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Pakistan Journal of Medical Sciences 2023To evaluate the clinical efficacy of dydrogesterone combined with non-steroidal anti-inflammatory drugs(NSAIDs) in the treatment of patients with mild endometriosis.
OBJECTIVE
To evaluate the clinical efficacy of dydrogesterone combined with non-steroidal anti-inflammatory drugs(NSAIDs) in the treatment of patients with mild endometriosis.
METHODS
This was a clinical comparative study. Eighty patients with mild endometriosis were recruited at Affiliated Hospital of Hebei University, randomly divided experimental group (n=40) and control group (n=40) from March 2022 to March 2023. Both groups started treatment with dydrogesterone on the 5th day of menstruation. Patients in the control group were treated with dydrogesterone monotherapy, while those in the experimental group were treated with mefenamic acid the basis of the therapy of the control group. The clinical efficacy, differences in the levels of humoral immune indexes, the levels of inflammatory factor and the incidence of adverse drug reactions of the two groups was compared and analyzed.
RESULTS
The efficacy of the experimental group was significantly higher than the control group, with a statistically significant difference(P=0.02). The levels of C3 and C4 in the experimental group after treatment were significantly lower than those in the control group, with a statistically significant difference(P=0.00). After treatment, TNF-a, CRP, IL-6 and other indexes in the experimental group were significantly lower than those in the control group, with statistically significant differences(P=0.00). The incidence of adverse reactions after treatment had no statistically significant difference(P=0.45).
CONCLUSION
Dydrogesterone combined with non-steroidal anti-inflammatory drugs is a safe and effective treatment for patients with endometriosis. It can improve various obvious curative effects, such as marked relief of pain symptoms, reduction of complement and inflammatory factor levels without a significant increase in adverse reactions.
PubMed: 37680832
DOI: 10.12669/pjms.39.5.7138 -
Journal of Integrative Neuroscience Jul 2023Mefenamic acid (MFA), a common analgesic, causes central nervous system (CNS) toxicity at high doses with a proposed activity on the Gamma-aminobutyric acid (GABA)...
BACKGROUND
Mefenamic acid (MFA), a common analgesic, causes central nervous system (CNS) toxicity at high doses with a proposed activity on the Gamma-aminobutyric acid (GABA) system. However, it remains unknown whether flumazenil (FMZ), a GABA type A receptor (GABAAR) antagonist, can reverse MFA toxicity.
METHODS
The behavioral and neurophysiological effects of MFA were investigated in mice with and without FMZ pre-treatment. The elevated zero maze (EZM) and marble burying tests were used to assess anxiety-like behaviors and burying activities, respectively. The standard bar test was used to evaluate catalepsy, while the actophotometer test was used to measure locomotor activity. Seizure intensity was scored, and fatalities were counted.
RESULTS
Without FMZ pre-treatment, MFA induced behavioral and neurophysiological effects in a dose-dependent manner as follows: At a dose of 20 mg/kg, i.p, MFA-treated mice exhibited anxiety-like behaviors, which was determined by a significant increase in the time spent in the closed areas and a significant decrease in the number of entries to the open areas of the EZM apparatus. These mice also showed a significant decrease in the burying activity, manifested as a significant decrease in the number of buried marbles. At 40 mg/kg, i.p., MFA-treated mice showed catalepsy that was associated with a significant decrease in locomotor activity. At a dose of 80 mg/kg, i.p., mice developed fatal tonic-clonic seizures (seizure score = 4). Pre-treatment with FMZ (5 mg/kg, i.p.) significantly reversed the anxiety-like behaviors and restored marble-burying activity. Additionally, FMZ prevented catalepsy, significantly restored locomotor activity, reduced seizure intensity (seizure score = 0.3) and significantly reduced mortalities.
CONCLUSIONS
The present study's findings indicate that activation of the GABAAR is involved in the CNS toxicity of MFA, and FMZ reverses MFA toxicity by interfering with this receptor.
Topics: Mice; Animals; Flumazenil; Mefenamic Acid; Receptors, GABA-A; Catalepsy; Central Nervous System; Seizures; gamma-Aminobutyric Acid; Behavior, Animal
PubMed: 37519168
DOI: 10.31083/j.jin2204104 -
Journal of Public Health in Africa Mar 2023The use of NSAIDs, also known as non-steroidal anti-inflammatory drugs, has numerous adverse effects and consequences. For this reason, it is necessary to develop...
BACKGROUND
The use of NSAIDs, also known as non-steroidal anti-inflammatory drugs, has numerous adverse effects and consequences. For this reason, it is necessary to develop rational drugs as safer anti-inflammatory drugs with fewer side effects. Temu Kunci rhizome contains Pinostrobin (5-hydroxy-7-methoxyflavanone), which is believed to have anti-inflammatory properties.
OBJECTIVE
This study aims to determine the strongest antiinflammatory activity at the cyclooxygenase-2 (COX-2) receptor through the 5-O-Benzoylpinostrobin derivative design. Methods: AutoDockTools on the COX-2 receptor (PDB code: 5IKR) were used in molecular docking in this study. The metrics employed were binding afinity (ΔG), inhibition constant (Ki), which serve as indicators of affinities, and amino acid residue similarity, which serves as a measure of the similarity of interactions. Predictive scores were confirmed by Molecular Docking Simulation.
RESULTS
The top five 5-O-Benzoylpinostrobin derivatives show a high affinity for the COX-2 receptor compared to Pinostrobin as a marker compound of Boesenbergia pandurata Roxb and furthermore give the lowest inhibition constant (Ki) and the highest negative binding free energy (ΔG), 35.40, 45.21, 54.75, 64.43, 76.97 nM and -10.16, -10.02, -9.91, -9.81, -9.7 kcal/mol. Interestingly, the five 5-O-Benzoylpinostrobin derivatives also have higher affinity than the native ligand Mefenamic acid, which is known to be a non-selective COX-2 inhibitor. The highest predicted affinity was shown by 4-Nitro-5-O-benzoylpinostrobin for the COX-2 receptor (PDP ID: 5IKR), with a higher predicted affinity for Mefenamic acid.
CONCLUSION
The five selected 5-O-Benzoylpinostrobin derivatives were potent modifications of pinostrobin as an antiinflammatory because they showed a higher affinity than Pinostrobin and Mefenamic acid. This study demonstrated that it is highly feasible to produce and test the novel 5-OBenzoylpinostrobin derivative , specifically 4-Nitro-5-Obenzoylpinostrobin.
PubMed: 37492536
DOI: 10.4081/jphia.2023.2532 -
International Medical Case Reports... 2023Pain management becomes important in the treatment of oral mucosal diseases since it can impair the quality of life. Photobiomodulation (PBM) as an alternative therapy,...
INTRODUCTION
Pain management becomes important in the treatment of oral mucosal diseases since it can impair the quality of life. Photobiomodulation (PBM) as an alternative therapy, has potency in reducing pain through several mechanisms targeting peripheral nerves in the target tissue.
PURPOSE
To discuss the effectiveness of PBM in the management of four cases of oral mucosal diseases.
CASE
Four patients, two females and two males, with an age ranging from 24 to 63 years came to the Oral Medicine Department complaining of painful lesions in their oral cavity. Three cases showed ulceration of the oral mucosa and had been diagnosed with recurrent aphthous stomatitis, recalcitrant chronic ulcer, and non-specific chronic sialadenitis. One patient who complained of intense pain and swelling on the right side of the face was diagnosed with post-herpetic neuralgia (PHN).
CASE MANAGEMENT
PBM was administered in all four cases (976 nm diode laser, three cases with spot size 0.01 cm, fluency 10 J/cm, and one case with spot size 0.5 cm; fluency 3 J/cm). Visual analog scale (VAS) control was performed before and after the PBM at each visit. The recorded VAS results show a reduction in pain that started at the post-laser time, with VAS before PBM ranging from 5 to 7 and after PBM ranging from 0 to 4. Three patients were given triamcinolone acetonide 0.1%, chlorhexidine gluconate 0.2% mouthwash, petroleum jelly, and multivitamins. One patient was given mefenamic acid and multivitamins.
CONCLUSION
PBM can be a useful adjunctive treatment to relieve the pain of oral mucosal diseases due to its ability to reduce pain intensity.
PubMed: 37465549
DOI: 10.2147/IMCRJ.S414313 -
Membranes Jun 2023The present work analyzes the H NOESY MAS NMR spectra of three fenamates (mefenamic, tolfenamic, and flufenamic acids) localized in the lipid-water interface of...
The present work analyzes the H NOESY MAS NMR spectra of three fenamates (mefenamic, tolfenamic, and flufenamic acids) localized in the lipid-water interface of phosphatidyloleoylphosphatidylcholine (POPC) membranes. The observed cross-peaks in the two-dimensional NMR spectra characterized intramolecular proximities between the hydrogen atoms of the fenamates as well as intermolecular interactions between the fenamates and POPC molecules. The peak amplitude normalization for an improved cross-relaxation (PANIC) approach, the isolated spin-pair approximation (ISPA) model, and the two-position exchange model were used to calculate the interproton distances indicative of specific conformations of the fenamates. The results showed that the proportions of the A+C and B+D conformer groups of mefenamic and tolfenamic acids in the presence of POPC were comparable within the experimental error and amounted to 47.8%/52.2% and 47.7%/52.3%, respectively. In contrast, these proportions for the flufenamic acid conformers differed and amounted to 56.6%/43.4%. This allowed us to conclude that when they bind to the POPC model lipid membrane, fenamate molecules change their conformational equilibria.
PubMed: 37367811
DOI: 10.3390/membranes13060607 -
Water, Air, and Soil Pollution 2023Due to the COVID-19 epidemic, the consumption of pharmaceuticals, especially paracetamol, has sharply increased on a global scale. The increasing concentration of...
UNLABELLED
Due to the COVID-19 epidemic, the consumption of pharmaceuticals, especially paracetamol, has sharply increased on a global scale. The increasing concentration of analgesic and anti-inflammatory drugs (AAIDs) in the aquatic medium is a global problem for human and aquatic life. Therefore, simple and effective treatment options for removing AAIDs from wastewater after the COVID-19 pandemic are needed. The removal of AAIDs (acetaminophen, acetylsalicylic acid, codeine, diclofenac, ibuprofen, indomethacin, ketoprofen, mefenamic acid, naproxen, and phenylbutazone) from sewage treatment plant (STP) effluents by the prepared magnetite nanoparticles synthesized from red mud (mNPs-RM) is presented for the first time in this study. The removal efficiencies of AAIDs onto mNPs-RM were determined to be between 90% (diclofenac) and 100% (naproxen, codeine, and indomethacin). Acetaminophen (paracetamol) was used as a model compound in kinetic and isotherm model studies. The adsorption of acetaminophen was matched well with the pseudo second order kinetic model. Film diffusion governed its rate mechanism. The Freundlich isotherm model preferably fitted the adsorption data with an adsorption capacity of 370 mg/g at 120 min contact time at pH 7.0 at 25 °C. Furthermore, the regenerated mNPs-RM were used four times without affecting the adsorption capacity and the magnetic separability. mNPs-RM can be used as a simple, inexpensive and effective adsorbent for removing AAIDs from STP effluents. Also, low cost adsorbent obtained from industrial waste could be employed to replace the high cost activated carbons for the adsorption of other micro pollutants in STP effluents.
SUPPLEMENTARY INFORMATION
The online version contains supplementary material available at 10.1007/s11270-023-06404-7.
PubMed: 37323133
DOI: 10.1007/s11270-023-06404-7 -
Applied Water Science 2023The consumption of pharmaceuticals has rapidly increased on a global scale due to the serious increase in Covid-19, influenza and respiratuar sinsityal virus, which is...
UNLABELLED
The consumption of pharmaceuticals has rapidly increased on a global scale due to the serious increase in Covid-19, influenza and respiratuar sinsityal virus, which is called "triple epidemic" in the world. The use of non-prescription analgesic and anti-inflammatory drugs (AAIDs), especially paracetamol, is higher compared to pre-pandemic. This increased the AAIDs load discharged to the aqueous media through sewerage treatment plant (STP). Therefore, simple and effective treatment options for removing AAIDs from STP effluents are needed. The aim of the study was to remove AAIDs (paracetamol, acetylsalicylic acid, codeine, diclofenac, ibuprofen, indomethacin, ketoprofen, mefenamic acid, naproxen, and phenylbutazone) from STP effluents by nearly pure natural clay Na-montmorillonite. The Na-montmorillonite taken from the Ordu region in the northern part of Turkey. Surface area of the Na-montmorillonite is 99.58 m/g and CEC is 92.40 meq/100 g. The removal efficiencies of AAIDs using Na-montmorillonite were between 82 ± 5% (ibuprofen) and 94 ± 4% (naproxen). Paracetamol was used as a model compound in kinetic and isotherm model studies. Freundlich isotherm model and the pseudo second order kinetic model were the best-fit using the obtained experimental data. Film diffusion governed its rate mechanism. The paracetamol adsorption capacity was acquired as 244 mg/g at 120 min contact time at pH 6.5 at 25 °C. With this study, it could be shown that montmorillonite can be used effectively to eliminate paracetamol from STP effluent. Natural clay can be used as a simple, inexpensive and effective adsorbent for removing AAIDs from STP effluents.
SUPPLEMENTARY INFORMATION
The online version contains supplementary material available at 10.1007/s13201-023-01930-5.
PubMed: 37192959
DOI: 10.1007/s13201-023-01930-5 -
Turkish Journal of Pharmaceutical... May 2023Mefenamic acid (MA) is a strong non-steroidal anti-inflammatory drug, but because of its limited oral bioavailability and the side effects that come with taking it...
OBJECTIVES
Mefenamic acid (MA) is a strong non-steroidal anti-inflammatory drug, but because of its limited oral bioavailability and the side effects that come with taking it systemically, it is better to apply it topically. The major goal of this study was to see how certain permeation enhancers affected MA is skin permeability. In manufactured Franz diffusion cells, MA permeability tests using rat skin pretreatment with several permeation enhancers such as corn oil, olive oil, clove oil, eucalyptus oil, and menthol were conducted and compared to hydrate rat skin as a control.
MATERIALS AND METHODS
The steady-state flux (Jss), permeability coefficient (Kp), and diffusion coefficient are among the permeability metrics studied. The permeability enhancement mechanisms of the penetration enhancer were investigated using fourier transform infrared spectroscopy (FTIR) to compare changes in peak position and intensities of asymmetric and symmetric C-H stretching, C=O stretching, C=O stretching (amide I), and C-N stretching of keratin (amide II) absorbance, as well as differential scanning calorimetry (DSC) to compare mean transition temperature and their enthalpies.
RESULTS
Clove oil, olive oil, and eucalyptus oil were the most effective enhancers, increasing flux by 7.91, 3.32, and 2.6 times, as well as diffusion coefficient by 3.25, 1.34, and 1.25, respectively, when compared to moist skin. FTIR and DSC data show that permeation enhancers caused lipid fluidization, extraction, disruption of lipid structures in the SC layer of skin, and long-term dehydration of proteins in this area of the skin.
CONCLUSION
According to the findings, the permeation enhancers used improved drug permeability through excised rat skin. The most plausible mechanisms for greater ERflux, ERD, and ERP ratios were lipid fluidization, disruption of the lipid structure, and intracellular keratin irreversible denaturation in the SC by eucalyptus oil, menthol, corn oil, olive oil, and clove oil.
PubMed: 37161659
DOI: 10.4274/tjps.galenos.2022.60669 -
International Journal of Molecular... Apr 2023This study examines the influence of mefenamic acid on the physical and chemical properties of silica aerogels, as well as its effect on the sorption characteristics of...
This study examines the influence of mefenamic acid on the physical and chemical properties of silica aerogels, as well as its effect on the sorption characteristics of the composite material. Solid state magic angle spinning nuclear magnetic resonance (MAS NMR) and high-pressure C NMR kinetic studies were conducted to identify the presence of mefenamic acid and measure the kinetic rates of CO sorption. Additionally, a high-pressure T-T relaxation-relaxation correlation spectroscopy (RRCOSY) study was conducted to estimate the relative amount of mefenamic acid in the aerogel's pores, and a high-pressure nuclear Overhauser effect spectoscopy (NOESY) study was conducted to investigate the conformational preference of mefenamic acid released from the aerogel. The results indicate that mefenamic acid is affected by the chemical environment of the aerogel, altering the ratio of mefenamic acid conformers from 75% to 25% in its absence to 22% to 78% in the presence of aerogel.
Topics: Mefenamic Acid; Kinetics; Silicon Dioxide; Magnetic Resonance Spectroscopy; Magnetic Resonance Imaging
PubMed: 37108046
DOI: 10.3390/ijms24086882 -
The British Journal of General Practice... Apr 2023Heavy menstrual bleeding (HMB) is common and can affect women's lives. Evidence on women's experiences and their treatment of this problem after seeking primary care is...
BACKGROUND
Heavy menstrual bleeding (HMB) is common and can affect women's lives. Evidence on women's experiences and their treatment of this problem after seeking primary care is lacking.
AIM
To explore women's experiences of HMB and their medical treatment up to 10 years after initial management in general practice.
DESIGN AND SETTING
This was a qualitative study in UK primary care.
METHOD
Semistructured interviews with a purposeful sample of 36 women who had participated in the ECLIPSE trial of medical treatments for HMB in primary care (levonorgestrel-releasing intrauterine system or other usual medical treatments - oral tranexamic acid, mefenamic acid, combined oestrogen-progestogen; or progesterone alone). Data were analysed thematically and a process of respondent validation was undertaken.
RESULTS
Women reported the wide-ranging and debilitating impact of HMB on their lives. They had often normalised their experience underlining persisting societal taboos about menstruation and reflecting low general awareness of HMB as treatable. Women commonly delayed seeking help for several years. They could then be frustrated by lack of a medical explanation for HMB. Women who had pathology identified felt able to make better sense of their HMB. Experiences of medical treatments varied considerably but were strongly influenced by the perceived quality of healthcare interactions with clinicians. Other influences on women's treatment included considerations for their fertility, health concerns, family and peers, and views when approaching menopause.
CONCLUSION
Clinicians should be aware of the considerable challenges faced by women with HMB; widely differing experiences of, and influences on, their treatment; and the value of patient-centred communication in this context.
Topics: Female; Humans; Intrauterine Devices, Medicated; Levonorgestrel; Menorrhagia; Primary Health Care; Progesterone; Qualitative Research
PubMed: 36997220
DOI: 10.3399/BJGP.2022.0460