The nonnarcotic antitussive drug dimemorfan: a review

A new method for quantitative determination of dimemorfan in human plasma using monolithic silica solid-phase extraction tips

“…Thus, the observed LOQ value for the drug was similar to that obtained in previous study. The therapeutic blood concentration of dimemorfan is reported to be 7-8 ng/mL [14]. Therefore, our present method can be used for monitoring of dimemorfan concentration.…”

“…There have been no reports of lethal or toxic cases of dimemorfan poisoning in humans. However, the median lethal dose of dimemorfan by oral administration in rats has been reported to be 690 mg/kg, which is between that of dextromethorphan and codeine [14]. This suggests dimemorfan poisoning cases could occur in the future.…”

“…Although dimemorfan is regarded as safe at recommended therapeutic doses, adverse effects in psychoneurologic and digestive systems are observed at high doses [14]. Therefore, methods for quantifying dimemorfan concentration in human blood samples are required to allow optimum dosage adjustments and for clinical and forensic toxicological analysis.…”

Neuropsychotoxic and Neuroprotective Potentials of Dextromethorphan and Its Analogs

“…Its antitussive action appears to arise from a direct effect on the cough center in the medulla. It does not induce any significant physical or psychological dependence (89), and its antitussive action is not affected by the opioid receptor-blocker levallorphan. Studies in animal models indicate that DF is up to three times more potent as an antitussive agent than codeine and is equivalent in potency to DM.…”

“…Dimemorfan (DF, 3-methyl-17-methylmorphinan), an effective non-narcotic antitussive agent with a low incidence of adverse events (89), was discovered through extensive screening of morphinan analogs and was first used in Japan in 1975 (89,90). Its antitussive action appears to arise from a direct effect on the cough center in the medulla.…”