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Salbutamol is a B<sub>2</sub> [[Adrenergic|adrenergic]]&nbsp; [[Agonist|agonist]] drug. In 1969 one of the biggest pharmaceutical companies, [[GlaxoSmithKline|GlaxoSmithKline]] launched salbutamol l(also kown as [[Ventolin|Ventolin]]).The company focused on discovering chemical substances to change their natural [[Mediators|mediators]] and observe their effects in specific organs of patients.&nbsp;The research was led by [[David Jack|David Jack]]&nbsp;<ref>http://www.gsk.com/about/history-nofalsh.htm</ref>. Salbutamol was found to dilate the [[Bronchi|bronchi]] by acting on B<sub>2</sub> receptors on bronchial smooth muscle, salbutamol acts on [[G-protein Coupled Receptor|G-protein receptors]] causing activation of [[Adenylyl cyclase|adenylyl cyclase]] and increasing [[CAMP|cAMP]] then causing smooth muscle to be relaxed <ref>Heitsch H,Drug News Perspect 'Bradykinin B2 receptor as a potential therapeutic target', 2000 May;13(4):213-25</ref>. Salbutamol is commonly administered in an aerosol form puff inhailler.<u><br></u>
Salbutamol is a B<sub>2</sub> [[Adrenegic receptor|adrenergic]] [[Agonist|agonist]] drug. In 1969 one of the biggest pharmaceutical companies, [[GlaxoSmithKline|GlaxoSmithKline]] launched salbutamol l (also kown as [[Ventolin|Ventolin]]).The company focused on discovering chemical substances to change their natural [[Mediators|mediators]] and observe their effects in specific [[Organ|organs of]] patients.&nbsp;The research was led by [[David Jack|David Jack]]&nbsp;<ref>http://www.gsk.com/about/history-nofalsh.htm</ref>. Salbutamol was found to dilate the [[Bronchi|bronchi]] by acting on B<sub>2</sub> receptors on bronchial smooth muscle, salbutamol acts on [[G-protein Coupled Receptor|G-protein receptors]] causing activation of [[Adenylyl cyclase|adenylyl cyclase]] and increasing [[CAMP|cAMP]] then causing [[Smooth muscle|smooth muscle to]] be relaxed <ref>Heitsch H,Drug News Perspect 'Bradykinin B2 receptor as a potential therapeutic target', 2000 May;13(4):213-25</ref>. Salbutamol is commonly administered in an aerosol form puff inhaler.  


=== Salbutamol and Asthma<br>  ===
=== Salbutamol and [[Asthma|Asthma]]<br>  ===


It was also discovered that Salbutamol inhibits realease of [[Mast cells|mast cells]], hence decreasing [[Histamine|histamine]] as well <ref>Heitsch H,Drug News Perspect'Bradykinin B2 receptor as a potential therapeutic target',2000 May;13(4):213-25</ref>. Salbutamol is administered to treat [[Asthma|asthma]] by inhaling it, using an [[Inhaler|inhaler]].&nbsp;The [[Elimination half-life|elimination half-life]], [[Clearance rate|clearance rate]] and [[Elimination rate constant|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<sup>-1</sup>, respectively. Salbutamol lasts for 4-6 hours in the body <ref>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</ref>. Other drugs used to treat asthma are [[Muscaranic|Muscaranic]] [[Agonists|agonists]] like [[Ipratropium|Ipratropium]], [[Xanthines|Xanthines]] like [[Theophylline|Theophylline]], also [[Glucorticoids|Glucorticoids]] like [[Beclomethasone|Beclomethasone]],[[Prednisolone|Prednisolone]] and [[Hydrocortisone|Hydrocortisone]]. [[Sodium Cromolyn|Sodium Cromolyn]] a mast cell stabiliser and inhibits hyper-responsivity is also used to treat asthma <ref>http://www.healthcentral.com/asthma/find-drug.htm</ref>.<br>  
It was also discovered that Salbutamol inhibits realease of [[Mast cells|mast cells]], hence decreasing [[Histamine|histamine]] as well <ref>Heitsch H,Drug News Perspect'Bradykinin B2 receptor as a potential therapeutic target',2000 May;13(4):213-25</ref>. Salbutamol is administered to treat [[Asthma|asthma]] by inhaling it, using an [[Inhaler|inhaler]].&nbsp;The [[Elimination half-life|elimination half-life]], [[Clearance rate|clearance rate]] and [[Elimination rate constant|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<sup>-1</sup>, respectively. Salbutamol lasts for 4-6 hours in the body <ref>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</ref>. Other drugs used to treat asthma are [[Muscaranic|Muscaranic]] [[Agonist|agonists]] like [[Ipratropium|Ipratropium]], [[Xanthines|Xanthines]] like [[Theophylline|Theophylline]], also [[Glucorticoids|Glucorticoids]] like [[Beclomethasone|Beclomethasone]],[[Prednisolone|Prednisolone]] and [[Hydrocortisone|Hydrocortisone]]. [[Sodium Cromolyn|Sodium Cromolyn]] a [[Mast cells|mast cell stabiliser]] and inhibits hyper-responsivity is also used to treat [[Asthma|asthma]] <ref>http://www.healthcentral.com/asthma/find-drug.htm</ref>.<br>  


=== <u></u>Side effects of using Salbutamol as a treatment<u></u><br>  ===
=== <u></u>Side effects of using Salbutamol as a treatment<u></u><br>  ===


[[Tremor|Tremor]], increased pulse and [[Tolerance|tolerance]] are the main side effects of using salbutamol.<br>  
[[Tremor|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|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 [[Hypokalemia|hypokalaemia]]&nbsp;<ref>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</ref>.
 
Increased pulse and [[Tolerance|tolerance]] are the main side effects of using salbutamol.<br>  
 
=== '''Genetic variation in drug response'''  ===
 
Several polymorphisms in the gene encoding the beta-adrenoreceptor can affect drug response in individuals.&nbsp;Up to half the&nbsp;variability between individuals&nbsp;to the&nbsp;response of&nbsp;beta 2 [https://teaching.ncl.ac.uk/bms/wiki/index.php/Agonist agonists], such as Salbutamol, has been suggested to be due to polymorphisms in the genome <ref>Drazen J M, Silverman E K, Lee T H. Heterogeneity of therapeutic responses in asthma. Br Med Bull 2000. 561054–1070.1070</ref>.


=== References  ===
=== References  ===


<references />
<references />

Latest revision as of 15:14, 20 October 2017

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.

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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