Nexium online in Australia

Use

Therapeutic indications

Nexium Control is indicated for the short-term treatment of symptoms of gastroesophageal reflux (eg, heartburn and acid regurgitation) in adults.

Dosage and method of administration

Dose

The recommended dose is 20 mg of esomeprazole (one tablet) per day.

It may be necessary to take the tablets for 2 or 3 consecutive days to improve symptoms. The duration of treatment can be up to 2 weeks. Once symptoms disappear, treatment should be discontinued.

If symptoms persist after 2 weeks of continuous treatment, the patient should be recommended to consult a doctor.

Specific populations

Patients with kidney failure.

No dosage adjustment is necessary in patients with renal impairment.

Patients with severe renal impairment should be treated with caution due to limited experience in these patients (see section Pharmacokinetic properties).

Patients with liver failure.

No dosage adjustment is necessary in patients with mild to moderate hepatic impairment. However, patients with severe hepatic impairment should be advised by a physician before taking Nexium Control (see sections 4.4 and 4.4).

Elderly (≥ 65 years old)

No dosage adjustment is necessary in elderly patients.

Pediatric population

There is no relevant use of Nexium Control in the pediatric population under 18 years of age in the indication: "short-term treatment of symptoms of gastroesophageal reflux (eg, heartburn and acid regurgitation)".

Administration form

The tablets should be swallowed whole with half a glass of water. The tablets should not be chewed or chewed.

In addition, the tablet can be disintegrated in half a glass of non-carbonated water. No other liquid should be used as the enteric coating can dissolve. Mix the solution until the tablet has disintegrated. The solution with the granules should be ingested immediately or within 30 minutes. The glass should be rinsed with half a glass of water and the water should be swallowed. The granules must not be chewed or chewed.

Prescription and delivery conditions

Lack of information in the Marketing Authorization.

Duration and special precautions for conservation

Shelf life: 3 years.

Special precautions for storage: Store at a temperature not exceeding 30 ° C.

Store in the original package in order to protect from moisture.

Preclinical safety data

Non-clinical data from conventional studies of safety pharmacology, repeated-dose toxicology, genotoxicity, and reproductive and developmental functions have revealed no particular risk to humans.

The following side effects have not been seen in clinical studies, but have been seen in animals with exposure levels similar to those used in humans and may have clinical significance:

Carcinogenicity studies in rats with the racemic mixture have shown ECL gastric cell hyperplasia and carcinoid tumors. In the rat, these gastric changes are the result of prolonged and significant hypergastrinemia secondary to reduced gastric acid secretion and are observed in rats during long-term treatment with inhibitors of gastric acid secretion.

Incompatibilities

Aimlessly.

Employment precautions

Contraindications

Hypersensitivity to esomeprazole, benzimidazole derivatives or to any of the excipients (see

Composition section).

Esomeprazole should not be used concomitantly with nelfinavir (see section Interactions with other medicinal products and other forms of interaction).

Pregnancy and lactation

Pregnancy

A moderate number of data in pregnant women (between 300 and 1000 pregnancy outcomes) did not show any malformation or toxic effect to the fetus or newborn with esomeprazole. Animal studies have shown no direct or indirect harmful effects on reproduction (see Preclinical Safety Data section).

As a precaution, it is best to avoid the use of Nexium Control during pregnancy.

Breastfeeding

It is not known whether esomeprazole / metabolites are excreted in human milk. There are insufficient data on the effects of esomeprazole in newborns / infants. Esomeprazole should not be used during lactation.

Fertility

Animal studies with the racemic mixture of omeprazole, taken by mouth, do not indicate any effect on fertility.

Warnings and precautions for use

general

Patients are advised to seek medical advice in case of:

• significant and involuntary weight loss, repeated vomiting, dysphagia, hematemesis or melena and, in case of suspicion or presence of a gastric ulcer, the possibility of malignancy should be excluded since treatment with esomeprazole may reduce symptoms and delay in diagnosis.

• a history of gastric ulcer or digestive surgery.

• continuous symptomatic treatment for indigestion or heartburn for 4 weeks or more.

• jaundice or severe liver disease.

• new symptoms or recent changes in symptoms in patients older than 55 years

Patients who have persistent and recurring disorders, such as difficult digestion (dyspepsia) or heartburn (heartburn) should see their doctor regularly. Patients over the age of 55 who take over-the-counter medications daily due to difficult digestion or heartburn should inform their pharmacist or doctor.

Nexium Control should not be taken by patients as a long-term preventive medicine.

Treatment with proton pump inhibitors (PPIs) may lead to a slight increase in the risk of gastrointestinal infections, in particular Salmonella and Campylobacter, and possibly Clostridium difficile in hospitalized patients (see section Pharmacodynamic properties).

Patients should consult their physician before taking this medication if an endoscopy or urea breath test is planned.

Combination with other drugs.

The combination of esomeprazole with atazanavir is not recommended (see section Interactions with other medicinal products and other forms of interaction). If the combination of atazanavir with a proton pump inhibitor is considered essential, close clinical monitoring associated with an increase in the dose of atazanavir to 400 mg with 100 mg of ritonavir is recommended. A 20 mg dose of esomeprazole should not be exceeded.

Esomeprazole is a CYP2C19 inhibitor. At the start or end of treatment with esomeprazole, the risk of interactions with medicinal products metabolized by CYP2C19 should be considered. An interaction between clopidogrel and esomeprazole has been observed. The clinical relevance of this interaction is uncertain. The concomitant use of esomeprazole and clopidogrel should be discouraged (see section Interactions with other medicinal products and other forms of interaction).

Patients should not take another PPI or H2 blocker concomitantly.

Saccharose

This medicine contains sugar spheres (sucrose). It is not recommended for use in patients with fructose intolerance, glucose-galactose malabsorption syndrome, or sucrase / isomaltase deficiency.

Interference with laboratory tests.

An increase in the level of chromogranin A (CgA) can interfere with the tests carried out for the exploration of neuroendocrine tumors. To avoid this interference, esomeprazole treatment should be temporarily suspended 5 days before the CgA dose.

Subacute cutaneous lupus erythematosus (LECS)

Proton pump inhibitors are associated with very rare cases of LECS. If lesions develop, especially on areas of the skin exposed to the sun, and if they are accompanied by arthralgia, the patient should consult a doctor promptly and the healthcare professional should consider discontinuing Nexium control. The appearance of LECS after treatment with a proton pump inhibitor may increase the risk of LECS with other proton pump inhibitors.

Interaction with other medicinal products and other forms of interaction

Interaction studies have only been performed in adults.

Effects of esomeprazole on the pharmacokinetics of other drugs.

Since esomeprazole is an enantiomer of omeprazole, the reported interactions with omeprazole should be considered.

Protease inhibitors

An interaction between omeprazole and certain protease inhibitors has been reported. The clinical significance and mechanisms of these interactions are not always known. Increased gastric pH during omeprazole treatment may affect the absorption of protease inhibitors. There are other possible mechanisms of interaction that occur through CYP2C19 inhibition.

For atazanavir and nelfinavir, decreased plasma concentrations of these medicinal products have been reported when administered concomitantly with omeprazole; Therefore, the concomitant administration of omeprazole and these medicinal products is not recommended. Co-administration of omeprazole (40 mg once daily) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers resulted in a substantial decrease in plasma atazanavir concentrations (a decrease of approximately 75% in AUC, Cmax, and Cmin) . Increasing the atazanavir dose to 400 mg did not compensate for the effect of omeprazole on plasma concentrations of atazanavir. Co-administration of omeprazole (20 mg once daily) and atazanavir 400 mg / ritonavir 100 mg in healthy volunteers resulted in an approximately 30% decrease in exposure to atazanavir from the exposure observed after administration of atazanavir 300 mg / ritonavir 100 mg once daily, without omeprazole 20 mg once daily. Concomitant administration of omeprazole (40 mg once daily) decreased the mean AUC, Cmax, and Cmin of nelfinavir by 36 to 39% and the average of 75 to 92% AUC, Cmax, and Cmin of its pharmacologically active metabolite M8. . Due to the similar pharmacodynamic and pharmacokinetic properties of omeprazole and esomeprazole, concomitant administration of esomeprazole and atazanavir is not recommended and concomitant administration of esomeprazole and nelfinavir is contraindicated (see sections Contraindications and Warnings and precautions for use).

For saquinavir (in combination with ritonavir), an increase in plasma concentration (80 to 100%) has been reported during concomitant treatment with omeprazole (40 mg once daily). Treatment with omeprazole 20 mg once daily did not affect exposure to darunavir (in combination with ritonavir) or exposure to amprenavir (in combination with ritonavir).

Treatment with esomeprazole 20 mg once daily did not affect exposure to amprenavir (with or without ritonavir). Treatment with omeprazole 40 mg once daily did not affect exposure to lopinavir (combined with ritonavir).

Methotrexate

An increase in methotrexate concentrations has been observed in some patients when methotrexate is co-administered with proton pump inhibitors (PPIs). When large doses of methotrexate are administered, temporary discontinuation of esomeprazole therapy may be necessary.

Tacrolimus

Increased serum tacrolimus concentrations have been reported with co-administration of tacrolimus and esomeprazole. Enhanced monitoring of tacrolimus concentrations and renal function (creatinine clearance) should be carried out, and the tacrolimus dose should be adjusted if necessary.

Drugs whose absorption depends on pH.

Inhibition of stomach acid during treatment with esomeprazole and other PPIs may decrease or increase drug absorption if it depends on gastric pH. The absorption of oral medications such as ketoconazole, itraconazole, and erlotinib may decrease during treatment with esomeprazole, and the absorption of digoxin may increase during treatment with esomeprazole.

Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (up to 30% in two out of ten subjects). Digoxin toxicity has rarely been reported. However, special care should be taken when high-dose esomeprazole is administered in elderly patients. Monitoring of digoxin therapy should therefore be reinforced.

Drugs metabolized by CYP2C19

Esomeprazole inhibits CYP2C19, the main metabolizing enzyme of esomeprazole. Therefore, when co-administered with medicinal products metabolized by CYP2C19, such as warfarin, phenytoin, citalopram, imipramine, clomipramine, diazepam, etc., the plasma concentrations of these medicinal products may be increased and reduced doses may be necessary. In the case of clopidogrel, a prodrug transformed into its active metabolite through CYP2C19, plasma concentrations of the active metabolite may be reduced.

Warfarin

A clinical trial has shown that when co-administered with 40 mg esomeprazole in patients receiving warfarin, clotting times remain within the normal range. However, since its commercialization, some isolated cases of clinically significant INR elevation have been reported during concomitant therapy. Monitoring at the beginning and at the end of concomitant treatment of esomeprazole with warfarin or other coumarin derivatives is recommended.

Clopidogrel

The results of studies in healthy subjects have shown a pharmacokinetic (PK) / pharmacodynamic (PD) interaction between clopidogrel (300 mg loading dose followed by 75 mg daily as maintenance dose) and esomeprazole (40 mg orally daily). resulting in a decrease in exposure to the active metabolite of clopidogrel by 40% on average and a decrease in maximum inhibition of platelet aggregation (induced by ADP) by 14% on average.

In a study in healthy subjects, a reduction of approximately 40% in the exposure of the active metabolite of clopidogrel was observed when taking a fixed combination of esomeprazole 20 mg and acetylsalicylic acid (ASA) 81 mg with clopidogrel compared to clopidogrel alone. However, the maximum levels of inhibition of platelet aggregation (induced by ADP) in these patients were identical in the two groups.

Contradictory data on the clinical consequences of this PK / PD interaction in terms of the occurrence of major cardiovascular events have been reported in observational and clinical studies. As a precaution, the concomitant use of esomeprazole and clopidogrel should be discouraged.

Phenytoin

Co-administration of 40 mg esomeprazole leads to a 13% increase in plasma phenytoin concentrations in epileptic patients. It is recommended to monitor plasma phenytoin concentrations when starting or stopping treatment with esomeprazole.

Voriconazole

Omeprazole (40 mg once daily) has increased plasma concentrations of voriconazole (a CYP2C19 substrate), with Cmax and AUCτ increased by 15% and 41% respectively.

Cilostazol

Like omeprazole, esomeprazole is an inhibitor of CYP2C19. In a crossover study, omeprazole administered in a 40 mg dose to healthy subjects increased the Cmax and AUC of cilostazol by 18 and 26% respectively, and of one of its active metabolites by 29 and 69% respectively.

Cisapride

In healthy volunteers, co-administration of 40 mg of esomeprazole resulted in a 32% increase in the area under the plasma concentration curve (AUC) and a 31% prolongation of the elimination half-life. (t1 / 2) without a significant increase in the plasma peak of cisapride. The slight prolongation of the QTc interval observed after administration of cisapride alone does not increase during concomitant administration of cisapride with esomeprazole.

Diazepam

Co-administration of 30 mg of esomeprazole resulted in a 45% decrease in clearance of the diazepam metabolite, metabolized by CYP2C19.

Drugs without clinically significant interaction.

Amoxicillin and quinidine

Esomeprazole has not shown a clinically significant effect on the pharmacokinetics of amoxicillin and quinidine.

Naproxen or rofecoxib

Short-term studies evaluating co-administration of esomeprazole with naproxen or rofecoxib have shown no clinically relevant pharmacokinetic interaction.

Effects of other medicinal products on the pharmacokinetics of esomeprazole

Drugs that inhibit CYP2C19 and / or CYP3A4

Esomeprazole is metabolized by CYP2C19 and CYP3A4. Concomitant administration of esomeprazole with a CYP3A4 inhibitor clarithromycin (500 mg twice daily) leads to a doubling of exposure (AUC) to esomeprazole. Concomitant administration of esomeprazole with a combined CYP2C19 and CYP3A4 inhibitor can more than double the exposure of esomeprazole. Voriconazole, an inhibitor of CYP2C19 and CYP3A4, increased the AUCτ of omeprazole by 280%. Systematic adjustment of the esomeprazole dose is not necessary in any of these situations. However, dose adjustment should be considered in patients with severe hepatic impairment and if long-term treatment is indicated.

Medicines that induce CYP2C19 and / or CYP3A4

Drugs known to induce CYP2C19 or CYP3A4 or both (such as rifampicin and St. John's wort (Hypericum perforatum)) can reduce serum esomeprazole levels by increasing esomeprazole metabolism.

Caution

Undesirable effects

Summary of the job security profile

Headache, abdominal pain, diarrhea, and nausea are some of the most common side effects reported in clinical trials (and also during post-marketing use). Furthermore, the safety profile is similar for different formulations, indications for treatment, age groups, and patient populations. No dose-related adverse reactions have been identified.

Tabulated summary of adverse reactions

The following side effects have been reported or suspected in clinical trials of esomeprazole and since its commercialization. Unwanted effects are ranked by frequency according to the MedDRA convention: very common ≥ 1/10; common ≥ 1/100; minus 1/10; infrequent ≥ 1/1000; minus 1/100; rare ≥ 1 / 10,000; minus 1/1000; very rare less than 1 / 10,000; frequency not known (cannot be estimated from the available data).

Frequent

Rare

Rare

Very rare

Indeterminate

Blood and lymphatic system disorders.

leukopenia, thrombocytopo-

denies

Agranulocyte

I know pancytopenia

Frequent

Rare

Rare

Very rare

Indeterminate

Affects of

system

immune

Reactions

hypersensitivity

like fever

angioedema

reaction / shock

anaphylactic

Metabolism and nutrition disorders.

peripheral edema

hyponatremia

hypomagnetic

sememia, a hypomagnet

severe sememia may be associated with

hypocalcemia a hypomagnet

semen can also

cause hypokalemia

Psychiatric disorders

insomnia

agitation

confusion

depression

aggressiveness, hallucinations

Nervous system disorders

headache

dizziness, paraesthesia, drowsiness

taste disorders

Eye conditions

blurry vision

Ear and labyrinth disorders.

dizziness

Respiratory, thoracic and mediastinal disorders.

bronchospasm

Gastrointestinal disorders.

abdominal pain,

constipation

tion, diarrhea, flatulence, nausea / vomiting

ment

dry mouth

Stomatitis and gastrointestinal candidiasis

intestinal

colitis

microscopes

that

Hepatobiliary disorders.

increased liver enzymes

hepatitis with or without jaundice

liver failure, encephalopa

thie in patients with pre

existing

Frequent

Rare

Rare

Very rare

Indeterminate

Skin and subcutaneous tissue disorders.

dermatitis, pruritus, rash, urticaria

alopecia, photosensitivity

erythema multiforme, Stevens syndrome

Johnson, Lyell syndrome

(toxic epidermal necrolysis)

Muscle disorders

skeletal and systemic

arthralgia

myalgia

muscular weakness

Kidney and urinary tract disorders.

interstitial nephritis

Reproductive system and breast disorders.

gynecomastia

General disorders and abnormalities.

site

from admin-

tion

discomfort, increased sweating

Notification of suspected adverse reactions.

Notification of suspected adverse reactions after authorization of the medicinal product is important. Allows continuous monitoring of the benefit / risk ratio of the medication. Health professionals are requested to report any suspected adverse reactions through the national reporting system listed in Appendix V.

Overdose

To date, experience with voluntary overdose has been very limited. The symptoms described when taking 280 mg are gastrointestinal symptoms and signs of fatigue. Single doses of 80 mg esomeprazole were well tolerated. There is no specific antidote known. Esomeprazole binds strongly to plasma proteins and therefore cannot be easily dialyzed. In case of overdose, appropriate symptomatic treatment should be started.