Ephedrine

WHAT IS EPHEDRINE?
Ephedrine is a class of drug known as a sympathomimetic. Specifically it is both an alpha and beta andrenergenic agonist. In addition, ephedrine enhances the release of norepinephrine, a strong engogenous alpha agonist. The action of this compound is notably similar to that of the body's primary adrenergenic hormone epinephrine (adrenaline), which also exhibits action toward both alpha and beta receptors. When administered, ephedrine will noticably stimulate the central nervous system, increasing the heart rate and has an overall heat producing (thermic) effect on most tissues in the body - this includes muscle and fat tissue, helping the user burn more body fat, as well as having stimulatory effect on other target cells. Individuals using ephedrine should notice a slight rise in body temperature as more free fatty acids are produced from the breakdown of triglycerides in adipose tissue (stimulating the metabolism) however this is usually not uncomfortable. Originally the drug was released as an asthma treatment, as one of it's actions is as a bronchiol dilator (opening of the air ways), however, newer and better drugs are now being used for this application. Forms of ephedrine, however, can still now be found in common cold and flu medicines in chemists. Besides increasing heart and respiratory rate this drug also stimulates the thyroid gland to transform the weaker LT-4 (L-thyroxine) into the stronger LT-3 (Liothyronine), which accelerates metabolism.

Ephedrine is classed as an ergogenic drug that clearly enhances endurance, energy and strength - Firstly for athletes interested in muscle gain, ephedrine enhances the metabolic rate - the measure of fat, protein and carbohydrate conversion by the body. And an enhanced metabolic rate could clearly increase the speed of depositing new muscle mass. Secondly the stimulant effect of the drug also increases the force of skeletal muscle contractions. The adrenaline rush provided allows the user to push harder through their training and can indirectly lead to further muscle and strength gains. Finally it is important to note that the powerful mental edge the drug can provide, typically making the user feel far more energetic and much better able to concentrate on the tasks at hand. The action of the drug, used correctly, can dramatically increase fat loss and spare lean muscle tissue.

USING EPHEDRINE TO INCREASE STRENGTH, MUSCLE AND BURN FAT
While the strength boosting effects of this drug are worth noting it's primary use remains as an aid to fat loss. An effective dose of ephedrine has been shown to increase metabolic rate by upto ten percent. An effective dose being usually 25mg. Some people, generally those 200 lbs of muscle and above, occasionally push the dose higher to around 50mg per dose. Although powerful when used alone, Ephedrine seems to be even more effective, according to numerous studies, when combined with caffeine (200 mg) and aspirin (300mg). In this combination the caffeine acts also as a noticable thermogenic and the aspirin inhinbits lipogenesis by blocking the incorporation of acetate into fatty acids. Aspirin may inhibit the bad prostagladins that actually lower your body temperature. In combined supplements we often see ephedrine or one of it's herbal forms combined with herbal forms of caffeine and aspirin such as guarana and white willow bark. These days research into fat loss supplementation has increased rapidly and in herbal forms of Ephedrine (ephedra), caffeine and aspirin mixes we see a whole host of other fat loss agents all intended to work synergisticly together.

SIDE EFFECTS OF EPHEDRINE
Unfortunately Ephedrine can carry a few unwelcome side effects for a few suseptable individuals that should be made aware of. It is possible to become anxious or quite nervous and jittery due to the strong stimulant effect. Especicially when combined as a stack with caffeine and aspirin, the compound can often interrupt or disprupt proper sleeping patterns. It is not advisable to take if you already are aware that something like caffeine doesn't agree with you - it is a pretty safe bet Ephedrine, likewise, will be quite similar. However with some people this may take just a few days to adjust or perhaps an alteration in dosage to allow these side effects to subside. 

It must be noted that ephedrine can cause a rise in blood pressure in most individuals. It is therefore not very wise to use this drug if you suffer from high blood pressure or cardiac irregularities. It is also good advise to stay away from this substance if you are taking thyroid medication or have any thyroid problems, anxiety problems, nervousness, depression, insomnia, diabetes or are taking any MAO inhibitors.

It must be noted that ephedrine can cause a rise in blood pressure in most individuals. It is therefore not very wise to use this drug if you suffer from high blood pressure or cardiac irregularities. It is also good advise to stay away from this substance if you are taking thyroid medication or have any thyroid problems, anxiety problems, nervousness, depression, insomnia, diabetes or are taking any MAO inhibitors.

EPHEDRINE SUPPRESSES APPETITE
One positive side effect commonly noticed during dieting however, is ephedrine's strong appetite suppressing effect. Some people have gone so far as to say ephedrine primarilly helps the user lose fat, not due to it's stimulatory properties, but due to this high inhibition of hunger experienced while using the drug. 

HOW DOES IT WORK?
Ephedrine notably stimulates the beta₁, beta₂ and beta₃ receptors. The beta₁ and beta₂ are related to increased heart rate. Beta₂ receptors increase blood pressure and seem to cause muscle building. About 40% of ephedrines effectiveness comes from stimulating beta₃ receptors where there is actually very little down regulation as there is with the other two receptors. This means that heart rate and blood pressure tend to normalize quite fast - within a few weeks, whereas the thermogenic effects of ephedrine may last much longer. Lipolysis is the process of breaking down triglyceride molecules into one 3 - carbon glycerol molecule and three fatty acids. To complete this process, an enzyme called hormone-sensitive lipase or HSL is required. Ephedrine act to increase this process.

As a guide to exactly how this works here is a simple over view:

Ephedrine stimulates the release of norepinerphrine, and increases circulating levels of epinerphrine. These then bind to the alpha and beta-receptors. As they bind, a subsequent rise is seen in levels of the enzyme adenylate cyclase. Adenylate cyclase is responsible for converting ATP into Cyclic adenosine monophosphate (cAMP). cAMP is what is known as a secons messenger, due to the fact that it works indirectly, triggering another sequence of events to attain a certain outcome. cAMP binds to the regulatory protein kinase, which subsequently frees up its atalytic subunit. This catalytic sub unit is what then phosphorylates HSL to its active form. HSL then catalyses another sequence of events that breaks the bonds of a triglyceride molecule, exposing the free fatty acids for utilization as ATP or energy.

HOW SHOULD EPHEDRINE BE USED?
Dosing schedules for ephedrine use vary depending on the desired goal and the users body weight. Generally it is recommended nobody takes more than 75 - 100 mg of ephedrine in any 24 hours. Normally this dose is split into two or three seperate doses throughout the day of between 20 - 50 mg. The last dose should not be taken much closer than four hours before you intend to sleep as mentioned earlier, the stimulatory effects can interrupt your ability to get a good nights sleep. Your body will also become very resistant to this drugs effect very fast. Some studies have shown ephedrine can significantly depress the beta andrenergenic response within only one week. The adrenal glands get a good wearing out whilst this drug is applied and although this, initially can be quite anabolic, soon will become catabolic as the adrenalin creates more and more cortisol tearing muscle apart. For these reasons it is a good idea to cycle the drug. Methods most popular for ephedrine cycling are day on, day off regimes or five days a week and taking a break at the weekends or at least two days together. It is further good advise to never use ephedrine for more than 4 weeks non stop without a break or the drug becomes pretty much useless and even counterproductive. Most people cycle it's use in one of the above manners for around eight weeks before laying off a while. To clear your system and allow ample recovery leave around 4 weeks before continuing use although it has been shown after heavy long term ephedrine use it can take upto 6 months to completely recover from the drugs effects although these cases are severe.

Supplemeting ephedrine as a fat loss aid has become extremely popular and much research has been done on it's effectiveness and safety. From this research it has been found that numerous other substances can be added to work alongside as an aid to fat loss or to directly increase the rate at which ephedrine works. For this reason many of the supplements you may buy will contain things like L-Tyrosine or guggulsterones and not just a straight forward ephedrine, caffeine, aspirin mix.

LEGALITIES REGARDING EPHEDRINE USE
It should also be noted that ephedrine use is banned in most drug tested sports and the drug is actually illegal in England. Supplements are available however which contain the herbal form of ephedrine - ephedra. As far as the law surrounding ephedra is concerned it is currently a legal herb and a good alternative to ephedrine, however with new legislation regarding the release of medicinal herbs (herbs with clearly potent medicinal potential now being classed almost as a drug) it is possibly ephedra may also eventually be withdrawn from sale.

EPHEDRINE AND THE MEDIA
It would be unfair not to also look at the negative press attributed to this drug. As far as the media goes, ephedrine seems to be labeled as dangerous as radioactive plutonium and seems to be portrayed as a serious killer. However true this may be with abuse of ephedrine, the same can be seen with any drug that is abused. Most cases of fatalities or problems arising from ephedrine use stem mostly from misuse and combining the drug with other drugs especially alcohol. In recent years the misuse of this substance as a so called 'party' drug and mixing high doses with high levels of alcohol have become popular and as it should be noted very dangerous and unwise practice. One case in America of a few teenagers who died were portrayed by the media to have taken a few ephedrine tablets and that was that. In reality the levels of ephedrine (hundreds of miligrams - many more times than the recommended safe dose) were combined with high levels of alcohol. The teenagers died from the combination - not from the ephedrine alone. Of course you should pay attention to the above safety concerns and if you are taking any other prescribed or unprescribed drugs do be careful and check it with your GP but for the average, healthy adult, ephedrine use is safe.