what is nexium Uses, Dosage, Side Effects, Precautions & Warnings

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nexium Generic drug of the therapeutic class: Stomach Medicines
active principles: esomeprazole

what is nexium?

• Esomeprazole reduces the production of acid in the stomach.
• In case of upset stomach (heartburn, pain due to rising stomach acid or bloating with nausea), ulcers, duodenal ulcers and in Zollinger-Ellison syndrome (rare stomach disease with many stomach complaints). Also to prevent stomach problems if you use medications that can damage the stomach.
• Works within 1 to 2 hours and about 12 hours long. The damage will begin to heal within a few days. You will then suffer less from your stomach.
• Tablets and capsules : take without chewing. Do you have difficulty swallowing? You can disintegrate the tablet into half a glass of tap water. Open the capsule and put the granules in half a glass of tap water. Stir and drink. Swallow the granules through.
• Bags: sprinkle the grains in half a glass of tap water. Stir and drink. Do not chew on grains.
• How long you should use esomeprazole depends on your condition. Sometimes you have to use it for a long time to prevent a return of your symptoms. Do you take it against stomach problems due to medication? You only have to take esomeprazole on the days when you are using the stomach-damaging medicine.
• You may become nauseous, dizzy or sleepy. You may also experience abdominal pain or headaches. Do you suffer from these side effects? Consult your doctor.
• There are interactions with other means. Ask your pharmacist if you can use esomeprazole safely with your other medicines, including medicines that you have purchased without a prescription.

what is nexium used for and indication?

Nexium Control is indicated for the short-term treatment of symptoms of gastroesophageal reflux (eg, heartburn and acid regurgitation) in adults.

Nexium Dosage

nexium 20 mg dose

1. The recommended dose is 20 mg esomeprazole (one tablet) daily.
2. Taking tablets for 2 or 3 consecutive days may be necessary to improve symptoms. The duration of treatment can be up to 2 weeks. Once the symptoms are gone, treatment should be stopped.
3. If symptoms persist after 2 weeks of continuous treatment, the patient should be advised to consult a physician.

Specific populations

Patients with renal insufficiency

• No dosage adjustment is necessary in patients with renal impairment.
• Patients with severe renal impairment should be treated with caution because of limited experience in these patients .

Patients with hepatic impairment

• No dose adjustment is required in patients with mild to moderate hepatic impairment. However, patients with severe hepatic impairment should be advised by a physician before taking Nexium Control (see Warnings and Precautions and Pharmacokinetic Properties sections ).
• Seniors (≥ 65 years old)
• No dose adjustment is required in elderly patients.

Pediatric population

There is no justified use of Nexium Control in the pediatric population under 18 years of age in the indication: “short-term treatment of symptoms of gastroesophageal reflux (eg, heartburn and acid regurgitation)”.

Administration mode

The tablets should be swallowed whole with half a glass of water. The tablets should not be chewed or chewed.

Moreover, the tablet can be disintegrated in half a glass of non-carbonated water. No other liquid should be used as the enteric coating can be dissolved. Mix the solution until the tablet is disintegrated. The solution with the granules should be ingested immediately or within 30 minutes. The glass should be rinsed with half a glass of water and the water should be ingested. The granules should not be chewed or chewed.

how does nexium work

Pharmacotherapeutic group: Drugs for acidity disorders, proton pump inhibitors.

ATC Code: A02B C05.

Esomeprazole is the S-isomer of omeprazole and decreases acidic gastric secretion by a specifically targeted mechanism of action. It is a specific inhibitor of the proton pump at the level of the parietal cell. Both R and S isomers of omeprazole have similar pharmacodynamic activity.

Action mechanism

• Esomeprazole is a weak base. It is concentrated and converted into an active form in the highly acidic environment of secretory canaliculi of the parietal cell, where it inhibits the enzyme H + K + -ATPase (the proton pump), basal acid secretion and stimulated acid secretion.

Pharmacodynamic effects

• After oral administration of 20 mg and 40 mg esomeprazole, the effect occurs within one hour. After repeated administration of 20 mg esomeprazole once daily for 5 days, the acid medium peak obtained after stimulation by pentagastrin decreases by 90% in the 5 ^th day, 6-7 hours after dosing.
• 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 20 mg of esomeprazole were 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

• 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, the complete resolution of heartburn defined by the absence of burns.
• 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 resolution of heartburn, defined by 7 consecutive days without burning of stomach since the first observation of heartburn, was significantly shorter in the group receiving 20 mg of esomeprazole (39.7% – 48.7% at day 14 vs 11.0% – 20.2% under 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 evaluation of the resolution of heartburn by the investigators 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 bad side effects of Nexium?

In addition to the desired effect, this can cause drug side effects.

The main side effects are the following.

Rarely (from 1 to 10 in 100 people)

• Gastrointestinal complaints such as nausea, vomiting, abdominal pain, diarrhea, constipation and flatulence.
• Headache .
• Irritation at the injection site , especially at high doses .

Very rare (affects less than 1 in 100 people)

• Dizziness and drowsiness .
• Itching, skin rash, sweating and hair loss . If you stop this medication, these side effects will go over again.
• Blurred vision or double vision, sensory disturbances and fluid retention in the legs. If you stop this medication, these side effects will go over again.
• Confusion , depression and hallucinations in the elderly. If you stop this medication, these side effects will go over again.
• Hypersensitivity to this medication. You can then get skin rash, hives or itching. In rare cases, fever, swollen lips, tongue or face, tightness , fainting, or severe skin abnormality develop. Then discontinue use and consult your doctor. You may not use this medicine in the future. Therefore, tell the pharmacist that you are hypersensitive to esomeprazole. The pharmacy team can then ensure that you do not get this medication again.
• In the man: breast formation and impotence . These side effects will pass if you stop taking this medicine. Contact your doctor if you suffer from this.
• Complaints of the mouth and throat , such as dry mouth and throat, mouth ulcers and inflammation of the oral mucosa. You notice this with a scarlet color of the mucous membranes, painful tongue or throat. Eating and drinking can be painful because of this. Also taste changes occur. Take good care of your mouth and teeth. Consult your doctor if you continue to suffer from this
• Inflammation of the kidneys or liver and blood disorders . Tell your doctor one or more of the following symptoms: sudden severe upper abdominal pain, jaundice, unexplained bruising, extreme fatigue or sore throat with fever and blisters in the throat.
• Bone fractures or fractures in the vertebrae. Contact your doctor if you suffer from this.
• Deficiency of potassium , a specific substance in the blood. You notice this first with muscle weakness, muscle cramps or muscle pain usually first in the thighs and arms, severe fatigue, palpitations , severe abdominal complaints. If you have diarrhea or vomiting a lot, contact your doctor.
• Heart rhythm disorders. You sometimes only notice this by sudden dizziness or if you just get lost. Especially people with the congenital form of cardiac arrhythmiaprolonged QT interval are more likely. Do NOT use this medicine if you have this congenital heart rhythm disorder .

Consult your doctor if you suffer too much from one of the above mentioned side effects or if you experience other side effects that you are worried about.

nexium drug interactions

Interaction studies were performed in adults only.

nexium interactions with other medications

Since esomeprazole is an enantiomer of omeprazole, interactions reported with omeprazole should be considered.

Protease inhibitors

• 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 about 75% of AUC, C _max and C _min). 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 nelfinavir AUC, C _max,and C _min by 36 to 39%, and mean the SC,of its pharmacologically active metabolite M8. Due to the similarity of the pharmacodynamic 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).

methotrexate

• 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.

tacrolimus

• 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-mediated 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.

warfarin

• 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.

clopidogrel

• 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) 81 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.

phenytoin

• 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.

voriconazole

• Omeprazole (40 mg once daily) increased plasma concentrations of voriconazole (a CYP2C19 substrate) with C _max and AUCτ increased by 15% and 41%, respectively.

cilostazol

• Like omeprazole, esomeprazole is an inhibitor of CYP2C19. In a cross-over study, omeprazole administered at 40 mg to healthy subjects increased C _max and cilostazol AUC by 18 and 26%, respectively, and one of its active metabolites of 29 and 69% respectively.

cisapride

• 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. (t _1/2 ) without a significant increase in the 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.

diazepam

• Concomitant administration of 30 mg esomeprazole resulted in a 45% decrease in clearance of the CYP2C19-metabolized diazepam metabolite.

Drugs without clinically significant interaction

Amoxicillin and quinidine

• Esomeprazole did not show a clinically relevant effect on the pharmacokinetics of amoxicillin and quinidine.

Naproxen or rofecoxib

• Short-term studies evaluating co-administration of esomeprazole with naproxen or rofecoxib have not shown a clinically significant pharmacokinetic interaction.

Effects of other drugs on the pharmacokinetics of esomeprazole

Drugs that inhibit CYP2C19 and / or CYP3A4

Esomeprazole is metabolized by CYP2C19 and CYP3A4. Concomitant administration of esomeprazole with a CYP3A4 inhibitor, clarithromycin (500 mg twice daily), leads to a doubling of exposure (AUC) to esomeprazole.Concomitant administration of esomeprazole and a combination inhibitor of CYP2C19 and CYP3A4 may result in an increase of more than double the exposure to esomeprazole. Voriconazole, an inhibitor of CYP2C19 and CYP3A4, resulted in an increase in AUCτ of omeprazole by 280%. A systematic dose adjustment of esomeprazole is not required in either of these situations. However, dose adjustment should be considered in patients with severe hepatic impairment,

Drugs that induce CYP2C19 and / or CYP3A4

Drugs known to induce CYP2C19 or CYP3A4 or both (such as rifampicin and St. John’s Wort ( Hypericum perforatum )) can lead to decreased serum esomeprazole levels by increasing the metabolism of esomeprazole.

Nexium Warnings and Precautions

General

Patients are advised to take medical advice in case of:

• significant and unintentional weight loss, repeated vomiting, dysphagia, haematemesis 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 Control 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 .

Patients should consult their physician before taking this medication 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. 
• Patients should not take another PPI or H ₂ concomitantly. 

Sucrose

• This medicine 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 Control. The occurrence of a LECS after treatment with a proton pump inhibitor may increase the risk of LECS with other proton pump inhibitors.

Drive and use machines

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.

Nexium and PREGNANCY / BREAST FEEDING / FERTILITY:

Nexium in Pregnancy

• 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 Control during pregnancy.

Nexium in feeding

• 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.

Nexium in Fertility

• Animal studies with the racemic mixture of omeprazole administered orally do not indicate an effect on fertility.

What should I do if nexium missed dose?

• If you take this medicine once a day : does it take more than 8 hours before you take the next dose normally? Take the forgotten dose as yet. Does it take less than 8 hours? Skip the forgotten dose .
• If you take this medicine twice a day : does it take more than 4 hours before you take the next dose normally? Take the forgotten dose as yet. Does it take less than 4 hours? Skip the forgotten dose .

What happens if I overdose from Nexium ?

To date, experience with voluntary overdose is very limited.

The symptoms described when taking 2 80 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  Forms and Composition Nexium?

Enteric coated film-coated tablet 20 mg (14 mm x 7 mm, pale pink, oblong, biconvex, engraved “20 mg” on one side and “A / EH” on the other side):  Boxes of 7 and 14.

NOT’s

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general information:

• Includes a general description of the drug, its use, brand names, FAQs, and relevant news and articles

Additional information:

• General explanation about dealing with the medicine: how to take the medicine, the doses and times of it, the start and duration of its effectiveness, the recommended diet during the period of taking the medicine, the method of storage and storage, recommendations in cases for forgetting the dose and instructions to stop taking the drug and take additional doses.

Special warnings:

• For pregnant and breastfeeding women, the elderly, boys and drivers, and use before surgery.

Side effects:

• It treats possible side effects and drug interactions that require attention and its effect on continuous use.
• The information contained in this medicine is based on medical literature, but it is not a substitute for consulting a doctor.

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