Escar

Uses

Esomeprazole is used for:

• Treatment of Gastroesophageal Reflux Disease (GERD)
• Healing of Erosive Esophagitis
• Maintenance of Healing of Erosive Esophagitis
• Symptomatic Gastroesophageal Reflux Disease
• H. pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence
• Zollinger-Ellison Syndrome
• Acid Related Dyspepsia
• Duodenal and Gastric Ulcer

Management of acidosis in cardiac arrest.

Management of metabolic acidosis in:

• Severe renal disease
• Uncontrolled diabetes
• Circulatory insufficiency from shock or dehydration
• Severe primary lactic acidosis

Alkalinization of urine.

Escar is also used to associated treatment for these conditions: Duodenal Ulcer, Erosive Esophagitis, Gastro-esophageal Reflux Disease (GERD), Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Stress Ulcers, Upper Gastrointestinal Hemorrhage, Zollinger-Ellison Syndrome, Acute benign gastric ulcers, Maintenance of healing Erosive esophagitis, Postendoscopy BleedingAcid indigestion, Barbiturate intoxication, Breast Cancer, Constipation, Dental Decay, Duodenal Ulcer, Dyspepsia, Gastro-esophageal Reflux Disease (GERD), Gingival Bleeding, Heartburn, Helicobacter Infections, Hyperkalemia, Ischaemia, Metabolic Acidosis, Myocardial Infarction, Plaque, Dental, Pruritis of the skin, Skin Irritation, Upset stomach, Zollinger-Ellison Syndrome, Abdominal bloating, Benign, active Gastric Ulcer, Methyl alcohol poisoning, Prophylaxis of Contrast-induced nephropathy, Salicylate poisoning, Severe Diarrhea, Swelling of the gums, Bowel preparation therapy

How Escar works

Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect that persists longer than 24 hours.

Sodium bicarbonate is a systemic alkalizer, which increases plasma bicarbonate, buffers excess hydrogen ion concentration, and raises blood pH, thereby reversing the clinical manifestations of acidosis. It is also a urinary alkalizer, increasing the excretion of free bicarbonate ions in the urine, thus effectively raising the urinary pH. By maintaining an alkaline urine, the actual dissolution of uric acid stones may be accomplished. Sodium bicarbonate acts as an antacid and reacts chemically to neutralize or buffer existing quantities of stomach acid but has no direct effect on its output. This action results in increased pH value of stomach contents, thus providing relief of hyperacidity symptoms. [PharmGKB]

Dosage

Escar dosage

Tablet:

Healing of erosive esophagitis: 20 mg or 40 mg once daily for 4 to 8 Weeks. For those patients who have not healed after 4-8 weeks of treatment, an additional 4-8 weeks course of Esomeprazole may be considered.

Long-term management of esophagitis: 20 mg once daily.

Symptomatic gastroesophageal reflux disease: 20 mg once daily for 4 weeks.

H. pylori eradication for treatment of duodenal ulcer:

Triple therapy: 20 mg Esomeprazole once daily with 500 mg Clarithromycin twice daily, and 1 g Amoxicillin twice daily for 7-10 days.

Injection:

The recommended adult dose in GERD with Erosive Esophagitis is either 20 or 40 mg Esomeprazole given once daily by intravenous injection (no less than 3 minutes) or intravenous infusion (10 to 30 minutes). Pediatric dose (1 to 11 years old):

• Short term treatment of symptomatic GERD: 10 mg once daily for up to 8 weeks.

Healing of erosive esophagitis:

• Weight <20 kg: 10 mg once daily for up to 8 weeks.
• Weight ≥20 kg: 10 mg or 20 mg once daily forup to 8 weeks.

Oral: The usual dose is 300 mg to 2 grams, 1 to 4 times daily.

Intravenous (Severe metabolic acidosis):

• Adult: By slow inj of a hypertonic solution of up to 8.4% (1000 mmol/L), or by continuous infusion of a weaker solution, usually 1.26% (150 mmol/L). For correction of acidosis during advanced cardiac life support procedures, 50 ml of an 8.4% solution may be given.
• Elderly: Dosage adjustments may be required.

Directions for reconstitution of solution: Solution for injection is prepared by adding 5 ml of 0.9% Sodium Chloride for intravenous injection into the vial containing the dry powder. The reconstituted solution for injection is clear and colorless to very slightly yellow.

Preparations for Use and Administration of Esomeprazole 40 IV Injection: A solution for intravenous infusion is prepared by first reconstituting the contents of one vial with 5 ml of 0.9% Sodium Chloride and further diluting the resulting solution to a final volume of 50 ml. The resultant concentration after diluting to a final volume of 50 ml is 0.8 mg/ml.

• 20 mg dose: Withdraw 25 ml of the final solution and administer as an intravenous infusion over 10 minutes to 30 minutes.
• 10 mg dose: Withdraw 12.5 ml of the final solution and administer as an intravenous infusion over 10 minutes to 30 minutes.

Side Effects

In general, esomeprazole is well tolerated in both short and long term use. Adverse events reported with esomeprazole include headache, diarrhoea, nausea, flatulence, abdominal pain, constipation and dry mouth.

This medication is generally well tolerated. However, high doses may cause headache, nausea or irritability. If any of these effects continue or become bothersome, inform your doctor. Notify your doctor if you develop: muscle weakness, slow reflexes, confusion, swelling of the feet or ankles, black tar-like stools, coffee-ground vomit. If you notice other effects not listed above, contact your doctor or pharmacist.

Toxicity

Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating

Precaution

Symptomatic response to therapy with Esomeprazole does not preclude the presence of gastric malignancy. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long-term with omeprazole, of which Esomeprazole is an enantiomer.

Pre-existing heart disease, kidney disease, liver disease, high blood pressure, any allergies.

Interaction

Drug interaction studies have shown that Esomeparzole does not have any clinically significant interactions with Phenytoin, Warfarin, Quinidine, Clarithromycin or Amoxicillin. Esomeprazole inhibits gastric acid secretion. Therefore, Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, Ketoconazole, Iron salts and Dogoxin). Coadministration of oral contraceptives, Diazepam, Phenytoin or Quinidine did not seem to change the pharmacokinetic profile of Esomeprazole.

This medication has the potential to interact with many medications. Should not take any other medication within 1 to 2 hours of taking an antacid. Potentially hazardous interactions with Corticosteroids and Corticotropin, Alkalis, Calcium, Diuretics and Potassium.

Volume of Distribution

The apparent volume of distribution at steady state in healthy volunteers is approximately 16 L.

Elimination Route

After oral administration, peak plasma levels (Cmax) occur at approximately 1.5 hours (Tmax). The Cmax increases proportionally when the dose is increased, and there is a three-fold increase in the area under the plasma concentration-time curve (AUC) from 20 to 40 mg. At repeated once-daily dosing with 40 mg, the systemic bioavailability is approximately 90% compared to 64% after a single dose of 40 mg. The mean exposure (AUC) to esomeprazole increases from 4.32 μmolhr/L on Day 1 to 11.2 μmolhr/L on Day 5 after 40 mg once daily dosing. The AUC after administration of a single 40 mg dose of Esomeprazole is decreased by 43% to 53% after food intake compared to fasting conditions. Esomeprazole should be taken at least one hour before meals.

Combination Therapy with Antimicrobials:

Esomeprazole magnesium 40 mg once daily was given in combination with Clarithromycin 500 mg twice daily and Amoxicillin 1000 mg twice daily for 7 days to 17 healthy male and female subjects. The mean steady state AUC and Cmax of esomeprazole increased by 70% and 18%, respectively during triple combination therapy compared to treatment with esomeprazole alone. The observed increase in esomeprazole exposure during co-administration with clarithromycin and amoxicillin is not expected to produce significant safety concerns.

Half Life

1-1.5 hours

Elimination Route

The plasma elimination half-life of esomeprazole is approximately 1 to 1.5 hours. Less than 1% of parent drug is excreted in the urine. Approximately 80% of an oral dose of esomeprazole is excreted as inactive metabolites in the urine, and the remainder is found as inactive metabolites in the feces.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies on the use of Esomeprazole in pregnant women. Therapeutic doses during pregnancy are unlikely to pose a substantial teratogenic risk. Esomeprazole should be used during pregnancy only if the potential benefit to pregnant women justifies the potential risk to the fetus.

Lactation: Esomeprazole is excreted in human milk. Thus, a decision should be taken to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Esomeprazole is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted Benzimidazoles.

This drug is contraindicated in hypoventilatory states, chloride depletion owing to continuous gastric fluid loss, metabolic and/or respiratory alkalosis, hypocalcemia and diuretics known to produce hypochloremic alkalosis.

Special Warning

Geriatric: Dosage adjustment is not necessary.

Pediatric: Safety and effectiveness in pediatric patients have not been established.

Hepatic insufficiency: No dosage adjustment is recommended for patients with mild to moderate hepatic insufficiency. However, in patients with severe hepatic insufficiency a dose of 20 mg once daily should not be exceeded.

Renal insufficiency: Dosage adjustment is not necessary.

Acute Overdose

There is no experience to data with deliverate overdose. Data are limited but single doses of 80 mg Esomeprazole were uneventful. Esomeprazole is extensively plasma protein bound and is therefore not readily dialyzable. As in any case of overdose, treatment should be symptomatic and general supportive measures should be utilised.

If alkalosis results, the bicarbonate should be stopped and the patient managed according to the degree of alkalosis present. 0.9% sodium chloride injection intravenous may be given; potassium chloride also may be indicated if there is hypokalemia. Severe alkalosis may be accompanied by hyperirritability or tetany and these symptoms may be controlled by calcium gluconate. An acidifying agent such as ammonium chloride may also be indication in severe alkalosis.

Storage Condition

Store between 15-30°C. Protect from light.

Store in a cool & dry place protected from light. Keep out of reach of children.

Innovators Monograph

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