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Biomedical subjects

A Marco

Publications and source records attributed to A Marco.

69 records · Page 4Linked to original sources

Pharmacokinetics and metabolism of [14C]rosaramicin in dogs.

The pharmacokinetics and metabolism of [14C]rosaramicin were studied in dogs after intravenous (i.v.; 10 mg/kg [bodyweight]) and oral (25 mg/kg) administration. After i.v. administration, rosaramicin levels in plasma declined rapidly, with half-lives of 0.22 h for the distribution phase and 0.97 h for the elimination phase. The apparent volume of distribution was 3.43 liters/kg, and the total body clearance was 106 mg/min . kg, indicating extensive distribution in tissue or metabolism or both. The absorption of oral solution was 58%, and the absolute bioavailability of rosaramicin was 35%. The plasma area under the curve of unchanged rosaramicin was only 5% that of total radioactivity after oral administration and 8% after i.v. administration, indicating extensive metabolism of the drug. The total radioactivity excreted in urine accounted for only 24% of the i.v. dose and 17% of the oral dose. Fecal radioactivity accounted for 71% of the i.v. dose and 68% of the oral dose. Several metabolites were observed in the plasma and urine. The amount of unchanged rosaramicin in urine (1 to 2% of the dose) was quite small after drug administration by either route.

Administration, Oral↗

[Echography in the diagnosis on childhood nephrocalcinosis. Apropos of 5 cases].

We have studied 5 patients with nephrocalcinosis by means of plain film and sonography. Our results, which are in agreement with other authors, show that it is possible to find nephocalcinosis with no findings in the plain film. We correlate both examinations and propose a new radiologic approach for this condition.

Child↗

Surgical treatment of an aneurysm of the vein of Galen in a newborn with heart failure.

Congestive heart failure is the usual complaint and cause of death in neonates with aneurysms of the great vein of Galen. Direct surgical obliteration of the feeding arteries cures the heart failure, but few such newborns survive the operation. The authors report a case of primary aneurysm of the great vein of Galen treated successfully by clipping the afferent arteries and reduction of the bulk of the aneurysm by bipolar coagulation. Five months after the operation the child's development is normal.

Cerebral Angiography↗

Transient idiopathic subpleural cysts in the newborn: an observation in two patients.

We present two cases of transient idiopathic cystic formations in the subpleural region in full-term newborns, that do not fit into any known cystic process to our knowledge. The features of the cystic formations, their subpleural location, their spontaneous regression, the histopathological study, as well as the absence of a clear etiology, have led us to propose the name of "Transient Idiopathic Subpleural Cysts in Full-term Newborns", for this process.

Cysts↗

Comparative pharmacokinetics of Sch 28191 and amphotericin B in mice, rats, dogs, and cynomolgus monkeys.

The pharmacokinetics of Sch 28191, the N-D-ornithyl methyl ester of amphotericin B, and amphotericin B were studied in mice, rats, dogs, and cynomolgus monkeys after an intravenous dose of 0.6 mg/kg was administered. The decline in the concentrations of Sch 28191 and amphotericin B in serum appeared to be biphasic in nature. The half-life at the distribution phase and the half-life at the elimination phase of Sch 28191 were similar to those of amphotericin B in all animals studied. The half-life at the distribution phase in serum was 0.9 to 1.5 h in all animals studied. The half-lives at the elimination phase in serum were 25 to 28 h in mice, 16 to 18 h in rats, 44 to 47 h in dogs, and 35 h in cynomolgus monkeys. The areas under the serum concentration-time curves of Sch 28191 were five- to eightfold larger than those of amphotericin B in rats, dogs, and cynomolgus monkeys but were only slightly larger than those of amphotericin B in mice. In dogs, the urinary excretion (over 9 days) of unchanged drug accounted for 23% of the Sch 28191 dose and 25% of the amphotericin B dose. The concentrations of Sch 28191 in serum were also studied after the intravenous administration of 0.3, 0.6, or 1.25 mg/kg to dogs. The serum concentration-time curves were parallel for these doses. There was a linear relationship between the areas under the concentration-time curves and the doses, indicating dose proportionality.

Amphotericin B↗

Pharmacokinetics and metabolism of rosaramicin in humans.

The pharmacokinetics of rosaramicin was studied in subjects receiving 500 mg of the drug (i) by 1-h intravenous infusion, (ii) in solution orally, or (iii) as tablets orally. After intravenous administration, the rosaramicin levels in serum declined rapidly with t1/2S of 0.27 h for the distribution phase and 3.28 h for the elimination phase. The apparent volume of distribution was 3.78 liter/kg, and the total body clearance was 13.41 ml/min per kg, indicating extensive tissue distribution or metabolism or both. Similar pharmacokinetic data were obtained after oral administration of the drug in solution or tablets and after intravenous dosing. The absolute bioavailability of the drug administered orally, in either tablets or solution, was 32 to 39%. The metabolism and excretion of [14C]rosaramicin administered orally were also evaluated in volunteers. The serum area under the curve (infinity) of unchanged rosaramicin was 19% of that of total radioactivity, indicating extensive metabolism of the drug. About 7.0% of the radioactivity was recovered in the urine, and 86.7% was recovered in the feces. Only a small amount of unchanged rosaramicin was present in the urine (7 to 9% of urinary radioactivity), but none was present in the feces. The major metabolite, 20-bis-ureidorosaramicin, represented 17 to 38% of the radioactivity in the urine and 26 to 29% of the radioactivity in the feces.

Administration, Oral↗

Synthesis and antitumor activity of 4-demethoxydaunorubicin, 4-demethoxy-7,9-diepidaunorubicin, and their beta anomers.

Four new derivatives of daunorubicin, characterized by the absence of the methoxyl group at the C-4 position, have been obtained by chemical synthesis. 4-Demethoxydaunorubicin (NSC-256439) was effective against L1210 and Gross leukemias and ascites and solid Sarcoma 180 at doses four to eight times lower than those effective for daunorubicin. The beta anomer of 4-demethoxydaunorubicin was active at doses 13and eight times higher than those of its corresponding alpha anomer against L1210 and Gross leukemias respectively. 4-Demethoxy-7,9-diepidaunorubicin and its beta anomer were devoid of any biologic activity at the doses tested.

Animals↗

DNA complexing antibiotics: daunomycin, adriamycin and their derivatives.

9-Acetyl-4-methoxy-7,8,9,11-tetrahydroxy-6,7,9,11-tetrahydroxy-o-(3'-amino-2',3',6'-trideoxy-alpha-L-lyxohexopyranoside) (daunomycin, daunorubicin, NSC-82 131, Daunoblasin), 14-hydroxy-daunorubicin (adriamycin, doxorubicin, NSC-123 127, Adriblastin), dihydrodaunomycin, their aglycones and other related compounds represent the group of S. peucetius derived antibiotics. The biosynthetic glycosides as well as some semisynthetic analogues or derivatives form strong complexes with double stranded DNA, which can be understood in terms of the known intercalation model. A clear relationship is found between the complex forming ability and the biological activity of the different compounds. The structure and configuration of the sugar moiety appear of primary importance for the stabilization of the complex and, therefore, for action. A class of side chain derivatives, namely adriamycin 14-0-esters, looks promising. Different tissue distribution of such derivatives may result in new useful anticancer drugs.

Animals↗

Antioxidant status in a squirrel monkey (Saimiri sciureus) with chronic pancreatitis and degenerative myopathy.

A squirrel monkey (Saimiri sciureus) presented with wasting, vomiting and diarrhoea. Haematology revealed elevation of creatinine phosphokinase, lactic dehydrogenase, alanine aminotransferase, amylase and lipase, together with azotaemia and hypoalbuminaemia. Prominent findings were chronic pancreatitis with acinar and ductal plugs, granulomatous and necrotizing peripancreatic steatitis, degenerative myopathy, testicular atrophy, candidiasis and bacterial necrotizing glossitis. Antioxidant analyses revealed low concentrations of serum vitamin E (and apparently A), hepatic selenium and hair zinc. Pancreatitis may have caused malabsorption and maldigestion, associated with deficiency of multiple antioxidants.

Animals↗

Effect of selenium deficiency on the development of central nervous system lesions in murine listeriosis.

The effect of selenium (Se) deficiency, produced by feeding a Se-deficient diet, on the development of central nervous system (CNS) lesions was studied in mice infected with Listeria monocytogenes, administered in drinking water for 1 or 7 days in a daily dose of 10(9)organisms, or for 7 days in a daily dose of 10(7). Se-deficient mice differed from Se-normal controls in developing CNS lesions significantly more frequently. Moreover, regardless of Se status, mice receiving repeated doses of 10(9)organisms differed from those receiving a single 10(9)dose in showing CNS lesions at least twice as often. The majority of animals with CNS lesions showed an inflammatory pattern of rhombencephalitis (17/24), while only two of 24 showed choroiditis-ventriculitis-meningitis; five of 24 animals showed both inflammatory patterns. Listeria monocytogenes antigen was identified within the areas of inflammation by an immunoperoxidase technique. Neuritis of the trigeminal nerve was present in eight animals. The relative lack of pathological changes in the liver and spleen validates this murine model for the study of CNS listeriosis.

Animals↗

[Resolution of a neck chylous fistula with oral diet treatment].

Chylous fistula after neck dissection is a well-described complication. This pHatology can lead to serious respiratory and nutritional complications. Therapeutical options for chylous fistula remains controversial. On last reviews, there are an agreement on the conservative management. Within of this management, low long-chain triglycerides fat diet is an essential part.

Adult↗