The Medicinal Value of Omeprazole - Coursework Example

OMEPRAZOLE Background and Introduction Through the functioning of the immune system, the human body and for that matter the bodies of most living organisms, both animate and inanimate alike are empowered to resist the activities of pathogens and other germs, which bring about diseases (Äbelö et al, 2000). This means that on its own, the body should be able to either prevent diseases or fight against diseases to ensure constant healing. However, this functionality of the human body is limited to a certain extent as the immune system has not always achieved disease prevention and disease defenses (Andersson et al, 2000). It is against this background that it is necessary that third party disease fighting defenses be introduced. Through chemistry and medicine, the commonest form of third party or external disease fighting defense that has been given to the human body has been by the use of drugs or what is commonly known as medicine. Depending on the disease that a person is battling, different drugs are introduced. One typical drug that has been very keen in body disease defenses is Omeprazole, having the been useful in the treatment of a host of diseases including dyspepsia, peptic ulcer disease (PUD), Zollinger-Ellison syndrome, gastroesophageal reflux disease among others (Hassan-Alin et al, 2001). With a market name of Losec, Omeprazole comes in several forms including tablets and capsules. In this essay, a very detailed chemistry analysis is made of the drug with an aim of trying to understand the medicinal value of the drug, background to the diseases that the drug treats, functionality of the drug, as well as an evaluation of how the drug performs its chemical roles in the human body. Disease Omeprazole is used to treat Gastro-oesophageal reflux disease Omeprazole has been found to be suitable in the treatment of gastro-oesophageal reflux disease, otherwise known as GORD or GERD (Lagerström and Persson, 1984). Gastro-oesophageal reflux is more of a medical condition, which involves the abnormal relaxation of the lower part of the oesophageal sphincter in such as way that easily allows the back flow or reflux of the stomach’s acidic content into the gullet (Andersson, 1991). It will be noted that the stomach’s acidic content has its special role that it plays in the stomach and has special compartments within the stomach specially designed to contain it (Hassan-Alin et l, 2000). For this reason, if the acidic content flows into undesignated places like the gullet, it causes uncomfortable reactions to patients involved. In most cases, it is the muscular ring found beneath the oesophagus that gets malfunctioning, resulting in the abnormal relaxation. Smoking and drinking, as well as heavy eating are all associated with the disease (Cederberg, Heggelund and Lundborg, 1991) and it comes with symptoms such as burning sensation in upper abdomen, sour taste of acid reflux in the mouth, excess belching and difficulty in breathing for some patients (Edvardsson, Heggelund and Lundborg, 1990). Fig. 1: A Person suffering from heartburns Source: Henderson, 2012 Peptic ulcers Peptic ulcer is a bacterial disease that involves damages to areas of the mucosa, commonly referred to as the inner lining of the stomach (Andersson et al, 1993). It would be noted that ulcers are generally wounds or open damages that affects various parts of the human body. Once such ulcers occur in the upper part of the intestine, also known as the duodenum or the mucosa of the stomach, peptic ulcer is said to have resulted. Peptic ulcers are commonly associated with the Helicobacter pylori, which causes the ulcer in the identified spots of the stomach. As far as peptic ulcers are concerned, it is important that people know their state of risk to the disease so that they can moderate most of their intake contents including smoke, alcohol, some food and some medicine. This is because these intake contents have the potential of worsening risk of contracting the disease (Miners, Veronese and Birkett, 1994). Hitherto, it is advised that people who often feel pains in the upper part of their abdomen as depicted in the picture see their doctor immediately. Fig 2. A person with upper abdominal pain Source: Macnair, 2012 Dyspepsia Dyspepsia is commonly known as indigestion and constitutes a very unpalatable health condition with several consequences and complication in some cases (Junghard et al, 2000). People who suffer dyspepsia are likely to experience key characteristics such as chronic upper abdominal pain. Such pains may worsen right after eating or when the patient overeats (Lind et al, 1993). Upper abdominal fullness is also another characteristic, which has to do with a person always having a feeling that the abdomen is filled with food content. Once contracted, a person is very much likely to experience heartburns as there is constant gastrointestinal acidic activity that is pushed up the heart area. Nausea is also common and it also caused by the wrongful activity of gastrointestinal acidic content. In dyspepsia, the likelihood that a person may be having the condition as a result of other diseases such as peptic ulcer is higher and so medications are advised to be undertaken only under strict professional supervision (Lind et al, 2000) How drug is involved in disease It has been indicated earlier that most forms of Omeprazole exists on the market with the name Losec and comes in different forms including tablet, injection and capsules. This notwithstanding, there are others with no brand names and are just called Omeprazole (Hunt, 2009). But regardless of the form in which the drug comes, how the drug is involved with diseases and thus reacts to disease to bring about treatment or cure is the most important issue. The medicine is a proton pump inhibitor and so has the ability to slow down on the activities of most agents involved in symptomatic diseases that the drug threats. In the cases of the diseases named above like peptic ulcer, dyspepsia and Gastro-oesophageal reflux, it will be noted that stomach acid plays vital roles in giving patients the kinds of discomfort they experience. To this end, Omeprazole’s major function has been to suppress the production of stomach acid so that activities of these acids either getting up the oesophagus or damaging wounds in the duodenum become hindered. It would be noted that there are proton pumps on the cells in the lines of the stomach. Therefore as a proton pump inhibitor, Omeprazole inhibits the normal functioning of the proton pumps, which is the production of stomach acid as the acid is the major causative factor with diseases that the drug treats (Atthobari et al, 2006). Discovery, Design and development of drug Omeprazole was initially discovered with the presence of two optical isomers namely S-omeprazole (esomeprazole) and R-omeprazole. Structurally, these can be shown in a 1:1 ratio of the two optical isomers as given in figure 3. Fig. 3: (S)- and (R)-enantiomers of omeprazole With these compositions, Omeprazole can be seen as being a racemate with a presence of tricoordinted sulfinyl sulfur depicted in a pyramidal formation (Asselbergs et al, 2006). The two compositions existing in equal amounts as (S)- and (R)- enantiomers can actuallt both be converted into achiral products, creating room for the chemical bases to react with other cysteine groups namely H+/K+ ATPase (Bos et al, 2005). With to the reaction, there will then be an inhibition of the parietal cell from forming gastric acid to hamper the functionality of the gastrointestinal organs. With time, the design and development of the drug has changed significantly with a parent company named AstraZeneca coming in with the development of esomeprazole after the original product lost its patent rights and received much competition from the market. The difference that was recorded with the esomeprazole that was produced was that it presented euromer, which is the (S)-enantiomer in its pure form unlike omeprazole that presented a racemate (Monster et al, 2004). With a chiral shift in vivo, omeprazole is able to double its concentration of active ingredients as a result of activity by CYP2c19 isozyme, meaning that efficacy also experiences a level of increased efficacy especially for people with poor metabolism. Efficacy of drug Omeprazole has been found to be highly effective in not just the three diseases mentioned above as peptic ulcers, dyspepsia and Gastro-oesophageal reflux but also highly effective in other disease and disease symptoms that involves the activities of stomach acids (Boersma et al, 2006). Examples of these are various forms of side effects of non-steroidal anti-inflammatory drugs. For total efficacy however, one must stick to dosage prescriptions pertaining to specific condition being used to treat. Much of the efficacy of the drug also comes with the nature or form by which the drug is taken. Generally, because Omeprazole is broken down by an internal mechanism by stomach acid, Losec are given special coating as protection to allow the drug to pass through the stomach successfully into the small intestine. Should a patient chew or crush the drug, the efficacy of the drug will be rendered ineffective as it will be broken down in the stomach. In cases of difficulty in chewing, it is recommended that 10ml of the drug be dispersed into a non-carbonated water and mixed with fruit juice for immediate consumption. This will still keep the efficacy of the drug but once milk or carbonated water is used, efficacy becomes hampered (Miners, Veronese and Birkett, 1994). Criticisms of drug The commonest form of criticism that exists against the use of Omeprazole is the number of side effects that the disease comes with. This is because there are numerous possible side effects with the disease including headaches, diarrhea, constipation, nausea, vomiting, wind, dizziness, malaise, increase liver enzymes, among others (Lind et al, 2000). Though it is clear that almost all drugs come with side effects, side effects of Omeprazole are particularly mentioned as in some cases, the percentage of possible occurrence or experience with the side effects is said to be on the larger side. For example with basic side effects like vomiting, headaches, nausea, constipation and flatulence, the percentage is given as between 1% and 10% (1 in 100 and 1 in 10), which is deemed by many medical experts to be on the higher side (Hassan-Alin et l, 2000). Another criticism levels against the disease is the incompatibility that is commonly existed with other drugs when in use. For example patients are advised to make their doctors aware if they are taking any of citalopram, digoxin, escitalopram, methotrexate, tacrolimus, benzodiazepines, phenytoin and anti-HIV medicines as combination is not safe with these drugs. Future variations Going into the future, much of the weaknesses associated with omeprezole that has become basis for criticism are expected to be addressed. For instance it is expected that there will be room for more cohesive interaction with existing drugs. This is because most patients with medicinal problems that omeprezole caters for also tend to have other diseases that require that they use other medications (Miners, Veronese and Birkett, 1994). Should it therefore not be possible that there will be the combination of the drug with other chemicals, it would mean that such patients cannot benefit from the drug. Even more, it is expected that there will be an improvement in the method used in the preparation of (s)-omeprazole from omeprazole racemate where there will be the use of optical resolution agents. With such optimal resolution agent, it is expected that there will be the maximization of therapeutic effects of (s)-omeprazole (Lind et al, 2000). This may be achieved when right-handed isomer (s)-omeprazole are eliminated when optically preparing the solution so that left-handed isomer (s)-omeprazoles are used alone. Summary and Conclusion Through this essay, the medicinal value of Omeprazole, otherwise referred to as Losec has been discovered. This was done by giving a thorough chemistry of the medicine by looking at the disease it treats, the target of the disease and how the drug is involved in treatment as well as basic ideas of how the drug was discovered, designed and developed. What is more, a vivid evaluation covering not just the strengths but the weaknesses for future variations have also been discussed. In all, it can be concluded that Omeprazole was discovered at a timely moment when the world was battling with most diseases, most of which proved very difficult for the natural defenses of the human body in the form of the immune system to battle. It is not surprising therefore that for diseases like cancer, there were total blackout with them as far as treatments were concerned. Through constant development of the drug from the very first moment it was used for any chemical purposes, it has proved to be one of the most useful drugs that makes the future of medicine even more promising. With this said, it would also be mentioned that constant research on the drug ought to continue if the very best of the drug needs to recorded. As much as possible, there should be further studies on ways of reducing the side effects associated with the drugs as well continuing to find other potent drugs that Omeprazole could be combined with to make cure more effective. REFERENCE LIST Äbelö A, Andersson TB, Antonsson M, Naudot AK, Skånberg I, Weidolf L 2000. Stereoselective metabolism of omeprazole by human cytochrome P450 enzymes. Drug Metab Dispos 28:96–972 Andersson T 1991 Pharmacokinetics of omeprazole in man; with special reference to single and repeated administration, drug interactions and polymorphic metabolism. 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The effect of hypertension and hypercholesterolemia screening with subsequent intervention letter on the use of blood pressure and lipid lowering drugs. Br J Clin Pharmacol. 2004 Mar;573:328-36. Read More