{"title":"The relationship between serum and sputum levels of azithromycin and clinical endpoints in patients with bronchiectasis using azithromycin maintenance treatment","authors":"J. Altenburg, E. Wilms, W. Boersma","doi":"10.29328/JOURNAL.APPS.1001014","DOIUrl":"https://doi.org/10.29328/JOURNAL.APPS.1001014","url":null,"abstract":"Background: Azithromycin (AZM) is a macrolide antibiotic with distinct pharmacokinetic properties and is increasingly used as maintenance treatment in patients with bronchiectasis in order to reduce infectious exacerbations and improve pulmonary symptoms. The exact mechanism of action is not known and the relation between azithromycin dose level, local and systemic drug levels and clinical effect however, has not been extensively studied yet. Objectives: To explore the relation between AZM serum and sputum concentrations, clinical effect parameters and side effects. Methods: Azithromycin concentrations were measured in serum and sputum samples of bronchiectasis patients receiving one year of AZM treatment (250mg OD) enrolled in the Bronchiectasis and Azithromycin Treatment (BAT) trial, a double blind, randomised placebo-controlled trial. Results were correlated with data on AZM dose level, exacerbation frequency, lung function (forced expiratory volume in 1 second (FEV1) and forced vital capacity (FVC), quality of life and symptoms collected within the same year. Results: 83 sputum samples from 31 patients and 151 serum samples from 43 patients were available for analysis. Mean AZM dose-level ranged from 18.8 to 39.8 mg/kg body weight/ week, generating mean AZM concentrations of 7.57 mg/L (SD 9.49) in sputum and 0.11 mg/L (SD 0.085) in serum. No correlation was found between side effects and AZM dose level, sputumor serum concentrations. Signifi cant correlation was found between AZM sputum concentration and CRP-level (r= -0.6). Conclusion: High and stable AZM sputum levels were reached during long term treatment, as opposed to low AZM levels in serum. Apart from CRP-levels to AZM sputum concentration, no other outcome parameter showed signifi cant correlation to AZM serumor sputum levels. AZM doseor exposure levels were not predictive for the occurrence of side effects. The relationship between serum and sputum levels of azithromycin and clinical endpoints in patients with bronchiectasis using azithromycin maintenance treatment Published: July 16, 2019 020 chronic respiratory infections, such as non-CF bronchiectasis (hereafter referred to as ‘bronchiectasis’) and COPD after favourable results of clinical trials [3-6]. Bronchiectasis –abnormal dilated bronchi, resulting from a vicious circle of mucus retention, bacterial colonization and in lammationis a chronic lung disease, characterized by a variable course. Stable periods with a mild productive cough are interspersed with infectious exacerbations which importantly contribute to reduced quality of life. Since 2012 three randomised clinical trials have con irmed the ef icacy of long term macrolide treatment in bronchiectasis.7-9 Patients treated with azithromycin (250 OD or 500 mg three times weekly) or erythromycin (400 mg BD) showed a marked reduction of infectious exacerbations annually. Favourable effects were also noted with respect to lung function and quality of life but these were not ","PeriodicalId":8316,"journal":{"name":"Archives of Pharmacy and Pharmaceutical Sciences","volume":"106 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87913960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Pharmacodynamics of cannabinoids","authors":"A. Šulcová","doi":"10.29328/JOURNAL.APPS.1001013","DOIUrl":"https://doi.org/10.29328/JOURNAL.APPS.1001013","url":null,"abstract":"How to cite this article: Sulcova A. Pharmacodynamics of cannabinoids. Arch Pharm Pharma Sci. 2019; 3: 011-018. https://doi.org/10.29328/journal.apps.1001013 “Pharmacodynamics of cannabinoids “(i.e. a set of biological effects elicited in the living organism by interaction with its biochemical and biophysical functions up to the cellular level) is studied for a long time during both, physiological and pathological conditions. Cannabinoids received their names according to their natural occurrence as constituents of Cannabis sativa L. (marijuana). The species was classi ied in the “Linnaeus’s Species Plantarum (1753)”, the word “sativa” means things that are cultivated [1]. For ages, people have used cannabis-based preparations for healing and pain suppression until the discovery (in 1897) of aspirin (acetylsalicylic acid) which contemporary medicine uses until today. Chemical investigation of marijuana con irmed various cannabinoid-type components called cannabinoids (presently estimated at about 150). Regarding their possible pharmacodynamic effects, tetrahydrocannabinol (THC) and cannabidiol (CBD) are the most explored. The determination of THC structure by means of nuclear magnetic resonance imaging increased sharply the number of professional scienti ic reports dealing with the studies of THC pharmacodynamic mechanisms of action [2]. Thus, it has been possible to verify THC speci ic binding sites in the vertebrate organisms including humans named “cannabinoid receptors” [3]. Subsequently, discoveries of endogenous cannabinoid receptor ligands were of high signi icance. The irst such N-arachidonoyl-ethanol amide was isolated from the brain of a pig and called anandamide [4]. Subsequently, other endocannabinoids with various stimulatory, i.e. “agonistic” receptor activity were discovered: 2AG (arachidonoyl glycerin ether) [5], NADA (N-arachidonoyl dopamine) [6]. The last endocannabinoid identi ied virodhamine (O-arachidonoyl-ethanolamine), shows on the contrary, an “antagonistic” effect on the irst discovered cannabinoid receptors, now called CB1 receptors [7]. The cannabinoid CB1 receptor was originally discovered in the central nervous system (in the cortex, basal ganglia, hippocampus, hypothalamus, cerebellum, spinal cord, spinal cord ganglia), then also in the enteric nervous system and on cells of fat, endothelial cells, liver, gastrointestinal tract.","PeriodicalId":8316,"journal":{"name":"Archives of Pharmacy and Pharmaceutical Sciences","volume":"117 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89856985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Stepwise regression modeling on the monitoring of separation of Salvianolate through macroporous resin chromatographic column using UV spectral data","authors":"Yongsuo Liu, Yong Wang, G. Luo","doi":"10.29328/journal.apps.1001012","DOIUrl":"https://doi.org/10.29328/journal.apps.1001012","url":null,"abstract":"","PeriodicalId":8316,"journal":{"name":"Archives of Pharmacy and Pharmaceutical Sciences","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90909214","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Application of the Pyphagor’s Theorem for Correction of Ki and Ka constants of enzyme inhibition and activation","authors":"Vi Krupyanko, PV Krupyanko","doi":"10.29328/journal.apps.1001011","DOIUrl":"https://doi.org/10.29328/journal.apps.1001011","url":null,"abstract":"","PeriodicalId":8316,"journal":{"name":"Archives of Pharmacy and Pharmaceutical Sciences","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78240684","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}