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Esomeprazole

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(British Approved Name, rINN)

Esomeprazole Magnesium

Drug Approvals

(BANM, US Adopted Name, rINNM)

Synonyms: Esomeprazol magnésico; H199/18 (esomeprazole); Perprazole (esomeprazole)
BAN: Esomeprazole Magnesium [BANM]
USAN: Esomeprazole Magnesium
INN: Esomeprazole Magnesium [rINNM (en)]
INN: Esomeprazol magnésico [rINNM (es)]
INN: Ésoméprazole Magnesique [rINNM (fr)]
INN: Magnesii Esomeprazolum [rINNM (la)]
INN: Магния Езомепразол [rINNM (ru)]
Chemical name: 5-Methoxy-2-{(S)-[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}benzimidazole magnesium (2:1) trihydrate
Molecular formula: C34H36MgN6O6S2,3H2O =767.2
CAS: 119141-88-7 (esomeprazole); 217087-09-7 (esomeprazole magnesium)
ATC code: A02BC05

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Esomeprazole Magnesium). A white to slightly coloured powder. Slightly soluble in water soluble in methyl alcohol practically insoluble in heptane. Store in airtight containers. Protect from light.

Esomeprazole Sodium

Drug Approvals

(BANM, US Adopted Name, rINNM)

BAN: Esomeprazole Sodium [BANM]
USAN: Esomeprazole Sodium
INN: Esomeprazole Sodium [rINNM (en)]
INN: Esomeprazol sódico [rINNM (es)]
INN: Ésoméprazole Sodique [rINNM (fr)]
INN: Natrii Esomeprazolum [rINNM (la)]
INN: Натрий Езомепразол [rINNM (ru)]
Molecular formula: C17H19N3NaO3S =368.4
CAS: 161796-78-7
ATC code: A02BC05

Adverse Effects and Precautions

As for Omeprazole.

Effects on the cardiovascular system. For discussion of cardiac effects ostensibly seen with esomeprazole, see under Omeprazole.

Effects on the kidneys. For reports of interstitial nephritis associated with esomeprazole see site.

Effects on the skin. For mention of exacerbation ofvitiligo with esomeprazole.

Fever. For a report of hyperpyrexia associated with esomeprazole, see under Omeprazole.

Interactions

As for Omeprazole.

Pharmacokinetics

Esomeprazole is rapidly absorbed after oral doses, with peak plasma levels occurring after about 1 to 2 hours. It is acid labile and an enteric-coated formulation has been developed. Bioavailability of esomeprazole increases with both dose and repeated administration to about 68 and 89% for doses of 20 and 40 mg respectively. Food delays and decreases the absorption of esomeprazole, but this does not significantly change its effect on intragastric acidity. Esomeprazole is about 97% bound to plasma proteins. It is extensively metabolised in the liver by the cytochrome P450 isoenzyme CYP2C19 to hydroxy and desmethyl metabolites, which have no effect on gastric acid secretion. The remainder is metabolised by the cytochrome P450 isoenzyme CYP3A4 to esomeprazole 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 is about 1.3 hours. Almost 80% of an oral dose is eliminated as metabolites in the urine, the remainder in the faeces.

Metabolism. As for omeprazole, the cytochrome P450 isoenzyme CYP2C19 is involved in the metabolism of esomeprazole, and individuals who are deficient in this enzyme are poor metabolisers of esomeprazole. However, there is some suggestion that the metabolism of esomeprazole is less dependent on this genotype, as there may be a metabolic shift towards the CYP3A4-medrated pathway

Uses and Administration

Esomeprazole is the S-isomer of the proton pump inhibitor omeprazole and is used similarly in the treatment of peptic ulcer disease and NSAID-associated ulceration, in gastro-oesophageal reflux disease, and the Zollinger-Ellison syndrome. It is given as the magnesium or sodium salt but doses are calculated in terms of esomeprazole. Esomeprazole magnesium 22.2 mg and esomeprazole sodium 21.3 mg are each equivalent to about 20 mg of esomeprazole.

Usual doses for peptic ulcer disease, as a component of a triple therapy regimen with amoxicillin and clari-thromycin, are the equivalent of 20 mg esomeprazole orally twice daily for 7 days, or 40 mg once daily for 10 days.

Oral doses of 20 mg daily, for 4 to 8 weeks, are used in the treatment of NSAID-associated ulceration a dose of 20 mg daily may also be used for prophylaxis in patients at risk of such lesions who require continued NSAID treatment.

In the UK, the dose for treatment of severe (erosive) gastro-oesophageal reflux disease is 40 mg once daily for 4 weeks, extended for a further 4 weeks if necessary in the USA, where doses of 20 or 40 mg daily are permitted for initial treatment, a further 4 to 8 weeks of treatment may be considered for patients who do not heal after 4 to 8 weeks. For maintenance, or for symptomatic disease without erosive oesophagitis, doses equivalent to 20 mg of esomeprazole daily may be used in both countries.

For the treatment of Zollinger-Ellison syndrome, the recommended initial oral dose of esomeprazole is 40 mg twice daily, which is then adjusted as needed. The majority of patients can be controlled on doses between 80 and 160 mg daily, although doses of 240 mg have been given. Doses above 80 mg daily should be given in 2 divided doses.

PARENTERAL DOSAGE.

Similar doses to the above may be given intravenously for gastro-oesophageal reflux disease and NSAID-associated ulceration. Esomeprazole is given as the sodium salt by slow intravenous injection over at least 3 minutes or by intravenous infusion over 10 to 30 minutes.

Doses of esomeprazole may need to be reduced in patients with hepatic impairment (see below).

Administration. In-vitro studies found that almost the entire contents of an esomeprazole capsule is deliverable through small calibre and standard sizes of nasogastric and gastrostomy tubes.

Administration in children. UK licensed product information allows for the use of adult doses of esomeprazole (see Uses and Administration, above) in children over 12 years. In the USA licensed doses, which may be given once daily for up to 8 weeks for the treatment of gastro-oesophageal reflux in children, are:

• 1 to 11 years: 10 mg

• 12 to 17years: 20 or 40 mg

For healing erosive oesophagitis in children, the following doses based on body-weight are licensed in the USA to be given once daily for up to 8 weeks:

• less than 20 kg: 10 mg

• 20 kg or over: 10 or 20 mg

Administration in hepatic impairment. No dosage adjustment of esomeprazole is considered necessary for patients with mild to moderate hepatic impairment (Child-Pugh Classes A and B, respectively). For patients with severe hepatic impairment (Child-Pugh Class C), a daily dose of 20 mg should not be exceeded.

Administration in renal impairment. Although no dosage adjustment is considered necessary in patients with renal impairment, UK licensed product information advises caution in those with severe renal impairment, as experience in these patients is limited.

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