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Acetaminophen, paracetamol

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https://www.readbyqxmd.com/read/28816033/selection-of-12-hour-sustained-release-acetaminophen-paracetamol-formulation-through-comparison-of-pharmacokinetic-profiles-of-4-sustained-release-prototype-formulations-and-standard-acetaminophen-formulation-an-open-label-randomized-proof-of-principle-pharmacokinetic
#1
Yong Yue, Dongzhou J Liu
Acetaminophen (APAP; paracetamol), a widely used analgesic and antipyretic, is available in modified-release and immediate-release (IR) formulations requiring 3- or 4-times-daily dosing. This phase 1 open-label crossover study compared pharmacokinetic profiles of single 2000-mg doses of 4 different sustained-release (SR) formulations of APAP (designed to allow twice-daily dosing) against two 1000-mg doses (taken 6 hours apart) of standard IR APAP in 14 healthy volunteers. The primary end point was duration of time that plasma APAP concentration exceeded a plasma concentration (TC ) of 4 μg/mL...
August 16, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28816026/evaluation-of-a-12-hour-sustained-release-acetaminophen-paracetamol-formulation-a-randomized-3-way-crossover-pharmacokinetic-and-safety-study-in-healthy-volunteers
#2
Yong Yue, Agron Collaku, Dongzhou J Liu
Acetaminophen (paracetamol) is a first-line treatment for mild and moderate pain. A twice-daily sustained-release (SR) formulation may be more convenient for chronic users than standard immediate-release (IR) acetaminophen. This randomized, 3-way crossover study evaluated pharmacokinetics and safety of single-dose 1500- and 2000-mg SR acetaminophen formulations and 2 doses of IR acetaminophen 1000 mg given 6 hours apart in healthy adults (n = 14). Primary outcome was time that plasma acetaminophen concentration was ≥4 μg/mL (TC≥4μg/mL )...
August 16, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28815997/bioequivalence-and-safety-of-twice-daily-sustained-release-paracetamol-acetaminophen-compared-with-3-and-4-times-daily-paracetamol-a-repeat-dose-crossover-pharmacokinetic-study-in-healthy-volunteers
#3
Dongzhou J Liu, Agron Collaku
Twice-daily sustained-release (SR) paracetamol (acetaminophen) offers convenient administration to chronic users. This study investigated at steady state (during the last 24 hours of a 3-day dosing period) the pharmacokinetics, bioequivalence, and safety of twice-daily SR paracetamol compared with extended-release (ER) and immediate-release (IR) paracetamol. In this open-label, randomized, multidose, 3-way crossover study, 28 healthy subjects received paracetamol SR (2 × 1000 mg twice daily), ER (2 × 665 mg 3 times daily), and IR (2 × 500 mg 4 times daily)...
August 16, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28812385/increased-acetaminophen-related-calls-to-finnish-pic-better-reflect-acetaminophen-sales-than-serious-poisonings
#4
Mikko J Parry, Helena Isoniemi, Anna-Maria Koivusalo, Kalle Hoppu
OBJECTIVE: Acetaminophen (APAP) or paracetamol is a commonly encountered medicine in poisonings. We studied the changes in APAP related calls to the Finnish poison information centre (FPIC), and serious intoxications, involving hepatotoxicity or death in 2001-2014. These data were compared with paracetamol sales in Finland. METHODS: This is a retrospective analysis of the FPIC database calls, national cause of death registry, registries of liver transplantations and molecular adsorbent recycling system (MARS)-treated patients from Helsinki University Hospital together with the National Institute of Health and Welfare registry of patients hospitalized...
August 16, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28797958/quantification-of-paracetamol-and-5-oxoproline-in-serum-by-capillary-electrophoresis-implication-for-clinical-toxicology
#5
Tomáš Hložek, Tomáš Křížek, Petr Tůma, Miroslava Bursová, Pavel Coufal, Radomír Čabala
High anion gap metabolic acidosis frequently complicates acute paracetamol overdose and is generally attributed to lactic acidosis or compromised hepatic function. However, metabolic acidosis can also be caused by organic acid 5-oxoproline (pyroglutamic acid). Paracetamol's toxic intermediate, N-acetyl-p-benzoquinoneimine irreversibly binds to glutathione and its depletion leads to subsequent disruption of the gamma glutamyl cycle and an excessive 5-oxoproline generation. This is undoubtedly an underdiagnosed condition because measurement of serum 5-oxoproline level is not readily available...
July 26, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28782093/metabolic-acidosis-caused-by-concomitant-use-of-paracetamol-acetaminophen-and-flucloxacillin-a-case-report-and-a-retrospective-study
#6
J K Berbee, L A Lammers, C T P Krediet, J C Fischer, E M Kemper
PURPOSE: A patient was identified with severe metabolic acidosis, a high anion gap and 5-oxoproline accumulation, probably caused by the simultaneous use of paracetamol (acetaminophen) and flucloxacillin. We wanted to investigate the necessity to control the interaction between both drugs with an automatic alert system. METHODS: To investigate the relevance of the interaction of paracetamol and flucloxacillin, a retrospective study was conducted. Data on paracetamol and flucloxacillin prescriptions and laboratory data (pH, Na(+), HCO3(-), Cl(-), albumin and 5-oxoproline levels) were combined to assess the prevalence of acidosis, calculate the anion gap and analyse 5-oxoproline levels in clinically admitted patients using both drugs simultaneously...
August 7, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28770975/paracetamol-acetaminophen-for-chronic-non-cancer-pain-in-children-and-adolescents
#7
REVIEW
Tess E Cooper, Emma Fisher, Brian Anderson, Nick Mr Wilkinson, David G Williams, Christopher Eccleston
BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past, pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as important...
August 2, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28766264/acetaminophen-paracetamol-induces-hypothermia-during-acute-cold-stress
#8
Josh Foster, Alexis R Mauger, Andrew Govus, David Hewson, Lee Taylor
BACKGROUND: Acetaminophen is an over-the-counter drug used to treat pain and fever, but it has also been shown to reduce core temperature (T c) in the absence of fever. However, this side effect is not well examined in humans, and it is unknown if the hypothermic response to acetaminophen is exacerbated with cold exposure. OBJECTIVE: To address this question, we mapped the thermoregulatory responses to acetaminophen and placebo administration during exposure to acute cold (10 °C) and thermal neutrality (25 °C)...
August 1, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28754173/a-randomized-double-blind-placebo-controlled-trial-on-the-role-of-preemptive-analgesia-with-acetaminophen-paracetamol-in-reducing-headache-following-electroconvulsive-therapy-ect
#9
Amila Isuru, Asiri Rodrigo, Chamara Wijesinghe, Dileepa Ediriweera, Shan Premadasa, Carmel Wijesekara, Lalith Kuruppuarachchi
BACKGROUND: Electroconvulsive therapy (ECT) is a safe and efficient treatment for several severe psychiatric disorders, but its use is limited by side effects. Post-ECT headache is one of the commonest side effects. Preemptive analgesia is effective in post-surgical pain management. The most commonly used analgesic is acetaminophen (paracetamol). However, acetaminophen as a preemptive analgesic for post-ECT headache has not been studied adequately. This study was conducted to compare the incidence and severity of post-ECT headache in patients who were administered acetaminophen pre-ECT with a placebo group...
July 28, 2017: BMC Psychiatry
https://www.readbyqxmd.com/read/28752572/effect-of-paracetamol-on-semen-quality
#10
REVIEW
S A Banihani
Several published studies, both direct and indirect, have connected paracetamol, also named acetaminophen, a commonly used over-the-counter analgesic and antipyretic medication, with semen quality and male infertility, although as yet this connection is unclear. This review addresses the effect of paracetamol on semen quality and hence on male factor infertility. We searched the MEDLINE database from January 1980 through January 2017 for English-language articles using the key words "paracetamol" and "acetaminophen" versus "sperm...
July 28, 2017: Andrologia
https://www.readbyqxmd.com/read/28729056/discovery-and-structure-activity-relationship-of-auriculatone-a-potent-hepatoprotective-agent-against-acetaminophen-induced-liver-injury
#11
Meng Zhou, Min Wang, Rui-Feng Zhong, Xiang-Ming Liao, Lian-Li Deng, Guo-Bo Xu, Xun He, Jing Li, Yong-Jun Li, Ting Liu, Yong-Lin Wang, Shang-Gao Liao
Acetaminophen (APAP, paracetamol) overdose has been the most frequent cause of drug-induced liver failure. APAP-induced liver toxicity can be fatal in many cases even with treatment of the clinically used N-acetylcysteine (NAC), and the need for novel therapeutic agents is apparent. Through evaluating the hepatoprotective effects of the co-occurring substances present in oleanolic acid tablets which have been used in China for decades as an adjuvant therapy for acute and chronic hepatitis, auriculatone was found to protect HL-7702 cells from APAP-induced liver injury comparable to NAC at the concentration of 10μM...
July 10, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28720398/perinatal-and-neonatal-use-of-paracetamol-for-pain-relief
#12
REVIEW
Karel Allegaert, John N van den Anker
Paracetamol (acetaminophen) is the most widely used drug to treat pain or fever in pregnant women or neonates, but its pharmacokinetics (PK) and pharmacodynamics (PD) warrant a focused analysis. During pregnancy, there is an important increase in paracetamol clearance. Consequently, it is reasonable to anticipate that the analgesic effect of paracetamol will decrease faster, whereas higher doses may result in even higher oxidative toxic metabolites. Therefore, most peripartal PD data relate to multimodal analgesia strategies...
July 15, 2017: Seminars in Fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28700092/oral-paracetamol-acetaminophen-for-cancer-pain
#13
REVIEW
Philip J Wiffen, Sheena Derry, R Andrew Moore, Ewan D McNicol, Rae F Bell, Daniel B Carr, Mairead McIntyre, Bee Wee
BACKGROUND: Pain is a common symptom with cancer, and 30% to 50% of all people with cancer will experience moderate to severe pain that can have a major negative impact on their quality of life. Non-opioid drugs are commonly used to treat mild to moderate cancer pain, and are recommended for this purpose in the WHO cancer pain treatment ladder, either alone or in combination with opioids.A previous Cochrane review that examined the evidence for nonsteroidal anti-inflammatory drugs (NSAIDs) or paracetamol, alone or combined with opioids, for cancer pain was withdrawn in 2015 because it was out of date; the date of the last search was 2005...
July 12, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28668582/selective-laser-sintering-sls-3d-printing-of-medicines
#14
Fabrizio Fina, Alvaro Goyanes, Simon Gaisford, Abdul W Basit
Selective laser sintering (SLS) 3-dimensional printing is currently used for industrial manufacturing of plastic, metallic and ceramic objects. To date there have been no reports on the use of SLS to fabricate oral drug loaded products; therefore, the aim of this work was to explore the suitability of SLS printing for manufacturing medicines. Two thermoplastic pharmaceutical grade polymers, Kollicoat IR (75% polyvinyl alcohol and 25% polyethylene glycol copolymer) and Eudragit L100-55 (50% methacrylic acid and 50% ethyl acrylate copolymer), with immediate and modified release characteristics respectively, were selected to investigate the versatility of a SLS printer...
June 29, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28633104/transcriptional-and-cellular-effects-of-paracetamol-in-the-oyster-crassostrea-gigas
#15
M J Bebianno, A C P Mello, M A S Serrano, F Flores-Nunes, J J Mattos, F L Zacchi, C E Piazza, M N Siebert, R S Piazza, C H A M Gomes, C M R Melo, A C D Bainy
Acetaminophen (paracetamol) (PAR) is one of the most popular non-steroidal anti-inflammatory drugs (NSAIDs) with analgesic and antipyretic properties consumed worldwide and often detected in the aquatic environment. Due to the fact that PAR induces oxidative stress in mammals, the aim of this study was to evaluate if similar effects were observed in oysters Crassostrea gigas, given their economic and ecological importance and worldwide distribution. Oysters were exposed for 1, 4 and 7 days to two different sublethal PAR concentrations (0, 1 and 100μgL(-1))...
June 17, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28621528/unsupervised-discovery-and-comparison-of-structural-families-across-multiple-samples-in-untargeted-metabolomics
#16
Justin J J van der Hooft, Joe Wandy, Francesca Young, Sandosh Padmanabhan, Konstantinos Gerasimidis, Karl E V Burgess, Michael P Barrett, Simon Rogers
In untargeted metabolomics approaches, the inability to structurally annotate relevant features and map them to biochemical pathways is hampering the full exploitation of many metabolomics experiments. Furthermore, variable metabolic content across samples result in sparse feature matrices that are statistically hard to handle. Here, we introduce MS2LDA+ that tackles both above-mentioned problems. Previously, we presented MS2LDA, which extracts biochemically relevant molecular substructures ("Mass2Motifs") from a collection of fragmentation spectra as sets of co-occurring molecular fragments and neutral losses, thereby recognizing building blocks of metabolomics...
July 18, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28596036/the-oriented-processes-for-extraction-and-recovery-of-paracetamol-compound-across-different-affinity-polymer-membranes-parameters-and-mechanisms
#17
E H El Atmani, A Benelyamani, H Mouadili, S Tarhouchi, S Majid, K Touaj, L Lebrun, M Hlaibi
Membrane processes represent one of the most promising technologies for separation and extraction in modern industries, because they have several advantages. Today these processes are an important research topic, including affinity polymer membranes that are highly efficient for oriented processes. Three affinity polymer membrane types containing lipophilic compounds, methyl cholate (MC) and cholic acid (CA) as extractive agents were prepared and characterized. They have been used to extract active ingredient paracetamol (acetaminophen), from concentrated solutions (0...
June 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28586638/efficacy-of-codeine-when-added-to-paracetamol-acetaminophen-and-ibuprofen-for-relief-of-postoperative-pain-after-surgical-removal-of-impacted-third-molars-a-double-blinded-randomized-control-trial
#18
Adrian D Best, R K De Silva, W M Thomson, Darryl C Tong, Claire M Cameron, Harsha L De Silva
PURPOSE: The use of opioids in combination with nonopioids is common practice for acute pain management after third molar surgery. One such combination is paracetamol, ibuprofen, and codeine. The authors assessed the efficacy of codeine when added to a regimen of paracetamol and ibuprofen for pain relief after third molar surgery. MATERIALS AND METHODS: This study was a randomized, double-blinded, placebo-controlled trial conducted in patients undergoing the surgical removal of at least 1 impacted mandibular third molar requiring bone removal...
May 15, 2017: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28577513/synergistic-protective-effect-of-picrorhiza-with-honey-in-acetaminophen-induced-hepatic-injury
#19
Prashant Gupta, Alok Tripathi, Tripti Agrawal, Chandradeo Narayan, B M Singh, Mohan Kumar, Arvind Kumar
Rhizome of picrorhiza along with honey prevents hepatic damage and cure the acetaminophen (paracetamol) induced hepatotoxicity by modulating the activity of hepatic enzymes. Here, we studied the in vivo effects of Picrorhiza kurroa and honey on acetaminophen induced hepatotoxicity Balb/c mice model. Hepatic histopathological observations of acetaminophen fed (day-6) group showed more congestion, hemorrhage, necrosis, distorted hepatic architecture and nuclear inclusion. Such damages were recompensed to normal by picrorhiza or honey alone or both in combinations...
August 2016: Indian Journal of Experimental Biology
https://www.readbyqxmd.com/read/28559473/paracetamol-acetaminophen-impairs-brain-masculinisation
#20
Anders Hay-Schmidt, Olivia Finkielman, Benjamin Jensen, Christine Høgsbro, Jacob Bak Holm, Kristoffer Haurum Johansen, Tina Kold Jensen, Anderson Martino Andrade, Shanna Swan, Carl-Gustaf Bornehag, Søren Brunak, Bernard Jegou, Karsten Kristiansen, David Møbjerg Kristensen
Paracetamol/acetaminophen (N-Acetyl-p-Aminophenol; APAP) is the preferred analgesic for pain relief and fever during pregnancy. It has therefore caused concern that several studies have reported that prenatal exposure to APAP results in developmental alterations in both the reproductive tract and the brain. Genitals and nervous system of male mammals are actively masculinized during foetal development and early postnatal life by the combined actions of prostaglandins and androgens, resulting in the male-typical reproductive behaviour seen in adulthood...
May 30, 2017: Reproduction: the Official Journal of the Society for the Study of Fertility
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