ABSTRACT
BACKGROUND: Two classes of medications are used to treat Alzheimer's disease (AD); donepezil, galantamine, and rivastigmine are acetylcholinesterase inhibitors, and memantine is a non-competitive antagonist of the N-methyl-D-aspartate receptor. Although these are typically taken orally, there are transdermal therapeutic systems (TTSs) commercially available for rivastigmine and donepezil. The transdermal route has been preferable for guardians/caregivers due to ease of use, reduced side effects, and improved adherence to therapy. OBJECTIVE: The study aimed to obtain knowledge of the properties of these drugs and to search for patents relating to the TTS for AD using the Espacenet platform. METHODS: The search terms were "rivastigmine AND transdermal AND skin delivery AND Alzheimer's", changing the drugs "memantine", "donepezil", and "galantamine", between January 2015 and January 2022. Title and abstract were used to choose patents. RESULTS: TTSs present some limit factors in terms of absorption due to skin physiology and the size of the molecules with established limits of percutaneous penetration (molecular mass of 500 g/mol and log P of 5). We found 1, 4, 4, and 2 patents for galantamine, rivastigmine, donepezil, and memantine, respectively. Galantamine TTS seems to be more challenging due to the molecular mass of 287.35 g/mol and logP of 1.8. The permeator of absorption is necessary. Memantine, rivastigmine, and donepezil present logP of 3.28, 2.3, and 4.27 and molecular weights of 179.30, 250.34, and 415.96 g/mol, respectively. CONCLUSION: TTSs are primarily effective for delivering small molecules. The use of absorption enhancers and irritation mitigators can be necessary to enhance the performance. The development of these technologies is essential for the convenience of patients and caregivers.
ABSTRACT
Introdução: Interações entre fármacos e nutrientes são frequentes em ambiente hospitalar, sobretudo nas áreas em que há maior número de medicamentos prescritos, como em unidades de terapia intensiva (UTI). Método: O presente estudo exploratório e descritivo foi realizado por meio da análise da prescrição de pacientes em uso de nutrição enteral via sonda internados na UTI de um hospital referência. A presença de possíveis interações fármaco-nutrientes foi verificada no website Drug Reax® e no guia de administração de medicamentos desenvolvido pelo Hospital Clínico San Carlos. Os dados foram analisados a fim de determinar a frequência das variáveis estratificadas, e uma avaliação cruzada com o uso do teste do Qui-Quadrado foi utilizada para determinar a significância entre os valores (p=0,05). Resultados: Foram verificadas as prescrições de 72 pacientes. Destes, 65,3% eram do gênero masculino, com média de 55,2±17,8 anos. A média de medicamentos prescritos foi de 11 (9-13). Dentre os 72 indivíduos, em 26 (36,1%) foram observadas interações fármaco-nutrientes moderadas, sendo que em um paciente foram observadas duas interações. Conclusões: A necessidade da padronização na administração de medicamentos simultaneamente a nutrição enteral é uma etapa importante na prevenção de interações fármaco-nutriente. Porém, ainda faltam estudos com desfechos clínicos definidos que comparem diferentes abordagens de manejo para diminuição dessas interações.(AU)
Introduction: Interactions between drugs and nutrients are frequent in the hospital environment, especially in areas where there are more prescribed drugs, such as in intensive care units (ICUs). Objective: To verify the occurrence of drug-nutrient interactions and the presence of incompatibilities in the administration of drugs by catheter in an ICU. Methods: The present exploratory and descriptive study was performed through the analysis of the prescription of patients admitted to the ICU of a reference hospital. The presence of drug-nutrient interactions was verified on the Drug Reax® website and the incompatibilities in drug administration via the probe in the Medication Administration Guide developed by Hospital San Carlos Clinic. Data were analyzed to determine the frequency of the stratified variables, and a cross-chi-square test was used to determine the significance between the values (p=0.05). Results: The prescriptions of 72 patients were verified. Of these, 65.3% were males, with a mean of 55.2±17.8 years. The mean number of drugs prescribed was 11 (9-13). Among the 72 subjects, moderate drug-nutrient interactions were observed in 26 (36.1%) patients, and in one patient two interactions were observed, and the incompatibilities were identified. Conclusion: The need for standardization in drug administration simultaneously to enteral nutrition is an important step in the prevention of drug-nutrient interactions. However, there aren´t studies with defined clinical outcomes that compare different management approaches to decrease these interactions.(AU)
