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Salbutamol, also known as albuterol and marketed as Ventolin among other names,
Common side effects include shakiness, headache, fast heart rate, dizziness, and feeling anxious.
Salbutamol was first made in 1967 in Britain and became commercially available in the UK in 1969.
1 Medical uses
2 Adverse effects
4.1 Structure and activity
6 Society and culture
8 Veterinary use
9 See also
11 External links
Salbutamol is typically used to treat bronchospasm (due to any cause—allergic asthma or exercise-induced), as well as chronic obstructive pulmonary disease.
As a β 2 agonist, salbutamol also has 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 While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium channel blocker nifedipine, which is more effective, better tolerated, and administered orally.
Salbutamol has been used to treat acute hyperkalemia, as it stimulates potassium flow into cells, thus lowering the potassium in the blood.
The most common side effects are fine tremor, anxiety, headache, muscle cramps, dry mouth, and palpitation.
The tertiary butyl group in salbutamol makes it more selective for β 2 receptors,
Salbutamol is either filtered out by the kidneys directly or is first metabolized into 4′-O-sulphate, which is excreted in the urine.
Structure and activity
( R )-(−)-salbutamol (top) and ( S )-(+)-salbutamol (bottom)
Salbutamol is sold as a racemic mixture. The ( R )-(−)- enantiomer ( CIP nomenclature ) is shown in the image at right (top), and is responsible for the pharmacologic activity; the ( S )-(+)-enantiomer (bottom) blocks metabolic pathways associated with elimination of itself and of the pharmacologically active enantiomer ( R ).
Salbutamol was discovered in 1966 by a team led by David Jack at the Allen and Hanburys laboratory (a subsidiary of Glaxo ) in Ware, Hertfordshire, England, and was launched as Ventolin in 1969.
The 1972 Munich Olympics were the first Olympics where anti-doping measures were deployed, and at that time beta-2 agonists were considered to be stimulants with high risk of abuse for doping. Inhaled salbutamol was banned from those games, but by 1986 was permitted (although oral beta-2 agonists were not). After a steep rise in the number of athletes taking beta-2 agonists for asthma in the 1990s, Olympic athletes were required to provide proof that they had asthma in order be allowed to use inhaled beta-2 agonists.
Society and culture
International wholesale price of 200 doses of salbutamol
Ventolin 2 mg tablets made by GSK (Turkey)
Salbutamol is the INN (international nonproprietary name) while albuterol is the USAN (United States adopted name). The drug is usually manufactured and distributed as the sulphate salt (salbutamol sulphate).
It was first sold by Allen & Hanburys (UK) under the brand name Ventolin, and has been used for the treatment of asthma ever since.
As of 2011
Abuse of the drug may be confirmed by detection of its presence in plasma or urine, typically exceeding 1000 ng/mL. 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,
Salbutamol has been studied in subtypes of congenital myasthenic syndrome associated with mutations in Dok-7.
It has also been tested in a trial aimed at treatment of spinal muscular atrophy ; it is speculated to modulate the alternative splicing of the SMN2 gene, increasing the amount of the SMN protein whose deficiency is regarded as a cause of the disease.
Salbutamol’s low toxicity makes it safe for other animals and thus is the medication of choice for treating acute airway obstruction in most species.
Toxic effects require an extremely high dose, and most overdoses are due to dogs chewing on and puncturing an inhaler or nebulizer vial.
Levosalbutamol – the ( R )-(−)-enantiomer
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