13 research outputs found
Impact of opioid-free analgesia on pain severity and patient satisfaction after discharge from surgery: multispecialty, prospective cohort study in 25 countries
Background: Balancing opioid stewardship and the need for adequate analgesia following discharge after surgery is challenging. This study aimed to compare the outcomes for patients discharged with opioid versus opioid-free analgesia after common surgical procedures.Methods: This international, multicentre, prospective cohort study collected data from patients undergoing common acute and elective general surgical, urological, gynaecological, and orthopaedic procedures. The primary outcomes were patient-reported time in severe pain measured on a numerical analogue scale from 0 to 100% and patient-reported satisfaction with pain relief during the first week following discharge. Data were collected by in-hospital chart review and patient telephone interview 1 week after discharge.Results: The study recruited 4273 patients from 144 centres in 25 countries; 1311 patients (30.7%) were prescribed opioid analgesia at discharge. Patients reported being in severe pain for 10 (i.q.r. 1-30)% of the first week after discharge and rated satisfaction with analgesia as 90 (i.q.r. 80-100) of 100. After adjustment for confounders, opioid analgesia on discharge was independently associated with increased pain severity (risk ratio 1.52, 95% c.i. 1.31 to 1.76; P < 0.001) and re-presentation to healthcare providers owing to side-effects of medication (OR 2.38, 95% c.i. 1.36 to 4.17; P = 0.004), but not with satisfaction with analgesia (beta coefficient 0.92, 95% c.i. -1.52 to 3.36; P = 0.468) compared with opioid-free analgesia. Although opioid prescribing varied greatly between high-income and low- and middle-income countries, patient-reported outcomes did not.Conclusion: Opioid analgesia prescription on surgical discharge is associated with a higher risk of re-presentation owing to side-effects of medication and increased patient-reported pain, but not with changes in patient-reported satisfaction. Opioid-free discharge analgesia should be adopted routinely
Inhibition of myeloperoxidase activity by the alkaloids of Peganum harmala L. (Zygophyllaceae).
Seeds and aerial parts of Peganum harmala L. (Peganum harmala) are widely used in Algeria as anti-inflammatory remedies. Evaluation of Peganum harmala total alkaloids extracts and pure β-carboline compounds as an anti-inflammatory treatment by the inhibition of an enzyme key of inflammatory, myeloperoxidase (MPO) and HPLC quantification of the alkaloids from the different parts of plant.JOURNAL ARTICLESCOPUS: ar.jinfo:eu-repo/semantics/publishe
Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors.
Due to its production of potent antimicrobial oxidants including hypochlorous acid, human myeloperoxidase (MPO) plays a critical role in innate immunity and inflammatory diseases. Thus MPO is an attractive target in drug design. (Aminoalkyl)fluoroindole derivatives were detected to be very potent MPO inhibitors; however, they also promote inhibition of the serotonin reuptake transporter (SERT) at the same concentration range. Via structure-based drug design, a new series of MPO inhibitors derived from 3-alkylindole were synthesized and their effects were assessed on MPO-mediated taurine chlorination and low-density lipoprotein oxidation as well as on inhibition of SERT. The fluoroindole compound with three carbons in the side chain and one amide group exhibited a selectivity index of 35 (Ki/IC50) with high inhibition of MPO activity (IC50 = 18 nM), whereas its effect on SERT was in the micromolar range. Structure-function relationships, mechanism of action, and safety of the molecule are discussed.Journal ArticleSCOPUS: ar.jinfo:eu-repo/semantics/publishe
Design, Synthesis, and Structure–Activity Relationship Studies of Novel 3‑Alkylindole Derivatives as Selective and Highly Potent Myeloperoxidase Inhibitors
Due to its production of potent antimicrobial
oxidants including
hypochlorous acid, human myeloperoxidase (MPO) plays a critical role
in innate immunity and inflammatory diseases. Thus MPO is an attractive
target in drug design. (Aminoalkyl)fluoroindole derivatives were detected
to be very potent MPO inhibitors; however, they also promote inhibition
of the serotonin reuptake transporter (SERT) at the same concentration
range. Via structure-based drug design, a new series of MPO inhibitors
derived from 3-alkylindole were synthesized and their effects were
assessed on MPO-mediated taurine chlorination and low-density lipoprotein
oxidation as well as on inhibition of SERT. The fluoroindole compound
with three carbons in the side chain and one amide group exhibited
a selectivity index of 35 (<i>K</i><sub>i</sub>/IC<sub>50</sub>) with high inhibition of MPO activity (IC<sub>50</sub> = 18 nM),
whereas its effect on SERT was in the micromolar range. Structure–function
relationships, mechanism of action, and safety of the molecule are
discussed