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Analgesics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Limited data are available on the pharmacokinetics of analgesics during pregnancy, and the findings are not entirely consistent. For example, acetaminophen has a decreased half-life and increased clearance in one study, but it is unchanged in another at about the same gestational age (Table 8.1). The pharmacokinetics of meperidine in pregnancy are unchanged compared to non-pregnant controls, and the same is true of the kinetics of meptazinol. In contrast, morphine has a decreased half-life and increased clearance, implying the need for increased frequency or dose regimen to maintain adequate analgesia. Indomethacin has a decreased half-life, and Cmax, which also implies dose or frequency regimen adjustment. In contrast, sodium salicylate has an increased half-life during late pregnancy. Low-dose aspirin apparently does not significantly affect umbilical artery circulation (Owen et al., 1993; Veille et al., 1993). Notably, the half-life for aspirin increases during pregnancy, implying that a dose decrease in amount and/or frequency may be needed (Table 8.1).
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
A 47-year-old man, with osteochondrosis dissecans of the right talotibial joint, received local treatment with a gel containing hydroxyethyl (glycol) salicylate. After 2 weeks, he developed acute contact dermatitis at the site of application. Eight months later, after an arthroscopy of the same joint, the gel was again applied and, over the next 24 hours, he developed acute contact dermatitis once more. Patch tests were positive to the gel ‘as is’ and to glycol salicylate 0.1%, 0.5%, 1%, 2%, 5% and 10% pet. Patch tests with acetylsalicylic acid and sodium salicylate were negative. Orally administered acetylsalicylic acid in a cumulative dose of 1000 mg and sodium salicylate 500 mg were well-tolerated (4).
Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
In an effort to throw some light on the contribution of the prostaglandin or eicosanoid system to the effect of ASA, sodium salicylate was tested in a way similar to ASA (Figure 6). It became evident that the salicylate was effective in all tests of the battery and the differences with respect to ASA were only quantitative. Even in the endothelial stability test, a significant positive effect was observed amounting to about 80% inhibition. The effective dose was, in general, 4 to 5 times higher than in the case of ASA with a somewhat larger difference in the arterial in comparison with the venous model. Both are, of course, acute models and any speculations regarding the effect on coagulation factor synthesis in the liver would be out of place.
Mechanism of Elian granules in the treatment of precancerous lesions of gastric cancer in rats through the MAPK signalling pathway based on network pharmacology
Published in Pharmaceutical Biology, 2022
Zhirong Yi, Qingling Jia, Yili Lin, Yujiao Wang, Jun Cong, Zhijian Gu, Jianghong Ling, Gan Cai
After 9 SPF male SD rats were fed a normal diet for one week, the rats were randomly divided into the normal, model, and Elian granules groups. The normal group was given SPF diet and clean drinking water. The model and Elian granules groups were used to produce the PLGC rat model via the MNNG comprehensive method. Briefly, (1) Rats were treated with the MNNG solution at 170 μg/mL via drinking. The MNNG water bottle was wrapped in tin foil to protect it from light. (2) Granular SPF rat feed containing 0.03% ranitidine hydrochloride was used for feeding. (3) The animals were fed for 2 days and then fasted for 1 day. (4) Intragastric administration of 2% sodium salicylate solution was performed in the afternoon of fasting at 10 mL/kg/d. In parallel, the model group was given normal saline intragastric administration (10 mL/kg/d) for 24 weeks. Intragastric administration of Elian granule aqueous solution (3.24 g/kg/d) was administered to the Elian granules group as an intervention for 24 weeks.
Anti-inflammatory effects of troxerutin are mediated through elastase inhibition
Published in Immunopharmacology and Immunotoxicology, 2020
Ramachandran Vidhya, Carani Venkatraman Anuradha
Troxerutin (TX), a derivative of bioflavonoid rutin has anti-obesity effect. TX is abundantly present in flower buds of Sophora japonica, tea, coffee, cereal grains and in a wide variety of fruits and vegetables [11]. Literature search reveals that TX also has antioxidant [12], anti-inflammatory [13], anti-diabetic [14] and anti-cancer properties [15]. Previous studies show that TX attenuates diet-induced oxidative stress and lipid changes in the heart of high-fat, high-fructose diet-fed mice [16]. We hypothesize that the anti-inflammatory properties of TX are mediated through inhibition of elastase. To verify this hypothesis, we investigated the effect of TX on elastase activity and the expression of adipokines in 3T3-L1 adipocytes treated with TNFα, an obesity-associated inflammatory cytokine. Elastatinal (ELAS), an elastase inhibitor [17] and sodium salicylate (SAL), a non-steroidal anti-inflammatory drug [18] were included in the study for comparison. The elastase inhibitory potential of TX was assessed by in vitro enzyme assay. Molecular docking analysis of HNE crystal structure (PDB ID: 3Q76) with TX and ELAS was done using Schrödinger maestro suite of Glide [19] for comparing the binding properties.
Growth differentiation factor 15 and its role in carcinogenesis: an update
Published in Growth Factors, 2019
Anupama Modi, Shailender Dwivedi, Dipayan Roy, Manoj Khokhar, Purvi Purohit, Jeewanram Vishnoi, Puneet Pareek, Shailja Sharma, Praveen Sharma, Sanjeev Misra
Studies on GDF-15 in lung cancer, albeit few, demonstrate its apoptotic effect. A study reports that apoptotic effects of sodium salicylate in A549 cells was seen to be mediated by GDF-15, also combined treatment of sodium salicylate and inhibitor of the PI3K-Akt-PKB and ERK1/2 pathways induced apoptosis in A549 cells (Kim et al. 2008). Additionally, salinomycin impeded invasiveness of LNM35 and A549 cells in a concentration-dependent manner which was mediated by GDF-15 (Arafat et al. 2013). In urethane-induced mice models, Cekanova et al. 2009, revealed that GDF-15 induces apoptosis through the activation of caspase 3/7 (Cekanova et al. 2009). They also showed its anti-tumorigenic properties through downregulation of the p38-MAPK signaling pathway (Cekanova et al. 2009). Thus, the apoptotic effect of GDF-15 further enhances its claim as an effective tumor marker in lung cancer.