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1.
J Stroke Cerebrovasc Dis ; 25(8): 1891-5, 2016 Aug.
Article in English | MEDLINE | ID: mdl-27160382

ABSTRACT

BACKGROUND: Human immunodeficiency virus (HIV)-infected individuals are at high risk for ischemic stroke. To investigate the physiological basis for this risk, we used magnetic resonance imaging (MRI) to measure oxygen extraction fraction (OEF) and cerebral blood flow (CBF) in treatment-naive asymptomatic HIV-infected subjects and controls. METHODS: In treatment-naive asymptomatic HIV-infected subjects and age-, gender-, and race-matched controls, OEF was measured by MRI asymmetric spin-echo echo-planar imaging sequences and CBF was measured by MRI pseudocontinuous arterial spin labeling. RESULTS: Twenty-six treatment-naive HIV-infected subjects and 27 age-, gender-, race-matched controls participated. Whole-brain, gray matter (GM), and white matter OEF were not different between the groups (all P > .70). Unexpectedly, HIV-infected subjects had significantly higher CBF in cortical GM (72.9 ± 16.2 mL/100 g/min versus 63.9 ± 9.9 mL/100 g/min; P = .01) but not in subcortical GM (P = .25). CONCLUSIONS: The observed increase in cortical GM CBF in treatment-naive HIV-infected subjects is unexpected, contrary to CBF decreases reported in HIV-infected subjects on treatment, and may represent an initial increase in metabolic activity due to an HIV-mediated inflammation.


Subject(s)
Cerebral Cortex/pathology , Cerebrovascular Circulation/physiology , HIV Infections/pathology , Adult , Anti-Retroviral Agents/therapeutic use , Case-Control Studies , Cerebral Cortex/diagnostic imaging , Cerebral Cortex/virology , Female , Glafenine/administration & dosage , Glafenine/analogs & derivatives , HIV Infections/diagnostic imaging , HIV Infections/drug therapy , Humans , Image Processing, Computer-Assisted , Magnetic Resonance Imaging , Male , Retrospective Studies , Spin Labels , Young Adult
3.
Fundam Clin Pharmacol ; 6(4-5): 197-203, 1992.
Article in English | MEDLINE | ID: mdl-1358775

ABSTRACT

Pharmacokinetic parameters were evaluated in 12 patients with alcoholic cirrhosis and 12 healthy volunteers after a single 400 mg oral dose of glafenine. Glafenine (G) and its major active metabolite glafenic acid (GA) were measured at regular intervals using a specific high performance liquid chromatographic method. Glafenine absorption was significantly delayed in cirrhotic patients (CP) (Tmax = 2.8 +/- 1.3 hvs 1.5 +/- 0.4 h, p less than 0.01) and was dramatically reduced in 3 patients. The large hepatic 'first pass' effect observed in healthy volunteers was markedly reduced in CP (ratio Cmax GA/Cmax G = 3.6 +/- 2.9 vs 18.9 +/- 9.8, p less than 0.001; ratio areas under the curves AUC GA/AUC G = 2.3 +/- 2.3 vs 18.2 +/- 11.2, p less than 0.001). The elimination half-life of G was prolonged in the CP (13.0 +/- 13.1 h vs 1.5 +/- 0.5 h, p less than 0.01). In CP, GA elimination half-life was increased (12.0 +/- 13.4 h vs 4.3 +/- 1.3 h, NS) but the difference did not reach statistical significance because of large variability. The significant rise of G plasma concentrations (Cmax = 2.2 +/- 2.1 mg/L vs 0.7 +/- 0.2 mg/L, p less than 0.05) and its longer half-life would lead to an accumulation if the usual dosage regimen was prescribed for CP and could result in nephrotoxicity. On the other hand, lower dosage would be ineffective because only GA is active and nephrotoxic. Hence, G should be given with great caution to CP.


Subject(s)
Glafenine/analogs & derivatives , Glafenine/pharmacokinetics , Liver Cirrhosis, Alcoholic/metabolism , Administration, Oral , Adult , Female , Glafenine/administration & dosage , Humans , Liver/metabolism , Liver Cirrhosis, Alcoholic/drug therapy , Male , Middle Aged
4.
J Microencapsul ; 6(3): 355-60, 1989.
Article in English | MEDLINE | ID: mdl-2569511

ABSTRACT

The bioavailability and gastric ulcerogenic activity of oxyphenbutazone and glafenine (acidic and basic nonsteroidal anti-inflammatory drugs), coated with different cellulose derivatives were assessed in albino rats. The cellulose derivatives chosen have different functional groups, acidic (carboxymethyl cellulose), basic (chitosan) and neutral (hydroxypropylmethyl cellulose). The bioavailability was dependent on the drug and polymers. Generally, all the cellulose derivatives chosen decreased the gastric ulcerogenic activity of the drugs studied.


Subject(s)
Glafenine/administration & dosage , Oxyphenbutazone/administration & dosage , Stomach Ulcer/chemically induced , ortho-Aminobenzoates/administration & dosage , Animals , Biological Availability , Capsules/adverse effects , Carboxymethylcellulose Sodium , Chitin/analogs & derivatives , Chitosan , Glafenine/adverse effects , Glafenine/pharmacokinetics , Hypromellose Derivatives , Male , Methylcellulose/analogs & derivatives , Oxyphenbutazone/adverse effects , Oxyphenbutazone/pharmacokinetics , Rats , Time Factors
5.
J Chromatogr ; 427(2): 307-14, 1988 Jun 03.
Article in English | MEDLINE | ID: mdl-2900842

ABSTRACT

A high-performance liquid chromatographic method for an effective determination of glafenine and its main metabolite, glafenic acid, is described. The assay involves separate extraction procedures for glafenine and for its metabolite, but the same internal standard (floctafenine) and the same chromatographic conditions (including a 5-micron C8 column, a quaternary solvent mixture of water-acetonitrile-diethylamine-acetic acid and an ultraviolet detector set at 360 nm). For 1 ml of plasma, the detection limit is 0.05 mg/l for glafenine and 0.25 mg/l for glafenic acid. Compared with previously described techniques, this assay uses a very low glafenine linearity range, which allows the true pharmacokinetics of this drug to be described for the first time.


Subject(s)
Glafenine/blood , ortho-Aminobenzoates/blood , Chromatography, High Pressure Liquid , Glafenine/administration & dosage , Glafenine/pharmacokinetics , Humans
6.
Allerg Immunol (Paris) ; 18(3): 17-20, 1986 Mar.
Article in French | MEDLINE | ID: mdl-2456076

ABSTRACT

Challenge test puts in evidence the responsibility of a drug. The biological checking by plasmatic histamine leads to distinguish between a specific histamine-release reaction and a non-specific one. Thus, glafenine has proved to be a non specific histamine release where as in some cases, acetyl-salicylic-acid (A.S.A.) behaves like a specific histamine release.


Subject(s)
Aspirin/adverse effects , Drug Hypersensitivity/diagnosis , Glafenine/adverse effects , ortho-Aminobenzoates/adverse effects , Adult , Anaphylaxis/chemically induced , Angioedema/chemically induced , Aspirin/administration & dosage , Glafenine/administration & dosage , Histamine Release , Humans , Urticaria/chemically induced
9.
Ann Biol Clin (Paris) ; 41(2): 105-11, 1983.
Article in French | MEDLINE | ID: mdl-6136242

ABSTRACT

The role of glafenine in certain cases of acute renal failure was described several years ago, but very little work has been done on the intratubular precipitates generally responsible for these manifestations. We have been able to study 6 cases of acute poisoning and 5 cases of glafenine renal stones which have shown that several mechanisms are likely to be involved. In 4 cases, the acute poisoning resulted in reversible oliguria which resolved after several days. In 3 of the 5 cases of renal stones, variable amounts of glafenine were found in the zone of nucleation. Infrared spectrophotometric and chromatographic examination of the first urine after the return of diuresis in the oliguric subjects and in the patients with renal stones, revealed that several metabolites of glafenine could be implicated in the development of these renal precipitates. In the different cases, free metabolites and conjugated derivatives were found to be responsible. The authors discuss the relationship between the products detected and the clinical manifestations observed.


Subject(s)
Acute Kidney Injury/chemically induced , Glafenine/adverse effects , Kidney Calculi/chemically induced , ortho-Aminobenzoates/adverse effects , Acute Kidney Injury/physiopathology , Adult , Aged , Female , Glafenine/administration & dosage , Humans , Kidney Calculi/physiopathology , Male , Middle Aged
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