Esomeprazole


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
NSAID-associated ulceration
Adult: For healing and prevention: 20 mg once daily via slow inj over at least 3 minutes or infusion over 10-30 minutes. Treatment duration: Up to 10 days. Switch to oral therapy as soon as possible.

Intravenous
Prophylaxis of rebleeding of duodenal ulcer, Prophylaxis of rebleeding of gastric ulcer
Adult: Prophylaxis of rebleeding following therapeutic endoscopy: 80 mg via infusion over 30 minutes, followed by 8 mg/hour continuous infusion for a total of 72 hours, then switch to oral therapy given as 40 mg once daily for 4 weeks.

Intravenous
Gastro-oesophageal reflux disease
Adult: Erosive reflux oesophagitis: 40 mg once daily. Symptomatic treatment: 20 mg once daily. Doses are given via slow inj over at least 3 minutes or infusion over 10-30 minutes. Treatment duration: Up to 10 days. Switch to oral therapy as soon as possible.
Child: 1-11 years Erosive reflux oesophagitis: <20 kg: 10 mg once daily; ≥20 kg: 10 mg or 20 mg once daily. Symptomatic treatment of GERD: 10 mg once daily. 12-18 years Same as adult dose. Doses are given via slow inj over at least 3 minutes or infusion over 10-30 minutes. Switch to oral therapy as soon as possible. Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).

Oral
NSAID-associated ulceration
Adult: 20 mg once daily for 4-8 weeks.

Oral
Prophylaxis of NSAID-induced ulcers
Adult: 20 mg or 40 mg once daily for up to 6 months.

Oral
Zollinger-Ellison syndrome
Adult: Initially, 40 mg bid, may be adjusted according to patient response or needs. Usual range: 80-160 mg daily; may be increased up to 240 mg daily if necessary. Daily doses of >80 mg should be given in 2 divided doses.

Oral
Eradication of H. pylori associated with peptic ulcer disease
Adult: As a component of triple therapy regimen with amoxicillin and clarithromycin: 20 mg bid for 7 days or 40 mg once daily for 10 days.
Child: ≥12 years ≥30 kg: As a component of triple therapy regimen with amoxicillin and clarithromycin: 20 mg bid for 7 days.

Oral
Gastro-oesophageal reflux disease
Adult: Erosive reflux oesophagitis: 20 mg or 40 mg once daily for 4-8 weeks, may extend for an additional 4-8 weeks if necessary. Maintenance (to prevent relapse of erosive oesophagitis): 20 mg once daily for up to 6 months. Symptomatic treatment of GERD (without oesophagitis): 20 mg once daily for 4 weeks, may extend for an additional 4 weeks if necessary.
Child: As granules for oral susp: 1 month to <1 year Erosive reflux oesophagitis: 3-5 kg: 2.5 mg once daily for up to 6 weeks; >5-7.5 kg: 5 mg once daily for up to 6 weeks; >7.5-12 kg: 10 mg once daily for up to 6 weeks. 1-11 years Erosive reflux oesophagitis: <20 kg: 10 mg once daily for 8 weeks; ≥20 kg: 10 mg or 20 mg once daily for 8 weeks. Symptomatic treatment of GERD: 10 mg once daily for up to 8 weeks. As tab, cap, or granules for oral susp: 12-17 years Erosive reflux oesophagitis: 20 mg or 40 mg once daily for 4-8 weeks. Symptomatic treatment of GERD (without oesophagitis): 20 mg once daily for 4 weeks.
Nhóm bệnh nhân đặc biệt
Pharmacogenomics:

Esomeprazole is metabolised by CYP2C19, a polymorphic enzyme, and to a lesser extent by CYP3A4 isoenzyme. Systemic exposure of esomeprazole varies with individual metabolism status. Approx 3% of Caucasians and 15-20% of Asians lack a functional CYP2C19 enzyme and are called poor metabolisers. In these individuals, esomeprazole is probably metabolised mainly by the CYP3A4 isoenzyme and exposure may be higher. However, studies suggest that this change in exposure is not considered clinically meaningful and dosage adjustment is not necessary.
Suy gan
Oral:
Severe (Child-Pugh class C): Max: 20 mg daily.

Intravenous:
Gastro-oesophageal reflux disease; NSAID-associated ulceration:
Severe (Child-Pugh class C): Max: 20 mg daily.
Prophylaxis of rebleeding of gastric ulcer; Prophylaxis of rebleeding of duodenal ulcer:
Mild to moderate (Child-Pugh class A or B): Initially, 80 mg via infusion over 30 minutes, followed by 6 mg/hour continuous infusion for a total of 72 hours. Severe (Child-Pugh class C): Initially, 80 mg via infusion over 30 minutes, followed by 4 mg/hour continuous infusion for a total of 72 hours.
Cách dùng
delayed-release cap: Should be taken on an empty stomach. Take 1 hr before meals.
tab: May be taken with or without food.
Hướng dẫn pha thuốc
Oral: Granules for oral suspension: Mix the contents of 2.5 mg or 5 mg packet with 5 mL water or the 10 mg, 20 mg, or 40 mg packet with 15 mL water. Stir the solution and leave for 2-3 minutes to thicken. IV: Slow inj: Reconstitute vial with 5 mL of 0.9% NaCl inj. IV infusion (10-30 minutes): Reconstitute vial with 5 mL of 0.9% NaCl, Lactated Ringer's solution, or 5% dextrose in water, then further dilute to reach a final volume of 50 mL or a concentration of 0.8 mg/mL. IV infusion (loading dose and continuous infusion): Reconstitute 2 vials labelled as 40 mg with 0.9% NaCl inj (5 mL each), then further dilute the resulting solution in 100 mL of 0.9% NaCl inj.
Chống chỉ định
Concomitant use with nelfinavir or rilpivirine.
Thận trọng
Patient with reduced body stores or risk factors for reduced vitamin B12 absorption, at risk of osteoporosis-related fractures. Hepatic and severe renal impairment. Children. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Hypomagnesaemia (prolonged use), osteoporosis-related fractures of the hip, wrist, and spine (particularly in high doses and prolonged use), may increase the risk of Clostridium difficile-associated diarrhoea or gastrointestinal infections (e.g. Salmonella, Campylobacter); fundic gland polyps, acute tubulointerstitial nephritis; vitamin B12 deficiency (prolonged use), subacute cutaneous lupus erythematosus (SCLE), SLE.
Blood and lymphatic system disorders: Rarely, leucopenia, thrombocytopenia.
Ear and labyrinth disorders: Vertigo.
Eye disorders: Rarely, blurred vision.
Gastrointestinal disorders: Nausea, vomiting, constipation, diarrhoea, abdominal pain, flatulence, dry mouth.
General disorders and administration site conditions: Inj site reactions (IV). Rarely, malaise, increased sweating.
Hepatobiliary disorders: Rarely, hepatitis with or without jaundice.
Immune system disorders: Rarely, hypersensitivity reactions (e.g. fever, angioedema, anaphylactic shock/reaction).
Investigations: Increased liver enzymes.
Metabolism and nutrition disorders: Peripheral oedema. Rarely, hyponatraemia.
Musculoskeletal and connective tissue disorders: Rarely, myalgia, arthralgia.
Nervous system disorders: Headache, dizziness, somnolence, paraesthesia.
Psychiatric disorders: Insomnia. Rarely, agitation, confusion, depression.
Reproductive system and breast disorders: Very rarely, gynaecomastia.
Respiratory, thoracic and mediastinal disorders: Rarely, bronchospasm.
Skin and subcutaneous tissue disorders: Dermatitis, pruritus, rash, urticaria. Rarely, alopecia, photosensitivity.
Potentially Fatal: Very rarely, severe cutaneous adverse reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms, acute generalised exanthematous pustulosis).
IV/Parenteral/PO: C
Chỉ số theo dõi
Obtain serum Mg (particularly when used with agents that may cause hypomagnesaemia) and Ca (in at risk-patients [e.g. hypoparathyroidism]) at baseline and periodically thereafter. Monitor for rebleeding in patients with peptic ulcer bleed. Consider further follow-up and diagnostic testing in patients with suboptimal response or early symptomatic relapse following completion of therapy. Rule out malignancy in case of any alarm symptoms (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, melaena or haematemesis).
Quá liều
Symptoms: Weakness, confusion, headache, drowsiness, blurred vision, tachycardia, diaphoresis, flushing, dry mouth, nausea and other gastrointestinal symptoms. Management: Symptomatic and supportive treatment.
Tương tác
May decrease the exposure and efficacy of atazanavir. May diminish the therapeutic effect of clopidogrel. Increased risk of hypomagnesaemia with digoxin or diuretics. May increase the serum concentrations of saquinavir, tacrolimus, methotrexate, cilostazol, and drugs metabolised by CYP2C19 (e.g. diazepam, citalopram, imipramine, phenytoin). May reduce the absorption of agents dependent on gastric pH for absorption (e.g. ketoconazole, itraconazole, Fe salts, erlotinib, dasatinib, mycophenolic acid). Concomitant use with warfarin may increase INR and prothrombin time. Esomeprazole serum levels may be decreased with CYP2C19 and/or CYP3A4 inducers (e.g. rifampicin) and increased with CYP3A4 inhibitors (e.g. clarithromycin) or combined inhibitors of CYP2C19 and CYP3A4 (e.g. voriconazole). May prolong the elimination half-life of cisapride.
Potentially Fatal: Decreases the serum levels of nelfinavir or rilpivirine which may lead to reduced antiviral effect and development of drug resistance.
Tương tác với thức ăn
May decrease serum concentrations with St. John's wort.
Ảnh hưởng đến kết quả xét nghiệm
May increase chromogranin A (CgA) levels and interfere with investigations for neuroendocrine tumours; discontinue treatment for at least 5 days before CgA measurements. May cause a hyper response in gastrin secretion with secretin stimulation test which may falsely suggest gastrinoma; discontinue 4 weeks before testing.
Tác dụng
Description: Esomeprazole, the S-isomer of omeprazole, is a substituted benzimidazole proton pump inhibitor (PPI) that blocks the final step in gastric acid secretion by specific inhibition of H+/K+-ATPase enzyme system present on the secretory surface of the gastric parietal cells.
Pharmacokinetics:
Absorption: Rapidly absorbed (oral). Bioavailability: Oral: 64% (single 40 mg dose); approx 90% (repeated 40 mg dose). Time to peak plasma concentrations: Approx 1-2 hours.
Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 97%.
Metabolism: Extensively metabolised in the liver primarily by CYP2C19 isoenzyme to form inactive hydroxy and desmethyl metabolites, and to a lesser extent by CYP3A4 isoenzyme to sulfone metabolite (main metabolite in plasma).
Excretion: Mainly via urine (approx 80% as inactive metabolites; <1% as unchanged drug); faeces (20%). Elimination half-life: Approx 1-1.5 hours.
Đặc tính

Chemical Structure Image
Esomeprazole

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9568614, Esomeprazole. https://pubchem.ncbi.nlm.nih.gov/compound/Esomeprazole. Accessed Oct. 26, 2022.

Bảo quản
Store between 15-30°C. Protect from light and moisture. Storage recommendations may vary between products. Refer to specific product guidelines.
Phân loại MIMS
Thuốc kháng acid, chống trào ngược & chống loét
Phân loại ATC
A02BC05 - esomeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Tài liệu tham khảo
Anon. Esomeprazole. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/08/2022.

Buckingham R (ed). Esomeprazole. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2022.

Esomeprazole 20 mg Gastro-resistant Capsules, Hard (Ethypharm). MHRA. https://products.mhra.gov.uk. Accessed 02/08/2022.

Joint Formulary Committee. Esomeprazole. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/08/2022.

Nexium 20 mg Gastro-resistant Tablets (AstraZeneca UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/08/2022.

Nexium 24HR Tablet (GlaxoSmithKline Consumer Healthcare Holdings [US] LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/08/2022.

Nexium 40 mg Powder for Solution for Injection/Infusion (AstraZeneca Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/08/2022.

Nexium Capsule, Delayed Release; Granule, Delayed Release (AstraZeneca Pharmaceuticals LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/08/2022.

Nexium I.V. 40 mg Powder for Solution for Injection/Infusion (AstraZeneca UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/08/2022.

Nexium I.V. Injection (AstraZeneca Pharmaceuticals LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/08/2022.

Nexium MUPS Delayed-release Tablets 20 mg and 40 mg (AstraZeneca Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/08/2022.

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