PROTOLOC

Description

Protoloc Capsule (Omeprazole)

Indications:

• Peptic Ulcer (duodenal and gastric)
• Helicobacter pylori (H. pylori) infection (as part of combination therapy)
• Gastro-oesophageal Reflux Disease (GERD)
• Zollinger-Ellison Syndrome
• Oesophagitis (including erosive oesophagitis)
• Acid-Related Dyspepsia
• NSAID-Associated Ulceration
• Prophylaxis of acid aspiration during general anaesthesia

Dosage

Adults (Oral):

• Peptic Ulcer: 20 mg or 40 mg once daily in severe cases for 4 weeks (duodenal ulcer) or 8 weeks (gastric ulcer). Maintenance: 10-20 mg once daily. All doses should be taken once in the morning.
• NSAID-Associated Ulceration: 20 mg once daily in the morning.
• Gastro-oesophageal Reflux Disease (GERD): 20 mg once daily for 4 weeks; may continue for another 4-8 weeks if necessary. Refractory oesophagitis: 40 mg once daily. Maintenance: 20 mg once daily (after healing of oesophagitis); 10 mg once daily (for acid reflux). All doses should be taken once in the morning.
• Zollinger-Ellison Syndrome: Initially, 60 mg once daily in the morning, adjusted as required. Dose range: 20-120 mg/day. Doses >80 mg are administered in 2 divided doses.
• Prophylaxis of Acid Aspiration during General Anaesthesia: 40 mg given in the evening and another 40 mg 2-6 hours pre-operation.
• Acid-Related Dyspepsia: 10 mg or 20 mg once daily in the morning for 2-4 weeks.
• Erosive Oesophagitis: 20 mg once daily for 4-8 weeks. Maintenance of healing: 20 mg once daily for up to 12 months. All doses should be taken once in the morning.
• H. pylori Infection (Eradication Therapy):
  • Triple Therapy (7 or 10 days): 20 mg twice daily OR 40 mg once daily, combined with amoxicillin 500 mg and metronidazole 400 mg (both three times daily); OR combined with clarithromycin 250 mg and metronidazole 400 mg (or tinidazole 500 mg) (both twice daily); OR combined with amoxicillin 1 g and clarithromycin 500 mg (both twice daily).
  • 2-week Dual Therapy: 20 mg twice daily OR 40 mg once daily, combined with either amoxicillin 750 mg to 1 g twice daily OR with clarithromycin 500 mg three times daily.

Adults (Intravenous – IV):

• Gastro-oesophageal Reflux Disease; Gastric and Duodenal Ulcers; NSAID-associated Ulceration: 40 mg once daily infused over 20-30 minutes or slow injection over 5 minutes until oral administration is possible.
• Zollinger-Ellison Syndrome: Initially, 60 mg/day, adjusted according to response. Daily doses >60 mg/day should be given in 2 divided doses.

Children (Oral):

• GERD:
  • <1 year: Safety and efficacy not established.
  • $\ge$1 year:
    • 5-10 kg: 5 mg orally once daily.
    • 10-20 kg: 10 mg orally once daily.

    • 20 kg: 20 mg orally once daily.

• Erosive Oesophagitis (Treatment and Maintenance of Healing):
  • 1 month to <1 year:
    • 3 to <5 kg: 2.5 mg once daily.
    • 5 to <10 kg: 5 mg once daily.

    • 10 kg: 10 mg once daily. (May treat for up to 6 weeks).

  • 1-16 years:
    • 5 to <10 kg: 5 mg orally once daily.
    • 10 to <20 kg: 10 mg orally once daily.

    • 20 kg: 20 mg orally once daily. (May treat for 4-8 weeks).

Special Populations:

• Elderly: No dosage adjustment needed.
• Hepatic Impairment: 10-20 mg/day.
• Renal Impairment: No dosage adjustment needed.

Administration

• Delayed-release capsules/Powder for oral suspension: Should be taken on an empty stomach, at least 1 hour before meals. Swallow capsules whole; do not chew or crush. For patients with difficulty swallowing, capsules may be carefully opened and the entire contents sprinkled in a spoonful of applesauce. Swallow the drug/food mixture without chewing immediately after preparation. The drug/food mixture should not be stored for future use.
• MUPS tablet: May be taken with or without food.
• Capsule (general): Should be taken with food, immediately before a meal.

Contraindications

• Known hypersensitivity to omeprazole or any of its components.
• Concomitant use with rilpivirine, nelfinavir, and atazanavir due to potentially fatal interactions.

Precautions

• Gastric malignancy should be ruled out before initiating treatment.
• Pregnancy and Lactation: Use with caution; omeprazole distributes into human breast milk.
• Children: Use with caution in children <1 year unless specifically indicated.
• Monitoring Parameters: Monitor magnesium concentrations prior to initiation and periodically thereafter.

Interactions

• Increased Risk of: Hypomagnesaemia (with diuretics); increased INR and prothrombin time (with warfarin); digoxin-induced cardiotoxic effects; increased plasma concentration of benzodiazepines (e.g., diazepam), clarithromycin, and methotrexate.
• Decreased Absorption of: Itraconazole, ketoconazole, posaconazole, dasatinib, iron salts.
• May Prolong Elimination of: Diazepam, cilostazol, phenytoin, and ciclosporin.
• May Reduce the Antiplatelet Effect of: Clopidogrel.
• Potentially Fatal: May decrease plasma concentrations and pharmacological effects of rilpivirine, nelfinavir, and atazanavir.

Adverse Effects

• Common (1-10%): Headache, abdominal pain, diarrhea, nausea, vomiting, flatulence, dizziness, upper respiratory infection, acid regurgitation, constipation, rash, cough.
• Less Common (Frequency Not Defined): Bone fracture (osteoporosis-related), hepatotoxicity (rare), agranulocytosis, anorexia, gastric polyps, hip fracture, alopecia, atrophic gastritis, interstitial nephritis (rare), pancreatitis (rare), rhabdomyolysis, taste perversion, abnormal dreams, toxic epidermal necrolysis (rare).
• Potentially Fatal: Anaphylaxis.

Mechanism of Action

Omeprazole is a substituted benzimidazole gastric antisecretory agent, also known as a Proton Pump Inhibitor (PPI). It blocks the final step in gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system (the proton pump) present on the secretory surface of the gastric parietal cell. Both basal and stimulated acid production are inhibited.

Note: Protoloc 10mg Capsule is manufactured by Usv Ltd. Its generic name is Omeprazole. Protoloc is available in Nepal. This information is not intended for diagnosis, medical advice, or treatment; neither is it intended to be a substitute for the exercise of professional judgment