Copper-Catalyzed N-Arylation of Nitroenamines with Diaryliodonium Salts.

A novel synthetic methodology was developed for the N-arylation of nitroenamine derivatives utilizing diaryliodonium triflates and copper(I) chloride as a catalyst. The procedure enables the easy aryl transfer from the hypervalent species under mild catalytic conditions with unusual heteroatom preference and high efficiency.

Consumer habits and interests regarding non-prescription medications in Hungary.

PURPOSE: Patients increasingly use over-the-counter medicines for self-treatment but such products can be misused and/or abused. The primary aim of the present study is to survey the relationship between pharmacists and self-medication, to give an overview of their opinions on advertisements of non-prescription drugs and to evaluate the knowledge of and familiarity with medicines held by individuals purchasing them for self-treatment. METHODS: A marketing research study of non-prescription drugs in multiple pharmacies between March and July 2008 was conducted. A total of 2000 questionnaires were handed out, of which 1486 were evaluated. Statistical analysis was performed using SPSS 13.0 software. RESULTS: The majority of participants (72.5%) visited a community pharmacy at least once per month. Half of the respondents reported taking medications regularly. Forty per cent of those surveyed consult a qualified professional about their decision before buying non-prescription medications. Forty-four per cent of respondents reported asking pharmacists about the effects of non-prescription medications. CONCLUSION: This survey revealed that the general public has a high level of awareness concerning the abuse potential of over-the-counter medicines. Health care professionals should seek to understand and respect patients' choices to assure optimal care. Pharmacists could be more proactive in the management of inappropriate over-the-counter drug use.

Self-medication in Hungary, from the perspective of pharmacy workers.

The primary objective of this research was to evaluate the pharmacist's views on self-medication, their perceptions of advertisements for OTC medicines, and their knowledge and awareness of people that purchase OTC medicines. The data were gathered in Hungarian pharmacies with questionnaires distributed as inserts in two trade journals--Gyógyszertár and Pirulatrend. The questionnaires dealt with five main issues: advertisements for OTC medicines, questions related to self-medication, patient-pharmacist communication, questions related to the usefulness of patient information sheets, and demographic data. The gathered data were coded and analyzed with the SPSS 13 software. Some respondents (34.9%) believed that the effects of OTC medicines are exaggerated in advertisements. According to 58.2% of professionals, members of the public are aware of the medicine that is currently being advertised, but not of other medicines with similar effects. Providing assistance in self-medication is perhaps one of the most important means of promoting the correct use of medicines. Our results highlighted the need to strengthen communication between patients and pharmacists. Pharmacy workers are in a position to assist the public. However, little is known regarding the patient experience of the distribution and services provided by pharmacies related to OTC medicines. These experiences should be researched and combined with our findings in order to draft a set of guidelines for purchasing OTC medicines. We recommend that pharmacists keep individual records detailing patient experience and use of OTC medicines.

Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.

Heteroaromatic carboxylic esters of (nor)tropine were synthesized. Tropine esters displaced [(3)H]strychnine binding to glycine receptors of rat spinal cord with low Hill slopes. Two-site displacement resulted in nanomolar IC(50,1) and micromolar IC(50,2) values, and IC(50,2)/IC(50,1) ratios up to 615 depending on the heteroaromatic rings and N-methyl substitution. Nortropeines displayed high affinity and low heterogeneity. IC(50,1) and IC(50,2) values of tropeines did not correlate suggesting different binding modes/sites. Glycine potentiated only the nanomolar displacement reflecting positive allosteric interactions and potentiation of ionophore function. Affinities of three (nor)tropeines were different for glycine receptors but identical for 5-HT(3) receptors.

Synthesis of (nor)tropeine (di)esters and allosteric modulation of glycine receptor binding.

(Hetero)aromatic mono- and diesters of tropine and nortropine were prepared. Modulation of [3H]strychnine binding to glycine receptors of rat spinal cord was examined with a ternary allosteric model. The esters displaced [3H]strychnine binding with nano- or micromolar potencies and strong negative cooperativity. Coplanarity and distance of the ester moieties of diesters affected the binding affinity being nanomolar for isophthaloyl-bistropane and nortropeines. Nortropisetron had the highest affinity (K(A) approximately 10 nM). Two esters displayed negative cooperativity with glycine in displacement, while three esters of low-affinity and nortropisetron exerted positive cooperativity with glycine.

[Cost study of NSAID use in rheumatoid arthritis based on recent therapeutic protocols]. / NSAID szerek költség-ertékelése rheumatoid arthritisben az ervényben 1évo terápiás protokoll alapján.

In today's health care beside the medical perspective, economic aspects should also be taken into consideration. Because of the significant opportunity-cost, only the most cost-effective techniques should be subsidized, which result the highest net-benefit for the society. This paper focuses on the economic aspects of the chronic NSAID use in rheumatoid arthritis. Based on recent therapeutic protocols a cost study (partial economic evaluation) was carried out. Our results indicate that for patients with an average GI-risk retard diclofenac could be a possible good choice. For patients with moderate to severe GI risk, retard diclofenac + pantoprazole combination therapy should be prescribed. COX-2 inhibitors are advised only for a limited group of patients with specific conditions; because of their higher price and side effect profile (severe CV adverse effect and uncertain GI benefits). We would also highlight the importance of individual therapy. In complex our purpose was to evaluate current therapeutic guidelines from a pharmacoeconomic perspective.

[Medicating outside the consulting room]. / Gyógyszerelés a rendelon kívül.

INTRODUCTION: Self-medication is a means, besides changing one's lifestyle, of buying and taking non-prescription medicaments. This practice has several advantages. People save time and energy by not sitting for hours in the consulting room of the doctor with a simple ailment, and the doctors also have more time to deal with those requiring more serious treatment. Moreover, the expenditures of the state also decrease, as patients do not visit the doctor but buy non-prescription, i.e. non-supported, medicaments. AIMS: The authors surveyed the habits and demands of a survey population concerning non-prescription medicaments, primarily in the pharmacies of Fejér county. A marketing research programme was completed in order to establish better co-operation between patients and pharmacists, within the framework of which 1450 questionnaires were distributed from March to June in 2005, 743 of which were completed and evaluated. METHOD: The authors examined, whether there were differences within the answers given to professional questions (questions 1-25 of the questionnaire) through sex, age, qualifications and earning power. Answers were analyzed by statistical methods. Statistical analyses were carried out with the SPSS 13.0 program group. Those results were published, where significant differences were found. RESULTS: Half of the respondents take medicaments regularly, 65% of them watch advertisements about medicaments several times a day. 40% of those surveyed consult a professionally-qualified person about their decision before buying non-prescription medicaments. The population obtains much information from the brochures enclosed with medicaments, and almost 70% of them read these brochures. According to their opinions, when buying non-prescription products, pharmacists always recommend other possibilities as well, and they give details about the information concerning the application of the medicaments. CONCLUSIONS: In order for people to use non-prescription products properly, it would be definitely necessary to elaborate a successful national education strategy. The population expects information concerning medicaments to be communicated in the pharmacies in an understandable way. It should be in the pharmacy where patients learn about the medicaments they take, where the pharmacist knows what other medicines have been prescribed by a doctor, and whether patients have any illnesses whereby they should not take other products.

[Practice of antidiabetic therapy in Hungary]. / Az antidiabetikum terápia gyakorlata Magyarországon.

Type 2 diabetes is one of the biggest public health problems of our age. In the present study the authors analyse the development of the therapy of type 2 diabetic patients. National antidiabetic consumption data and data of National Health Insurance Fund Administration (OEP) were used. From OEP database definite method were used to choose 1002 type 2 diabetic patients. The Hungarian therapeutic practice develops according to guidelines of multi centered studies, and the consumption of antidiabetics dynamically increases. Increasing the number of patients who get insulin therapy and among patients who get oral antidiabetics more of them get insulin resistance decreasing therapy. However the out-of-date drugs (non-micronized glibenclamide, buformin) are still in daily therapy. The authors revealed the ratio of diet and drug (monotherapy, combination therapy) therapy, the higher use of Sulfanylurea monotherapy than recommended and the use of unreasonable combinations.

[Analysis of quality of life among patients with bronchial asthma or rheumatoid arthritis]. / Eletminóség vizsgálata asthma bronchialés és rheumatoid arthritises betegek körében.

AIMS: The authors have analysed the quality of life of 228 asthmatic patients and of 81 patients suffering from rheumatoid arthritis with a general and a disease specific instrument. RESULTS: Their results indicate that the subjects experience a lower level of quality of life. Despite the availability the valid clinical tests they can not predict how the patients feel, what is their health status like. CONCLUSIONS: In every day clinical practice it is necessary to quantify the patients quality of life especially in chronically ill patients. To do so it is important to use reliable instruments which are easy to use. They have found strong correlation between the Euro-QoL and the disease specific instruments both in asthma and rheumatoid arthritis, so they could conclude that the Euro-QoL questionnaire is an easy and reliable instrument in daily practice to assess the quality of life of asthmatics and patients suffering from rheumatoid arthritis.

[Pathogenesis and treatment of Wilson's disease]. / A Wilson-kór patomechanizmusa és gyógyszeres kezelése.

Authors review the pathogenesis, symptoms and diagnosis of Wilson's disease. Wilson's disease or hepatolenticular degeneration is an autosomal recessive disorder. It is caused by defective hepatic excretion of copper. The disease is fatal without treatment. The prevention of severe permanent damage depends upon early recognition and diagnosis followed by appropriate lifelong anticopper treatment. The purpose of the therapy of Wilson's disease is to eliminate the copper by chelators (D-penicillamine, triethylene tetramine, ammonium tetrathiomolibdate) and to inhibit the absorption and accumulation of copper by zinc salts (zinc sulphate, zinc acetate, zinc gluconate).

Self-reported medication and lifestyle adherence in Hungarian patients with Type 2 diabetes.

BACKGROUND: Type 2 diabetes is a complex disorder that requires the patient to pay constant attention to diet, physical activity, glucose monitoring and medication. OBJECTIVE: To evaluate the medication, lifestyle adherence and factors associated to these in Type 2 diabetes in Hungarian patients. SETTING: Fourteen community pharmacies in Hungary between March and May 2004. METHOD: A questionnaire was given to every tenth Type 2 diabetic patient who presented to one of the 14 pharmacies included in this study with a prescription for oral antidiabetics, oral antidiabetics and insulin or exclusively insulin. For the latter two groups, the prerequisite for inclusion in the study was also that their diabetes had developed after the age of 35 and that at some in their treatment regimen they had taken only oral antidiabetics. These latter two criteria were controlled in the patient's general practitioners' (GP) database. General and diabetes-related data were collected in the questionnaire, and the adherence and lifestyle of the participant were assessed. An adapted and validated Hungarian version of the EQ-5D (EuroQol Group, 1993) quality-of-life questionnaire was also included. Descriptive and chi(2) test statistical methods and two sample t-test were used. A significance level of P<0.05 was considered to be significant. MAIN OUTCOME MEASURE: Patient self-reported adherence to diet, physical activity, self monitoring of blood glucose, purchasing of drug(s), drug regimen, association of demographic factors, treatment, lifestyle and quality of life on adherence. RESULTS: Of the 220 questionnaires distributed to diabetic patients, 151 were returned, of which 142 were evaluated (nine did not satisfy the above-mentioned inclusion criteria). With respect to the factors assessed, sub-optimal adherence was assessed for: diet (76.8%), physical activity (33.8%), self-monitoring of blood glucose (81%), drug purchasing (20.4%) and drug taking (52.1%). Smokers comprised 14.8% of the respondents, while 8.5% were heavy drinkers. Fewer than five meals a day were eaten by 46.5% of the patients, and about 43.6% of the patients did not self-monitor blood glucose. The results indicate few significant associations between at least one of the four main areas of adherence (diet, physical activity, purchasing of drug(s), drug regimen) and body mass index, GP consultation frequency, quality-of-life parameters and EQ-5D index. CONCLUSION: The adherence of Hungarian Type 2 diabetics in some areas does not reach optimal levels, especially for diet, self-monitoring, drug purchasing and adherence to drug taking.

Factorial design for the analysis of patient's quality of life in asthma.

Chronic diseases like asthma have a great impact on the everyday life of patients. Evaluation of a patient's quality of life informs us about how the patient is feeling and whether or not he or she is able to function physically, socially and emotionally. The objectives of this study were to assess the quality of life of asthmatic patients and to study the influence of age and disease severity, as independent variables, on the patient's quality of life. A 2-factor, 3-level face-centred central composite design was applied to construct a second-order polynomial model describing the effects of age and the severity on the quality of life. The second-order polynomial model was successfully applied to describe the effect of age and asthma severity with good correlation on the quality of life measured by either generic (Visual analogue scale) or disease specific (St George's Respiratory Questionnaire) instruments in the examined subjects. Our findings suggest quality of life may be used as a non-invasive patient-centred monitoring system as a guide for disease management if measured regularly.

Antidiabetic drug utilization in hungary.

OBJECTIVE: To evaluate the utilization trends of antidiabetics in Hungary. METHOD: The analysis includes the drugs of antidiabetic therapy which were registered between 1998 and 2002 in Hungary. The consumption of antidiabetic drugs was analyzed by the ATC/Defined Daily Dose (DDD) method. The data used in this study were derived from the National Health Insurance and from MIS Consulting Company. RESULTS: Between 1998 and 2002, the total consumption of antidiabetics increased by 41.8%, and reached 47.59 DDD/1000 inhabitants/day in 2002. The consumption of oral antidiabetics (OAD) increased by 33.41% (33.86 DDD/1000 inhabitants/d ay in 2002), while in the case of insulin the increase was 67.8% (13.74 DDD/1000 inhabitants/day). Sulphonylureas were the most frequently used class (21.11 DDD/1000 inhabitants/day in 2002). Glibenclamide was the most frequently used antidiabetic drug (12.63 DDD/1000 inhabitants/day in 2002). CONCLUSION: The insulin class had greater emphasis in therapy. Among OAD, the consumption rate of sulphonylureas decreased and the consumption rate of Biguanides and acarbose increased. By 2002 metformin replaced 90% of the buformin in use. The limited effect of therapeutic recommendations could explain these changes, although the out-of-date buformin and the non-micronized glibenclamide were still in use in 2002.