Search results for "Pyrrolidines"
showing 10 items of 66 documents
Efficacy of trifluridine and tipiracil (TAS-102) versus placebo, with supportive care, in a randomized, controlled trial of patients with metastatic …
2016
[Purpose] TAS-102 is a combination of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil. Efficacy and safety of TAS-102 in patients with metastatic colorectal cancer (mCRC) refractory or intolerant to standard therapies were evaluated in the phase 3 RECOURSE trial. Results of RECOURSE demonstrated significant improvement in overall survival (OS) and progression-free survival (PFS) with TAS-102 versus placebo [hazard ratio (HR) = 0.68 and 0.48 for OS and PFS, respectively; both P < 0.001]. The current analysis evaluates efficacy and safety of TAS-102 in the RECOURSE Spanish subgroup.
Effectiveness and safety of glecaprevir/pibrentasvir in chronic hepatitis C patients: Results of the Italian cohort of a post-marketing observational…
2021
Abstract Background and Aims The MARS post-marketing, observational study evaluates glecaprevir/pibrentasvir in a large population of Italian patients who are infected with HCV. Patients and Methods Achievement of SVR12 was the primary endpoint in the overall population and by subpopulations of interest (treatment-naive and treatment-experienced patients, subjects infected with different HCV genotype/sub-genotype, cirrhotic and non-cirrhotic patients, patients with different severity of fibrosis, patients with an APRI score ≥1, subjects with comorbidities, HIV-coinfected patients, elderly patients and people who use drugs). Safety and quality of life (assessed by SF-36 and Work Productivity…
A model-based meta-analysis of sofosbuvir-based treatments in chronic hepatitis C patients.
2016
The objective of this study was to compare the efficacy of sofosbuvir-based treatments in patients with chronic hepatitis C virus (HCV) infection using a model-based meta-analysis (MBMA). A bibliographic search was performed to identify clinical trials involving sofosbuvir as a unique direct-acting antiviral (DAA) agent or together with daclatasvir, ledipasvir or simeprevir for the treatment of diagnosed HCV infection. The time course of the virological response (VR) was modelled to estimate the effect of treatment and the influence of population characteristics on the longitudinal efficacy profile. The model was validated and simulations of 10 different treatment schedules were performed. …
High Cure Rate With 24 Weeks of Daclatasvir-Based Quadruple Therapy in Treatment-Experienced, Null-Responder Patients With HIV/Hepatitis C Virus Geno…
2015
BACKGROUND Few direct anti-hepatitis C virus (HCV) agents have been studied in difficult-to-treat null responder and cirrhotic human immunodeficiency virus (HIV)-coinfected patients. Daclatasvir and asunaprevir combined with pegylated interferon/ribavirin (peg-IFN/RBV) have shown promising results in HCV-monoinfected patients. METHODS An open-label, single-arm, phase 2 study was conducted in HIV/HCV genotype 1/4-coinfected patients who were null responders to prior peg-IFN/RBV standard therapy and on a raltegravir-based regimen with HIV RNA <400 copies/mL. They received a 4-week lead-in phase with peg-IFN/RBV, followed by 24 weeks of asunaprevir (100 mg twice daily), daclatasvir (60 mg once…
In vivo imaging of dopamine receptors in a model of temporal lobe epilepsy
2010
Alterations in dopamine neurotransmission in animal models of epilepsies have been frequently demonstrated using invasive neuroscience or ex vivo techniques. We aimed to test whether corresponding alterations could be detected by noninvasive in vivo brain imaging with positron emission tomography (PET) in the chronic phase of the rat pilocarpine model of temporal lobe epilepsy.Six pilocarpine-treated Wistar rats exhibiting spontaneous recurrent seizures and nine control rats were studied with PET using [(18)F]-fallypride, a high-affinity dopamine D(2/3) receptor ligand. Parametric images of [(18)F]-fallypride specific binding were calculated using a reference tissue method, and the two grou…
Effects of prostaglandin E1 and buflomedil on left ventricular function in patients with severe chronic occlusive arterial disease: a prospective, ra…
1999
In this study, the effect of a course of prostaglandin E ( 1 ) (60 microg/d intravenously [i.v.]) or buflomedil (150 mg/d i.v.) treatment on parameters of left ventricular systolic function was investigated by echocardiography in patients of comparatively advanced age with severe peripheral occlusive arterial disease (Fontaine's stage III or IV). The study population was 20 patients, 12 men and 8 women, between 51 and 85 years of age (average age, 73. 7 years), with multiple coexisting medical conditions. These patients were no longer suitable candidates for other forms of interventional or surgical treatment. The patients were treated with prostaglandin E ( 1 ) or buflomedil in the dosages…
The pathogenetic role of adulterants in 5 cases of drug addicts with a fatal outcome
2013
The purpose of the present study is to determine the role of lidocaine, caffeine and dextromethorphan, used as adulterant substances, in five cases of drug overdose which have come to our attention. Taking into account the pharmacological mechanism, blood concentration and route of administration (intravenous) we evaluated the hypothesis that these substances could act with a synergistic effect - or at least additive - with the illicit drugs on the central nervous system and cardiovascular system.
Effects of Vildagliptin/Metformin Therapy on Patient-Reported Outcomes: Work Productivity, Patient Satisfaction, and Resource Utilization
2013
Introduction: Type 2 diabetes mellitus (T2DM) is associated not only with high direct healthcare costs, but also with indirect costs, as diabetic complications and the disease itself result in loss of productivity. Vildagliptin is a novel dipeptidyl peptidase-4 inhibitor that is given either alone or in combination with oral hypoglycemic drugs, including metformin. The study was designed to assess the hypothesis that fixed-combination vildagliptin/metformin improves work productivity measured as Work Productivity and Activity Impairment (WPAI) scores. Secondary objectives were the assessment of patient satisfaction by means of the Diabetes Treatment Satisfaction Questionnaire (DTSQs), the c…
Some pharmacological properties of the false cholinergic transmitter acetylpyrrolidinecholine and its precursor pyrrolidinecholine
1976
The acetylchline analogue acetylpyrrolidinecholine as well as the choline analogue pyrrolidinecholine were synthesized and the cholinergic properties of both substances were investigated on the guinea-pig ileum, rat blood pressure and frog rectus abdominis muscle. Acetylpyrrolidinecholine was 3-5 times less potent than acetylcholine on the three preparations tested. The dose-response curves to acetylpyrrolidinecholine were shifted to the right in a parallel manner by atropine and (+)-tubocurarine. The dissociation constants for atropine and (+)-tubocurarine obtained with acetylpyrrolidinecholine as agonist were not different from those obtained with acetylcholine. This indicates that acetyl…
Does concomitant diabetes affect treatment responses in overactive bladder patients?
2013
Summary Aims To compare the efficacy and tolerability of a muscarinic receptor antagonist, darifenacin, in the treatment of overactive bladder (OAB) patients with concomitant diabetes as compared with those without comorbidities. Methods Post hoc exploratory analysis of a published, large, non-interventional study in OAB patients treated with darifenacin including 532 diabetics and 1315 controls. Associations of diabetes with treatment responses were evaluated by multiple regression models. Results Diabetics (largely type 2 patients) and controls differed in baseline age, body weight, duration of OAB symptoms and presence of comedications. However, they exhibited similar OAB symptom episode…