[Tibiotalocalcaneal arthrodesis using a retrograde nail locked in the sagittal plane]. / Tibiotalokalkaneální artrodéza retrográdním hrebem jisteným v rovine sagitální.

PURPOSE OF THE STUDY: To evaluate our experience with the use of a retrograde nail locked in the sagittal plane for tibiotalocalcaneal arthrodesis indicated in severe post-traumatic arthritis of the ankle. MATERIAL: Twenty patients, 16 men and four women at an average age of 58.7 years (range, 23 to 72) were evaluated. All patients had severe post-traumatic changes in the talocrural and talocalcaneal joints. Five patients also had an equinus deformity. In two patients arthrodesis followed the treatment of purulent arthritis of the talocrural joint. A local fasciocutaneous flap was used for soft tissue reconstruction in three patients. All patients were operated on using the standard surgical technique. METHODS With the patient in a supine position, reamed by hand with the use of a driving rod, a straight retrograde AAN Orthofix nail was inserted through the heel bone and talus into the distal tibia and locked in these bones in the sagittal plane. RESULTS: No complications such as injury to the neurovascular plexus or pseudoarthrosis were recorded. Four patients showed a reaction to the proximal locking screw on the proximal tibial surface, which was treated by earlier screw removal under topical anaesthesia. Due to infectious complications, the nail had to be removed prematurely in one patient. The average Foot Function Index was 12 points (range, 10 to 15) and the average ankle-hindfoot score was 67.6 points (range, 59 to 84). Thirteen patients (65 %) were not limited in their daily activities or recreational sports, six (30 %) experienced pain in sports but not daily activities and one patient (5 %) reported pain even when walking. All fusions healed in the correct position within 18 weeks. DISCUSSION: Tibiotalocalcaneal arthrodesis is not a frequent surgical procedure in either trauma surgery or orthopaedics. For this complicated procedure, rather than intramedullary nails, internal fixation with screws or plates or external fixation are preferred. The high rate of bony healing can be explained by maintenance of exact nail locking in the sagittal plane. The antero- posterior approach provides a more secure locking in the bone and assists in neutralizing sagittal forces at the site of arthrodesis. The use of reamed interlocking nails can therefore be accepted not only for treatment of long-bone fractures, but also for treating pseudoarthrosis and in complicated or failed arthrodesis. CONCLUSIONS: Patients' satisfaction is the primary goal we strive to achieve in severe post-traumatic conditions of the talus and foot. Repeat surgery, spongioplasty, external fixation revision for pin-tract infection, persistent pain, activity restriction and poor clinical results reduce patients' satisfaction. In our group, the rate of healed arthrodesis was high and the number of complications was low, therefore our patients' satisfaction was high.

[Blockers of beta-adrenergic receptors--a group of chiral agents stereoselective synthesis of beta-blockers]. / Blokátory beta-adrenergických receptorov--skupina chirálnych lieciv stereoselektívna syntéza beta-blokátorov.

Besides chromatographic methods and biocatalyzed reactions, another alternative method of obtaining enantiomeric forms of beta-blockers is stereoselective synthesis. This paper links up with two preceding surveys concerning beta-blockers--groups of chiral agents and presents a survey of the hitherto published enantioselective syntheses of (R)- and (S)-enantiomers of beta-blockers. In the group of arylaminoethanols, mainly selective reduction of prochiral ketones in the presence of metallic complexes is used in this type of synthesis. Enantiomerically pure beta-blockers of the aryloxyaminopropanol type are synthesized by means of a reaction of pertinent phenols with different chiral precursors, such as (R) and (S)-chloromethyloxirans, (S)-glycidoltosylate, (S)- or (R)-2,3-O-isopropylideneglyceroltosylate, E-(2S,3S)-3-trimethylsilylglycidol and (S)-3-terc-butyl-5-phenyl-oxazolidine-5-ylmethanol. Many of these chiral semiproducts can be prepared from natural substances, such as D-mannitol and L-ascorbic acid.

[Adrenergic beta-receptor blockers--a group of chiral drugs: enantioseparation in the group of beta-blockers]. / Blokátory beta-adrenergických receptorov--skupina chirálnych lieciv: enantioseparácie v skupine beta-blokátorov.

The preparation of pure individual enantiomers represents a topical problem from the standpoint of efficacy and safety of drugs. This paper continues in the preceeding review of the blockers of beta-adrenergic receptors as a group of chiral drugs, which is concerned with different pharmacodynamic, pharmacokinetic, and toxicological effects of individual enantiomers of this group. The review paper pays attention to the problems of enantioseparation of this group of chiral drugs, listing individual examples of the methods of enantioseparation, such as crystallization, biocatalysis, chromatographic methods (HPLC, GC, TLC), capillary electrophoresis, and the method of nuclear magnetic resonance (NMR). The individual methods of enantioseparation including enantioseparation in biological material (urine, serum) are illustrated on examples on beta-blockers used in clinical practice (e.g., propranolol, atenolol, metoprolol) as well as potential agents of this group of drugs.

[Chiral switch: pure enantiomers of drugs instead of racemic mixtures]. / Chirální zamena--"chiral switch": cisté enantiomery léciv místo racemických smesí.

Chirality of drugs, particularly the comparison of efficacy of enantiomers and their racemic mixtures, has become an object of serious interest of pharmaceutical researchers in recent ten or fifteen years. Advances in chemical technologies connected with the synthesis, separation, and analysis of pure enantiomers from racemates, together with administrative regulatory measures, have resulted in an increase in the number of newly registered chiral drugs containing only one of the enantiomers. Besides new chemical entities, many "old" racemates are being re-evaluated as potentially new sources of pure enantiomers which should improve the therapeutic profile of the drug. Due to this replacement of a racemic mixture with a pure enantiomer, the literature lists both drugs containing a racemate and drugs containing only one of the enantiomers. Nevertheless, the required therapeutic effect is not always achieved, and unexpected undesirable effects have also occurred. The paper summarizes therapeutic and economic problems concerning chiral switch drugs.

[Radioprotective effects of basic copper carboxylate complexes]. / Radioprotektivní úcinek nekterých základních karboxylatomednatých komplexu.

The radioprotective activity of eight selected copper (II) carboxylates--Cu (RCOO)2.nL (R = alkyl, aryl, 2-furyl and 2-thienyl; L usually represents water)--was assayed in a model of lethally gamma-irradiated (9 Gy, 0.97 Gy/min) mice. The compounds tested were applied (as solutions in saline) s.c. in three single doses of 20 mumol/kg 48.24 and 6 h before irradiation. The highest radioprotective effects were measured by survival of mice achieved after premedication of animals with copper (II) 2-thenoate monohydrate (77%), copper (II) acetylsalicylate (64%), copper (II) 2-methoxybenzoate monohydrate (62%) and copper (II) acetate monohydrate (54%). On the other hand, survival of vehicle-pretreated mice was only 10%. The observed biological properties of complexes are discussed in relation to their structures.

[Anti-ulcer effectiveness of mono- and dibasic carbamates with local anesthetic effects]. / Studium antiulcerózního úcinku mono a dibazických karbamátu s lokálne anestetickou úcinností.

An evaluation of anti-ulcer effects of mono- and dibasic carbamate local anaesthetics was performed using two experimental models of gastric ulcers, i.e. those induced by stress, or by ligation of the pylorus. These models have been found not to be identical. In the case of stress-induced ulcers, no experimental animal died as compared to the second experimental group with a 30% mortality rate due to the more frequent occurrence of ulcer perforations. Result similarities of both models could only be found with respect to the range of damage of the mucous membrane of the stomach. A premedication with a majority of basic carbamates decreased the incidence and range of ulcer lesion. The anti-ulcer activity of monobasic carbamates was more significant when compared with dibasic compounds.

The influence of carbamate local anesthetics on the occurrence of experimental gastric ulcers.

Evaluation of the antiulcer effects of a series of 2-piperidineethylesters of o-alkoxy-substituted phenylcarbamic acids were performed using two experimental models of gastric ulcers, e.g. induced by stress or by ligation of the pylor. It was found that these models were not identical. In the case of stress-induced ulcers, no experimental animal died as compared to the second experimental group with a 30% mortality rate due to the more frequent occurrence of ulcer perforations. Result similarities of both models could only be found with respect to the range of damage of the mucous membrane of the stomach. A premedication of rat with basic carbamates in the dose 20 mg.kg-1 p.o. resulted in a reduced incidence of stress- and ethanol-induced ulcerous lesions. The most significant antiulcer activity was found using compounds designated as the No. XIII, XVI and XIX. Pretreatment of rats with basic carbamates in the case of Shay ulcers has again resulted in a reduced range of ulcer lesions which was most expressive using compounds No. XVI and XIX.