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SPECIAL REPORT on EPHEDRINE:

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The scientific facts behind ephedrine and our top picks for safe, healthy alternatives to help to reach your desired weight-loss goals.

Ephedrine is classed as a "beta-adrenergic agonist," which means it works on adrenergic receptors on the surface of fat cells, which ultimately causes a breakdown of fat within fat cells. In a nutshell, you're likely to lose greater amounts of fat when you take it than when you don't. Research clearly shows it aids weight loss and also increases energy expenditure. Thus, because of all this good news, ephedra is one of the most widely sold weight-control products on the market today.

The problem with that is ephedrine works — that is, it works almost as well as what might be classified as a "drug." (In fact, ephedrine, the active component in the herb ephedra and/or ma huang, is classified as a drug! So, on one side, you have the major, billion-dollar pharmaceutical companies waging a war against ephedra being sold as an over-the-counter supplement, instead of as a drug (so they can make money on it). And on the other, you have general public concerns over the safety.

Yes, we obviously have some issues, but is it really a matter of safety? I don't think so. When compared to many of the approved prescription drugs, ephedrine is one of the safest compounds available. In fact, many pharmaceutical companies use synthetic forms of ephedrine (look for pseudoephedrine, for example) in their over-the-counter cold and allergy products, which many of us use whenever we're sick.

In my opinion, the media stories about adverse reactions (including deaths allegedly associated directly with the use of ephedra or ephedrine) have been blown out of proportion. Few compounds share ephedrine's extraordinary safety record. The facts are that the deaths associated with ephedrine use clearly stated the individuals consumed levels way above those recommended (or even considered sane) by nutritional practitioners. Like anything else in life, there's no escaping the law of toxicology, which says too much of anything, even apple pie or water, can hurt you. Therefore, I can't stress enough that more is not better with anything, and that includes supplements!

Think of this way: when you take your car in to change the oil, you'd never say to the technician, "Hey, since I'd like my car to run a little better, instead of the normal 5 quarts, why not throw in 10?!" Nope. Even your car doesn't work this way... Let me say it again: more is not better!

Another part of the problem comes to light with the FDA's proposal to reduce the levels of ephedrine-based products sold on the market, which has been seriously objected by millions of people who use ephedrine regularly. So, what's the solution? Actually, I'm in agreement with the FDA's call for a mandatory daily usage limit on all ephedrine-containing products. But pulling it from the market altogether is, I believe, too hard-lined. I don't feel that a few individuals who choose not to follow proper usage instructions and over-abuse the daily limit should spoil the availability of this supplement for everyone.

As you can see, I am a supporter of the benefits of ephedrine. It simply doesn't deserve the bad rap the media gives it. But I do not advocate using it regularly either. Reason is with any stimulant, there is a downside. Overuse (or abuse) can lead to an over-stimulated adrenal system, which often leads to lethargy, reduced immune system functioning, or the dreaded "I wish this ephedra would wear off so I could get some sleep" feeling. If you have used ephedrine regularly for an extended period of time (more than three or four weeks at a time), then I know you follow me.

If you are sensitive to ephedrine and cannot tolerate its side effects, as literally millions of people can't, it may be best to avoid it altogether. Instead, consider trying some other supplements for energy and fat-loss support. The herbs ginseng and cordyceps and the amino acid tyrosine seem to support energy enhancement — both physical and mental. And supplements like Citrus aurantium, good old caffeine or the herb guarana, and an exciting new ingredient called Coleus forskohlii may help the body burn more calories (in a process called thermogenesis), leading to more fat burned. And best of all, you'll be able to get to sleep at night, and you won't feel that creepy, tingly sensation crawling over your head that comes with ephedra use.
 
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Ephedrine (ephedra)

Ephedrine, or ephedra as it is also called is very controversial drug which has been used for fat-burning for some time now. It cannot be stated clearly enough that this drug can have disastrous results even death if it is used by the wrong people. You should not use any supplement containing ephedrine it you fall into the following categories:

pregnant, nursing, high blood pressure, heart, liver or thyroid disease
or phychiatric disease, diabetes, anemia or nervousness

Over 800 injuries including 50 deaths have been reported as being caused by ephedra. Most of these cases involve heart attacks or high blood pressure leading to bleeding in the brain or stroke. To read more on this as well as FDA recommendations, please visit the following ephedrine-ephedra site.

No-one doubts that this potent stimulant has great medical benefit. So does marijuana. But ephedrine needs regulation and control - something that has not happened so far. It is likely that with proper control, this drug would not get into the hands of people to whom serious damage may result. Ephedrine is not the problem, eduaction and control are.


Where does ephedra come from?

Ephedra is a shrub-like plant that groes in arid regions of Asia. The leaves, when dried, have been used medicinally in asthma medications.

Ephedrine side effects

The FDA has received more than 800 reports of problems associated with ephedrine including:

hypertension (elevated blood pressure)
palpitations (rapid heart rate)
neurophathy (nerve damage)
myopathy (muscle injury)
psychosis
stroke
memory loss
heart rate irregularities
insomnia
nervousness
tremors
seizures
heart attacks
death


The number of cases seen to be caused by this drug has caused wide-spread panic and been blown out of proportion. The numbers quoted are probably far fewer than those caused by other freely available over-the-counter drugs available today. People do have reactions to all sorts of things. Some people can die if they eat peanuts. Ephedrine is a drug. It is classed as a drug. It needs to be respected as a drug.

Be aware that ephedrine...

...is found in many fatburners available on the market. Since this drug is taken from natural plants like Ma Huang, companies do tend to advertise their products as natural (implying safe).


And finally

I would not advise anyone to take supplements containing ephedrine or ephedra without their doctors consent. If you do, you run risks, and some of these are very serious. If however, you do decide to buy this stuff without medical advice, or even against medical advice, please start off on very low dosages. Problems that may arise will robably exert smaller effects so that you can gauge how you feel before moving up to recommended doses. If however, you do have side effects, then don't delay, see your doctor
 
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FDA Investigates Herb Ephedra


by Cathy Wong

Results from a study conducted at the University of California, San Francisco and funded by the Food and Drug Administration (FDA) were released on November 6th, more than six weeks prior to the scheduled publication date in the New England Journal of Medicine. Researchers examined the safety of popular dietary supplements containing ephedra and concluded that they pose serious health risks to some consumers, indicating a need to identify risk groups and establish guidelines for safe daily doses and warnings.

Consumers have been surprised by the urgency of the preliminary report. The reason is that ephedra is a common ingredient found in herbal preparations for asthma, weight loss, athletic performance, and cold and allergy medications. Furthermore, the appearance of side effects not only in people with existing health conditions, but even in young adults with no prior health conditions have caused concern. This article will provide an in-depth examination of the uses and action of ephedra, safety and regulatory issues, and possible reasons for the adverse effects reported by the study.

Traditional and Clinical Use of Ephedra

Ephedra is an important herb in the Chinese medical tradition, with over 4000 years of clinical use as a primary treatment for asthma, bronchitis, cough with difficulty breathing, joint symptoms, inability to perspire, swelling, and pain in the bones. It has long been recognized in China, Germany, Japan, and India as a herb that can treat the common cold, bronchial asthma, hay fever, and allergy.

In contemporary China, ephedra is often a component of a multi-herb cold formula made by boiling ephedra with cinnamon twig, licorice root, and almond. In Germany, it is a major ingredient in licensed prepared medicine for respiratory conditions. The World Health Organization (WHO) has found the following uses of ephedra preparations to be supported by clinical data: treatment of nasal congestion due to hay fever, allergic rhinitis, common cold, sinusitis, and as a bronchodilator in treatment of bronchial asthma. In the United States, ephedra is considered a dietary supplement under the Dietary Supplement Health and Education Act of 1994 (DSHEA).

Supported by a long history of clinical use in established systems of traditional and conventional medicines and animal and human research studies, ephedra is sold in health food stores as an infusion, tincture, or extract in capsules or tablets and prescribed by licensed acupuncturists, herbalists, and naturopathic doctors.

Ephedra is also found in common conventional cold medications.

Aside from its proven use, ephedra is a main component of many herbal preparations for weight loss, athletic performance, and physical and mental stimulation.

Pharmacological Action of Ephedra
The main constituents of ephedra, notably ephedrine and pseudoephedrine, are plant alkaloids that are responsible for the ephedra's medicinal action. These alkaloids can cross the barrier protecting the brain from unwanted chemicals in the blood and mimic activity of the sympathetic nervous system (“fight or flight”) by interacting with various neurotransmitter receptors. Specifically, it enhances the release of the neurotransmitter norepinephrine and stimulates alpha and beta–adrenergic receptors. The problem with this non-specific stimulation of adrenergic receptors is that while the desired receptors (beta-2) in the lungs are stimulated to open the airways, other types of receptors are also stimulated, including the beta-1 receptors in the heart that increase heart rate and force of contraction, and the alpha-1 receptors that increase blood pressure and decrease circulation to the renal system and other parts of the body.

Epinephrine, which is similar to ephedrine but much more active and short-acting, was once a conventional treatment for asthma. It was replaced by current asthma medications which are able to act more selectively on beta-2 receptors.

Side Effects and Contraindications of Ephedra
Non-specific stimulation of adrenergic receptors means that ephedra should not be used in people with anxiety and restlessness, high blood pressure, glaucoma, impaired circulation of the cerebrum, prostate adenoma with residual urine accumulation, pheochromocytoma, and thyrotoxicosis.

Common side effects resulting from the stimulatory effects of ephedra include headache, irritability, restlessness of muscles, nausea, sleeplessness, increased heart rate, urinary disturbances and vomiting. Higher dosages may result in drastic increases in blood pressure and cardiac rhythm disorders.

Dependence has been suggested as a possible result of extended intake. Although products containing ephedrine are listed as addictive by the International Olympic Committee, later analysis at the U.S. National Institute on Drug Abuse suggests that the potential for addiction is minimal and did not recommend imposing stricter regulation.

Pregnancy: Ephedra should not be used during pregnancy or lactation.

Drug interactions:

Ephedra has an additive effect on the nervous system when used in conjunction with caffeine, decongestants, and other central nervous system stimulants.

Cardiac heart glycosides or halothane: disturbance of heart rhythm

Guanethidine: enhancement of the effect on the sympathetic nervous system

MAO inhibitors greatly raise the action of ephedrine on the sympathetic nervous system.

Secale alkaloid derivatives or oxytocin: development of high blood pressure.

Overdose: Life threatening poisonings are seen with very high dosages of the drug (over 100g, lethal dosage with oral administration corresponding to approximately 1-2 g L-ephedrine). Signs of poisoning include severe sweating, enlarged pupils, spasms, and increased body temperature. Heart failure and suffocation are causes of death due to overdose.
 
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Over 800 injuries including 50 deaths have been reported as being caused by ephedra. Most of these cases involve heart attacks or high blood pressure leading to bleeding in the brain or stroke. To read more on this as well as FDA recommendations, please visit the following ephedrine-ephedra site.
"Are reported as being caused by ephedra." Key words, there. With any new drug, and millions of users, you're going to see something like this. Everyone's afraid of it. It's safer than caffeine.


No-one doubts that this potent stimulant has great medical benefit. So does marijuana. But ephedrine needs regulation and control - something that has not happened so far. It is likely that with proper control, this drug would not get into the hands of people to whom serious damage may result. Ephedrine is not the problem, eduaction and control are.
I agree with the last sentence except for the "control" part. And they're completely wrong about ephedrine not being controlled; it's a List 1 substance. Control will NOT keep ephedrine from getting into the hands of "people from whom serious damage may result." It will simply take it out of the hands of legitimate users. The same is true with prohibition of any substance. Make it illegal, you increase: 1)Crime, 2)Impurities in the drug (which are almost always the main cause of death), 3)Clog in the prison system (the murderers and rapists go out, the pot smokers go in), 4)Misinformation ("It's illegal/controlled so it must be evil"), and 5)Infringements on freedom and rights. And that is only the tip of the iceberg.

Where does ephedra come from?

Ephedra is a shrub-like plant that groes in arid regions of Asia. The leaves, when dried, have been used medicinally in asthma medications.
"Ephedra" is not "a" plant. It is a genus consisting of over 40 different species.

The number of cases seen to be caused by this drug has caused wide-spread panic and been blown out of proportion. The numbers quoted are probably far fewer than those caused by other freely available over-the-counter drugs available today. People do have reactions to all sorts of things. Some people can die if they eat peanuts. Ephedrine is a drug. It is classed as a drug. It needs to be respected as a drug.
Words of wisdom.

David
 
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Hey guys, here is a synopsis of a paper written by another mod at skinnyguy.net forum, where I also frequent (moderate). His name is Jay MC, a med student. I'll attach the full 20 page paper at the end for those interested.
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Ephedrine and the ECA stack

This post has been adapted from a review paper I wrote. THe full paper can be found here. I feel like everyone agrees that ephedrine works so I'm going to try and address mostly safety issues here. If you wanna know more about the research showing it works check the paper it is covered in depth.

Ephedrine vs Ma Huang

Ephedrine is a chemical controlled by the FDA. It is approved for use only as a drug to treat asthma and congestion. It works by activating the beta 2 adrenergic pathways causing smooth muscles in the bronchioles to relax. Ma Huang is an herb used by the chinese for over 5000 years. Ma Huang is any one of the herbs from the Ephedra family. Most commonly Ephedra sinica is the herb of choice. The Ephedra family of plants contain ephedrine alkaloids (The ephedrine alkaloids are (-)ephedrine, (+)psuedoephedrine,
(-)methylephedrine, (-)norephedrine, and (+)norspuedoephedrine) but the most effective for weight control is (-)ephedrine and E. sinica contains mostly this from and psuedoephedrine making it the best choice. As far as pharmacokinetics (how quickly the drug enters the blood stream) and pharacological aspects the herb and the synthetic version work identically.

Why is ephedrine good for skinny guys

Due to sympathomimetic properties ephedrine helps suppress appetite and works to spare lean muscle and increase protein synthesis. This makes it an EXCELLENT choice as a "cutting" agent. Ephedrine helps gear the body to burn fat while preserving lean tissues. In fact, one study (conducted in vitro showed cellular respiration of brown adipose tissue increased when treated with ephedrine!).

A word about caffeine

Caffeine is a well-studied CNS stimulant with known effects as a pressor agent through peripheral vasoconstriction through an á-adrenergic stimulation pathway. Evidence presented by Battig (1993) shows these effects are seen in doses starting at 200-300 milligrams daily (roughly the amount of caffeine in a cup of coffee) and may engender increases in blood pressure from 10-15 mmHg. Battig points out an interesting characteristic of the pressor effect. The effects of a mid-morning cup of coffee are at least two times less than the effects of the morning’s first cup. In fact, replacement of caffeinated coffee with decaffeinated showed no increase or decrease amongst frequent coffee drinkers. Also, as the reported number of cups per day increases so does the tolerance to the pressor effect. Caffeine has also been shown to cause gastric stimulation.

Safety
IV. Associate health risks
Ephedrine’s notorious reputation began in 1983 when the FDA banned the combination of caffeine and phenylpropanolamine, also known as norephedrine, due to numerous reports of adverse reactions. Norephedrine was again the target of an FDA banning when over the counter (OTC) weight loss aids and nasal decongestants containing the chemical were banned due to the increased risk of stroke. Of important note is that the phenylpropanolamine sold in these products existed as a racemic mixture while the form found in Ephedra is only the (-)-isomer (Haller, Jacob & Benowitz). It is becoming increasingly clear that herbal supplements do, in fact, act as drugs and have serious interactions and profound clinical significance (Stein, 2002). As far as supplements containing ma huang, the only alkaloid present in great enough concentration to possibly cause any health problems is ephedrine. And since most supplements containing ma huang also contain caffeine and ASA, the safety of both ephedrine and the ECA stack will be evaluated.

This part is directly from the paper

(1) Cardiovascular complications
A number of cardiovascular complications have been credited to ephedrine and the use of the herb ma huang including ischemic and hemorrhagic stroke, myocardial infarction, clinical hypertension, tachycardia or palpitation, arrhythmia, and cardiac arrest (Halter & Benowitz, 2000).



(a) Cardiac complications
In the study by Pasquali & Casimirri (1993) a total of 88 individuals were studied for 2-4 months while using ephedrine in doses up to 150 mg a day. Palpitations were one cardiac- related side effect and were reportedly well tolerated and diminished with time. The other noted cardiac related side effect was an increased heart rate when compared to the placebo groups.
The study by Astrup et al. (1992) examined 16 individuals taking ephedrine and caffeine for 8 weeks. There was only one report of palpitations and it was described as well tolerated and transient in nature. The palpitations were no longer reported after 6-14 days.
The study by Daly et al. (1993) studied 24 individuals from 8 weeks to thirteen months. This study reported no significant difference in reported side effects between placebo and herbally treated groups.
The study by Boozer et al. (2001) studied 67 individuals. Of these individuals in the group taking ephedrine and caffeine there were four reports of palpitations, one report of palpitations and chest pain, and two reports of elevated blood pressure. ECG’s performed on all these individuals showed no abnormalities and the side effects were not characterized as serious or lasting.
A study by White et al. (1997) evaluated 12 individuals who ingested ma huang and looked specifically for cardiac type complications by use of ambulatory blood pressure devices. Their research showed that only 50% of the individuals showed increased heart rate, increasing on average by 9 bpm. Four participants showed slight increases in systolic blood pressure and two showed slight decreases. No other adverse effects were reported by participants.
The study conducted by Haller, Jacob & Benowitz (2002) evaluated 8 individuals given a single dose of 20 mg ephedrine and 200 mg caffeine for increases in heart rate and blood pressure. They received only two complaints of palpitations. An increase in heart rate was still seen 11 hours after ingestion. An increase in systolic blood pressure was also noted with one individual increasing by 14 mmHg above baseline 90 minutes after ingestion.
Two other studies approached the assessment of possible adverse reactions to ma huang containing supplements in a different way. Haller & Benowitz (2000) examined 140 reports of adverse effects to the FDA MedWatch system and ranked the symptoms as definitely, probably, possibly, or unrelated to ephedrine use based on symptoms resurfacing upon renewed ephedrine use, pharmacological probability of symptoms, or an improbable relation. 31% of the cases were definitely linked to ephedra, 31% possibly related, 17% unrelated, and 21% undetermined due to insufficient data. Of the 87 cases found to be feasibly related to ephedrine, the most common complication was hypertension. In 10 cases death was reported and 13 cases reported permanent impairment. The second study conducted by Samenuk et al. (2002) studied 926 reports made to the FDA’s Adverse Reaction Monitoring System (ARMS) from 1995 to 1997. Of these reports ma huang was temporarily related to myocardial infarction in 10 and “sudden or unwitnessed death” in 11.


(b) Ischemic an hemorrhagic stroke
Despite increases in systolic blood pressure in several of the clinical trials, none of the systolic blood pressures obtained ever exceeded 143 mmHg and none of the diastolic ever exceeded 90 mmHg.
Analysis of reports to the FDA’s ARMS determined 16 cases of stroke out of 926 cases reported could be related to ephedrine use (Samenuk et al., 2002). A similar study evaluating reports to the FDA’s MedWatch from June 1, 1997 to March 31, 1999 reveal 15 cases of stroke or transient ischemic attack (TIA) (Haller & Benowitz, 2000).

(2) CNS and behavioral effects
Effects on the CNS and behavior related to ephedrine use have been as serious as acute psychosis to mild effects such as headache and tremors.
Participants in the study by Astrup et al. (1992) linked ephedrine use to three instances of insomnia and one instance of tremors. Both of the reported were mild, transient and vanished completely after 6-14 days never to resurface during the eight week study.
A study by Pasquali & Casimirri (1993) had reports of agitation, insomnia, headache, weakness, giddiness, and tremor among its 88 participants. The adverse effects were reported as transient and well tolerated. Similarly, another study conducted by Daly et al. (1993) showed no significant differences between herbally supplemented groups and placebo controlled groups.
A fourth study by Boozer et al. (2001) showed symptoms of irritability in both placebo and herbal supplemented groups. The major side effects seen only in the herbal supplemented group were dry mouth, insomnia, and headache.
An analysis of the FDA MedWatch reports found 10 instances of seizures at least possibly related to ephedrine use (Haller & Benowitz, 2000). One report of a 22 year old male who was hospitalized for unexplained seizures and unresponsiveness was intimately linked to use of a popular ECA stack known as Hydroxycut. Toxicological urinary analysis as well as MRI-MRA scans both came back negative. The patient was found to be atraumatic and otherwise normal based on emergency department reports (Kockler, McCarthy & Lawson, 2001).
An instance of acute psychosis was also reported in a male who mixed an ECA type (Vigueur Fit) with alcohol. The man became agitated and violent and was eventually arrested and charged with criminal conduct (Tormey & Bruzzi, 2001).

Instances of side effects in long term studies involving both ephedrine and the ECA stack are generally low and comparable to those of the placebo group with the exception of occurrences of increased heart rate, dry mouth, and insomnia (Astrup et al., 1992; Pasquil & Casimirri, 1993; Daly et al., 1993; Boozer et al., 2001). Of the studies that reported increases in blood pressure, most examined only a single dose and all contained caffeine as one of the ingredients of the supplement in a dosage of at least 200 mg (White et al., 1997; Haller, Jacob & Benowitz, 2002). Based on information provided by Battig (1993) this can be explained by the pressor effect of caffeine since all increases in blood pressure were within the known ranges of those imposed by caffeine. The description of the rapid accumulation of a tolerance to the pressor effect may also explain why these complications were absent or transient in many of the long term studies and in those studies using only ephedrine (Pasquali & Casimirri, 1993; Daly et al., 1993).
Based on the research presented in this paper, healthy or normotensive obese individuals may use ephedrine with relatively low risk (Daly et al., 1993; Boozer et al., 2001). When increased risks known to be associated with obesity are considered (including, but not limited to, increased occurrence of all forms of cancer, increased occurrence of hypertension, and increased occurrence of congestive heart failure) and compared to the risks clearly and clinically associate with ephedrine use, the benefits of the supplement are highlighted even more. According to Boozer et al. (2001), compared to the prescription drug sibutramine, currently approved for weight reduction by the FDA and described as well tolerated, the ECA stack encourages comparable weight loss, increases heart rate in parity with sibutramine, and has similar reported side effects. The most important difference between the two substances is related to elevation of blood pressure. Research on the ECA stack shows elevated blood pressure that diminishes through the course of treatment while the elevation of blood pressure by sibutramine persists throughout treatment.
Clearly, those suffering from hypertension, renal impairment, angina, cardiovascular problems, diabetes and expectant or nursing mothers should avoid ephedrine or the ECA stack until further research has been completed or unless otherwise advised by their physician.

(3) FDA intervention
Many feel FDA intervention in the marketing and sale of ephedrine and the ECA stack is warranted. However, under the 1994 Dietary Supplement Health and Education Act (DSHEA) the FDA is forced to first prove a supplement unsafe before it imposes sanctions on its sale and labeling (Geiger, 2002). In 1997 the FDA tried to impose guidelines on dosage and duration of use of ephedrine containing products; however, a report from the General Accounting Office criticized this decision for relying heavily on a large number of questionable adverse event reports. This criticism has delayed the implementation of the FDA recommendations (Gurley, 2000). Health Canada has already banned the use of ephedrine or ma huang for the treatment of anything other than congestion and asked for a voluntary recall of all Ephedra products intended for other purposes (Sibbald, 2002).
The FDA recommendation was based largely on the same evidence presented by Samenuk et al. (2002). In a report on the same data by Hutchins (2002) no medical certainty could assign ephedrine a primary or even contributing role in the instances of sudden death stating, “…the current information offers little reason to believe that ephedra alkaloids, used in recommended amounts, are a threat to well-being.”
An estimated 17.2 million Americans used ma huang containing diet aids from 1996-1998 (Blanck, Khan & Serdula, 2001) with only 926 reported cases of toxicity from 1995-1997. Since roughly, only 0.005% of users reported complications, many of which have been proven unrelated to ephedrine use (Hutchins, 2002), the need for FDA intervention is still questionable. More in depth, long term, research needs to be conducted on a wider variety of populations before any definitive decision on the herbs safety may be established.
 

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Excellent post!!

That's what I like to see. Hard data and objective analysis.

David
 
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I agree with the last sentence except for the "control" part. And they're completely wrong about ephedrine not being controlled; it's a List 1 substance. Control will NOT keep ephedrine from getting into the hands of "people from whom serious damage may result." It will simply take it out of the hands of legitimate users. The same is true with prohibition of any substance. Make it illegal, you increase: 1)Crime, 2)Impurities in the drug (which are almost always the main cause of death), 3)Clog in the prison system (the murderers and rapists go out, the pot smokers go in), 4)Misinformation ("It's illegal/controlled so it must be evil"), and 5)Infringements on freedom and rights. And that is only the tip of the iceberg.
Hear ye, hear ye!

Well said, my good man.
 

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