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Treatment of asthma research paper
Treatments for asthma essay
Treatment of asthma research paper
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A series of new 10-(alkylamino)-8-methyl-2,6-dihydroimidazo[1,2-c]pyrimido[5,4-e]pyrimidine-5(3H)-thiones (4a-g) were subjected to molecular property prediction (drug-likeness, lipophilicity and solubility parameters) using Osiris Property Explorer, ALOGPS 2.1, Molinspiration and ACD/Chemsketch 12.0 software programmes. The calculated drug-related properties of the designed molecules were similar to those found in most marketed drugs. Amongst the proposed analogues, four promising candidates were chosen (4a-d) for synthesis on the basis of Lipinski’s ‘Rule of Five’ and drug likeness scores. The significant biological activity of the test compounds in two in vitro modes (isolated guinea pig tracheal chain preparation, isolated guinea pig ileum) supports the promise and accuracy of the prediction. Among them, 4a was the most potent antihistaminic [IC50 value of 30.2 µM; Standard, chlorpheniramine maleate -IC50 = 14.1 µM].
Key words: Antihistaminic, asthma, bronchodilator, drug likeness, property, pyrimidine
Asthma is primarily a complex, chronic inflammatory disease of the airways, which affects more than 300 million people worldwide, making it a serious global health problem [1]. It is characterized by recurrent reverse obstruction of the airways, airway inflammation and bronchial hyper responsiveness to stimuli which are not in themselves noxious and which do not affect non-asthmatic subjects [2]. Bronchial asthma results from a complex interplay between genetic and environmental factors [3]. An asthmatic subject suffers from intermittent attacks of dyspnoea (difficulty in breathing), wheezing and cough. Epidemiological studies show that its occurrence has been on a rise in children and young adults since early 1970’s, with the greatest incidence in more industrialized and urbanized societies, worldwide[4,5]. Nearly 7-10% of the world population suffers from bronchial asthma and India alone has an estimated burden of more than 15 million patients [6].
Currently bronchodilators (anticholinergics, selective β2-adrenergic agonists, methylxanthines, antihistaminics) and antiinflammatory agents (inhaled steroids, leukotriene antagonists, mast cell stabilizers etc) are used in the treatment of asthma[7]. Despite the availability of a wide range of drugs, asthma control is poor globally and especially in developing countries due to the underutilization of these agents in view of their cost and adverse drug reaction (ADR) profiles[8-10]. Moreover, the relief offered by these drugs is not only symptomatic but short-lived. Poorly controlled asthma is associated with significant morbidity, mortality and consequent socio-economic issues[11]. Hence, there is a dire need to search for new, effective and safer remedies to treat bronchial asthma.
While reviewing the recent perspectives in the design of antiasthmatic agents, we observed that different angularly fused heterocyclic ring systems like imidazoquinolines, imidazonaphthyridines, thienopyrimidines, triazolothienopyrimidines, benzimidazolo -quinazolines, imidazoquinazolines, benzimidazolopyridopyrimidines, imidazothienopyrimidines and triazinoquinazolines are potentially useful compounds[12,13].
Discussion and Conclusions: Interpreting these results have concluded that relative reactivity of these three anilines in order of most reactive to least reactive go; Aniline > Anisole > Acetanilide. Aniline, has an NH2 , the most active substituent , and adds to any ortho/para position available on the ring. This data is confirmed with the product obtained, (2,4,6 tribromoaniline, mp of 108-110 C). As for anisole, it has a strongly activating group attached, OMe an alkoxy group, and it added in two of the three available spots, both ortho. The results conclude: (2,4-Dibromoanisol mp 55-58 C ). Acetanilide has a strong activating group attached, acylamino group, but this group is large and the ortho positions are somewhat hindered so the majority of the product obtained added at the para position, results conclude: (p-bromoacetanilide mp 160-165 C). Since all the substituents attached to the aromatic rings were activators the only products able to be obtained were ortho/para products.
Asthma is a chronic inflammatory disease of the airways. It is a reversible airway obstruction, occurring 8 to 10% of the population worldwide. According to a study in 2005, asthma affects over 15 million Americans, with more than 2 million annual emergency room visits. Asthma patients have a hyper-responsiveness in their airways and generally and increase in their airway smooth muscle cell mass. This hyperplasia is due to the normal response to the injury and repair to the airway caused by exacerbations. The main choice of therapy for asthma patients is β2- adrenergic agonists. Racemic albuterol has been the drug of choice for a short acting bronchodilator for a long time, but since the development of levalbuterol, there is the question of which drug is a better choice for therapy. Efficacy and cost of treatment must both be taken into consideration in each study of these therapies to determine which is best for the treatment of asthma.
Asthma is treated with two types of medicines: long-term control and quick-relief medicines. Long-term control medicines help reduce airway inflammation and prevent asthma symptoms. Quick-relief, or "rescue," medicines relieve asthma symptoms that may flare up.
The use of illegal substances in sports is a trendy topic in today’s society. In the last few years a copious amount of players have been under the spotlight of substance abuse, which led to a punishment for their actions. Andrew Sullivan wrote an article in the year 2004 called “In a Drugged-up Nation, the Steroid Sports Star is King”, in which he illustrates how these “pharmaceuticals” have revolutionized sports around the world but mostly in America. These drugs have had a large influence in the overall performance of the players, even if it the use of drugs is “often denied or simply overlooked”(Sullivan 1), it will lead to a lack of judgment in what is right and what is wrong.
Imagine a young child competing with his or her fellow classmates during recess and immediately losing the ability to breathe normally. He or she stops in the middle of the competition and falls to the ground while holding his or her chest trying to find air. When you are young, being able to keep up with your peers during recess and sporting events is very important, however, having asthma restricts this. Asthma has a significant impact on childhood development and the diagnosis of asthma for children 18 years and younger has dramatically increased over the years. Asthma is known as a “chronic inflammation of the small and large airways” with “evident bronchial hyper-responsiveness, airflow obstruction, and in some patients, sub-basement fibrosis and over-secretion of mucus” (Toole, 2013). The constant recreation of the lung walls can even occur in young children and “lead to permanent lung damages and reduced lung function” (Toole, 2013). While one of the factors is genetics, many of the following can be prevented or managed. Obesity, exposure to secondhand smoke, and hospitalization with pneumonia in the early years of life have all been suggested to increase children’s risk of developing asthma.
As we discussed above that pharmacokinetic and pharmacodynamics can be seen as two sides of the same coin in order to gain better understanding of their efficacy and safety profiles.” Generally it is possible to make fairly robust predictions of the pharmacokinetic profile in man using in vitro systems and preclinical pharmacokinetic studies. A previously published survey on the causes of failure in drug development indicated that inappropriate pharmacokinetics were a major cause such as; factors as low bioavailability due to high extraction or poor absorption characteristics, short elimination half-life leading to short duration of action and excessive variability due to genetic or environmental factors. This observation has led to an increased emphasis on pharmacokinetic input to the drug discovery process throughout the pharmaceutical industry. However, it is important to realise that this may only permit the rejection of compounds to b...
Some high schools require athletes to submit to random chemical testing for illegal drug use. On the other hand, other schools and coaches believe that random drug testing is stating that all athletes are guilty of wrongdoing instead of believing they are innocent. There can be advantages and disadvantages to both sides, although random chemical testing for illegal drug use is the smartest idea. Having random drug tests is used for precautions, influences some to not do drugs if they are considering it, and encourages students to be their best.
Most of you may not think of asthma as a killer disease, yet more that 5,000 Americans die of asthma each year. According to the Mayo Clinic web page, asthma also accounts for more that 400,000 hospital discharges annually. As the number of people with asthma increases, the more likely you are to come in contact with a person who has the disease. As far as I can remember, I have had asthma my whole life. My mother and one of my sisters also have asthma, so I have a first hand experience with it. This morning, I will discuss some interesting facts about asthma, I will specifically focus on what it is, warning signs, symptoms, causes, and the treatments that are used.
Becoming an ever more present topic of controversy in today’s world is drug testing in selection. With this dispute comes a multitude of ethical dilemmas. Some believe it is an infringement of rights while others believe it is a necessary requirement for workplace safety and organization protection. In the world of business it is important to push the organization for success while maintaining employee/employer safety and consumer satisfaction. One way to accomplish these requirements is to utilize drug testing in the selection process but it is a subject easier said than done.
The purpose of this paper is to describe the pathophysiology mechanisms of chronic asthma and acute asthma exacerbation, and explanation of arterial blood gas pattern during an asthma exacerbation. Also, explain how age might impact pathophysiology of asthma and asthma exacerbation. The diagnosis and treatment plan needed to relieve the presented signs and symptoms will be reviewed. Lastly, the construction of two mind maps for chronic asthma and asthma exacerbation including its epidemiology, pathophysiology, clinical presentation, diagnosis and treatment.
All these derivatives have the same pharmacodynamics and mechanism of action, but differ tremendously in their pharmacokinetics.
Asthma is a disease that currently has no cure and can only be controlled and managed through different treatment methods. If asthma is treated well it can prevent the flare up of symptoms such as coughing, diminish the dependence on quick relief medication, and help to minimize asthma attacks. One of the key factors to successful treatment of asthma is the creation of an asthma action plan with the help of a doctor that outlines medications and other tasks to help control the patient’s asthma ("How Is Asthma Treated and Controlled?"). The amount of treatment changes based on the severity of the asthma when it is first diagnosed and may be the dosage may be increased or decreased depending on how under control the patient’s asthma is. One of the main ways that asthma can be controlled is by becoming aware of the things that trigger attacks. For instance staying away from allergens such as pollen, animal fur, and air pollution can help minimize and manage the symptoms associated with asthma. Also if it is not possible to avoid the allergens that cause a patient’s asthma to flare up, they may need to see an allergist. These health professionals can help diagnosis what may need to be done in other forms of treatment such as allergy shots that can help decrease the severity of the asthma ("How Is Asthma Treated and Controlled?").
Clancy, J., & Blake, D. (2013). Pathophysiology and pharmacological management of asthma from nature-nurture perspective. Primary Health Care, 23 (7), 34-41
This article relates very well to clinical practice. The article provides evidence that patients who smoke have significant differences in terms of clinical and therapeutic effects compared to non-smokers. This is relevant because it is proving in the actual article that asthmatic patients who smoke have many more complications and a greater likelihood of asthma exacerbations. We would recommend the article in clinical practice because it has a specific purpose in dealing with exacerbations. Some limitations would include that this article did not have a very large sample size, so this can also be a future recommendation to improve it. A strength is that it was conducted in an actual Asthma Genome Research Center, carrying a greater prestige and validity. The research article by Kupczyk, et al., (2014) holds a level IV evidence, also known as a descriptive study. This study is relevant because it focuses on the smoking history of the participants. The clinical relativity is that health care providers can look at the history of the patients, and thus have a factual idea of the contributions to the frequent exacerbations. This study would be highly recommended to be used in clinical situations because a patient's history is a key indicator of their present status, therefore knowing their history of smoking may help with the treatment of exacerbations. Limitations of this study can include the small study size and
Enlightenment, Maturation, and a Shot of the Past (3 Themes from Lines Composed a Few Miles Above Tintern Abbey) This is an essay composed a few hours after Mcgee’s lecture on the theory of Platonics. This lecture left me feeling sentimental and as if I’m on a higher plane of thought. These feelings tied directly into the themes of Lines Composed a Few Miles Above Tintern Abbey, a poetic essay written by William Wordsworth. Wordsworth wrote this poem while at Tintern Abbey, five years after his first trip; the poem is considered to be the model for the romantic era.