Salbutamol
Discovery
Chiral chemistry was introduced in 1848 by French chemist and biologist, Louis Pasteur. He discovered this new branch of chemistry after he separated two isomers of ammonium tartate (1). This paved the way for several progressions in the pharmaceutical industry. Although it took approximately a century for scientists to use chiral compounds as effective drugs, they have played a remarkable role in the life of plants and animals (1). The credit for discovering the chiral drug Salbutamol goes to Sir David Jack (2). Sir David Jack was highly respected and known for his dedication and innovation in drug development. He worked at the Allen and Hanburys site at Ware and developed several new medicines (2). One of his greatest …show more content…
Within the Salbutamol molecule, there is an active and inactive component. The active component is known as albuterol sulphate (10). Below is the chemical structure for albutemol sulphate.
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Albutemol sulphate is a white crystalline powder that is soluble in water, thus rendering it for good use as medication (10). The albutemol sulphate is suspended in hydrofluoroalkane propellant known as HFA – 134a, in asthma inhalers (12). The propellant HFA – 134a is the inactive component of salbutamol (10). Below is the chemical structure for HFA – 134a.
http://www.intechopen.com/books/advances-in-modeling-of-fluid-dynamics/pmdi-sprays-theory-experiment-and-numerical-simulation
After inhalation, beta2-adrenergic receptors on the smooth muscles of the airways are activated. This activation leads to the activation of the enzyme adenycyclase and an increase in concentration of cyclic AMP. The increase of cyclic AMP results in activating the protein kinase which lowers ionic calcium concentrations within the cells and stops the phosphorylation of myosin (12). This result is relaxation in the muscles, opening the airways and bringing an asthmatic patient relief. Albuterol relaxes smooth muscles from the trachea to the terminal bronchioles bringing about relief from any problems caused by bronchoconstriction …show more content…
Pharmacological activity of enantiomers of Salbutamol:
Salbutamol, the most generally utilized short-acting β2-agonist, comprises of a racemic mixture of equivalent measures of two enantiomers, (R)-salbutamol and (S)-salbutamol. The bronchodilator impacts of salbutamol are credited altogether to (R)-salbutamol (levosalbutamol), while (S)-salbutamol has been demonstrated to have bronchospastic and expert provocative impacts both in vitro and in vivo studies. Levosalbutamol, the (R)-enantiomer of salbutamol is presently accessible just in a fluid detailing for utilization through a nebulizer.
Beta2-adrenoceptor agonists, for example salbutamol, are broadly utilized as bronchodilators within the treatment of asthma. They are chiral medications verifiably showcased as racemic mixtures of an active (eutomer) and basically idle (distomer) stereoisomer. Regardless of their clear restorative quality and far reaching utilization, beta2-agonists have been ensnared, to a degree dubiously, in creating an increment in asthma mortality and a decay of asthma control by an instrument that remaining parts
Discovery
Chiral chemistry was introduced in 1848 by French chemist and biologist, Louis Pasteur. He discovered this new branch of chemistry after he separated two isomers of ammonium tartate (1). This paved the way for several progressions in the pharmaceutical industry. Although it took approximately a century for scientists to use chiral compounds as effective drugs, they have played a remarkable role in the life of plants and animals (1). The credit for discovering the chiral drug Salbutamol goes to Sir David Jack (2). Sir David Jack was highly respected and known for his dedication and innovation in drug development. He worked at the Allen and Hanburys site at Ware and developed several new medicines (2). One of his greatest …show more content…
Within the Salbutamol molecule, there is an active and inactive component. The active component is known as albuterol sulphate (10). Below is the chemical structure for albutemol sulphate.
http://www.drugs.com/pro/ventolin.html
Albutemol sulphate is a white crystalline powder that is soluble in water, thus rendering it for good use as medication (10). The albutemol sulphate is suspended in hydrofluoroalkane propellant known as HFA – 134a, in asthma inhalers (12). The propellant HFA – 134a is the inactive component of salbutamol (10). Below is the chemical structure for HFA – 134a.
http://www.intechopen.com/books/advances-in-modeling-of-fluid-dynamics/pmdi-sprays-theory-experiment-and-numerical-simulation
After inhalation, beta2-adrenergic receptors on the smooth muscles of the airways are activated. This activation leads to the activation of the enzyme adenycyclase and an increase in concentration of cyclic AMP. The increase of cyclic AMP results in activating the protein kinase which lowers ionic calcium concentrations within the cells and stops the phosphorylation of myosin (12). This result is relaxation in the muscles, opening the airways and bringing an asthmatic patient relief. Albuterol relaxes smooth muscles from the trachea to the terminal bronchioles bringing about relief from any problems caused by bronchoconstriction …show more content…
Pharmacological activity of enantiomers of Salbutamol:
Salbutamol, the most generally utilized short-acting β2-agonist, comprises of a racemic mixture of equivalent measures of two enantiomers, (R)-salbutamol and (S)-salbutamol. The bronchodilator impacts of salbutamol are credited altogether to (R)-salbutamol (levosalbutamol), while (S)-salbutamol has been demonstrated to have bronchospastic and expert provocative impacts both in vitro and in vivo studies. Levosalbutamol, the (R)-enantiomer of salbutamol is presently accessible just in a fluid detailing for utilization through a nebulizer.
Beta2-adrenoceptor agonists, for example salbutamol, are broadly utilized as bronchodilators within the treatment of asthma. They are chiral medications verifiably showcased as racemic mixtures of an active (eutomer) and basically idle (distomer) stereoisomer. Regardless of their clear restorative quality and far reaching utilization, beta2-agonists have been ensnared, to a degree dubiously, in creating an increment in asthma mortality and a decay of asthma control by an instrument that remaining parts