160 resultados para atropisomerism of drugs
Resumo:
Large volume parenteral solutions (LVPS) are widely used as vehicles for intravenous administration of drugs and polyvinyl chloride (PVC) flexible bags are, nowadays, the plastic containers most commonly used to pack and drip-feed LVPS. An advantage of using bags is that they collapse flat and thus reduce the risk of airborne contamination and embolism caused by air in the bloodstream. They are mainly used in hospitals. This review deals with some important aspects of the PVC packaging containing the plasticizer DEHP, generally used to pack LVPS. The interaction between drug and package is discussed, with an emphasis on the migration of DEHP from the PVC bag to LVPS containing the immunosuppressant cyclosporin, and toxicological aspects are considered.
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This study was carried out in order to identify the interactions that occur most often between prescribed drugs as they are taken by elderly patients attending municipal public health centers in the city of Jaú, São Paulo State, Brazil. It is known that older people frequently have to live with chronic health problems, which oblige them to use the health service a great deal and to consume large quantities of medicines. When concomitant diseases are present, and polytherapy is being applied, the likelihood of adverse reactions and interactions between drugs increases. The population under study consisted of 148 persons aged 65 or more who frequented the pharmacy at the Núcleo de Gestão Assistencial (Municipal Health Centre, NGA25) in Jaú, between August and December 2004. Data were collected from medical prescriptions, the independent variables being the age and sex of the patient. For each patient, the pharmacological classes of drugs taken and drug-drug interactions were recorded. It was found that the mean numbers of drugs consumed were 3.8 among women and 3.9 among men. In terms of age, the highest number of drugs (4.2) was used in the group aged 75 to 84 years. The most frequently prescribed classes, in decreasing order, were: antihypertensives, 25.0%, heart drugs, 15.5%, diuretics, and anti-diabetic drugs, 10.7%. It was concluded that the classes most involved in drug-drug interactions were heart drugs, diuretics and antihypertensives. The most problematic active constituents were digoxin, amiodarone, frusemide, captopril, propranolol and nifedipine.
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The aim of this work was to evaluate the influence of compression force and humidity in the dissolution profile of tablets formulation. As hidroclorotyiazide presents real problems of bioavailability, it was incorporate as standard drug in a formulation of tablets to study the mechanical resistance, time of disintegration and dissolution profile in function of humidity and compression force. The time of disintegration was not affected by the compression force, but it was influenced by humidity. The dissolution profile was altered by the compression force and for the humidity as well. Both factors can alter the bioavailability of drugs dispensed in the form of tablets.
Resumo:
The use of the nasal route for drug delivery has attracted much interest in recent years in the pharmaceutical field. Local and principally systemic drug delivery can be achieved by this route of administration. But the nasal route of delivery is not applicable to all drugs. Polar drugs and some macromolecules are not absorbed in sufficient concentration due to poor membrane permeability, rapid clearance and enzymatic degradation into the nasal cavity. Thus, alternative means that help overcome these nasal barriers are currently in development. Absorption enhancers such as phospholipids and surfactants are constantly used, but care must be taken in relation to their concentration. Drug delivery systems including liposomes, cyclodextrins, micro- and nanoparticles are being investigated to increase the bioavailability of drugs delivered intranasally. This review article discusses recent progress and specific development issues relating to colloidal drug delivery systems in nasal drug delivery. © 2006 Bentham Science Publishers Ltd.
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Aim: To evaluate the presence of preservatives, dyes, sweeteners and flavouring substances in 73 pharmaceutical preparations of 35 medicines for oral administration, according to drug labeling information about the excipients. Methods: 35 medications were selected, both over-the-counter and prescription durgs, marketed in Brazil. The sample included: analgesic/antipyretic, antimicrobial, mucoregulatory, cough and cold, decongestant, antihistamine, bronchodilator, corticosteroid, antiinflammatory and vitamin medications. We collected data on 73 preparations of these drugs, according to drug labeling information regarding preservatives, dyes, sweeteners and flavourings. Results: Methylparaben and propylparaben were the most common preservatives found (43% and 35.6% respectively). The most common sweeteners were: sucrose (sugar) (53.4%), sodium saccharin (38.3%) and sorbitol (36.9%). Twenty-one medicines (28,7%) contained two sweeteners. Colourless medicines predominated (43.8%), followed by those with sunset yellow dye (FD&C yellow no. 6) (15%). Five products (6.8%) contained more than one colour agent. Tartrazine (FD&C yellow no. 5) was present in seven preparations (9.5%). Fruit was the most common flavouring found (83%). Labelings of drugs which contained sugar frequently omitted its exact concentration (77%). Of the four labelings of medicines which contained aspartame, two did not warn patients regarding phenylketonuria. Conclusions: Omission and inacuracy of drug labeling information on pharmaceutical excipients may expose susceptible individuals to adverse reactions caused by preservatives and dyes. Complications of inadvertent intake of sugar-containing medicines by diabetics, or aspartame intake by patients with phenylketonuria may also occur.
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The present work aims to raise the costs of high-cost drugs used to treat patients of Refractory Schizophrenia in ambulatory unit. The study was carried out in the Psychosocial Support Center, which treated 33 patients with these medications, during the period of June, 2005 to May, 2006. Data analysis disclosed that the mostly used drugs to treat the carriers of Refractory Schizophrenia were: clozapina and risperidona. It was observed that the treatment with olanzapina is more expensive than that with risperidona. The study concluded that the analysis of the consumption and costs of drugs of high cost is necessary to subside better management of the expenses and new investments in the service. Moreover, the necessity of more studies in the area was also identified to contribute with the control of costs.
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Due to great difficulty of penetration of drugs through skin, different organized systems, such as liposomes, have been studied in order to increase percutaneous penetration. The aims of this work were to obtain and characterize small unilamellar liposomes containing caffeine (CAF). Liposomes composed by soy phosphatidylcholine - PS (40 mM) or hydrogenated PS - PSH (40 mM), with and without cholesterol - CHO (6 mM) and CAF (30 mg/mL), were characterized by size distribution, determination of mean diameter and encapsulation efficiency. Uniform size distribution with low polidispersity was observed. The mean of diameters obtained were: PS/CHO (64 nm), PS (80 nm), PSH/CHO (85 nm), PS/CAF (145 nm), PS/CHO/CAF (147 nm), PSH/CHO/CAF (152 nm), PSH (166 nm) and PSH/CAF (481 nm). The obtained encapsulation efficiency was 10.84% for PSH/CHO/CAF, followed by PS/CHO (6.61%), PSH/CAF (3.07%) and PS/CAF (1.57%).
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A rapid, sensitive and reliable thin-layer chromatography/spectrophotometry screening procedure was developed for quantitative determination of diuretics associated in pharmaceutical dosage forms. The chromatographic method employed microcrystalline cellulose and butanol : acetic acid : water (4:1:1) or amilic alcohol : ammonium hydroxide 25% (9:1) as mobile phases and detection by U.V. light. The drugs were extracted using a simple procedure and were quantified by U.V. spectrophotometry. Results varied from 97.5 to 102.5% and are similar to those obtained by conventional methods. This method of quantification of diuretics is promising for quality control of drugs.
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The anthracyclines constitute a group of drugs widely used for the treatment of a variety of human tumors. However, the development of irreversible cardiotoxicity has limited their use. Anthracycline-induced cardiotoxicity can persist for years with no clinical symptoms. However, its prognosis becomes poor after the development of overt heart failure, possibly even worse than ischemic or idiopathic dilated cardiomyopathies. Due to the successful action of anthracyclines as chemotherapic agents, several strategies have been tried to prevent/ attenuate their side effects. Although anthracycline-induced injury appears to be multifactorial, a common denominator among most of the proposed mechanisms is cellular damage mediated by reactive oxygen species. However, it remains controversial as to whether antioxidants can prevent such side effects given that different mechanisms may be involved in acute versus chronic toxicity. The present review applies a multisided approach to the critical evaluation of various hypotheses proposed over the last decade on the role of oxidative stress in cardiotoxicity induced by doxorubicin, the most used anthracycline agent. The clinical diagnosis and treatment is also discussed. © 2008 Bentham Science Publishers Ltd.
Resumo:
According to the possible influence of systemic diseases and of drugs used for its treatment in buccal cavity, the aim of present study is to carry out a review of literature on this topic, emphasizing on influence of these factors on use of the total prostheses (PTs), allowing to surgeon-dentist a better scientific knowledge to creation of this type of rehabilitation treatment.
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Recent studies have shown consistent results using the physical therapy in cases of pain and limitation of movement from temporomandibular dysfunction. Thus, our objective was to assess the effect of ten sessions of physical therapy and laser therapy in treatment of muscular pain and arthralgias in a woman with temporomandibular dysfunction. The painful symptoms relief achieved by session was over 20 %, up to zero at the end of treatment. Results demonstrated that the treatment protocol used was effective to reduce the temporomandibular joint and the masseter muscle tension and a decreased of drugs by patient. However, more studies are needed to define with more accuracy the effect of other physiotherapy programs and its interaction with other treatment modalities.
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Triamcinolone (TRI), a drug widely used in the treatment of ocular inflammatory diseases, is practically insoluble in water, which limits its use in eye drops. Cyclodextrins (CDs) have been used to increase the solubility or dissolution rate of drugs. The purpose of the present study was to validate a UV-Vis spectrophotometric method for quantitative analysis of TRI in inclusion complexes with beta-cyclodextrin (B-CD) associated with triethanolamine (TEA) (ternary complex). The proposed analytical method was validated with respect to the parameters established by the Brazilian regulatory National Agency of Sanitary Monitoring (ANVISA). The analytical measurements of absorbance were made at 242nm, at room temperature, in a 1-cm path-length cuvette. The precision and accuracy studies were performed at five concentration levels (4, 8, 12, 18 and 20μg.mL -1). The B-CD associated with TEA did not provoke any alteration in the photochemical behavior of TRI. The results for the measured analytical parameters showed the success of the method. The standard curve was linear (r2 > 0.999) in the concentration range from 2 to 24 μg.mL -1. The method achieved good precision levels in the inter-day (relative standard deviation-RSD <3.4%) and reproducibility (RSD <3.8%) tests. The accuracy was about 80% and the pH changes introduced in the robustness study did not reveal any relevant interference at any of the studied concentrations. The experimental results demonstrate a simple, rapid and affordable UV-Vis spectrophotometric method that could be applied to the quantitation of TRI in this ternary complex.
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Polymorphism can cause quality deviations during the production of medicines and can influence their effectiveness. Therefore, an understanding of this phenomenon and its implications opens a wide field of possibilities to be explored in the pharmaceutical field, including the emergence of new paradigms and tools for the quality assurance of medicines. This paper presents an introduction to basic aspects of the polymorphism phenomenon and its implications for the production and control of medicines, with emphasis on drug polymorphs.
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The objective of this paper was to review data on residues of medical products in aquatic environments and at wastewater treatment plants. Secondarily the paper presents a discussion about the need for a good management of drugs residues and effluents generated by this sector. Bringing the evidences of environmental possible damages reported by ecotoxicity data on the effects of fluoxetine to Vibrio fischeri and H. azteca, aquatic organisms daily exposed to environmental contaminants. From the results we observed that 0.3 mg.l-1 of fluoxetine hidrochloride induced lethality to H. azteca and 30 mg.l-1 reduced the luminescence of Vibrio fischeri. This assay evidenced higher toxicity when we used the generic product.
Resumo:
The incidence of fungal infections has increased significantly, so contributing to morbidity and mortality. This is caused by an increase in antimicrobial resistance and the restricted number of antifungal drugs, which retain many side effects. Candida species are major human fungal pathogens that cause both mucosal and deep tissue infections. Recent evidence suggests that the majority of infections produced by this pathogen are associated with biofilm growth. Biofilms are biological communities with a high degree of organization, in which micro-organisms form structured, coordinated and functional communities. These biological communities are embedded in a self-created extracellular matrix. Biofilm production is also associated with a high level of antimicrobial resistance of the associated organisms. The ability of Candida species to form drugresistant biofilms is an important factor in their contribution to human disease. The study of plants as an alternative to other forms of drug discovery has attracted great attention because, according to the World Health Organization, these would be the best sources for obtaining a wide variety of drugs and could benefit a large population. Furthermore, silver nanoparticles, antibodies and photodynamic inactivation have also been used with good results. This article presents a brief review of the literature regarding the epidemiology of Candida species, as well as their pathogenicity and ability to form biofilms, the antifungal activity of natural products and other therapeutic options. © 2013 SGM.