Salbutamol

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Salbutamol is a B2 adrenergic agonist drug. In 1969 one of the biggest pharmaceutical companies, GlaxoSmithKline launched salbutamol l (also kown as Ventolin).The company focused on discovering chemical substances to change their natural mediators and observe their effects in specific organs of patients. The research was led by David Jack [1]. Salbutamol was found to dilate the bronchi by acting on B2 receptors on bronchial smooth muscle, salbutamol acts on G-protein receptors causing activation of adenylyl cyclase and increasing cAMP then causing smooth muscle to be relaxed [2]. Salbutamol is commonly administered in an aerosol form puff inhaler.

Contents

Salbutamol and Asthma

It was also discovered that Salbutamol inhibits realease of mast cells, hence decreasing histamine as well [3]. Salbutamol is administered to treat asthma by inhaling it, using an inhaler. The elimination half-life, clearance rate and elimination rate constant of salbutamol in the body is 3.35 ± 1.07 h, 256.12 ± 3.55 ml/min and 0.24 ± 0.09 h-1, respectively. Salbutamol lasts for 4-6 hours in the body [4]. Other drugs used to treat asthma are Muscaranic agonists like Ipratropium, Xanthines like Theophylline, also Glucorticoids like Beclomethasone,Prednisolone and Hydrocortisone. Sodium Cromolyn a mast cell stabiliser and inhibits hyper-responsivity is also used to treat asthma [5].

Side effects of using Salbutamol as a treatment

Tremor, a salbutamol induced tremor can either be long term or short term and occurs in 2-4% of regular Salbutamol takers. The tremor is dose-related, and the theory of why it causes the tremor is still unexplained. However, the initial understanding suggests that the B2 adrenoreceptor agonist (salbutamol) has a direct effect on the muscles active state this ' leads to incomplete fusion and reduced tension of tetanic contractions. More recently, tremor has been correlated closely with hypokalaemia [6].

Increased pulse and tolerance are the main side effects of using salbutamol.

Genetic variation in drug response

Several polymorphisms in the gene encoding the beta-adrenoreceptor can affect drug response in individuals. Up to half the variability between individuals to the response of beta 2 agonists, such as Salbutamol, has been suggested to be due to polymorphisms in the genome [7].

References

  1. http://www.gsk.com/about/history-nofalsh.htm
  2. Heitsch H,Drug News Perspect 'Bradykinin B2 receptor as a potential therapeutic target', 2000 May;13(4):213-25
  3. Heitsch H,Drug News Perspect'Bradykinin B2 receptor as a potential therapeutic target',2000 May;13(4):213-25
  4. Narasimha Murthy S,Int J Pharm,'Clinical pharmacokinetic and pharmacodynamic evaluation of transdermal drug delivery systems of salbutamol sulfate',2004 Dec 9;287(1-2):47-53
  5. http://www.healthcentral.com/asthma/find-drug.htm
  6. Cazzola M1, Matera MG. fckLRPulm Pharmacol Ther. 2012 Feb;25(1):4-10. doi: 10.1016/j.pupt.2011.12.004. Epub 2011 Dec 24.fckLR http://www.ncbi.nlm.nih.gov/pubmed/22209959
  7. Drazen J M, Silverman E K, Lee T H. Heterogeneity of therapeutic responses in asthma. Br Med Bull 2000. 561054–1070.1070
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