"When I tell you these stories, do you see it, or do you just write it down?"
   
                                         -Zuni speaking to an Ethnobotanist

Psychoactive Plant Based Drugs

  Alcohol  Atropine  Caffeine  Cocaine  Marijuana  Mescaline  Opiates Strychnine

 

  The table, Seminole Canyon, Texas

    Indios family, Sierra Madre del Sur, Mexico

         7000 years cutting table and altar

"The stump of the thigh, which was very fleshy, presented a dreadful and large surface of mangled 
flesh.  All the service I could render this unfortunate man was to put dressings over the part and give 
him drink." 
                                   --An amputation, in 1797, by Surgeon Robert Young aboard the HMS Ardent (6)

Opiates: Heroin, Morphine from Papaver somniferum L. (Papaveraceae).

Morphine, heroin and other derivative opiate category drugs from the Opium poppy.

Process: The crude drug was prepared by drying and powdering the milky juice extracted from the almost ripened seeds of Papaver somniferum L..  

Uses: Opiates are anti-diarrhea, anti-dysentery narcotic analgesics and have been useful tools in medicine for thousands of years.  they are the premier analgesic for pain and suffering.   Opiates also produce feelings of euphoria, a sense of well being and a broad array of psycho and physical side effects.  It is a highly addictive substance that leads to tolerance and dependence.  Humans have endogenous opiods that provide a gentler array of the same effects of plant and chemical based opiates.

In addition, analgesic qualities opiates are sedative, hypnotic, mood altering and effect mental clarity and physical response.   Physical effects include constipation, reduced respiration, slowed heart rate and perhaps pupil constriction.

Morphine, from Morpheus, the god of dreams,  was isolated from opium in the 1803.  This synthesis provided a more controllable and predictable drug for treating pain.  heroin was produced in 1874 as an improvement over morphine, but later proved to have all the undesirable side effects of morphine and was faster acting.  An analgesic dose of 5-10 mg. causes (almost immediately) the following Central Nervous System effects:  drowsiness, loss of inhibition, decrease sensory response, loss of anxiety, pain relief, pupil constriction and slightly depressed respiration, impaired concentration.  These effects usually lead to a dream laden sleep.

Function: Morphine is absorbed through mucus membranes and is typically injected under the skin.  At greater than analgesic therapy doses CNS effects are heightened.   A state of elation and euphoria may be displayed or felt.   this effect is immediate after injection.  A rush.  There is an sudden orgasmic feeling in the abdomen, a warm flush.   This orgasmic rush is not the present in people who snort or smoke opiates.  The users state of mind often dictates the degree of the rush.  If in an agitated, restless, depressed, excited state the rush is typically there.   Side effects include nausea,  nausea for addicts is addictive as it is the prelude to the euphoric state. 

Interestingly, morphine does not cloud thinking, impair physical coordination or slur speech.  

Chemistry:  alkaloids: morphine, codeine, thebaine, papaverine, narcotine and narceine.

 

Mescaline

Peyote, Lophophora williamsii (Lemaire) Coult, family Cataceae: Mescaline

Uses: Peyote is a member of the family Cataceae, a desert plant of religious significant to First People of Meso-America. Originally, the mescal bean was used as a ritual/religious hallucinogen, but due to its potential toxicity the bean was replaced with the extract from the Peyote cactus. Mescaline belongs to a family of psychoactive drugs called phenethylamines. Structurally similar to amphetamines, phenethylamines have stimulating as well as hallucinogenic qualities. By comparison with other hallucinogens peyote mescaline requires a more significant dose than say LSD to get the desired effect. A hallucinogenic effect from mescaline requires on average about 5mg. mescaline per kilogram body weight. A 150 pound person would require 325mg of the drug. LSD is over 3000 times more potent. The therapeutic use of this drug and other related hallucinogenic drugs including LSD for psychotherapy did not yield significant positive results in controlled studies with human beings. Studies suggest the plant extract is hypoglycemic, may improve endurance, courage and lesson hunger and thirst. Drug may not be addictive, but feelings of well-being may make the drug psychologically habit forming.

Through and act of Congress Native Americans have established the Native American Church that provides legal ritual use of peyote.

Chemistry: alkaloid mescaline, N-methlymescaline, N-formylmescaline, N-acetylmescaline and related alkaloids as well as hordenine, candicine, anhalamine, anhalanine and other related chemicals.

 

Cocaine, coca from Erythroxylon coca Lam., 
Family: Erythroxylaceae)

A psycho-stimulating alkaloid that inhibits uptake of Norepinephrine and Dopamine. It is euphoriant, hallucinogenic, anesthetic, bacterialcidal and ergogenic (increase work output).

Uses: Indigenous people of the eastern Andes have been using coca leaves from the shrub Erythroxylon coca for over 5000 years. Incas used the drug in rituals and ceremonies revering the Sun god. The leaves were chewed with a bit of lime or ash to raise the pH. Increasing the pH improves absorption of the active principle through the mucus membranes of the oral cavity. Spanish conquistadors outlawed the use of cocaine briefly, but gave it another try when they discovered their Inca slaved worked harder and longer on the drug. Sigmund Freud used cocaine to treat morphine addiction (Duke). Freud also recommended its use for treating alcoholism and depression. Vin Mariani a concoction of wine and cocaine was considered a 19th century cure-all. An Italian neurologist, Mantegazza once wrote: "I would rather have a lifespan of ten years with coca than a million centuries without coca." From there Pharmacist John Pemberton invented Coca Cola a beverage made with cocaine and caffeine. Parke Davis & Company offered cocaine inhalants, cocaine laced cigars and cigarettes. Soon there were Coke knock offs: Nerv Ola; Koca Nola and Cola nitida. Dentists gave painkilling cocaine tooth drops to babies cutting teeth. Prohibition of alcohol boosted the sales of cocaine products until at the turn of the century it was being widely abused. In 1910, President Taft labeled cocaine "Public enemy number one!" Laws were passed the local and national level banning cocaine use (including the 1914 Harrison Narcotic Act). Prohibition of the drug pushed underground where its use was restricted to musicians, artists and actors. Drug experimentation in the "Sixties" spawned a wave of increasing use and abuse. By 1990 surveys suggested that 23 million people had experimented with cocaine in their lifetime. Habitual users numbered over 1.3 million.

Accelerated Performance

Cocaine is extracted from the coca leaf and made into a paste. The paste is then converted to cocaine hydrochloride salt. This water soluble crystalline form may be snorted or mixed in drink. These forms of administration are not as potent as inhaling or injecting the drug. Cocaine hydrochloride however is heat degradable, and worthless as a "smoke". A ghetto chemist can percolate the hydrochloride out of the cocaine with an alkaline solution. The end result is freebase, crack or rock cocaine-an addictive substance that can be smoked, heightening the pharmacological effects of the drug. Intravenous injection or freebasing are the most potent ways to take cocaine. However, a mountain tribesman, chewing for three hours on cocaine leaves gets the plasma equivalent of a "Los Angelino's" after work "snort".

High School Users

It is reported that 1 out of twenty high school students have used cocaine at least once.  

Pregnancy and the Use of Cocaine

Cocaine passes easily through the placenta and impairs fetal development. Results are pre-term births, low birth weight infants and more frequent SIDS (Sudden Infant Deaths). Cognitive development is impaired and addiction and withdrawal symptoms are exhibited.

Alcohol (Ethanol: CH3-CH2-OH)

Solvent, Low lipid solubility, completely miscible in water partition coefficient between water and oil is 30 to 1.

Alcohol is fermented from carbohydrates by airborne yeast.  The end product of this yeast assisted conversion of sugar is alcohol and carbon dioxide. Alcohol has the shortest possible metabolic pathway, making it the fastest source of Kcalories from food. In contrast to other drugs, it takes a relatively large amount of alcohol to get the desired effect. Low lipid solubility of alcohol and high diffusion rate shortens the duration of effects because it does not bind to lipids as does longer acting drugs like Valium (diazepam). Alcohol enters the highly vascular, blood rich brain rather quickly...And more slowly in other tissues. Thus, the central nervous system effects of alcohol are quickly felt.

Ethyl alcohol (ethanol) is, in low doses a central nervous system stimulant, in moderate doses, a central nervous system depressant. Low doses of alcohol stimulates locomotor activity. If alcohol consumption is limited to an ounce or two this central nervous system effect is quickly dissimilated as alcohol eventually enters muscles and other organs reducing the concentration gradient between the brain and the blood. The rate of absorption of alcohol into the blood is fastest when it is ingested in a 15% to 30% solution common in wine. In concentrations above this level, alcohol depresses peristalsis and may produce spasm of the pyloric valve between the stomach and duodenum (entrance to the small intestine) slowing the assimilation of alcohol in the small intestine.. About 90% of alcohol is absorbed from the small intestine and only 10% from the stomach.. Food, especially protein and carbohydrates, slow the absorption of alcohol in the stomach.(5).History

Alcohol was probably one of the first drugs to be abused by primal man. It is a anodyne, that is: it relaxes, calms, soothes and comforts. It has an initial euphoric effect and reduces anxiety. These factors accounts for its desirability and universal use . The Moslem culture stands out for its staunch alcohol temperance.

Accidental fermentation of fruit juices, honey, potato starch and grain beverages in prehistoric times gave rise to the manifest use of alcoholic beverages seen worldwide today. Perhaps the oldest alcoholic beverage is Mead, a Paleolithic fermentation product of honey and water. Egyptians brewed and fermented wine and beer over 5700 years ago. By 800AD Arabs learn how to concentrate alcohol through distillation. The word alcohol is Arabic (alkuhl) meaning "something subtle".(4)

19th Century Anesthetic

At near the lethal dose alcohol was used as a general anesthetic during 19th century surgery.

"(Patients) would be given gin or rum...." "...The surgeons waded in blood, cutting off arms, legs and trepanning heads to rescue their fellow creatures from untimely deaths. To hear the poor creatures crying, "Oh, Dear! Oh, Dear! Oh, my God, my God!"        --Surgeon William Beaumont performing surgery after the battle of York Town, 1812. (6)

The duration of alcohol as an anesthetic is short lived and required swift and deft knife wielded by the surgeon. Although surgeons were renowned, too often their swiftness led to irrecoverable mistakes. Wrong limbs amputated. Organs incised and destroyed. Sepcis to putrefaction and/or contamination.

20th Century Diuretic for Treating Dropsy

A Russian physician once explained to me how in the old Soviet Union alcohol and Lily of the Valley was used to treat dropsy. Alcohol was administered intravenously as a diuretic and analgesic while Lily of the Valley (Convallaria majalis) was administered orally for its cardiac glycosides, stimulating the left ventricle contraction and dilation of coronary arteries. The diuretic property of alcohol, and the consequent pain of urine retention in the absence of a bathroom, is known to all who have tasted it.

Here are a few properties of alcohol and how it effects the central nervous system:

Chronic, high alcohol consumption increases homocysteine levels in the the blood, there is a link to higher incidence of cancer and Alzheimer's disease in people with high serum levels of homocysteine.  Vitamin B supplements lower homocysteine, especially B6, B 12 and folate (folic acid).    Moderate amounts of wine and beer may lower homocysteine levels (1 -2 servings).

Alcohol and Epilepsy

Alcoholism increases the effective anticonvulsant dose of Phenobarbital. This cross tolerance diminishes the effectiveness of barbiturates in alcoholics. Alcohol may enhance GABA (Gamma Amino Butyric Acid) action leading to anticonvulsant activity in seizure prone individuals (3). However, this seizure inhibition rebounds upon abstinence from alcohol. That is, neural discharge from the epileptic foci is increased and may lead to lethal consequences. A personal friend of mine, with a lifelong history of epileptic seizures, lost his life to a seizure that induced heart failure, shortly after we had applauded him for beating his drinking habit.

May reduce Serotonin Levels

Alcohol may reduce serotonin levels. This could induce dependence and initiate depression. In animal studies, increased alcohol consumption reduced serotonin.(9). In human studies, stimulation of serotonin or blockage of serotonin uptake diminished alcohol consumption. Serotonin increases also stimulated alcohol tolerance.(10)

Alcohol may diminish dopamine an important neural transmitter. This may help induce the hypothermic effect.

Inefficient Sleep

Thyrotropin-releasing Hormone (TRH)--an important hormone and neurotransmitter--may antagonize the effects of alcohol, causing, for example, a reduction of sleep time that was initially induced by the alcohol. One goes to sleep quickly under the influence of alcohol but does not sleep well or long. (Ibid. (3) p. 471.).

Alcohol stimulates locomotor activity at low doses and depresses the central nervous system at moderate to high doses. This psycholocomotor activity is facilitated by the increased transmission of dopamine when alcohol is consumed (Ibid.(3) P.579).

Alcohol Metabolism

The liver metabolizes 90% of the alcohol consumed. The other 10% is excreted in urine, lost to perspiration or exhaled from the lungs. In the liver, alcohol dehydrogenase (ADH) oxidizes alcohol to acetaldehyde. To a lesser degree alcohol is also oxidized by catalase and mixed function oxidases to acetaldehyde. Alcohol dehydrogenase is also found in small amounts in the stomach where some oxidation occurs. Women typically have less alcohol dehydrogenase than men, especially in the stomach, and are prone to more severe and prolonged effects of alcohol. Acetaldehyde is toxic but is quickly converted to acetate and moved to the hepatic venous blood to combine with coenzyme A to form acetyl CoA From there it enters the citric acid cycle to be oxidized to carbon dioxide and water yielding 7 Kcalories of energy per gram of alcohol. The average person metabolizes from 6-8 grams of alcohol per hour and up to 170 grams in 24 hours.

As yet, there does not appear to be a chemical or mechanism to speed this alcohol clearance thereby shortening the time from intoxication to sobriety. (For greater detail see P.627-628 resource (3).

Alcohol and Pregnancy

Alcohol readily passes into fetal circulation subjecting the fetus to the profound effects of the drug.

This may lead to fetal alcohol syndrome, abnormal changes in the infants brain.leading to physical and mental handicaps.

Prenatal alcohol consumption of alcohol may induce Attention Deficit Hyperactivity Disorder (ADHD) in children. (8).

Alcohol Abuse

Approximately three out of every 4 adults in America drink alcohol.. It is suggested that this is done to reduce tension and anxiety in a modern informational society. This same excuse holds true for common use in industrial, pre-industrial, agricultural and paleolithic societies. Fifteen percent of alcohol users in the United States abuse the drug. These are people who have lost control over the consumption of alcohol and are chronically intoxicated. This is the most severe form of substance abuse in America and most other countries. It is second only to cigarette consumption as a cause of death. Half the arrests in the country are alcohol related. There are over 24,000 alcohol related automobile fatalities and over 11 million other accidents due to the over consumption of alcohol. Alcohol is the most significant contributing factor to divorce, child abuse, poverty and abandonment. According to Buck and Harris 1991, over $136 billion dollars are drained from the economy by alcohol abuse due to lost production, illness, welfare, accidents, property damage and medical expenses. Alcohol end products are oxidized to formic acid and formaldehyde which are toxic to the optic nerve.

Fatalities

As a cause of death by poisoning alcohol is second only to carbon monoxide. Alcohol induced edema (swelling) at the base of the brain eventually causes death. College drinking competitions, 21st birthday celebrations and "chugging" of alcohol by young adults causes rapid consumption of large amounts of alcohol too often leading to death. Barbituates have an additive, synergistic effect with alcohol and can induce fatal physiological consequences. by alcohol poisoning.

Alcoholism Damages all Organ Systems

Excessive, chronic consumption of alcohol has adverse effects on the liver and kidneys leading to dysfunction. Excessive drinking depresses the appetite (whereas a single drink may stimulate it).

Alcoholic beverages have no nutritional advantage, and are nearly devoid of nutrition save for the empty calories. Alcohol may induce cancer of the esophagus, stomach, liver, breast, tongue , mouth oropharynx.. It may cause bleeding in the organs of the digestive systems. Liver cancer has a direct association with cirrhosis caused by excessive alcohol consumption. Additional primary and secondary tumors are seen in people who continue to abuse alcohol while trying to survive cancer.

Alcohol upsets fat synthesis and leads to fat accumulation in the liver perhaps a precursor to cirrhosis of the liver (approximately 30 thousand people die every year in the United States from cirrhosis of the liver).

There is a correlation between alcohol consumption and increased incidence of breast cancer in women.

Heart Disease Protection

Moderate intake of alcohol (2 ounces 90 proof alcohol) may reduce risk of heart attack perhaps by increasing serum levels of HDL cholesterol and its subfractions HDL2 and HDL3. (1) Alcohol consumption in greater amounts has no beneficial effect and may increase the risk of liver disease, cancer and accidental death.. (2).

Whereas, light drinking may be beneficial to the heart, heavy drinking may cause cardiomyopathy, damage to the heart muscle. This may lead to arrhythmia and eventually congestive heart failure.

Alcohol induces thiamine deficiency and this stimulates the destruction of the heart and other organs. As little as three drinks per day can cause hypertension leading to atherosclerosis and heart disease.

Sexual Dysfunction and Disease

Alcohol abuse may lead to impotence. In men, alcohol abuse may cause testicular atrophy, drop in testosterone, shrinkage of the prostate and testicles, loss of body hair and loss of sexual interest. In women, ovulation may be interrupted and ovarian function disrupted leading to dysmenorrhea or amenorrhea. Women who consumed six or more drinks per day were subject to more gynecological surgery.

Alcohol Induced Hypothermia

Vasodilation caused by alcohol at first flushes the skin and warms, but these dilated peripheral blood vessels too soon give back their warmth to the environment and can cause greater heat loss than gain. After the warm-up a person gets cold. Do not use alcohol to warm someone, use hot soup. Vasodilation caused by alcohol is evidenced by broken blood vessels on the faces of alcoholics. Alcohol diminishes dopamine an important neural transmitter. This may help induce the hypothermic effect.

Central Nervous System Effects

Alcohol relaxes and inhibits. The first cerebral functions to be impaired are locomotion (walking), fine motor skills, talking (speech). Abusive drinkers damage nerves, lacerate the brain and induce subdural blood clots (probably induced by drunken falls). Brain scans of alcoholics showed brain shrinkage and death of some of the corpus callosum and subcortical white matter (Marchiafava-Bignami disease). Alcoholics eventually exhibit dementia, poor speech articulation and locomotor impairment. The loss and shrinkage of brain matter in alcoholics leading to impaired behavior and mental processes. Brain structure is destroyed because alcohol inhibits the synthesis of RNA and brain protein..

Some brain damage is irreversible. Some alcoholics who abstain from alcohol experience as reversal of fortune: the re-myelination and growth of the brain.. Cerebellum destruction is not reversed and locomotor loses are manifested.

Wernicke-Korsakoff syndrome in alcoholics cause peripheral neuritis and painful sensitivity in the victims lower extremities and may migrate in later stages to the upper extremities. In later stages there may be loss of vision, blind spots, optic nerve damage and acute toxic delirium and loss of memory (amnesia). Alcohol induced thiamine deficiency and malnutrition may be contributing factors. Thiamine therapy may reverse amnesia.

Women more Susceptible to Brain Damage

Research shows women are more likely to have brain damage than men. Women do not metabolize alcohol as efficiently as men and attain higher peak levels. Higher peak levels are due to the higher muscle to fat ratio in women leading to lower blood vessel volume. Fat has less water than muscle so more alcohol is in the blood of women due to alcohol's hydrophilic and lipophobic characteristics. The lack of alcohol dehydrogenase in the stomach also is a contributing factor in women(11). Thus, alcohol is in higher volume and thus more bio-available in women.

Treatment, Withdrawal and Alcoholics Anonymous

Alcohol abstinence may lead to withdrawal symptoms and physiological disorders. Spontaneous withdrawal without hospitalization may be fatal. Typically, detoxification will start in a hospital with compulsory AA attendance. Drugs are targeted at reducing the craving and withdrawal symptoms. A focus is on quieting the discomfort of abstinence. Treatment has limited effectiveness. There are numerous therapies including a whole pharmacopeia of anti-alcoholism drugs, but what seems to work best is counseling and self- help, an overpowering will and motivation to abstain. Fifteen year studies in the United States and Sweden show that 30- 35% of alcoholics quit of their own free will (spontaneous abstinence) without drugs or therapy (12) (13). It is difficult to validate the 75% success rate claimed by Alcoholics Anonymous. An AA counselor friend of mine claims the 75% success rate is not valid. He has been a member for over ten years ans suggests the rate for retention beyond five years is more like 3-5%. I once asked him why he went to so many meetings: "Do you go to stave off your craving?" His answer was, "Do you shop for groceries because you are hungry. No. You shop for groceries because you will become hungry without them.. I go to AA meetings not because I'm thirsty for alcohol., but because if I don't go I will become thirsty for it. It's the fellowship that keeps me sober."

Alcoholics Anonymous WEB SITE: http://www.alcoholics-anonymous.org/

Kcalory Values of Alcoholic Beverages (1)

Resources:

(1) McArdle, William, Katch, Frank, Katch, Victor: Exercise Physiology. Williams and Wilkins. P.456-463; 1996.

(2) Fuchs, G.S., et al.: Alcohol consumption and mortality among women. New England journal , 332:1245, 1995.

(3) Feldman, Robert, Meyer, Jerrold, Quenzer, Linda: Principles of Neuropsychopharmacology; Sinauer. P.471. 1997.

(4) Roueche, B. Cultural factors and drinking patterns. Annals of N.Y. Academy of Sci..133, 846-855., 1966.

(5) Pohorechy, L.A. and Brick, J. Pharmacology of ethanol. In Psychotorpic Drugs of Abuse, ppl 189-281. Pergamon Press, N.Y.

(6) Williams, Guy, The Age of Agony. Academy Chicago Publishers 1986.

(7) Buck and Harris, 1991. Neuroadaptive responese to chronic alcohol. Alcohol. Clin. Exp. Res., 15, 460-470.

(8) Nanson and Hiscock. Attention deficits in children exposed to alcohol prenatally. Alcohol Clin, Exp. Res. 14, 656-661, 1990.

(9) Frankel and LeBlanc (1978) Effect of p-chlorophenylalanine on the loss and maintenance of tolerance to ethanol. Psychopharmacology, 56, 139-143.

(10)Roy and Linnoila (1989) CSF studies on alcoholism and related disorders. Prog. Neuropsychopharmacolgy. Biol. Psychiatry Res., 24, 187-194.

(11) Whitney and Rolfes, Understanding Nutrition 7th edition; West Publishing. P.266. 1996.

(12) Ojesjo (1981) long term outcome in alcohol abuse and alcoholism among males in the Lundby general population, Sweden.. British Journal of Addiction, 76, 391-400.

(13) Vaillant: (1983) The natural history of alcoholism. Harvard University Press, Cambridge MA.

Caffeine

Caffeine is a lipid soluble compound, a methylxanthine.

Caffeine, a stimulant, is found in coffee, tea, mate leaves, guarana paste, cola nuts, soft drinks, chocolate and numerous other plant products. Caffeine is also found in pharmaceutical preparations including Anacin, Excedrin, Vivarin and No Doz. The liver converts caffeine to metabolite, 95% of which is excreted through the kidneys in urine.(1)(2)(3)(4)(6)

Pure caffeine is obtained as a by-product from the manufacture of caffeine free coffee (6)

Metabolic Activity

Caffeine increases:

Caffeine decreases:

*-muscle glycogen depletion in liver and muscles (trial was with 330mg caffeine 60 minutes before exercise)(7)

Sensitivity and Dependence

A few people are less sensitive to caffeine and may not be as severely effected by it as others.

A few have weak tolerance and are severely effected.

Caffeine dependence may develop where when a person attempts to stop drinking coffee may experience headaches, fatigue, poor concentration, fatigue and compromised motor activity

Craving for coffee may be so severe as to leave the abstainer dysfunctional. Anxiety and depression may be manifested. Chronic and large volume consumption of caffeinated beverages and lead to "caffeinism". symptoms include insomnia, restlessness and anxiety with increased heart rate, in the extreme, a person may suffer from severe psychological disturbance (when consuming over 10 cups of coffee per day or 1000mg of caffeine)

Therapeutic Uses

Caffeine acts synergistically with aspirin for treating non-migraine headaches. Cafergot is a combination of caffeine and ergotamine and may be used for treating migraines.

Newborn infants who have periodic cessation of breathing (apneic episodes) may treated with caffeine.

As a stimulant there is the intriguing possibility that caffeine may actually calm hyperactive (HADD) child who had been taking Ritalin or Prozac.

MYTHS

MYTH 1: Caffeine and Alcohol: Coffee does not speed alcohol metabolism.. It is not a cure for a hangover.

MYTH 2: Caffeine and improved athletic performance: As a stimulant caffeine may help sprinters. But it may be detrimental for endurance or distance athletes, and athletes who participate in events that go beyond a few minutes. Caffeine increases energy expenditure by stimulating the adrenal glands to release epinephrine. Naturopathic Physicians suggest that long term, frequent use of caffeine may exhaust the adrenal glands.

CAUTION: Caffeine products are not a good substitute for water because it is a diuretic actually increasing excretion of liquids and salts (electrolytes) from the body. Caffeine also raises blood pressure and kicks up metabolism

Effects on Women, Pregnancy and Children

A caffeine imbibing child who drinks two cokes per day and weighs approximately 60 pounds receives the metabolic equivalent of eight (8) cups of coffee, making the youngster sleepless, restless and prone to all the physiological stressors of caffeine consumption.

Pregnant mothers should curtail their caffeine consumption because there is evidence that heavy coffee drinkers may have children with lower birth rate.

Nursing Mothers: Caffeinated coffee drinking during lactation may make the breast fed youngster irritable and restless, perhaps unable to sleep. Even one cup per day may interfere with the ability of the child to absorb and use iron.

Fibrocystic breast disease is sometimes associated with caffeine consumption. Vitamin E therapy and abstinence from caffeine has been a helpful therapy.

Decaf Coffee

Methyl Chloride decaffeination process may increase the incidence of cancer by one in one million in coffee drinkers who imbibe 2-3 cups of coffee per day.

Water process decaffeination is considered by most consumers as safer.

Warning: decaffeination does not remove all xanthine chemistry from coffee. Acids and alkaloids are little effected.

Osteoporosis and Caffeine Consumption

Osteoporosis may be accelerated by caffeine consumption because of the drugs ability to increase calcium excretion. Diuretic effect of caffeine increases excretion of calcium, potassium, magnesium, iron and zinc.

Heart Disease

One 1990 study reviewed evidence linking caffeine consumption with an increased incidence of coronary heart disease. Increased blood pressure is indicative of the stress that caffeine can put on the heart. (Benowitz, 1990, Clinical Pharmacology of Caffeine, Annual Reviews of Medicine; pp 227-28.)Tyramine Interaction with Caffeine

If you are on a tyramine controlled diet avoid all consumption of caffeine. Caffeine increases the availability of Monoamine Oxidase inhibitors, with less MAO available tyramine is not inactivated and may lead to headaches, hypertension and possibly death.

Pharmacology

Caffeine is completely absorbed in the digestive tract within approximately 45 minutes. Absorption occurs in the stomach and small intestine, with the small intestine being the main site of absorption. The half life persistence of caffeine in a human is from 2.5 to 4.5 hours. People who drink throughout the day may experience rising plasma concentrations of caffeine. Most clearing occurs during sleep. Caffeine is metabolized in the liver and most of the metabolites are excreted through the urine, about 5% or less through the feces. Less than 2% of caffeine is excreted unchanged. Caffeine metabolites are: 1-methyluric acid; 1,7-dimethyluric acid, 1-methylxanthine, paraxanthine, and 5k-acetylamino-6-formylamino-3-methyluracil. (Source Principles of Neuropsychopharmacology, Feldman, Meyer, Quenzer; Sinauer Associates, Inc. 1997.)

Behavioral Effects

In addition to what has been mentioned previously, caffeine may improve performance in several measurable tasks. A survey in Great Britain of 7000 men and women caffeine drinkers were tested for their performance of several tasks. The four tasks: simple reaction time, choice reaction time, incidental verbal memory, visual/spatial reasoning. Results showed an improvement in task performance significant to caffeine consumption. There was improved performance in each task with caffeine drinkers. Optimum improved performance for all four tasks appeared to require 4 cups of coffee equivalent per day. Thus, one might obtain increased performance at the cost of several physiological deficits such as increased arousal, fatigue, anxiety, increased respiration and elevated blood pressure

Caffeinism

Caffeinism describes chronic consumption of high doses of caffeine. Symptoms include nervousness, insomnia, restlessness, tachycardia. At doses over 1000mg/day (over 12 five ounce cups of coffee)severe psychiatric stress may result. Caffeine may trigger premature left ventricular contractions. Too much caffeine, a powerful diuretic may upset thermoregulatory mechanisms in the body which could be deleterious in a hot or cold environment.

Veterinarian

Has been used with animals as a diuretic, cardiac and respiratory stimulant (6)

Athletic Performance

Ingestion of 330 mg to500 mg of caffeine approximately one hour before endurance exercise may spare liver and muscle glycogen by specific ergogenic effect on skeletal muscles. Caffeine may increase muscle fiber (myofibril) sensitivity to Calcium thereby making the mineral more available to muscles improving muscle contraction efficiency. Caffeine acts directly or indirectly by stimulating the adrenal glands to release epinephrine as an antagonist of the adenosine receptors on fat cells. This fat mobilizing mechanism is facilitated by caffeine stimulated catecholamine release from the adrenal medulla. (7)

CAUTION: IMPROVED PERFORMANCE IS NOT CONSISTENT AND MAY NOT BE FACILITATED IN HABITUAL COFFEE DRINKERS..6. The Merck Index; 11th Edition; Merck &Co., Inc. p.1634. 1989.

7. McArdle, William, Katch, Frank, Katch, Victor: Exercise Physiology. Williams and Wilkins. P.456-463; 1996.



Strychine and Brucine from (Strychnos nux vomica L.)

Family: Loganaceae

Glycine is a major inhibitory amino acid neurotransmitter in the Central Nervous System.  Glycine's primary pathway is the inhibition of spinal cord interneurons.  Some of these neurons are called Renshaw cells and they mediate recurrent inhibition of spinal motor neurons (GABA too plays an important role in recurrent inhibition).  Glycine is also implicated in a number of brain pathways too, playing an important role in behavioral and physiological regulation.  

Strychnine is a potent alkaloid from the seeds of Strychnos nux vomica and is used to study glycine pharmacology.  It is a glycine receptor antagonist.  Antagonist strychnine binds to the alpha 1 isoform of the glycine receptor, which also contains the agonist receptor site.  Thus, strychnine is a marker for the glycine receptor complex and was used to map the distribution of glycine receptors in the brain and spinal cord. 

In clinical studies, strychnine heightens perceptual acuity, including visual, auditory and cutaneous.  It initiates convulsions and spasms and induces hyperalgesia (supersensitivity to pain) associated with convulsions.  Its antagonist effect on glycine receptors increases the respiratory rate, causing bradycardia and hypertension.  Convulsion are initiated by visual and acoustic stimuli.  In rat studies, a mere clap of the hands sends a strychnine dosed rat into wild, convulsive activity.  The medial vestibular nucleus is effected causing disequilibrium.

The supersensitivity effect of strychnine as it antagonizes the neurotransmitter inhibitor glycine, may result in the folk medicine use of strychnine as an aphrodisiac.

The chemical has been used down through history as a rodent poison, a rat poison, and is today used in poisonous rat food that may be ingested by unsuspecting children leading to fatal results.

Nux vomica seeds also contain the similar but less potent alkaloid brucine.