Nexium is used to treat symptoms of gastroesophageal reflux disease (GERD) and other conditions involving excessive stomach acid such as Zollinger-Ellison syndrome. It is also used to promote healing of erosive esophagitis (damage to your esophagus caused by stomach acid). Nexium (esomeprazole magnesium) is a proton pump inhibitor that decreases the amount of acid produced in the stomach.
Drug Fact
Class : Proton Pump Inhibitor
Category: Prescription Only and OTC
Uses: treat symptoms of gastroesophageal reflux disease (GERD) and other conditions involving excessive stomach acid such as Zollinger-Ellison syndrome
Consumed by: adults and children > 1 month old
Pregnancy category: C
Category C: Either studies in animals have revealed adverse effects on the fetus (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 fetus.
Dosage form: tablet, injection
Side Effect :
- headache,
- drowsiness,
- mild diarrhea,
- nausea,
- stomach pain,
- gas,
- constipation, and
- dry mouth
Tell the doctor if you have any side effect that bothers you or that does not go away. These are not all the possible side effects of Nexium. For more information, ask your doctor or pharmacist.
Administration
Delayed-Release Cap: Should be taken on an empty stomach. Take 1 hr before meals.
Tab: May be taken with or without food.
Reconstitution
IV inj: Reconstitute vial labelled as 20 mg or 40 mg with 5 mL 0.9% NaCl. IV infusion (10-30 minutes): Reconstitute vial with 5 mL of 0.9% NaCl, lactated Ringer’s inj or 5% dextrose in water, then further dilute to reach final volume of 50 mL. IV infusion (loading dose and continuous infusion): Reconstitute 2 vials labelled as 40 mg with 5 mL normal saline each, then further dilute the 2 vials in 100 mL normal saline.
Contraindications
Concomitant use with rilpivirine, atazanavir, and nelfinavir.
Special Precautions
Patient with gastric malignancy, reduced body stores or risk factors for reduced vitamin B12 absorption, or those at risk of fractures and osteoporosis. Severe renal and hepatic impairment. Children. Pregnancy and lactation. CYP2C19 ultrarapid metabolisers.
Adverse Reactions
Significant: Hypomagnesaemia, osteoporosis-related fractures, fundic gland polyp, subacute cutaneous lupus erythematosus, SLE, acute interstitial nephritis, atrophic gastritis, Clostridium difficile-associated diarrhoea, gastrointestinal infections (e.g. Salmonella, Campylobacter), vitamin B12 deficiency (long-term therapy).
Blood and lymphatic system disorders: Rarely, leucopenia, thrombocytopenia.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Flatulence, diarrhoea, nausea, abdominal pain, vomiting, constipation, xerostomia.
General disorders and admin site conditions: Inj site reactions, fever, malaise.
Hepatobiliary disorders: Increased liver enzymes. Rarely, hepatitis.
Immune system disorders: Rarely, hypersensitivity reactions (e.g. angioedema, anaphylactic shock, urticaria).
Investigations: Altered thyroid hormone levels, increased gastrin, increased serum creatinine.
Metabolism and nutrition disorders: Peripheral oedema. Rarely, hyponatraemia.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, weakness.
Nervous system disorders: Headache, dizziness, drowsiness, vertigo, paraesthesia.
Psychiatric disorders: Insomnia, agitation, confusion, depression.
Reproductive system and breast disorders: Very rarely, gynaecomastia.
Respiratory, thoracic and mediastinal disorders: Cough, bronchospasm.
Skin and subcutaneous tissue disorders: Pruritus, rash, dermatitis. Rarely, alopecia.
Pregnancy Category (US FDA)
IV/Parenteral/PO: C
Patient Counseling Information
This drug may cause dizziness and blurred vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor serum Mg levels prior to treatment initiation and periodically thereafter. Assess for signs or symptoms of rebleeding, bone fractures, and Clostridium difficile-associated diarrhoea (CDAD).
Overdosage
Symptoms: Weakness, confusion, headache, drowsiness, tachycardia, nausea, diaphoresis, flushing, dry mouth and other gastrointestinal symptoms. Management: Symptomatic and supportive treatment.
Drug Interactions
Increased risk of digoxin-induced cardiotoxic effects. May diminish the therapeutic effects of clopidogrel. Increased risk of hypomagnesaemia with diuretics. May increase serum concentrations of tacrolimus, methotrexate, cilostazol, and drugs metabolised by CYP2C19 (e.g. diazepam, citalopram, imipramine, phenytoin). May reduce absorption of ketoconazole, itraconazole, Fe salts, erlotinib. Concomitant use with warfarin may increase INR and prothrombin time. Esomeprazole serum levels may be decreased with CYP2C19 or CYP3A4 inducers (e.g. rifampicin) and increased with CYP3A4 inhibitors (e.g. voriconazole, clarithromycin). May prolong elimination half-life of cisapride.
Potentially Fatal: May substantially decrease the serum levels of atazanavir, nelfinavir, or rilpivirine which may lead to the development of drug resistance.
Food Interaction
Decreased serum concentrations with St. John’s wort.
Lab Interference
May increase serum chromogranin A (CgA) levels causing false-positive result in diagnostic test for neuroendocrine tumours.
Action
Description: Esomeprazole, the S-isomer of omeprazole, is a substituted benzimidazole proton pump inhibitor (PPI) that blocks the final step in gastric acid secretion by specific inhibition of H+/K+-ATPase enzyme system present on the secretory surface of the gastric parietal cells.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Delayed and reduced absorption with food. Bioavailability: Approx 64% (single dose); approx 89% (repeated dose). Time to peak plasma concentration: Approx 1-2 hours.
Distribution: Plasma protein binding: Approx 97%.
Metabolism: Extensively metabolised in the liver primarily by CYP2C19 isoenzyme to form inactive hydroxy and desmethyl metabolites, and to a lesser extent by CYP3A4 isoenzyme to sulfone metabolite.
Excretion: Mainly via urine (approx 80% as inactive metabolites; <1% as unchanged drug); faeces (20%). Elimination half-life: Approx 1-1.5 hours.
Chemical Structure
Storage
Store between 20-25°C. Protect from light and moisture.
ATC Classification
A02BC05 - esomeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
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