Ezium (Esomeprazole ) 20mg , 40 mg capsules ...pharmacyteach

                        

   Ezium (Esomeprazole ) 20mg , 40 mg capsules 

Ezium (Esomeprazole ) 20mg , 40 mg capsules ...pharmacyteach .


DESCRIPTION:- 

Due to the acid nature of the medium capsule, the esomeprazole is enteric-coated with magnesium. Esomeprazole is reduced gastric acid secretion more effectively than omeprazole.
The molecular formula of esomeprazole is (C17H16 N3O3S)Mg.3H2O and the structural formula is :


 the structural formula of esomeprazole.



Mechanism of action:- 

                                                  Esomeprazole binds irreversibly to the H+/k+ ATPase in the proton pump. Because the proton pump is the end pathway of secretion of HCL from parietal cells in the stomach. In this way, it decreases the secretion of HCL into the stomach and alters gastric pH. 


Therapeutic indication:-

              Ezio capsule (esomeprazole)  is used for : 

1 . Gastroesophageal reflux disease (GERD)  - the cure of erosive reflux esophagitis- long-term management of patients with healed esophagitis prevents relapse. 

2 . As a triple therapy( amoxicillin and clarithromycin + esomeprazole) for the complete killing or distraction of H-pylori use for duodenal ulcer associated with Helicobacter pylori infection. 
 Preventing peptic ulcer in patients with Helicobacter pylori.

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 Pharmacokinetics:- 


Absorption:-

                    After oral administration maximum plasma level(Cmax) occurs at approximately 1.5 hours.  the ( Cmax) increase opportunity when the dose has increased and there is a three-fold increase in area under the plasma concentration-time curve from 20 to 40 mg at repeated once Daily dosing With  40 mg the system bioavailability is approximately 90%. 

Distribution;-

                    esomeprazole has 97% bound to the plasma protein. protein binding ata constant over the concentration range of 2 to 20 umol/L  the Apparent volume of distribution at a steady state in healthy volunteers is approximately 16 L.

Metabolism:-  

                    The cytochrome P450 (CYP) enzyme system is responsible for metabolizing the esomeprazole extensively in the liver. the metabolites of esomeprazole lack antisecretory activity .\

Excretion:- 

                 Total plasma clearance is about 17 L/h after one dose and about 9 L/h after repeated administration.  The half-life of esomeprazole is approximately 1-1.5 hours. 
less than 1% of the parent drug is excreted in the urine.

Dosage and administration:- 

                                           the recommended adult dosage is outlined in the table below. Ezium capsules should be administered whole and taken at least one hour before meals. 



Indication                                       Dose                                   Frequency     

1 . Gastroesophageal Reflux                            40mg once daily for 4 to 8 weeks.
 Disease healing of resolve or esophagitis.                                          20mg 


2. symptomatic gastroesophageal           40 mg once daily for 4 to 8 weeks.
    reflux disease without esophagitis         or 
                                                                  20mg 



Contraindication:- 
                            EZIUM (esomeprazole ) is not used in patients with known hypersensitivity to drugs.


ADVERSE  effects:-          
       
Common : 
 Headache, 
abdominal pain, 
diarrhea, 
flatulence,
 nausea, 


Uncommon

Dermatitis,
 pruritus, 
urticaria, 
Dizziness,
 dry mouth.


Rare : 
 Hypersensitivity reaction e.g. angioedema, anaphylactic reaction. 








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