Salbutamol (also known as albuterol in USA) is one of the most famous short-acting β2 agonists. It has become first line treatment for asthma due to its effectiveness. I met this drug in a dispensing session in the first term and I think is a good example of what we have learnt so far. In this essay I will tell you what I know about this drug. Salbutamol is sold in its sulphate form and is marketed as a racemic product. According pharmaceutical chemistry this means that in it, it has 50% of the R enantiomer and 50% of the S enantiomer. However, only the R enantiomer is active at the β receptors. It is thought that the S enantiomer is inactive or causes adverse effects. Because of this, the pure R enantiomer was marketed – levalbuterol. β receptor agonists are used in the treatment of asthma and COPD (chronic obstructive pulmonary disease) to relax the muscles in the air passages in the lungs. Salbutamol is a selective β2 adrenergic agonist, although this selectivity is relative and dose-dependent. This means that the selectivity is lost at high concentration and thus causing side-effects. Albuterol has affinity to β 2 receptors and binds to them, causing a relaxation effect. β2 receptors are members of the adrenergic family of receptors and therefore its effects are caused by an interaction with G proteins. β
Ever wonder about the chemical makeup of tablets that people take for pain relief? Before a tablet can be successfully made, the limiting and excess reactants must be considered. The limiting reactant will affect the amount of the product that can be made. Another reason why the starting reactants must be determined carefully is to make reduce the amount of the reactant in excess so that reactants are not wasted. This experiment uses an Alka-Seltzer tablet. Alka-Seltzer dissolves in water and is an antacid and a pain reliever1. The Alka-Seltzer tablet has many uses such as relief of headaches, ingestion, heart burns, or even upset stomachs2. The active ingredients in an Alka-Seltzer tablet is aspirin, also known as acetyl-salicylic acid (C8H12O4), citric acid (C6H8O7), and sodium bicarbonate (NaHCO3)2. The aspirin in the Alka-Seltzer tablet helps with pain relief. Because of the acid-base chemistry (Brønsted-Lowry), citric acid and sodium bicarbonate produce O2, which makes the tablet fizz when it is dropped in liquid. The Brønsted-Lowry theory shows how the Brønsted-Lowry acid donates a hydrogen ion while the Brønsted-Lowry base accepts the hydrogen ions3. The remaining NaHCO3 that is in excess post reaction with the citric acid is what is used to neutralize stomach acid which helps relief heart burn2. The problem in
Clenbuterol is similar to steroids in chemistry without being an actual steroid. Traditionally, it is used to treat respiratory illnesses in horses. It is considered to be in the category of beta2 adrenergic agonists, which simply means it works on the beta2 adrenergic receptor. The drug was initially created to treat equine asthma, but it has a similar effect on humans as stimulant drugs. It has not been tested or approved for human use.
Fluticasone propionate is a synthetic triflourinated corticosteroid that possess anti-inflammatory properties (RxList). This corticosteroid targets cells and mediators involved in inflammation, having an anti-inflammatory effect on the airways (RxList). Salmeterol Xinafoate is a long acting- beta agonist (LABA), targets the beta2-adrenoceptors that are present in the smooth muscle of the bronchioles (RxList). By targeting the beta2-adrenoceptors, intracellular adenyl cyclase is stimulated, which will lead to the production of more cyclic AMP. An increased level of cyclic AMP then leads to relaxation of the smooth muscle of bronchioles
Asthma is a “chronic inflammatory disease of the airways” and causes difficulties in breathing due to the widespread narrowing of the bronchial airways1. Asthma can occur in people of all ages and affects approximately 10.2% of Australians (2011-12) 2. Generally asthma is reversible with or without treatment however over time damage may occur3. Therefore it is important for patients to manage their asthma well in order to maintain a healthy and quality lifestyle. One of the most effective treatments used to control asthma is Salbutamol. Salbutamol is a short acting B2 adrenergic agonist and it is mainly used for quick relief or to prevent the onset of asthma3. This essay will explain the physiology of the respiratory system and the effect on the system when a person has asthma. It will also discuss the use of salbutamol as a treatment for asthma.
The production of aspirin begins salicylic acid which has been derived from the active site of salicin found in willow bark. This is done through multi-step process where substrates of salicin are converted into more basic products such as salicylic acid. Salicylic acid cannot be consumed by itself due to the fact that it is bitter and irritates the stomach causing side effects such as nausea and internal bleeding within the stomach. This is due to the fact that salicylic acid exists in protonated form in the stomach; therefore, the pH of the salicylic acid is low, thus affecting the lining of the stomach. Therefore, to stabilise salicylic acid, it is synthesized into acetylsalicylic acid also known as aspirin. Acetylsalicylic acid is not pronated in the stomach and thus, the pH of acetylsalicylic acid is not as low compared to salicylic acid, thus it does not affect the lining of the stomach as much compared to salicylic acid.
Albuterol also known as Salbutamol is a common medication used to treat asthma and similar respiratory ailments.[1] Albuterol is a bronchodilator and works to open the airways of the lungs. Albuterol can be taken intravenously or orally. The preferred method of this substance is orally, which in itself have various ways of being administered. One way is by inhalation, either from a vapor mist in the form of an inhaler and a nebulizer or, as a powder like Advair. In addition to inhalation, albuterol can be ingested as syrup or a tablet. Because of it varying forms Albuterol is can easily meet the need of the patient, making it a popular medication to treat asthma, emphazma, bronchitis and other airway constricting disorders.
The good thing about asthma is that there are a lot of medications available to help treat asthma sufferers with acute onset of symptoms as well as help with the long term prognosis of patients. Asthma medications are classified into two groups, Controller and quick-relief. Controller medications are designed to help prevent asthma attacks. Their purpose is to try and reduce the chronic inflammation thus making the body less likely to react to triggers. Some of these include long-acting beta-agonists, Leukotriene modifiers, Mast cell stabilizers, Theophylline, and immunomodulators. Long-acting beta agonists are bronchodilators that assist in opening up your airways. These are normally aerolized medications. The bronchodilator causes the muscles
Beta-2 agonist builds an athlete’s muscles while decreasing their body fat, here are some examples of Beta-2 agonist clenbuterol, terbutaline, salbutamol, fenoterol, and bambuterol. Some of the side effects of using Beta-2 agonist is headaches, dizziness, nausea, and muscle cramps(Drug addiction in athletes).
She was prescribed Salbutamol as inflammatory mediators in asthma cause airway smooth muscles to contract, reducing the diameter of airways throughout the lung. Albuterol is a beta-2 agonist that acts by relaxing smooth muscle. Side effects include a fine tremor in the hands and nervousness are the most common side effects of salbutamol. It may also causes palpitation, tachycardia, chest discomfort, headache, muscle cramps, hypokalemia, difficulty in micturition and paradoxical bronchospasm ("Salbutamol - mechanism of action, dosage, usage, side effects", 2017).
Abstract: theophylline has been used since ages in the treatment of asthma and remains the most widely prescribed anti-asthma drug worldwide, although the progress of newer anti-asthma medications, especially inhaled steroids, has resulted in declining use of theophylline in modern countries.
Partial agonist is a drug having same affinity for receptor as an agonist but less intrinsic activity than full agonist is called “PARTIAL AGONIST”. A partial agonist in presence of full agonist acts as antagonist, as it occupies the receptor and does not allow the full agonist to bind with receptor. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, and norclozapine. Examples of ligands
Ipratropium, Tiotropium bromide are anticholinergic agents widely used as second-line bronchodilator (after β2-agonists). The anticholinergic agents are effective for patients with severe airway obstruction and acute asthma exacerbations leads to cholinergic activation through viral infection, allergen exposure and air pollution. The combination of anticholinergic agent with SABA is the best treatment option for the of β-blocker induced asthma.
Atenolol is a beta-adrenergic blocking agent. It is a drug of choice for hypertension. The exact mechanism by which beta blockers reduce blood pressure is not known. All the therapeutic effects of the beta adrenergic antagonists result from blockade of beta 1 receptors in the heart. Recent studies show that with long term use beta blockers reduce peripheral vascular resistance, which could account for much of their antihypertensive effects
Cholinergic agonists are drugs that mimic or potentiate the action of acetylcholine, acetylcholine released at all parasympathetic post ganglionic endings, postganglionic sympathetic nerve ending to sweet gland and some blood vessels, all autonomic ganglia, adrenal medulla, skeletal muscles and CNS.
GPCRs are essential in numerous processes through the body (i.e. immunological function and normal cell growth) 1. Therefore, pharmaceutical drugs are known to target these G-protein-coupled receptors and this is expected to increase with our knowledge of GPCRs. Cimetidine is one GPCR drug that blocks the action of Beta-adrenergic receptors (βARs) and H2 histamine