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Ketorolac pharmacodynamics

Pierluigi Marzuillo, Lorenzo Calligaris, Stefano Amoroso, Egidio Barbi
In June 2013, the European Medicine Agency recommended limiting codeine use in paediatric patients, creating a void in managing moderate pain. We reviewed the literature published in English (1985-June 2017) on the pharmacokinetic, pharmacodynamic and safety profile of ketorolac, a possible substitute for codeine and opioids, for treating moderate-to-severe pain. We found that gastrointestinal side effects were mainly reported with prolonged use, significant bleeding was reported in adenotonsillectomy, and adverse renal effects appeared to be limited to patients with specific coexisting risk factors...
April 2018: Acta Paediatrica
Nicholas Schwier, Nicole Tran
Aspirin (ASA) and non-steroidal anti-inflammatory drugs (NSAIDs) are a mainstay of therapy for the treatment of idiopathic pericarditis (IP). A comprehensive review consisting of pertinent clinical literature, pharmacokinetic, and pharmacodynamic considerations, has not been released in recent years. This review will facilitate the clinician's understanding of pharmacotherapeutic considerations for using ASA/NSAIDs to treat IP. Data were compiled using clinical literature consisting of case reports, cohort data, retrospective and prospective studies, and manufacturer package inserts...
March 23, 2016: Pharmaceuticals
Xin Li, Lina Du, Xu Chen, Pingju Ge, Yu Wang, Yangmu Fu, Haiyan Sun, Qingwei Jiang, Yiguang Jin
Ketorolac tromethamine (KT) was potent to treat moderate to moderately severe pains. However, KT solutions for nasal delivery lost quickly from the nasal route. Thermo- and ion-sensitive in-situ hydrogels (ISGs) are appropriate for nasal drug delivery because the intranasal temperature maintains ∼37 °C and nasal fluids consist of plentiful cations. In this study, a novel nasal thermo- and ion-sensitive ISG of KT was prepared with thermo-sensitive poloxamer 407 (P407) and ion-sensitive deacetylated gellan gum (DGG)...
July 15, 2015: International Journal of Pharmaceutics
Daniel J Wilson, Scott M Schutte, Steven R Abel
OBJECTIVE: To review the commercially available ophthalmic nonsteroidal anti-inflammatory drugs (NSAIDs), identify opportunities for therapeutic substitutions within and outside of their Food and Drug Administration (FDA)-approved indications, and identify clinically superior drugs within the class for specific indications. DATA SOURCE: A PubMed search (1992 through January 2014) was performed on the terms diclofenac, ketorolac, flurbiprofen, bromfenac, and nepafenac...
June 2015: Annals of Pharmacotherapy
Iu I Hubs'kyĭ, T A Bukhtiarova, H H Horiushko, N V Litvinova, H I Paramonova, T M Kurapova, O M Velychko, L P Babenko
Methods of fluorescent probing, spectrophotometry and microcalorimetry were applied to investigate the alterations in biophysical parameters of erythrocytes membranes, and specifically microviscosity, surface charge, molecular organization of lipid bilayer and lipid-protein interactions under conditions of acute pain syndrome produced by experimental chemical lesion. The distinctive features of non-opiod analgesics interactions and binding to the erythrocytes membranes of rats subjected to acute nociceptive pain accompanied with oxidative stress development were investigated...
May 2014: Ukrainian Biochemical Journal
Benjamin M Jones, Michael W Neville
OBJECTIVE: To examine the efficacy of nepafenac in the treatment of pain and inflammation in patients after cataract surgery using evidence from controlled clinical studies. DATA SOURCES: Citations in Google Scholar, PubMed, and Web of Science from January 1, 2005, to March 25, 2013, were identified using nepafenac and cataract as search terms. STUDY SELECTION AND DATA EXTRACTION: The literature search was limited to human studies published in English...
June 2013: Annals of Pharmacotherapy
Kuntheavy Ing Lorenzini, Marie Besson, Youssef Daali, Denis Salomon, Pierre Dayer, Jules Desmeules
A pharmacokinetic/pharmacodynamic, randomized, crossover, placebo-controlled study was conducted in healthy human volunteers with the primary objective of exploring the existence of a positive interaction between paracetamol 1 g and ketorolac 20 mg intravenously on experimental pain models. Further, the simplified UVB model was validated as a screening tool for analgesics or a combination of analgesics in clinical drug development. It was observed that the UVB irradiation induced primary hyperalgesia, evidenced by significant decreases of the heat pain threshold from (mean ± SD) 46...
2012: Chimia
H O Ammar, M Ghorab, A A Mahmoud, T S Makram, A M Ghoneim
CONTEXT: Ketorolac is one of the most potent nonsteroidal anti-inflammatory drugs and is an attractive alternative to opioids for pain management. OBJECTIVE: Development and evaluation of transdermal ketorolac film forming polymeric solution. MATERIALS AND METHODS: Eudragits(®) RLPO, RSPO and E100 as well as polyvinyl pyrrolidone K30 dissolved in ethanol were used as film forming solutions. In vitro experiments were conducted to optimize formulation parameters...
September 2013: Pharmaceutical Development and Technology
Kuntheavy Ing Lorenzini, Marie Besson, Youssef Daali, Denis Salomon, Pierre Dayer, Jules Desmeules
The combination of paracetamol with non-steroidal anti-inflammatory drugs (NSAIDs) is widely used; however, the nature and mechanism of their interaction are still debated. A double-blind, pharmacokinetic/pharmacodynamic, randomized, cross-over, placebo-controlled study was carried out in human healthy volunteers. The aim was to explore the existence of a positive interaction between paracetamol 1 g and ketorolac 20 mg administered intravenously on experimental pain models in human beings. The effects of the paracetamol-ketotolac combination were compared with similar doses of respective single analgesic and to placebo on the sunburn model (UVB-induced inflammation), cold pain tolerance and the nociceptive flexion reflex...
November 2011: Basic & Clinical Pharmacology & Toxicology
Kayode Ogungbenro, Leon Aarons
Population pharmacodynamic experiments sometime involve repeated measurements of ordinal random variables at specific time points. Such longitudinal data presents a challenge during modelling due to correlation between measurements within an individual and often mixed-effects modelling approach may be used for the analysis. It is important that these studies are adequately powered by including an adequate number of subjects in order to detect a significant treatment effect. This paper describes a method for calculating sample size for repeated ordinal measurements in population pharmacodynamic experiments based on analysis by a mixed-effects modelling approach...
February 2010: Journal of Pharmacokinetics and Pharmacodynamics
Tom Walters, Michael Raizman, Paul Ernest, Johnny Gayton, Robert Lehmann
PURPOSE: To evaluate the aqueous humor concentrations and cyclooxygenase (COX) inhibitory activities of nepafenac, amfenac, ketorolac, and bromfenac after topical ocular administration of Nevanac (nepafenac 0.1%), Acular LS (ketorolac 0.4%), or Xibrom (bromfenac 0.09%). SETTING: Five private ophthalmology practices throughout the United States. METHODS: Patients requiring cataract extraction were randomized to 1 of 3 treatment groups: Nevanac, Acular LS, or Xibrom...
September 2007: Journal of Cataract and Refractive Surgery
N I Voloshchuk, A A Pentiuk, A D Durnev
Non-narcotic analgetics sodium diclofenac, indomethacin, naproxen, nimesulid, ketorolac, and celebrex (cytochrome P-450(2)c substrates) produce more pronounced and prolonged analgesic effect in pubertate female rats than in males. This can be related to the slower elimination of drugs from the female organism. The liver of females is characterized by a lower content of cytochrome P-450 and by less pronounced activity of amidopyrine-N-, indomethacin-O-, and naproxen-O-demethylase activity. No sex-related differences in pharmacodynamics were observed for meloxicam, and ethoricoxib, benzofurocaine, and amison, and acetylsalicylic acid, which are the substrates predominantly for CYP3A...
July 2005: Eksperimental'naia i Klinicheskaia Farmakologiia
V Puri, A K Bansal
One of the prerequisites for a parenteral preparation is that the excipients incorporated are biocompatible and biodegradable. In the present study hydrophilic and hydrophobic excipients were investigated for developing an intramuscular sustained-release formulation of ketorolac. Kollidon 17 PF, Peceol (glyceryl monooleate), and castor oil were chosen as the potential release-retarding agents, each with a distinct mechanism of action. They were evaluated by in vitro drug-release profiles and in vivo pharmacodynamic and pharmacokinetic study in mice...
July 2004: Drug Development and Industrial Pharmacy
Mellar P Davis, Manish Srivastava
The prevalence of pain increases with each decade of life. Pain in the elderly is distinctly different from pain experienced by younger individuals. Cancer is a leading cause of pain; however, other conditions that cause pain such as facet joint arthritis (causing low back pain), polymyalgia rheumatica, Paget's disease, neuropathies, peripheral vascular disease and coronary disease most commonly occur in patients over the age of 50 years. Poorly controlled pain in the elderly leads to cognitive failure, depression and mood disturbance and reduces activities of daily living...
2003: Drugs & Aging
J A Cordero, M Camacho, R Obach, J Domenech, L Vila
The aim of the present work was to generate an index to predict topical efficiency of a series of nonsteroidal anti-inflammatory drugs (NSAIDs): indomethacin, diclofenac, ketoprofen, piroxicam, tenoxicam and ketorolac. This index took into account both biopharmaceutic and pharmacodynamic aspects. The biopharmaceutic aspect, based on the maximal flux (J(m)), was determined experimentally from transdermal studies carried out with human skin in previous work. The pharmacodynamic aspect, based on the ability to inhibit cyclooxygenase-2 (COX-2) in vitro, was determined by incubating human dermal fibroblasts in culture, pre-treated with phobol-12-myristate-13-acetate (PMA) for 6 h, with 25 microM [(14)C]-arachidonic acid (AA) in the presence of several drug concentrations...
March 2001: European Journal of Pharmaceutics and Biopharmaceutics
M Amanzio, A Pollo, G Maggi, F Benedetti
Individual differences in pharmacokinetics and pharmacodynamics, the type of pain and the method of drug administration can account for the response variability to analgesics. By integrating a clinical and an experimental approach, we report here that another important source of variability is represented by individual differences in non-specific (placebo) activation of endogenous opioid systems. In the first part of this study, we analyzed the effectiveness of buprenorphine, tramadol, ketorolac and metamizol in the clinical setting, where the placebo effect was completely eliminated by means of hidden infusions...
February 15, 2001: Pain
J C Gillis, R N Brogden
Ketorolac is a nonsteroidal anti-inflammatory drug (NSAID) with strong analgesic activity. The analgesic efficacy of ketorolac has been extensively evaluated in the postoperative setting, in both hospital inpatients and outpatients, and in patients with various other acute pain states. After major abdominal, orthopaedic or gynaecological surgery or ambulatory laparoscopic or gynaecological procedures, ketorolac provides relief from mild to severe pain in the majority of patients and has similar analgesic efficacy to that of standard dosages of morphine and pethidine (meperidine) as well as less frequently used opioids and other NSAIDs...
January 1997: Drugs
J W Mandema, D R Stanski
OBJECTIVE: To derive a population pharmacokinetic-pharmacodynamic model that characterizes the distribution of pain relief scores and remedication times observed in patients receiving intramuscular ketorolac for the treatment of moderate to severe postoperative pain. BACKGROUND: The data analysis approach deals with the complexities of analyzing analgesic trial data: (1) repeated measurements, (2) ordered categorical response variables, and (3) nonrandom censoring because the patients can take a rescue medication if their pain relief is insufficient...
December 1996: Clinical Pharmacology and Therapeutics
S Toon, B L Holt, F G Mullins, R Bullingham, L Aarons, M Rowland
1. The potential interaction between racemic warfarin given as a 25 mg single oral dose and chronically administered ketorolac was studied in 12 young healthy male volunteers. 2. Ketorolac produced no major change in the pharmacokinetics of (R)- or (S)-warfarin. 3. Ketorolac did not alter the pharmacodynamic profile of racemic warfarin. 4. Ketorolac increased template bleeding time by a factor of 1.35 as compared with placebo. 5. The results suggest that the ketorolac-warfarin interaction is unlikely to be of major clinical significance; however, combined use of ketorolac and warfarin in patients should be undertaken with due caution and appropriate monitoring...
November 1990: British Journal of Clinical Pharmacology
M M Buckley, R N Brogden
Ketorolac is a non-steroidal agent with potent analgesic and moderate anti-inflammatory activity. It is administered as the tromethamine salt orally, intramuscularly, intravenously, and as a topical ophthalmic solution. Clinical studies indicate single-dose efficacy greater than that of morphine, pethidine (meperidine) and pentazocine in moderate to severe postoperative pain, with some evidence of a more favourable adverse effect profile than morphine or pethidine. In single-dose studies ketorolac has also compared favourably with aspirin, paracetamol (acetaminophen) and a few other non-steroidal anti-inflammatory drugs...
January 1990: Drugs
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