Sergel ®

esomeprazole

Active ingredient and the pellets inside the capsule carefully emptied onto the applesauce. The
Each capsule contains esomeprazole 20 mg as esomeprazole magnesium pellets should be mixed with the applesauce and then swallowed immediately.
trihydrate INN in enteric coated pellets. The applesauce used should not be hot and should be soft enough to be
swallowed without chewing. The pellets should not be chewed or crushed. The
Properties and effects pellet/applesauce mixture should not be stored for future use.
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion Antacids may be used while taking esomeprazole.
by specific inhibition of the H+/K+-ATPase, the ‘Proton Pump’ of the gastric
parietal cell. Pregnancy
There are no adequate and well-controlled studies in pregnant women. Animal
Indication studies have revealed no teratogenic effects.
Esomeprazole is indicated
● To relieve from chronic heartburn symptoms and other symptoms associated Nursing Mothers
with GERD The excretion of esomeprazole in milk has not been studied. Breast-feeding
● For the healing of erosive esophagitis should be therefore be discontinued if the use of esomeprazole is considered
● For maintenance of healing of erosive esophagitis essential.
● In combination with amoxicillin and clarithromycin for eradication of
Helicobacter pylori infection in-patients with duodenal ulcer disease. Paediatric Use
● Zollinger-Ellison Syndrome Safety and effectiveness in paediatric patients have not been established.
● Acid related Dyspepsia
● Duodenal & Gastric ulcer Geriatric Use
No overall differences in safety and efficacy have been observed between the
Pharmacokinetics elderly and younger individuals, and other reported clinical experience has not
Absorption identified differences in responses between the elderly and younger patients, but
Esomeprazole capsules contain an enteric-coated pellet formulation of greater sensitivity of some older individuals cannot be ruled out.
esomeprazole magnesium. After oral administration peak plasma levels (Cmax)
occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when Hepatic Insufficiency
the dose is increased, and there is a three-fold increase in the area under the No dosage adjustment is recommended for patients with mild to moderate
plasma concentration- time curve (AUC) from 20 to 40 mg. At repeated once hepatic insufficiency. However, in-patients with severe hepatic insufficiency a
daily dosing, the systemic bioavailability is approximately 90% compared to 64% dose of 20 mg once daily should not be exceeded.
after a single dose. The AUC after administration of a single dose of
esomeprazole is decreased by 33-53% after food intake compared to fasting Renal Insufficiency
conditions. Esomeprazole should be taken at least one hour before meals. The Pharmacokinetics of Esomeprazole in patients with renal impairment are not
expected to be altered relative to healthy volunteers as less than 1% of
Distribution Esomeprazole is excreted unchanged in urine.
Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is
constant over the concentration range of 2-20 µmol/L. The apparent volume of Undesirable effects
distribution at steady state in healthy volunteers is approximately 16 L. The most frequently occurring adverse events reported with Esomeprazole
include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation
Metabolism and dry mouth. There are no difference in types of related adverse events seen
Esomeprazole is extensively metabolised in the liver by the cytochrome P450 during maintenance treatment upto 12 months compared to short term
(CYP) enzyme system. The metabolites of esomeprazole lack antisecretory treatment.
activity. The major part of esomeprazole’s metabolism is dependent upon the
CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The Drug Interaction:
remaining amount is dependent on CYP3A4 which forms the sulphone Esomeprazole is extensively metabolized in the liver by CYP2C19 and CYP3A4. In
metabolite. vitro and in vivo studies have shown that Esomeprazole is not likely to inhibit
CYPs 1A2, 2A6, 2C9, 2D6, 2E1 and 3A4. No clinically relevant interactions with
Excretion drugs metabolized by these CYP enzymes would be expected. Drug interaction
The plasma elimination half-life of esomeprazole is approximately 1–1.5 hours. studies have shown that Esomeprazole does not have any clinically significant
Less than 1% of parent drug is excreted in the urine. Approximately 80% of an interactions with phenytoin, warfarin, quinidine, clarithromycin or amoxicillin.
oral dose of esomeprazole is excreted as inactive metabolites in the urine, and
the remainder is found as inactive metabolites in the faeces. Esomeprazole may potentially interfere with CYP2C19, the major Esomeprazole
metabolising enzyme. Co-administration of Esomeprazole 30 mg and diazepam, a
Combination Therapy with Antimicrobials CYP2C19 substrate has resulted in a 45% decrease in clearance of diazepam.
Esomeprazole magnesium 40 mg once daily is given in combination with Increased plasma levels of diazepam have been observed 12 hours after dosing
clarithromycin 500 mg twice daily and amoxicillin 1000 mg twice daily for 7 days. and onwards. Esomeprazole inhibits gastric acid secretion. Therefore,
The mean steady state AUC and Cmax of Esomeprazole increased by 70% and Esomeprazole may interfere with the absorption of drugs where gastric pH is an
18%, respectively, during triple combination therapy compared to treatment with important determinant of bioavailability (e.g., ketoconazole, iron salts and
Esomeprazole alone. digoxin).

The pharmacokinetic parameters for clarithromycin and amoxicillin are similar Co-administration of oral contraceptives, diazepam, phenytoin, or quinidine do
during triple combination therapy and administration of each drug alone. not seem to change the pharmacokinetic profile of Esomeprazole.
However, the mean AUC and Cmax for 14-hydroxyclarithromycin are increased by
19% and 22%, respectively, during triple combination therapy compared to Combination Therapy with Clarithromycin
treatment with clarithromycin alone. This increase in exposure to 14- Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted
hydroxyclarithromycin is not considered to be clinically significant. in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.

Dosage & Administration Overdose

Esomeprazole capsules should be swallowed whole and taken one hour before A single oral dose of Esomeprazole at 510 mg/kg (about 103 times the human
meal. dose on a body surface area basis), has been lethal to rats. The major signs of
Healing of Erosive Esophagitis: 20 mg or 40 mg Once Daily for 4-8 Weeks. The acute toxicity are reduced motor activity, changes in respiratory frequency,
majority of patients are healed within 4 to 8 weeks. For patients who don’t heal tremor, ataxia, and intermittent clonic convulsions. There have been no reports of
after 4-8 weeks, an additional 4-8 weeks of treatment may be considered. overdose with Esomeprazole.
Maintenance of Healing of Erosive Esophagitis: 20 mg Once Daily (Clinical studies
did not extend 6 months). Symptomatic GERD: 20 mg Once Daily for 4 Weeks. If No specific antidote for Esomeprazole is known. Since Esomeprazole is
symptoms do not resolve completely after 4 weeks, an additional 4 weeks of extensively protein bound, it is not expected to be removed by dialysis. In the
treatment may be considered. Helicobacter Pylori eradication: Triple Therapy to event of overdosage, treatment should be symptomatic and supportive. As with
reduce the risk of Duodenal Ulcer recurrence-Esomeprazole 40 mg Once Daily the management of any overdose, the possibility of multiple drug ingestion
for 10 days, Amoxicillin 1000 mg Twice Daily for 10 days, Clarithromycin 500 mg should be considered.
Twice Daily for 10 days. Zollinger-Ellison Syndrome: The dose is 20-80 mg once
daily. The dosage should be adjusted individually and treatment continued as Packs
long as clinically indicated. Acid related Dyspepsia: 20-4o mg once daily for 2-4 60's capsules.
weeks according to response. Duodenal ulcer: 20 mg once daily for 2-4 weeks.
Gastric ulcer: 20-40 mg once daily for 4-8 weeks. Storage
Store in a dry place below 30 ºC.
Contraindication
Esomeprazole is contraindicated in-patient with known hypersensitivity to any of Keep out of reach of children.
the formulation.

Precaution
General
Symptomatic response to therapy with esomeprazole does not preclude the
presence of gastric malignancy.

Information for patients

Esomeprazole capsules should be taken at least one hour before meals. For Made in Bangladesh by:
patients who have difficulty swallowing capsules, one tablespoon of applesauce Healthcare Pharmaceuticals Limited
can be added to an empty bowl and the Esomeprazole capsules can be opened, Rajendrapur
HP 5212