Progut MUPS Tablet: An Advanced Proton Pump Inhibitor (Esomeprazole)

Progut MUPS tablet contains Esomeprazole in a Multiple-Unit Pellet System (MUPS) formulation. It is a proton pump inhibitor (PPI) designed to effectively suppress gastric acid secretion and is indicated for various acid-related gastrointestinal conditions.

Understanding MUPS Technology

MUPS stands for Multiple-Unit Pellet System. In pharmaceutical terms, it generally refers to tablets formed by compacting modified-release coated multiparticulates or pellets. This technology combines the advantages of both tablets and pellet-filled capsules in one dosage form, offering several benefits:

• Greater bioavailability: More of the drug is absorbed into the bloodstream.
• Uniform emptying: Micro-pellets empty uniformly from the stomach into the small intestine.
• Rapid dissolution & release: Facilitates quick dissolution of the enteric coating and drug release, leading to earlier peak plasma levels (Tmax​) and peak concentration (Cmax​).
• Lesser possibility of dose dumping: Reduces the risk of sudden, uncontrolled release of the entire drug dose.
• Combination of fast and sustained action: Provides both immediate and prolonged effects.
• Uniform drug release and absorption: Leads to consistent and controlled pharmacological action.
• Lesser chance of localized irritation: Due to uniform dispersion.
• Better and more uniform drug absorption: Improves overall efficacy.
• Reduced esophageal residence time: Better than capsules for patients.
• Minimizes fluctuation in plasma concentration of drug.

How Progut MUPS Works (Pharmacology)

Esomeprazole, the active ingredient in Progut MUPS, is a proton pump inhibitor. It suppresses gastric acid secretion by specifically blocking the hydrogen-potassium adenosine triphosphatase (H+/K+-ATPase) enzyme system (the proton pump) located in the gastric parietal cells of the stomach. This enzyme is the final common pathway for acid secretion.

Esomeprazole (the S-isomer of omeprazole) is a single optical isomer PPI, designed to provide superior acid control compared to racemic (mixture of S- and R-isomers) proton pump inhibitors.

Key Indications & Benefits

Progut MUPS is indicated for:

• Gastro-esophageal Reflux Disease (GERD), including the healing of erosive esophagitis and maintenance of healing.
• Risk reduction in NSAID-associated gastric ulcer.
• H. pylori eradication (Triple therapy) in combination with antibiotics.
• Zollinger-Ellison syndrome and idiopathic hypersecretion (conditions characterized by excessive stomach acid production).

Dosage & Administration

Progut MUPS tablets should be swallowed whole with liquid. They should not be chewed or crushed. Always consult a registered physician for medication use.

If swallowing whole is difficult, the tablets can be dispersed:

• Add the tablet to half a glass of non-carbonated water (mineral water is not suitable).
• Stir until the tablet disintegrates, then drink immediately or within 30 minutes.
• Rinse the glass with half a glass of water and drink.
• The pellets must not be chewed or crushed.

Oral Dosage:

• Erosive esophagitis:
  • Adults (≥18 years): 40 mg once daily for 4 weeks.
  • Children & adolescents (12-18 years): 40 mg once daily for 4 weeks.
• Maintenance of healing of erosive esophagitis:
  • Adults (≥18 years): 20 mg once daily.
  • Children & adolescents (12-18 years): 20 mg once daily.
• Risk reduction in NSAID associated gastric ulcer:
  • Adults (≥18 years): 20 mg once daily for 4-8 weeks.
• H. pylori eradication (Triple therapy with 1000 mg Amoxicillin and 500 mg Clarithromycin):
  • Adults (≥18 years): 20 mg twice daily for 7 days.
  • Children & adolescents (12-18 years): 20 mg twice daily for 7 days.
• Zollinger-Ellison syndrome and idiopathic hypersecretion:
  • Adults (≥18 years): 40-80 mg twice daily.

Pediatric Dosage (1-11 years):

• Erosive esophagitis:
  • Weight <20 kg: 10 mg once daily for 8 weeks.
  • Weight ≥20 kg: 10 mg or 20 mg once daily for 8 weeks.
• Maintenance of healing of erosive esophagitis: 10 mg once daily.
• Children below 1 year of age: Progut MUPS tablet is not approved for use.

Important Considerations & Warnings

It is crucial to discuss your full medical history with your doctor before taking Progut MUPS.

Contraindications:

• Patients with known hypersensitivity to Esomeprazole or any of the formulation components.

Side Effects:

• The most frequently reported adverse events include headache, diarrhea, nausea, flatulence, abdominal pain, constipation, and dry mouth.
• The types of adverse events seen during maintenance treatment (up to 12 months) are similar to those seen during short-term treatment.

Pregnancy & Lactation:

• Pregnancy: The manufacturer advises caution. There are no adequate and well-controlled studies in pregnant women. Animal studies have not revealed teratogenic effects. Use only if clearly essential and the therapeutic benefits outweigh possible risks.
• Lactation: It is not known if Esomeprazole or its metabolites appear in human breast milk. Therefore, breast-feeding should be discontinued if the use of Esomeprazole is considered essential.

Precautions & Warnings:

• Liver and Renal Dysfunction: Progut MUPS should be used carefully if the patient has severe liver dysfunction and severe renal impairment.
• Gastric Malignancy: Symptomatic response to therapy with Progut MUPS does not preclude the presence of gastric malignancy.
• Bone Fracture Risk: Taking a proton pump inhibitor like Progut MUPS may slightly increase the risk of hip, wrist, and spine fracture, particularly with use over a period of more than one year.

Drug Interactions:

Esomeprazole is extensively metabolized in the liver by CYP2C19 (major) and CYP3A4.

• No clinically relevant interactions expected with: Drugs metabolized by CYPs 1A2, 2A6, 2C9, 2D6, 2E1, and 3A4, as Progut MUPS is not likely to inhibit these enzymes.
• No clinically significant interactions found with: Phenytoin, warfarin, quinidine, clarithromycin, or amoxicillin.
• Potential Interference with CYP2C19:
  • Diazepam: Co-administration of Progut MUPS 30 mg with diazepam (a CYP2C19 substrate) resulted in a 45% decrease in clearance of diazepam, leading to increased plasma levels 12 hours after dosing and onwards.
• Interference with Drug Absorption (due to reduced gastric pH): Progut MUPS inhibits gastric acid secretion, which may interfere with the absorption of drugs where gastric pH is important for bioavailability (e.g., ketoconazole, iron salts, and digoxin).
• Oral contraceptives, diazepam, phenytoin, or quinidine: Co-administration does not seem to change the pharmacokinetic profile of Progut MUPS.
• Combination Therapy with Clarithromycin and Amoxicillin: Results in increases in the plasma levels of Progut MUPS and 14-hydroxyclarithromycin.

Overdose Effects:

• While there are no reports of overdose with Progut MUPS in humans, high single oral doses were lethal in rats.
• Major signs of acute toxicity in animals were reduced motor activity, changes in respiratory frequency, tremor, ataxia, and intermittent clonic convulsions.
• No specific antidote is known.
• Since Esomeprazole is extensively protein-bound, it is not expected to be removed by dialysis.
• In case of overdosage, treatment should be symptomatic and supportive. The possibility of multiple drug ingestion should also be considered.

Storage Conditions

Store in a cool & dry place below 25°C, protected from light. Keep out of reach of children.