Albuterol Medical Drug

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Description

Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed by GlaxoSmithKline as Ventolin or Ventorlin depending on the market; by Cipla as Asthalin; by Schering-Plough as Proventil and by Teva as ProAir. Generic names are currently not available in the U.S. because of a federal ban on the use of CFCs.[1]

Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebuliser or other proprietary delivery devices (e.g. Rotahaler or Autohaler). In these forms of delivery, the maximal effect of Salbutamol can take place within five to twenty minutes of dosing, though some relief is immediately seen. Salbutamol can also be given orally as an inhalant or intravenously.

Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the trade name Ventolin.

Clinical use
Salbutamol is specifically indicated in the following conditions:

Acute asthma
Symptom relief during maintenance therapy of asthma and other conditions with reversible airways obstruction (including COPD and bronchitis)
Protection against exercise-induced asthma
Can induce Hypokalemia, especially in patients with renal failure
Can be aerosolized with a nebulizer for patients with cystic fibrosis, along with ipratropium bromide and pulmozyme.
As a β2-agonist, salbutamol also finds use in obstetrics. Intravenous salbutamol can be used as a tocolytic to relax the uterine smooth muscle to delay premature labour. While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine which is more effective, better tolerated and orally administered.[2]

In an emergency, EMS providers consider the administration of Albuterol when they see Active Wheezing, bronchospasm and a past diagnosis of Asthma. The drug is most often administered through a nebulizer with 15 liters of pure oxygen. A normal dose is aprox. 2.5mg in 3 mL of respiratory saline.


Side effects / health consequences

Tachycardia (rapid heart rate)
Shakiness, nervousness
Hyperkinesis (overactive restlessness, agitation)
Nausea and Vomiting
Reactive bronchospasm
Drowsiness
Aggression
Agitation
Allergic reaction
Anxiety
Back Pain
Excitement
Fluid Retention and Swelling
Flushing
General Bodily Discomfort
Headache
Heart Palpitations
Heartburn
Hives
Hyperactivity
Hypertension
Increased Appetite
Increased Difficulty Breathing
Indigestion
Insomnia, especially in children
Irritability
Lightheadedness
Muscle Cramps
Muscle tremor
Nasal Inflammation
Nervousness
Nightmares
Nosebleed
Rash
Throat irritation
Tooth Discoloration
Tremors
Unusual Taste
Urinary Problems
Weakness
Wheezing
Xerostomia (dry mouth)

Ban of CFC-containing salbutamol inhalers

Ventolin HFA inhaler made by GSK
Asthalin HFA inhaler made by Cipla (India)The U.S. Food & Drug Administration in April 2005 mandated that all (including salbutamol) inhalers containing chlorofluorocarbons (CFCs) will be prohibited in the United States as of 12/31/2008. CFC inhalers had previously been given "essential use" status, exempting it from a CFC-production ban, however in accordance with the Montreal Protocol they will be phased out; in many other countries patients have been transitioned to non-CFC based inhalers using hydrofluoroalkane (HFA) propellant. Pharmaceutical manufacturers are expected to produce adequate supplies of alternative (HFA) inhalers by 2009.

One drawback of this transition to HFA inhalers is that due to patent restrictions all of the HFA salbutamol inhalers are "brand-name" (ProAir, Proventil, and Ventolin). They cost approximately $20 more per inhaler than existing generic CFC salbutamol inhalers. Because the HFA propellants have different chemical and physical properties, inhaler formulations with the new propellants had to be developed. In order to protect the huge investment in time and money, these new formulations were patented. An industry consortium was formed to spread the costs of the FDA safety studies to get propellants such as 134a and 227 approved. See [1]


Generic HFA salbutamol inhalers are not expected on the United States market until 2012 due to existing patents.[2]

Another drawback that is coming to light now as the use of HFA/HFA+ethanol inhalers is expanding seems to be a far higher intolerance of the new inhalers compared to CFC propellant in patients. Registered complaints run the gamut from "doesn't seem to work as well" all the way to serious anaphylaxis in response to using an HFA or HFA+ethanol inhaler.[3]

Salbutamol is widely used, and accounts for anywhere from 78% of all bronchodilator prescriptions in 2005 to 85% in 2008. [4] However, patients in the United States who cannot tolerate the HFA salbutamol inhalers will not have a single salbutamol alternative available to them domestically after December 31, 2008.[5] The FDA did not approve any alternatives to HFA and there are few standard inhaled lung medications in the United States that come in Dry Powder Inhaler (DPI) versions. Noticeably missing is salbutamol in DPI form in the United States, although it is available in most of the rest of the world in salbutamol DPIs.


Diet and bodybuilding use

Salbutamol is taken by some as an alternative to Clenbuterol for purposes of fat burning.[6]


References

^ Unlikely Victims of Banning CFCs--Asthma Sufferers (SciAm)
^ Rossi S (Ed.) (2004). Australian Medicines Handbook 2004 (AMH). Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
^ Home Page
^ IMS Health Sales & Prescription data for all inhalers sales and prescriptions (July 2008)
^ FDA Advises Patients to Switch to HFA-Propelled Albuterol Inhalers Now
^ Carter WJ, Lynch ME (September 1994). "Comparison of the effects of salbutamol and clenbuterol on skeletal muscle mass and carcass composition in senescent rats". Metab. Clin. Exp. 43 (9): 1119-25. PMID 7916118. http://linkinghub.elsevier.com/retrieve/pii/0026-0495(94)90054-X.

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