Drug reference

Esomeprazole

Proton Pump Inhibitor · Antiulcer

Also known as Esomeprazole magnesium, Esomeprazole strontium, S-omeprazole

Proton Pump InhibitorAntiulcerATC A02BC05

CDSCO approvedJan AushadhiNPPA price-controlledATC A02BC05

Pharmacokineticsplasma · t hours

ONSET: 1h · Acid suppression effects begin within 1 hour; symptomatic relief typically observed within days.
PEAK: 1.8h · Plasma concentration peak at 1.5-2 hours.
t½: 1.3h · Approximately 1-1.5 hours.
DURATION: 1d · Up to 24 hours (due to irreversible proton pump inhibition).

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA Pregnancy Category B. Generally considered to have a low risk, but should be used during pregnancy only if clearly needed and the potential benefits outweigh the potential risks.

FDA category + note

Top interactionssee all 12 →

AcalabrutinibSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
CitalopramSevereDatabaseDDInter
ClopidogrelSevereDatabaseDDInter

Mechanism

Esomeprazole is the S-isomer of omeprazole. It functions as a proton pump inhibitor by irreversibly binding to and inhibiting the H+/K+-ATPase enzyme system in the secretory canaliculi of gastric parietal cells. This action blocks the final step in gastric acid production, leading to a potent and prolonged reduction in gastric acid secretion.

Indications

Gastroesophageal Reflux Disease (GERD)Healing of erosive esophagitisMaintenance of healing of erosive esophagitisSymptomatic GERDRisk reduction of NSAID-associated gastric ulcersHelicobacter pylori eradication (in combination with antibiotics)Pathological hypersecretory conditions including Zollinger-Ellison syndromePrevention of rebleeding of gastric ulcers following endoscopic therapy (IV formulation)Dyspepsia (off-label)heartburnGastric ulcersDuodenal ulcersErosive esophagitisGastroesophageal reflux diseaseHelicobacter pylori eradicationZollinger-Ellison syndromePathological hypersecretory conditionsReducing the risk of duodenal ulcer recurrence associated with H. pylori infectionsSelf-treatment of acid reflux (over-the-counter)Treatment of acute bleeding ulcers (off-label)Peptic ulcer (including anti-H. pylori therapy)

Dosing

Adult: GERD/Erosive Esophagitis: 20-40 mg once daily for 4-8 weeks. Maintenance: 20 mg once daily. H. pylori eradication: 20 mg twice daily for 7-14 days in combination with antibiotics. Zollinger-Ellison Syndrome: Initial 40 mg twice daily, adjust based on patient response; doses up to 240 mg/day have been used.
Pediatric: GERD (1-11 years, weighing ">= 10 kg"): 10-20 mg once daily. GERD (>= 12 years): 20-40 mg once daily.
Renal adjustment: No dose adjustment is necessary for patients with renal impairment.
Hepatic adjustment: For severe hepatic impairment (Child-Pugh Class C), limit dose to a maximum of 20 mg once daily. No adjustment needed for mild to moderate impairment.
Geriatric: No specific dose adjustment is needed based solely on age. However, consider potential polypharmacy and increased risk of long-term adverse effects like bone fractures and C. difficile infection.
Max dose: Generally 40 mg once daily for most indications; up to 240 mg/day for Zollinger-Ellison syndrome under specialist supervision.

Pharmacokinetics

Onset

Acid suppression effects begin within 1 hour; symptomatic relief typically observed within days.

Peak effect

Plasma concentration peak at 1.5-2 hours.

Duration

Up to 24 hours (due to irreversible proton pump inhibition).

Half-life

Approximately 1-1.5 hours.

Bioavailability

Approximately 64% (single 40 mg dose), increasing to 89% with repeated dosing.

Protein binding

Approximately 97%.

Metabolism

Extensively metabolized in the liver by the cytochrome P450 system, primarily via CYP2C19 and CYP3A4.

Excretion

Mainly renal (approx. 80%) and fecal (approx. 20%) as metabolites.

Contraindications

Hypersensitivity to esomeprazole, substituted benzimidazoles, or any component of the formulation.
Concomitant use with rilpivirine due to reduced absorption and potential for viral load increase.

Side effects

Common

HeadacheNauseaAbdominal painDiarrheaFlatulenceConstipationDry mouthLoose stoolsMuscle and joint painDizziness

Serious

Clostridium difficile-associated diarrhea
Bone fractures (with long-term use)
Acute interstitial nephritis
Hypomagnesemia (with long-term use)
Vitamin B12 deficiency (with long-term use)
Cutaneous and systemic lupus erythematosus
Fundic gland polyps (with long-term use)
Severe skin reactions (e.g., SJS, TEN)
Subacute myopathy
Arthralgias
Interstitial nephritis
Pharyngitis
Skin rashes
Increased risk of bone fracture
Increased susceptibility to hospital-acquired pneumonia
Increased susceptibility to community-acquired Clostridium difficile infection
Increased susceptibility to spontaneous bacterial peritonitis (in patients with ascites)
Hypomagnesemia
Vitamin B12 (cobalamin) deficiency (with long-term use, >3 years)
Hypergastrinemia leading to ECL hyperplasia and fundic gland polyposis
Atrophic gastritis
Rashes (1.5% incidence)
Leucopenia (infrequent)
Hepatic dysfunction (infrequent)
Atrophic gastritis (occasionally on prolonged treatment)
Gynaecomastia (on prolonged use)
Erectile dysfunction (on prolonged use)
Accelerated osteoporosis (among elderly patients with high-dose long-term use for GERD)

Pregnancy & lactation

Pregnancy

FDA Pregnancy Category B. Generally considered to have a low risk, but should be used during pregnancy only if clearly needed and the potential benefits outweigh the potential risks.

Lactation

Esomeprazole is excreted into breast milk in animal studies. Use with caution in nursing mothers, weighing potential benefits against risks to the infant.

Drug interactions

Acalabrutinib

Severe

Database

Drug interaction classified as: absorption

Source: DDInter

Atazanavir

Severe

Database

Substantially reduced atazanavir concentrations, leading to loss of antiviral effectiveness.

Proton pump inhibitors should be avoided in patients receiving atazanavir without ritonavir.

Source: DDInter

Citalopram

Severe

Database

Drug interaction classified as: metabolism.

Source: DDInter

Clopidogrel

Severe

Database

Reduced effectiveness of clopidogrel, potentially increasing cardiovascular risk.

Pantoprazole is less likely to result in this interaction. Concurrent use of clopidogrel and PPIs (mainly pantoprazole) significantly reduces GI bleeding without increasing adverse cardiac events.

Source: DDInter

Dacomitinib

Severe

Database

Clinical effect not specified

Source: DDInter

Dasatinib

Severe

Database

Clinical effect not specified

Source: DDInter

Erlotinib