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ny science
(Salbutamol)
Joel Torres
Youssef Tahiri

Salbutamol
 Accession Number: DB01001 (APRD00553)
 Type: small molecule
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.

 Systematic (IUPAC) name
(RS)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
 Pharmacokinetic data
Metabolism: Hepatic
Half-life: 1.6 hours
Excretion: Renal

 Identifiers
CAS number: 18559-94-9
ATC code: R03AC02 R03CC02
PubChem: CID 2083
IUPHAR ligand: 558
Drug Bank: DB01001
 Chemical data
Formula: C13H21NO3
Mol. Mass: 239.311

Brand names
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.

Pharmacology
Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic
receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of
bronchial smooth muscles.
Chemistry
Structure-activity relationships
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.

Synthesis
Salbutamol can be prepared from an acetophenone derivative which is itself derived from
salicylic acid

Medical uses
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.

Adverse effects
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.

Society and culture
Doping
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.

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.

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Salbutamol Joel Torres

  • 2. Joel Torres Youssef Tahiri Salbutamol  Accession Number: DB01001 (APRD00553)  Type: small molecule 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.  Systematic (IUPAC) name (RS)-4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
  • 3.  Pharmacokinetic data Metabolism: Hepatic Half-life: 1.6 hours Excretion: Renal  Identifiers CAS number: 18559-94-9 ATC code: R03AC02 R03CC02 PubChem: CID 2083 IUPHAR ligand: 558 Drug Bank: DB01001  Chemical data Formula: C13H21NO3 Mol. Mass: 239.311 Brand names 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. Pharmacology Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles.
  • 4. Chemistry Structure-activity relationships 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. Synthesis Salbutamol can be prepared from an acetophenone derivative which is itself derived from salicylic acid Medical uses 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. Adverse effects
  • 5. 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. Society and culture Doping 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. 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.