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Esomeprazole(一)
2013-07-23 18:16:48 来源: 作者: 【 】 浏览:1808次 评论:0

See Available Brands of Esomeprazole in India
P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
LI - Lab *

Esomeprazole is a proton pump inhibitor (brand names Sompraz, Zoleri, Nexium®, Lucen, Esopral; Axagon in Italy, Nexiam in Belgium) developed and marketed by AstraZeneca which is used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. Esomeprazole is the S-enantiomer of omeprazole (marketed as Losec/Prilosec), and AstraZeneca claims improved efficacy of this single enantiomer product over the racemic mixture of omeprazole.

Pharmacodynamics

Pharmacokinetics

Esomeprazole is a PPI that suppresses gastric acid secretion by specific inhibition of the H+/K+ ATPase in the gastric parietal cell.
Absorption
Rapid (oral). Peak plasma levels after 1-2 hours; food delays and decreases absorption.

Distribution
Protein-binding: 97%

Metabolism
Extensively hepatic; converted to hydroxy and desmethyl metabolites.

Excretion
Urine (as metabolites); 1.3 hours (elimination half-life).

Esomeprazole Indications / Esomeprazole Uses

Information Not Available

Esomeprazole Adverse Reactions / Esomeprazole Side Effects

Headache, diarrhoea, abdominal pain, nausea, flatulence, dry mouth, constipation, hyponatraemia, photosensitivity, angioedema, anaphylaxis.

Precautions

Hypersensitivity

May occur; angioedema and anaphylactic reaction/shock have been reported.

Atrophic gastritis
Has been reported in patients receiving long-term treatment with omeprazole, of which esomeprazole is an enantiomer.

Overdosage
Symptoms
Blurred vision, confusion, diaphoresis, drowsiness, dry mouth, flushing, headache, nausea, tachycardia.

Special Precautions

Paediatric; pregnancy, lactation. Malignancy and hepatic impairment. Increased risk of developing certain infections such as community-acquired pneumonia.

Other Drug Interactions

May interfere with the elimination of drugs metabolised by CYP2C19. Changes in gastric pH can affect the bioavailability of ketoconazole and Fe salts. Clarithromycin and amoxicillin may increase plasma level. May cause changes to prothrombin time when used with warfarin.

Other Interactions

Food Interaction
Absorption delayed with food.

Dosage

Oral
Erosive oesophagitis
Adult: 40 mg once daily for 4 wk, extended for another 4 wk if necessary. Maintenance: 20 mg once daily.
Child: <20 kg: 10 mg once daily for 8 wk; ≥20 kg: 10-20 mg once daily for 8 wk.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Peptic ulcer
Adult: 20 mg bid for 7 days or 40 mg once daily for 10 days given as a triple therapy with amoxicillin and clarithromycin.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
NSAID-associated ulceration
Adult: 20 mg once daily for 4-8 wk.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Zollinger-Ellison syndrome
Adult: Initially, 40 mg twice daily. Usual range: 80-160 mg daily. Doses >80 mg should be given in 2 divided doses.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Gastro-oe

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