Albuterol’s Mode Of Fat-Loss Action
One of the most effective means of promoting rapid fat loss is activation (agonism) of beta-adrenergic receptors. Beta receptor activation increases lipolysis and metabolic rate, and can decrease appetite. All these work to improve fat loss.
Prior to changes in the law, the most widely used means of doing this had been with ephedrine. The most hardcore way has been with clenbuterol. Perhaps the best way, for most, is with albuterol.
Medically, albuterol is used to improve breathing of asthmatics and patients with chronic obstructive pulmonary disease. Safe initial dosing is typically 2-4 mg taken three to four times per day. (Higher dosings are needed only with time, as downregulation occurs.)
The same dosing levels can also be effective for fat loss, for maintenance of muscle during fat loss, and often for significant increase in endurance performance and/or slight increase in strength.
Another positive effect of beta receptor activation is improvement in blood lipid profile. Albuterol can provide a significant benefit in this regard..
Pharmacological Differences Between Albuterol And Other Beta Agonists
Pharmacologically, albuterol differs from ephedrine in four important ways:
- Albuterol acts directly at beta receptors, while ephedrine works mostly indirectly by stimulating norepinephrine release. This allows greater activity from albuterol.
- Albuterol acts selectively at beta-2 receptors which promote fat loss, with relatively little effect at beta-1 receptors of the heart. In contrast, ephedrine works about equally at both receptor types. This selectivity enables higher effective dosing of albuterol for same or lesser effect on the heart.
- Albuterol does not activate alpha receptors, which act to impede fat loss. Ephedrine indirectly activates alpha receptors as well as beta receptors, which reduces its potential efficacy particularly with “stubborn fat.”
Albuterol is more similar pharmacologically to clenbuterol than to ephedrine. Here, the differences are:
- Albuterol has a half-life of only 4-6 hours, while clenbuterol’s half-life is about 36 hours. This means albuterol levels can be higher during waking hours and lower while sleeping. In contrast, clenbuterol levels remain near-constant day and night, giving the body no respite from the stimulation. Sleep disturbance is common.
- Clenbuterol is an effective agonist of beta-3 receptors as well as beta-2 receptors, while albuterol has little effect at beta-3 receptors. While there’s some dispute as to the importance of beta-3 receptors in man, their activation certainly has some benefit to fat loss. On this point, the advantage is to clenbuterol.
- Clenbuterol acts towards blocking sodium current in muscle fibers, which can interfere with strength. Albuterol has no such adverse effect, and in fact typically provides a small increase in strength.
- Clenbuterol appears to pose greater risk to the heart than albuterol does. For example, clenbuterol administration can cause cardiac lesions, while albuterol has not been found able to cause this.
Additionally, albuterol typically seems not as “harsh” feeling as clenbuterol or may even be enjoyed for its feel or effect on mental focus, and seems more effective for nutrient partitioning while seeking to gain muscle mass.
Receptor Downregulation, And How To Avoid It
When used two or more times per day every day, albuterol will slowly induce downregulation of beta receptors. At first, efficacy can be restored by increasing dose. This can be an acceptable approach, although dose shouldn’t be more than doubled. However, the increased dose results in yet more downregulation, and further loss of efficacy that cannot be regained.
However, avoiding downregulation is simplicity itself. All that’s needed is to take ketotifen 1 mg daily before bed.
Ketotifen use not only allows continued efficacy of albuterol without increase of dose, it also aids sleep – which sometimes is a problem during an albuterol cycle – and provides beneficial reduction of TNF-alpha, which often is elevated from intensive exercise. Since elevated TNF-alpha can lower testosterone and IGF-1, this action of ketotifen can be a significant benefit.
I definitely advocate using ketotifen, if possible, when using albuterol two or more times per day.
Benadryl 25-50 mg can be used as an alternate to ketotifen, but is less preferred.
For long term usage, another approach to avoid or minimize downregulation is to take albuterol only on arising at an amount of 4-6 mg. While this of course is less effective than a full-on albuterol cycle, it can still provide significant benefit with no apparent issues with downregulation, and can be continued as long as desired.
How To Take Albuterol
Albuterol should be taken as tablets or liquid, not via inhaler.
If having no experience with albuterol, a usually-suitable starting dose is 4 mg on arising, 2 mg about 4-6 hours later only if feeling ready for it, and another 2 mg four to six hours after that, again only if feeling ready for it. If at the end of the day it seems dosing should have been a little more, the next day, dosing can be increased, until total dosing for the day reaches about 16 mg. This is assuming that ketotifen or Benadryl are being taken as well, as is highly preferable.
Optionally, albuterol dosing can be twice per day, with the second dose in the early afternoon. This may be preferred if having trouble with sleep.
Caffeine at about 200 mg about three times per day will considerably improve albuterol’s fat loss effect, and is highly recommended.
While albuterol can be dosed multiple times per day continuously within the dosage limits discussed, it’s not necessarily completely safe to do so. When considering benefits to risk, doing so is safe enough for diseased patients, but it would be unwarranted to say they experience no harm from unending stimulation. While I have no proof that it’s unwise to use albuterol multiple times per day continuously, as opinion I suggest that it’s more conservative to cycle such use.
When ketotifen or Benadryl aren’t used to avoid downregulation, tapering is advisable after an albuterol cycle. The specific method is not important: any gradual reduction is fine.
A taper may be omitted or may be quicker when ketotifen or Benadryl were used to avoid downregulation.
When To Use Albuterol
Particularly effective times to use albuterol are during anabolic steroid cycles and fat loss cycles, and when particularly needing to increase strength or endurance. (Note: improved exercise endurance is experienced only by some, not all.)
When using ketotifen or Benadryl, albuterol use can continue effectively and with reasonable safety throughout the duration of such cycles.
Possible Adverse Side Effects
The principal possible adverse side effects of albuterol are increased or irregular heart rate, increased blood pressure, chest pain, increased difficulty in urination if having BPH, tremors, headache, anxiety, cramps, allergic reaction, or excessive muscle pumps. Albuterol use can also cause loss of potassium and loss of taurine.
Taurine supplementation, for example 3-5 g/day, generally solves any muscle pump problem and almost certainly addresses any problem of loss. Potassium supplementation is probably unnecessary when consuming a diet with ample fruits and vegetables, but is advisable where these are lacking. A simple way to supplement potassium is to use Lite Salt in moderate amounts.
During an anabolic steroid cycle, it can be especially problematic for a drug to increase blood pressure, as anabolic steroids themselves also can have this effect. In some cases this can rule out or limit concurrent albuterol use.
What About Stacking Albuterol With Thyroid Hormone?
Both albuterol and thyroid hormone (T3 or T4) are effective fat loss agents, and therefore one might desire to combine them. However because both act to stimulate the heart, DO SO ONLY WITH EXTREME CAUTION AND NEVER WITH HIGH THYROID DOSING.
Other Drug And Disease Interactions
Albuterol should be used only with medical supervision where heart conditions, high blood pressure, diabetes, high blood pressure, seizures, glaucoma, kidney disease, potassium imbalance, psychiatric conditions, or hyperthyroidism exist, or during pregnancy or breastfeeding. It should not be combined with beta blockers, asthma medications, allergy medications, cold medicines, antidepressants, or MAO inhibitors without medical supervision.
Choosing Between Ephedrine, Albuterol, And Clenbuterol
Ephedrine can be the choice when wishing a natural supplement or when it can be obtained but not albuterol or clenbuterol, or when simply having a personal preference for it. Its fat-loss effectiveness is very good, but not as good as that of the pharmaceuticals.
Albuterol can be the choice when wishing near-optimal fat loss together with excellent aid in muscle and strength retention or even gain, or when seeking improved muscle gain while minimizing or avoiding fat gain.
Clenbuterol can be the hardcore choice when needing even a slightly greater edge in cutting at the price of greater perceived harshness and possible small compromise in strength.
While I don’t dissuade any bodybuilder from trying clenbuterol at least once, I’d suggest any clenbuterol user try albuterol for comparison. Many or most who do, don’t go back.
Despite the needed cautions above, albuterol is a generally safe compound for fat loss when used correctly and also can be of value for improved endurance and strength. Best use is typically two or three doses per day totaling up to 16 mg/day together with caffeine 200 mg 3x/day and ketotifen 1 mg/day taken before bed.