Analysis and Disposition of Dextromoramide in Body Fluids

Pharmacokinetics of Dextromoramide in Surgical Patients

“…Since the drug was given orally, clearance (Cl/F) and volume of distribution (V/F) values may represent overestimates. The observation that only negligible amounts of the drug were excreted unchanged in urine during the first 8 h (at a time when a considerable proportion of the drug had probably been already eliminated) suggests that the compound is cleared by biotransformation, possibly via multiple metabolic pathways (Caddy et al, 1980). Our data, however, indicate that unlike other narcotic analgesics, dextromoramide may not undergo extensive pre-systemic elimination in the liver.…”

“…Although the drug has been available since 1957, a rational approach to its clinical use is still hampered by virtually complete lack of information concerning its pharmacokinetics. In the only clinical study in which an attempt was made to measure dextromoramide levels, only 4 patients were studied and meaningful interpretation of data was complicated by the use of a spectrophotometric assay that lacked the necessary specificity (Caddy et al, 1980). A new, highly specific and sensitive method for measuring dextromoramide in biological fluids has recently been developed in our laboratories.…”

Treatment of pain in patients with renal insufficiency: The World Health Organization three-step ladder adapted

“…The major metabolite is thought to be 2-hydroxydextromoramide. 24 The pharmacologic activity of these metabolites is unknown. Less than 1% of a dose is excreted unchanged in the urine 8 hours after administration.…”

Investigations on the in vitro and in vivo metabolic fate of the new synthetic opioid desmethylmoramide using HPLC–HRMS/MS for toxicological screening purposes

“…Among them were hydroxylations of the morpholine and phenyl ring, as well as N-oxide formation. 6 However, they themselves merely described the detection of a metabolite formed after the morpholine ring hydroxylation in human urine and reported a personal communication with colleagues that detected an N-oxide. 6 Another metabolite, formed after the hydroxylation of one of the phenyl rings and served as a screening target in human urine using gas chromatography mass spectrometry (MS), was described by Maurer et al 7 Therefore, the aim of this study was to elucidate the metabolic fate of DMM in rat, as well as in pooled human liver S9 fraction were obtained from VWR International (Darmstadt, Germany).…”

“…6 However, they themselves merely described the detection of a metabolite formed after the morpholine ring hydroxylation in human urine and reported a personal communication with colleagues that detected an N-oxide. 6 Another metabolite, formed after the hydroxylation of one of the phenyl rings and served as a screening target in human urine using gas chromatography mass spectrometry (MS), was described by Maurer et al 7 Therefore, the aim of this study was to elucidate the metabolic fate of DMM in rat, as well as in pooled human liver S9 fraction were obtained from VWR International (Darmstadt, Germany). 3 0phosphoadenosine-5 0 -phosphosulphate (PAPS), S-adenosylmethionine (SAM), dithiothreitol (DTT), reduced glutathione (GSH), acetylcarnitine transferase (AcT), acetylcarnitine, acetyl coenzyme A (AcCoA), magnesium chloride (MgCl 2 ), dipotassium phosphate (K 2 HPO 4 ), monopotassium phosphate (KH 2 PO 4 ), superoxide dismutase, isocitrate dehydrogenase, isocitrate, tromethamine (Tris), ammonium formiate, and formic acid were purchased from Sigma (Taufkirchen, Germany).…”