How does it work? What are its effects?
Esomeprazole is a member of the proton pump inhibitor (PPI) class of medications. In adults and children, it is used to treat conditions such as reflux esophagitis (tissue damage caused by reflux of gastric contents into the esophagus) and symptoms of gastro esophageal reflux, or GERD., people with reflux esophagitis or non-erosive reflux, or RNE (heartburn and regurgitation not associated with tissue damage). In combination with other drugs, esomeprazole is used to treat duodenal ulcers caused by the presence of Helicobacter pylori bacteria.
Esomeprazole may be used to treat or reduce the risk of gastric ulcers caused by drugs called NSAIDs (eg ibuprofen, naproxen, ketorolac) that irritate the stomach. It is also used to treat a condition associated with overproduction of stomach acid, including Zollinger-Ellison syndrome.
Esomeprazole works by reducing the amount of acid produced by the stomach.
In what forms does Nexium Generic occur?
Each pale pink, oblong, biconvex, delayed-release tablet, debossed with “A” and “EH” on one side and “20 mg” on the other side, contains 20 mg of esomeprazole equivalent to 22.3 mg esomeprazole magnesium trihydrate. Nonmedicinal ingredients: microcrystalline cellulose, triethyl citrate, methacrylic acid / ethyl acrylate copolymer, crospovidone, titanium dioxide, hydroxypropylcellulose, hypromellose, monostearin, iron oxide, synthetic paraffin, polyethylene glycol, polysorbate, magnesium stearate , sodium stearyl fumarate, sugar spheres and talc.
Each pink, oblong, biconvex, delayed release tablet, debossed with “A” and “EI” on one side and “40 mg” on the other, contains esomeprazole 40 mg equivalent to 44.5 mg of esomeprazole magnesium trihydrate. Microcrystalline cellulose, crospovidone, glyceryl monostearate, hydroxypropylcellulose, hypromellose, iron oxide, magnesium stearate, methacrylic acid / ethyl acrylate copolymer, polyethylene glycol, polysorbate, sodium stearyl fumarate, sugar spheres, synthetic paraffin, talc, titanium dioxide and triethyl citrate.
Granules for oral suspension
Each bag of pale yellow (may also be brownish) delayed release granules contains 10 mg of esomeprazole. Dextrose, crospovidone, citric acid, glyceryl monostearate, hypromellose, hydroxypropylcellulose, iron oxide, magnesium stearate, methacrylic acid copolymer type C, polysorbate, sugar spheres, talc, trietyl citrate, and gum xanthan.
How should Nexium generic be used?
The recommended dose of esomeprazole for reflux esophagitis and GERD symptoms is 40 mg once daily for 4 to 8 weeks. After 8 weeks, treatment can be continued at a dose of 20 mg once daily for 4 additional weeks.
To treat non-erosive GERD or heartburn, the recommended dose is 20 mg once daily for 2 to 4 weeks. Subsequently, esomeprazole may be taken at a dose of 20 mg once daily as needed to control symptoms.
To treat stomach ulcers associated with the use of NSAIDs, the dose is 20 mg taken once a day for 4 to 8 weeks. To prevent such ulcers, the dose is 20 mg taken once a day. To treat adult duodenal ulcers caused by Helicobacter pylori, the dose of esomeprazole is 20 mg twice daily in combination with amoxicillin 1000 mg twice daily and clarithromycin 500 mg. mg taken twice a day for 7 days in total.
To treat reflux esophagitis in children aged 12 months to 11 years, the recommended dose of esomeprazole is based on the child’s body weight and ranges from 10 mg to 20 mg once daily for 8 weeks. . For MNER (heartburn and reflux), the recommended dose is 10 mg once daily for up to 8 weeks.
For children 11 to 17 years old, the recommended dose of esomeprazole for reflux esophagitis is 20 mg to 40 mg taken once a day for 4 to 8 weeks. For non-erosive GERD (heartburn and reflux), the recommended dose is 20 mg taken once a day for 2 to 4 weeks.
There are several factors that can be considered in determining the dose a person needs: weight, health, and other medications. If your doctor has recommended a dose other than those listed here, do not change the way you take the medicine without first consulting it.
Esomeprazole tablets can be taken with or without food. They must swallow without chewing or chewing – and they should not be crushed either. Otherwise, the tablet can be put in half a glass of still water that you can stir until it breaks up. Drink immediately or within 30 minutes the liquid containing the small particles of the drug. To get the full dose of the medicine, rinse the glass with water and drink this water.
The bags of esomeprazole contain granules for oral suspension. Empty a whole packet of granules into a glass containing 1 tablespoon (15 mL) of water, stir and let stand a few minutes for the mixture to thicken. Stir again and drink the mixture in the next 30 minutes. To get the full dose of the medicine, rinse the glass with water and drink this water.
It is important to use Nexium as directed by your doctor. If you miss a dose, take the medicine as soon as you notice the omission and resume the treatment as soon as possible. If it is almost time for your next dose, do not worry about the missed dose and go back to the usual dosing schedule. Do not use a double dose to compensate for a missed dose. If you are unsure of what to do after you miss a dose, ask your doctor or pharmacist for advice.
Store Esomeprasol at room temperature, away from light and moisture and out of the reach of children.
Do not dispose of medicines in wastewater tank (eg, in the sink or in the toilet bowl) or with household waste. Ask your pharmacist how to get rid of unused or expired medications.
After oral administration of 20 mg and 40 mg of esomeprazole, the effect occurs within one hour. After repeated administration of esomeprazole 20 mg once daily for 5 days, the mean acid peak obtained after pentagastrin stimulation decreases by 90% at day 5, 6-7 hours post dose.
After 5 days of oral doses of 20 mg and 40 mg of esomeprazole, an intragastric pH greater than 4 was maintained for an average of 13 hours and 17 hours over 24 hours, respectively, in patients with symptomatic gastroesophageal reflux disease (GERD). The percentages of patients whose intragastric pH remained above 4 for at least 8, 12 and 16 hours after a 20 mg dose of esomeprazole are 76%, 54% and 24%, respectively. With a dose of 40 mg, the corresponding percentages were 97%, 92% and 56%.
Using the area under the curve as a parameter reflecting plasma concentration, a relationship between acid secretion inhibition and exposure has been demonstrated.
During antisecretory treatment, serum gastrin concentration increases in response to reduced acid gastric secretion. CgA also increases because of the decrease in gastric acidity.
An increase in the number of ECL cells in relation to the increase in serum gastrin concentrations has been observed in some long-term patients treated with esomeprazole.
The reduction of gastric acidity, whatever the cause, especially that induced by proton pump inhibitors IPPs, increases in the stomach the number of bacteria that are normally found in the digestive tract. IPPs treatment may slightly increase the risk of gastrointestinal infections caused by germs such as Salmonella and Campylobacter and possibly by Clostridium difficile in hospitalized patients.
Clinical efficiency of Nexium Generic
Esomeprazole 20 mg has been shown to effectively treat frequent heartburn in subjects receiving a 24-hour dose for 2 weeks. In two pivotal, randomized, double-blind, placebo-controlled, multicenter studies, 234 subjects with recent history of frequent heartburn were treated with 20 mg esomeprazole for 4 weeks. Symptoms associated with acid reflux (such as heartburn and acid regurgitation) were evaluated retrospectively over a 24-hour period. In both studies, esomeprazole 20 mg was significantly more effective than placebo on the primary endpoint, complete resolution of heartburn defined by the absence of heartburn during the 7 days prior to the final visit. (33.9% – 41.6% vs 11.9% – 13.7% for placebo (p <0.001) .The secondary endpoint, namely complete resolution of heartburn defined as the absence of burns reported in the patient’s diary for 7 consecutive days, was statistically significant at week 1 as well (10.0% – 15.2% vs 0.9% – 2.4% on placebo, p = 0.014, p <0.001) than at week 2 (25.2% – 35.7% vs 3.4% – 9.0% on placebo, p <0.001).
The other secondary endpoints were consistent with the primary endpoint, including heartburn relief at weeks 1 and 2, the percentage of 24-hour days without heartburn at weeks 1 and 2, the mean stomach at weeks 1 and 2 and the time to first resolution and lasting resolution of heartburn over a 24-hour period and during the night, compared with placebo. Approximately 78% of subjects receiving esomeprazole 20 mg reported a first resolution of heartburn during the first week of treatment versus 52% to 58% of subjects on placebo. The time to obtain a lasting heartburn resolution, defined as 7 consecutive days without heartburn since the first heartburn was detected, was significantly shorter in the 20 mg esomeprazole group ( 39.7% – 48.7% on day 14 vs 11.0% – 20.2% on placebo). The median time to first resolution of nocturnal heartburn was 1 day, this value was statistically significant compared to placebo in one study (p = 0.048) and close to the significance in the other (p = 0.069). About 80% of the nights were heartburn free during all periods and 90% of the nights were heartburn-free the second week of each trial, compared to 72.4% to 78.3% for the placebo. The investigators’ assessment of the resolution of heartburn was consistent with that of the subjects, with statistically significant differences between esomeprazole (34.7% -41.8%) and placebo (8.0% -11%). , 4%).
The investigators also found that esomeprazole was significantly more effective than placebo in resolving acid regurgitations (58.5% – 63.6% vs. 28.3% – 37.4% for placebo) during the evaluation. 2 weeks.
As a result of the overall therapeutic evaluation of patients at week 2, 78.0% – 80.7% of patients receiving esomeprazole 20 mg, compared to 72.4% – 78.3% of patients receiving placebo, reported that their state of health was improved. The majority of them felt the importance of this change from Important to Extremely Important in carrying out their activities of daily living (79% – 86% at week 2).
What are the possible side effects?
Many medications can cause side effects. A side effect is an undesirable response to a drug when taken at normal doses. It can be mild or severe, temporary or permanent.
Most of the side effects listed below do not occur very often, but they could cause serious problems if you do not see your doctor or if you do not receive medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
- An alteration of the taste sensations
- A drowsiness
- Abdominal pain
- Dryness of the mouth
- Sleep disorders.
- Shortness of breath
- Joint pain
- Skin reactions (such as rash, itching, or hives)
- A sensitivity to the sun
- Signs of depression (eg, lack of concentration, weight fluctuations, changes in sleep, disinterest in many activities, suicidal thoughts)
- Signs of liver problems (eg, nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
- A blurred vision.
Stop taking the medication and seek immediate medical attention if there is an answer such as:
- Severe skin problems (blisters, ulcers or lesions)
- Signs of a serious allergic reaction such as hives, difficulty breathing, swelling of the tongue, face, mouth or throat.
Some people may experience side effects other than those listed. Consult your doctor if you notice a symptom that worries you while you are using Nexium.
Conduct for vehicle drivers
Esomeprazole has a minor influence on the ability to drive or use machines. Side effects such as dizziness and visual disturbances are uncommon (see section 4.8). Patients with these types of side effects should not drive or use machines.
What are some contraindications of Nexium?
Hypersensitivity to esomeprazole, benzimidazole derivatives or to any of the excipients.
Esomeprazole should not be used concomitantly with nelfinavir.
Precautions for use
Patients are advised to take medical advice in case of:
- Significant and unintentional weight loss, repeated vomiting, dysphagia, hematemesis or melena, and if there is suspicion or presence of a gastric ulcer, the possibility of malignancy should be excluded as treatment with esomeprazole may reduce symptoms and delay the diagnosis.
- History of gastric ulcer or digestive surgery.
- Continuous symptomatic treatment for indigestion or heartburn for 4 weeks or more.
- Jaundice or severe liver disease.
New symptoms or recent changes in symptoms in patients over 55 years of age:
- Patients with persistent and relapsing disorders such as difficult digestion (dyspepsia) or heartburn (heartburn) should consult their doctor regularly. Patients over the age of 55 who take daily non-prescription medications due to difficult digestion or heartburn should inform their pharmacist or doctor.
- Patients should not take Nexium as a long-term preventative medicine.
- Treatment with proton pump inhibitors (PPIs) may lead to a slight increase in the risk of gastrointestinal infections, including Salmonella and Campylobacter, and possibly Clostridium difficile in hospitalized patients (see section 5.1).
- Patients should consult their physician before taking Esomeprasol if an endoscopy or urea breath test is planned.
Association with other drugs
The combination of esomeprazole with atazanavir is not recommended (see section Interactions with other medicinal products and other forms of interaction). If the combination of atazanavir with a proton pump inhibitor is considered essential, close clinical monitoring is recommended, together with an increase in the dose of atazanavir 400 mg with 100 mg ritonavir. A dose of 20 mg esomeprazole should not be exceeded.
Esomeprazole is an inhibitor of CYP2C19. At the beginning or end of treatment with esomeprazole, the risk of interactions with drugs metabolized by CYP2C19 should be considered. An interaction between clopidogrel and esomeprazole was observed. The clinical relevance of this interaction is uncertain. Concomitant use of esomeprazole and clopidogrel should be discouraged (see section 4.5). Patients should not take another PPI or H2 block concomitantly.
Nexium contains spheres of sugar (sucrose). It is not recommended for use in patients with fructose intolerance, glucose-galactose malabsorption or sucrase / isomaltase deficiency.
Interference with laboratory tests
Increased levels of Chromogranin A (CgA) may interfere with tests performed for the exploration of neuroendocrine tumors. In order to avoid this interference, treatment with esomeprazole should be stopped for 5 days before the determination of CgA.
Subacute cutaneous lupus erythematosus (LECS)
Inhibitors of the proton pump are associated with very infrequent cases of LECS. If lesions develop, especially on sun-exposed skin areas, and if accompanied by arthralgia, the patient should seek medical attention promptly and the healthcare professional should consider stopping Nexium. The occurrence of a LECS after treatment with a proton pump inhibitor may increase the risk of LECS with other proton pump inhibitors.
Interaction studies were performed in adults only. Effects of esomeprazole on the pharmacokinetics of other drugs Since esomeprazole is an enantiomer of omeprazole, interactions reported with omeprazole should be considered.
An interaction between omeprazole and some protease inhibitors has been reported. The clinical importance and mechanisms of these interactions are not always known. Increased gastric pH when treated with omeprazole may alter the absorption of protease inhibitors. There are other possible mechanisms of interactions that occur via inhibition of CYP2C19.
For atazanavir and nelfinavir, decreased plasma concentrations of these drugs have been reported when administered concomitantly with omeprazole; Concomitant administration of omeprazole and these drugs is therefore not recommended. Concomitant administration of omeprazole (40 mg, once daily) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers resulted in a substantial decrease in atazanavir plasma concentrations (a decrease in approximately 75% of the AUC, Cmax and Cmin). The increase in dosage of atazanavir to 400 mg did not offset the effect of omeprazole on the plasma concentrations of atazanavir. Concomitant administration of omeprazole (20 mg once daily) and atazanavir 400 mg / ritonavir 100 mg in healthy volunteers resulted in approximately a 30% decrease in exposure to atazanavir compared with exposure observed after administration of atazanavir 300 mg / ritonavir 100 mg once daily, without omeprazole 20 mg once daily. Concomitant administration of omeprazole (40 mg once daily) decreased the mean AUC, Cmax, and Cmin of nelfinavir by 36 to 39%, and mean AUC, Cmax and Cmin of its pharmacologically active metabolite M8. Due to the similarity of the pharmacokinetic and pharmacokinetic properties of omeprazole and esomeprazole, concomitant administration of esomeprazole and atazanavir is not recommended and co-administration of esomeprazole and nelfinavir is contraindicated (see sections Contraindications and Warnings and Precautions for Use).
For saquinavir (in combination with ritonavir), an increase in plasma concentration (from 80 to 100%) has been reported during concomitant treatment with omeprazole (40 mg once daily). Treatment with omeprazole 20 mg once daily did not affect exposure to darunavir (ritonavir-associated) or amprenavir (ritonavir-associated).
Treatment with esomeprazole 20 mg once daily did not affect exposure to amprenavir (with or without ritonavir). Treatment with omeprazole 40 mg once daily did not affect exposure to lopinavir (ritonavir-associated).
An increase in methotrexate concentrations has been observed in some patients when concomitant administration of methotrexate with proton pump inhibitors (PPIs). When administering high doses of methotrexate, temporary discontinuation of esomeprazole may be necessary.
Increases in serum tacrolimus have been reported with concomitant use of tacrolimus and esomeprazole. Enhanced monitoring of tacrolimus concentrations and renal function (creatinine clearance) should be performed and the dosage of tacrolimus should be adjusted as needed.
Drugs whose absorption is pH dependent
Inhibition of gastric acid during treatment with esomeprazole and other IPPs may decrease or increase drug absorption if it is dependent on gastric pH. Absorption of oral medications such as ketoconazole, itraconazole and erlotinib may decrease during treatment with esomeprazole and absorption of digoxin may increase during treatment with esomeprazole.
Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (up to 30% in two of the ten subjects). Toxicity of digoxin has been reported rarely. However, special attention should be paid when esomeprazole is given in high doses in elderly patients. Monitoring of treatment with digoxin should therefore be strengthened.
Drugs metabolised by CYP2C19
Esomeprazole inhibits CYP2C19, the major metabolizing enzyme of esomeprazole. Therefore, when co-administered with CYP2C19 metabolized drugs, such as warfarin, phenytoin, citalopram, imipramine, clomipramine, diazepam, etc., the plasma concentrations of these drugs may be increased and dose reduction may be necessary. In the case of clopidogrel, a prodrug converted to its active metabolite via CYP2C19, plasma concentrations of the active metabolite may be decreased.
A clinical trial has shown that when co-administered with 40 mg esomeprazole in patients treated with warfarin, clotting times remain within normal range. However, since marketing, only isolated cases of clinically significant INR elevations have been reported during concomitant treatment. Monitoring is recommended at initiation and at the end of concomitant treatment of esomeprazole with warfarin or other coumarin derivatives.
The results of studies in healthy subjects showed a pharmacokinetic (PK) / pharmacodynamic (PD) interaction between clopidogrel (300 mg loading dose followed by 75 mg daily maintenance dose) and esomeprazole (40 mg per day orally) resulting in a decrease in exposure to the active metabolite of clopidogrel by an average of 40% and a decrease in the maximum inhibition of platelet aggregation (ADP-induced) by an average of 14%.
In a study in healthy subjects, a decrease in the exposure of approximately 40% of the active metabolite of clopidogrel was observed when taking a fixed combination of esomeprazole 20 mg and acetylsalicylic acid (ASA). mg with clopidogrel in comparison with clopidogrel alone. However, the maximum levels of inhibition of platelet aggregation (ADP-induced) in these patients were identical in both groups.
Contradictory data on the clinical consequences of this PK / PD interaction in terms of the occurrence of major cardiovascular events have been reported in observational and clinical studies. As a precaution, the concomitant use of esomeprazole and clopidogrel should be discouraged.
Co-administration of 40 mg esomeprazole leads to a 13% increase in plasma phenytoin concentrations in epileptic patients. It is recommended to monitor the plasma concentrations of phenytoin when starting or stopping treatment with esomeprazole.
Omeprazole (40 mg once daily) increased plasma concentrations of voriconazole (a CYP2C19 substrate) with Cmax and AUCτ increased by 15% and 41%, respectively.
Like omeprazole, esomeprazole is an inhibitor of CYP2C19. In a cross-over study, omeprazole at a healthy dose of 40 mg increased the Cmax and AUC of cilostazol by 18% and 26%, respectively, and one of its active metabolites of 29%. and 69% respectively.
In healthy volunteers, concomitant administration of 40 mg esomeprazole resulted in a 32% increase in plasma AUC and a 31% prolongation of the elimination half-life. (t1 / 2) without significant increase in plasma peak of cisapride. The slight prolongation of the QTc interval observed after administration of cisapride alone is not increased when cisapride is co-administered with esomeprazole.
Concomitant administration of 30 mg esomeprazole resulted in a 45% decrease in clearance of the CYP2C19-metabolized diazepam metabolite.
A moderate number of data in the pregnant woman (between 300-1000 pregnancy results) showed no malformative or toxic effects for the fetus or newborn with esomeprazole. Studies in animals have not shown any direct or indirect harmful effects on reproduction (see section 5.3).
As a precaution, it is best to avoid the use of Nexium during pregnancy.
It is not known whether esomeprazole / metabolites are excreted in breast milk. There is insufficient data on the effects of esomeprazole in newborns / infants. Esomeprazole should not be used during breastfeeding.
Animal studies with the racemic mixture of omeprazole administered orally do not indicate an effect on fertility.
What to do in case of overdose?
To date, experience with voluntary overdose is very limited. The symptoms described when taking 280 mg are gastrointestinal symptoms and signs of fatigue. Single doses of 80 mg esomeprazole were well tolerated. There is no known specific antidote. Esomeprazole is highly bound to plasma proteins and therefore not easily dialyzable. In case of overdose, appropriate symptomatic treatment should be initiated.
What is a good alternatives?
While Nexium gives you long-lasting heartburn relief but has some risks if used long term, Zantac 75 (ranitidine) is an effective and inexpensive medicine for hearburn with few side effects, but may interfere with other drugs.
Zantac 75 doesn’t work as quickly as some other acid reducers and do not last as long as Nexium, but does not need several days or weeks to manifest benefits. It may be a better choice for patients 65 years and older, due to risk of bone fractures and severe diarrhea.
Nexium Questions and Answers
Do I need a prescription for esomeprazole?
Yes for Nexium and Nexium IV. No for Nexium 24 hour.
Is it safe to take Nexium long term?
Nexium is designed for short-term treatment of four to eight weeks, although a doctor will likely issue a second prescription if the heartburn problems are not relieved. Sometimes doctors prescribe Nexium for up to six months if other health problems have been ruled out that can also cause heartburn-like symptoms, such as cardiovascular disease.
Are there risks to take Nexium for more than a year?
In higher doses for long term than a year, a slight increase in bone fracture risk can be observed. If you experience symptoms of B12 deficiency along with your Nexium treatment, you should take advice from your.
Can I take Nexium with HIV drugs?
Some HIV drugs should not be taken with Nexium: people taking ripivirine, nelfinavir or atazanavir. Nexium decreases the blood levels of these drugs, and could make them less effective at treating HIV.
Are there other treatments than can interfere with Nexium?
Other drugs may affect the effect of Nexium or may be influenced by it. These are, for example, tuberculosis, epilepsy, depression, mycosis, gastrointestinal activity disorders or heart problems, tranquilizers and / or sleeping pills, anticoagulants, certain drugs used to prevent organ rejection after transplantation, and certain anti-cancer drugs.
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