keyword
https://read.qxmd.com/read/38639103/effect-of-hepatic-impairment-on-trilaciclib-pharmacokinetics
#21
JOURNAL ARTICLE
Chao Li, Richard A Preston, Emily Dumas, Andrew Beelen, Thomas C Marbury
Trilaciclib is a first-in-class, intravenous cyclin-dependent kinase 4 and 6 inhibitor approved for reducing the incidence of chemotherapy-induced myelosuppression in adult patients with extensive-stage small cell lung cancer receiving a platinum/etoposide-containing or topotecan-containing regimen. No dose adjustment is recommended for participants with mild hepatic impairment (HI) based on previous population pharmacokinetic (PK) analysis. This open-label, parallel-group study examined the impact of moderate and severe HI on the PK of trilaciclib...
April 19, 2024: Journal of Clinical Pharmacology
https://read.qxmd.com/read/38638746/cervical-intramedullary-spinal-cord-abscess-secondary-to-discitis-and-osteomyelitis-in-an-immunocompromised-patient
#22
Ashlie Maldonado-Pérez, Samuel Estronza, Hiram J Maldonado, Emil A Pastrana, Orlando De Jesus
Intramedullary spinal cord abscess is a rare neurological condition, not commonly suspected and often misdiagnosed. Even after a prompt diagnosis and treatment, most patients persist with permanent neurological deficits. In adults, factors such as immunocompromised, intravenous drug use, endocarditis, and sepsis could be associated with its development. In this study, we present the case of a 63-year-old male patient who developed a chronic cervical intramedullary spinal cord abscess after being treated for multiple abscesses in the paravertebral and psoas muscles...
March 2024: Curēus
https://read.qxmd.com/read/38636481/brain-permeable-immunoproteasome-targeting-macrocyclic-peptide-epoxyketones-for-alzheimer-s-disease
#23
JOURNAL ARTICLE
Ji Eun Park, Chhabi L Chaudhary, Deepak Bhattarai, Kyung Bo Kim
Previously, we demonstrated that linear peptide epoxyketones targeting the immunoproteasome (iP) could ameliorate cognitive deficits in mouse models of Alzheimer's disease (AD) independently of amyloid deposition. We also reported the first iP-targeting macrocyclic peptide epoxyketones, which exhibit improved metabolic stability compared with their linear counterparts. Here, we prepared additional macrocyclic peptide epoxyketones and compared them with existing macrocyclic iP inhibitors by assessing Caco2 cell-based permeability and microsomal stability, providing the four best macrocyclic iP inhibitors...
April 18, 2024: Journal of Medicinal Chemistry
https://read.qxmd.com/read/38633322/decreased-incidence-of-kawasaki-disease-in-south-korea-during-the-sars-cov-2-pandemic
#24
JOURNAL ARTICLE
Kyung Jin Oh, Sang-Yun Lee
PURPOSE: Analyzing Kawasaki disease epidemiology during the SARS-CoV-2 pandemic in South Korea using 2012-2020 National Health Insurance Service data. METHODS: The incidence of Kawasaki disease for 2012-2020 was investigated to identify changes in incidence after the start of the pandemic. National Health Insurance Service data from the Republic of Korea were used. Kawasaki disease was defined based on the International Statistical Classification of Diseases and Related Health Problems, the Tenth Revision diagnostic code (M30...
2024: Frontiers in Pediatrics
https://read.qxmd.com/read/38632826/population-pharmacokinetic-modeling-and-exposure-efficacy-and-body-weight-response-analyses-for-tezepelumab-in-patients-with-severe-uncontrolled-asthma
#25
JOURNAL ARTICLE
Yanan Zheng, Lubna Abuqayyas, Angelica Quartino, Ye Guan, Yuying Gao, Lu Liu, Åsa Hellqvist, Gene Colice, Alexander MacDonald
Tezepelumab is a human monoclonal antibody that blocks the activity of thymic stromal lymphopoietin. This analysis assessed the suitability of a fixed-dose regimen of tezepelumab 210 mg every 4 weeks (Q4W) in adults and adolescents with severe, uncontrolled asthma. A population pharmacokinetic model was developed using data from 1368 patients with asthma or healthy participants enrolled in 8 clinical studies (phases 1-3). Tezepelumab exposure-efficacy relationships were analyzed in the phase 3 NAVIGATOR study (NCT03347279), using asthma exacerbation rates over 52 weeks and changes in pre-bronchodilator forced expiratory volume in 1 s at week 52...
April 17, 2024: Journal of Clinical Pharmacology
https://read.qxmd.com/read/38631564/%C3%AE-caryophyllene-inhibits-heroin-self-administration-but-does-not-alter-opioid-induced-antinociception-in-rodents
#26
JOURNAL ARTICLE
Ewa Galaj, Guo-Hua Bi, Zheng-Xiong Xi
A growing body of research indicates that β-caryophyllene (BCP), a constituent present in a large number of plants, possesses significant therapeutic properties against CNS disorders, including alcohol and psychostimulant use disorders. However, it is unknown whether BCP has similar therapeutic potential for opioid use disorders. In this study, we found that systemic administration of BCP dose-dependently reduced heroin self-administration in rats under an FR2 schedule of reinforcement and partially blocked heroin-enhanced brain stimulation reward in DAT-cre mice, maintained by optical stimulation of midbrain dopamine neurons at high frequencies...
April 15, 2024: Neuropharmacology
https://read.qxmd.com/read/38629941/comparison-between-the-protective-effect-of-isoflurane-and-propofol-on-myocardium-during-coronary-artery-bypass-grafting-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#27
REVIEW
Qi Bao, Min Lei, Dongju Xiao, Junran Xie
OBJECTIVE: Intravenous non-volatile anaesthetics like propofol are commonly used in cardiac surgeries across several countries. Volatile anaesthetics like isoflurane may help in protecting the myocardium and minimize ischaemia-reperfusion injury. Hence, we did this review to compare the cardioprotective effect of isoflurane and propofol among patients undergoing coronary artery bypass grafting (CABG). METHODS: We conducted a search in the databases Medical Literature Analysis and Retrieval System Online (or MEDLINE), Embase, PubMed Central®, ScienceDirect, Google Scholar, and Cochrane Library from inception until April 2021...
April 17, 2024: Brazilian Journal of Cardiovascular Surgery
https://read.qxmd.com/read/38629000/neonatal-outcomes-in-labor-after-intravenous-remifentanil-analgesia-vs-epidural-analgesia-a-retrospective-observational-study
#28
JOURNAL ARTICLE
Suzana Sobot Novakovic, Sanja Cuk, Dragan Rakanovic, Dragana Loncar Stojiljkovic, Branka Cancarevic Djajic, Miroslav Gajic
Background Some evidence indicates that maternal analgesia during labor may have adverse effects on neonates due to exposure to specific drugs or the potential effects of analgesia on the course of labor. We assessed the clinical outcome of term neonates born to mothers who received epidural analgesia (E) or systemic analgesia with remifentanil (R) during labor. Methods Data was collected retrospectively over one year. We have evaluated the medical records of 247 full-term neonates; 208 were born to mothers who received E and 39 to mothers who received R...
March 2024: Curēus
https://read.qxmd.com/read/38628619/fabrication-and-in-vitro-vivo-evaluation-of-quercetin-nanocrystals-stabilized-by-glycyrrhizic-acid-for-liver-targeted-drug-delivery
#29
JOURNAL ARTICLE
Baode Shen, Yuwen Zhu, Fengxia Wang, Xiang Deng, Pengfei Yue, Hailong Yuan, Chenying Shen
The purpose of this study was to design novel drug nanocrystals (NCs) stabilized by glycyrrhizic acid (GL) for achieving liver targeted drug delivery due to the presence of GL receptor in the hepatocytes. Quercetin (QT) exhibits good pharmacological activities for the treatment of liver diseases, including liver steatosis, fatty hepatitis, liver fibrosis, and liver cancer. It was selected as a model drug owing to its poor water solubility. QT NCs stabilized by GL (QT-NCs/GL) were fabricated by wet media milling technique and systemically evaluated...
June 2024: International journal of pharmaceutics: X
https://read.qxmd.com/read/38627941/administration-mode-matters-for-5-fluorouracil-therapy-physiologically-based-pharmacokinetic-evidence-for-avoidance-of-myelotoxicity-by-continuous-infusion-but-not-intravenous-bolus
#30
JOURNAL ARTICLE
Chih-Jia Chao, Iain Gardner, Chun-Jung Lin, Kun-Huei Yeh, Wan-Chen Lu, Khaled Abduljalil, Yunn-Fang Ho
AIMS: Pre-emptive prediction to avoid myelosuppression and harmful sequelae is difficult given the complex interplay among patients, drugs and treatment protocols. This study aimed to model plasma and bone marrow concentrations and the likelihood of myelotoxicity following administration of 5-fluorouracil (5-FU) by diverse intravenous (IV) bolus or continuous infusion (cIF) regimens. METHODS: Using physicochemical, in vitro and clinical data obtained from the literature consisting of various regimens and patient cohorts, a 5-FU physiologically based pharmacokinetic (PBPK) model was developed...
April 16, 2024: British Journal of Clinical Pharmacology
https://read.qxmd.com/read/38626389/feasibility-study-of-single-photon-emission-computed-tomography-with-iodine-123-labeled-metaiodobenzylguanidine-for-preclinical-evaluation-of-labetalol-as-a-%C3%AE-adrenergic-receptor-blocker
#31
JOURNAL ARTICLE
Yiseul Choi, Eun Sang Lee, Sang-Keun Woo, Kyo Chul Lee, Hye Kyung Chung, Joo Hyun Kang
Among clinically used radiopharmaceuticals, iodine-123 labeled metaiodobenzylguanidine ([123 I]mIBG) serves for diagnosing neuroendocrine tumors and obtaining images of myocardial sympathetic innervation. mIBG, a structural analogue of norepinephrine (NE), a neurotransmitter acting in peripheral and central nerves, follows a pathway similar to NE, transmitting signals through the NE transporter (NET) located at synaptic terminals. It moves through the body without decomposing, enabling noninvasive image evaluation...
April 16, 2024: Molecular Pharmaceutics
https://read.qxmd.com/read/38625037/transfer-of-ans-like-drugs-from-micellar-drug-delivery-systems-to-albumin-is-highly-favorable-and-protected-from-competition-with-surfactant-by-reserved-binding-sites
#32
JOURNAL ARTICLE
Iulia Carabadjac, Leonie C Vormittag, Thomas Muszer, Jakob Wuth, Maximilian H Ulbrich, Heiko Heerklotz
Micellar drug delivery systems (MDDS) for the intravenous administration of poorly soluble drugs have great advantages over alternative formulations in terms of the safety of their excipients, storage stability, and straightforward production. A classic example is mixed micelles of glycocholate (GC) and lecithin, both endogenous substances in human blood. What limits the use of MDDS is the complexity of the transitions after injection. In particular, as the MDDS disintegrate partially or completely after injection, the drug has to be transferred safely to endogenous carriers in the blood, such as human serum albumin (HSA)...
April 16, 2024: Molecular Pharmaceutics
https://read.qxmd.com/read/38623799/prospective-evaluation-of-the-emetogenic-profile-and-analgesic-efficacy-of-intravenous-ibuprofen-and-metamizole-in-the-immediate-postoperative-period-of-pediatric-acute-appendicitis
#33
JOURNAL ARTICLE
J Arredondo Montero, G Antona, E Murillo Jaso, P Unzué Rico, I Antuñano Unanua, N Martín-Calvo
BACKGROUND: Literature comparing different alternatives for pain control in the immediate postoperative period of pediatric acute appendicitis (PAA) is scarce. MATERIALS AND METHODS: We prospectively compared the analgesic and emetogenic profile of intravenous ibuprofen and metamizole in the immediate postoperative period of PAA. For this purpose, we used a sample of patients operated on in 2021 in our center. Participants were recruited on arrival at the Emergency Department and histopathological confirmation of the diagnosis was obtained in all of them...
April 1, 2024: Cirugía Pediátrica: Organo Oficial de la Sociedad Española de Cirugía Pediátrica
https://read.qxmd.com/read/38623486/fine-tuning-the-activation-behaviors-of-ternary-modular-cabazitaxel-prodrugs-for-efficient-and-on-target-oral-anti-cancer-therapy
#34
JOURNAL ARTICLE
Mingyang Zhang, Yifan Miao, Can Zhao, Tong Liu, Xiyan Wang, Zixuan Wang, Wenxin Zhong, Zhonggui He, Chutong Tian, Jin Sun
The disulfide bond plays a crucial role in the design of anti-tumor prodrugs due to its exceptional tumor-specific redox responsiveness. However, premature breaking of disulfide bonds is triggered by small amounts of reducing substances ( e.g. , ascorbic acid, glutathione, uric acid and tea polyphenols) in the systemic circulation. This may lead to toxicity, particularly in oral prodrugs that require more frequent and high-dose treatments. Fine-tuning the activation kinetics of these prodrugs is a promising prospect for more efficient on-target cancer therapies...
April 2024: Asian journal of pharmaceutical sciences
https://read.qxmd.com/read/38622469/efficacy-of-different-routes-of-acetaminophen-administration-for-postoperative-pain-in-children-a-systematic-review-and-network-meta-analysis
#35
JOURNAL ARTICLE
Danilo Osorio, Diana Maldonado, Koen Rijs, Caroline van der Marel, Markus Klimek, Jose A Calvache
PURPOSE: Acetaminophen is the most common drug used to treat acute pain in the pediatric population, given its wide safety margin, low cost, and multiple routes for administration. We sought to determine the most efficacious route of acetaminophen administration for postoperative acute pain relief in the pediatric surgical population. METHODS: We conducted a systematic review of randomized controlled trials (RCTs) that included children aged between 30 days and 17 yr who underwent any type of surgical procedure and that evaluated the analgesic efficacy of different routes of administration of acetaminophen for the treatment of postoperative pain...
April 15, 2024: Canadian Journal of Anaesthesia
https://read.qxmd.com/read/38618666/oral-iron-supplementation-new-formulations-old-questions
#36
JOURNAL ARTICLE
Kostas Pantopoulos
Iron deficiency anemia and pre-anemic iron deficiency are the most frequent pathologies. The first line of treatment involves oral iron supplementation. The simplest, least expensive, and most frequently prescribed drug is ferrous sulfate, while other ferrous salts and ferric complexes with polysaccharides or succinylated milk proteins are also widely used. In recent years, novel iron formulations have been developed, such as the lipophilic iron donor ferric maltol, or nanoparticle encapsulated sucrosomial® iron...
April 11, 2024: Haematologica
https://read.qxmd.com/read/38618283/dexmedetomidine-prolongs-lidocaine-intravenous-regional-anesthesia-in-rats-by-blocking-the-hyperpolarization-activated-cation-current
#37
JOURNAL ARTICLE
Tongtong Zhang, Xincheng Liao, Yuzhi Chen, Xinru Shu, Deshan Liu, Yusheng Yao
PURPOSE: Intravenous regional anesthesia (IVRA) using lidocaine provides effective localized analgesia but its duration is limited. The mechanism by which dexmedetomidine enhances lidocaine IVRA is unclear but may involve modulation of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. MATERIALS AND METHODS: Lidocaine IVRA with varying dexmedetomidine concentrations was performed in the tails of Sprague-Dawley rats. Tail-flick and tail-clamping tests assessed IVRA analgesia and anesthesia efficacy and duration...
2024: Drug Design, Development and Therapy
https://read.qxmd.com/read/38618137/maximum-tolerated-dose-and-toxicity-evaluation-of-orally-administered-docetaxel-granule-in-mice
#38
JOURNAL ARTICLE
Xiaowei Dong, Jinmin Zhang
Oral delivery of chemotherapy drugs is the most favorable and preferred route of drug administration. However, because of poor solubility and/or permeability, most chemotherapy drugs are given by intravenous administration. Docetaxel (DTX) is a potent chemotherapy drug that inhibits microtubular depolymerization and is widely used to treat numerous cancers. DTX is highly lipophilic and insoluble in water; thus, 50% polysorbate 80, which may cause hypersensitivity reactions and reduce drug uptake by tumor tissue, is used in the commercial DTX injection to dissolve DTX...
June 2024: Toxicology Reports
https://read.qxmd.com/read/38615256/dysgeusia-increases-the-risk-for-death-and-other-side-effects-during-antineoplastic-systemic-treatment-for-solid-tumors-a-cross-sectional-study
#39
JOURNAL ARTICLE
P-G Silva, G-A Barreto, A-C Carlos, M-M Borges, C-E Malta, J-V Barbosa, A-A Crispim, S-F Juaçaba, L-F Gonzaga-Silva
BACKGROUND: Chemotherapy (QT) is a systemic treatment using a combination of antineoplastic drugs, orally or intravenously, that inhibit tumor growth and fast-growing normal cells. Due to its nonspecificity, chemotherapy can cause a series of adverse effects, such as altered taste (dysgeusia), associated with malnutrition and, consequently, other adverse effects in the gastrointestinal tract and increased mortality risk. This study aimed to evaluate the influence of dysgeusia on the incidence of other adverse effects and overall survival during antineoplastic chemotherapy (chemotherapy)...
April 14, 2024: Medicina Oral, Patología Oral y Cirugía Bucal
https://read.qxmd.com/read/38614019/reinforcing-and-adverse-observable-effects-of-nicotine-and-minor-tobacco-alkaloids-in-squirrel-monkeys
#40
JOURNAL ARTICLE
Emily L Burke, Rajeev I Desai
The most prevalent psychoactive chemical in tobacco smoke is nicotine, which has been shown to maintain tobacco consumption as well as cause acute adverse effects at high doses, like nausea and emesis. Recent studies in laboratory animals have suggested that many non-nicotine constituents of tobacco smoke (e.g., minor tobacco alkaloids) may also contribute to tobacco's overall reinforcing and adverse effects. Here, we used intravenous (IV) self-administration (n = 3) and observation (n = 4) procedures in squirrel monkeys to, respectively, compare the reinforcing and adverse observable effects of nicotine and three prominent minor tobacco alkaloids, nornicotine, anatabine, and myosmine...
April 2, 2024: Drug and Alcohol Dependence
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