|Systematic (IUPAC) name|
|Pregnancy cat.||A (AU) C (US)|
|Legal status||Pharmacist Only (S3) (AU) F (prescription) (CA) POM (UK) ℞-only (US)|
|Routes||Oral, inhalational, IV|
|ATC code||R03 R03|
|(what is this?)|
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 as Ventolin among other brand names.
Salbutamol was the first selective β2-receptor agonist to be marketed in 1968. It was first sold by Allen & Hanburys under the brand name Ventolin. The drug was an instant success, and has been used for the treatment of asthma ever since.
Salbutamol sulfate is sold in the USA as Ventolin HFA, ProAir HFA, or Proventil HFA, and is also available in extended release tablets. It is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebulizer 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 20 minutes of dosing, though some relief is immediately seen. It can also be given intravenously.
Salbutamol is typically used to treat bronchospasm (due to any cause, allergen asthma or exercise-induced), as well as chronic obstructive pulmonary disease. The dose of Salbutamol remains controversial. It is marketed as a metered dose inhaler which produces an average of 90 micrograms per puff. Most commonly only 2 puffs are recommended every 4 hours as needed for symptoms of asthma by the manufacturer. This produces an average dose of 180 micrograms. Emergency medical practice commonly treats patients presenting with asthma who report taking their Salbutamol (albuterol) inhaler as prescribed. The Emergency Room treatment recommended is a massive dose of Salbutamol given by aerosol nebulization in doses of > 7.5 mg / hour. This is continued until the side effects of tremor or tachycardia become annoying to the patient. In general, patients tolerate this large (> 40 times) fairly well. It is logical to recommend that patients consult with a doctor if albuterol does not provide adequate relief, as using more medication may worsen the patient's condition.
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 labor. 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.
Salbutamol has also been trialled in spinal muscular atrophy where it appears to show modest benefits. The drug is speculated to modulate the alternative splicing of the SMN2 gene, increasing the amount of the SMN protein whose deficiency is regarded as the root cause of the disease.
The most common side effects are fine tremor, anxiety, headache, muscle cramps, dry mouth, and palpitation. Other symptoms may include tachycardia, arrhythmia, flushing, myocardial ischemia (rare), and disturbances of sleep and behaviour. Rarely occurring, but of importance, are allergic reactions of paradoxical bronchospasm, urticaria, angioedema, hypotension, and collapse. High doses may cause hypokalaemia, which is of concern in patients with renal failure and those on certain diuretics and xanthine derivatives.
Society and culture
Diet and bodybuilding use
Salbutamol has been shown to improve muscle weight in rats  and anecdotal reports hypothesise that it might be an alternative to clenbuterol for purposes of fat burning and muscle gain, though there have been no studies of this variety undertaken. Abuse of the drug may be confirmed by detection of its presence in plasma or urine, typically exceeding 1000 µg/L.
Clinical studies show no compelling evidence that salbutamol and other β2-agonists can increase performance in healthy athletes. In spite of this, salbutamol required "a declaration of Use in accordance with the International Standard for Therapeutic Use Exemptions" under the 2010 WADA prohibited list. This requirement was relaxed when the 2011 list was published to permit the use of "salbutamol (maximum 1600 micrograms over 24 hours) and salmeterol when taken by inhalation in accordance with the manufacturers’ recommended therapeutic regimen." 
Another study contradicts the above findings, however. The double blind, randomised test conducted on 12 non-asthmatic athletes concluded that salbutamol had a negligible effect on endurance performance. Nevertheless, the study also showed that the drug's bronchodilating effect may have improved respiratory adaptation at the beginning of exercise.
Detection of use
Salbutamol may be quantified in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients or to aid in a forensic investigation. Urinary salbutamol concentrations are frequently measured in competitive sports programs, for which a level in excess of 1000 μg/L is considered to represent abuse. The window of detection for urine testing is on the order of just 24 hours, given the relatively short elimination half-life of the drug.
The tertiary butyl group in salbutamol (or albuterol) makes it more selective for β₂-receptors. The drug is sold as a racemic mixture mainly because the (S)-enantiomer blocks metabolism pathways while the (R)-enantiomer shows activity.
Salbutamol can be prepared from an acetophenone derivative which is itself derived from salicylic acid (hence the "sal" in salbutamol).
It is marketed by GlaxoSmithKline as Ventolin, Ventoline, Ventilan, Aerolin or Ventorlin, depending on the market; by Cipla as Asthalin and Asthavent; by Schering-Plough as Proventil, by Teva as ProAir, Salamol or Airomir, by Beximco (Bangladesh) as AZMASOL by Ad-din Pharma as Ventosol and by Alphapharm as Asmol.
- Health Canada
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- Volmax Drug Information
- Side Effects
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