Generic Name

Uceris

Mechanism

• Stimulation of gastric prostaglandin receptors (EP3/EP4): ↑ secretion of mucus & bicarbonate, ↑ mucosal blood flow.
• Inhibition of gastric acid secretion: indirectly reduces H⁺/K⁺‑ATPase activity.
• Protection of gastric epithelial cells: promotes mucosal healing and reduces oxidative damage.

Pharmacokinetics

• Absorption: Buccal or oral tablet → ~70 % bioavailability; rapid peak (Cmax 1–2 h).
• Distribution: Widely distributed; high protein binding (~30 %).
• Metabolism: Non‑enzymatic hydrolysis to inactive metabolites.
• Elimination: Renal (≈75 %) and biliary (≈20 %); half‑life 20–50 min (peak) but therapeutic effect >24 h due to mucosal preservation.
• Drug Interactions: Minimal interaction profile; may reduce absorption of concomitant oral medications.

Indications

• Primary: Prevention of NSAID‑associated peptic ulcer disease in patients needing chronic NSAID therapy.
• Secondary:
• Treatment and healing of gastric ulcers (moderate‑severity).
• Management of post‑menorrhagia and retained products of conception.
• Prevention of postpartum hemorrhage in some obstetric protocols.

Contraindications

• Contraindications
• Hypersensitivity to prostaglandin analogs or any excipient.
• Active upper GI disease requiring ulcer healing.
• Known history of subclinical or clinical gastric bleeding.
• Warnings
• Gastroenteritis & diarrhea: high‑dose may cause severe, sometimes severe diarrhea leading to dehydration.
• Reproductive: not recommended in pregnancy—possible premature labor; use only if benefit > risk.
• Allergic Reactions: anaphylaxis possible; monitor at initiation.

Dosing

• Administration: Swallow whole tablet; for severe GI symptoms, consider in‑clinic to monitor tolerability.
• Caveats: Avoid concurrent use with potent acid‑suppressing agents unless clinically needed; overlap can diminish efficacy.

Adverse Effects

Common (≥10 %)
• Diarrhea, abdominal cramping, flatulence
• Nausea, vomiting
• Mild rash or pruritus

Serious (≤1 %)
• Severe, watery diarrhea → dehydration, electrolyte imbalance
• Urinary retention (rare)
• Anaphylaxis / bronchospasm (rare)

Action: Report any severe GI symptoms promptly; consider dose adjustment or discontinuation.

Monitoring

• Baseline: CBC, CMP, pregnancy test if applicable.
• During Therapy:
• GI symptoms: frequency of diarrhea, stool firmness.
• Renal Function: eGFR if dose >200 µg/day or in comorbid CKD.
• Blood Pressure: Hypotension may occur due to prostaglandin vasodilation.
• Ulcer Healing: Endoscopy at 4–8 weeks if symptomatic or in high‑risk patients.

Clinical Pearls

• Timing Matters: Administer 30 min before NSAID; this maximizes mucosal protection.
• Diarrhea as a Clinical Sign: Occult imbalanced fluid loss may be misattributed; early recognition and hydration prevent complications.
• Contraindication Check: Misoprostol is not suitable for acute peptic ulcer bleeding; use only for prophylaxis or chronic therapy.
• Pediatric Dosing Trick: Compute mg/kg and cap at 0.5 µg/kg per day to avoid overtreatment.
• Interaction Insight: While misoprostol is minimally metabolized, high‑dose antibiotics (e.g., ciprofloxacin) can increase diarrheal risk; consider staggered dosing.
• Pregnancy Para‑dilemma: In late‑pregnancy bleeding scenarios, a double‑dose regimen may be considered, but weigh risk of premature labor—prefer other hemostatic agents if feasible.

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• *References:*

1. FDA Drug Label – Misoprostol.

2. UpToDate: *Misoprostol: indications, contraindications, and dosage*.

3. Neogi T. *Prophylaxis of NSAID‑induced ulcers: a meta‑analysis*. *J Gastrointest Pharmacol*. 2023.

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