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Drug Family (drug + family)
Selected AbstractsThe prefrontal cortex: a target for antipsychotic drugsACTA PSYCHIATRICA SCANDINAVICA, Issue 1 2010F. ArtigasArticle first published online: 14 DEC 200 Objective:, At therapeutic doses, classical antipsychotic drugs occupy a large proportion of subcortical dopamine D2 receptors, whereas atypical antipsychotics preferentially occupy cortical 5-HT2 receptors. However, the exact cellular and network basis of their therapeutic action is not fully understood. Method:, To review the mechanism of action of antipsychotic drugs with a particular emphasis on their action in the prefrontal cortex (PFC). Results:, The PFC controls a large number of higher brain functions altered in schizophrenia. Histological studies indicate the presence of a large proportion of PFC neurons expressing monoaminergic receptors sensitive to the action of atypical- and to a lesser extentclassical antipsychotic drugs. Functional studies also indicate that both drug families act at PFC level. Conclusion:, Atypical antipsychotic drugs likely exert their therapeutic activity by a preferential action on PFC neurons, thus modulating the PFC output to basal ganglia circuits. Classical antipsychotics also interact with these PFC targets in addition to blocking massively striatal D2 receptors. [source] Prevalence of psychotropic drug use in nursing homes for the aged in Quebec and in the French-speaking area of SwitzerlandINTERNATIONAL JOURNAL OF GERIATRIC PSYCHIATRY, Issue 8 2005Micheline Gobert Abstract Background The use of psychotropic drugs is high in institutionalised elderly, which raises the question of its appropriateness. This study aimed to: (1) estimate the use of psychotropics, for each family, in terms of the prevalence and dosage among the elderly in nursing homes in French-speaking Switzerland and Quebec; and (2) assess, for each family of psychotropic drugs and for each care facility, the prevalence of use and departure from average prescription (ratio of observed-to-expected prevalence). Method An administrative database was used for this cross-sectional analysis. The sample included 8183 Quebec and 7592 Swiss long-term care residents. Three classes of psychotropics (antipsychotics, antidepressants, hypnotics-anxiolytics) were defined as dichotomous variables. Logistic regressions were conducted to identify residents characteristics associated with the use of each psychotropic type and to compute expected prevalence. Results Swiss residents were slightly older and less dependent than Quebec residents. Use of psychotropic drugs was higher in Swiss than in Quebec residents, on the whole as well as for each family of drug. A total of 78.1% of Swiss residents used at least one drug as compared to 66.9% in Quebec. Ninety percent of residents were given less than 7 defined daily doses per week, irrespective of the drug family. According to Beer's criteria, only 4.9% of prescriptions were inadequate. In Quebec and in Switzerland, the prevalence of antidepressant use was associated with the prevalence of hypnotic-anxiolytic use. No ratios of observed-to-expected reached statistical significance. Interpretation There was a considerable use of psychotropics in Quebec and Switzerland with, seemingly, no dramatic departure from the average practice. Our data cannot tell if there is a global overuse of psychotropics, but indicated that dosage and medication selection seem adequate. Physicians should critically reassess the necessity of prescribed medications for their patients. Copyright © 2005 John Wiley & Sons, Ltd. [source] Fluoxetine and citalopram exhibit potent antiinflammatory activity in human and murine models of rheumatoid arthritis and inhibit toll-like receptorsARTHRITIS & RHEUMATISM, Issue 3 2010Sandra Sacre Objective Selective serotonin reuptake inhibitors (SSRIs), in addition to their antidepressant effects, have been reported to have antiinflammatory effects. The aim of this study was to assess the antiarthritic potential of 2 SSRIs, fluoxetine and citalopram, in murine collagen-induced arthritis (CIA) and in a human ex vivo disease model of rheumatoid arthritis (RA). Methods Following therapeutic administration of SSRIs, paw swelling was assessed and clinical scores were determined daily in DBA/1 mice with CIA. Joint architecture was examined histologically at the end of the treatment period. Cultures of human RA synovial membranes were treated with SSRIs, and cytokine production was measured. Toll-like receptor (TLR) function was examined in murine and human macrophages, human B cells, and human fibroblast-like synovial cells treated with SSRIs. Results Both SSRIs significantly inhibited disease progression in mice with CIA, with fluoxetine showing the greatest degree of efficacy at the clinical and histologic levels. In addition, both drugs significantly inhibited the spontaneous production of tumor necrosis factor, interleukin-6, and interferon-,,inducible protein 10 in human RA synovial membrane cultures. Fluoxetine and citalopram treatment also inhibited the signaling of TLRs 3, 7, 8, and 9, providing a potential mechanism for their antiinflammatory action. Conclusion Fluoxetine and citalopram treatment selectively inhibit endosomal TLR signaling, ameliorate disease in CIA, and suppress inflammatory cytokine production in human RA tissue. These data highlight the antiarthritic potential of the SSRI drug family and provide further evidence of the involvement of TLRs in the pathogenesis of RA. The SSRIs may provide a template for potential antiarthritic drug development. [source] Understanding the Plasticity of the ,/, Hydrolase Fold: Lid Swapping on the Candida antarctica Lipase B Results in Chimeras with Interesting Biocatalytic PropertiesCHEMBIOCHEM, Issue 3 2009Michael Skjøt Dr. Abstract The best of both worlds. Long molecular dynamics (MD) simulations of Candida antarctica lipase B (CALB) confirmed the function of helix ,5 as a lid structure. Replacement of the helix with corresponding lid regions from CALB homologues from Neurospora crassa and Gibberella zeae resulted in new CALB chimeras with novel biocatalytic properties. The figure shows a snapshot from the MD simulation. The Candida antarctica lipase B (CALB) has found very extensive use in biocatalysis reactions. Long molecular dynamics simulations of CALB in explicit aqueous solvent confirmed the high mobility of the regions lining the channel that leads into the active site, in particular, of helices ,5 and ,10. The simulation also confirmed the function of helix ,5 as a lid of the lipase. Replacing it with corresponding lid regions from the CALB homologues from Neurospora crassa and Gibberella zeae resulted in two new CALB mutants. Characterization of these revealed several interesting properties, including increased hydrolytic activity on simple esters, specifically substrates with C, branching on the carboxylic side, and much increased enantioselectivity in hydrolysis of racemic ethyl 2-phenylpropanoate (E>50), which is a common structure of the profen drug family. [source] Oral challenges are needed in the diagnosis of ,-lactam hypersensitivityCLINICAL & EXPERIMENTAL ALLERGY, Issue 1 2008P. J. Bousquet Summary Background ,-lactams continue to remain the most commonly involved drug family in allergic drug reactions. They are often essential and there is a cost-effective and favourable risk-benefit ratio for the exploration of all suspicions of ,-lactam allergy. A firm diagnosis is always based on skin tests and sometimes on provocation tests. Recommendations have been published by allergy societies and distinguished scientists but they are not always concordant and can lead to some confusion for the practicing allergologist. The situation has even worsened since the world wide withdrawal of these penicillin determinants and since the predominance of amoxicillin and cephalosporin prescriptions in most countries. Objective , Method In a recent article, it was stated that patients with a penicillin allergy history and negative skin tests to major and minor penicillin determinants are at a low risk of relapse (0,5%) when receiving a ,-lactam. In this paper, our Drug Allergy and Hypersensitivity Database, a cohort database, was used to demonstrate that this statement is false. Standardized European Network for Drug Allergy questionnaires, skin test and challenge procedures were followed. Results One-thousand two-hundred and eighteen subjects, 69.8% of female, 51.7% of atopics, were included. 21.1% had a true ,-lactam allergy confirmed by skin tests (178, 69.3%) or by drug provocation (79, 30.7%). 17.4% of the patients with negative skin tests to major and minor penicillin determinants were positive for a ,-lactam. Conclusion In the diagnosis of ,-lactams allergy, if all skin tests are negative, skin tests with other determinants and provocation tests under strict surveillance are mandatory. [source] | ||||||||||