Ephedrine

Ephedrine Description

Ephedrine is a stimulant drug that belongs to the group of medicines known as sympathomimetics. Specifically, it is both an alpha and beta-adrenergic agonist (you may remember Clenbuterol is a selective beta-2 agonist). In addition, ephedrine enhances the release of norepinephrine, a strong endogenous alpha agonist. The action of this compound is notably similar to that of the body’s primary adrenergic hormone epinephrine (adrenaline), which also exhibits action toward both alpha and beta receptors. When administered, ephedrine will notably increase the activity of the central nervous system, as well as have a stimulatory effect on other target cells. This may produce some effects that can be beneficial to a bodybuilder or athlete. For starters, the user’s body temperature should rise slightly as more free fatty acids are produced from the breakdown of triglycerides in adipose tissue (stimulating metabolism). This may aid in body fat reductions and increased vascularity. It is also believed that the anabolic effects of steroids might be increased with this substance (mildly), as an increase in metabolic rate may equate to an increase in fat, protein and carbohydrate conversion by the body. The stimulant effect of this drug will also increase the force of skeletal muscle contractions.

History

Ephedrine is a fairly old medication and has been used in the United States for a number of medical applications over the years including that of a stimulant, appetite suppressant, decongestant, and hypotension treatment associated with anesthesia. Today, it is approved as an over-the-counter medicine, and sales are largely found in this sector. Controls over ephedrine in the United States are growing in recent years, however, due to the fact that it can be used as a primary base for the manufacture of methamphetamine. With ephedrine available as an over-the-counter product, underground manufacturers have been able to easily obtain it. A trend involving large volume retail purchases for OTC ephedrine products had been developing, and many states have responded with legislation controlling the sale of precursor materials like ephedrine. In 2006, a federal law was passed further restricting the record-keeping requirements and available sale channels for ephedrine in the United States. With the widespread increase of methamphetamine addiction (and related crime), some speculate ephedrine may soon join the list of federally controlled substances. In spite of tighter regulations, it is still presently available for over-the-counter sales.

How Supplied

Ephedrine (as ephedrine hydrochloride or ephedrine sulfate) is most commonly supplied in tablets of 25 mg or 50 mg each.

Structural Characteristics

Ephedrine is a sympathomimetic amine related in structure to amphetamine and methamphetamine. It has the chemical designation (1R,2S)-2-(methylamino)-1-phenylpropan-1-ol.

Side Effects

Ephedrine can produce a number of unwelcome side effects that the user should be aware of. For starters, the stimulant effect can produce shaky hands, tremors, sweating, rapid heartbeat, dizziness, and feelings of inner unrest. Often these effects subside as the user becomes more accustomed to the effect of this drug, or perhaps the dosage is lowered. In general, those negatively impacted by caffeine would probably not like the stronger effects of ephedrine. The mental and physical state produced by this drug is also quite similar to that seen with clenbuterol, so those who find little discomfort with that treatment should (presumably) be fine with this item (and vice versa). While taking this drug one may also endure a notable loss of appetite, usually a welcome effect when dieting. Ephedrine is in fact a popular ingredient in combination (prescription) appetite suppressants. The user may further notice headaches and an increase in blood pressure with regular use of ephedrine. Those suffering from thyroid dysfunctions, high blood pressure, or cardiac irregularities should also not be taking this drug, as it will certainly not mix well with such conditions. Ephedrine is a CNS stimulant with the potential for a fatal overdose. Signs of overdose may include rapid breathing, blood pressure irregularities, irregular heartbeat, unconsciousness, trembling, shaking, panic, extreme restlessness, and severe nausea, vomiting or diarrhea.¹ 

Administration

The primary application for ephedrine among bodybuilders and athletes (off-label) is that of a cutting (fat-loss) agent. Here, the individual will generally take this drug a few times per day during a dieting phase of training, at a dosage of 25 to 50 mg per application. The widely touted stack of ephedrine (25-50 mg), caffeine (200 mg), and aspirin (300 mg) (E/C/A) is shown to be extremely potent for fat loss and is more commonly applied than ephedrine alone. In this combination, the ephedrine and caffeine both act as notable thermogenic stimulants². The added aspirin also helps to inhibit lipogenesis by blocking the incorporation of acetate into fatty acids. The athlete may use an increase in body temperature as a marker that the drug combination is working. This is usually a degree or so (not an uncomfortable raise). This combination is taken 2 to 3 times daily, for several consecutive weeks. It is discontinued once the user’s body temperature drops back to normal, a clear sign these drugs are no longer working as desired. A break of at least 4-6 weeks is usually taken so that this stack may once again work at an optimal level.

Ephedrine is also used by some competitive athletes (including powerlifters) as a stimulant before workouts or competitions. The resulting (slight) strength and energy increase may improve anaerobic performance and weight totals on major lifts. On this same note, it is also believed by some to provide a mental edge, making the user more energetic and better able to concentrate on the tasks ahead. A pre-event dose of 25-50 mg of ephedrine is typically used for this purpose. It is important to note that this compound is not used continuously as a pre-workout or pre-event stimulant, as its effect will diminish as the body becomes accustomed to the drug. In most instances, the user will take the drug only 2 or 3 times per week, usually on those days personally “important”. The individual would also be wise to take a break (at least 1 to 2 months) from ephedrine after several weeks have passed, so as to continue receiving the optimal effect from this drug.

Availability

Ephedrine is widely available in the U.S. and in a number of countries abroad. It is not commonly a target of counterfeiting operations.

References:

1. Ephedrine Sulfate Drug Information. Medilibrary.org. 
2. The effect and safety of an ephedrine/caffeine compound compared to ephedrine, caffeine and placebo in obese subjects on an energy restricted diet. A double blind trial. Astrup A1, Breum L, Toubro S, Hein P, Quaade F. Int J Obes Relat Metab Disord. 1992 Apr;16(4):269-77.