Esomeprazole (esomeprazole) instructions
Common name: esomeprazole
Trade name: Nexium
All names: esomeprazole, Nexium, esomeprazole, Nexium
Indications:
1. This product is used for the treatment of gastroesophageal reflux disease (GERD), including the treatment of erosive reflux esophagitis, long-term maintenance treatment to prevent recurrence of cured esophagitis patients, and symptom control of gastroesophageal reflux disease (GERD).
2. This product can be used in combination with appropriate antibacterial therapy to eradicate Helicobacter pylori, heal duodenal ulcers related to Helicobacter pylori infection, and prevent the recurrence of peptic ulcers related to Helicobacter pylori infection.
Usage and dosage:
1. Treatment of erosive reflux esophagitis: 40 mg once a day for 4 weeks. For patients whose esophagitis is not cured or whose symptoms persist, a further 4 weeks of treatment is recommended.
2. Long-term maintenance treatment to prevent recurrence of cured esophagitis patients: 20 mg once a day.
3. Symptom control of GERD (gastroesophageal reflux disease): patients without esophagitis take 20 mg once a day. If symptoms are not controlled after 4 weeks of medication, the patient should undergo further examination. After the symptoms disappear, immediate therapy can be used (ie, 20 mg orally, once a day if necessary).
4. Combined antimicrobial therapy to eradicate Helicobacter pylori: Use a combined medication regimen of 20 mg of this drug once, 1 g of amoxicillin once, and 500 mg of clarithromycin once, twice a day for 7 days.
Tablets should be swallowed whole with liquid and should not be chewed or crushed.
For patients with difficulty swallowing, put it into boiled water until the tablet is completely disintegrated and take it within 30 minutes.
Adverse reactions:
>10%:
Central nervous system: headache (2%-11%)
1%-10%:
Central nervous system: irritability (infants: ≥5%), dizziness (intravenous injection: ≤3%; oral: < 1%), dizziness (intravenous injection: ≤3%), drowsiness (children: 2%; adults: <1%)
Dermatology: pruritus (intravenous injection: 1%; oral administration: <1%)
Endocrinology and metabolism: changes in thyroid hormone levels (increased thyroxine: ≤1%), decreased serum potassium (≤1%) , decreased serum sodium (≤1%), decreased thyroid hormone (decreased thyroxine: ≤1%), increased gastrin (≤1%), increased serum potassium (≤1%), increased serum sodium (≤1%), increased thyroid-stimulating hormone (≤1%), increased uric acid (≤1%)
Gastrointestinal tract: flatulence (static Intravenous injection: 10%; oral administration: ≥1%), diarrhea (2%-4%), abdominal pain (1%-6%), nausea (IV injection: 6%; oral administration: ≥1%-2%), vomiting (infants: 1% to ≥5%; adults: <1%), dry mouth (IV injection: 4%; oral administration: ≥1%), constipation (intravenous injection: 6%; oral administration: ≥1%-2%) Internal: 3%; Oral: ≥1%)
Hematology and Oncology: Platelet count disorders (≤1%)
Liver: Elevated serum alkaline phosphatase (≤1%), elevated serum alanine aminotransferase (≤1%), elevated serum aspartate aminotransferase (≤1%)
Local: Injection site reaction ( Intravenous: 2%-4%)
Renal: Elevated serum creatinine (≤1%)
Respiratory: Cough (Intravenous: 1%; Oral: <1%), tachypnea (Infants, Oral: 1%)
Others: Fever (Intravenous: 4%; Oral: <1%)
Undefined frequency :
Cardiovascular: Esophageal varices
Gastrointestinal: Barrett's esophagus, duodenitis, esophageal stricture, esophageal ulcer, esophagitis, gastritis, mucosal discoloration
Hematology and Oncology: Benign polyps
Other: Benign nodules
<1%:
Post-marketing or case reports : Acne vulgaris, acute interstitial nephritis, aggressive behavior, restlessness, agranulocytosis, proteinuria, alopecia, altered sense of smell, anaphylactic shock, allergic reaction, anemia, angioedema, anorexia, apathy, aphtha, joint pain, arthritis, fatigue, back pain, blurred vision, fractures, bronchospasm, candidiasis, etc.
Taboos:
Hypersensitivity reaction (e.g., anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, urticaria) to esomeprazole, other substituted benzimidazole proton pump inhibitors, or any component of the formulation; use with products containing rilpivirine.
Notes:
Carcinoma: There have been no reports of enterochromaffin-like (ECL) cell carcinoid tumors, dysplasia, or neoplasia.
Clostridium difficile-associated diarrhea (CDAD): Use of proton pump inhibitors (PPIs) may increase the risk of CDAD (Clostridium difficile-associated diarrhea), especially in hospitalized patients; patients with persistent diarrhea do not feel that a diagnosis of CDAD (Clostridium difficile-associated diarrhea) will improve. Use the lowest dose and shortest duration of PPI (proton pump inhibitor) therapy appropriate to treat the disease.
Cutaneous and Systemic Lupus Erythematosus: New onset or exacerbations of autoimmune diseases have been reported; most cases are cutaneous lupus erythematosus (CLE), most commonly subacute CLE (occurring within weeks to years after continued treatment). Systemic lupus erythematosus (SLE) is less common (usually occurring within days to years after starting treatment) and occurs primarily among young and older adults. If symptoms of CLE or SLE occur, stop treatment and seek evaluation by a specialist; most patients improve within 4 to 12 weeks after stopping treatment.
Fractures: Proton pump inhibitor (PPI) treatment can increase the incidence of osteoporosis-related fractures of the hip, spine, or wrist. Patients receiving high-dose or long-term therapy (≥1 year) should be monitored. Use the lowest effective dose for the shortest time, supplement with vitamin D and calcium, and follow appropriate guidelines to reduce the risk of fractures in high-risk patients.
Fundic gland polyps: Use of proton pump inhibitors (PPIs) increases the risk of fundic gland polyps, especially in patients with long-term use for more than 1 year. It may be asymptomatic, but nausea, vomiting, or abdominal pain may occur; gastrointestinal bleeding or anemia may occur with ulcerative polyps. A diagnosis of polyps may also increase the risk of small bowel obstruction. Use the lowest dose and shortest duration of PPI (proton pump inhibitor) therapy appropriate to treat the disease.
Gastrointestinal infections (eg, Salmonella, Campylobacter): Use of proton pump inhibitors may increase the risk of these infections.
Hypomagnesemia: Rarely reported, usually with long-term PPI (proton pump inhibitor) use for ≥3 months (most cases >1 year of treatment). It may be symptomatic or asymptomatic; severe cases may cause tetany, seizures, and irregular heartbeats. Consider obtaining serum magnesium concentrations before initiating long-term therapy, especially if digoxin, diuretics, or other drugs known to cause hypomagnesemia are concurrently administered and regularly thereafter. Hypomagnesemia can be corrected with magnesium supplementation and may require discontinuation of esomeprazole. Magnesium levels usually return to normal within 1 week after stopping the medication.
Interstitial Nephritis: Acute interstitial nephritis has been observed in patients taking PPIs (proton pump inhibitors); it may occur at any time during treatment, usually due to idiopathic hypersensitivity reactions. If acute interstitial nephritis occurs, treatment should be discontinued.
Vitamin B12 Deficiency: Long-term treatment ((≥2 years)) may lead to vitamin B12 malabsorption and subsequent vitamin B12 deficiency. The degree of deficiency is dose-related, with a stronger association in women and younger individuals (under 30 years); the prevalence decreases after discontinuation of treatment.
Storage:
Sealed , stored below 30°C.
Mechanism of action:
Esomeprazole is the S-isomer of omeprazole, which reduces gastric acid secretion through a specific targeting mechanism and is a specific inhibitor of proton pumps in parietal cells. The R-isomer and S-isomer of omeprazole have similar pharmacodynamic properties. Site and mechanism of action Esomeprazole is a weak base, which is concentrated in the high-acid environment of parietal cell acid secretion microtubules and converted into an active form, thus inhibiting the H+/K+-ATPase (proton pump) at this site and inhibiting both basic gastric acid secretion and stimulated gastric acid secretion.
Efficacy and safety: In a clinical comparative study of esomeprazole and omeprazole in the treatment of reflux esophagitis, the total effective rate of esomeprazole was 97.18%, which was significantly higher than 84.51% of omeprazole, and there was no significant difference in the incidence of adverse reactions. Chen Caiming conducted a cost-effectiveness analysis of omeprazole and esomeprazole in the treatment of duodenal ulcer. The recovery rate of the esomeprazole group was 92.6%, which was higher than that of omeprazole, 78.6%. The results proved that esomeprazole has cost and effectiveness advantages. Esomeprazole maintains gastric pH >4 for a longer period of time. A study on the duration of gastric pH > 4 and the healing rate of reflux esophagitis showed that the longer the duration of pH > 4 within 24 hours, the greater the number of patients who healed after 8 weeks. After taking different drugs orally for 5 days, the duration of pH>4 in the stomach within 24 hours from longest to shortest is: esomeprazole 40 mg, omeprazole 40 mg, lansoprazole 30 mg, pantoprazole 40 mg and rabeprazole 20 mg. This shows that esomeprazole 40mg has a stronger acid-suppressing effect than other proton pump inhibitors. Clinical trials have also fully confirmed the excellent pH control ability of esomeprazole 40mg. In general, esomeprazole is very effective in treating early gastric cancer.
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