Pharmaceutical Evaluation Report: The drug is Singulair - Literature review Example

? PHARMACEUTICAL EVALUATION REPORT Introduction The drug singulair is a drug that is an inhibitor of leukotriene. Leukotrienes arechemicals that the human body releases. These chemicals are released when people breathe in and out pollens which are considered to be allergens. These chemicals usually have negative side effects on individuals (B, 2011). They cause swellings on the lungs and muscles along the airways are usually tight. These can result in symptoms that resemble asthma. The drug is usually used to prevent attacks that are asthma-related in children who are as young as 12 months and adults. The drug is also used to relieve sneezing that is as a result of allergies and runny noses, on both and children. The drug should never be administered without the doctor’s advice. The drug is also used prevent bronchoconstriction in children during exercising. Bronchoconstriction results during exercising and the air passage ways narrow in the lungs. A. Invention of the drug Its chemical IUPAC Name is 2-[1-[[1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methyl-ethyl] The molecular formula for the drug is C35H36ClNO3S The diagram below shows its chemical structure The drug was discovered by scientists who wanted to understand the genetic makeup of human beings. Receptors were the background study of this drug and the main receptor for this drug was the cysLT1 receptor. This receptor was discovered in 1999 and the receptor was referred to as a gene. The discovery was as a result of human characterization of the cysteinyl leukotriene receptor. This was also referred to as CysL T 1 receptor. It is well understood that leukotriene 4, leukotriene D4, and leukotriene C4 are some of the important mediators in of bronchial asthma in humans. Pharmacological studies have shown that the cysteinyl Leukotrienes usually activate a minimum of two receptors (Monson, 2008). The receptors are designated CysLT2 and CysLT1. Singulair is a selective antagonist against CysLT-1. Other selective antagonists include Accolate and Onon. These drugs are believed to be quite important CysLT 1 antagonists and its receptors. Pharmacological and molecular characterization was reported for the cloned CysL T1 receptor. It was detected that CysL T1-receptor messenger RNA peripheral leukocytes, lung and spleen. It is believed that the expression of the CysL T1-receptor mRNA was only confined to tissue macrophages and the smooth muscle cells. It was finally mapped out that the CysL T1-receptor gene was linked to the X chromosome. Biological mode of action of the drug Singulair The formulation of the drug singulair is in the tablet form. The formulation is usually a 10mg with an active ingredient that is known as montelukast (Nevoigt, 2009). Montelukast is type of medication that is known by many pharmacologists as a leukotriene receptor antagonist. The drug works by blocking or simply inhibiting leukotrienes from performing their functions. Leukotrienes are chemicals that are usually released during inflammatory and allergic reactions by the human body (Dubrin, 2011). People with asthma usually release leukotrienes which result in inflammation and high levels of mucous production within the airways. The other effects that are caused by leukotrienes include contraction of the muscle lining that result in the contraction of the airways. This contraction makes it quite difficult for the air to get into the lungs and out. The drug montelukast works by inhibiting the receptors that are found in the lungs. By inhibiting the receptors, action by leukotrienes are inhibited and this prevents the production of excess mucous in the lungs. Narrowing and inflammation of the airways is also prevented hence an individual cannot suffer from an asthma attack. The drug montelukast is normally used by people or recommended for people who never get treated by using inhaled corticosteroids. The drug is usually used in addition to other medicines such as salbutamol. Leukotrienes are also produced by people who suffer from seasonal fevers such as hay fever. The trigger for these kinds of allergies is allergens such as pollen and dust. The medicine is said to quite effective as it inhibits an individual from having a runny nose or even a blocked nose (Ortiz, 2011). B. Engineering solutions for manufacturing One of the largest manufacturing companies in the world is Merck & Co.., Inc. The company is also known as Merck and Sharp & Dohme or MSD outside Canada and the United States. The company is one of the largest pharmaceutical companies in the world. Drug manufacturing industries have produced variety health-related and medicinal products. The health products are some of the most imaginative products that even the most imaginative apothecaries can master. Thousands of drugs are available today and they are used for different purposes. Some of the reasons why drugs are manufactures include; therapeutic, diagnostic and preventive reasons. The drug in this case is singulair is a drug that is used to treat asthma-related illnesses such as blockage of the airways and runny noses. The drug in this case cannot be considered to be diagnostic but a therapeutic drug (Wolpert, 1979). Drugs have saved many people from illnesses and death. New and innovative drugs have been developed by many companies so that are able to deal with the emergent challenges in the modern day world. Vaccines have also come in handy so that they are able to complement the use of drugs as preventive measures against deadly diseases. Examples of vaccines that have drastically reduced deadly diseases and illnesses include; polio vaccine, measles and whooping cough. It said that the drug industry employs around 1,700 people in at least each and every country. These include industries or establishments that that make the finished products or the pharmaceutical preparations. The finished products include; botanicals and bulk chemicals that are used to make finished drugs, and diagnostic tools or kits that. The kits include diabetic and pregnancy kits. During the manufacturing process of the drug singulair, there are key steps or inputs that are supposed to be adhered to. These processes are necessary so that the laid down procedures are adhered to and maximum production is realized by the manufacturing company. The engineering solutions for the manufacturing of the drug singulair include; the efficiency process, environmental impact, cost, specification and consistency. An in depth analysis of this solutions will be analyzed. 1. Efficiency process Majority of the manufacturing companies have put place measures to ensure that they use the most efficient processes to achieve a maximum output of their products. Efficiency mechanisms have been put in place to ensure that this particular goal is achieved. A good example is when MSD, the largest drug company that manufactures the drug singulair, invest heavily on research so as to come up with necessary therapeutic molecules. Due to the emergence of new stains of pathogens, it is also imperative that the drug companies come up with the necessary methods to combat the new forms of diseases (Whitney, 1993). Scientific research has greatly revolutionized pharmaceutical industries (Ortiz, 2011). This has made them quite efficient in terms of productivity and investments. The research departments begin by finding out the new chemical compounds that have the potential to inhibit or alleviate the new diseases. To improve efficiency during the discovery process, scientists have devised new and innovative methods to assist them in this process. By using computer simulators and combinational chemistry, this has greatly hastened the discovery process and its efficiency. In this case the drug singulair can be manufactured efficiently through simulation and combinational chemistry. To improve efficiency in the discovery and manufacturing process, the drug companies have employed highly qualified personnel to assist in the process. The personnel are highly skilled and specialized in different areas of the drug discovery process. By ensuring that skilled people are in different places, the final products are usually of high quality. A unit may be specifically involved in analyzing a certain population while another may be studying populations that are resistant to the drug. 2. Impact on the environment The environment plays a key role in the manufacturing process as it ensures that the company is able to sustain its growth and expansion strategies. During the discovery process and the manufacturing process of the drug singulair, there are a lot of raw materials that are used in the process. To improve the manufacturing process, raw materials should be utilized in an efficient manner and by products disposed in a way that does not interfere with the environment. The reason why the environment plays a key role in the success of a manufacturing plant is that the authorities can decide to deregister the company due to pollution (Wastaff, 2009). During the laboratory screening during the drug discovery process, clinical investigations are usually carried out and the environment plays a key role in the discovery process. A clean and healthy environment usually assures researchers of achieving favourable results. This improves efficiency and reliability of the results. An environment that is polluted attracts unfavorable results and authorizing agencies such as the Food and Drug Administration can never approve of the drug. The environmental impact of releasing refuse to the environment by the manufacturing plants can be quite detrimental to the health of individuals within and without the manufacturing plant. The impact on the environment can also result to new and emergent forms of diseases in case the by products are handled carelessly. Most manufacturing plants have put in place measures that reduce the environmental impact. The plants have also greatly invested in safety measures like purchasing of equipment that can be used to culture bacteria hence preventing their release into the external environment. 3. Cost of manufacturing Cost of production plays a key role in determining how much a manufacturing company will make in terms of profits. In most production setups, drug manufacturers have come up with high levels of automation so as to be quite efficient and save money in terms of loses. Micronizing and milling machines have been utilized in handy during the manufacturing of the drug singulair. These machines are said to be quite expensive therefore it is imperative that companies do their level best to maintain them. The mentioned machines crush drug materials into very fine particles. The efficiency with which these machines work especially in the production commendable considering how expensive they are. The machines are used to decrease bulk of the chemicals in the drug to the prerequisite size. These sizes are usually determined by the Food and Drug Administration. Their guidelines assist the manufacturing companies in producing the required items. During the processing stage, cost of production can come into play when the process that is carried out ends up producing an unfinished end product (Ortiz, 2011). The completed drug products are usually processed and combined during the manufacturing process. By using cost effective machines, the cost of producing these drugs can be greatly reduced. It is advisable that manufacturing plants should purchase machines that will never incur the plants a lot of maintenance costs. Machines such as the mixer can be used to mix many different ingredients so that the formulation will be well accounted for. The mixed ingredients could be capsulated mechanically depending on the customers’ requirements. Most people prefer to capsules formulation over the tablet formulation. The reason is that the capsules usually prevent the sick patient tasting the bitter ingredients that are present in the drug. Tablets are also an option to produce drugs. Syrups or even tablets are usually used to ensure that the customer’s needs are taken into account. A multinational company such as MSD usually invests in purchasing of highly efficient machines. The essence of this is to ensure that maximum profits are realized after the drugs have been marketed efficiently. As example of a machine that is used in the manufacturing of the drug singulair is one that automatically stamps, seals and fills the singulair capsules. There other types of machines that a plant can install so that they can be able produce other types of formulations such as the syrups. These are quite cost effective and they work by filling bottles with the syrup. Other machines fill the bottles with liquids, tablets, and capsules. They then assist in the sealing, packaging and labeling of the bottles. This greatly contributes to attractive packaging and reduces the cost of doing all these processes manually that can result in a lot of errors. 4. Specifications Manufacturing plants ensure that the best practices are usually adhered to. This ensures that the products are of high quality and the necessary standards. The FDA has ensured that the manufacturing companies adhere to the laid down procedures. Most manufacturing companies have got quality assurance departments within the plants. These departments work to ensure that the manufacturing process is followed to the latter. In the manufacture of the drug singulair, quality assurance is extremely vital in the manufacturing industry. Many qualified workers are usually assigned full time in these departments so that the drugs are constantly under scrutiny. Most of these employees devote most of their time to ensure that the manufacturing process reaches to its perfection. 5. Consistency Most manufacturing companies are quite successful financially simply because they are extremely consistent in their production. Consistency is quite essential especially when a company is trying to progress financially. The reason is that manufacturing and distributing companies will maintain a close relationship with the manufacturing companies. This relationship is quite necessary especially in the health sector. Consistency is necessary especially when the manufacturing plants want to meet the market requirements that are constantly changing every now and then. In this case, the drug singulair is always being produced constantly because people are usually being exposed to different types of allergens every now and then (Wolpert, 1979). C. Pharmacology of singulair Pharmacology is the study of drugs and their effects that they have on the body. Drugs are chemical compounds that have both primary and secondary effects on the body. The primary effects are the intended or therapeutic effects that the drugs are expected to have on the body. They usually have their target areas that they are intended to act on. The target areas could either be the pathogens that cause diseases one way or another or they could be receptor cells that are many drug targets. The drugs that target receptors, usually work by either being agonists or being antagonists. In pharmacology drug study can be classified either as pharmacokinetics and pharmacodynamics. The study of what the drug does to the body do to the drug is pharmacodynamics while the study of what the body does to the drug is known as pharmacokinetics. Under pharmacokinetics, there are four basic principles that are usually adhered to and they are; drug administration, drug distribution, drug metabolism and finally drug excretion (Vink, 2011). a) Mechanism of Action of the drug Singulair is a drug that is usually designed to treat asthma. The drug works fast enough so that it inhibits the action of asthma when somebody is under attack. The formulation of the drug singulair is in the tablet form. The formulation is normally in tablet form and it is usually in a 10mg tablet. The key active ingredient is known as montelukast. Montelukast is type of medication that is known by many pharmacologists as a leukotriene receptor antagonist. The drug works by blocking or simply inhibiting leukotriene from performing their functions. Leukotrienes are chemicals that are usually released during inflammatory and allergic reactions by the human body. By inhibiting the leukotriene from binding in certain receptors, it prevents individuals from suffering from asthmatic attacks. b) Bioavailability The drug singulair is normally in tablet form and it can also be in chewable form. It is rapidly absorbed orally immediately after administration. A tablet of singulair that is chewable contains 4.2 and 5.2mg of the active ingredient of montelukast. The inactive ingredients that are found in the chewable form of the drug include; cherry flavor, aspartame, ferric oxide, mannitol, cellulose, hydroxyl propyl cellulose and microcrystalline cellulose. Bioavailability refers to the maximum concentration that the drug will reach in the blood at a particular time (Nevoigt E. , 2008). Bioavailability plays a key role in determining the route of administration of may drugs. By intravenous route of administration, many drugs achieve their bioavailability very fast. An oral route of administration slows down drug absorption therefore this greatly affects bioavailability of the drug. There are factors that affect bioavailability of drugs and a perfect example is the first pass effect that many drugs undergo (Barton, 2009). Clinical studies that were carried out showed that, a single tablet of singulair that has 10mg could be taken two hours before an individual decides to take exercises. Some patients were safe against asthmatic attacks after a period of 8.5 and 24 hours immediately after the drug administration. From this analysis and assessment, we can say that the bioavailability of the drug is around four hours after the drug has been administered. The actual mean oral bioavailability of the drug singulair is said to be 64%. The maximum concentration of the drug is usually influenced by a meal that is standard in nature in the morning. c) Metabolism Metabolism refers to the breakdown of the active components of the drug into components that can be easily eliminated through excretion. The drugs are normally converted into highly polar compounds that can be able to bind with water for their rapid elimination. The liver plays a key role during this process because there are certain enzymes that are found within the liver that convert the hydrophobic drug substances into hydrophilic compounds. Montelukast which is the main active ingredient in the drug is usually extensively metabolized by the liver enzymes. Studies that have been carried out have indicated that metabolites of montelukast that are within the plasma are usually in a steady state that is extremely undetectable. This state has been reported in both adults and children. Invitro studies that have been carried out about the drug indicate that liver enzymes such as cytochrome P450 2C9 and 3A4 are involved in the metabolism process. Inhibitors to this enzymes have been discovered and the include fluconazole and ketoconazole. The clearance of the drug montelukast usually averages a minimum of 45mL/min. This is usually possible in healthy adults. Studies have indicated that fecal collections after the drug has been administered in an individual are believed to be around 86% of the fecal content. This is a great indicator that the drug is usually eliminated via the bile. In other studies, the plasma half -life of the drug has also been determined severally. The half-life of the drug is sad to be from 2.8 to 5.5 hours. This applies to healthy adults. The dosing of the drug is usually once in a day. d) Off target effects of the drug Off target effects are the secondary effects that the drugs were targeted to carry out. Off target effects are also referred to as side effects. Side effects can be quite dangerous or lethal. One should get emergency medical assistance when they experience any of the signs of an allergic nature to the drug Singulair. The side effects of the drug singulair include; difficulty breathing swelling of the throat, tongue or even the throat, face and lips. An individual may also suffer from hives (Wastaff, 2009). A patient should be in a position to call their doctors or even clinicians in case of any problems. The following are some of the symptoms that are experienced by people when the drug has been administered. skin rash, severe tingling, bruising, muscle weakness, pain and numbness, Worsening asthma symptoms. spots under the patients skin tremors or shaking mood or behavior changes, anxiety, depression, or thoughts about suicide or hurting yourself easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint swelling, severe sinus pain, and irritation Less serious Singulair side effects may include; headache that are most common in many people, mild rash that is common in children, stomach pain, heartburn, upset stomach, nausea, diarrhea, tooth pain, tired feeling, fever, stuffy nose, sore throat, cough, hoarseness. Most drug companies are working extremely hard to ensure that most of these side effects are reduced significantly. The reduction in side effects of drugs has been the basis or the selling point of most marketing and pharmaceutical companies. D) Business/market analysis of the drug Business analysis tries to analyze the market that exists for any particular drug. The Global Data projected that the worldwide market for asthma will be valued at $12.8 billion in the year 2009. The value is said to be extremely useful especially to drug marketers and distributors in many parts of the world. These indicators of the market share that exists in a particular country help in the identity of the market segmentation (Becker, 2007). To assist with the identification how the market is segmented, the marketers should always know the competitor molecules that exist in the market. This is quite essential as it helps them know the strengths, weaknesses and opportunities that they can explore in order to realize maximum profits. This helps the marketers to identify the value of the expected margins of profits. Profits could be expected to decline or sharply rise depending on the market profiling. Manufacturing companies also play a play a key role in determining whether certain drugs will have the largest market shares of lose out completely. Most of the multinational companies enjoy the comfort of being the beneficiaries by virtue of their names and their ability to have their companies based internationally. Examples of multinational companies that have greatly benefited in the pharmaceutical industries include, GlaxoSmithKline, Pfizer and Novartis. Other drug manufactures within the pharmaceutical market are the MSD that manufactures the drug singulair. Other firms that are involved in the marketing of generic drugs seem to be really gaining in the market simply because many people are opting to purchase generic drugs simply because they are cheaper. This has led many multinationals partnering with most of these companies. Although the respiratory market has considerably expanded from the year 2003 to 2009, there has been considerable growth in the many major markets. It will be expected that there will be a slowdown from the years 2009 to 2014 in the financial markets. The decline is attributed to many market pressures that will exist in future. This is the reason why it is highly imperative that the pharmaceutical companies invest in research. This is quite necessary as this give the company an edge over the rest of their competitors in the market. 1) Patent strategy Patent strategies are quite necessary especially when marketers and distributors are authorized to market a particular brand of drug for certain manufactures. The essence of having market strategies is to ensure that there are no fake drugs out there in the market. Patents usually have expiry dates that are always renewable depending on the agreement that exists between different companies 2) Competitor analysis Competition is quite important in any economy so that the monopoly of any product is eliminated. Competition could at times be a nasty affair or it could be a fair affair between competing companies (Bajaj, 2005). In the pharmaceutical industry, competition usually lies in the competitor molecules that are in existence. Many companies will usually have the same products in the market but will have different competing molecules. Many drugs have different side effects. The lower the side effects that a drug has, the higher the chances of that particular drug gaining a large market share. This has been the major selling point of many drug companies. Other factors that enable a company to have a large market share is the king of formulation of the drug and the dosages. People prefer small dosages compared to larger ones because the chances of being mixed up are quite little in the process. In this case, singulair has got many competitors in the market. The competitors mainly come from the multinational companies. A god example of a competitor is GlaxoSmithKline. The asthmatic drug that the company produces is known as Beyond Advair. The other competitor company is known as Novartis is QVA 149. Growth of these companies is usually driven by the expansion strategies that have been put in place (Becker, 2007). On the sales perspective, there exist classes that assist sales departments of most companies in determining the futures of most of the companies. Among the strategies that the companies are involved include launching of new products in the market. During the launch of the new products, the presence of key opinion leader is extremely necessary as they help in sale of the products through their prescriptions. Differential product performance This refers to the difference that arises from the use of different products that exist in the market. During the drug discovery process, there is the last bit that is left for to doctors to study and analyze in case there are any reported cases of adverse drug interactions. These may arise due to combinational therapy that many people may not be aware of. It is important for patients to seek the advice of medical practitioners especially when they try to get treatments for diseases such as asthma. Different products have different performance levels. Singulair is a more potent than many asthmatic drugs in the market due to its mode of action. The drug is preferred to many other drugs that exist in the market due to its ability to treat asthma effectively. People who have got asthma usually release leukotrienes which result in inflammation and high levels of mucous production within the airways. The other effects that are caused by leukotrienes include contraction of the muscle lining that result in the contraction of the airways. This contraction makes it quite difficult for the air to get into the lungs and out. The drug montelukast works by inhibiting the receptors that are found in the lungs. By inhibiting the receptors, action by leukotrienes are inhibited and this prevents the production of excess mucous in the lungs. 3) Cost control The cost of the drug varies from one country to another. The reason is that market pressures greatly determine the pricing of the products in the market. We find that most companies are usually involved in placing prices that are highly competitive in the market and ones that are affordable. Singulair has a competitive price tag as it competes with other asthmatic drugs that are made of corticosteroids such as the inhalers (Becker, 2007). 4) End-user management This is quite an essential component in the marketing world. This is even more important for drug companies as they sell there products to many different people. It is important to ensure that the drugs are properly labeled and stored in an amicable place. 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