Albuterol 18559-94-9
Salbutamol or albuterol 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, Aerolin or Ventorlin depending on the market; by Cipla as Asthalin; by Schering-Plough as Proventil and by Teva as ProAir. 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 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 twenty minutes of dosing, though some relief is immediately seen. Salbutamol can also be given orally as an inhalant or intravenously.
Clinical use
Salbutamol is specifically indicated in the following conditions:*Acute asthma*Symptom relief during maintenance therapy of asthma and other conditions with reversible or irreversible airways obstruction (including COPD and bronchitis)*Protection against exercise-induced asthma*Can be aerosolized with a nebulizer for patients with cystic fibrosis, along with ipratropium bromide, acetylcysteine, and pulmozyme. *Subtypes of congenital myasthenic syndromes associated to mutations in Dok-7. 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 While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine which is more effective, better tolerated and orally administered. In an emergency, EMS providers consider the administration of salbutamol when they see active wheezing, bronchospasm and a past diagnosis of asthma. The drug is most often administered through a nebulizer with 6-8 liters per minute of oxygen. A normal dose is 2. 5 mg in 3 mL of respiratory saline.
Side effects / health consequences
The most common side effects are of fine tremor, nervousness, headache, muscle cramps, dry mouth, and palpitation. Other symptoms may be tachycardia (rapid heart rate), arrhythmias, flushing, myocardial ischaemia, and disturbances of sleep and behaviour. Abuse of the drug may be confirmed by detection of its presence in plasma or urine, typically in the 10-500 µg/L range.
Doping
Clinical studies show no compelling evidence that Salbutamol and other beta 2 antagonists can increase performance in healthy athletes. In spite of this, Salbutamol remains on WADAs prohibited list and many athletes have been banned for use of salbutamol. According to two small and limited studies, performed on 8 and 16 subjects respectively, Salbutamol increases the performance even for a person without asthma.
Ban of CFC-containing inhalers
Asthalin HFA inhaler made by Cipla (India){{Globalize/North America
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date=December 2009
discuss=Talk:Salbutamol#Globalize
| Systematic (IUPAC) name: | (RS)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol |
|---|---|
| Albuterol CAS number: | 18559-94-9 |
| ATC code: | R03AC02 R03CC02 |
| PubChem: | 2083 |
| DrugBank: | APRD00553 |
| Formula: | C13H21N1O3 |
| Molecular mass: | 239.311 g/mol |
| Albuterol Assay/Purity: | Typically NLT 98% |
