Drinking Albuterol new trend for body builders

Just like any other medicine, albuterol can be abused.  Surely you have the asthmatic or COPD patient who uses it too much.  But I'm referring to the body builder who ingests vials of albuterol to help burn fat and build muscle.

metamorphosis.com describes how Albuterol is used by body builders as a fat burner. It is a stimulant much like "Benadryl with Clenbuterol" but without the shakes.

The author explains how it works:

But in my own personal experience, Albuterol produces a much "cleaner" type of stimulant effect than Clenbuterol. I don’t know how to really describe this other than to say that the "Clen-shakes" just aren’t as bad with Albuterol…in addition, I’m able to focus better on my work when I use Albuterol, while with Clen I’m stimulated but not really focused."

Like short acting anabolic steroids, the author said, albuterol is a shorter acting version of Clen, and thus burns fat quicker.

You'd think if albuterol helped with weight loss I would stick thin, considering I've been inhaling the stuff since 1985.  Apparently I haven't been taking enough.

According to the author, it works this way:

It should come as no surprise to anyone who has used Clenbuterol as well as Albuterol is that when you stimulate your beta receptors, it causes something called vasodilatation (increased blood flow). Stimulation of these receptors also stimulates the break down of fatty acids into the blood stream for use as fuel, which causes a reduction in stored fat. Of course, this increased blood flow also comes with an increased heart rate.

This explains how Beta-2 adrenergic stimulation can also increase your body temperature a bit…however this isn’t something that’s too noticeable on a hermometer…most people will feel a bit hotter, and some will even break a sweat

(I fall into the latter category). Beta-agonists work to do this by increasing heat production in the cell’s powerhouse, the mitochondria, which will also increase your basal metabolic rate, and decrease your appetite. Not too many people feel hungry after a whopping dose of stimulants.

These guys even have a dose down pat. He (or she) said it's 4-8 mg three times a day. He recommends, for those who can get their hands on it, drinking it.

Other sites I've Googled give similar advice, with a similar dosing.

There have even been some studies done to prove this.

One post I found described how some people are faking asthma just so they can get a prescription to Albuterol just for this reason. Yet the author explained that Albuterol has no bronchodilator effect on non-asthmatics, thus "technically, albuterol is not a performance-enhancing drug in a non-asthmatic."

A study published in the European Journal of Applied Physical and Occupational Physiology proved that Albuterol has no effect on performance. The study followed 15 highly trained cyclists, and some of them were given 4 puffs (400 micrograms) of Albuterol 20 minutes prior to exercise, and this had no effect on performance.

However, this dosing was way less than the 4-8 mg recommended by some bodybuilders.

Albuterol, I suppose, is a lot safer than other body building drugs, such as anabolic steroids.  Still, such an abuse of a medicine could potentially result in undesirable side effects. So abuse at your own risk.

This post was originally published on August 29, 2008; it has since been edited.

Further reading:

• What happens when you drink albuterol?
• thinksteroids.com: albuterol
• Neurology.org.  Randomized, double bind, placebo controlled trial, of albuterol in facioscapulohumeral dystrophy, J.T. Kissel, et al, Oct. 23, 2001, 
• European Journal of Applied Physical and Occupatoinal Physiology: "The effect of salbutamol on performance in endurance cyclists, 1996, Norris, et al

Brovana: A better COPD medicine

A relatively new medicine on the market that is slowly gaining acceptance by the medical community is aformoterol (Brovana).  The medicine is quickly gaining acceptance by the medical community to the benefit of the many patients with chronic obstructive pulmonary disease (COPD).

There are four reasons why Brovana is gaining acceptance

1.  It's fast acting beta adrenergic (SABA) like albuterol (Ventolin).

2.  It's long acting beta adrenergic (LABA) like Salmeterol (Serevent), a medicine in the common inhaler Advair

3.  It's only available as a solution, and must be taken using a nebulizer.

4.  The nebulizer route allows better airway distribution in patients with airflow limitation as compared with the Advair inhaler.

5.  It can be taken with Pulmicort to get the same medicinal benefits as Advair.

6.  Both Brovana and Pulmicort only need to be taken twice a day, once in the morning and once in the evening.

7.  Ventolin can still be prescribed for as needed use between doses of Brovana.

Albuterol versus Levalbuterol: What have we concluded?

Editors Tip:  If a doctor prescribes levalbuterol for a patient Q4,
it's highly recommended he not prescribe albuterol Q2prn
The is because albuterol has the S-Isomer, which would offset
any advantages of using levalbuterol (the R-Isomer).  

Albuterol (Ventolin,Proventil) is the best selling asthma drug of all time, and there isn't even a close second.  It was approved by the FDA in 1981, and it was quickly proven to be safe and effective in relieving bronchospasm.  Then levalbuterl was introduced to the market and it was initially proven to be safer and stronger than albuterol. After several years of using these two drugs side by side, is there any evidence that any one is better than the other?  Let us examine the evidence.

Albuterol is a beta adrenergic medicine, which means it was made to mimic the bronchodilating effect of adrenaline.  As of 1999, all beta adrenergic drugs were considered racemic drugs, containing a mixture of 50% R-Isomer and 50% S-Isomer.  Levalbuterol is 100% R-Isomer.  So, what are these Isomers?

1. R-Isomer:  This is the good isomer that causes bronchodilation.  I remember it because I think of r is for relief.  I call it the relief isomer.  They cause bronchodilation and clinical benefit.  They make people breathe better. Another name for the R-Isomer once it was isolated was levalbuterol. 
2. S-Isomer:  It is the bad isomer.  I remember it's bad because s is for shit.  I call it the shit isomer.  It has no clinical benefit. It may oppose the bronchodilation effect over time, and may also be pro inflammatory, thus exacerbating airway reactivity.  It is slowly metabolized by the body, and therefore it sticks around for a while, perhaps causing paradoxical bronchospasm long term, thus requiring the need for even more albuterol, and this becomes a vicious lifelong cycle.  

So a theory developed that the S-Isomer may lead to inert bronchospasm and worse asthma in those who use albuterol every day.

Another theory developed that occupational exposure to albuterol may cause asthma, as what occurs in the profession of respiratory therapy.  Of 2,086 Rhode Island respiratory therapists and 2,030 physical therapists, physicians diagnosed 16% of the respiratory therapists with asthma, and only 8% of the physical therapists with asthma.  Even when asthma is not diagnosed until after entry into the profession, 7.4% of RTs were diagnosed with asthma compared with 2.8 of PTs being diagnosed with asthma.

Of course their are other reasons an RT might be more likely to develop asthma other than occupational exposure (such as increase awareness of the disease among the RT community), so the study does not prove albuterol causes asthma, only that it could cause asthma. Yet other studies came up with similar findings. 

When the S-Isomer is taken out of albuterol you have levalbuterol (Xopenex).  I will delve into studies comparing albuterol and levalbuterol in a later post.  All of the problems of the S-Isomer are completely avoided with levalbuterol.  In other words, levalbuterol is a much stronger medicine than albuterol due to the absence of the S-Isomer.  

Studies have confirmed, however, that there is no clinical benefit to using levalbuterol over albuterol in the clinical setting.  While levalbuterol is considered stronger than albuterol, it is also more expensive.  Studies have shown that simply by giving greater amounts of albuterol generates the same effect as when lower doses of levalbuterol are given.  

Also, studies have confirmed that patients entering the emergency room with exacerbations of asthma or COPD are equally likely to be discharged or admitted regardless of whether albuterol or levalbuterol is used.

Likewise, since both albuterol and levalbuterol are beta adrenergic medicine, and both attracted to B2 agonists throughout the body, side effects (such as tachycardia, and tremors) are the same (albeit negligible) regardless of which of these two medicines is used.  This conclusion is contrary to earlier studies.

So, based on the evidence, the less expensive albuterol should be used on most patients admitted to the hospital.  Only when there is no perceived benefit from albuterol should levalbuterol be trialed.  

References:

1. Handley, D., "The asthma-like pharmacology and toxicology of (S)-isomers of beta agonists," Journal of Allergy and Clinical Immunology, August, 1999, 104(2) pages 69-76.
2. Borkowski Jaime, Marsha Crader, "Nebulized albuterol versus levalbuterol in pediatric and adult patients: A review," Formulary Journal of Modern Medicine, April 1, 2009, http://formularyjournal.modernmedicine.com/formulary-journal/news/clinical/clinical-pharmacology/nebulized-albuterol-versus-levalbuterol-pediat, accessed 1/28/2014
3. Christiani, David C., David G. Kern, "Asthma risk and occupation as a respiratory therapist," September, 1993, 148 (3), pages 671-674

The link between Albuterol and Potassium

It's a proven fact that beta-adrenergic medicine such as epinephrine, Albuterol, and Levalbuterol cause a decrease in serum levels of potassium.  I've received several questions about this including the following:

• If I use Ventolin, do I need to be concerned about my potassium level?
• Can Ventolin be used to lower potassium in patients with hyperkalemia?

In a quest to answer these questions I did the following research. To get started, we'll answer some of the basic questions about the beta-adrenergic/ potassium relationship?

What is potassium?  

It's a mineral that is important to maintain normal function of cells.  It's also an electrolyte that plays a vital role in heart function and skeletal muscle contraction.  The effects of potassium inside the body are kept at a balance by the sodium/ potassium pump, which I describe below.  If potassium is high (hyperkalemia) it can cause muscles spasms or cramps, and this can also lead to abnormal heart rhythms and death.  I describe the importance of potassium in the link provided in the next paragraph.  

How is potassium maintained in the body?

To understand how medicines like Albuterol lower Potassium it's important to understand some of the basics of human anatomy.  To answer this question I will quote myself, "The balance of sodium and potassium:" 

Ann Crawford in her article "Balancing act:  Sodium and Potassium" in the July issue of Nursing (pp. 44-50) describes the pump as the main mechanism of moving sodium "from inside cells to the extracellular compartments, and returns potassium from the extracellular compartments into cells using adenosine triphosphate (ATP) as an energy source."

She likewise explains that electrolytes tend to move from areas of high concentrations to lower concentrations.  So the body naturally works to maintain potassium inside cells 35 times greater than outside cells so potassium has a tendency to want to get out of cells.  Likewise, sodium outside cells is kept 14 times greater than inside cells so sodium has a natural tendency to want to go into cells.

Sodium attracts water. So if sodium levels inside the cell were to get too high the cells would absorb water and would swell and ultimately explode.  Obviously this wouldn't be good.

Rene Fester Kratz in his book "Molecular & Cell Biology for Dummies" explains the pump as a protein in cellular walls and "for every round of action, the sodium potassium pump moves three sodium ions out of the cell and two potassium ions into the cell.  Thus the pump creates a higher concentration of sodium outside the cell, a higher concentration of potassium inside the cell, and a greater positive charge outside the cell.  These differences in ion concentration and electrical charge are important in the functioning or nerve and muscle cells in animals."

Why do beta-adrenergic lower potassium?

According to livestrong.com, "Why Albuterol lowers potassium," the following is how beta-adrenergic medicine lowers potassium:

To understand how albuterol can decrease your potassium levels, you need to understand how certain hormones, known as catecholamines, affect potassium. Catecholamines, such as the hormone epinephrine and adrenaline, increase the activity of a protein known as a sodium-potassium ATPase. When this protein is activated, it pumps potassium into cells while also pumping sodium out of cells. The movement of potassium into the cells causes a decrease in the amount of potassium in the blood.

Albuterol (and Levalbuterol) is known as a beta-2 agonist. This means that it is able to bind to and mimic the effects of adrenaline on certain cells, including its ability to trigger the transport of potassium out of the blood. Consequently, taking albuterol can lower your potassium levels. This may make your muscles weak or cause muscle spasms, and it can also cause an abnormal heart rhythm. Other symptoms of hypokalemia include fatigue, constipation and the breakdown of muscle fibers.

In this way, adrenaline and beta-adrenergic medicine induce a similar effect to inscausing theing  the sodium/ potassium ATPase pump to pump more potassium into cells, and thereby reducing serum potassium levels.

Does Levalbuterol (Xopenex) have the same ability to lower potassium?
Yes. A 2005 report by the Emergency Medicine Residency, Grand Rapids MERC/ Michigan State University, "Nebulized levalbuterol or albuterol for lowering serum potassium," notes that Xopenex is equally capable at lowering potassium as albuterol.

In medical emergencies, is albuterol an effective therapeutic means of lowering potassium?

This is something that many respiratory therapists frown upon, because we find that many doctors will order one breathing treatment of 0.5cc albuterol with the intent of lowering potassium. Past studies have concluded the therapeutic dose should be 5-20 mg of Albuterol over a 15-20 minute period.

According to "Hyperkalemia Revisited" (Parham, Walter A, et al, Tex Heart Inst J. 2006; 33(1): 40–47), the following should be considered as the evidence:

Growing evidence suggests that there may be a role for albuterol in the treatment of patients with severe hyperkalemia. Catecholamines activate Na-K ATPase pumps through β₂ receptor stimulation in a manner that is additive to the effect of insulin.(1, 2) In a study by Montoliu and coworkers, (3) 0.5 mg of intravenous albuterol was given to patients with hyperkalemia, leading to a 1-mEq/L decrease in serum potassium levels with minimal adverse effects. (4) Because there are no approved intravenous forms of β agonists available in the United States, studies have been performed to determine whether nebulized β agonists would have a similar effect on serum potassium levels. One such study found that albuterol, when given in very high doses (10–20 mg vs the normal 0.5 mg), decreased potassium levels by 0.62 to 0.98 mEq/L.⁴⁵ The onset of action for inhaled albuterol was immediate and lasted for 1 to 2 hours. Although in these studies the effects varied among individuals, β₂agonist administration was found to be safe and was associated with a significant decrease in serum potassium levels. Therefore, β₂ agonist therapy should be considered as an adjunctive treatment for patients with severe hyperkalemia.

Emphasis added by this author.  So you can see there is mounting evidence that Albuterol can be an effective therapy for hyperkalemia, if given in therapeutic doses.

Should Albuterol be a front line therapy for hyperkalemia?

The authors of oxford journals (Kamel, S. Kamel, Charles Wei, "Controversial issues in the treatment of hyperkalemia," Nephrology Dialysis Transplantation, 2003, Vol. 18, Issue 11, pages 2215-2218) agree with the study results as mentioned in the last section. They go on to question the use of albuterol as a front line therapy for hyperkalemia:

Nonetheless, we have reservations about the use of β₂ agonists as a first-line therapy in emergency treatment of hyperkalaemia. First, 20–40% of patients studied have a decline in P_K of <0.5 mM and it is not possible to predict who will fail to respond. Secondly, there are safety concerns because the doses used are 4–8 times those prescribed for the treatment of acute asthma. Although no severe adverse events were reported, most of these studies were performed in stable patients. Some of these studies excluded patients on β-blockers and those with significant coronary heart disease or unstable heart rhythms. Therefore, the safety of these agents was determined in a group of patients that may not resemble the general ESRD population.

Allon and Copkney (5) examined whether the effect of nebulized β₂ agonists is additive to that of insulin. There was a similar decrease in P_K with insulin (0.65 mM) or albuterol (0.66 mM). There was a substantially greater fall in P_K with the combined regimen (1.2 mM). The dose of intravenous regular insulin used in this study was only 10 units, and P_K fell less than in studies when higher doses of insulin were used (6). Thus, it remains uncertain whether β₂ agonists would have a P_K-lowering effect additive to that of insulin if insulin were given at the higher doses.

So should I be worried if I use Albuterol?  

While the potassium lowering effects of albuterol are often discussed in medical circles, the effect on those of us who use albuterol on a regular basis is rarely mentioned.  In fact, recently it was posed to me by a fellow asthmatic, and I humbly responded  by stating that one albuterol treatment shouldn't affect potassium enough to worry about.  Yet if you take Ventolin a lot, meaning you use it more than 2 puffs every 4-6 hours, then you may want to supplement your diet with potassium.  Bananas are a good source of potassium.  If you us it a lot, and you continue to have symptoms of a high potassium (heart palpitations, muscle cramps), then you should call your doctor.

Your doctor will (should) also check your serum potassium level on a regular basis, like once a year.  If your potassium levels are out of range your physician should inform you of this.  Again, however, chances are your doctor won't say anything because, so long as you're not excessively abusing the substance, your potassium level should be fine.  

We often do continuous breathing treatments in the emergency room, and I have never observed a doctor being overly concerned about potassium.  If he is he will simply supplement the patient with potassium chloride through the IV.  Yet for the general asthmatic who uses albuterol, you shouldn't have anything to be concerned about.  If you're still concerned, eat bananas. Perhaps that's why I love bananas so much.  I eat 1-3 every day.

Related links:

1. The balance of sodium and potassium
2. The balance of sodium and potassium part II

Further references:

1. Greenberg A. Hyperkalemia: treatment options. Semin Nephrol 1998;18:46–57. [PubMed] 
2. Flatman JA, Clausen T. Combined effects of adrenaline and insulin on active electrogenic Na+−K+ transport in rat soleus muscle. Nature 1979;281:580–1. [PubMed] 
3. Montoliu J, Lens XM, Revert L. Potassium-lowering effect of albuterol for hyperkalemia in renal failure. Arch Intern Med 1987;147:713–7. [PubMed] 
4. Montoliu, ibid 
5. Allon, M. Copney, C., "Albuterol and insulin for treatment of hyperkalemia in hemodialysis patients," Kidney International, 1990, 38: 869-872 
6. Blumberg A, Weidmann P, Shaw S et al, "Effect of various therapeutic approaches on plasma potassium and major regulating factors in terminal renal failure," American Journal of Medicine, 1998; 85: 507-512

Generic and brand names: why are there so many names for meds?

Every day at MyAsthmaCentral.com we get lots of asthma related questions. Below are some questions I thought my readers at the RT Cave would enjoy.

Question: Is Ventolin in Canada the same as Albuteral? I get very confused with all these names of medications. The ones in Canada I think are called something else??

My humble answer: The medicine is exactly the same in both countries.

Merck.com explains all the names. I'll give a quick review here.

Every drug has more than one name. You have the chemical name that describes "the atomic or molecular structure of the drug." Usually this name is too complex for for the public to understand

Once the product is approved by the FDA it is given a generic name, which is basically an easy to pronounce version of the chemical name. Then the company comes up with a brand name that marks that particular product as made by that company.

Likewise, "When a drug is under patent protection, the company markets it under its brand name. When the drug is off-patent (no longer protected by patent which usually takes 25 years), the company may market its product under either the generic name or brand name. Other companies that file for approval to market the off-patent drug must use the same generic name but can create their own brand name. As a result, the same generic drug may be sold under either the generic name or one of many brand names."

Most doctors, nurses and RTs will refer to the drugs generic name, because it refers to the product itself not the company that makes it. Thus, a doctor will write an order for Albuterol. The pharmacy can choose whichever brand it wants. Usually it chooses the one with the lowest cost at that time.

For Albuterol it would look like this:

Generic name: Albuterol in the U.S. (Salbutamol in Europe and Canada)

Brand names: Ventolin, Proventil (AccuNeb, Vospire, ProAir in Europe and Canada)

Every one of the above refers to the exact same medicine, and they all have the same components, and thus all work exactly the same. So, yes, the Ventolin in Canada is the same as Albuterol.

If you have any further questions email me, or Visit MyAsthmaCentral.com's Q&A section.

What's the difference between Albuterol and Atrovent?

Every day at MyAsthmaCentral.com we get lots of asthma related questions. Below are some questions I thought my readers at the RT Cave would enjoy.

Question: What is the difference between Ventolin and Atrovent? I have been getting jittery when using Advair, Prednisone, Theophylline and Ventolin, and my doctor says Atrovent may help instead of Ventolin

My humble answer: With all those meds, it sounds like you have hardluck asthma.

The problem is, every one of those medicines you're on can cause the jitters. That's the thing with asthma is you have to balance the advantages of taking asthma meds with the disadvantages. And sometimes we asthmatics, while we're trying to get our asthma under control, have to put up with side effects -- mainly the jitters.

The thing about Ventolin, as I'm sure you know, is it gives you immediate relief you can feel, and that's why it's called a rescue medicine. Atrovent can open your airways too, but its effects are generally mild and may take longer than Ventolin. While Atrovent is generally not recommended by the asthma guidelines as a frontline medicine for most asthmatics, it has proven beneficial for some. So you should try it and see if it works for you. But Keep your Ventolin on hand just in case you need it.

Here's some information about Ventolin and Atrovent:

Ventolin is a beta adrenergic medicine. It is a medicine that attaches to beta 2 receptors that are on the muscles that surround the air passages in your lungs (bronchioles) and cause the air passages to relax. It can rapidly open up your lungs making it easier to breathe. It is considered a front line medicine for treating acute asthma symptoms.

Atrovent is an anticholinergic medicine. Our bodies release a natural neurotransmitter (Acetylcholine) that attaches to cholinergic receptors in the muscles surrounding the air passages in our lungs. This cause these muscles to spasm, and your air passages to become narrow (bronchoconstriction). Thus, Atrovent particles attach to these cholinergic receptor sites and block the cholinergic response, thus prevening this airway narrowing. To control asthma, usually there are better medicines than this. However, when all else fails, this is a good option to try. Most experts call Atrovent a back door bronchodilator.

I hope this information helps. Good luck.

If you have any further questions email me, or Visit MyAsthmaCentral.com's" Q&A section.