Salbutamol
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Salbutamol
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Systematic (IUPAC) name | |
4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol | |
Identifiers | |
CAS number | |
ATC code | R03 R03CC02 |
PubChem | |
DrugBank | |
Chemical data | |
Formula | C13H21NO3 |
Mol. mass | 239.311 |
SMILES | & |
Pharmacokinetic data | |
Bioavailability | ? |
Metabolism | Hepatic |
Half life | 1.6 hours |
Excretion | Renal |
Therapeutic considerations | |
Pregnancy cat. | |
Legal status | |
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 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), 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 as an inhalant or intravenously. However, some asthmatics do not have the required DNA base sequence in a specific gene and may not respond to these medications.
Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the trade name Ventolin.
Contents[hide] |
[edit] Clinical use
Salbutamol is specifically indicated in the following conditions:
- acute asthma
- symptom relief during maintenance therapy of asthma and other conditions with reversible airways obstruction (including COPD)
- protection against exercise-induced asthma
- hyperkalaemia, especially in patients with renal failure
- can be aerosolized with a nebulizer for patients with cystic fibrosis, along with ipratropium bromide and pulmozyme.
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 Whilst preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine which is more effective, better tolerated and orally administered.[1]
[edit] Diet and bodybuilding use
Salbutamol is taken by some as an alternative to Clenbuterol for purposes of fat burning.[2]
[edit] Ban of CFC-containing albuterol inhalers
The U.S. Food & Drug Administration in April of 2005 mandated that all (including albuterol) inhalers containing chlorofluorocarbons (CFCs) will be prohibited in the United States as of 12/31/2008. CFC inhalers had previously been given "essential use" status, exempting it from a CFC-production ban, however in accordance with the Montreal Protocol they will be phased out; in many other countries patients have been transitioned to non-CFC based inhalers using hydrofluoroalkane (HFA) propellant. Pharmaceutical manufacturers are expected to produce adequate supplies of alternative (HFA) inhalers by 2009.[citation needed]
One drawback of this transition to HFA inhalers is that due to patent restrictions all of the HFA albuterol inhalers are "brand-name" (ProAir, Proventil, and Ventolin). They cost approximately $20 more per inhaler than existing generic CFC albuterol inhalers. Generic HFA albuterol inhalers are not expected on the market until 2017 due to existing patents, although some pharmaceutical companies will offer discounts for those who cannot afford the HFA inhalers.[citation needed]
Benefits of transitioning to HFA inhalers include (1) increased drug deposition in the distal airways, (2) more consistent drug delivery from nearly empty canisters, and (3) more consistent drug delivery at a greater range of canister temperatures. It should be noted that the spray force of HFA inhalers is less than that of CFC inhalers, which may mislead some patients to believe that they may not be receiving enough albuterol when in fact they are seeing the benefits as outlined above.[citation needed]
[edit] References
- ^ Rossi S (Ed.) (2004). Australian Medicines Handbook 2004 (AMH). Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
- ^ Carter WJ, Lynch ME. Comparison of the effects of salbutamol and clenbuterol on skeletal muscle mass and carcass composition in senescent rats. Metabolism. 1994
[edit] Additional notes
- 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.
- 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
- 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
- The effects of Albuterol and isokinetic exercise on the quadriceps muscle group.Med Sci Sports Exerc. 1995 Nov;27(11):1471-6
- Salbutamol, a beta 2-adrenoceptor agonist, increases skeletal muscle strength in young men.Martineau L, Horan MA, Rothwell NJ, Little RA
- 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
- 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
[edit] External links
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