Abstract
Omeprazole is available in the market under the brand name Prilosec and Losec. It is a medication that is used for the treatment of reducing acid levels in the body. It was discovered in the year 1979. It was later introduced in the marketed in the United States in the year 1989. The World Health Organization (WHO) has included it in the list of essential medications that are needed in a primary health system. It is available in generic medication. The paper will be discussing the omeprazole medicine. It will be covering the class that the drug belongs to and its purpose. It will also include the pharmacokinetics and pharmacodynamics of the omeprazole. The paper will also discuss the side effects of the medication covering the common, uncommon and severe impacts. It will also address benefits and risks that are associated with omeprazole.
Synopsis
In this paper, omeprazole has been explained to be in the class of proton pump inhibitors (PPIs). It is used by medical practitioners as an over-the-counter (OTC) or a prescription drug. It is widely used in managing disorders that are related to the level of acid in the body. Oral administration is commonly used and has been termed useful by patients. The PPIs have been widely applied in the treatment of a range of acid-peptic disorders. For instance, peptic ulcer and gastroesophageal reflux disease (GERD). Pharmacokinetics of omeprazole covered absorption, metabolism and excretion procedures. The absorption process of the medication starts in the small intestine. As a result, it is advisable for patients to use omeprazole in the morning when their stomachs are empty.
They should also take some time before eating to prevent digestion of the drug in the stomach. The metabolism process of omeprazole occurs in the liver. The excretion of about 80% of metabolites is through urine. The remaining amount is excreted in feces. Pharmacodynamics of the medication has covered antisecretory activities, enterochromaffin-like (ECL) cells effects, and serum gastrin effects. The medication has side effects that negatively affect the health of patients.
The levels of adverse reactions depend on a combination of therapies. Severe impacts of using medication include swelling of different body parts, for instance, eyes, tongue, feet and lips. Patients should seek medical guidance if they experience adverse effects after medication. There are common side effects like nausea and vomiting. Gaining of body weight is the primary uncommon negative impact of using omeprazole. Benefits of the drug are in its ability to inhibit the amount of acid in the body. Risks associated with the drug include dementia, kidney and heart diseases.
Omeprazole
Omeprazole was first introduced to the public in the United States in the year 1989 by Astra AB Company. It was marketed under the brand name Losec. In the year 1990, United States Food and Drug Administration (FDA) requested the change of brand name, and it has been modified to Prilosec. The alteration was meant to prevent users from confusing it with diuretic Lasix drug. However, the changes resulted in people mistaking omeprazole (Prilosec) for fluoxetine (Prozac) medicine that is used as an antidepressant. The drug can be used in the form of a liquid suspension or a capsule. Patients use it by swallowing in the mouth. According to Vaduganathan et al. (2016), it is available in the market as a brand-name Prilosec and can also be available as a generic drug that is not costly. Omeprazole is used in lowering the amount of acid in the body. It has side effects that are supposed to be reported to the doctor to avoid future health complications.
Class of the Drug and Its Purpose
Omeprazole is grouped among antisecretory compounds. It is grouped among the drugs that are found in the class of pump inhibitors (PPIs). It contains benzimidazoles substitutes that inhibit secretion of gastric acid. According to Moore, Derry, Simon, and Emery (2014), the drug functions through suppressing the H+/K+ ATPase enzyme system. The process takes place at the secretory part of the gastric parietal cell. The catalyst system inhibited is referred to as the acid proton pump, and it is found in the gastric mucosa. As a result, omeprazole has been described as the acid pump inhibitor. It stops the final step of producing acid in the body. Rostom, Moayyedi and Hunt (2009) argue that the effect of stopping production of acid is related to the dose used. The medication leads to suppression of basal and stimulated acid secretion regardless of the stimulus. Scholars support that omeprazole rapidly disappears from plasma but, it can be detected in the gastric mucosa for a minimum period of one day (Wang et al., 2016).
Omeprazole is an over-the-counter (OTC) and a prescription drug. Recommended medicine by the doctor can be accessed as a delayed-release oral capsule or suspension. Peura et al. (2009) argue that, as a delayed drug, it is meant to slow the release of the medication up to a time that it passes through the stomach. Slowing the process is essential because it protects omeprazole from being activated and be digested in the stomach. The drug can be used as a combination therapy in that patients may be required to take it with other prescribed or OTC medications. The purpose of omeprazole is used decrease the level of acid in the stomach. According to Liang et al. (2011), the medication is prescribed to the patients when treating gastric or gastroesophageal reflux disease (GERD).
It is used during the treatment of hypersecretory conditions that causes stimulation and production of the high amount of acid. It is also used to treat erosive esophagitis that causes inflammations in the esophagus. The medication can be utilized when providing treatment for infections in the stomach that are caused by bacteria that are found in the digestive system. Helicobacter pylori cause peptic ulcers and can be cured by the use of triple therapy combination of omeprazole and other drugs. Patients use a full dose for seven to fourteen days. The purpose of the medicine is hence to lower the level of acid in the stomach. It also helps in preventing bacterial infections that are caused by Helicobacter pylori (Delchier, Malfertheiner, & Thieroff-Ekerdt, 2014).
Pharmacokinetics
Absorption
The process of absorbing omeprazole in the body commences in small intestines. It takes a minimum of three hours to be completely absorbed. The period can be prolonged to a maximum of 6 hours. Lee, Lee, and Lee (2007) explain that the drug has a systematic bioavailability of approximately sixty percent, especially after a repeated dose. The percentage keeps on increasing if a patient repeatedly continues to use Prilosec delayed-release capsules. Omeprazole is grouped in the same category with other PPIs medicines. The class of these drugs has been observed by scholars to be effective when they are in contact with an active H+/K+-ATPase pumps (Yu, Bauer, Bain, & Bauer, 2011).
Stimulation of pumps is only possible in the presence of food. Any digestible substance helps in enhancing digestion. Patients should, therefore, take the drug using water and should ensure that they have not been eating for the last three hours. The stomach should be free from any digestible substance. Individuals who are using omeprazole should also avoid eating any food for a minimum period of thirty minutes after use. The time will be essential since it will help in ensuring that the absorption did not commence in the stomach (Sheen & Triadafilopoulos, 2011). The time gap will allow the medicine to be absorbed in small intestines as required. However, scholars differ on their opinion concerning the waiting period before eating. Wang et al. (2016) argue that, with the use of delayed-release types of omeprazole, it is not necessary for patients to wait before eating after they take medication.
The absorption is fast, and peak plasma levels of the drug occur within a time interval of between half to three and half hours. It is argued that “prilosec delayed-release capsules contain an enteric-coated granule formulation of omeprazole” (Peura et al., 2009, p. 1015). The drug is acid-labile that ensures that the absorption does not start before the granules get out of the stomach. Omeprazole has a peak plasma concentration that is approximately equal to doses of up to 40 mg. However, the saturable fast pass effects cause greater than linear response during the absorption process. As a result, a peak plasma concentration can only take places with a dosage that is higher than 40 milligrams (Teng et al., 2015)
Metabolism and Excretion
The metabolic process of omeprazole mainly takes place in the liver. It is completely metabolized by the cytochrome P450 enzyme system. Gargiulo et al. (2016) confirmed that the Sulfone derivatives of omeprazole, hydroxy-omeprazole and sulfide are the only identified substances that are involved as products of the metabolism process. The three metabolites contribute insignificantly to the antisecretory activity. The excretion of an approximate amount of 80% of an orally administered dose passes with urine. The remaining amount is excreted in feces, and it mainly originates from bile secretion. The percentages hence indicate that there is a significant biliary excretion of metabolites of the omeprazole.
Pharmacodynamics
Antisecretory Activity
According to Yu, Qian, Guo, Li and Liu (2016), omeprazole functions in an irreversible and selective manner inside the body. It decreases the secretion of stimulated acid and blocks final step of acid production irrespective of the stimulus. Impacts of the inhibitory function of the omeprazole drug take place within a period of one hour after it is administered orally. Its optimal effects are experienced within two hours of administration. The suppression time can be up to a maximum of 72 hours. The baseline of the secretory activity of the stomach acid resumes after a period of three to five days after the omeprazole becomes inactive. Its suppressive effect increases with a repeat in daily dosage. Vaduganathan et al. (2016) argue that the continued administration of the required dose will cause its inhibitory impact on acid secretion to reach a stable state after four days. Extra consumption will have minimal suppressing effects.
Enterochromaffin-like (ECL) Cell Effects
Use of omeprazole in the long-run can cause an abnormal increase in the number of cells. Gargiulo et al. (2016) argue that using the medication for an extended period has a possibility of causing malignant and premalignant conditions. However, many studies have ruled out the likeliness of omeprazole to cause the enlargement of organs and tissues through increasing the number of abnormal cells in the body. Scholars have also ruled out the possibility of the medication to cause a pathological process that results in the formation and growth of a tumor (Teng et al., 2015).
Serum Gastrin Effects
Administration of omeprazole causes the patients’ level of serum gastrin to increase in the first one to two weeks. The levels become constant after that even if treatment procedure continues. Lee et al. (2007) support that, the gastrin value returns to the initial levels between first to second weeks after the discontinuation of the medication process. The increased level of gastrin that is caused by administering omeprazole causes enterochromaffin-like cell hyperplasia. It also results in an increment of the amount of serum Chromogranin A (CgA). High levels of CgA create a possibility of having false positive outcomes when conducting a diagnostic analysis for neuroendocrine tumors. As a result, medical practitioners are required to discontinue omeprazole treatment momentarily. They should wait for a minimum time of fourteen days before they assess CgA levels. Doctors should repeat the test if the amount is still high to avoid giving their patients false positive results and wrong drug prescriptions (Delchier et al., 2014).
Adverse Effects and Side Effects
The negative effects of using the medication vary depending on the combination of therapy and individuals. Medical practitioners may opt to use a monotherapy like in the case of treating Zollinger-Ellison syndrome, duodenal and resistant ulcers that cause patients to experience specific adverse effects. They could suffer from nausea, abdominal pain, headache, vomiting, flatulence, and diarrhea. Using monotherapy can also cause adverse effects like infections of upper respiratory, dizziness, acid regurgitation, asthenia, back pain, constipation, cough, and rashes. Children at the age of two years and below who are diagnosed with “prilosec delayed-release capsules experiences adverse reactions of the respiratory system, frequent accidental injuries and fevers, ” (Yu et al., 2016, p. 1105).
According to Sheen and Triadafilopoulos (2011), the combination of therapy for H. pylori eradication minimizes the adverse effects of the medication. For instance, combining prilosec and clarithromycin causes reduced adverse effects like flu-syndrome, rhinitis, coloring of tongue and pharyngitis. Triple therapy can be through combining prilosec, clarithromycin, and amoxicillin. The common side effects of the omeprazole include headaches, diarrhea, and taste perversion. Negative impacts of triple and duo therapy have lesser frequency compared to the administering of antimicrobial agents alone.
Omeprazole medication can affect different organs, senses or body as a whole. For instance, it can cause hypersensitivity reactions in the body that include anaphylactic shock, fatigue, interstitial nephritis, angioedema, urticaria, bronchospasm and anaphylaxis (Lee et al., 2007). Cardiovascular adverse effects of the medication include palpitations, peripheral edema, tachycardia, increased blood pressure, angina, and bradycardia. Gastrointestinal adverse effects of the omeprazole are fecal discoloration, mucosal atrophy of the tongue, irritable colon, Pancreatitis, abdominal swelling, anorexia, microscopic colitis, esophageal candidiasis, and stomatitis.
The medication has the potential of causing liver diseases like hepatic failures, cholestatic illness and hepatic encephalopathy hepatocellular. Other adverse effects include severe generalized skin reactions, metabolism and nutritional disorders, muscle cramps and weakness, bone fracture, ocular, urogenital and hematologic disease. Sheen and Triadafilopoulos (2011) explain that there are common side effects of prilosec that should be reported to the medical practitioners. Patients should be cautious of severe impacts of medications like increased gas in the stomach, vomiting, nausea, constipation, and headache. They should be reported to the medical care specialists when they become severe.
Serious Side Effects
Some adverse impacts of the omeprazole require patients to contact their doctors and seek emergency medical assistance. They include throaty harshness, rashes, swelling of the face, tongue, eyes, throat, feet, hands and lips. Individuals should seek medical advice if they experience difficulties when breathing or swallowing substances. Patients can experience irregular, fast heartbeat, extreme fatigue, dizziness, muscles spasms, seizure and diarrhea with watery stools. According to Lee et al. (2007), severe side effects can also cause stomach pain, fever and uncontrollable shaking of a single part of the body.
Uncommon side effects
Patients can develop sudden and unusual body weights after they use omeprazole. The side effect is not common but, it is risky. Patients should seek prompt medical attention. Weight gain could be an indication of responsive or allergy to the drug. The weight gain could also be a reflection of a potential separate and a serious problem. Doctors may prescribe the use of omeprazole for the treatment of gout. Patients suffering from acute gout attack can experience an increase in body weight (Yu et al., 2011). Pasternak and Hviid (2010) affirms that pregnant women who could be taking medication can experience rare side effects of swelling, and bloating particularly in ankles, face or legs. Water retention in the body parts can appear to be a weight gain. The side effect is mild, and patients do not have to seek medical attention from specialists. However, the persistence of adverse effects of the medication requires patients to consult with doctors. It is also likely for the fetus to increase weight if the mother is taking omeprazole medication.
Risk versus Benefits
Omeprazole offers many advantages when compared with other drugs, particularly, in the treatment of reflux and erosive oesophagitis. It is also an effective medicine when treating duodenal and gastric ulcers. According to Scarpignato, Gatta, Zullo and Blandizzi, (2016), omeprazole can heal a large number of patients and at a high rate when compared to histamine H2-receptor antagonists. The adverse effects of medication can also be observed within a short period after treatment. The frequency of maintenance of omeprazole of reflux oesophagitis is substantially greater than that of H2-antagonist therapy. The research supports that there is no clinical proved evidence that the medication causes gastric bacterial overgrowth or hypergastrinemia (Scarpignato et al., 2016).
Omeprazole can cause risks that can be associated with missing doses, overdose and suddenly avoiding the medicine. Too much consumption can result in having dangerous levels of the drug in the body. Risks that are associated with overdose include confusion, blurred vision, dry mouth, flushing sweating, and drowsiness. Missing doses will cause the medication to stop working efficiently, and it could also be terminated immediately. Other risks that are caused by suddenly avoiding to follow medication are the reduction in the improvements that were initially experienced. For instance, the risk that heartburn, ulcers and acid reflux symptoms may fail to improve. Omeprazole belongs to the class of PPIs drugs that are associated with risks such as dementia, heart and kidney diseases. It is also linked with the reduced rate of vitamin B12 absorption and risk of causing cancer of the stomach and esophagus (Scarpignato et al., 2016).
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