Nexol 20
For stomach and duodenum Ulcer
  • Esomeprazole, is a new proton pump inhibitor. It is the S-isomer of omeprazole and is the first such inhibitor to be developed as a single isomer.
  • Esomeprazole reduces gastric acid secretion through a specific targeted mechanism of action.It’s a specific inhibitor of the acid proton pump in the parietal cell where it inhibits the enzyme H+,K+-ATpase and inhibit both basal and stimulated acid secretion. Both the R-and S-isomer of omeprazole have similar pharmcodynamic activity.
  • Absorption of Esomeprazole is rapid with peak plasma levels occurring approximately 1- 2 hours after oral dose. The absolute bioavailability is 64% after a single dose of 40mg and increases to 89% after repeated once daily administration. For 20mg of Esomeprazole the corresponding values are 50% and 68% respectively .The apparent volume of distribution at steady state in healthy subjects is approximately 0.22L/kg of body weight.
  • Esomeprazole is 97% plasma protein bound.
  • Food intake both delays and decreases the absorption of Esomeprazole although this has no significant influence on the effect of Esomeprazole on intragastric acidity.
  • Esomeprazole is completely metabolised in the liver by the cytochrome P450 system .The major part of the metabolism of Esomeprazole is dependent on the polymorphic CYP2C19 responsible for the formation of hydroxy and desmethyl metabolites of Esomeprazole. The remaining part is dependent on another specific (isoform), CYP3A4, responsible for the formation of Esomeprazole sulphone main metabolite in plasma. The major metabolites of Esomeprazole have no effect on the gastric acid secretion.
  • The plasma clearance is about 17L/h after a single dose and about 9L/h after repeated administration.The plasma elimination half-life is about 1.3 hours after repeated once daily dosing.
  • Esomeprazole is completely eliminated from plasma between doses with no tendency for accumulation during once- daily administration 
  • Almost 80% of an oral dose of Esomeprazole is excreted as metabolites in urine, the remainder in the faces. Less than 1% of the parent drug is found in urine.

Each enteric coated tablet of Nexol® 40 contains:

  • Esomeprazole 40mg (as Magnesium Trihydrate).

Each enteric coated tablet of Nexol®  20 contains:

  • Esomeprazole 20mg (as Magnesium Trihydrate)

Each capsule of Nexol®  40 contains:

  • Esomeprazole 40mg enteric coated pellets (as Magnesium Trihydrate).

Each capsule of Nexol®  20 contains:

  • Esomeprazole 20mg enteric coated pellets (as Magnesium Trihydrate).

Nexol® is indicated  for:
¤ Treatment of Gastroesophageal Reflux Disease (GERD)

  • Healing of Erossive Esophagitis.
  • Nexol® is indicated for the short-term treatment (4 - 8 weeks) in the healing and symptomatic resolution of erosive esophagitis. For those patients who have not healed after 4 - 8 weeks of treatment, an additional 4 - 8 week course of Nexol® may be considered.
  • Maintenance of healing of erossive esophagitis.
  • Prevention of relapse of esophagitis.

¤ H.pylori Eradication to reduce the risk of peptic ulcer recurrence.

¤ Nexol® in combination with an appropriate anti-bacterial therapeutic regimen is indicated for healing or prevention relaps of peptic ulcer in patients with Helicobacter pylori associated ulcers.

  • Nexol® is contraindicated in patient with known hypersensitivity to any component of the formulation or to substituted benzimidazoles.
  • In patient with known hypersensitivity to penicillins, or macrolide antibiotics, should not be given Nexol® for treating H.pylori.
  • Nexol® inhibits gastric acid secretion. Therefore, it may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g, Ketoconazole, Itraconazole,  Iron salts and Digoxin)
  • Nexol® inhibits CYP2C19, thus, when it  is combined with drugs metabolised by CYP2C19 such as( Diazepam, Citalopram, Imipramine, Clomipramine& Phenytoin ) the plasma concentrations of these drugs may increase and dose reduction could be needed .This should be especially when prescribing Nexol® for on-demand therapy .
  • Concomitant administration of Nexol® warfarin treated patients, a few isolated cases of elevated INR of clinical significance have been reported. Monitoring is recommended when initiating and ending concomitant treament .
  • Caution should be exercised when Nexol® prescribing to pregnant women and should not be used during breast –feeding.

¤ Nexol® was well tolerated in both short and long –term clinical trials.

¤ The following side effects have been identified.None was found to be dose- related:

  • Common: headache, abdominal pain, diarrhea, flatulence, nausea, vomiting and constipation.  
  • Uncommon: Dermatitis, pruritus, urticaria, dizziness and dry mouth.   
  • Rare: Hypersensitivity reactions.

¤ Nexol® is recommended to be taken before eating and should be swallowed completely with liquid 

Gastroesophageal Reflux Disease (GERD):

  • Healing of Erossive Esophagitis: 20 mg or 40 mg once daily for 4 to 8 weeks
  • Maintenance of healing of Erossive Esophagitis: 20 mg once daily
  • prevention of relapse of Esophagitis: 20 mg once daily

 Treatment should not extend beyond 6 month.

H. pylori  Eradication to Reduce the Risk of Peptic Ulcer Recurrence: (Triple Therapy)

  • NEXOL®: 40 mg Once daily for lo days
  • G - MOX®:1000 mg Twice daily lo days
  • KLARI® tab:500 mg Twice daily lo days
  • Symptomatic response to therapy with Nexol® does not preclude the presence of gastric malignancy should be excluded, as the treatment with Nexol® may alleviate symptoms and delay diagnosis .
  • Patient on long-term treatment (particulary those treated for more than a year) should be kept under regular surveillance.
  • Clarithromycin is a potent inhibitor of CYP3A4 and hence its contraindications and interactions should be considered when the triple therapy is used in patients concurrently taking other drugs metabolised via CYP3A4 such as Cisapride.
  • Patient on on-demand treatment should be instructed to contact their physicain if their symptoms change in character also the implications for interactions with other pharmaceuticals, due to fluctuating plasma concentration of Nexol® should be considered .
  • Patient with severe liver dysfunction, a maximum of 20mg of Nexol® should not be exceeded .
  • Patients with rare hereditary problems of fructose intolerance, glucose- galactose malabsorption or sucrose-isomaltase insufficiency should not take Nexol®.
  • Blister of 7 Tablets or capsules, pack of two blisters.
  • Store in a cool dry place below 30° C, protect from light.