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Pharmacology: Pharmacodynamics: The mechanism of rebamipide's anti-inflammatory and gastroprotective actions involves increased mucus secretion, enhanced generation of endogenous prostaglandin E2 (PGE2) in the gastric mucosa, inhibition of pro-inflammatory cytokine secretion by immune cells, inhibition of neutrophil activation, and scavenging of cytokine-induced reactive oxygen species.
Rebamipide is poorly absorbed into systemic circulation; thus, it exhibits only local activity at the target organ and essentially has no systemic activity.
The suppressive effect of rebamipide on nonsteroidal anti-inflammatory drug (NSAID) induced gastric mucosal injury can be attributed to reduced 15-hydroxyprostaglandin dehydrogenase expression, which increases the PEG2 concentration in the gastric tissue.
Pharmacokinetics: Following single oral administration of 100 mg in 12 healthy volunteers, the peak plasma concentration of rebamipide (210 ng/mL) was achieved in 2 hours with an elimination half-life of 1.94 hours. Repeated dose administration in humans revealed that rebamipide does not accumulate in the body.
Pharmacokinetic parameters of patients with renal impairment given a single oral dose of 100 mg rebamipide showed 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. Thus, rebamipide is not considered to accumulate in the body.
In 6 healthy volunteers, the absorption of rebamipide appears to be slow following an oral dose of 150 mg given after a meal. However, food did not affect the bioavailability of the drug.
Approximately 98.4 % to 98.6% of rebamipide is bound to plasma proteins when 0.05 to 5 mcg/mL was added to human plasma in vitro.
Rebamipide is primarily excreted in the urine as unchanged drug following a single oral dose of 600 mg to healthy male adults. Approximately 10% of the administer dose was excreted in the urine following a single oral dose of 100 mg.
