Pharmacology: Prostaglandin-increasing effect: The drug has the effect of increasing the PGE2 content in the gastric mucosa and protected the gastric mucosa from injury caused by Ethanol loading.
Cytoprotective effect: The drug inhibits gastric mucosal injury induced by Aspirin, Ethanol, or HCl-ethanol loading.
Effect on inflammatory cytokine release (interleukin-8) in the gastric mucosa Rebamipide, taken by the oral route, suppressed the increase production of interleukin-8 in the mucosa of patients with Helicobacter pylori. The drug also inhibited the activation of NF-κB and suppressed the expression of interleukin-8 mRNA in epithelial cells cocultured with Helicobacter pylori (in vitro).
Pharmacokinetics: Plasma Concentration: The Table 1 shows the pharmacokinetic parameters of Rebamipide following
single oral administration of Rebamipide tablets at the dose 100 mg in a fasted state.
Pharmacokinetic Parameters of Rebamipide: (See Table 1.)
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The absorption of Rebamipide following single oral administration at a dose of 150 in a fed state tended to be slower than that in a fasted stage. However, food did not affect bioavailability of the drug in humans. Pharmacokinetic parameters obtained from patients with renal impairment after single oral administration of Rebamipide at 100 mg revealed higher plasma concentrations and a longer elimination half-life compared with those in healthy subjects. At steady-state, Rebamipide plasma concentrations observed in dialyzed renal patients following repeated administration were very close to the values simulated from single administration. Therefore, the drug was not considered to accumulate.
Metabolism: Rebamipide was primarily excreted as the unchanged compound in the urine after single oral administration to healthy adult males at a dose of 600 mg. A metabolite with a hydroxyl group at the 8th position was identified in the urine. However, the excretion of this metabolite was only 0.03% of the administered dose. The enzyme involved in the formation of the metabolite was CYP3A4.
The usual dosage in adults is 100 mg three times daily.
Excretion: Approximately 10% of the administered dose was excreted in the urine when Rebamipide was administered as a single oral dose to healthy adult males at 100 mg.
Protein Binding: Rebamipide at 0.05-5 μg/mL was added to human plasma, in vitro, and 98.4%-98.6% of the drug was bound to plasma proteins.