Structure-activity relations in organophosphorus inhibited acetylcholinesterase reactivators. I. Methiodides of new mono- and dioximes with pyridine nucleus.
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Cholinesterase Inhibitors↗
Biomedical subjects
S Martelli
Publications and source records attributed to S Martelli.
Structure-activity relations in organophosphorus-inhibited acetylcholinesterase reactivators. II. Methiodides of hydroxyimino derivatives of 1-pyridyl-2-phenylethanes.
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Animals↗
The hypophosphatemic and hyperkalemic effect of arginine in man.
The effects of a 0.5 g/kg body weight arginine infusion on plasma inorganic phosphate and potassium were examined in 15 normal subjects, and 6 recently diagnosed insulinopenic diabetics. Plasma phosphorus displayed a highly significant (p less than 0.001) fall in normal subjects, with a maximum fall below the baseline of 1.11 +/- 0.15 mg/100 ml or 33 + 3% (mean +/- SE). In addition, there was a highly significant correlation (p less than 0.01) between these falls and the insulin peaks induced by arginine. Plasma potassium levels, on the other hand, displayed a distinct and significant increase in 7 of the 8 subjects studied in this connection. The maximum increase over the baseline was 1.23 +/- 0.17 meq/l or 33 +/- 6% (p less than 0.01). In diabetic patients, arginine too led to a fall in phosphorus. While this was still significant, it was clearly less than in normal subjects: maximum fall = 0.64 +/- 0.09 mg/100 ml or 15 +/- 3%. Plasma potassium increased to a greater extent than in normal subjects: maximum increase = 1.63 +/- 0.21 meq/l or 42 +/- 6%. These findings show that arginine is responsible for a fall in plasma phosphorus that may well be partly related to the insulin response, and an increase in plasma potassium of clinical significance, whose mechanism(s), however, are still obscure.
Adolescent↗
Molecular adsorbent recirculating system treatment for acute hepatic failure in patients with hepatitis B undergoing chemotherapy for non-Hodgkin's lymphoma.
Hepatitis B virus (HBV) is a serious cause of morbidity and mortality in hepatitis B surface (HBsAg) antigen-positive patients treated with chemotherapy. Because the hepatitis is related to HBV virological reactivation, application of effective antiviral therapy, such as Lamivudine, has been attempted. Despite the use of these antiviral agents at the time of clinical hepatitis, some HBsAg-positive patients still develop hepatic failure and die. We used the Molecular Adsorbent Recirculating System (MARS) (MARS Monitor; Teraklin AG, Rostock, Germany) to treat 5 HBsAg-positive lymphoma patients with acute hepatic failure due to chemotherapy despite lamivudine treatment. Before and after each treatment we monitored the parameters of neurological status (EEG, cerebral CT and Glasgow coma score), hemodynamic parameters, acid-base equilibrium and blood gases as well as hepatic and renal function. The inclusion criteria were these of the King's College Hospital. Statistical analysis by Student t method showed significant results (P < .01). Three of 5 patients are alive without signs of reactivation of viral or hematological diseases at 1 year follow-up. The 2 patients died because MARS treatment was started too late, with Glascow coma score grade IV, hemodynamic instability, and mechanical ventilator assistance. Despite the limited number of cases, we believe that MARS can be applied to patients with a high tolerance and yield good results, but the treatment has to start at the first signs of hepatic failure.
Adult↗
One hundred sixteen cases of acute liver failure treated with MARS.
The various definitions of acute liver failure do not accurately reflect the differences in clinical signs and prognosis. Liver support devices to improve the clinical condition before liver transplantation (LT) were used in 13 patients with primary nonfunction, 24 with fulminant hepatitis, 17 were affected by delayed nonfunction, and 56 of acute on chronic hepatic failure. The average age of these patients was 41.8 years. The average number of applications of molecular absorbing recirculating system (MARS) was about 6 (range: 1-24). The mean length of application was about 9 hours (range: 8-20). MARS treatment was carried out in HLF patients with continuous acute-on-chronic hepatic failure dialisate flow similar to continuous veno venus hemofiltration (CVVH), albumin flow < 20% of hematic flow, heparin 5/10 UI/kg. In acute on chronic hepatic failure (AoCHF) patients, 6- to 11-hour (average 8.5) treatments were performed for a minimum of three treatments. The majority of patients were treated in the intensive care unit (ICU). Laboratory results were also monitored and showed progressive modification: bilirubin (before treatment 22.37 +/- 11.6 mg/dL, after treatment 11.36 +/- 7.5 mg/dL) and ammonium (before treatment 238.2 +/- 19 microg/dL, after treatment 115.4 +/- 12 microg/dL) showed significant change (P < .01). Lactates (before treatment 3.48 +/- 1.3 mmol/L, after treatment 1.76 +/- 1.1 mmol/L) and creatinine (before treatment 2.36 +/- 0.18 mg/dL, after treatment 1.26 +/- 0.67 mg/dL) also showed significant changes (P < .02 and P < .04). Glasgow Coma Score (GCS) went from 8.6 +/- 1.4 to 11.9 +/- 3.9 (P < .05). The mean middle cerebral artery flow (V media) went from 46 cm/s/26-59) to 73 cm/s (52-106) representing decreased cerebral edema, a difference that was not significant. INR scores (before treatment 2.4 after treatment 1.8) also showed no significant change. The MARS can be applied with tolerability for long periods for patients with PDF and FH as a bridge to transplant. In patients with PDF, it is used for a waiting recovery of the transplanted organ. Therefore MARS can also limit the necessity to perform further transplants.
Adult↗
Gastro-resistant microspheres containing ketoprofen.
Ketoprofen gastroresistant microspheres were prepared by spray-drying using common pH dependent polymers, such as Eudragit S and L, CAP, CAT and HPMCP. The long ketoprofen recrystallization time was a serious hindrance to the preparation of microspheres having a drug content higher than 35%. Microspheres were characterized by scanning electron microscopy, differential scanning calorimetry, X-ray diffractometry and in vitro dissolution studies, and used for the preparation of tablets. During this step, the compaction ability of the spray-dried powders was measured. While the compressibility of the microspheres containing the enteric cellulosic derivatives are not acceptable and different from those of the microcrystalline cellulose, the compaction properties of ketoprofen/Eudragit L or S microspheres are comparable to those of the Avicel PH 101. In vitro dissolution studies were performed on the microspheres and the tablets. All microspheres showed a good gastroresistance, but some differences among the five polymers in reducing drug release at low pH values are present. Acrylic polymers (Eudragit L or S) are considerably more effective than the cellulosic derivatives CAP and CAT, while the HPMCP profile is in an intermediate position. These differences are erased by the microspheres compression process. In HCl 0.1 N, the percentage of ketoprofen released from the tablets is always close to zero, independently from the polymer used.
Acrylates↗
Rotational laxity after anterior cruciate ligament injury by kinematic evaluation of clinical tests.
Despite the numerous studies on anterior cruciate ligament biomechanics and clinical tests, some disagreements still exist in the literature on the role of ACL in restraining rotations and which kinematic test after ACL injuries is the most suitable to evaluate this instability. This work analyses the capability of passive clinical and stress tests to detect an ACL state quantifying rotational instability. The study was conducted on animal knees with a new protocol. We found that an internal-external stress test can give a useful indication on the ACL state when used to estimate the side to side differences while varus-valgus laxity and secondary motions in standard kinematic tests did not seem to be affected by ACL injury. The kinematic protocol performed could be used intra-operatively to quantify rotations, allowing a more accurate evaluation of knee instability to guide surgical reconstruction and improve its final outcome.
Animals↗
Pyrimidoacridine derivatives as potential antitumor agents.
A series of some N-alkylaminoalkyl derivatives of pyrimido[5,6,1-d,e]acridine-1,3,7-trione (3) was synthesized as new potential antitumor drugs, starting from the suitable 9,10-dihydro-9-oxo-4-acridinecarboxamides and using phosgene as cyclizing agent. 1-(9,10-dihydro-9-oxo-4-acridinecarbonyl)-3-alkyl-2-imidazolido nes were also obtained as side products. The final products 3 and some carboxamides were tested "in vitro" against L 1210 leukemia and "in vivo" against P388 leukemia. Of the tested compounds, one is active "in vivo", another shows significant cytotoxic activity "in vitro", but is inactive or toxic "in vivo".
Acridines↗
[Epidemiological survey of a Siena school population. 1. Prevalence of malocclusion].
The Authors made a transversal epidemiological study on 256 children attending the elementary schools in a commune of Siena. The subjects aged between 6 and 11 years have been examined having in view a registration of prevalence of dysgnathia problems in children.
Child↗
Antibacterial activity of metal complexes of benzil and benzoin thiosemicarbazones.
The metal (II) complexes of benzyl and benzoin thiosemicarbazones have been synthesized and characterized. They were studied for their antibacterial, antifungal and amoebicidal activity in vitro and for their toxicity in vivo. The ligands and their metal complexes exhibited low antibacterial and amoebicidal activity. The metal chelates of benzoin thiosemicarbazone seem to be the most active compounds.
Animals↗
[Indications for laparoscopy in the diagnosis and treatment of abdominal trauma].
The use of laparoscopy as a diagnostic method dates back to the first decades of this century. Laparoscopic surgical techniques were first used by gynecologists and later, in 1989, Dubois performed the first cholecystectomy using a laparoscopic approach. Since then, in the space of a few years, there has been an overwhelming spread of videolaparoscopic operating methods, extending the therapeutic possibilities to gastroenterological surgery, as well as to thoracic, oncological, urological, and of course, gynecological surgery. The use of the laparoscope as a diagnostic method in abdominal trauma was proposed in the 70s by a number of authors, but only now, due to technological progress and the constant use of elective laparoscopic surgery, have surgeons been able to use this method for the diagnosis and treatment of patients with blunt or penetrating abdominal trauma. The experience accumulated to date includes a restricted number of cases, but preliminary results are encouraging and it is expected that this method will also be extended to emergency traumatology. The authors' preliminary experience consists of 7 laparoscopic examinations in subjects with abdominal trauma and hemoperitoneum. In 6 patients the examination confirmed hemoperitoneum caused by splenic lesion in 5 cases and hepatic lesion in 1 case. A hematoma of the left mesocolon was observed in one patient and the authors refrained from other treatment. In one subject with a splenic rupture at the ileum it was necessary to convert the operation into splenectomy. In a further 5 cases repeated washing and aspiration were used, using biological necks when necessary, until bleeding had completely ceased.(ABSTRACT TRUNCATED AT 250 WORDS)
Abdominal Injuries↗
[Specific complications in laparoscopic cholecystectomy: 610 cases].
The authors report their experience of 610 cases of laparoscopic cholecystectomy (VLC) and focus attention on the specific complications of this operation, in other words those not linked to the access phase (pneumoperitoneum and introduction of the trocars). The total percentage of complications reported was 1.3%. The most frequent complication was hemorrhage (0.6%), a finding which is in line with international literature. It is emphasised that complications almost always occur postoperatively, sometimes after the early discharge of patients and for this reason they may be more severe. The importance of an accurate dissection of the cholecystic ileum is underlined as being the only real guarantee against lesions to the common bile duct. In overall terms, however, after appropriate training and under the guidance of an expert surgeon, VLC may be considered as the new "gold standard" for treatment of cholelithiasis.
Adolescent↗