Excretion profiles of ethyl glucuronide in human urine after internal dilution.

Ethyl glucuronide (EG) is a useful marker of alcohol consumption because its presence in urine can be detected up to five days. We investigated the impact of diuresis on the urinary excretion of EG, a minor ethanol metabolite. Seven healthy volunteers drank 250 mL of wine (25 g ethanol) in 15 min and, 240 min later, ingested 1 L of water within 15 min.

Ritonavir increases loperamide plasma concentrations without evidence for P-glycoprotein involvement.

Background: The antidiarrheal drug loperamide is frequently used to treat ritonavir-associated diarrhea in patients with human immunodeficiency virus. The absence of marked central opioid effects has been attributed to its low bioavailability and its poor penetration of the blood-brain barrier, both of which might be altered by ritonavir, a potent P-glycoprotein and cytochrome P4503A inhibitor.

Methods: A 16-mg dose of loperamide was administered to 12 healthy male and female volunteers together with either 600 mg of ritonavir or placebo.

Hemoglobin diffusion across a venous wall: an experimental study.

The aim of this study was to investigate the permeation behavior of a large molecule through a venous wall; hemoglobin was chosen as a model substance. In vitro experiments were performed using a Chien-Valia diffusion chamber. Postmortem, hemolyzed, and fresh nonhemolyzed blood samples were investigated as permeants.

A preliminary study on the distribution of morphine and its glucuronides in the subcompartments of blood.

The distribution of morphine, morphine-3-glucuronide (M3G), and morphine-6-glucuronide (M6G) in whole blood, plasma, and packed erythrocytes was studied. Parameters investigated were the hematocrit values (10, 42, 44, and 71%) and the water content of the samples. The blood-to-plasma ratio of morphine concentrations was unaffected by variations in hematocrit and water content, whereas the corresponding ratios for M3G and M6G were strongly influenced.

[Fatal poisoning with clozapine and perazine. A case report].

An intoxication following an apparent overdose of clozapine (Leponex) and perazine (Taxilan) is reported. There was a wide range of variation in postmortem blood and tissue concentrations of clozapine, desmethyclozapine and perazine. Clozapine/norclozapine blood and tissue ratios and perazine-pill-fragments in the gastric content could be used as a sign of suspected acute clozapine and perazine overdose.

An in vitro experiment for postmortem vascular permeation. The passage of morphine and morphine glucuronides across a vascular wall.

A venous blood sample taken at autopsy cannot be considered to represent the antemortem blood concentration of a particular substance. Autolytic processes cause disintegration and increasing permeability of the physiological and anatomical barriers such as vascular walls and lead to changes in substance concentrations. In the present study, the experimental design represents an in vitro postmortem simulation of a drug substance crossing a venous wall.

Plasma concentrations of heroin and morphine-related metabolites after intranasal and intramuscular administration.

The disposition of heroin and its metabolites was investigated in four healthy male volunteers following intranasal administration of 6 and 12 mg heroin hydrochloride. In addition, two doses of 6 mg heroin hydrochloride were injected intramuscularly for comparison of pharmacokinetic parameters. Serum samples were analyzed for heroin, 6-acetylmorphine, and morphine by solid-phase extraction-gas chromatography-mass spectrometry.

Postmortem distribution pattern of morphine and morphine glucuronides in heroin overdose.

The postmortem distribution of morphine and its metabolites was investigated in four cases of heroin overdose to evaluate some of the factors that influence intravasal blood concentrations. Variables included were the chemical stability of morphine conjugates, hemoconcentration, incomplete distribution of the drug and diffusion processes. Blood samples from different sampling sites including the aorta, the infra- and suprarenal portion of the inferior vena cava, the superior vena cava, the femoral and subclavian veins, and the right and left ventricles were examined for morphine, morphine-3-glucuronide and morphine-6-glucuronide, hematocrit and water content.