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Nexium - Nexium Side Effects - Nexium - Canada Pharmacy

Nexium
Esomeprazole Magnesium Trihydrate

Note: When used in combination with amoxicillin and clarithromycin, the Product Monographs for those agents must be consulted and followed. rx canada pharmacy

Pharmacology: Nexium delayed-release tablets contain esomeprazole (the S-isomer of omeprazole). Esomeprazole is acid labile and therefore is administered orally as enteric-coated granules compressed into a tablet. rx canada pharmacy

Esomeprazole (a substituted benzimidazole), reduces gastric acid secretion through a highly targeted mechanism of action. It is a specific inhibitor of the gastric enzyme H ⁺,K ⁺-ATPase (the proton pump) which is responsible for acid secretion by the parietal cells of the stomach.. rx canada pharmacy

Pharmacokinetics: Absorption of esomeprazole in healthy subjects results in peak plasma levels occurring 1 to 2 hours after dosing. The systemic bioavailability is 64% after a single 40 mg dose and 89% after repeated once daily oral administration (40 mg for 5 days). The apparent volume of distribution at steady state in healthy subjects is approximately 0.22 L/kg body weight. Esomeprazole is 97% protein bound and optically stable in vivo, with negligible inversion to the other isomer. rx canada pharmacy

A pharmacokinetic profile of esomeprazole was studied in 36 patients with symptomatic GERD after repeated once daily administration of 20 and 40 mg see Table I. rx canada pharmacy

Food intake delays and decreases the absorption of esomeprazole although this has no significant influence on the effect of esomeprazole on intragastric acidity.. rx canada pharmacy

Pharmacokinetics in Combination with Antibiotics: Interactions between esomeprazole (20 mg b.i.d.), amoxicillin (1 g b.i.d.) and clarithromycin (500 mg b.i.d.), were evaluated in a 4-way cross-over study (each study period was 7 days). When given as the triple combination, the bioavailability (AUC and C _max) of amoxicillin and clarithromycin were not significantly changed in healthy volunteers, compared with either drug given alone. The AUC and C _max of the 14-hydroxyclarithromycin metabolite were both increased by 53% during dosing with the triple combination, compared to values following dosing with clarithromycin alone. There were also significant increases in the AUC (2-fold increase) and C _max (39%) values for esomeprazole during concomitant administration with the antibiotic drugs, compared with esomeprazole alone. rx canada pharmacy

Metabolism: Esomeprazole is completely metabolized by the cytochrome P450 system, mainly in the liver (via CYP2C19 and CYP3A4). The major metabolites of esomeprazole (hydroxy and desmethyl metabolites) have no effect on gastric acid secretion. The CYP2C19 isozyme, which is involved in the metabolism of all available proton pump inhibitors, exhibits polymorphism. Some 3% of Caucasians and 15 to 20% of Asians lack CYP2C19 and are termed poor metabolizers. At steady state (40 mg for 5 days), the ratio of AUC in poor metabolizers to AUC in the rest of the population is approximately 2. Dosage adjustment of esomeprazole based on CYP2C19 status is not necessary. rx canada pharmacy

Almost 80% of an oral dose of esomeprazole is excreted as metabolites in urine with the remainder recovered in feces. Less than 1% of the parent drug is found in urine. Total recovery from urine and feces is 92 to 96% within 48 hours of a single oral dose.. rx canada pharmacy

Pharmacodynamics: Esomeprazole accumulates in the acidic environment of the parietal cells after absorption, where it is converted into the active form. This active sulfenamide specifically binds the H ⁺, K ⁺-ATPase (proton pump), to block the final step in acid production, thus reducing gastric acidity. Esomeprazole is effective in the inhibition of both basal acid secretion and stimulated acid secretion.. rx canada pharmacy

In healthy male subjects (n=12), repeated administration with 20 mg of esomeprazole once daily for 5 days, decreased mean peak acid output after pentagastrin stimulation by 90% when measured 6 to 7 hours after dosing. rx canada pharmacy

The effect of antisecretory therapy can be predicted from the duration of suppression of intragastric acidity to above pH 4.0 achieved by each drug regimen, and the length of treatment.. rx canada pharmacy

The antisecretory activity of esomeprazole was studied in patients with symptomatic gastroesophageal reflux disease. Esomeprazole 20 and 40 mg tablets were administered over 5 days and the proportion of time over 24 hours was assessed on Day 5, as shown in Table II. rx canada pharmacy

Eradication of H. pylori : Infection with H. pylori is associated with peptic ulcer disease and is a major factor in the development of gastritis. Approximately 90 to 100% of patients with duodenal ulcers, and 80% of patients with gastric ulcer, are infected with H. pylori . Treatment with esomeprazole alone has been shown to suppress, but not eradicate H. pylori . rx canada pharmacy

Eradication of H. pylori with triple therapy consisting of esomeprazole and clarithromycin/amoxicillin for 7 days is associated with healing and improvement of symptoms of duodenal ulcers. rx canada pharmacy


Indications: Treatment of conditions where a reduction of gastric acid secretion is required such as: reflux esophagitis, maintenance treatment of patients with reflux esophagitis, symptomatic gastroesophageal reflux disease (i.e., heartburn and regurgitation) and H. pylori eradication. rx canada pharmacy

Esomeprazole, in combination with clarithromycin and amoxicillin, is indicated for the treatment of patients with duodenal ulcer disease associated with H. pylori infection to eradicate the H. pylori and heal ulcers. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence. rx canada pharmacy

Contraindications: Hypersensitivity to esomeprazole, substituted benzimidazoles or any of the components of this medication (see Supplied). rx canada pharmacy

When used for eradication of H. pylori , the contraindications for amoxicillin and clarithromycin as found in the corresponding Product Monographs should be taken into consideration. rx canada pharmacy


Warnings: In the presence of any alarm symptom (e.g., significant unintentional weight loss, recurrent vomiting, dysphagia, hematemesis or melena), and/or when gastric ulcer is suspected or present, malignancy should be excluded, as treatment may alleviate symptoms and delay diagnosis. rx canada pharmacy

Pregnancy: The safety of esomeprazole in pregnancy has not been established. Esomeprazole should not be administered to pregnant women unless the expected benefits outweigh the potential risks. rx canada pharmacy

Lactation: It has not been investigated whether or not esomeprazole is excreted in human breast milk. No studies in lactating women have been performed. Therefore, esomeprazole should not be given to nursing mothers unless its use is considered essential. rx canada pharmacy

Children: The safety and effectiveness of esomeprazole in children have not yet been established. rx canada pharmacy

Precautions: Geriatrics: The metabolism of esomeprazole is not significantly changed in elderly subjects. Following repeated oral dosing with 40 mg of esomeprazole in healthy elderly subjects (6 males, 8 females; 71 to 80 years of age), AUC and C _max values measured were similar to those previously measured in young GERD patients (ratio of AUC values in elderly vs GERD subjects: 1.25; ratio of C _max values: 1.18). Therefore, dose adjustment is not required in the elderly. rx canada pharmacy

Gender: The AUC and C _max values were slightly higher (13%) in females than in males at steady state. Dosage adjustment based on gender is not necessary. rx canada pharmacy

Poor metabolizers: The CYP2C19 and CYP3A4 isozymes are responsible for metabolism of esomeprazole. CYP2C19, which is involved in the metabolism of all available proton pump inhibitors, exhibits polymorphism. Approximately 3% of Caucasians and 15 to 20% of Asians lack CYP2C19 and are termed poor metabolizers. At steady state, the ratio of AUC in poor metabolizers to AUC in the rest of the population is approximately 2. Dosage adjustment of esomeprazole based on CYP2C19 status is not necessary. rx canada pharmacy

Hepatic Insufficiency: The metabolism of esomeprazole in patients with mild to moderate liver dysfunction (Child Pugh Class A or B), is similar to that in patients with symptoms of GERD with normal liver function. Metabolism of esomeprazole is decreased in patients with severe liver dysfunction (Child Pugh Class C) resulting in a doubling of the area under the plasma concentration-time curve of esomeprazole. The plasma elimination half-life in patients with severe liver dysfunction is still very short (3 hours) relative to the dosing interval (24 hours). Esomeprazole and its major metabolites do not show any tendency to accumulate with once-daily dosing. Dose adjustment is not required in patients with mild to moderate liver impairment. A daily dose of 20 mg in patients with severe liver disease should not, as a rule, be exceeded (see Dosage). rx canada pharmacy

Renal Insufficiency: Since the kidney is responsible for the excretion of metabolites of esomeprazole but not for the elimination of the parent compound, the metabolism of esomeprazole is not expected to be changed in patients with impaired renal function. Esomeprazole is extensively protein-bound and is, therefore, not expected to be readily dialyzable. Dose adjustment is not required in patients with impaired renal function (see Dosage). rx canada pharmacy

Carcinogenicity: Long-term toxicity studies of omeprazole, revealed the gastric mucosa as the target organ. The carcinogenic potential of esomeprazole was assessed using omeprazole studies. In the rat carcinogenicity study (24 months), ECL-cell carcinoids were found in some animals treated with 14 to 140 mg/kg/day for their normal life span. ECL-cell carcinoids were seen in a background of ECL-cell hyperplasia. No ECL-cell carcinoids were identified in the carcinogenicity study in mice or in long-term (up to 7 years) general toxicity studies in dogs. rx canada pharmacy

A vast number of studies have revealed that pronounced and sustained hypergastrinemia is the mechanism behind the development of the gastric ECL-cell carcinoids in the rat. Such ECL carcinoids have been seen in rats after life-long treatment with other inhibitors of acid secretion such as H2-receptor blockers and other proton pump inhibitors. Partial fundectomy in rats results in hypergastrinemia and gastric ECL-cell carcinoids in the remaining part of the fundic mucosa, towards the end of the rats' life span. rx canada pharmacy

Treatment with esomeprazole for up to 1 year in more than 800 patients has not resulted in any significant pathological changes in the gastric oxyntic endocrine cells. Short-term treatment and long-term treatment with the racemate, omeprazole, capsules in a limited number of patients for up to 11 years have not resulted in any significant pathological changes in gastric oxyntic endocrine cells. rx canada pharmacy

During treatment with all antisecretory drugs serum gastrin increases in response to the decreased acid secretion. The effect of esomeprazole on serum gastrin concentrations was evaluated in approximately 2700 patients in clinical trials up to 8 weeks and in over 1300 patients for up to 6 to 12 months (daily doses of either 20 or 40 mg). The mean fasting gastrin level increased in a dose-related manner. This increase reached a plateau (approximately 100 pg/mL) within 2 to 3 months of therapy and returned to baseline levels (approximately 30 to 40 pg/mL) within 4 weeks after discontinuation of therapy. rx canada pharmacy

Drug Interactions : Esomeprazole is metabolized by the cytochrome P450 system (CYP), mainly in the liver, through CYP2C19 and CYP3A4. There are no clinically significant interactions between esomeprazole and diazepam, phenytoin, warfarin, quinidine or cisapride. rx canada pharmacy

Diazepam: Concomitant administration of esomeprazole (30 mg once daily for 5 days) resulted in a 45% decrease in the clearance of diazepam in healthy male volunteers. Studies in females have not been conducted. Increased levels of diazepam were seen some 12 hours after dosing and later when the plasma levels of diazepam were below its therapeutic range. Therefore, this interaction is unlikely to be of clinical significance. rx canada pharmacy

Warfarin: Concomitant administration of 40 mg of esomeprazole (once daily for 3 weeks) to male and female patients on stable anticoagulation therapy with warfarin, resulted in a 13% increase in trough plasma levels of R-warfarin (the less potent enantiomer) while that of S-warfarin was unchanged. Coagulation times were stable throughout the entire study period. No clinically significant interaction was observed. rx canada pharmacy

Phenytoin: Concomitant administration of 40 mg of esomeprazole (once daily for 2 weeks) to male and female epileptic patients stabilized on phenytoin, resulted in a 13% increase in trough plasma levels of phenytoin. This minor interaction is unlikely to be of clinical relevance as dose reduction was not required in any patient nor was the profile and frequency of adverse events affected. rx canada pharmacy

Results from a range of interaction studies with esomeprazole vs other drugs indicate that daily doses of 40 mg of esomeprazole, given for 5 to 21 days in male and/or female subjects, has no clinically relevant interactions with CYP1A2 (caffeine), CYP2C9 (S-warfarin) and CYP3A (quinidine, estradiol and cisapride). rx canada pharmacy

Adverse Effects: Esomeprazole is well-tolerated. Most adverse events have been mild and transient, showing no consistent relationship with treatment. Adverse events have been recorded during controlled clinical investigations in 6808 patients exposed to esomeprazole. An additional 1198 subjects/patients were exposed to esomeprazole in Phase I studies. Among events which occurred with a frequency of >1% in clinical studies, only headache, diarrhea, flatulence, abdominal pain, nausea, vomiting, dizziness and dry mouth are thought to be associated with the use of esomeprazole. rx canada pharmacy

The adverse events shown in Table III, irrespective of causal relationship, were reported (at a rate of more than 1%) in controlled short-term (up to 8 weeks) clinical trials involving 5668 patients. rx canada pharmacy

Additionally, the following adverse events (irrespective of causality) were each reported at a rate of >1% with esomeprazole in these same long-term studies (N=519): rash, fracture, hernia, dizziness, duodenitis, dyspepsia, epigastric pain, serum gastrin increased, gastroenteritis, gastrointestinal mucosal discoloration, esophageal disorder, tooth disorder, ALT increased, hypertension, coughing, rhinitis, anemia, benign gastrointestinal neoplasm, back pain, chest pain and fatigue. rx canada pharmacy

Clinical experience for up to 1 year in over 800 patients with doses of esomeprazole of 40 mg have shown a similar adverse event pattern to that seen in short-term trials. In addition to the adverse events listed above, the following adverse events were reported (at a rate of more than 1%), irrespective of causal relationship (mean duration of treatment = 294 days): accident/injury (7.6%), pain (4.3%), urinary tract infection (3.7%), bronchitis (3.6%), arthralgia (2.9%), hypertension (2.6%), allergy (2.1%), insomnia (2.1%), hypercholesterolemia (2%), anxiety (1.7%), gastroesophageal reflux (1.6%), fever (1.5%), ear infection (1.5%), flu-like disorder (1.4%), myalgia (1.2%), arthropathy (1.1%), dyspnea (1.1%), overdose (1.1%). rx canada pharmacy

Events reported less frequently in either short- or long-term studies that have been associated with the use of esomeprazole include dermatitis, pruritus and urticaria. rx canada pharmacy

H. pylori Eradication Combination Therapy: In clinical studies, a total of 446 patients received esomeprazole in combination with amoxicillin and clarithromycin for 7 days. The following adverse events were reported (at a rate of more than 1%), irrespective of causal relationship: diarrhea (21.5%), taste perversion (12.6%), headache (3.6%), dry mouth (3.4%), ALT increased (1.8%), flatulence (1.6%), nausea (1.3%), stomatitis (1.3%), vomiting (1.1%) and pharyngitis (1.1%). However, it should be noted that taste perversion is commonly associated with clarithromycin treatment and diarrhea is commonly associated with antibiotic treatment. When esomeprazole is used in combination with amoxicillin and clarithromycin, the Product Monographs for those agents must be consulted and followed. rx canada pharmacy

Overdose: Symptoms and Treatment: No information is available on the effects of higher doses in man, and specific recommendations for treatment cannot be given. Data are limited but single doses of 80 mg of esomeprazole were uneventful. No specific antidote is known. Esomeprazole is extensively protein-bound and is therefore not readily dialyzable. Treatment should be symptomatic and general supportive measures should be utilized. rx canada pharmacy

The maximum nonlethal oral dose in male and female rats ranged from 240 to 480 mg/kg. rx canada pharmacy

When used in combination with antibiotics, the Prescribing Information/Product Monograph for those antibiotics should be consulted. rx canada pharmacy


Dosage: The tablets should be swallowed whole with sufficient water. The tablets may also be dispersed in half a glass of noncarbonated water. No other liquids should be used as the enteric coating may be dissolved. Stir until the tablets disintegrate and drink the liquid with the pellets immediately or within 30 minutes. Rinse the glass with half a glass of water and drink. The pellets must not be chewed or crushed. rx canada pharmacy

Treatment of Conditions Where a Reduction of Gastric Acid Secretion is Required: Reflux Esophagitis: The recommended adult dose in patients with reflux esophagitis is 40 mg once daily for 4 to 8 weeks in order to optimize the healing rate and symptom resolution. Healing occurs in the majority of patients within 4 weeks. Sustained freedom from symptoms is achieved rapidly for most patients. An additional 4 weeks of treatment is recommended for patients in whom esophagitis has not healed or who have persistent symptoms. rx canada pharmacy

Maintenance of Healing of Erosive Esophagitis: For the long-term treatment of patients whose reflux esophagitis has been healed with acid suppression therapy, the recommended adult dose is 20 mg esomeprazole once daily. Controlled studies do not extend beyond 6 months. rx canada pharmacy

Symptomatic Gastroesophageal Reflux Disease: In patients with heartburn and/or acid regurgitation, without esophagitis, the recommended adult dose is 20 mg once daily for 2 to 4 weeks. If symptom control is not achieved after 4 weeks of treatment, further investigation is recommended. rx canada pharmacy

H. pylori Eradication: Patients with H. pylori -associated Active Duodenal Ulcer: The recommended dose is esomeprazole 20 mg, amoxicillin 1000 mg and clarithromycin 500 mg, all twice daily for 7 days. No further treatment with esomeprazole is required to ensure healing and/or symptom control. This dosing regimen can also be known as Nexium 1-2-3 A. rx canada pharmacy

In Patients with a History of Duodenal Ulcer: The recommended dose is esomeprazole 20 mg, amoxicillin 1000 mg and clarithromycin 500 mg, all twice daily for 7 days. This dosing regimen can also be known as Nexium 1-2-3 A. Eradication of H. pylori has been shown to reduce the risk of duodenal ulcer recurrence. rx canada pharmacy

Special Populations: When used in combination with amoxicillin and clarithromycin, please refer to the Product Monographs of these drugs for prescribing information regarding Contraindications, Warnings and Dosage (in elderly and patients with renal and hepatic insufficiency). rx canada pharmacy

Renal Insufficiency: No dose adjustment is required (see Precautions). rx canada pharmacy

Hepatic Insufficiency: No dose adjustment is required for patients with mild to moderate hepatic impairment. The daily doses of 20 mg in patients with severe hepatic impairment should not, as a rule, be exceeded (see Precautions). rx canada pharmacy

Elderly Patients: No dose adjustment is required (see Precautions). rx canada pharmacy

Information for the Patient: See Blue Section--Information for the Patient Nexium. rx canada pharmacy


Supplied: 20 mg: Each light pink, oblong and biconvex, delayed-release tablet, engraved with 20 mg on one side and AEH on the other side, contains: esomeprazole 20 mg equivalent to esomeprazole magnesium trihydrate 22.3 mg. Nonmedicinal ingredients: cellulose microcrystalline, crospovidone, glycerol monostearate, hydroxypropylcellulose, hypromellose, iron oxide, magnesium stearate, methacrylic acid ethylacrylate copolymer, polyethylene glycol, polysorbate, sodium stearyl fumarate, sugar spheres, synthetic paraffin, talc, titanium dioxide and triethyl citrate. Press-through blister compliance strips, cartons of 14, 28 and 56. HDPE bottles of 100. rx canada pharmacy

40 mg: Each pink, oblong and biconvex, delayed-release tablet, engraved with 40 mg on one side and AEI on the other side, contains: esomeprazole 40 mg equivalent to esomeprazole magnesium trihydrate 44.5 mg. Nonmedicinal ingredients: cellulose microcrystalline, crospovidone, glycerol monostearate, hydroxypropylcellulose, hypromellose, iron oxide, magnesium stearate, methacrylic acid ethylacrylate copolymer, polyethylene glycol, polysorbate, sodium stearyl fumarate, sugar spheres, synthetic paraffin, talc, titanium dioxide and triethyl citrate. Press-through blister compliance strips, cartons of 14, 28 and 56. HDPE bottles of 100. rx canada pharmacy

Store in a dry place at controlled room temperature (15 to 30°C). Tablets are moisture-sensitive and are therefore provided in blister compliance packages suitable for direct distribution to the patient.

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