Esomeprazole: Mechanism-Dosage forms-Indication-Dosage Guideline-Disease Profile
You will find detailed information about 'Esomeprazole: Mechanism-Dosage
forms-Indication-Dosage Guideline-Disease Profile' in this article. This
article clearly explains how this medicine works and for which conditions
it is used, in a simple way.
You will also get a clear understanding of the various dosage forms of
Esomeprazole and the dosage guidelines based on different diseases. All
the necessary aspects of its proper use are presented here. This content
will be a valuable resource for effective solutions to gastric problems.
Table of contents
Check out what you will learn from this blog-
Esomeprazole: Mechanism-Dosage forms-Indication-Dosage Guideline-Disease Profile
Esomeprazole is a proton pump inhibitor that helps reduce the secretion
of stomach acid. It is widely used as a safe and effective treatment for
gastric problems, GERD (gastroesophageal reflux disease), and peptic
ulcers.
It is typically taken once daily in 20 mg or 40 mg doses. Depending on
the patient's condition, it is available in tablet, capsule, and
injectable forms. When used correctly, Esomeprazole provides quick
relief and helps prevent long-term complications.
Esomeprazole Mechanism of action | Esomeprazole mode of action
Esomeprazole inhibits the H+/K+-ATPase in the Proton Pump of gastric parietal
cells, thus the concentration of H+ is decreased & also the formation of
HCl acid is reduced.
Step 1: Medicine intake
When a person takes an Esomeprazole tablet, it enters the body and becomes active.
Step 2: Targets gastric parietal cells
Esomeprazole works in the gastric parietal cells of the stomach, which are responsible for acid production.
Step 3: Blocks the proton pump
Inside these cells, there is a special protein enzyme called H⁺/K⁺-ATPase, also known as the Proton Pump.
Esomeprazole blocks this pump.
Step 4: Reduces hydrogen ion (H⁺) secretion
When the proton pump is blocked, the H⁺ ions (hydrogen ions) cannot be released into the stomach.
Step 5: Decreases acid (HCl) formation
Since H⁺ and Cl⁻ (chloride) combine to form HCl (hydrochloric acid), a reduction in H⁺ leads to less acid production.
Step 6: Relief from acidity-related problems
Because stomach acid is reduced, conditions like gastritis, acid reflux, and ulcers improve, giving relief to the patient.
In summary: Esomeprazole blocks the proton pump in stomach cells, which reduces acid production and helps relieve acid-related stomach problems.
Various dosage forms and strengths of Esomeprazole
Tablet | 20mg |
Tablet | 40mg |
MUPS Tablet | 20mg |
MUPS Tablet | 40mg |
Capsule | 20mg |
Capsule | 40mg |
Inj (IV) | 40mg |
Major Indication
- Treatment of GERD.
- Healing of Erosive Esophagitis.
- Risk reduction of NSAID associated ulcer.
- Zollinger Ellision syndrome.
Indication & Dosage Guideline
Indication | Patient Category | Recommended Dose |
---|---|---|
GERD | Adults | 20 mg or 40 mg, once daily for 4 to 8 weeks. |
GERD | 12 to 17 years | 20 mg or 40 mg, once daily for up to 8 weeks. |
GERD | 1 to 11 years | 10 mg or 20 mg, once daily for up to 8 weeks. |
Risk Reduction of NSAID-Associated Gastric Ulcer | - | 20 mg or 40 mg, once daily for up to 6 months. |
H.pylori Eradication (Triple Therapy) | - | Esomeprazole 40 mg, once daily for 10 days Amoxicillin 1000 mg, twice daily for 10 days Clarithromycin 500 mg, twice daily for 10 days. |
Disease Profile
GERD: GERD stands for Gastroesophageal Reflux Disease which refers to
the backward movement of gastric content from the stomach into the
esophagus. When reflux leads to inflammation of the esophagus it is called
reflux (erosive) esophagitis.
Dyspepsia: It is defined as the persistent or recurrent abdominal
pain or abdominal discomfort centered in the upper duodenum.
Functional Dyspepsia (FD): FD is defined as the presence of symptoms
thought to originate in the gastroduodenal region in the absence of any
organic, systemic or metabolic disease.
Zollinger-Ellison syndrome: It is a serious form of peptic ulcer
disease (PUD). It occurs when one or more tumors form in the pancreas or
the upper part of the small intestine (duodenum). These tumors, called
gastrinomas, secrete large amounts of the hormone gastrin, which causes
the stomach to produce too much acid.
Heartburn: Heartburn is the substernal burning or regurgitation that
may radiate to the neck. Other symptoms of heartburn include: belching,
chest pain, asthma & chronic cough etc.
Parietal cell: Parietal cells are the epithelial cells that secrete
hydrochloric acid (HCI) and intrinsic factor. These cells are located in the
gastric glands found in the lining of the fundus and in the cardia of the
stomach.
Metabolism pathway of Esomeprazole (Maxima): Esomeprazole is
extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme
system. The major part of Esomeprazole metabolism is dependent upon the
CYP2C19 isoenzyme and the remaining amount is dependent on CYP3A4 enzyme.
Specialization
- GP
- Gastro
- Medicine
- Gynae
- Ortho
Maxima by ACME (Generic: Esomeprazole)
How long Maxima (Esomeprazole) maintains a sustained pH level?
Maintains intragastric pH>4 for a longer period of time 17.5 hours for
twice daily 20 mg dose and 19.2 hours for twice daily 40 mg dose.
Why is Maxima (Esomeprazole) the rational choice of drug for diabetic
patients (T2DM)?
PPIs (Esomeprazole) indirectly elevate serum gastrin levels via a negative
feedback effect. PPIs (Esomeprazole) improve glycemic control by enhancing
both serum levels of gastrin and ẞ cell mass. Most of the studies have
demonstrated a significant improvement of glycemic control by PPI
(Esomeprazole) administration to diabetic patients.
Why is Maxima (Esomeprazole) the rational choice of drug for the asthma
patient?
Acid reflux causes bronchoconstriction by micro aspiration into the
airways as well as by reflex-mediated effects of acid on the esophagus or
upper airway. Alternatively, asthmatic bronchoconstriction can induce acid
reflux. As Esomeprazole is indicated to control acid reflux, thus,
Esomeprazole is the rational choice of drug for the asthma patient.
FAQs
1. What are the common side effects of Esomeprazole?
Ans: Common side effects are: headache, diarrhea, and abdominal pain.
2. What is the pregnancy category of Esomeprazole?
Ans: Category B.
3. Is Esomeprazole safe for the lactating mother?
Ans: Yes, because maternal doses of 20 mg daily produce low levels in milk
and would not be expected to cause any adverse effects in breastfed
infants.
4. What is the pKa value of Esomeprazole?
Ans: pKa = 4.06
Conclusion
Having a clear understanding of 'Esomeprazole: Mechanism-Dosage
forms-Indication-Dosage Guideline-Disease Profile' ensures its correct
application based on the disease. Knowing the mechanism, dosage, and
disease-specific uses helps in effective and accurate consumption,
offering quick relief from gastric, GERD, and peptic ulcers. This is a
safe and effective medicine for treating gastric disorders. Always take
it as per your doctor's advice to get the maximum benefit from it.