The purpose of this study was to assess prescription rationality and most common prescription errors at the primary care clinic of a Mexican university. A retrospective drug utilization review of indication prescription type was carried out. A random sample of 370 medical records of patients assisted over a year period, were reviewed. Prescription appropriateness was evaluated according to the variables: indication, dosage regimen, administration route, contraindications, interactions, medication duplicity, unnecessary or missing medications. Prescriptions were rated as appropriate (no prescription errors found) or inappropriate (at least one prescription error found). The benefit-risk ratio was calculated for each prescription. This study revealed a 58% of inappropriate prescriptions in the Mexican primary care university clinic, mostly due to errors on dosage regimen and innapropiate drug selection. As a result of chi(2) analysis, it was found that the pharmacotherapeutic variables chosen for the prescription assessment in this study, were determinant in prescription appropriateness rating. Nimesulide, ciprofloxacin, ranitidine, ketorolac and paracetamol were the most prescribed drugs as well as the most common cause of errors found The prescription error rate revealed by this study addresses the need for strategies to improve prescription's quality. Introducing pharmacists as a key part of health care team is a mean proposed to prevent medication errors and to solve the urgency of pharmaceutical care implementation in all primary care facilities in Mexico.
Aqueous and acetone extracts from 15 fruits have been screened for antioxidant activity using DPPH method and beta-carotene/linoleic acid model. All fruits studied showed antioxidant activity, but in different extent. Acerola, cashew-apple, popaya "formosa", papaya "solo", orange and guova showed the higher antioxidant activity); (> 70%) in DPPH method, followed by pineapple, bergamont, mango "rosa", melon "reticulares", melon "inodorus", melon "orange flesh" and sugar-apple aqueous extract (moderate, 60-70%) and mango "espada" and watermelon aqueous extract, the lowest activity Acerola, cashew-apple, sugar-apple and guava acetone extracts exhibited higher scavenging activity toward DPPH radicals (> 70%). beta-carotene/linoleic acid model index of sugar-apple aqueous extract and guava acetone extract demonstraled moderate antioxidant activity (60-70%), meanwhile acerola aqueous extract and papaya "formosa" acetone extract the lower. According to antioxidant activity, fruits can be indicated as natural antioxidants sources, pointing out acerola, cashew-apple, papaya "solo", papaya "formosa", guava, orange and sugar apple as the highest in antioxidant capacity.
In an attempt to analyze how processing enhances the nutritional value of the mandim fish (Arius spixii) marketed in Maceio-AL, Brazil, the following nutritional components were determined in fresh and processed (salted-dried)fish: centesimal composition, calorie count, chloride,fatty acid and cholesterol profile. The presence of cholesterol oxides was also investigated. Respective results for fresh and processed mandim fish were: moisture (70.13% and 40.31%), proteins (51.73% and 38.07%, dried), carbohyrdrates (4.67% and 2.24%, dried), calories (486 kcal/100g and 367 kcal/100g, dried), fatty acids (polyunsaturated 14,54% and 15,49%, omega-3 8,51 % and 6,51%), cholesterol (82.66 mg/100g and 61.30 mg/100g) and oxides (7-ketocholesterol 8.31 mu g/g and 17.90 mu g/g). These figures clearly showed that processing led to significant change in the nutritional value of the mandim fish.
The suitable patients' medication knowledge is a essential factor for the medication compliance. The level of medication knowleage in patients with chronic kidney disease (CKD) and the medication knowledge associated factors were assessed in a cross-sectional study petforined with 130 subjectsfroin a nephrology outpatient university clinic, continuously taking some self-administered drug from the C, H02 or L04 groups of the Anatomical Therapeutic Chemical classification system and who were not on a kidney replacement therapy. The level of medicationknowledge was measured through a researcher-administered questionnaire and a score ranking from zero to ten points. Three levels of knowledge were defined: low (less than six points), moderate (six to eight points) and high (more than 8 points). The patients' medication knowledge average score was 7.8 +/- 1.7 points and 51.5% of the patients showed low or moderated level of knowledge. The factors associated to the high level of medication knowledge were: fast decline of the glomerular filtration rate, control of the blood pressure and the patients' belief that they suffered adverse drug reaction to any of the prescribed medcines. Most patients had insufficient knowledge for a safe and effective use of prescribed medicines, soa better patient counseling is necessary.
The purpose of this research was to determine the potential of papain and pequi oil as penetration enhancers for diclofenac sodium (DS) across human skin in vitro. The permeation studies were conducted with vertical diffusion cells. The enhancers were associated or not in gels in different concentrations. In vitro studies reveled that papain 0.2% (w/v) presented an elevated enhancer property for diclofenac sodium (J = 0.3369 mu g/cm(2)x h). Pequi oil 10% (w/v) generated a reduced flux value (J = 0.1848 mu g/cm(2) x h) and a combination of both enhancers presented a medium value of J = 0.2187 mu g/cm(2) x h. Papain was found to be better enhancer than pequi oil.
Plinia edulis (Myrtaceae), popularly known as "cambuca", is a Brazilian medicinal plant employed in the treatment of stomach problems and throat affections by the "caicaras", fishermen of coastal localities. Aiming to contribute with the species knowledge the leaves of P. edulis were analyzed macro and microscopically and the chemical composition of the volatile oil was determined using a combination of GC/MS and retention indices. The antimicrobial assay and the phytochemical screening of the aqueous ethanol extract of the leaves have been performed to correlate the secondary metabolites and the traditional use. Leaves present morphological characteristics of others Myrtaceae species and some particularities, such as the circular idioblasts in number of 2 to 4, scattered perpendicularly at the adaxial surface, with druses or prismatic crystals. In the volatile oil fifteen components have been identified, of which epi-α-cadinol (21.7%), α-cadinol (20.2%) and trans-caryophyllene (14.2%) were major. The phytochemical screening of the aqueous ethanol extract showed the presence of substances with pharmacological interest, such as flavonoids, tannins, saponins and terpenoids but, despite of the presence of these classes, the extract did not inhibit the growth of Aspergillus niger, Candida albicans, Escherichia coli and Staphylococcus aureus in a concentration of 1,000 mg/mL.
Pharmacy Benefits Management (PBM), a system that manages benefits in the purchase and sale of drugs, is of relatively recent implementation in Brazil. Taking into relatively recent implementation in Brazil. Taking into account that the development of bacterial resistance is related to the inadequate prescription of antibiotics or to the use of low activity antibiotics, this study sought to assess the capability of PBM to provide useful information on the profiles of prescription and purchase of systemic antibiotics. The data used for this pin-pose were collected from the database of a Brazilian PBM company and related to a group of 6 525 metalworkers of a company located in the region of Campinas, SP and to their dependents, covering the period from January to April 2005. Of the drugs purchased, 7.7% were systemic antibiotics, with a mean of 2.4 antibiotics undo mean cost of R$ 51.80 per prescription. Amoxicillin was the most prescribed drug. In 92.7% of cases, users purchased the prescribed drug within one day of the Medical visit. Based on the lists of purchased pharmaceutical specialties (per retail package), manufacturers, antibiotics present in the composition of each product, prescription dates, and dispensation dates, the system was found capable of providing relevant information on the theme investigated.
Variabels on therapeutic knowledge in pre- and post-intervention periods and the social and demographic characetristics of 80 middle-aged and elderly (45 years or more) patients in three parish communities in Cascavel. PR-Brazil are provided. A pharmacoepidemiological survey was developed; a prospective study between November 2003 and December 2004 was undertaken; data were collected in a semi-structured form. Females (82.5%) were predominant; average age 67.3 years old; schooling less than 8 years; most of them married (57.5%); only the couple inhabits the house (63.7%); income 1 to 3 salaries (80%); mean numbers of prescribed medcines pre- and post-intervention were 4.3 and 3.5, respectively. Medicine for the cardiovascular system (48%) was the most described (48%). Variables-reading information on drug and its frequency, knowledge on the medicine used and importance of information- were statistically non-significant, although difference in relative frequency from the pro- to the post-intervention period existed. Nevertheless, difference with regard to degree of progress in results shows clinical relevance with a favorable trend towards the benefit/risk ratio.
Papain is a thiol proteolytic enzyme widely used in dermatology that found applications in wound treatment. Recently, papain was also used as absorption enhancer which can modify the peptide/ protein material in the bilayer domain. We investigated papain safety using human skin that was exposed to papain in vitro at different times: 4, 24 and 48 hours. The samples were examined using Light and Transmission Electron Microscopy (TEM) to study of the mechanisms involved in enhancer-skin interaction. After 24 hours, changes occurred in corneosomes. However, samples of 48 hours did not show major changes in agreement with the control. These findings indicated that papain could be used safely onto the skin.
Microemulsions are transparent, homogeneous and thermodynamically stable systems, formed spontaneously under a specific set of experimental conditions from mixtures of water and oil phases stabilized by a surfactant or a mixture of surfactant and cosurfactant. These systems exhibit some unique properties that make them particularly interesting as delivery systems, as much for the oral as for the topical route. In the present work, we have studied the domain of existence of non-ionic microemulsion systems within pseudo-ternary phase diagrams. The results show a large area of microemulsion domain for O/W and W/O microemulsions. Depending on the proportion of components the apparent viscosity of the systems varied significantly. We have found that the presence of ethanol as cosurfactant affects the physical properties particularly the apparent viscosity and relative density. Analysis of the data indicated that the studied systems behave as non-Newtonian pseudoplastic shear-thinning fluids appropriated for pharmaceutical and cosmetic applications.
Synadenium umbellatum Pax. (Euphorbiacea) is a native plant from tropical Africa known as "cola-nota", "avelos", "cancerola", "milagrosa", among others. The plant is used by Brazilian folks for having anti-inflammatory and analgesic properties, among others. It was evaluated the depressor effects over the central nervous system (CNS) of the ethanolic extract of the leaves of Synadenium umbellatum (EES) and its fractions - hexane (HF), chloroformic (CF) and methanol/water fractions (MF). Several tests were used in Swiss mice (Mus musculus), among them, barbiturate-induced sleep, open field and rota-rod test. The EES was tested at 25, 50 and 100 mg/kg doses, while the HF was tested at 10mg/kg dose, the CF at 20 mg/kg dose and the MF at 25 mg/kg dose. The EES and the HF and the CF fractions, but not the MF, have presented a possible depressor effect over the CNS once they were able to increase the stop time and decrease the number of fecal boli on the openfield, besides they were able to potencialize the barbiturate-induced sleep. The rota-rod test showed that the EES and the fractions were not able to cause motor incoordination or muscle relax. Therefore, we conclude that Synadenium umbellatum Pax. have a possible depressor effect over the CNS.
Schistosomiasis, an important disease in Brazil, is caused by a trematode of the genus Schistosoma, reaching millions of person in one of the most endemic region of this disease in the whole globe. The main goal of this work was to syntetize the 6-formyl-oxamniquine derivative and evaluate its biological activity. The 6-formyl-oxamniquine derivative was obtained by the oxidation of oxamniquine with MnO2, applying CH2Cl2 as solvent at room temperature for 24 hours. The obtaintion of 6-formyl-oxamniquine derivative compound was confirmed by IR spectroscopy and 13C NMR and 1H NMR, presenting similar activity when compared to the commercial oxamniquine (Mansil®).
In conjunction with the spread of HIV infection, tuberculosis (TB) has been among the worldwide health threats. Mycobacteria resistance to the drugs currently used in the therapeutics is the main cause of TB resurgence. In view of this severe situation, the new and selective anti-TB design is of utmost importance. Fatty acid biosynthesis is a prokariontes and eucariontes biochemical process that supplies essential precursors for the assembly of important cellular components, such As phospholipids, lipoproteins, lipopolysaccharides, mycolic acids and cellular envelope. However; the biochemical and functional differences between the bacterial and mammals fatty, acid synthetic path way have endowed the mycobacterial enzymes with distinct properties. These provide valuable opportunities structure- or catalytic mechanism-based design of selective inhibitors as novel anti-TB drugs with improved properties. The enoyl-reductases are essential enzymes in the fatty acids elongation pathway towards the mycolic acids, the main micobacteria cell wall constituents, biosynthyesis and so they are potential targets to the rational new antimycobacteria drug design. This paper highlights recent approaches regarding the design of new anti-TB agents, particularly the enoyl-ACP reductase inhibitors.
Dapsone (DDS) (4,4' diaminodiphenylsulfone), the drug of choice for the treatment of leprosy, frequently induces hemolytic anemia and methemoglobinemia. N-hydroxylation, one of the major pathways of biotransformation, has been constantly related to the methemeglobinemia after the use of the drug. In order to prevent the dapsone-induced hemotoxicity, N-acetylcysteine, a drug precursor of glutathione, was administered in combination with DDS to male Wistar rats, weighting 220-240 g. The animals were then anaesthetized and blood was collected from the aorta for determination of plasma DDS concentration by HPLC, determination of methemoglobinemia and glutathione by spectrophotometry, and for biochemical and hematological parameters. Our results showed that N-acetylcysteine enhanced dapsone-induced methemoglobinemia due to increased dapasone plasmatic concentration and consequent increased N-hydroxylamine formation. We concluded that drug interactions with dapsone require individually studies in order to avoid undesirable effects of dapsone.
Nystatin is a polyenic antibiotic with fungistatic and fungicide characteristics that acts by de-structuring the cellular membrane of fungi and yeast. The nystatin vaginal cream is used for the treatment of vaginal candidiasis. Until recently, the official compendia professed the microbiological trial for dosing this antibiotic, method considered as non-feasible in the routine of quality control centers due to the excessive time for release of results. Aiming at obtaining an alternative method for dosing nystatin vaginal cream, a chromatographic method (HPLC) Was developed and validated. The method developed used a reversible phase column of C188, 3.9 x 150 mm, 4 mm, at 30 degrees C. The mobile phase was made lip of a 0.25 mM sodium phosphate buffer and 0.025 mMEDTA, pH 6.00, methanol and acetonitrile (40:30:30), rate of 1.0 mL/minute and wavelength of 305 nm. The validated method showed to be accurate, precise, robust, linear and specific, in addition to being fast and practical, able to be used for analytic dosing of nystatin vaginal cream.
The secondary lichen metabolite usnic acid [2,6-diacetyl-7,9-dihydroxy-8,9b-dimethyl-1,3(2H,9bH)-dibenzofuran] has demonstrated pharmacological potential activities such as antitumor, antimicrobial, antiviral, antiproliferative, and anti-inflammatory. Liposomes are vesicles composed of phospholipid bilayers surrounding aqueous compartments and they have been used a colloidal drug carriers. The aim of this study was to develop and validate a quantitative UV spectrophotometric method for determination of usnic acid in liposomal formulations. The validation parameters were assessed according to The International Conference on Harmonization (ICH) and American Pharmacopeia guidelines. The linearity range was of 3-15 mu g. mL(-1), regression equation: absorbance = 0.070 x UA concentration (mu g.mL(-1)) + 0.013, and r = 0.9997. The repeatability (relative standard deviation) of the method was 1.96% and intermediate precision indicated that the difference among mean was statistically insignificant (P < 0.05). The accuracy revealed a mean percentage recovery of 100.4% of usnic acid. The method was robust for the variation of temperature and solvent . The detection and quantization limits were found to be 0.34 and 1.13 mu g.mL(-1) respectively. The content of usnic acid in liposomes was of 96.8% (+/- 0.2). The proposed method is accurate, precise and reproducible for estimation of usnic acid as raw material and in pharmaceutical dosage forms such as liposomes.
Tobacco smoking is the major individual benzene source for no occupationally exposed subjects. This solvent is a volatile carcinogen and can induce serious health problems. Several biomarkers for benzene have been proposed, the most used is its metabolite trans, trans-muconic acid (ttMA) in urine, a suitable indicator since it reflects the internal close of low benzene exposure. The present study aimed to evaluate the influence of smoking on urinary ttMA excretion. The analysis was performed by High Pressure Liquid Chromatography in a reversed-phase column and UV detection after extraction of ttAM from urine using SAX cartridges. The method was validated, showing linearity between 0.006 to 10 mu g mL(-1) (r = 0.996), detection and quantification limits of 1.41 x 10(-3) mu g mL(-1) and 6.0 x 10(-3) mu g mL(-1) respectively, CVs from 1.79 to 2.91% (intra assay precision) and 3.53 to 18.37% (interassay precision). A significant positive correlation was observed between ttMA excretion and smoking (p = 0.005388). However, the cigarette number smoked by day seems have no influence on the urinary ttMA excretion.
The present study investigated the effect of crude extracts from yacon leaves, obtained by aqueous cold (YC) or hot (YH) extraction, or hydroethanolic extraction (YE), on glycemia of the diabetic (induced by streptozotocine, 50 mg/kg, ip) and nondiabetic rats. The animals were treated orally with the extracts (400 mg/kg) or water for 3, 7, 10, and 14 days. After this period, the animals were anesthetized and blood samples were collected for measurement of plasmatic glucose and creatinine and activity of the enzymes (AST, ALT, ALP). Also were evaluated the consumption of food, water, urine volume, body weight of the animals and LD50 of YE. Treatment with YE for 14 days reduced glycemia in diabetic and nondiabetic animals. No similar reduction was observed in animals treated with YC or YH. Additionally, YE restored the activity of the plasmatic enzymes that were altered, and improved weight gain in the diabetic animals. These results showed that the effectiveness of the yacon extracts is related to the method of preparation and to the time of treatment. The effect of YE on glycemia in diabetic rats is not related to reduction of food intake or to interference of the extract with intestinal absorption of carbohydrates. *Correspondence:
To study the possible effects of carbamazepine in rats during pregnancy and fetuses' physical development, carbamazepine solubilized in propilenglycol was orally administered (20 and 40 mg/kg) to the female rats from the 2nd to the 19th days of pregnancy. Propilenglycol was administered to the control group. The animals were sacrificed on the 20th day, when 50% of the offspring were fixed in Bouin's solution and the remaining 50% were submitted to diaphanization. The carbamazepine administration caused reduction on weight gain of pregnant rats and did not damage the females' reproductive performance. In the fetuses' physical development, it was observed a flattening on the skull soft tissues and bones; delay in the skull bone development; cartilage calcification increase between hip and femur and reduction in the number of the sternum ossifications. Although carbamazepine has not caused general changes over female rats' reproductive performance, it produced significant alterations in the development of the fetuses' skeletal parameters.
