Consumer medicine information

What is in this leaflet

This leaflet answers some of the common questions people ask about Esomeprazole AN. It does not contain all the information that is known about Esomeprazole AN.

It does not take the place of talking to your doctor or pharmacist.

All medicines have risks and benefits. Your doctor will have weighed the risks of your being given Esomeprazole AN against the benefits they expect it will have for you.

If you have any concerns about being given this medicine, ask your doctor or pharmacist.

Keep this leaflet. You may need to read it again.

What ESOMEPRAZOLE AN is used for

Esomeprazole AN will only be used if you are unable to take tablets.

Reflux Oesophagitis

Esomeprazole AN is used to treat reflux oesophagitis or reflux disease in the short-term. This can be caused by "washing back" (reflux) of food and acid from the stomach into the food pipe (oesophagus).

Reflux can cause a burning sensation in the chest rising up to the throat, also known as heartburn.

Bleeding Peptic Ulcers

Peptic ulcers are ulcers in the stomach or duodenum (tube leading out from the stomach). When these ulcers become severe enough, they start to bleed. Esomeprazole AN can be injected into your veins to treat these bleeding ulcers. Treatment with Esomeprazole AN should be followed with other therapy to reduce the amount of acid made by the stomach. This is to help your ulcer/s to heal.

Upper gastrointestinal symptoms associated with non-steroidal anti-inflammatory drugs (NSAIDs) therapy

If you are unable to eat or drink, Esomeprazole AN may be given to treat the symptoms of pain or discomfort in the stomach caused by NSAIDs (medicines used to treat pain or inflammation). Esomeprazole AN may also be used to help and prevent ulcers caused by NSAIDs.

How ESOMEPRAZOLE AN works

Esomeprazole AN is a type of medicine called a proton-pump inhibitor.

Esomeprazole AN works by decreasing the amount of acid made by the stomach, to give relief of symptoms and allow healing to take place. This does not stop food being digested in the normal way.

Your doctor will have explained why you are being treated with Esomeprazole AN and told you what dose you will be given.

Follow all directions given to you by your doctor carefully. They may differ from the information contained in this leaflet.

Your doctor may prescribe this medicine for another use. Ask your doctor if you want more information.

There is no evidence that Esomeprazole AN is addictive.

Before you are given ESOMEPRAZOLE AN

When you must not have it

Do not use Esomeprazole AN if you have allergies to:

• Esomeprazole or any ingredient listed at the end of this leaflet
• Any medicines containing a proton-pump inhibitor.

Some of the symptoms of an allergic reaction may include shortness of breath, wheezing or difficulty in breathing, swelling of the face, lips, tongue or other parts of the body, rash, itching or hives on the skin.

Do not use Esomeprazole AN if you are taking atazanavir or cilostazol. Please check with your doctor or pharmacist if you are taking these medicines. These medicines will be affected by Esomeprazole AN.

Esomeprazole AN is not approved for use in children less than one year of age.

Esomeprazole AN will only be used if the solution is clear, the package is undamaged and the use by (expiry) date marked on the pack has not been passed.

Before you start to take it

You must tell your doctor if you have:

• any allergies to any other medicines, foods, dyes or preservatives.
• liver disease or any other medical conditions
• been diagnosed with osteoporosis
• if you have ever had a skin reaction after treatment with a medicine similar to Esomeprazole AN that reduces stomach acid.

Do not use Esomeprazole AN if you are pregnant or breastfeeding unless your doctor says so. Ask your doctor about the risks and benefits involved. It is not known if it is safe for you to be given Esomeprazole AN while you are pregnant. It may affect your baby.

It is not known if your baby can take in Esomeprazole AN from breast milk if you are breastfeeding.

Taking other medicines

Do not use Esomeprazole AN if you are taking the following medicines:

• atazanavir, a medicine used to treat Human Immunodeficiency Virus (HIV).
• cilostazol, a medicine used to treat intermittent claudication

Tell your doctor if you are taking any other medicines, including any that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines and Esomeprazole AN may interfere with each other. These include:

• phenytoin, a medicine used to treat epilepsy
• warfarin and clopidogrel, medicines used to prevent blood clots
• diazepam, a medicine used to treat anxiety and some other conditions
• medicines used to treat fungal infections such as ketoconazole, itraconazole and voriconazole
• cisapride
• medicines used to treat depression such as citalopram, clomipramine and imipramine
• St John's wort, a herbal remedy used to treat mood disorders
• medicines used to treat bacterial infections such as clarithromycin erythromycin and rifampicin
• medicines for HIV treatment such as nelfinavir
• digoxin, a medicine used to treat heart problems
• methotrexate, a medicine used to treat arthritis and some types of cancer
• tacrolimus and mycophenolate mofetil - medicines used to assist in organ transplants
• erlotinib or related medicines used to treat cancer.

These medicines may be affected by Esomeprazole AN or may affect how well it works. You may need different amounts of your medicine or you may need to take different medicines. Your doctor can tell you what to do if you are taking any other medicines.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while you are being given Esomeprazole AN.

If you have not told your doctor about any of these things, tell them before you are given Esomeprazole AN.

How ESOMEPRAZOLE AN is given

Esomeprazole AN can be either injected into a vein over a period of at least 3 minutes, infused over a period of 10 to 30 minutes, or infused slowly over a longer period of 3 days. This is called an intravenous infusion.

The dosage and the period of time over which it is given will depend on your condition.

Your doctor will have had experience injecting Esomeprazole AN and will choose the best dose for you. They will be willing to discuss this decision with you.

In most patients, Esomeprazole AN relieves symptoms rapidly and it will be replaced with oral treatment as soon as you are well enough to swallow.

Overdose

The doctor or nurse giving you Esomeprazole AN will be experienced in the use of Esomeprazole AN, so it is unlikely that you will be given an overdose.

Side Effects

Tell your doctor or nurse as soon as possible if you do not feel well while you are being given Esomeprazole AN.

Esomeprazole AN helps most people with stomach or duodenal ulcers or reflux disease, but it may have unwanted side effects in a few people.

All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.

Ask your doctor, nurse or pharmacist to answer any questions you may have.

Tell your doctor if you notice any of the following and they worry you:

• constipation
• nausea or vomiting
• diarrhoea
• headache
• wind
• stomach pain
• skin rash, itchy skin
• injection site reaction such as redness, discomfort or swelling
• dizziness
• dry mouth.

These side effects are usually mild.

Tell your doctor immediately if you notice any of the following:

• muscle pain or weakness, joint pain
• "pins and needles"
• changes in sleep patterns
• mood changes, confusion or depression
• increase in breast size (males)
• fever
• increased bruising
• increased sweating
• hair loss
• changes in vision
• tremor
• yellowing of the eyes and skin
• shortness of breath, wheezing or difficulty breathing
• swelling of the face, lips, tongue or other parts of the body
• severe skin reaction which may include rash, itching, redness, blistering or peeling of the skin
• skin reaction, especially in sun exposed areas, with joint pain
• fever, widespread skin rash, swollen lymph nodes and/or facial swelling.
• sudden skin eruptions of pustules, i.e. small red white or red elevations of the skin that contain cloudy or purulent material (pus).
• blood in the urine
• muscle spasms, an irregular heart rhythm, seizures (possible signs of low magnesium levels).

Occasionally, Esomeprazole AN may be associated with changes in your liver or blood, which may require your doctor to do certain blood tests.

Tell your doctor if you notice anything else that is making you feel unwell. Some people may get other side effects while being given Esomeprazole AN.

After being given it

Storage

Esomeprazole AN will be stored by your doctor or pharmacist under the recommended conditions.

It should be kept in a cool, dry place, out of the reach of children where the temperature stays below 25°C.

Disposal

Any Esomeprazole AN which is not used will be disposed of in a safe manner by your doctor or pharmacist.

Esomeprazole AN contains no antimicrobial agent. Each Esomeprazole AN vial is for single use in one patient only. Any remaining contents should be discarded.

Product description

Esomeprazole AN powder for injection contains esomeprazole sodium 42.50 mg (this is equal to 40 mg esomeprazole) as the active ingredient; plus, disodium edetate and sodium hydroxide.

Esomeprazole AN is a white or almost white powder in a vial. This powder has to be mixed with normal saline before injection or infusion.

Sponsor

Juno Pharmaceuticals Pty Ltd
42 Kelso Street, Cremorne,
VIC – 3121

This leaflet was prepared in March 2023.

Australian Registration Number Esomeprazole AN AUST R 203825

Published by MIMS April 2023

1 Name of Medicine

Esomeprazole AN contains esomeprazole sodium.

2 Qualitative and Quantitative Composition

Esomeprazole sodium is a white to yellowish white solid.
Esomeprazole is a proton pump inhibitor and is a substituted benzimidazole. Esomeprazole is the S-isomer of omeprazole. It is optically stable in vivo, with negligible conversion to the R-isomer.
Esomeprazole AN is available as a white or almost white lyophilized powder for injection.
Each vial contains esomeprazole sodium 42.5 mg, equivalent to 40 mg esomeprazole, disodium edetate 1.0 mg and sodium hydroxide q.s. for pH adjustment.

3 Pharmaceutical Form

See Section 2 Qualitative and Quantitative Composition.

4 Clinical Particulars

4.9 Overdose

The symptoms described in connection with deliberate esomeprazole overdose (limited experience of oral doses in excess of 240 mg/day) are transient. Single oral doses of 80 mg and intravenous doses of 100 mg esomeprazole were uneventful. No specific antidote is known. 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.
Reports of overdosage with omeprazole in humans may also be relevant. In the literature doses of up to 560 mg have been described and occasional reports have been received when single oral doses have reached up to 2400 mg omeprazole (120 times the usual recommended clinical dose). Nausea, vomiting, dizziness, abdominal pain, diarrhoea and headache have been reported from overdosage with omeprazole. Also apathy, depression and confusion have been described in single cases. The symptoms described in connection to omeprazole overdosage have been transient, and no serious clinical outcome due to omeprazole has been reported. The rate of elimination was unchanged (first-order kinetics) with increased doses and no specific treatment has been needed.
For information on the management of overdose, contact the Poison Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Preclinical bridging studies between the enantiomer esomeprazole and the racemate (omeprazole) showed that these compounds are pharmacologically and toxicologically similar at equivalent systemic exposure. Thus, the extensive preclinical database for omeprazole is also relevant for the safety assessment of esomeprazole.
Preclinical studies on esomeprazole reveal no particular hazard for humans, based on conventional studies of single and repeated dose toxicity, embryo-foetal toxicity and mutagenicity. As in the oral studies, repeated intravenous administration of esomeprazole to animals resulted in few and primarily mild effects. However, very high intravenous doses caused an acute toxic response that consisted of occasional, nonspecific and short-lived CNS signs. This effect appeared to be associated with the C_max rather than the AUC of esomeprazole. Comparison of the C_max values in humans given 40 mg as a 3-minute injection or 80 mg as a 30 minute infusion and the plasma concentrations that were acutely toxic in animals showed a wide margin of safety (at least 6-fold for total and 20-fold for unbound plasma concentrations).
Genotoxicity. Esomeprazole was negative in a bacterial gene mutation assay. In clastogenicity tests, esomeprazole was positive (as was omeprazole) in an in vitro chromosome aberration test in human lymphocytes. However, three oral in vivo tests (an oral mouse micronucleus test, an oral chromosome aberration test in rat bone marrow and an intravenous chromosomal aberration test in mouse bone marrow) in the presence of long and high systemic exposure to esomeprazole, showed that esomeprazole was not clastogenic under in vivo conditions. Exposure levels in man are well below those at which clastogenic effects occurred in vitro.
Carcinogenicity. No carcinogenicity studies have been conducted on esomeprazole. However, long-term treatment with omeprazole (the racemate) produced enterochromaffin-like (ECL) cell hyperplasia and gastric carcinoids in rats. In a 104-week study in rats, carcinoids were observed at doses (on a mg/m² basis), which ranged from 0.4 to 30-fold the maximum clinical dose of esomeprazole. A no-effect dose level was not determined in female rats. A similar effect was not observed in a 78-week mouse carcinogenicity study with omeprazole, nor in a 26-week study in wild type and heterozygous p53+/- knockout mice (at a maximum tolerated dose that was 90-fold the maximum clinical dose, on a mg/m² basis), although gastric cell hyperplasia occurred. These gastric effects in the rat are believed to be the result of sustained, pronounced hypergastrinaemia secondary to reduced production of gastric acid. Similar effects are elicited by other proton pump inhibitors, H₂-receptor antagonists and by partial fundectomy.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Chemical structure. The chemical name is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl) methyl] sulfinyl]-1H-benzimidazole sodium. The chemical structure of esomeprazole sodium is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSESOSOD.gif Molecular formula: C₁₇H₁₈N₃O₃SNa.
Molecular weight: 367.4.
CAS number. 161796-78-7.

7 Medicine Schedule (Poisons Standard)

Schedule 4 (Prescription Only Medicine).

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/ESOINJST.gif