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Biomedical subjects

J Benes

Publications and source records attributed to J Benes.

At least 19 recordsLinked to original sources

Synthesis, anticonvulsant properties and pharmacokinetic profile of novel 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide derivatives.

A series of novel derivatives of oxcarbazepine (5), 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide was synthesised and evaluated for their anticonvulsant activity and sodium channel blocking properties. The oxime 8 was found to be the most active compound from this series, displaying greater potency than its geometric isomer 9 and exhibiting also the highest protective index value. Importantly, the metabolic profile of 8 differs from the already established dibenz/b,f/azepine-5-carboxamide drugs such as 1 and 5 which undergo rapid and complete conversion in vivo to several biologically active metabolites. In contrast 8 is metabolised to only a very minor extent leading to the conclusion that the observed anti-convulsant effect is solely attributable to 8. It is concluded that 8 may be as effective as 1 and 5 at controlling seizures and that the low toxicity and consequently high protective index should provide the compound with an improved side-effect profile.

Amides↗

Abdominoinguinal pain syndrome treated by centrocentral anastomosis.

During operations in the lower part of the abdomen injuries to nerves located here arise in 1-4,2 per cent; the most frequently iliohypogastric, ilioinguinal, genitofemoral and lateral femoral cutaneous nerves. These injuries to nerves are often very painful and till to day very difficult to treat. Clinical terminology of their injuries is variable and not strict. Therefore we suggest an all embracing term "abdominoinguinal pain syndrome". The authors present four case reports, in whom centrocentral anastomosis with use of both autologous interposed segment of nerve and also without it, achieved successful treatment of chronic pain. On the basis of this experience the authors prefer centrocentral anastomosis without autologous interposed segment of nerve, which is technicaly more simple.

Abdominal Pain↗

Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives.

A series of esters of the major metabolite of oxcarbazepine (2), 10, 11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxamide, were synthesized and evaluated for their anticonvulsant and brain sodium channel-blocking properties. The compounds were assayed intraperitoneally and per os in rats against seizures induced by maximal electroshock (MES). Neurologic deficit was evaluated by the rotarod test. The enantiomeric acetates (R)-11 and (S)-12 were the most active of the series against MES-induced seizures with oral ED(50) values at t(max) of 10.9 +/- 2.3 and 4.7 +/- 0.9 mg/kg, respectively. After intraperitoneal administration, carbamazepine (1) behaved more potently than 2 and all other new dibenz[b, f]azepine-5-carboxamide derivatives in the MES test; compounds 2 and 12 were equally potent. In the rotarod test, low doses of 1 produced considerable motor impairment, which did not occur with 2, enantiomeric alcohols (S)-6, (R)-7, and racemic alcohol 8, or racemic acetate 10 or (R)-11. The potencies of the racemic and enantiomerically pure alcohols 8, (S)-6, and (R)-7 derived from 2 in the MES and rotarod test were found to be similar between them, and consequently they exhibit similar protective index values. All three forms of the alcohol and their corresponding acetates (pairs 8 & 10, 6 & 12, and 7 & 11) were found to differ in the MES or rotarod tests; the ED(50) value for (S)-6 against MES-induced seizures was nearly 3-fold that for (S)-12. The protective index also differed markedly between all stereoisomers of the alcohol and their corresponding acetates, most pronouncedly for compound (S)-12 which attained the highest value (12.5) among all compounds tested. Blockade of voltage-sensitive sodium channels was studied by investigating [(3)H]batrachotoxinin A 20-alpha-benzoate ([(3)H]BTX) binding. Acetates (R)-11 and (S)-12 were more potent than the standards 1 and 2 at inhibiting the binding of [(3)H]BTX to sodium channels and the influx of (22)Na(+) into rat brain synaptosomes. It is concluded that acetates (R)-11 and (S)-12 are not simple metabolic precursors of alcohols (R)-7 and (S)-6 in rodents but that they possess anticonvulsant and sodium channel-blocking properties in their own right.

Amides↗

[Treatment of chronic subdural hematoma with a closed drainage system].

The authors evaluate a group of 92 patients with the diagnosis of chronic subdural haematoma confirmed by CT. All patients were operated from two trepanation bores with insertion of drainage into the subdural space and its connection with the closed drainage system. They used three types of drainage systems. The best clinical results were obtained with the negative pressure suction system of Braun Co in 92%. This system was switched on intermittently only till the patient developed signs of headache. Attention is focused on possible types of complications in different systems. In the remaining 13 patients who did not improve reinsertion of the drain was used, or craniotomy with membranectomy with a 60% improvement. The mentioned negative pressure drainage system in treatment in chSDH seems most suitable and is associated with the least number of complications.

Adult↗

[Shock-wave lithotripsy in choledocholithiasis in a female patient with a cardiac pacemaker].

BACKGROUND: Extracorporeal shock wave lithotripsy is relatively contraindicated in patients with an implanted cardiac pacemaker. Shock waves can damage the pacemaker by mechanical pressure and also by electromagnetic induction. Since the distance between the applicator and the pacemaker is small during biliary lithotripsy, the risk of damaging the pacemaker is greater. In the following case, the patient presented with a stone in the common bile duct, and had an implanted pacemaker. Lithotripsy with non-synchronized shock waves was the method of choice since conventional surgery was high risk in this specific case. CASE REPORT: In an 84-year-old woman with a stone in the proximal part of the common bile duct, endoscopic attempts of extraction failed. Therefore, shock wave lithotripsy was indicated. This patient had serious heart disease with an interference of spontaneous heart action with the pacemaker at a ratio of 1:1. We decided to treat with shock wave lithotripsy. The application of shock waves was without side effects on the patient and the pacemaker. CONCLUSION: This case is interesting as it highlights the possibility of using the Czech made MEDILIT lithotriptor in the treatment of choledocholitiasis in patients with a pacemaker. Even so, it is necessary to monitor the patient's ECG to ensure the possibility of immediate external stimulation.

Aged↗

[Clinical experience with Timentin].

BACKGROUND: A combination of ticarcillin with clavulanate has been used for more than 12 years in many countries in the treatment of infections caused by Gram-negative microorganisms and a mixed microbe flora, in particular where the presence of beta-lactamase producers can be anticipated. In the Czech Republic it is not very well known, probably more for commercial than medical reasons, and the objective of the present paper to draw attention to this old but still useful antibiotic. METHODS AND RESULTS: In a simple open trial the therapeutic results in a group of 15 patients treated by the above preparation in 1992-1995 at the unit for septic infections of the Clinic for Infectious Diseases in Prague were summarized and compared with the results of a previous trial conducted in the same department in 1987-91 and with results published in the literature. The mean success of treatment was about 90%. CONCLUSIONS: A combination of ticarcillin, a semisynthetic broad spectrum penicillin with clavulanic acid is an antibiotic which is still very valuable in the treatment of sepsis and other severe forms of bacterial infection, incl. patients with a significantly reduced immunity. The tolerance is very good and an important factor is also the relatively favourable price. The author's results are consistent with experience published by departments abroad.

Adult↗

[Biological effects of interacting shock waves. A modeling study of the effects of interacting shock waves using erythrocyte hemolysis].

AIM: The effects of high-energy shock wave on tissues were discussed in literature. The shock wave sources which were used for experiments were developed for stone fragmentation. The side effects of the applicators are generally low. Increase of shock wave pressure induce bigger negative pressure amplitude and this may cause significantly bigger side effects. We used tow shock waves, with time interval of 5 microseconds. In our opinion, the first shock wave causes acoustic inhomogenity in shock wave focus and therefore second shock wave acts in a region with different acoustic parameters. The second shock wave may loss energy in the focus area by dissipation or absorption. We termed the coupled shock waves as "interacting shock waves". METHODS AND RESULTS: Hemolysis of erythrocytes was used for examination of biological toxicity. Shock wave pressure was 80 MPa, the ratio of positive to negative pressure of single shock waves is 30. For correlation we applied 50 and 100 single shock waves and 50 or 100 couples of two shock waves. Hemolysis after 50 simple shock waves was 4.28 times lower compared with hemolysis after the same number of coupled shock waves (interacting shock waves). CONCLUSION: After 50 couples of shock waves hemolysis is 2.14 times higher compared with 100 single shock waves. This result suggests that the hypothesis of some interaction existing between two shocks applied in a very short time interval make future study rightful.

Hemolysis↗

Immunosuppressive activity of bovine seminal ribonuclease and its mode of action.

Two preparations of dimeric BS RNase-native and recombinant proteins caused identical immunosuppressive effects on MLC-stimulated human lymphocytes. The monomers of RNase A and BS RNase were ten times less active. The inhibitory effect on MLC-stimmulation was followed by 90% inhibition of cell-mediated lympholysis (CML) caused by BS RNase (10 micrograms/ml). This effect indicated that BS RNase suppressed the recognition phase of the cytotoxic reaction, resulting in inhibition of generation of cytotoxic effector cells. BS RNase exerted a similar effect on generation of cytotoxic LAK cells. Cytotoxic activity of LAK cells or CTLs against K562 target cells was abrogated only when BS RNase was added at the beginning of the sensitizing phase, but the cytotoxicity of effector cells in the destruction phase was not influenced. The effect of RNase A on the generation of cytotoxic cells was much less pronounced. To get more information about the site of action, the effect of BS RNase on early lymphocyte stimulation by PHA was investigated by using fluorescein cell probes. BS RNase (100 micrograms/ml) prevented a shift in fluorescein emission occurring within one hour of activation using fluorescein diacetate as a marker for changes in the cytoplasmic matrix. On the contrary, it did not block the shift in fluorescence emission when tested with diphenylhexatrien as a marker for changes in membrane fluidity. Furthermore the effect of BS RNase on expression of membrane antigens expressed on activated human lymphocytes was estimated. BS RNase significantly inhibited the expression of CD25, CD38 and CD71 antigens on PHA-, Con A- and MLC-stimulated human T and B lymphocytes. No substantial change in expression of these antigens was observed on IL-2-stimulated cells, but DNA synthesis was totally abrogated. These results indicate that the mode of action of BS RNase on activated T and B lymphocytes is based mainly on the suppressed expression of receptors for interleukin-2-alpha-chain and transferrin.

ADP-ribosyl Cyclase↗

[Comparison of various methods of hemoculture tests].

Three methods of blood cultivation were compared: collection of blood into transport bottles containing only dextran-sulphate, collection into cultivation media containing bottles (aerobic, anaerobic and paediatric Dulab) and the semi-automatic continuous blood culture system (Bactec 9000, using aerobic, anaerobic and paediatric bottles). A total amount of 1.250 blood samples collected from 626 patients was divided equally into the compared bottles and processed parallelly. The yield of the Bactec aerobic bottles was significantly higher than the yield of the transport bottles and aerobic Dulab bottles (p < 0.001). However, this result was influenced by the higher rate of contaminating bacteria isolated from the aerobic Bactec bottles. The yield of the aerobic Dulab bottles was higher than the yield of the transport bottles (p < 0.01). The average time needed for the detection of microorganisms in the Bactec bottles was by 24 hours shorter than in the transport bottles and by 19 hours shorter than in the aerobic Dulab bottles (p < 0.001). The difference between the yields of the anaerobic and the paediatric bottles in our study was not significant. The time needed for the detection of microorganisms was by 17 hours shorter in the anaerobic Bactec bottles than in the transport bottles (p < 0.05).

Bacteria↗

[Treatment of pancreatic stones with extracorporeal lithotripsy with sonographic localization].

BACKGROUND: Pancreatic stones may be treated by endoscopic extraction or by surgery. Extracorporeal shock wave lithotripsy increased possibility of noninvasive steps to their elimination. The aim of this study was to describe our first experience with this method. METHOD AND RESULTS: 10 patients (6 men and 4 women) in average age 47 years (between 19 to 72 years) were treated. The lithotriptor MEDILIT with sonographic targeting was used for fragmentation of pancreatic stones. Fragmentation was achieved in 8 patients, in 4 cases we observed spontaneous disappearnace, in 3 cases an endoscopic extraction of fragments was necessary. In one case good fragmentation was observed at control ECRP, but the repeated Wirsungography showed a big pseudocyst which had not been diagnosed at the first examination and surgery was necessary. In 2 cases no fragmentation was achieved and in these cases surgery was also indicated. No serious side effects were observed, nor elevation of amylase values compared with the situation before the shock wave treatment. CONCLUSIONS: Extracorporeal shock wave lithotripsy of pancreatic stones revealed good fragmentation and disappearance stone from ductus Wirsungi without serious side effects on clinical course and surrounding soft tissues.

Adult↗

[Prophylaxis of infectious endocarditis].

In spite of introducing antibacterial agents in prophylaxis of infective endocarditis (I.E.) more than 50 years ago, the optimal scheme for indication and application of the prophylaxis has not been solved. Evidences accumulate that prophylaxis (being developed to cover some medical procedures leading to bacteremia) can prevent only a small part (< 10%) of cases of I.E. The most effective protection from I.E. is the systematic care for gums and mucosae of the mouth cavity.

Anti-Bacterial Agents↗

[Perianal pyoderma].

Perianal pyoderma (hidradenitis suppurativa-acne conglobata) is a chronic disease which in its progressive form cannot be treated by conservative methods. Extensive suppurative foci must be radically excised incl. all systems of fistulas right down to the fascia and the defects which develop are allowed to heal per secundam or after several weeks they can at a different period of time be covered by a skin transplant. The authors present their 30-year experience with surgical treatment of 39 patients. Treatment was in all instances successful after radical surgical excision. All these patients have fully recovered as regards work capacity as well as social aspects.

Adolescent↗

[Energy expenditures in patients with acute and chronic catabolic conditions].

The authors investigated the energy expenditure and utilization of different nutrients by indirect calorimetry. They examined three groups of subjects: patients with acute febrile diarrhoeal diseases (n = 36), patients with subacute to chronic severe febrile diseases (n = 10) and healthy subjects (n = 21). The measurements were made three times a day. In all groups the energy requirements of the organism were met in the morning above all by fats, in the course of the day the ration of utilized carbohydrates increased markedly. The authors discuss the problem of optimal nutrition of patients in a critical condition from the quantitative and qualitative aspect.

Acute Disease↗

Treatment of a gastric bezoar by extracorporeal shock wave lithotripsy.

A bezoar of the stomach was diagnosed by X-ray and endoscopy in an 8-year-old boy who presented with intermittent dull epigastric pain. Attempts at endoscopic extraction failed because of the size and hardness of the bezoar. Extracorporeal shock wave lithotripsy was therefore applied using ultrasound to locate the bezoar. Disintegration of the bezoar and spontaneous evacuation of the fragments was achieved.

Bezoars↗