Amygdalin (laetrile) does not come under the heading of either of these dramatic therapies. There are a number of factors that enter into the cancer treatment complex. The type of cancer involved is an important factor. Some types of cancer tend to be more sensitive to treatment than other. Amygdalin (laetrile) is not equally effective in all types of cancers. Rubin (1977) found in their clinical investigations in Israel that Amygdalin (laetrile) was most effective against Adenocarcinoma and Hodgkin's disease, somewhat less effective in certain other of the Sarcomas and Melanomas , and relatively poor results were achieved with the Leukemia. Similar results have been obtained by other clinicians in the United States and elsewhere. The best results with Amygdalin (laetrile) therapy have been achieved with Lung, Prostate, Breast, Lymphomas, Liver and Brain cancer. The chemical quality of the Amygdalin (laetrile) also has a bearing on the clinical therapeutic results.

Only the laevo isomer of Amydalin (laetrile) has been found to be therapeutically active. A high quality Amygdalin is now produced in Mexico and some products are currently under investigation in the United States and Germany . It is therefore of the utmost importance that quality products be utilized. Failure to recognize this point can result in inadequate dosage levels and false negative therapeutic results (Krible, 1912; Levi, et al, 1965; Rubin, 1978). Other factors relating directly to the administration of Amygdalin (laetrile) concern the dosage. In the past, most physicians have tended toward administering too low a dosage. Therefore the frequency of administration, the route of administration, and the dosage are of the utmost importance if adequate blood levels are to be maintained. In the past, most errors of administration have been made on the side of too little, rather than too much. However, it should be kept in mind that the most effective routes are by parenteral injection (I.M or I.V.) and the physician should not attempt to achieve the necessary dosage levels by the oral route. Rubin (1978) reports administering 70gr. per day to each patient with no ill effects. Another aspect that will have a bearing on the recovery of a patient depends upon the degree of tissue damage caused by excessive radiation and toxicity resulting from chemotherapy.

It is presently estimated in the United States, Mexico, and elsewhere, that about 90% or more of the patients begin using Amygdalin (laetrile) only after all other types of cancer therapies have failed. Most metabolic physicians are of the opinion that if the patient were to begin Metabolic Therapy earlier in the course of the disease, it would improve the patient's chances of Cancer Control. The adequacy of liver functions is of the utmost importance in cancer therapy. The liver has varied, intricate and extremely complex metabolic functions. Among other things the liver is concerned with fat, carbohydrate and protein metabolism.

The liver has a propensity for storing vitamins, especially A, D and B 12 , and Iron in the form of ferritin. The liver forms a large proportion of the blood constituents: Fibrinogen, Prothrombin, Accelerator Globulin, Factor VII, and other coagulation factors. The liver is involved in vitamin K metabolism. The liver is concerned with the vascular storage and filtration of blood, with about 1000ml of blood flowing from the portal vein through the liver sinusoids each minute, and an additional 400ml flows into the sinusoid from the hepatic artery. Thus when the liver or kidneys are damaged due to a primary or metastatic malignancy, it may adversely affect the entire metabolism of the body.

The studies conducted thus far on Amygdalin (laetrile) indicate that there is no damage to the liver or kidney function. Much of the effort of metabolic therapy is dedicated toward sustaining adequate liver and kidney functions, and to attempt to minimize the detoxification load placed upon them. It should be emphasized that Amygdalin (laetrile) therapy is most effective when used in conjunction with a comprehensive METABOLIC approach. Most physicians using this form of therapy provide adequate nutritional support with the use of proper vitamin and mineral supplements. The patient is placed on a complete vegetarian diet with a reduction of proteins, fats, refined sugars, and processed foods. All tobacco, alcohol, caffeinated drinks, and most toxic medications are eliminated. The patient is placed on a high intake of select fruit juices, fresh fruits and vegetables. A program of Detoxification is required. A minimum of 9gr of Amygdalin (laetrile) per day is administered, largely by the parenteral route, but even higher levels may be given if indicated. Patients that refuse to follow the general Metabolic Program are discouraged from taking Amygdalin (laetrile) .

Alternative Forms Of Cancer Treatments

There are probably as many different forms of cancer therapy as there are types of cancer. There are cancerous conditions which require surgery, radiation, and/or chemotherapy. There are certain types of cancer, and certain stages in the development of the cancer, that respond well to one or more modalities. Significant success has been obtained in the treatment of Hodgkin's disease, some leukemias, and certain other types of cancers. The patient is advised to consult with a physician and seek the best medical advice available. Most skin cancers can be readily treated with conventional methods of therapy if instituted early enough. However, the most common type of internal cancer is adenocarcinoma (involving the breast, intestinal tract, lung, etc.). When an adenocarcinoma and certain of the sarcomas undergo metastases, most conventional therapy is ineffective and the prognosis of the patient is poor, using conventional therapies. The patient is then left with the dilemma of Where do I go from here?

These cases should be encouraged to try Amygdalin (Laetrile) Therapy . If the cancer victim is trying to decide how to proceed, whether to stay with conventional therapy or the Life Without Cancer Amygdalin (laetrile) therapy the following procedure is recommended: The patient should determine from his physician the type of cancer with which he is afflicted and then visit the Cancer Ward at any major medical center in the United States. Most patients will find it very educational to visit a high-class conventional Cancer Ward, subsidized by the National Cancer Institute and the American Cancer Society , and check with the doctors, nurses and patients and see for themselves just how many "terminal cancer victims" actually survive the ordeal.

The fact that the wealthiest persons, most influential politicians, brightest Hollywood stars, highly educated persons, and skilled orthodox physicians are dying of metastatic malignancies should be suitable commentary as to the efficacy of conventional therapy. The studies made in 1977, indicate that persons that combine Amygdalin (laetrile) with conventional chemotherapy are able to tolerate higher doses of toxic chemotherapeutic agents with far less side effects. Interestingly enough, this synergism is characteristic of adaptogenic agents.

What Of The Future?

Here is the forecast based on the evidence currently on hand:

a) Clinical trials on Amygdalin (laetrile) therapy using good quality Amygdalin will continue to be conducted in the proper manner.

b) Amygdalin (laetrile) will be legalized in the United States with or without the cooperation of the FDA at some point in the future.

c) The atrocities now being committed in the name of orthodox medicine, the suppression of life-giving scientific data, the needless loss of lives, mutilation of bodies, and excessive suffering, all for the financial benefit of a ruthlessly powerful medical cartel which is flagrantly in violation of the antitrust laws of this government, will not continue to be tolerated by the American people.

Ultimately, these criminals and their political lackeys will be brought to trial and they will find themselves responsive to the American people. The following is one of the greatest rights ever given to a people: "NO STATE SHALL MAKE OR ENFORCE ANY LAW WHICH SHALL ABRIDGE THE PRIVILEGES OR IMMUNITIES OF CITIZENS OF THE UNITED STATES: NOR SHALL ANY STATE DEPRIVE ANY PERSON OF LIFE, LIBERTY, OR PROPERTY, WITHOUT DUE PROCESS OF LAW, NOR DENY TO ANY PERSON WITHIN ITS JURISDICTION THE EQUAL PROTECTION OF THE LAWS" . (from the 14th amendment of the constitution of the United States of America. 1868)

Laetrile - the answer to Cancer
by James South MA


The anti-cancer drug Laetrile is one of the most controversial subjects in the history of medicine. Laetrile's most ardent proponents consider it to be a natural cancer cure, literally built in to the normal "vitamin architecture" of mammalian food supplies as the primary natural exogenous cancer control for humans and animals. They have called Laetrile "vitamin B17."(1) Laetrile's opponents consider it, quite simply, as a "toxic drug that is not effective as a cancer treatment." The term "Laetrile" was coined by the father/son team of Ernest T. Krebs Sr.., M.D., and E.T. Krebs Jr. research biochemist. It is a contraction of the more formal name "LAEvo-mandeloniTRILE-glucoside

O.L. Oke has noted that "Cyanogenetic glycosides [nitrilosides] have been found in the following common vegetables: maize, sorghum, millet, field bean, lima bean, kidney bean..., sweet potato, cassava, lettuce, linseed [flaxseed], almond and seeds of lemons, limes, cherries, apples, apricots, prunes, plums and pears." (4) Thus Krebs has argued that their widespread presence in foods consumed by humans and animals all over the world argues against nitrilosides/laetriles being seriously or inherently toxic. Krebs also believed this gives "laetriles" the status of "accessory food factors," rather than their being a "drug," alien to normal human metabolism.

Laetrile" to treat cancer was reported in 1845 by T. Inosmetzeff, a professor at the Imperial University of Moscow. (5,6) A young male cancer patient of 20 received approximately 46,000 mg of amygdalin over a period of 3 months, and was still alive 3 years later. A women of 48, with extensive metastasis from a primary right ovarian tumor, received varying amounts of amygdalin over a period of years and had survived II years at the time of the report. No sustained pharmacologic harm was seen with these patients. In the modern era Laetrile was "rediscovered" in the 1940s by the Krebs. By the late 1940s - early 1950s, use of Laetrile to treat cancer had spread quietly around the world. Early dosages were extremely modest - only 50 - 100 mg by intravenous injection, with total patient dosage then seldom exceeding 2 gms. By the 1960s the Krebs were recommending 30 gms total Laetrile dosage, spread over a 10-30 day treatment course. (7) By the 1980-90s, intravenous dosages up to 9 gms, with total patient dose reaching 2-300gms, was not uncommon. (8) Classical Laetrile proponents, such as Krebs, Dean Burk, and P. Binzel, do not consider Laetrile a literal cancer cure, however, anymore than insulin injections are a "cure" for diabetes. Rather, Laetrile is considered a cancer control which will need to be taken indefinitely, in oral form, after the original "cancer crisis" is brought under control. This exactly parallels the situation of vitamin deficiency diseases, where intravenous injections may be used to bring a severe vitamin deficiency disease (e.g. pellagra or beri-beri) under control, with higher-than-normal oral doses needed indefinitely thereafter to prevent relapse, The typical oral Laetrile dose used after intravenous injections is 1 to 2 gms/day. (8) Yet Krebs suggested that 50-100 mg of Laetrile/day might suffice to prevent cancer in normal healthy adults. (1)

The "proof" of Laetrile's efficacy in preventing/controlling cancer has come from 3 different sets of data: epidemiological, animal tests, and human clinical use by experienced pro-laetrile doctors. The epidemiological evidence for Laetrile is controversial, like all epidemiological evidence, and provides only strong suggestions, not incontrovertible proof.

As Krebs points out, "Tribes in the Karakonims of West Pakistan, [the Hunzas], the aboriginal Eskimaux, tribes of South Africa and South America living on native foods, the North American Indian in his native state, the Australian aborigines and other native or so-called primitive peoples rely upon a diet containing as much as 250 to 3000 mg of nitriloside in a daily ration. Civilized, Westernized... man, on the other hand relies on a diet that probably provides on average less than 2 mg nitriloside a day". (3) Among these people, cancer tends to be rare compared to the high rates present in America and Europe. For example, Sir Robert McCarrison, famed medical nutritionist in the 1920s - 30s, failed to discover a single case of cancer among the Hunzas during a 20 year period, while John dark, M.D., a later medical missionary among the Hunza, also failed to find cancer among them. (3) The Hunza diet is based in significant part upon the apricot kernel, a rich source of Laetrile, which typically provides them with at least 150 - 250 mg "B17"/day. (3)

Among the Eskimaux living on their native diet, cancer was also so rare that it prompted famed anthropologist/explorer V. Steffanson to write a book on the subject: Cancer: Disease of Civilization? (9) Krebs notes that the salmon-berry is a rich nitriloside source, and is used by traditional Eskimaux to make pemmican, which is eaten year-round. The contents of caribou stomachs, partially-digested grasses unusually rich in nitrilosides, are a prized delicacy among the Eskimaux. (3)

Dr. M. Navarro of Santo Tomas Univ. of Manila, was a world-famed oncologist who was also an early Laetrile clinical pioneer. "By 1977 he had linked the low incidence of cancer in the native populations of Mindanao [the Philippines] to the continual ingestion of many sources of vitamin B17. That rate, about I per 100,000 [less than 1% of the U.S. cancer rate], is even smaller than the low rate of cancer in the non-urban Filipino north, where generations of Filipinos have subsisted on [nitriloside-rich] cassava, wild rice, wild beans, berries and fruits of all kinds." (10)

In a letter to Dean Burk, pro-laetrile head at that time of the Cytochemistry Dept. of the NCI, Krebs wrote concerning North American Indians: "I have analyzed from historical and anthropological records the nitriloside content of the diets of... carious North American tribes.... Some of these tribes would ingest over 8,000 mg of vitamin B17 (nitriloside) a day. My data on the Modoc Indians are particularly complete." (12) As an example of the low cancer incidence among Indians eating their high "B17" native diet, Krebs cited a report on the Navajo-Hopi Indians from JAMA. Feb. 5, 1949: "...the doctors wondered if [the Indians' diet] had anything to do with the fact that only 36 cases of malignant cancer were found out of 30,000 admissions to Ganado, Arizona Mission Hospital... In the same population of white persons, the doctors said that would have been about 1800." (12)

In his preface to A. Berglas' book Cancer: Cause and Cure. medical missionary Dr. Albert Schweitzer wrote that "On my arrival in Gabon [Africa] in 1913, I was astonished to encounter no cases of cancer. I saw none among the natives two hundred miles from the coast.... I can not, of course, say positively that there was no cancer at all, but, like other frontier doctors, I can only say that, if any cases existed they must have been quite rare. This absence of cancer seemed to be due to the difference in nutrition of the natives compared to the Europeans...." (13). Of course, such high nitriloside foods as cassava, millet, maize and sorghum are staples of the traditional African diet. Cassava may contain from 225 to 1830 mg/kg of the nitriloside linamarin (10)

In 1962 Dr. John Morrone reported his results from using Laetrile with 10 patients suffering from "inoperable cancer," The treatments ranged from 4 to 43 weeks in length, and a range of 9 to 133 gms Laetrile was given through intravenous injections, Morrone concluded his report: "The use of Laetrile... in 10 cases of inoperable cancer, all with metastases, provided dramatic relief of pain, discontinuance of narcotics, control of fetor [stench from a tumor], improved appetite, and reduction of adenopathy [swollen lymph nodes]. The results suggest regression of the malignant lesion.... No other side effects [other than transient episodes of low blood pressure] were noted except slight itching and a sensation of heat in the affected areas, which was transitory in all cases." (16)

In 1994, P.E. Binzel published his results from treating cancer patients with Laetrile between 1974 and 1991. He used a combination of intravenous and oral Laetrile. Intravenous doses started with 3 gms and worked up to 9 gms. After a period of months, oral Laetrile, I gm at bedtime, was begun in place of the injections. Binzel also used various nutrient supplements and pancreatic enzymes, as well as a low animal-protein, no junk-food diet as part of his regimen. Out of a series of 180 patients with primary cancer (non-metastasized, confined to a single organ or tissue), 138 were still alive in 1991 when he compiled his treatment results. At that time, 58 of the patients had been followed for 2 to 4 years, while 80 had a medical follow-up from 5 to 18 years. Of the 42 patients who had died by 1991, 23 died from their cancers, 12 from unrelated causes, and 7 died of "cause unknown."(8)

Among his metastatic cancer patients, 32 of 108 died from their disease, while 6 died of unrelated causes, and 9 died of "cause unknown." Of his 61 patients still alive in 1991, 30 had a follow-up between 2 and 4 years, while 31 had been followed for 5 to 18 years. (8) Binzel's results are impressive. Some of the individual patients discussed in his book were still alive (and well!) 15-18 years after their initial Laetrile treatment. Binzel also notes that none of the cancer diagnoses were made by him (a small town, "family doctor") - all patients had diagnoses from other physicians. Many had already suffered the ravages of standard "cut-bum-and poison" (surgery/X-ray/chemotherapy) medicine before being given up as hopeless cases by orthodox doctors.

Other physicians who have worked with Laetrile have also reported favorable results using it. Thus Manuel Navarro, M.D., former professor of medicine and surgery at the Univ. of Santo Tomas in Manilla wrote in 1971: "1... have specialized in oncology [the study of tumors] for the past eighteen years. For the same number of years I have been using Laetrile-amygdalin in the treatment of my cancer patients. During this eighteen year period I have treated a total of over five hundred patients with Laetrile-amygdalin by various routes of administration, including the oral and the I.V. The majority of my patients receiving Laetrile-amygdalin have been in a terminal state when treatment with this material commenced.

Dr. Hans Nieper is a world famous oncologist and the developer of the standard anti-cancer cytotoxic drug cyclophosphamide. In 1970 he co-authored a brief paper on Laetrile with Dean Burk, in which they stated that "...in the treatment of cancer, the active principle of nitrilosides is to be used mainly in prophylaxis [prevention] and early protective therapy.... On the other hand, the complete atoxicity [lack of toxicity] of this method of treatment, which is maybe nothing else but a rediscovered natural principle, permits the unlimited use of this substance." (18) In 1972 Nieper told reporters while in the U.S.: "After more than 20 years of such specialized work, I have found the non-toxic Nitrilosides - that is, Laetrile - far superior to any other known cancer treatment or preventive. In my opinion it is the only existing possibility for the ultimate control of cancer." (11)

Ironically, one record of Laetrile's high degree of safety, when properly used, was provided by a group of Laetrile opponents, led by Dr. Charles Moertal. In 1981 in JAMA, Moertal and co-workers wrote: "In our study, intravenous amygdalin was found to be free of clinical toxicity and no cyanide could be detected in the blood...In summation, the administration of amygdalin according to the dosages and schedules we employed seems to be free of significant side-effects. This conclusion appears to be validated by early observations in phase II study of 44 Mayo Clinic patients receiving intravenous amygdalin therapy and 37 receiving oral therapy who have not experienced any symptomatic toxic reaction." (27) Yet in an obvious display of their anti-laetrile bias Moertal et al concluded the one paragraph summary abstract on the first page of their paper with the statement "A definite hazard of cyanide toxic reaction must be assumed, however....," even though they state plainly in the conclusion of their report that they didn't find any Laetrile toxicity! When Laetrile is used therapeutically, it is usually given either intravenously, at doses from one to nine gms, or orally, at doses of 500mg, two to four times daily. To maximize the safety and effectiveness of oral Laetrile, it is imperative that it be taken on an empty stomach, either two hours before or three hours after a meal. Never combine oral Laetrile with raw almonds or raw apricot kernels, or raw vegetable or bean sprouts, as these are high in the cyanide-releasing beta-glucosidase enzyme. According to Krebs (the "father" of Laetrile), approximately 50-200 mg/day of Laetrile, taken like vitamins (which Krebs believed Laetrile to be) on an open-ended, on-going basis, will provide a cancer-preventive effect. Assuming one has not eaten for at least three hours before retiring, taking a small Laetrile preventive dose at bedtime may be the best strategy. Laetrile ingestion may occasionally cause a temporary low blood pressure reaction due to formation of thiocyanate, a powerful blood pressure lowering agent. (30)

 

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