1. NEXIUM HISTORY
How was Nexium discovered?

AstraZeneca discovered Nexium by making slight alteration in the formula for Prilosec (omeprazole).

Note: World-drugs.net sells generic version of Nexium

2. NEXIUM FACTS
Nexium is a product of Astra-Zeneca Internationa.

Astra-Zeneca is one of the world's leading pharmaceutical companies with 60,000 people - 12,000 in the US alone - dedicated to the discovery, development, and marketing of new pharmaceutical solutions, to enrich the quality of people's lives all over the world.

The focused areas of research include:

• Cardiovascular
• Gastrointestinal
• Infection
• Neuroscience
• Oncology
• Respiratory

Astra-Zeneca discovers new medicines that are designed to improve the health and quality of life of patients around the world - medicines which are innovative, effective and which offer added benefits such as reduced side effects or better ways of taking the treatment. Astra-Zeneca also focuses on getting the best from every medicine they make by exploring all the ways it can be used or improved.

At Astra-Zeneca, innovation is about more than just research.

3. ABOUT NEXIUM MEDICATION

Nexium contains the active ingredient esomeprazole, which is a type of medicine called a Proton Pump Inhibitor.

Proton Pumps are found on cells that line the stomach and are used by these cells to produce stomach acid. Nexium works by inhibiting the action of the Proton Pumps, and this reduces the production of stomach acid.

Acid is produced in the stomach as a normal part of the digestive process. However, in the condition known as gastro-oesophageal reflux disease or acid reflux, this acid is allowed to flow back into the food pipe (oesophagus), where it causes pain and a burning sensation known as heartburn. The acid can also irritate and cause inflammation of the lining of the foodpipe (reflux oesophagitis).

Nexium reduces the production of stomach acid and thus reduces acid flowing back into the foodpipe. It is used to relieve the symptoms of gastro-oesophageal reflux disease, such as heartburn. Nexium is also used to treat reflux oesophagitis, because stopping the acid flowing back into the foodpipe allows the lining of the foodpipe to heal. Nexium is also used for the long-term management of people with healed oesophagitis, as suppressing the production of stomach acid helps prevent this condition recurring.

Nexium is also used to treat ulcers in the stomach or upper intestine (peptic ulcers) that are associated with a type of bacteria called Helicobacter pylori. This type of bacteria is the most common cause of peptic ulcers. The bacteria cause the stomach to produce too much acid, which irritates the lining of the stomach and upper intestine and causes ulcers.

Nexium is used in combination with antibiotics to eradicate Helicobacter pylori from the gut. The esomeprazole creates an environment in the gut in which the antibiotics can work effectively against the H pylori bacteria. The reduced acid in the gut allows the ulcer to heal, and both actions help prevent the ulcer from recurring.

Nexium can also be used to prevent and treat peptic ulcers that can occur as a side effect of non-steroidal anti-inflammatory drugs (NSAIDs), such as diclofenac, often used to treat arthritis.

Diagrams to explain the mechanism of action of Nexium

The Digestive System

If you have GERD (the abbreviation for gastro-oesophageal reflux disease, also known as acid reflux disease) the LES opens at inappropriate times, allowing harsh stomach acid to back up into your esophagus.

4.NEXIUM EFFECTIVENESS
When is Nexium best taken?

Take Nexium capsules by mouth. Follow the directions on the prescription label. Swallow the capsules whole with a drink of water; do not crush, break or chew. The capsules can be opened and the contents sprinkled on applesauce or yogurt, given with fruit juices, or swallowed immediately with water. Do not crush the contents into the food. Nexium works best if taken on an empty stomach at least one hour before a meal. Take your Nexium doses at regular intervals. Do not take Nexium more often than directed.

Absorption
Nexium Delayed-Release Capsules contain an enteric-coated pellet formulation of esomeprazole magnesium. After oral administration peak plasma levels occur at approximately 1.5 hours.

The concentration increases proportionally when the Nexium dose is increased 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 Nexium dose of 40 mg.

Nexium should be taken at least one hour before meals.

The pharmacokinetic profile of Nexium was determined in 36 patients with symptomatic gastro-oesophageal reflux disease following repeated once daily administration of 20 mg and 40 mg capsules of Nexium over a period of five days.

Distribution
Nexium is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2-20 µmol/ L.

Metabolism
Nexium is extensively metabolized in the liver by the cytochrome enzyme system. The metabolites of Nexium lack antisecretory activity. The major part of Nexium's metabolism is dependent upon the isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on another enzyme, which forms the sulphone metabolite.

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

5. NEXIUM EFFECTS ON SPECIAL POPULATION
How do different people react to Nexium?

Geriatric
The concentration was slightly higher in the elderly as compared to younger subjects at steady state. Dosage adjustment based on age is not necessary.

Pediatric
The pharmacokinetics of Nexium have not been studied in patients < 18 years of age.

Gender
The concentration was slightly higher in females than in males at steady state. Dosage adjustment based on gender is not necessary.

6. NEXIUM EFFECTS ON MEDICAL CONDITIONS
How does Nexium affect your existing condition/ailment?

Hepatic Insufficiency
In patients with severe hepatic insufficiency the concentrations were 2 to 3 times higher than in the patients with normal liver function. 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
The pharmacokinetics of Nexium in patients with renal impairment are not expected to be altered to healthy volunteers as less than 1% of Nexium is excreted unchanged in urine.

7. OTHER/ALTERNATE USES OF NEXIUM
What else does Nexium treat?

Nexium is approved for the treatment of gastroesophageal reflux disease (GERD) and in combination with amoxicillin and clarithromycin (Biaxin) for the treatment of patients with ulcers and H. pylori infection.

Since it is very similar to omeprazole, it also is likely that Nexium will be used for the treatment of Zollinger-Ellison syndrome.

8. ADVERSE/SIDE EFFECTS of NEXIUM
What are the side effects of Nexium?

The safety of Nexium was evaluated in over 10,000 patients (aged 18-84 years) in clinical trials worldwide including over 7,400 patients in the United States and over 2,600 patients in Europe and Canada. Over 2,900 patients were treated in long-term studies for up to 6-12 months. In general, Nexium was well tolerated in both short and long-term clinical trials.

The safety in the treatment of healing of erosive esophagitis was assessed in four randomized comparative clinical trials, which included 1,240 patients on Nexium 20 mg and 2,434 patients on Nexium 40 mg. The most frequently occurring adverse events in all three groups were headache and diarrhea (no difference among the three groups). Nausea, flatulence, abdominal pain, constipation, and dry mouth occurred at similar rates among patients taking Nexium.

Additional adverse events that were reported as possibly or probably related to Nexium with an incidence < 1% are listed below by body system:

Body as a Whole: abdomen enlarged, allergic reaction, asthenia, back pain, chest pain, chest pain substernal, facial edema, peripheral edema, hot flushes, fatigue, fever, flu-like disorder, generalized edema, leg edema, malaise, pain, rigors;

Cardiovascular: flushing, hypertension, tachycardia;

Endocrine: goiter;

Gastrointestinal: bowel irregularity, constipation aggravated, dyspepsia, dysphagia, dysplasia GI, epigastric pain, eructation, esophageal disorder, frequent stools, gastroenteritis, GI hemorrhage, GI symptoms not otherwise specified, hiccup, melena, mouth disorder, pharynx disorder, rectal disorder, serum gastrin increased, tongue disorder, tongue edema, ulcerative stomatitis, vomiting;

Hearing: earache, tinnitus;

Hematologic: anemia, anemia hypochromic, cervical lymphoadenopathy, epistaxis, leukocytosis, leukopenia, thrombocytopenia;

Hepatic: bilirubinemia, hepatic function abnormal, SGOT increased, SGPT increased;

Metabolic/Nutritional: glycosuria, hyperuricemia, hyponatremia, increased alkaline phosphatase, thirst, vitamin B12 deficiency, weight increase, weight decrease;

Musculoskeletal: arthralgia, arthritis aggravated, arthropathy, cramps, fibromyalgia syndrome, hernia, polymyalgia rheumatica;

Nervous System/Psychiatric: anorexia, apathy, appetite increased, confusion, depression aggravated, dizziness, hypertonia, nervousness, hypoesthesia, impotence, insomnia, migraine, migraine aggravated, paresthesia, sleep disorder, somnolence, tremor, vertigo, visual field defect;

Reproductive: dysmenorrhea, menstrual disorder, vaginitis;

Respiratory: asthma aggravated, coughing, dyspnea, larynx edema, pharyngitis, rhinitis, sinusitis;

Skin and Appendages: acne, angioedema, dermatitis, pruritus, pruritus ani, rash, rash erythematous, rash maculo-papular, skin inflammation, sweating increased, urticaria;

Special Senses: otitis media, parosmia, taste loss, taste perversion;

Urogenital: abnormal urine, albuminuria, cystitis, dysuria, fungal infection, hematuria, micturition frequency, moniliasis, genital moniliasis, polyuria;

Visual: conjunctivitis, vision abnormal.

Endoscopic findings that were reported as adverse events include: duodenitis, esophagitis, esophageal stricture, esophageal ulceration, esophageal varices, gastric ulcer, gastritis, hernia, benign polyps or nodules, Barrett's esophagus, and mucosal discoloration.

The incidence of treatment-related adverse events during 6-month maintenance treatment was similar to placebo. There were no differences in types of related adverse events seen during maintenance treatment up to 12 months compared to short-term treatment.

Two placebo-controlled studies were conducted in 710 patients for the treatment of symptomatic gastroesophageal reflux disease (GERD). The most common adverse events that were reported as possibly or probably related to Nexium were diarrhea (4.3%), headache (3.8%), and abdominal pain (3.8%).

There have been spontaneous reports of adverse events with post marketing use of Nexium. These reports have included rare cases of anaphylactic reaction.

9. USEFUL LINKS

http://www.astrazeneca.com

http://www.purplepill.com/

http://www.pdrhealth.com/

http://www.drugs.com

http://www.healthscout.com

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