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salbutamol

  (săl-byū'tə-môl', -mōl', -mŏl') pronunciation
n.

A sympathomimetic agent, C13H21NO3, used as a bronchodilator, especially in the treatment of asthma.

[SAL(ICYLIC ACID) + BUT(YL) + AM(INO)– + –OL1.]


 
 

A drug belonging to the beta2-agonists. Salbutamol is an effective bronchodilator used to treat exercise-induced asthma and some other forms of respiratory distress. Although beta2-agonists are on the World-Doping Agency's (WADA's) 2005 Prohibited List, therapeutic use of inhaled salbutamol is permitted (subject to written notification) for the treatment of asthma and other respiratory conditions. However, it should be noted that WADA's 2006 guidelines stress that a concentration of greater than 1000 ng l−1 will be deemed a failure in dope tests, even if an athlete has been granted Therapeutic Use Exemption.

 
Medical Dictionary: sal·bu·ta·mol
(săl-byū'tə-môl', -mōl')
n.

A sympathomimetic agent used as a bronchodilator, especially in the treatment of asthma.

 
Wikipedia: salbutamol
Salbutamol-racemic-2D-skeletal.png
Salbutamol
Systematic (IUPAC) name
2-(hydroxymethyl)-4-[1-hydroxy-

2-(tert-butylamino)ethyl]phenol

Identifiers
CAS number 18559-94-9
ATC code R03AC02 R03CC02
PubChem 2083
DrugBank APRD00553
Chemical data
Formula C13H21NO3 
Mol. mass 239.311
SMILES search in eMolecules, PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 1.6 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

A(AU) C(US)

Legal status

Pharmacist Only (S3)(AU) ?(CA) POM(UK) -only(US)

Routes Oral, inhalational, IV

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.

Salbutamol sulphate 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 or intravenously. However, some asthmatics may not respond to these medications as they will not have the required DNA base sequence in a specific gene.

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:

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. Whilst 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.[1]

Diet and Bodybuilding use

Salbutamol is taken by some as an alternative to Clenbuterol for purposes of fat burning.[2]

Mode of action

As with other β2-adrenergic receptor agonists, salbutamol binds to β2-adrenergic receptors with a higher affinity than β1-receptors. In the airway, activation of β2-receptors results in relaxation of bronchial smooth muscle resulting in a widening of the airway (bronchodilation). Inhaled salbutamol sulfate has a rapid onset of action, providing relief within five to fifteen minutes of administration.

In tocolysis, the activation of β2-receptors results in relaxation of uterine smooth muscle, thus delaying labour.

Adverse effects

While salbutamol is well-tolerated, particularly when compared with previous therapies such as theophylline, like all medications there exists the potential for adverse drug reactions to occur - especially when in high doses, or when taken orally or intravenously.

Common adverse effects include: tremor, palpitations and headache. (Rossi, 2004)

Infrequent adverse effects include: tachycardia, muscle cramps, agitation, hypokalemia, tinnitus, hyperactivity in children, and insomnia.[1]

The (S) enantiomer of salbutamol can inhibit the anti-inflammatory effect of steroids prescribed to treat asthma. However, the (R) enantiomer can stimulate the steroid's effect and the overall effect of the two isomers is unclear.[3]

Other brand names

Salbutamol is sold under the brand names Aerolin, Airomir, Asthalin, Asthavent, Asmol, Buventol, ProAir, Proventil, Salamol, Sultanol, Ventolin, and Volmax.

Levalbuterol, the R-enantiomer of salbutamol, is sold as Xopenex.

Ban of CFC-Containing Albuterol Inhalers

U.S. regulators have announced that albuterol inhalers containing chlorofluorocarbons (CFCs) will be banned in the United States beginning in 2009. This type of asthma inhaler had previously been given "essential use" status, exempting it from a national CFC-production ban. However, GlaxoSmithKline, Ivax Corp., and other manufacturers are expected to produce adequate supplies of alternative inhalers by 2009 and will offer discounts for those who cannot afford the newer versions, which cost about $20 more.

Curiously, in the United Kingdom, Australia and New Zealand, inhalers have been CFC free for some years now, which could bring into question the pricing issue.

References

  1. Anabolic effects of the beta 2-adrenoceptor agonist salmeterol are dependent on route of administration N. G. Moore, G. G. Pegg, and M. N. Sillence Am J Physiol Endocrinol Metab, Sep 1994; 267: E475 - E484.
  2. Schiffelers SL, Saris WH, Boomsma F, and van Baak MA. beta(1)- and beta(2)-Adrenoceptor-mediated thermogenesis and lipid utilization in obese and lean men. J Clin Endocrinol Metab 86: 2191-2199, 2001
  3. Effect of salbutamol on muscle strength and endurance performance in nonasthmatic men. Med Sci Sports Exerc. 2000 Jul;32(7):1300-6. J Strength Cond Res. 2005 Feb;19(1):102-7. Oral Albuterol dosing during the latter stages of a resistance exercise program
  4. The effects of Albuterol and isokinetic exercise on the quadriceps muscle group.Med Sci Sports Exerc. 1995 Nov;27(11):1471-6
  5. Salbutamol, a beta 2-adrenoceptor agonist, increases skeletal muscle strength in young men.Martineau L, Horan MA, Rothwell NJ, Little RA
  6. Different Ability of Clenbuterol and Salbutamol to Block Sodium Channels Predicts Their Therapeutic Use in Muscle Excitability Disorders Jean-François Desaphy, Sabata Pierno, Annamaria De Luca, Paola Didonna, and Diana Conte Camerino Mol. Pharmacol., Mar 2003; 63: 659
  7. Metabolism. 1996 Jun;45(6):712-7 Effects of oral albuterol on serum lipids and carbohydrate metabolism in healthy men. Maki KC, Skorodin MS, Jessen JH, Laghi F

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    Copyrights:

    Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2007. Published by Houghton Mifflin Company. All rights reserved.  Read more
    Sports Science and Medicine. The Oxford Dictionary of Sports Science & Medicine. Copyright © Michael Kent 1998, 2006, 2007. All rights reserved.  Read more
    Medical Dictionary. The American Heritage® Stedman's Medical Dictionary Copyright © 2002, 2001, 1995 by Houghton Mifflin Company Read more
    Wikipedia. This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Salbutamol" Read more

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