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Therapeutic Efficacy of Black Pepper in Gastrointestinal Disorders
Published in Megh R. Goyal, Preeti Birwal, Durgesh Nandini Chauhan, Herbs, Spices, and Medicinal Plants for Human Gastrointestinal Disorders, 2023
In this respect, by enhancing absorption, piperine improves oral bioavailability of carbamazepine and phenytoin.47 The piperine (@ 20 mg) shows synergistic effect inthepresence ofphenytoin.48 Thecoadministration of coenzyme Q10 with piperine has proven to be statistically significant (P = 0.0348; 30%) superior plasma AUC in comparison with the standard coenzyme Q10.8 Studies reported that piperine remarkably increases the oral manifestation of fexofenadine in rats by blocking P-gp-mediated cellular efflux during absorption in intestine.36 Similarly, piperine has improved the bioavailability of nimesulide. Intense mice toxicological reports showed a decrease in the lethal dose (LD50) of the combination relative to nimesulide alone.24
The diagnosis and management of preterm labor with intact membranes
Published in Hung N. Winn, Frank A. Chervenak, Roberto Romero, Clinical Maternal-Fetal Medicine Online, 2021
Roberto Romero, Tinnakorn Chaiworapongsa, Francesca Gotsch, Lami Yeo, Ichchha Madan, Sonia S. Hassan
Prostaglandins are considered the universal mediators of labor and can induce uterine contractility and cervical ripening. The therapeutic target is the cyclooxygenase (COX) enzyme, which catalyzes the conversion of arachidonic acid to the intermediate product of prostaglandins, PGH. There are two COX enzymes, COX-1 and COX-2. The former is the constitutive enzyme, and the second is the inducible enzyme. Indomethacin is a non-specific inhibitor of COX, while nimesulide is a specific inhibitor of COX-2. One of the randomized clinical trials in which indomethacin was compared with placebo concluded that indomethacin resulted in a reduction in the rate of preterm birth (defined as <37 gestational weeks) (328,329). However, this trial included only 36 women, and there was no difference in neonatal outcome. Comparative trials (with either beta-adrenergic agents or magnesium sulfate) show that COX inhibitors reduced the rate of preterm birth before 37 weeks and the frequency of adverse events (329). However, there was no demonstrable improvement in neonatal outcome. Two studies comparing non-selected COX inhibitors versus COX-2 inhibitors did not demonstrate differences in maternal and neonatal outcome (329–331). It is recognized that the trials have been of small sample size.
Medicines in neonates
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Non-selective NSAIDs, such as both indomethacin and ibuprofen, have been used in neonates. They reversibly inhibit the enzymatic activity of both COX-1 and COX-2 [1,20]. Nimesulide, a Cox-2 selective inhibitor, is not recommended in the perinatal period owing to its toxicity [21–23]. Keeping in mind the above information on the crucial action of prostanoids on the perinatal kidney, especially those products synthesised from the over-expressed COX-2 at this time, it is evident that all these drugs administered during the last trimester of the pregnancy or during the first postnatal days may effect this organ in different ways, depending on the volume and salt-depleted state. Their use is therefore only recommended in some very restrictive well-balanced clinical conditions in term of risk/benefit ratio.
SLN and NLC for topical, dermal, and transdermal drug delivery
Published in Expert Opinion on Drug Delivery, 2020
Eliana B. Souto, Iara Baldim, Wanderley P. Oliveira, Rekha Rao, Nitesh Yadav, Francisco M. Gama, Sheefali Mahant
Moghddam et al. developed a nimesulide NLC for topical delivery [210], optimized through Box-Behnken design. Selecting the ratio of stearic to oleic acids and the concentrations of Poloxamer 188 and lecithin as independent variables, the particle size, and encapsulation efficiency (the dependent variables) were optimized. Additionally, skin permeation assay, in vitro release, confocal laser scanning microscopy (CLSM) and stability evaluation were performed. The optimized nimesulide NLC demonstrated reasonable encapsulation efficiency, particle size, and skin permeation. The results of preliminary studies displayed delayed drug release for the optimized batch, following a Higuchi release kinetics. CLSM revealed an improved penetration of Rhodamine loaded NLC to deeper skin layers. The findings of this study revealed NLC as a potential carrier for the topical application of nimesulide.
An update of cyclooxygenase (COX)-inhibitors in epilepsy disorders
Published in Expert Opinion on Investigational Drugs, 2019
In a mouse PTZ (50 mg/kg, IP) seizure test carried by Temp and colleagues, nimesulide (20 mg/kg, PO) was the only COX-2 inhibitor that displayed the anticonvulsant effect by attenuating seizures [69]. Nimesulide at 20 but not 0.2 and 2 mg/kg increased the latency to the first myoclonic jerk and generalized tonic-clonic seizures. Furthermore, the moleucle was effective inreducing the Racine seizure score. Celecoxib (0.2–20 mg/kg, PO) or etoricoxib (0.2–20 mg/kg, PO) did not affect any seizure phase caused by PTZ. Celecoxib was effective in reducing pro-inflammatory cytokines in the cerebral cortex and hippocampal regions of the mouse brain that were induced by PTZ [69]. In contrast, etoricoxib, another COX-2 inhibitor, did not affect cytokine levels [69]. The exact mechanism of the anticonvulsant effect of nimesulide in this study is unknown. The anticonvulsant effect of nimesulide may be associated with its ability to increase the level of anti-inflammatory cytokine, interleukin-10 (IL-10) [69]. It can be concluded from this study that not all COX-2 inhibitors maintain similar activity in this seizure model. It is possible that the antiseizure effect of these drugs is not class-dependent but drug-dependent.
Topical therapies for knee osteoarthritis
Published in Postgraduate Medicine, 2018
A study showed that topical nimesulide gel can have beneficial consequences and can ameliorate quality of life in patients with knee OA [10]. Seventy-four adult knee OA outpatients were enrolled in a double-blind, randomized, placebo-controlled study. Treatment group received topical nimesulide gel 1% on the knee skin three times a day, whereas placebo group received an identical-appearing gel for 30 days. There was a significant improvement in the nimesulide treatment group for all parameters studied. The overall Western Ontario and McMaster Universities OA (WOMAC) scores was significantly better than placebo, but physical functioning, stiffness, and pain scales did not reach statistical significance. For the Nottingham Health Profile (NHP) scores, there was an improvement at ‘energy level,’ ‘pain,’ ‘physical motion,’ and ‘NHP distress’ scores in the treatment group, whereas no improvement was found in the placebo group. Between-group differences were not significant. Both patient and physician satisfaction scores were significantly better in the treatment group.