Esomeprazole

Transcription

Esomeprazole
14/5/2015
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Esomeprazole
MARTINDALE ­ The Complete Drug Reference
See also Gastrointestinal Drugs
Esomeprazole
Physical And Pharmaceutical Properties
Name Status:BAN, rINN
Synonyms: Esomepratsoli;Esomeprazol;Ésoméprazole;Esomeprazolum;H­
199/18;Perprazole
Chemical Name: 5­Methoxy­2­{(S)­[(4­methoxy­3,5­dimethyl­2­
pyridyl)methyl]sulfinyl}benzimidazole
Molecular Formula: C17H19N3O3S
Molecular Weight:345.4
CAS Registry: 119141­88­7
ATC:A02BC05
Proprietary Names
Adikan (Rossmore, Arg.) ,Cor (Prater, Chile) ,Cucid­ES (Cubit, India) ,Es­Care (Zee,
India) ,Esocool (PC India, India) ,Es­OD (Piramal, India) ,Esofag (Micro, India) ,Esofag­D
(Micro, India) ,Esoflo (Intra­Labs, India) ,Esomax (Eurofarma, Arg.) ,Esomep (InnoGen,
Philipp.) ,Esomepra (Sidus, Arg.) ,Esonexa (Farmak, Ukr.) ,Esorest (Centaur, India)
,Esoriv (East African, India) ,Esotrax (Cadila, India) ,Esoxium (Cipla, Ukr.) ,Esoz
(Galeno, Venez.) ,Esoz (Glenmark, India) ,Esoz­D (Glenmark, India) ,Espra (Zydus,
India) ,Ezolong (Synmedic, Ukr.) ,Ezoran (Ranbaxy, Ital.) ,Izra (Unichem, India) ,Izra­D
(Unichem, India) ,Neksium (AstraZeneca, India) ,Neoren (Medipharm, Chile) ,Nepramel
(Clonmel, Irl.) ,Nexium (AstraZeneca, Philipp.) ,Nexium (AstraZeneca, Singapore)
,Nexium (AstraZeneca, Venez.) ,Nexomep (Sandoz, Turk.) ,Nexpro (Torrent, India)
,Nexpro­RD (Torrent, India) ,Nexstep (Mentis, Turk.) ,Nuloc (Alkem, India) ,Omidec­ES
(Daksh, India) ,Omipure (Mankind, India) ,Sompraz (Sun, India) ,Ulsan (Maver, Chile)
,Vimovo (AstraZeneca, Ital.) ,Zomel (Saval, Chile)
Esomeprazole Magnesium
Physical And Pharmaceutical Properties
Name Status:BANM, USAN, rINNM
Synonyms: Esomeprazol magnésico;Ésoméprazole magnésique;Ésoméprazole
Magnesique;Esomeprazolum magnesicum;Magnesii Esomeprazolum
Molecular Formula: C34H36MgN6O6S2,3H2O
Molecular Weight:767.2
CAS Registry: 217087­09­7
Pharmacopoeias:In Eur. (see About Martindale) and US.
Ph. Eur. 8 (Esomeprazole Magnesium Dihydrate). A white or slightly coloured, slightly
hygroscopic powder. It shows polymorphism. Slightly soluble in water; soluble in methyl
alcohol; practically insoluble in heptane. Store in airtight containers. Protect from light.
Ph. Eur. 8 (Esomeprazole Magnesium Trihydrate). A white or slightly coloured, slightly
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hygroscopic powder. Slightly soluble in water; soluble in methyl alcohol; practically
insoluble in heptane. Store in airtight containers. Protect from light.
USP 36 (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.
ATC:A02BC05
Proprietary Names
Aspaxa (AstraZeneca, Belg.) ,Aspaxa (AstraZeneca, Hung.) ,Axagon (Simesa, Ital.)
,Axanum (AstraZeneca, Cz.) ,Axanum (AstraZeneca, Ger.) ,Axanum (AstraZeneca,
Mex.) ,Axanum (AstraZeneca, Neth.) ,Axanum (AstraZeneca, Norw.) ,Axanum
(AstraZeneca, Switz.) ,Axiago (Beta, Spain) ,Ceso (Comed, India) ,Cronopep
(Biotoscana, Chile) ,Emanera (KRKA, Cz.) ,Emanera (KRKA, Denm.) ,Emanera (KRKA,
Pol.) ,Emazole (Rowex, Irl.) ,Emezol (Andromaco, Chile) ,Emozul (Consilient, UK)
,Emozul (KRKA, Cz.) ,Emozul (KRKA, Hung.) ,Emprozal (1A, Denm.) ,Epral
(Laboratorios Chile, Chile) ,Eprasol (Hexal, Denm.) ,Escadra (KRKA, Denm.) ,Esobax
(Ranbaxy, Neth.) ,Esodec (KRKA, Denm.) ,Esogasec (Aristo, Cz.) ,Esogastrosedol
(Nova Argentia, Arg.) ,Esolen (Torrent, Port.) ,Esomac (Cipla, India) ,Esomel (KRKA,
Denm.) ,Esomep (AstraZeneca, Switz.) ,Esomeprazole Magnesium Delayed­Release
Capsules USP 36,Esompro (Sandoz, Denm.) ,Esomylan (Generics, Cz.) ,Esopral
(Bracco, Ital.) ,Esopral (Euro Registratie, Neth.) ,Esopral (Farmagon, Norw.) ,Esopral
(Orifarm, Denm.) ,Esoprazol (Bago, Arg.) ,Esotar (KRKA, Denm.) ,Esovip (Celtis, Turk.)
,Esoxium Combi (Cipla, Ukr.) ,Espeyen (Specifar, Ital.) ,Essec (KRKA, Denm.) ,Estab
(Indoco, India) ,Eudresc (KRKA, Denm.) ,Exicross (Biocross, Chile) ,Ezoclip (Ranbaxy,
Port.) ,Ezolemito (Mithridatum, Port.) ,Ezolodisa (Mithridatum, Port.) ,Ezoret (KRKA,
Denm.) ,Helides (Zentiva, Cz.) ,Helides (Zentiva, Pol.) ,Hydresc (KRKA, Denm.) ,Ignis
(Alembic, India) ,Inexium (2care4, Denm. ; Europharma, Denm.) ,Inexium (AstraZeneca,
Fr.) ,Inexium (Farmagon, Norw.) ,Lucen (Malesci, Ital.) ,Mesopral (Polpharma, Cz.)
,Moproc (Ethypharm, Cz.) ,Neutraflux (Stedman, India) ,Nexiam (AstraZeneca, Belg.)
,Nexiam (AstraZeneca, S.Afr.) ,Nexium (AstraZeneca, Arg.) ,Nexium (AstraZeneca,
Austral.) ,Nexium (AstraZeneca, Austria) ,Nexium (AstraZeneca, Braz.) ,Nexium
(AstraZeneca, Canad.) ,Nexium (AstraZeneca, Chile) ,Nexium (AstraZeneca, China)
,Nexium (AstraZeneca, Cz.) ,Nexium (AstraZeneca, Denm.) ,Nexium (AstraZeneca, Fin.)
,Nexium (AstraZeneca, Ger.) ,Nexium (AstraZeneca, Gr.) ,Nexium (AstraZeneca, Hong
Kong) ,Nexium (AstraZeneca, Hung.) ,Nexium (AstraZeneca, Indon.) ,Nexium
(AstraZeneca, Irl.) ,Nexium (AstraZeneca, Israel) ,Nexium (AstraZeneca, Ital.) ,Nexium
(AstraZeneca, Jpn) ,Nexium (AstraZeneca, Malaysia) ,Nexium (AstraZeneca, Mex.)
,Nexium (AstraZeneca, Neth.) ,Nexium (AstraZeneca, Norw.) ,Nexium (AstraZeneca,
Pol.) ,Nexium (AstraZeneca, Port.) ,Nexium (AstraZeneca, Rus.) ,Nexium (AstraZeneca,
Spain) ,Nexium (AstraZeneca, Swed.) ,Nexium (AstraZeneca, Switz.) ,Nexium
(AstraZeneca, Thai.) ,Nexium (AstraZeneca, Turk.) ,Nexium (AstraZeneca, UK) ,Nexium
(AstraZeneca, Ukr.) ,Nexium (AstraZeneca, USA) ,Nexium 1­2­3 A (AstraZeneca,
Canad.) ,Nexium Hp (AstraZeneca, Austral.) ,Nexium Hp (AstraZeneca, Swed.) ,Nexpro
(Torrent, India) ,Nexpro­RD (Torrent, India) ,Omyprex (Teva, Hung.) ,Prazectol (Zentiva,
Cz.) ,Raciper (Ranbaxy, Hung.) ,Setarcos (Generis, Port.) ,Slodra (KRKA, Denm.)
,Tausolex (Mepha, Port.) ,Ulcratex (Recalcine, Chile) ,Ultrex (Beta, Arg.) ,Vimovo
(AstraZeneca, Arg.) ,Vimovo (AstraZeneca, Austral.) ,Vimovo (AstraZeneca, Belg.)
,Vimovo (AstraZeneca, Canad.) ,Vimovo (AstraZeneca, Chile) ,Vimovo (AstraZeneca,
Cz.) ,Vimovo (AstraZeneca, Denm.) ,Vimovo (AstraZeneca, Fin.) ,Vimovo (AstraZeneca,
Hung.) ,Vimovo (AstraZeneca, Irl.) ,Vimovo (AstraZeneca, Israel) ,Vimovo (AstraZeneca,
Malaysia) ,Vimovo (AstraZeneca, Mex.) ,Vimovo (AstraZeneca, Neth.) ,Vimovo
(AstraZeneca, Norw.) ,Vimovo (AstraZeneca, NZ) ,Vimovo (AstraZeneca, Port.) ,Vimovo
(AstraZeneca, Singapore) ,Vimovo (AstraZeneca, Spain) ,Vimovo (AstraZeneca, Swed.)
,Vimovo (AstraZeneca, Switz.) ,Vimovo (AstraZeneca, UK) ,Vimovo (Horizon, USA)
,Zivand (Generis, Port.) ,Zolex (Regiomedica, Neth.) ,Zomel HP (Saval, Chile)
Esomeprazole Potassium
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Physical And Pharmaceutical Properties
Name Status:BANM, USAN, rINNM
Synonyms: Esomeprazol potásico;Ésoméprazole Potassique;Kalii Esomeprazolum
Molecular Formula: C17H18KN3O3S
Molecular Weight:383.5
CAS Registry: 161796­84­5
ATC:A02BC05
Esomeprazole Sodium
Physical And Pharmaceutical Properties
Name Status:BANM, USAN, rINNM
Synonyms: Esomeprazol sódico;Ésoméprazole Sodique;Natrii Esomeprazolum
Molecular Formula: C17H19N3NaO3S
Molecular Weight:368.4
CAS Registry: 161796­78­7
ATC:A02BC05
Proprietary Names
Axagon (Simesa, Ital.) ,Demoel (Bluelife, Port.) ,Esmara (Dincsa, Turk.) ,Esomep
(AstraZeneca, Switz.) ,Esoz (Glenmark, India) ,Lucen (Malesci, Ital.) ,Nexium
(AstraZeneca, Arg.) ,Nexium (AstraZeneca, Austral.) ,Nexium (AstraZeneca, Austria)
,Nexium (AstraZeneca, Braz.) ,Nexium (AstraZeneca, Chile) ,Nexium (AstraZeneca,
China) ,Nexium (AstraZeneca, Denm.) ,Nexium (AstraZeneca, Fin.) ,Nexium
(AstraZeneca, Ger.) ,Nexium (AstraZeneca, Hong Kong) ,Nexium (AstraZeneca, Indon.)
,Nexium (AstraZeneca, Irl.) ,Nexium (AstraZeneca, Israel) ,Nexium (AstraZeneca, Ital.)
,Nexium (AstraZeneca, Mex.) ,Nexium (AstraZeneca, Neth.) ,Nexium (AstraZeneca,
Norw.) ,Nexium (AstraZeneca, Pol.) ,Nexium (AstraZeneca, Port.) ,Nexium
(AstraZeneca, Singapore) ,Nexium (AstraZeneca, Spain) ,Nexium (AstraZeneca, Swed.)
,Nexium (AstraZeneca, Switz.) ,Nexium (AstraZeneca, Thai.) ,Nexium (AstraZeneca,
Turk.) ,Nexium (AstraZeneca, UK) ,Nexium (AstraZeneca, Ukr.) ,Nexium (AstraZeneca,
USA) ,Nexium (AstraZeneca, Venez.)
Esomeprazole Strontium
Physical And Pharmaceutical Properties
Name Status:USAN, rINNM
Synonyms: Esomeprazol estroncio;Ésoméprazole Strontium;FM­0F67
Molecular Formula: (C17H18N3O3S)2Sr,4H2O
Molecular Weight:848.5
CAS Registry: 934714­36­0
Adverse Effects and Precautions
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As for Omeprazole, Omeprazole Sodium. (Last reviewed: 2013­10­11; last modified: 2013­10­
17)
General references. (Last reviewed: 2013­10­11; last modified: 2013­10­17)
1. Davies M, et al. Safety profile of esomeprazole: results of a prescription­event monitoring
study of 11 595 patients in England. Drug Safety 2008; 31: 313­23. (PubMed id:18366242)
­­ Effects on the cardiovascular system.
For discussion of cardiac effects ostensibly seen with esomeprazole, see under
Omeprazole, Omeprazole Sodium. (Last reviewed: 2013­10­11; last modified: 2013­10­
17)
­­ Effects on the kidneys.
For reports of interstitial nephritis associated with esomeprazole see Omeprazole
Sodium. (Last reviewed: 2013­10­11; last modified: 2013­10­17)
­­ Effects on the skin.
For mention of exacerbation of vitiligo with esomeprazole, see Omeprazole Sodium.
(Last reviewed: 2013­10­11; last modified: 2013­10­17)
­­ Fever.
For a report of hyperpyrexia associated with esomeprazole, see Omeprazole Sodium.
(Last reviewed: 2013­10­11; last modified: 2013­10­17)
­­ Porphyria.
The Drug Database for Acute Porphyria, compiled by the Norwegian Porphyria Centre
(NAPOS) and the Porphyria Centre Sweden, classifies esomeprazole as possibly
porphyrinogenic; it should be used only when no safer alternative is available and
precautions should be considered in vulnerable patients.1 (Last reviewed: 2013­10­11;
last modified: 2013­10­17)
1. The Drug Database for Acute Porphyria. Available at: http://www.drugs­porphyria.org
(accessed 03/10/11)
Interactions
As for Omeprazole, Omeprazole Sodium. (Last reviewed: 2013­10­11; last modified: 2013­10­
17)
References. (Last reviewed: 2013­10­11; last modified: 2013­10­17)
1. Andersson T, et al. Drug interaction studies with esomeprazole, the (S)­isomer of
omeprazole. Clin Pharmacokinet 2001; 40: 523­37. (PubMed id:11510629)
Pharmacokinetics
Esomeprazole is rapidly absorbed after oral doses and peak plasma levels occur after about 1
to 2 hours. It is acid labile and an enteric­coated formulation has been developed.
Bioavailability of esomeprazole increases on repeated dosage 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%
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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 first­pass 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 half­life is about 1.3
hours. Almost 80% of an oral dose is eliminated as metabolites in the urine, the remainder in
the faeces. (Last reviewed: 2013­10­11; last modified: 2013­10­17)
References. (Last reviewed: 2013­10­11; last modified: 2013­10­17)
1. Andersson T, et al. Pharmacokinetic studies with esomeprazole, the (S)­isomer of
omeprazole. Clin Pharmacokinet 2001; 40: 411­26. (PubMed id:11475467)
2. Sostek MB, et al. Effect of timing of dosing in relation to food intake on the pharmacokinetics
of esomeprazole. Br J Clin Pharmacol 2007; 64: 386­90. (PubMed id:17425628)
­­ Metabolism.
As for omeprazole (Omeprazole Sodium), 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 CYP3A4­mediated pathway.1 (Last reviewed: 2013­10­11;
last modified: 2013­10­17)
1. Schwab M, et al. Esomeprazole­induced healing of gastroesophageal reflux disease is
unrelated to the genotype of CYP2C19: evidence from clinical and pharmacokinetic data.
Clin Pharmacol Ther 2005; 78: 627­34. (PubMed id:16338278)
Uses and Administration
Esomeprazole is the S­isomer of the proton pump inhibitor omeprazole (Omeprazole Sodium)
and is used similarly in the treatment of peptic ulcer disease and NSAID­associated ulceration
(Gastrointestinal Drugs), in gastro­oesophageal reflux disease (Gastrointestinal Drugs), and
the Zollinger­Ellison syndrome (Gastrointestinal Drugs). It is given as the magnesium, sodium,
or strontium salts but doses are calculated in terms of esomeprazole. Esomeprazole
magnesium 22.2 mg, esomeprazole sodium 21.3 mg, and esomeprazole strontium 24.7 mg
are each equivalent to about 20 mg of esomeprazole.
Usual oral doses in peptic ulcer disease, for Helicobacter pylori eradication as a component of
a triple therapy regimen with amoxicillin and clarithromycin, are the equivalent of 20 mg
esomeprazole 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 NSAID­associated
ulceration; a dose of 20 or 40 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) gastro­oesophageal 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 Zollinger­Ellison 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 daily doses of 240 mg
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have been given. Doses above 80 mg daily should be given in 2 divided doses. For doses in
children, see Esomeprazole Strontium.
PARENTERAL DOSAGE.
Similar doses to the above may be given intravenously for gastro­oesophageal reflux disease
and NSAID­associated 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.
For the prevention of rebleeding of gastric and duodenal ulcers after therapeutic endoscopy,
80 mg esomeprazole can be given as an intravenous infusion over 30 minutes, followed by a
continuous intravenous infusion of 8 mg/hour over 72 hours. This parenteral treatment period
is then followed by oral therapy; 40 mg is given once daily for 4 weeks.
Doses of esomeprazole may need to be reduced in patients with hepatic impairment (see
Esomeprazole Strontium). (Last reviewed: 2013­10­11; last modified: 2013­10­31)
References. (Last reviewed: 2013­10­11; last modified: 2013­10­23)
1. Maton PN, et al. Safety and efficacy of long term esomeprazole therapy in patients with
healed erosive oesophagitis. Drug Safety 2001; 24: 625­35. (PubMed id:11480494)
2. Keating GM, Figgitt DP. Intravenous esomeprazole. Drugs 2004; 64: 875­82. (PubMed
id:15059043)
3. Metz DC, et al. Comparison of the effects of intravenously and orally administered
esomeprazole on acid output in patients with symptoms of gastro­oesophageal reflux disease.
Aliment Pharmacol Ther 2005; 22: 813­21. (PubMed id:16225490)
4. Edwards SJ, et al. Systematic review: proton pump inhibitors (PPIs) for the healing of reflux
oesophagitis ­ a comparison of esomeprazole with other PPIs. Aliment Pharmacol Ther 2006;
24: 743­50. (PubMed id:16918878)
5. Morgner A, et al. Esomeprazole: prevention and treatment of NSAID­induced symptoms and
ulcers. Expert Opin Pharmacother 2007; 8: 975­88. (PubMed id:17472543)
6. Blandizzi C, et al. Clinical efficacy of esomeprazole in the prevention and healing of
gastrointestinal toxicity associated with NSAIDs in elderly patients. Drugs Aging 2008; 25: 197­
208. (PubMed id:18331072)
7. McKeage K, et al. Esomeprazole: a review of its use in the management of gastric acid­
related diseases in adults. Drugs 2008; 68: 1571­1607. (PubMed id:18627213)
8. Sung JJY, et al. Peptic Ulcer Bleed Study Group. Intravenous esomeprazole for prevention
of recurrent peptic ulcer bleeding: a randomized trial. Ann Intern Med 2009; 150: 455­64.
(PubMed id:19221370)
­­ Administration.
In­vitro studies found that almost the entire contents of an esomeprazole capsule is
deliverable through small calibre and standard sizes of nasogastric and gastrostomy
tubes.1,2 (Last reviewed: 2013­10­11; last modified: 2013­10­17)
1. White CM, et al. Delivery of esomeprazole magnesium enteric­coated pellets through
small caliber and standard nasogastric tubes and gastrostomy tubes in vitro. Am J
Health­Syst Pharm 2002; 59: 2085­8. (PubMed id:12434721)
2. Shah SA, et al. Delivery of esomeprazole magnesium through nasogastric and
gastrostomy tubes using an oral liquid vehicle as a suspending agent in vitro. Am J
Health­Syst Pharm 2006; 63: 1882­7. (PubMed id:16990636)
­­ Administration in children.
Esomeprazole is given orally to children for the treatment of gastro­oesophageal reflux
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disease and erosive oesophagitis,1,2 and for duodenal ulcers caused by Helicobacter
pylori.
For gastro­oesophageal reflux disease, children aged from 1 to 11 years and weighing
10 kg and over are given 10 mg once daily for up to 8 weeks.
In erosive oesophagitis, doses are based on body­weight and given once daily for 8
weeks:
10 kg up to 20 kg: 10 mg
≥ 20 kg: 10 or 20 mg
For the eradication of H. pylori in duodenal ulceration in children over 4 years of age,
oral esomeprazole is given with amoxicillin and clarithromycin for 1 week; doses are
according to weight:
< 30 kg: 10 mg twice daily
≥ 30 kg: 20 mg twice daily
Regardless of indication, children from 12 years of age may be given adult doses, see
Esomeprazole Strontium.
For doses in children with hepatic impairment, see Esomeprazole Strontium.
Esomeprazole is unlicensed in children under 1 year of age; however, a pharmacokinetic
study in preterm and term neonates with gastro­oesophageal reflux disease found oral
esomeprazole 500 micrograms/kg once daily for 7 days reduced oesophageal acid
exposure and gastric acidity but had no effect on bolus reflex characteristics, findings
that were consistent with those reported in adults. Systemic exposure to esomeprazole
was proportionally higher in neonates compared with older infants.3
For findings from a review regarding the efficacy and safety of proton pump inhibitors in
infants, children, and adolescents, see Administration in Children, under Omeprazole,
Omeprazole Sodium. (Last reviewed: 2013­10­11; last modified: 2013­10­31)
1. Croxtall JD, et al. Esomeprazole: in gastroesophageal reflux disease in children and
adolescents. Paediatr Drugs 2008; 10: 199­205. (PubMed id:18454572)
2. Guimarães EV, et al. Management of gastroesophageal reflux disease and erosive
esophagitis in pediatric patients: focus on delayed­release esomeprazole. Ther Clin Risk
Manag 2010; 6: 531­7. (PubMed id:21063463)
3. Omari T, et al. Pharmacodynamics and systemic exposure of esomeprazole in
preterm infants and term neonates with gastroesophageal reflux disease. J Pediatr 2009;
155: 222­8. (PubMed id:19394048)
­­ Administration in hepatic impairment.
No dosage adjustment of esomeprazole is considered necessary for patients with mild to
moderate hepatic impairment (Child­Pugh Classes A and B, respectively). In severe
hepatic impairment (Child­Pugh Class C), US licensed product information recommends
that a daily dose of 20 mg, orally or intravenously, should not be exceeded. In the UK,
licensed product information specifies a maximum daily intravenous dose of
esomeprazole 20 mg in those aged 18 years and over, although when given for
prevention of rebleeding of gastric and duodenal ulcers after endoscopy in those with
severe hepatic impairment, an initial intravenous infusion of 80 mg over 30 minutes, may
be followed by a continuous intravenous infusion of 4 mg/hour over about 72 hours. A
maximum daily oral dose of esomeprazole 20 mg is recommended in patients from 12
years of age, and 10 mg in those aged 1 to 11 years. (Last reviewed: 2013­10­11; last
modified: 2013­10­17)
­­ 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. (Last reviewed: 2013­10­11; last
modified: 2013­10­17)
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© The Royal Pharmaceutical Society of Great Britain 2015
©2015 Truven Health Analytics Inc.
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