Paracetamol ist ein weit verbreitetes Schmerzmittel und normalerweise nicht zellschädigend. Bestimmte Enzyme können es jedoch in ein Toxin verwandeln. Diese toxische Nebenwirkung möchte man natürlich ...nicht haben, wenn man Kopfschmerz oder Fieber behandelt. Krebszellen damit zu vernichten, klingt aber verheißungsvoll. Ein Forscherteam um Hong‐Cai Zhou von der Texas A&M University in den USA hat jetzt einen Nanoreaktor entwickelt, der diese Reaktion auslösen kann und damit Tumorzellen zerstört. Er besteht aus einem Verbund von einem Enzym und einer metallorganischen Gerüstverbindung, einem „MOF“.
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The manufacture of immediate release high drug loading paracetamol oral tablets was achieved using an extrusion based 3D printer from a premixed water based paste formulation. The 3D ...printed tablets demonstrate that a very high drug (paracetamol) loading formulation (80% w/w) can be printed as an acceptable tablet using a method suitable for personalisation and distributed manufacture. Paracetamol is an example of a drug whose physical form can present challenges to traditional powder compression tableting. Printing avoids these issues and facilitates the relatively high drug loading. The 3D printed tablets were evaluated for physical and mechanical properties including weight variation, friability, breaking force, disintegration time, and dimensions and were within acceptable range as defined by the international standards stated in the United States Pharmacopoeia (USP). X-ray Powder Diffraction (XRPD) was used to identify the physical form of the active. Additionally, XRPD, Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR) and differential scanning calorimetry (DSC) were used to assess possible drug-excipient interactions. The 3D printed tablets were evaluated for drug release using a USP dissolution testing type I apparatus. The tablets showed a profile characteristic of the immediate release profile as intended based upon the active/excipient ratio used with disintegration in less than 60 s and release of most of the drug within 5 min. The results demonstrate the capability of 3D extrusion based printing to produce acceptable high-drug loading tablets from approved materials that comply with current USP standards.
In Europe, 50–60% of pregnant women uses paracetamol (PCM), also known as acetaminophen. While it was considered to be safe, recent studies have shown an association between prenatal exposure to PCM ...and increased incidences of autism, cryptorchidism, asthma and ADHD. In this study the transplacental transfer of PCM and its metabolites was investigated using an ex vivo human placenta perfusion model (closed circuit; n = 38). Maternal-to-foetal (M-F) and foetal-to-maternal (F-M) transplacental transfer was determined at a concentration correlating with the maximum and steady state concentration in normal clinical use. Antipyrine (AP) was added as reference compound. Samples of the foetal and maternal perfusion medium were taken until 210 (PCM) or 360 min (paracetamol sulphate (PCM-S) and paracetamol glucuronide (PCM-G). PCM and AP concentrations reached an equilibrium between foetal and maternal compartments within the duration of the perfusion experiment and irrespective of the transfer direction. The percentage placental transfer of PCM was 45% (M-F and F-M). For PCM-S, transfer was 39% (M-F) and 28% (F-M), while the PCM-G transfer was 34% (M-F) and 25% (F-M). During placenta perfusions with the metabolites slight conversion (3.5–4.1%) to PCM was observed. In conclusion, PCM crosses the placental barrier rapidly via passive diffusion. Differences in flow rate and villous placental structure explain the significantly faster M-F transfer than F-M transfer of PCM. The larger and more hydrophilic molecules PCM-S and PCM-G cross the placenta at a significantly lower rate. Moreover, their F-M transport is about 40% slower than M-F transport, suggesting involvement of a transporter.
•Paracetamol and its main metabolites cross the placenta bidirectionally•Paracetamol reaches an equilibrium between foetal and maternal compartments.•The metabolites cross the placenta at a significantly lower rate.•Foetal-to-maternal transport of the metabolites is 40% slower than vice-versa.•During the perfusions 4% of the metabolites was converted by the placenta into paracetamol.
The widespread occurence of pharmaceutical pollutants seriously threatens the environment and human well-being. In the present study, zinc ferrite nanoparticles (ZnFe2O4 NPs) have been synthesized by ...co-precipitation method and used as photocatalyst for the degradation of two most commonly prescribed painkillers, piroxicam (PXM) and paracetamol (PCM), via heterogeneous Fenton process under the solar light. The synthesized ZnFe2O4 NPs showed a narrower band gap i.e. 1.87 eV, signifying the ability to efficiently work in visible light range. In context of photocatalytic applications, the operational conditions were optimized to achieve maximum degradation. PCM and PXM were completely degraded (100%) at the optimized photocatalytic dose (20 mg L−1), reaction time (180 min), initial drug concentration (10 mg L−1), and pH (6.0), which is close to the natural environment. The extent of mineralization as estimated by the reduction of total organic carbon (TOC) was observed to be ∼91 and 82% for PCM and PXM respectively. Kinetic studies revealed that photocatalytic degradation followed pseudo-first-order kinetics. Moreover, the ZnFe2O4 NPs retained ∼90 % of photocatalytic activity after five consecutive reaction cycles, showing remarkable reusability and stability of catalyst.
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•ZnFe2O4 NPs synthesized via co-precipitation showed remarkable photocatalytic activity under solar light.•Complete removal of Paracetamol and Piroxicam with 91% and 82% mineralization by heterogeneous photocatalysis-Fenton system.•Kinetic studies for the solar light driven degradation of Paracetamol and Piroxicam.•High retention of catalytic activity after five consecutive cycles presenting the outstanding stability and reusability.
Highlights • There is a wide variation in the sales of OTC medicines containing codeine across the European Union. • All countries selling OTC codeine medicines impose a level of restriction but ...these vary substantially. • The relative merits of the regimes offered to prevent adverse effects including codeine misuse and dependence remain unknown.
Usage des antalgiques et antipyrétiques Menuey, A.; Corrard, F.; Cohen, R.
Journal de pédiatrie et de puériculture,
April 2021, 2021-04-00, Letnik:
34, Številka:
2
Journal Article
Recenzirano
Historiquement, quand les vaccins étaient moins purifiés, moins bien tolérés, il était classique d’administrer des antipyrétiques pour prévenir la fièvre induite par les vaccins (exemple les vaccins ...coquelucheux entiers ou grippaux entiers). Avec les vaccins récents le risque de réactions fébriles a beaucoup diminué et il a été démontré que pour certains d’entre eux l’administration précoce de paracétamol est susceptible de réduire la réponse anticorps. Maintenant, les médecins et beaucoup de parents savent que ce n’est pas contre l’importance de la fièvre qu’il faut lutter mais contre les douleurs, les désagréments qui l’accompagnent (comportement malade) et qu’il n’y a pas de corrélation entre la hauteur de la température et le confort de l’enfant (Corrard et al. 2017). Enfin, différentes études montrent qu’il n’y a pas non plus de corrélation entre la hauteur de la fièvre et le risque de convulsions fébriles (Smith et al. 2019) et pas d’effet de l’administration du paracétamol sur la survenue de cet événement. Aujourd’hui, l’administration prophylactique de paracétamol est nécessaire pour le Bexsero® et peut être envisagée dans certaines conditions, pour les enfants ayant des antécédents de convulsions fébriles.
Historically, when vaccines were less purified, less tolerated, it was traditional to administer antipyretics to prevent vaccine-induced fever (e.g., whole pertussis or whole influenza vaccines). With recent vaccines, the risk of febrile reactions has been greatly reduced and it has been shown that for some vaccines, early administration of paracetamol may reduce the antibody response. Now, doctors and many parents now know that it is not against the importance of the fever that paracetamol should be used to fight it, but against the pain, the inconveniences that accompany it (sick behaviour) and that there is no correlation between the height of the temperature and the comfort of the child. Finally, various studies show that there is also no correlation between the height of the fever and the risk of febrile convulsions and no effect of paracetamol administration on the occurrence of this event. Today, prophylactic administration of paracetamol is necessary for Bexsero® and may be considered for children with a history of febrile seizures.
Paracetamol, an emerging contaminant, in low concentration (ng/L to mg/L), is discharged as a pharmaceutical residue from wastewater plants into water bodies, endangering flora, fauna, and human ...health through bioaccumulation. Various adsorbents like titania (S1), silica (S2), titania and silica clay composites (S3 and S4) and montmorillonite K10, (S5) were tried for paracetamol uptake in a model wastewater system. All adsorbents were prepared by a sol-gel route at room temperature and were characterized by Fourier Transform Infra-Red, X-ray diffractometer, Scanning Electron Microscope, and Brunauer-Emmett Teller for the nature of functional groups, structure, and specific surface area. The silica clay composite (S4) showed a mesoporous network with an average pore diameter of 3.5 nm, leading to 74% removal of PCT in fifteen minutes of batch adsorption run time. A pseudo second order kinetic model was found fit for S4 with no formation of PCT metabolite as residue as observed from UV spectra. The maximum adsorption capacity of S4 was 1.86 mg/g of the silica clay composite material.
•Synthesis of benign mesoporous silica clay composite for the removal of paracetamol.•Synthesis route is economical and less energy consuming that can be easily escalated to industrial application.•Pseudo second order kinetics was proposed for the adsorption process.•PCT metabolite, if formed was adsorbed by the silica clay composite adsorbent.•Adsorptive capacity of silica clay composite was found to be 1.9 mg/g of the adsorbent material.
Aims
Paracetamol is commonly consumed by pregnant women, even though recent data have questioned its safety. Having chronic medical diseases (CMDs) may influence the prevalence of use during ...pregnancy. We aimed to assess the prevalence and patterns of use 3 months prior to pregnancy and in the first trimester among women with and without CMDs and the potential influence of CMDs on frequent use in the first trimester.
Methods
We used patient‐reported data from the Copenhagen Pregnancy Cohort from 1 October 2013 to 23 May 2019 with information on CMDs and paracetamol use. Prevalence and patterns of use were assessed descriptively and by multivariable logistic regression models.
Results
We included 24 019 pregnancies. Use of paracetamol prior to and in early pregnancy was significantly higher among women with CMDs compared to women without (40.7% vs. 35.8% and 9.1% vs. 5.1%, respectively). Women with CMDs were 2.7 times more likely to have a frequent intake compared to women without aOR 2.69 (95% CI 2.05–3.32). Migraine, rheumatoid arthritis and mental disease were associated with a higher use of paracetamol aOR 4.39 (3.20–6.02), aOR 4.32 (2.41–7.72) and aOR 2.74 (1.67–4.49), respectively.
Conclusions
Women with CMDs had a higher paracetamol use before and during pregnancy than women without CMDs. Women with migraine, rheumatoid arthritis and mental disease showed the highest risk of frequent use. This study highlights the importance of discussing pain relief in pregnancy and evaluating the influence of maternal CMDs when assessing adverse effects of paracetamol use during pregnancy.
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