OFIRMEV: An Old Drug Becomes New Again

Nishimoto, Rodney N.

doi:10.2344/0003-3006-61.3.99

Cited by 14 publications

(9 citation statements)

References 26 publications

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“…Acetaminophen is a synthetic, non-opiate, centrally acting analgesic and antipyretic derived from p-aminophenol [ 74 , 75 ]. Its high therapeutic index and efficacy to safety ratio makes it an attractive and widely used option for PICU mono and multimodal treatment of mild to severe pain as well as fever [ 74 ].…”

Section: Analgesiamentioning

confidence: 99%

Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit

Egbuta

Mason

2021

JCM

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Critically ill pediatric patients often require complex medical procedures as well as invasive testing and monitoring which tend to be painful and anxiety-provoking, necessitating the provision of analgesia and sedation to reduce stress response. Achieving the optimal combination of adequate analgesia and appropriate sedation can be quite challenging in a patient population with a wide spectrum of ages, sizes, and developmental stages. The added complexities of critical illness in the pediatric population such as evolving pathophysiology, impaired organ function, as well as altered pharmacodynamics and pharmacokinetics must be considered. Undersedation leaves patients at risk of physical and psychological stress which may have significant long term consequences. Oversedation, on the other hand, leaves the patient at risk of needing prolonged respiratory, specifically mechanical ventilator, support, prolonged ICU stay and hospital admission, and higher risk of untoward effects of analgosedative agents. Both undersedation and oversedation put critically ill pediatric patients at high risk of developing PICU-acquired complications (PACs) like delirium, withdrawal syndrome, neuromuscular atrophy and weakness, post-traumatic stress disorder, and poor rehabilitation. Optimal analgesia and sedation is dependent on continuous patient assessment with appropriately validated tools that help guide the titration of analgosedative agents to effect. Bundled interventions that emphasize minimizing benzodiazepines, screening for delirium frequently, avoiding physical and chemical restraints thereby allowing for greater mobility, and promoting adequate and proper sleep will disrupt the PICU culture of immobility and reduce the incidence of PACs.

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Section: Analgesiamentioning

confidence: 99%

Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit

Egbuta

Mason

2021

JCM

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“…The mechanism of action of APAP induced analgesia is not well understood . It has been postulated that the primary analgesic effect of APAP is induced by cyclooxygenase inhibition, N ‐methyl‐ d ‐aspartate receptor inhibition, and serotonergic antagonism in the central nervous system . Traditional formulations of APAP include oral and rectal forms.…”

Section: Introductionmentioning

confidence: 99%

“…Traditional formulations of APAP include oral and rectal forms. Aside from the route of drug delivery, there are other marked differences in the pharmacokinetic properties of the IV formulation . IV APAP results in a rapid elevation in plasma concentration .…”

Section: Introductionmentioning

confidence: 99%

“…Aside from the route of drug delivery, there are other marked differences in the pharmacokinetic properties of the IV formulation . IV APAP results in a rapid elevation in plasma concentration . Compared to the oral formulation, the time to reach maximum concentration for IV APAP (15 minutes) is more predictable than the oral immediate‐release (10–60 minutes), oral extended‐release (60–120 minutes), and rectal (variable) formulations .…”

Section: Introductionmentioning

confidence: 99%

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The Use of Intravenous Acetaminophen for Acute Pain in the Emergency Department

Sin

Wai

Tatunchak

et al. 2016

Academic Emergency Medicine

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Objectives: Acetaminophen (APAP) is a mainstay for pain management worldwide. The intravenous (IV) formulation has been widely used in Europe for more than 20 years in adults and children. In the United States, IV APAP obtained full approval from the Food and Drug Administration in 2010. There is emerging literature to suggest the use of IV APAP for pain reduction in the emergency department (ED). This evidence-based review examines the evidence pertaining to the use of IV APAP for acute pain control in the ED.Methods: The MEDLINE and EMBASE databases were searched. Randomized controlled trials (RCTs) that described or evaluated the use of IV APAP for acute pain in the ED were included. Duplicate articles, unpublished reports, abstracts, review articles, and non-English literature were excluded. The primary outcome of interest in this review was the difference in pain score between IV APAP and active comparator or placebo from baseline to a cutoff time specified in the original trials. Secondary outcome measures were the incidence of adverse events and reduction in the amount of adjuvant analgesics consumed by patients who received IV APAP. Methodologic quality of the trials was assessed using the Grading of Recommendations Assessment, Development, and Evaluation criteria.Results: Fourteen RCTs with various methodologic flaws, which enrolled a total of 1,472 patients, met the inclusion criteria. The level of evidence for the individual trials ranged from very low to moderate. In three of the 14 trials, a significant reduction in pain scores was observed in patients who received IV APAP. The first trial found a significant reduction in mean pain scores when IV APAP was compared to IV morphine at 30 minutes after drug administration (4.7 AE 2.3 vs. 2.9 AE 2.2). In the second trial, patients who received IV APAP reported of lower pain scores (31.7 AE 18 mm, 95% confidence interval [CI] = 8.2 to 25.2 mm) compared to those who received IV morphine (48.3 AE 14.1 mm, 95% CI = 8.2 to 25.2 mm), 15 minutes after drug administration. A third trial found a significant reduction (p = 0.005) in the mean pain scores when IV APAP was compared to intramuscular piroxicam at 90 minutes after drug administration. In the remaining eight trials, pain scores were not statistically different when IV APAP was compared to other pain medications. The incidence of side effects associated with IV APAP was very low. Conclusions

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“…model for a dual c-Met and VEGFR2 kinase inhibitor is important for tumor treatment. At present, several natural compounds are being used as chemopreventive agents for cancer, and there is increasing interest in identifying the antitumor activity of these agents (12,13). However, no natural products have been identified with an inhibitory profile towards both c-Met and VEGFR2.…”

Section: Structure Activity Relationships Of Chrysoeriol and Analogs mentioning

confidence: 99%

Structure activity relationships of chrysoeriol and analogs as dual c‑Met and VEGFR2 tyrosine kinase inhibitors

et al. 2018

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Vascular endothelial growth factor receptor 2 (VEGFR2) and c‑Met are tyrosine kinases, which are involved in the tumorigenesis of various types of cancer. Previous studies have demonstrated that the elevated activation of c‑Met is associated with the drug resistance of VEGFR2 inhibitors. Therefore, dual c‑Met and VEGFR2 kinase inhibitors are expected to overcome VEGFR2 inhibitor resistance and subsequently lead to a superior therapeutic outcome to regular VEGFR2 inhibitors. In the present study, it was found that chrysoeriol, which can be extracted from several natural plants, was a potential dual c‑Met and VEGFR2 kinase inhibitor. The results of docking experiments revealed that chrysoeriol was able to efficiently bind in the active site cavity of c‑Met and VEGFR2. The results of enzymatic assays showed relatively high binding affinities of chrysoeriol to c‑Met (Kd=12 µM) and VEGFR2 (Kd=11 µM). The structure activity relationships (SARs) of chrysoeriol and its analogs were investigated using pharmacological and molecular docking experiments. To the best of our best knowledge, the present study is the first to report a natural product with both c‑Met and VEGFR2 inhibitory profiles, and provides insights into future dual c‑Met and VEGFR2 kinase inhibitor development.

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OFIRMEV: An Old Drug Becomes New Again

Cited by 14 publications

References 26 publications

Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit

Current State of Analgesia and Sedation in the Pediatric Intensive Care Unit

The Use of Intravenous Acetaminophen for Acute Pain in the Emergency Department

Structure activity relationships of chrysoeriol and analogs as dual c‑Met and VEGFR2 tyrosine kinase inhibitors

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