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Ephedrine Hydrochloride
by Bill Roberts – While no longer legal for sale as a dietary supplement in most countries, ephedrine is the most effective herbal fat loss substance ever sold. It’s still worth talking about however, because it’s still available for worldwide shipping from some countries and is still as effective as ever.
How Does Ephedrine Relate To Ephedra And Ephedra Alkaloids?
Ephedra is a genus of plants which includes numerous species. Some, such as E. sinica, E. equisetina, and E. intermedia contain ephedra alkaloids in amounts sufficient to be useful for fat loss, and are collectively called Ma Huang. Others do not.
Ephedra alkaloids are a group of compounds which includes not only ephedrine but several other compounds such as norephedrine and methylephedrine. Legitimate ephedra extracts of the past contained multiple such alkaloids in varying ratios. Of these, ephedrine is the most important for fat loss, but is not the only active compound.
While pure ephedrine can be isolated from ephedra alkaloids, synthetic ephedrine is more economical and is by far the predominant type. Generally pure ephedrine is provided as ephedrine HCl or ephedrine sulfate, with no important difference existing between these.
Ephedra extracts on the market today may indeed be from the Ephedra genus, but to satisfy the law lack ephedrine or any ephedra alkaloid. Extracts which claim to be from E. nevadensis or E. viridis or make no species claim at all are invariably worthless.
As ephedrine-containing herbal extracts are now difficult to impossible to obtain, the practical way to use ephedrine is in tablet or liquid form, preferably without guaifenesin.
How Does Ephedrine Promote Fat Loss?
Rather than working directly itself at fat cells, ephedrine acts as a sympathomimetic to activate their beta adrenergic receptors, thus stimulating lipolysis and metabolic rate and reducing appetite. All these work together to improve fat loss.
As a sympathomimetic, it is a drug which causes nerves of the sympathetic nervous system to act as if they were stimulated. It does this by displacing norepinephrine from their nerve endings. Whatever level of activity the nerve already had in releasing norepinephrine, even more is released due to this displacement. The norepinephrine in turns acts at the beta receptors of cells.
Ephedrine also slows the reuptake and the breakdown of norepinephrine, thus increasing activity of norepinephrine even further.
All this is effective in stimulating beta receptors, though it’s not as effective as stimulating them directly, as albuterol and clenbuterol do.
Dosing Of Ephedrine
In a fat loss cycle, ephedrine is best dosed at 25 or 30 mg three times per day. Because ephedrine use often interferes with sleep, the last dose will usually be at least 5 hours before retiring. Some will wish to have their final dose even earlier than this.
Optionally, though with proportionally less effect, ephedrine may be taken only once or twice per day. Even the morning-only dosing provides significant maintenance benefit.
The above dosing, as well as being proven in bodybuilding for many years, also correlates with clinical usage. As a drug for treating asthma, ephedrine was typically provided at 15-30 mg three times per day.
Higher dosing of course has been tried, but increases side effects and risks with little if any increase in benefit compared to the above dosing.
For effective fat loss, ephedrine is very preferably combined with caffeine. A common method is take 200 mg caffeine three times per day at about the same times as ephedrine is taken, but for example 300 mg on arising and 300 mg a few hours later works equally well.
What If I Want Still More Effect Than This Amount of Ephedrine Provides?
Rather than increasing ephedrine dose beyond 30 mg three times per day, I’d consider using albuterol. I believe doing so to better than increasing ephedrine.
With Guaifenesin, Or Without?
Over the counter ephedrine is commonly combined with guaifenesin. However, I suggest avoiding such ephedrine and using a pure product instead. While I know of no study showing less effect when gauifenesin is included, from experience the combination certainly seems less effective. It’s so much less effective that relatively few choose to do it. A possible reason for this is that guaifenesin is a muscle relaxant.
Whether that is the cause or not, ephedrine with guaifenesin simply does not have the track record for fat loss that ephedrine itself does.
Should Ephedrine Be Cycled?
When reasonably dosed as described above, there are no or little issues with receptor downregulation and ephedrine need not be cycled for that reason. However, one may wish to target its use. Even while dieting it might be omitted on refeed days, for example.
Use can reasonably vary between, for example, cutting weeks, maintenance weeks, and bulking weeks.
Alternately, while not necessary it’s popular to use ephedrine on a 5 days on / 2 days off cycle. Such use has absolutely nothing to do with pharmacological need or benefit but can meet personal preference.
Can I Combine Ephedrine With High Dose Thyroid Hormone?
Under no circumstances do this. Cardiac risk is greatly increased.
Any dose of thyroid hormone which is high enough to provide noticeable tachycardia (increase in heart rate) is too high a dose to use together with ephedrine, because ephedrine also acts to stimulate the heart.
Take care with even low to moderate dose thyroid if ephedrine is being used as well.
Contraindications For Ephedrine Use
Ephedrine should not be used without medical supervision where cardiovascular conditions, high blood pressure, kidney disease, potassium imbalance, seizures, hyperthyroidism, glaucoma, or psychiatric conditions exist, and should not be used during pregnancy or breastfeeding. Do not combine with beta blockers, allergy medications, asthma medications, antidepressants, or MAO inhibitors without competent medical advice.
Adverse Side Effects And Risks of Ephedrine Usage
As a mass-marketed dietary supplement, ephedrine was often taken at doses beyond or even drastically beyond label recommendation.
In one study, documentation of reported occurrences indicates about twelve cardiovascular events and two deaths were likely caused by ephedrine use, with about half the cases distributed among individuals below age 30, a group usually nearly immune to cardiovascular events.
In another such study, about 50 events of death, stroke, hypertension, tachycardia, palpitations, and seizures over a three year period were determined to be probably related to ephedrine use.
While these numbers are low relative to adverse events seenm with many pharmaceutical drugs, safety concerns were increased by the facts that ephedrine indeed does have actions that can speed heart rate, change heart rhythm (shorten QTc interval,) activate cardiac potassium channels, and increase blood pressure. So there was a mechanism of action for the observed events.
These concerns resulted in the removal of ephedrine from the US dietary supplement market in 2004. It was, however, never demonstrated that serious risks were likely at dosing such as 15-30 mg three times per day.
At such dosing, the most likely adverse side effects are elevated heart rate and/or elevated blood pressure, headache, tremors, nausea, or anxiety, all correctable by reducing dosage or discontinuing use.
Summary
Although potentially dangerous, ephedrine is generally safe for those without adverse health conditions when used at dosing of 15-30 mg up to three times daily, and is effective in aiding fat loss. It is even more effective when combined with caffeine 200 mg taken at or about each ephedrine dosing. Ephedrine promotes fat loss by activating beta adrenergic receptors, which also results in cardiac stimulation. Albuterol may be considered as a more effective alternate to ephedrine.
by Bill Roberts – While no longer legal for sale as a dietary supplement in most countries, ephedrine is the most effective herbal fat loss substance ever sold. It’s still worth talking about however, because it’s still available for worldwide shipping from some countries and is still as effective as ever.
How Does Ephedrine Relate To Ephedra And Ephedra Alkaloids?
Ephedra is a genus of plants which includes numerous species. Some, such as E. sinica, E. equisetina, and E. intermedia contain ephedra alkaloids in amounts sufficient to be useful for fat loss, and are collectively called Ma Huang. Others do not.
Ephedra alkaloids are a group of compounds which includes not only ephedrine but several other compounds such as norephedrine and methylephedrine. Legitimate ephedra extracts of the past contained multiple such alkaloids in varying ratios. Of these, ephedrine is the most important for fat loss, but is not the only active compound.
While pure ephedrine can be isolated from ephedra alkaloids, synthetic ephedrine is more economical and is by far the predominant type. Generally pure ephedrine is provided as ephedrine HCl or ephedrine sulfate, with no important difference existing between these.
Ephedra extracts on the market today may indeed be from the Ephedra genus, but to satisfy the law lack ephedrine or any ephedra alkaloid. Extracts which claim to be from E. nevadensis or E. viridis or make no species claim at all are invariably worthless.
As ephedrine-containing herbal extracts are now difficult to impossible to obtain, the practical way to use ephedrine is in tablet or liquid form, preferably without guaifenesin.
How Does Ephedrine Promote Fat Loss?
Rather than working directly itself at fat cells, ephedrine acts as a sympathomimetic to activate their beta adrenergic receptors, thus stimulating lipolysis and metabolic rate and reducing appetite. All these work together to improve fat loss.
As a sympathomimetic, it is a drug which causes nerves of the sympathetic nervous system to act as if they were stimulated. It does this by displacing norepinephrine from their nerve endings. Whatever level of activity the nerve already had in releasing norepinephrine, even more is released due to this displacement. The norepinephrine in turns acts at the beta receptors of cells.
Ephedrine also slows the reuptake and the breakdown of norepinephrine, thus increasing activity of norepinephrine even further.
All this is effective in stimulating beta receptors, though it’s not as effective as stimulating them directly, as albuterol and clenbuterol do.
Dosing Of Ephedrine
In a fat loss cycle, ephedrine is best dosed at 25 or 30 mg three times per day. Because ephedrine use often interferes with sleep, the last dose will usually be at least 5 hours before retiring. Some will wish to have their final dose even earlier than this.
Optionally, though with proportionally less effect, ephedrine may be taken only once or twice per day. Even the morning-only dosing provides significant maintenance benefit.
The above dosing, as well as being proven in bodybuilding for many years, also correlates with clinical usage. As a drug for treating asthma, ephedrine was typically provided at 15-30 mg three times per day.
Higher dosing of course has been tried, but increases side effects and risks with little if any increase in benefit compared to the above dosing.
For effective fat loss, ephedrine is very preferably combined with caffeine. A common method is take 200 mg caffeine three times per day at about the same times as ephedrine is taken, but for example 300 mg on arising and 300 mg a few hours later works equally well.
What If I Want Still More Effect Than This Amount of Ephedrine Provides?
Rather than increasing ephedrine dose beyond 30 mg three times per day, I’d consider using albuterol. I believe doing so to better than increasing ephedrine.
With Guaifenesin, Or Without?
Over the counter ephedrine is commonly combined with guaifenesin. However, I suggest avoiding such ephedrine and using a pure product instead. While I know of no study showing less effect when gauifenesin is included, from experience the combination certainly seems less effective. It’s so much less effective that relatively few choose to do it. A possible reason for this is that guaifenesin is a muscle relaxant.
Whether that is the cause or not, ephedrine with guaifenesin simply does not have the track record for fat loss that ephedrine itself does.
Should Ephedrine Be Cycled?
When reasonably dosed as described above, there are no or little issues with receptor downregulation and ephedrine need not be cycled for that reason. However, one may wish to target its use. Even while dieting it might be omitted on refeed days, for example.
Use can reasonably vary between, for example, cutting weeks, maintenance weeks, and bulking weeks.
Alternately, while not necessary it’s popular to use ephedrine on a 5 days on / 2 days off cycle. Such use has absolutely nothing to do with pharmacological need or benefit but can meet personal preference.
Can I Combine Ephedrine With High Dose Thyroid Hormone?
Under no circumstances do this. Cardiac risk is greatly increased.
Any dose of thyroid hormone which is high enough to provide noticeable tachycardia (increase in heart rate) is too high a dose to use together with ephedrine, because ephedrine also acts to stimulate the heart.
Take care with even low to moderate dose thyroid if ephedrine is being used as well.
Contraindications For Ephedrine Use
Ephedrine should not be used without medical supervision where cardiovascular conditions, high blood pressure, kidney disease, potassium imbalance, seizures, hyperthyroidism, glaucoma, or psychiatric conditions exist, and should not be used during pregnancy or breastfeeding. Do not combine with beta blockers, allergy medications, asthma medications, antidepressants, or MAO inhibitors without competent medical advice.
Adverse Side Effects And Risks of Ephedrine Usage
As a mass-marketed dietary supplement, ephedrine was often taken at doses beyond or even drastically beyond label recommendation.
In one study, documentation of reported occurrences indicates about twelve cardiovascular events and two deaths were likely caused by ephedrine use, with about half the cases distributed among individuals below age 30, a group usually nearly immune to cardiovascular events.
In another such study, about 50 events of death, stroke, hypertension, tachycardia, palpitations, and seizures over a three year period were determined to be probably related to ephedrine use.
While these numbers are low relative to adverse events seenm with many pharmaceutical drugs, safety concerns were increased by the facts that ephedrine indeed does have actions that can speed heart rate, change heart rhythm (shorten QTc interval,) activate cardiac potassium channels, and increase blood pressure. So there was a mechanism of action for the observed events.
These concerns resulted in the removal of ephedrine from the US dietary supplement market in 2004. It was, however, never demonstrated that serious risks were likely at dosing such as 15-30 mg three times per day.
At such dosing, the most likely adverse side effects are elevated heart rate and/or elevated blood pressure, headache, tremors, nausea, or anxiety, all correctable by reducing dosage or discontinuing use.
Summary
Although potentially dangerous, ephedrine is generally safe for those without adverse health conditions when used at dosing of 15-30 mg up to three times daily, and is effective in aiding fat loss. It is even more effective when combined with caffeine 200 mg taken at or about each ephedrine dosing. Ephedrine promotes fat loss by activating beta adrenergic receptors, which also results in cardiac stimulation. Albuterol may be considered as a more effective alternate to ephedrine.
