Olzole-ES Uses

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What is Olzole-ES?

Olzole-ES strontium is used to treat conditions where there is too much acid in the stomach. It is used to treat duodenal and gastric ulcers, erosive esophagitis, gastroesophageal reflux disease (GERD), and the Zollinger-Ellison syndrome. Olzole-ES is also used with antibiotics (eg, amoxicillin, clarithromycin) to treat ulcers that are caused by the H. pylori bacteria. Olzole-ES strontium is also used to prevent stomach ulcers and stomach irritation in patients taking pain and arthritis drugs called NSAIDs, such as aspirin or ibuprofen, for long periods of time.

Olzole-ES strontium is a proton pump inhibitor (PPI). It works by decreasing the amount of acid that is produced by the stomach.

Olzole-ES strontium is available only with your doctor’s prescription.

Olzole-ES indications

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Treatment of Gastroesophageal Reflux Disease (GERD)

Healing of Erosive Esophagitis

Olzole-ES Magnesium Delayed-Release Capsules are indicated for the short-term treatment (4 to 8 weeks) in the healing and symptomatic resolution of diagnostically confirmed erosive esophagitis. For those patients who have not healed after 4 to 8 weeks of treatment, an additional 4 to 8 week course of Olzole-ES Magnesium Delayed-Release Capsules may be considered.

Maintenance of Healing of Erosive Esophagitis

Olzole-ES Magnesium Delayed-Release Capsules are indicated to maintain symptom resolution and healing of erosive esophagitis. Controlled studies do not extend beyond 6 months.

Symptomatic Gastroesophageal Reflux Disease

Olzole-ES Magnesium Delayed-Release Capsules are indicated for short-term treatment (4 to 8 weeks) of heartburn and other symptoms associated with GERD in adults and children 1 year or older.

Risk Reduction of NSAID-Associated Gastric Ulcer

Olzole-ES Magnesium Delayed-Release Capsules are indicated for the reduction in the occurrence of gastric ulcers associated with continuous NSAID therapy in patients at risk for developing gastric ulcers. Patients are considered to be at risk due to their age (≥ 60) and/or documented history of gastric ulcers. Controlled studies do not extend beyond 6 months.

H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence

Triple Therapy (Olzole-ES Magnesium Delayed-Release Capsules plus amoxicillin and clarithromycin): Olzole-ES Magnesium Delayed-Release Capsules, in combination with amoxicillin and clarithromycin, is indicated for the treatment of patients with H. pylori infection and duodenal ulcer disease (active or history of within the past 5 years) to eradicate H. pylori. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.

In patients who fail therapy, susceptibility testing should be done. If resistance to clarithromycin is demonstrated or susceptibility testing is not possible, alternative antimicrobial therapy should be instituted.

Pathological Hypersecretory Conditions Including Zollinger-Ellison Syndrome

Olzole-ES Magnesium Delayed-Release Capsules are indicated for the long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison Syndrome.

How should I use Olzole-ES?

Use Olzole-ES delayed-release capsules as directed by your doctor. Check the label on the medicine for exact dosing instructions.

Ask your health care provider any questions you may have about how to use Olzole-ES delayed-release capsules.

Uses of Olzole-ES in details

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Use: Labeled Indications

Oral:

Olzole-ES magnesium and Olzole-ES strontium:

Gastroesophageal reflux disease (Rx only):

Healing of erosive esophagitis: Short-term (4 to 8 weeks) treatment of erosive esophagitis

Maintenance of healing of erosive esophagitis: Maintaining symptom resolution and healing of erosive esophagitis

Symptomatic gastroesophageal reflux disease: Short-term (4 to 8 weeks) treatment of symptomatic gastroesophageal reflux disease (GERD)

Helicobacter pylori eradication (Rx only): As part of a multidrug regimen for Helicobacter pylori eradication in patients with duodenal ulcer disease (active or history of within the past 5 years)

Risk reduction of nonsteroidal anti-inflammatory drug-associated gastric ulcer (Rx only): Prevention of gastric ulcers associated with continuous NSAID therapy in patients at risk (age ≥60 years and/or history of gastric ulcer)

Pathological hypersecretory conditions, including Zollinger-Ellison syndrome (Rx only): Treatment (long-term) of pathological hypersecretory conditions including Zollinger-Ellison syndrome

Olzole-ES magnesium:

Heartburn (OTC labeling): Treatment of frequent heartburn (≥2 days per week).

IV: Olzole-ES sodium:

Gastroesophageal reflux disease (Rx only): Short-term (≤10 days) treatment of gastroesophageal reflux disease (GERD) with erosive esophagitis in pediatric patients 1 month to 17 years of age and adults when oral therapy is not possible or appropriate

Risk reduction of ulcer rebleeding postprocedure (Rx only): Decrease the risk of rebleeding postendoscopy for acute bleeding gastric or duodenal ulcers in adults

Off Label Uses

Barrett esophagus

Data from a meta-analysis of observational studies evaluating acid suppressive therapy and the risk of esophageal adenocarcinoma or high-grade dysplasia in patients with Barrett esophagus showed that proton pump inhibitors were associated with a reduction in the risk of esophageal adenocarcinoma and high-grade dysplasia associated with Barrett esophagus; a longer duration of PPI use was associated with a greater protective effect.

Olzole-ES description

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Each tablet contains 20 mg or 40 mg Olzole-ES (as magnesium trihydrate).

Each tablet contains esomeprazole as enteric-coated pellets (MUPS).

Olzole-ES MUPS is a proton pump inhibitor. The active ingredient in Olzole-ES MUPS is Olzole-ES magnesium trihydrate, a substituted benzimidazole. Olzole-ES is the S-isomer of omeprazole. It is optically stable in vivo, with negligible conversion to the R-isomer. The chemical name is di-(S)-5-methoxy-2-[[4-methoxy-3,5-dimethyl-2-pyridinyl)methyl] sulfinyl] -1H- benzimidazole magnesium salt trihydrate.

Its molecular formula is C34H36N6O6S2Mg·3H2O and has a molecular weight of 767.2 (trihydrate).

Excipients/Inactive Ingredients: Glycerol monostearate 40-55, hyprolose, hypromellose, iron oxide (E 172) (Tablet 20 mg, reddish-brown CI 77491, yellow, CI 77492) (Tablet 40 mg, reddish-brown CI 77491), magnesium stearate, methacrylic acid ethyl acrylate copolymer (1:1) dispersion 30 percent, cellulose microcrystalline, synthetic paraffin, macrogols, polysorbate 80, crospovidone, sodium stearyl fumarate, sugar spheres (sucrose and maize starch), talc, titanium dioxide (E 171), triethyl citrate.

Olzole-ES 20 mg: Sucrose 28 mg.

Olzole-ES 40 mg: Sucrose 30 mg.

Olzole-ES dosage

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Usual Adult Dose for Gastroesophageal Reflux Disease:

Olzole-ES Magnesium:

-20 mg orally once a day for 4 weeks

Olzole-ES Strontium:

-24.65 mg orally once a day for 4 to 8 weeks.

Comment:

-If symptoms do not resolve after 4 weeks, an additional 4 weeks may be considered.

GERD with Erosive Esophagitis:

Olzole-ES Sodium:

-20 mg or 40 mg IV injection once a day, over no less than 3 minutes; or IV infusion once a day, over no less than 10 to 30 minutes

Comment: Safety and efficacy of Olzole-ES sodium IV for Injection for more than 10 days have not been demonstrated.

Uses: Short term treatment of heartburn and symptomatic gastroesophageal reflux disease; short term treatment of GERD with erosive esophagitis, inclusively as an alternative to oral therapy, if unable to use oral route

Usual Adult Dose for Erosive Esophagitis:

Healing:

-Olzole-ES Magnesium: 20 to 40 mg orally once a day for 4 to 8 weeks

-Olzole-ES Strontium: 24.65 to 49.3 mg orally once a day for 4 to 8 weeks

-An additional 4 to 8 week course of therapy may be considered in patients not healed after initial treatment.

Maintenance of healing:

-Olzole-ES Magnesium: 20 mg orally once a day

-Olzole-ES Strontium: 24.65 mg orally once a daily

Comments:

-Olzole-ES Sodium injection may be used as an alternative to oral therapy, if unable to use oral route.

-Maintenance of healing: Controlled studies did not extend beyond six months.

Uses: Short-term treatment in the healing and symptomatic resolution of diagnostically confirmed erosive esophagitis; to maintain symptom resolution and healing of erosive esophagitis

Usual Adult Dose for Helicobacter pylori Infection:

Olzole-ES Magnesium:

Triple therapy:

-40 mg orally once a day for 10 days, along with amoxicillin 1000 mg and clarithromycin 500 mg orally twice a day for 10 days

Olzole-ES Strontium:

Triple therapy:

-49.3 mg orally once a day for 10 days, along with amoxicillin 1000 mg and clarithromycin 500 mg orally twice a day for 10 days

Comments:

-Susceptibility testing should be done in patients who fail therapy.

-If resistance to clarithromycin is demonstrated or susceptibility testing is not possible, alternative antimicrobial therapy should be instituted.

-Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence.

Use: Triple therapy (Olzole-ES plus amoxicillin and clarithromycin): Treatment of H. pylori infection and duodenal ulcer disease (active or history of within the past 5 years) to eradicate H. pylori

Usual Adult Dose for NSAID-Induced Gastric Ulcer:

Olzole-ES Magnesium:

-20 mg to 40 mg orally once daily for up to 6 months

Olzole-ES Strontium:

-24.65 mg to 49.3 mg orally once a day for up to 6 months

Comment:

-Patients older than 60 years and/or with history of gastric ulcers are considered to be at risk for developing gastric ulcers.

-Controlled studies do not extend beyond 6 months

Use: Reduction in the occurrence of gastric ulcers associated with continuous NSAID therapy in patients at risk for developing gastric ulcers.

Usual Adult Dose for Zollinger-Ellison Syndrome:

Olzole-ES Magnesium:

-40 mg orally twice a day

Olzole-ES Strontium:

-49.3 mg orally twice a day

Comment: Doses up to 240 mg daily have been used.

Use: Long term treatment of pathological hypersecretory conditions, including Zollinger-Ellison Syndrome

Usual Adult Dose for Pathological Hypersecretory Conditions:

Olzole-ES Magnesium:

-40 mg orally twice a day

Olzole-ES Strontium:

-49.3 mg orally twice a day

Comment: Doses up to 240 mg daily have been used.

Use: Long term treatment of pathological hypersecretory conditions, including Zollinger-Ellison Syndrome

Usual Adult Dose for Duodenal Ulcer Prophylaxis:

Olzole-ES Sodium:

-Initial dose: 80 mg IV infusion over 30 minutes

-Maintenance dose: 8 mg/hr IV continuous infusion for a total of 72 hours (includes initial 30 minute dose plus 71.5 hours of continuous infusion)

Comments:

-Intravenous therapy is aimed solely at the acute initial management of bleeding gastric or duodenal ulcers and does not constitute full treatment.

-Intravenous therapy should be followed by oral acid-suppressive therapy.

Use: Risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy

Usual Adult Dose for Gastric Ulcer Prophylaxis:

Olzole-ES Sodium:

-Initial dose: 80 mg IV infusion over 30 minutes

-Maintenance dose: 8 mg/hr IV continuous infusion for a total of 72 hours (includes initial 30 minute dose plus 71.5 hours of continuous infusion)

Comments:

-Intravenous therapy is aimed solely at the acute initial management of bleeding gastric or duodenal ulcers and does not constitute full treatment.

-Intravenous therapy should be followed by oral acid-suppressive therapy.

Use: Risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy

Usual Pediatric Dose for Gastroesophageal Reflux Disease:

Olzole-ES Magnesium:

Less than 1 year:

-Data not available

1 to 11 years:

-10 mg once a day for up to 8 weeks

-Comment: Doses over 1 mg/kg/day have not been studied.

12 to 17 years:

-20 mg once a day for 4 weeks

Olzole-ES Sodium:

GERD with Erosive Esophagitis:

Less than 1 month:

-Not recommended.

1 month to less than 1 year:

-0.5 mg/kg IV infused over 10 to 30 minutes

1 to 17 years:

-Less than 55 kg: 10 mg IV infused over 10 to 30 minutes

-55 kg or more: 20 mg IV infused over 10 to 30 minutes

Olzole-ES Strontium: Not recommended.

Uses: Short term treatment of symptomatic GERD; short term treatment of GERD with erosive esophagitis, inclusively as an alternative to oral therapy, if unable to use oral route

Usual Pediatric Dose for Erosive Esophagitis:

Olzole-ES Magnesium:

Healing:

Less than 1 year:

-Data not available

1 to 11 years:

-Less than 20 kg: 10 mg once a day for 8 weeks

-20 kg or more: 10 mg or 20 mg once a day for 8 weeks

12 to 17 years:

-20 or 40 mg once a day for 4 to 8 weeks

Comment: Doses over 1 mg/kg/day have not been studied.

Erosive Esophagitis due to acid-mediated GERD:

Less than 1 month:

-Data not available

1 month to less than 1 year old:

-3 kg to 5 kg: 2.5 mg once a day

-Greater than 5 kg to 7.5 kg: 5 mg once a day

-Greater than 7.5 kg to 12 kg: 10 mg once a day

Duration of therapy: For up to 6 weeks

Comment: Doses over 1.33 mg/kg/day have not been studied.

1 year and older:

-Data not available

Uses: Short-term treatment in the healing and symptomatic resolution of diagnostically confirmed erosive esophagitis; short term treatment of erosive esophagitis due to acid-mediated GERD in infants

Olzole-ES interactions

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What other drugs will affect Olzole-ES?

Effects of Olzole-ES on the Pharmacokinetics of Other Drugs: The decreased intragastric acidity during treatment with Olzole-ES, might increase or decrease the absorption of drugs if the mechanism of absorption is influenced by gastric acidity. In common with the use of other inhibitors of acid secretion or antacids, the absorption of ketoconazole and itraconazole can decrease during treatment with Olzole-ES.

Olzole-ES inhibits CYP2C19, the major Olzole-ES-metabolising enzyme. Thus, when Olzole-ES is combined with drugs metabolised by CYP2C19 eg, diazepam, citalopram, imipramine, clomipramine, phenytoin, etc, the plasma concentrations of these drugs may be increased and a dose reduction could be needed. This should be considered especially when prescribing Olzole-ES for on-demand therapy.

Concomitant administration of Olzole-ES 30 mg resulted in a 45% decrease in clearance of the CYP2C19 substrate diazepam. Concomitant administration of Olzole-ES 40 mg resulted in a 13% increase in trough plasma levels of phenytoin in epileptic patients. It is recommended to monitor the plasma concentrations of phenytoin when treatment with Olzole-ES is introduced or withdrawn.

Olzole-ES has been shown to have no clinically relevant effects on the pharmacokinetics of amoxicillin, quinidine or warfarin.

Effects of Other Drugs on the Pharmacokinetics of Olzole-ES: Olzole-ES is metabolised by CYP2C19 and CYP3A4. Concomitant administration of Olzole-ES and a CYP3A4 inhibitor, clarithromycin (500 mg twice daily), resulted in a doubling of the exposure (AUC) to Olzole-ES. Dose adjustment of Olzole-ES is not required.

Olzole-ES side effects

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What are the possible side effects of Olzole-ES?

Clinical Trials Experience With

Intravenous Olzole-ES

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Adults

The safety of intravenous Olzole-ES is based on results from clinical trials conducted in four different populations including patients having symptomatic GERD with or without a history of erosive esophagitis (n=199), patients with erosive esophagitis (n=160), healthy subjects (n=204) and patients with bleeding gastric or duodenal ulcers (n=375).

Symptomatic GERD and Erosive Esophagitis Trials

The data described below reflect exposure to Olzole-ES I.V. for Injection in 359 patients. Olzole-ES I.V. for Injection was studied only in actively-controlled trials. The population was 18 to 77 years of age; 45% Male, 52% Caucasian, 17% Black, 3% Asian, 28% Other, and had either erosive reflux esophagitis (44%) or GERD (56%). Most patients received doses of either 20 or 40 mg either as an infusion or an injection. Adverse reactions occurring in ≥ 1% of patients treated with intravenous Olzole-ES (n=359) in clinical trials are listed below:

Table 2 : Adverse reactions occurring at an incidence ≥ 1% in the Olzole-ES I.V. group

Adverse Reactions % of patients Olzole-ES

Intravenous (n=359)

Headache 10.9
Flatulence 10.3
Nausea 6.4
Abdominal pain 5.8
Diarrhea 3.9
Mouth dry 3.9
Dizziness/vertigo 2.8
Constipation 2.5
Injection site reaction 1.7
Pruritus 1.1

Intravenous treatment with Olzole-ES 20 and 40 mg administered as an injection or as an infusion was found to have a safety profile similar to that of oral administration of Olzole-ES.

Pediatric

A randomized, open-label, multi-national study to evaluate the pharmacokinetics of repeated intravenous doses of once daily Olzole-ES in pediatric patients 1 month to 17 years old, inclusive was performed. The safety results are consistent with the known safety profile of Olzole-ES and no unexpected safety signals were identified.

Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers in Adults

The data described below reflect exposure to Olzole-ES I.V. for Injection in 375 patients. Olzole-ES I.V. for Injection was studied in a placebo-controlled trial. Patients were randomized to receive Olzole-ES I.V. for Injection (n=375) or placebo (n=389). The population was 18 to 98 years old; 68% Male, 87% Caucasian, 1% Black, 7% Asian, 4% other, who presented with endoscopically confirmed gastric or duodenal ulcer bleeding. Following endoscopic hemostasis, patients received either 80 mg Olzole-ES as an intravenous infusion over 30 minutes followed by a continuous infusion of 8 mg per hour or placebo for a total treatment duration of 72 hours. After the initial 72-hour period, all patients received oral proton pump inhibitor (PPI) for 27 days.

Table 3 : Incidence (%) of adverse reactions that occurred in greater than 1% of patients within 72 hours after start of treatment*

Number(%)of patients
Olzole-ES

(n=375)

Placebo

(n=389)

Duodenal ulcer haemorrhage 16 (4.3%) 16 (4.1%)
Injection site reaction# 16 (4.3%) 2 (0.5)
Pyrexia 13 (3.5%) 11 (2.8%)
Cough 4 (1.1%) 1 (0.3%)
Dizziness 4 (1.1%) 3 (0.8%)
*Incidence ≥ 1% in the Olzole-ES group and greater than placebo group safety population

#Injection site reactions included erythema, swelling, inflammation, pruritus, phlebitis, thrombophlebitis and superficial phlebitis.

With the exception of injection site reactions described above, intravenous treatment with Olzole-ES administered as an injection or as an infusion was found to have a safety profile similar to that of oral administration of Olzole-ES.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of Olzole-ES. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Postmarketing Reports - There have been spontaneous reports of adverse events with postmarketing use of Olzole-ES. These reports occurred rarely and are listed below by body system:

Blood And Lymphatic System Disorders: agranulocytosis, pancytopenia;

Eye Disorders: blurred vision;

Gastrointestinal Disorders: pancreatitis; stomatitis; microscopic colitis;

Hepatobiliary Disorders: hepatic failure, hepatitis with or without jaundice;

Immune System Disorders: anaphylactic reaction/shock;

Infections and Infestations: GI candidiasis;

Metabolism and nutritional disorders: hypomagnesemia;

Musculoskeletal And Connective Tissue Disorders: muscular weakness, myalgia, bone fracture;

Nervous System Disorders: hepatic encephalopathy, taste disturbance;

Psychiatric Disorders: aggression, agitation, depression, hallucination;

Renal and Urinary Disorders: interstitial nephritis;

Reproductive System and Breast Disorders: gynecomastia;

Respiratory, Thoracic and Mediastinal Disorders: bronchospasm;

Skin and Subcutaneous Tissue Disorders: alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN, some fatal).

Other adverse events not observed with Olzole-ES, but occurring with omeprazole can be found in the omeprazole package insert, ADVERSE REACTIONS section.

Olzole-ES contraindications

See also:
What is the most important information I should know about Olzole-ES?

Olzole-ES is rapidly absorbed after oral doses, with peak plasma levels occurring after about 1-2 hrs. It is acid labile and an enteric-coated formulation has been developed. Bioavailability of Olzole-ES increases with both dose and repeated administration to about 68% and 89% for doses of 20 mg and 40 mg, respectively. Food delays and decreases the absorption of Olzole-ES, but this does not significantly change its effect of intragastric acidity. Olzole-ES is about 97% bound to plasma proteins. It is extensively metabolized in the liver by the cytochrome P450 (CYP450) isoenzyme CYP2C19 to hydroxy and desmethyl metabolites, which have no effect on gastric acid section. The remainder is metabolized by the CYP450 isoenzyme CYP3A4 to Olzole-ES sulfone. With repeated dosage, there is a decrease in first-pass metabolism and systemic clearance, probably caused by an inhibition of the CYP2C19 isoenzyme. However, there is no accumulation during once daily use. The plasma elimination half-life (t½) is about 1.3 hrs. Almost 80% of an oral dose is eliminated as metabolites in the urine, the remainder in the feces.



Active ingredient matches for Olzole-ES:

Esomeprazole in India.


Unit description / dosage (Manufacturer)Price, USD
OLZOLE-ES tab 40 mg x 10's (Olcare)$ 0.75

List of Olzole-ES substitutes (brand and generic names):

NULOC tab 40 mg x 10's (Bergen (Alkem Laboratories Ltd))$ 0.35
Omidec ES 40+30 Capsule (Daksh Pharma)$ 0.08
40 mg x 10's (Mankind)$ 0.37
Omipure 40mg FC-TAB / 10 (Mankind)$ 0.37
OMIPURE film-coated tab 40 mg x 10's (Mankind)$ 0.37
Omipure 40mg FC-TAB / 10 (Mankind)$ 0.37
OMIPURE FAST 40MG TABLET 1 strip / 10 tablets each (Mankind Pharma Ltd)$ 0.45
OMZEE-ES tab 40 mg x 10's (Zenon)
Omzol 20 mg x 1 Box (Synmedic Laboratories)
Omzol 20 mg Capsule (Synmedic Laboratories)$ 0.03
ONTO-ES tab 40 mg x 10's (Aronex)
Opec DSR 40+30 Tablet (Rhine Biogenics Pvt Ltd)$ 0.06
Peprazom delayed-release cap 20 mg 14's (Natrapharm)
Peprazom delayed-release cap 40 mg 14's (Natrapharm)
PIRAZOLE S 40 MG TABLET 1 strip / 10 tablets each (Abbott India Ltd)$ 0.53
PRAZONID-ES tab 40 mg x 10's (Nidus)$ 0.66
PREVZOLE 40MG TABLET 1 strip / 10 tablets each (Prevento Pharma)$ 1.14
RACIPER Capsule/ Tablet / 20mg / 10 units (Ranbaxy (Pharma))$ 0.32
RACIPER Capsule/ Tablet / 40mg / 10 units (Ranbaxy (Pharma))$ 0.58

References

  1. DailyMed. "ESOMEPRAZOLE STRONTIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. PubChem. "Esomeprazole". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
  3. DrugBank. "Esomeprazole". http://www.drugbank.ca/drugs/DB00736 (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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