Bio 1301 assignment 3
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University of the People**We aren't endorsed by this school
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BIO 1301
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Biology
Date
Dec 18, 2024
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5
Uploaded by EarlIbex1928
BIO 1301WRITTEN ASSIGNMENT UNIT 3UNIVERSITY OF THE PEOPLEDECEMBER, 2024
IntroductionOmeprazole belongs to the class of drugs known as proton pump inhibitors (PPIs). Other drugs in this group include esomeprazole, rabeprazole, and lansoprazole. PPIs are widely used to manage conditions associated with excessive stomach acid production, such as peptic ulcer disease and gastroesophageal reflux disease (GERD). Omeprazole reduces hydrochloric acid secretion in the stomach by targeting the enzyme H+/K+ ATPase, a crucial component in the final step of gastric acid production (Lindgren et al., 1993).Chemical Composition of OmeprazoleImage 1: Chemical Structure Depiction of omeprazole (Pubchem, n.d).Omeprazole is a synthetic drug with the chemical formula CHNOS. Its International Union₁₇₁₉₃₃of Pure and Applied Chemistry (IUPAC) name is 6-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole. This structure is integral to its function.
The benzimidazole moiety facilitates the binding of omeprazole to the H+/K+ ATPase enzyme, which is pivotal to its inhibitory effect.Mechanism of ActionOmeprazole’s mode of action centers on its interaction with the H+/K+ ATPase enzyme, commonly referred to as the proton pump. This enzyme, located in the gastric parietal cells, is essential for secreting hydrochloric acid into the stomach. The enzyme achieves this by exchanging potassium ions for hydrogen ions, a process that actively forms hydrochloric acid. By inhibiting this enzyme, omeprazole effectively halts acid production (Lindgren et al., 1993).Omeprazole is a prodrug, meaning it requires activation within the body to exert its effect. Once ingested, omeprazole is exposed to the acidic environment of the stomach, where it undergoes protonation to form its active sulfonamide form. This active metabolite binds irreversibly to the cysteine residues of the H+/K+ ATPase enzyme, thereby inhibiting its activity. The inhibition is permanent until new enzymes are synthesized by the body. This mechanism reveals omeprazole’s therapeutic effectiveness in reducing gastric acid secretion for up to 12 hours, necessitating dosing at 20-40 mg in 12-hour intervals (Katz et al., 2014).Type of InhibitorOmeprazole functions as an allosteric inhibitor. Unlike competitive inhibitors that bind to the active site of an enzyme, omeprazole binds to an allosteric site on H+/K+ ATPase. This binding induces conformational changes in the enzyme, rendering it inactive. Consequently, the enzyme’s ability to catalyze the production of gastric acid is significantly diminished (Katz et al.,2014).
Adverse Effects of OmeprazoleWhile omeprazole is effective in treating gastric acid-related conditions, its use is associated withcertain adverse effects, particularly with long-term usage. One significant risk is an increased susceptibility to infections caused by pathogens such as Clostridium difficile. The reduction in stomach acid compromises the stomach’s natural defense mechanism against ingested microbes, leading to gastrointestinal disturbances like diarrhea (Yang et al., 2017).Another notable adverse effect is vitamin B12 deficiency. Vitamin B12 is best absorbed in an acidic environment, and prolonged use of omeprazole reduces stomach acidity, impairing B12 absorption. This deficiency can result in neuropathy, anemia, and cognitive disturbances (Kiljanski et al., 2017). These potential adverse effects highlight the importance of using omeprazole judiciously and under medical supervision.Broader Implications of Enzyme InhibitionThe mechanism of omeprazole exemplifies how drugs can modulate enzyme activity to achieve therapeutic goals. This principle extends to various other drugs. For instance, statins inhibit HMG-CoA reductase to reduce cholesterol synthesis, and acetylcholinesterase inhibitors are usedin Alzheimer’s disease to enhance acetylcholine levels in the brain. These examples reveals the pivotal role of enzyme inhibition in modern pharmacology.ConclusionDrugs achieve their therapeutic effects by targeting specific biological pathways, often through the inhibition or stimulation of enzymes. Omeprazole serves as a prime example of this
mechanism, effectively reducing gastric acid production by irreversibly inhibiting the H+/K+ ATPase enzyme. While the drug is highly effective in managing conditions such as GERD and peptic ulcers, it carries risks, particularly with long-term use. Understanding the mechanisms by which drugs like omeprazole work not only enhances their safe and effective use but also provides insights into the broader landscape of enzyme-targeted therapies.ReferencesKatz, P. O., Gerson, L. B., & Vela, M. F. (2014). Guidelines for the diagnosis and management of gastroesophageal reflux disease. The American Journal of Gastroenterology, 109(1), 40-48.Kiljanski, J., Kaczmarek, J., & Laskus, T. (2017). The impact of proton pump inhibitors on vitamin B12 absorption. Nutrients, 9(9), 990.Lindgren, J. E., Röhss, K., & Rydén, J. (1993). Omeprazole: A specific inhibitor of gastric acid secretion. Gastroenterology, 105(1), 197-205.Pubchem (n.d). Chemical Structure Depiction of Omeprazole. Retrieved from https://pubchem.ncbi.nlm.nih.gov/compound/Omeprazole#section=StructuresYang, Y. X., Lewis, J. D., Epstein, A. J., & Metz, D. C. (2017). Long-term proton pump inhibitor therapy and risk of gastric cancer. Gastroenterology, 153(5), 1210-1215.