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Psychiatry Research Sep 2019People with schizophrenia and medical comorbidities are often on multiple medications to manage their symptoms. Herein we present a case of drug-drug interaction...
BACKGROUND
People with schizophrenia and medical comorbidities are often on multiple medications to manage their symptoms. Herein we present a case of drug-drug interaction (meloxicam and desmopressin), in a patient also on clozapine, that ultimately resulted in hyponatremia and seizure.
METHODS
The patient provided consent to have his case published. We searched PubMed and after reviewing 321 articles, 11 were chosen for relevance.
RESULTS
Meloxicam enhanced the adverse effect (hyponatremia) of desmopressin and was the likely culprit.
CONCLUSIONS
In a patient with higher ADH levels, as in our patient taking desmopressin, the addition of an NSAID could further increase water retention and worsen hyponatremia; indeed, meloxicam was the only new medication added to the patient's regimen, and a drug interaction calculator supports the desmopressin-meloxicam drug-drug interaction as the culprit. We urge clinicians to avoid the use of desmopressin in patients with schizophrenia as this can lead to water intoxication. As meloxicam may worsen desmopressin-induced hyponatremia and could result in seizure, one should avoid using NSAIDs in patients with schizophrenia whom are also prescribed vasopressin/desmopressin. Serum sodium levels should be closely monitored in patients with schizophrenia whose regimen includes desmopressin.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Antidiuretic Agents; Deamino Arginine Vasopressin; Drug Interactions; Drug-Related Side Effects and Adverse Reactions; Humans; Hyponatremia; Male; Meloxicam; Middle Aged
PubMed: 31084937
DOI: 10.1016/j.psychres.2019.05.009 -
Veterinary Medicine and Science Sep 2023Fish in aquatic environments are end consumers of the food chain and are widely used for the evolution effects of environmental pollution and their interactions in...
BACKGROUND
Fish in aquatic environments are end consumers of the food chain and are widely used for the evolution effects of environmental pollution and their interactions in aquatic ecosystem.
OBJECTIVE
In the present study, common carp (Cyprinus carpio) fingerlings were selected to assess the potential risk and aquatic toxicity of meloxicam as a non-steroidal anti-inflammatory and a commonly used pharmaceutical drug.
METHODS
In order to evaluate meloxicam toxicological effect on haematological, antioxidant status, enzymological and histological parameters, based on its LC50 24 h acute toxicity (10.05 mg L ), fish fingerlings were exposed to four doses of meloxicam including; 0 (control), 0.1 (low), 1 (medium) and 2 mg L (high) under static bioassay method for 28 days.
RESULTS
The results showed that sublethal doses of meloxicam significantly decreased alanine aminotransferase, alkaline phosphatase, superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) levels in comparison with the control group after 28 days (p < 0.05). However, red blood cell, haematocrit, haemoglobin and malondialdehyde values in fish exposed to meloxicam significantly increased alongside its concentration (p < 0.05) more than the control group after 28 days. SOD, CAT and GPX mRNA expression levels in gill, liver, kidney and brain organ of fish under meloxicam treatment were significantly down-regulated compared to the control group (p < 0.05). Histopathological assessment showed the increased vacuolation in hepatocytes in liver of fish exposure to medium and high doses of meloxicam.
CONCLUSION
In conclusion, meloxicam induces oxidative stress in common carp which results a disruption of physiological and health status of this species based on our current findings.
Topics: Animals; Antioxidants; Meloxicam; Carps; Ecosystem; Anti-Inflammatory Agents, Non-Steroidal; Glutathione Peroxidase
PubMed: 37616188
DOI: 10.1002/vms3.1207 -
Biochemical Pharmacology May 2020ATP-binding cassette (ABCG2) is an efflux transporter that extrudes xenotoxins from cells in liver, intestine, mammary gland, brain and other organs, affecting the...
ATP-binding cassette (ABCG2) is an efflux transporter that extrudes xenotoxins from cells in liver, intestine, mammary gland, brain and other organs, affecting the pharmacokinetics, brain accumulation and secretion into milk of several compounds, including antitumoral, antimicrobial and anti-inflammatory drugs. The aim of this study was to investigate whether the widely used anti-inflammatory drug meloxicam is an Abcg2 sustrate, and how this transporter affects its systemic distribution. Using polarized ABCG2-transduced cell lines, we found that meloxicam is efficiently transported by murine Abcg2 and human ABCG2. After oral administration of meloxicam, the area under the plasma concentration-time curve in Abcg2 mice was 2-fold higher than in wild type mice (146.06 ± 10.57 µg·h/ml versus 73.80 ± 10.00 µg·h/ml). Differences in meloxicam distribution were reported for several tissues after oral and intravenous administration, with a 20-fold higher concentration in the brain of Abcg2 after oral administration. Meloxicam secretion into milk was also affected by the transporter, with a 2-fold higher milk-to-plasma ratio in wild-type compared with Abcg2 lactating female mice after oral and intravenous administration. We conclude that Abcg2 is an important determinant of the plasma and brain distribution of meloxicam and is clearly involved in its secretion into milk.
Topics: ATP Binding Cassette Transporter, Subfamily G, Member 2; Administration, Intravenous; Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Dogs; Female; Humans; Madin Darby Canine Kidney Cells; Male; Meloxicam; Mice; Mice, Knockout; Milk; Tissue Distribution
PubMed: 32217099
DOI: 10.1016/j.bcp.2020.113924 -
Blood Coagulation & Fibrinolysis : An... Dec 2014Acetaminophen (Ace) and meloxicam (Mel) are the two types of analgesic and antipyretic medications. This study investigated the dose responses of acetaminophen and...
Acetaminophen (Ace) and meloxicam (Mel) are the two types of analgesic and antipyretic medications. This study investigated the dose responses of acetaminophen and meloxicam on platelet aggregation and coagulation function in human blood samples. Blood samples were collected from six healthy humans and processed to make platelet-adjusted (100 × 10 cells/μl) blood samples. Acetaminophen (Tylenol, Q-PAP, 100 mg/ml) was added at the doses of 0 μg/ml (control), 214 μg/ml (the standard dose, 1 ×), 4 ×, 8 ×, 10 ×, 12 ×, 16 ×, and 20 ×. Similarly, meloxicam (Metacam, 5 mg/ml) was added at doses of 0 μg/ml (control), 2.85 μg/ml (the standard dose, 1 ×), 4 ×, 8 ×, 10 ×, 12 ×, 16 ×, and 20 ×. Fifteen minutes after the addition of acetaminophen and/or meloxicam, platelet aggregation was stimulated with collagen (2 μg/ml) or arachidonic acid (0.5 mmol/l) and assessed using a Chrono-Log 700 aggregometer. Coagulation function was assessed by prothrombin time (PT), activated partial thromboplastin time (aPTT), and using Rotem thrombelastogram. A robust inhibition by acetaminophen and/or meloxicam was observed in arachidonic acid-stimulated platelet aggregation starting at 1 × dose. Collagen-stimulated platelet aggregation was inhibited by ACE starting at 1 × (78 ± 10% of control), and by meloxicam starting at 4 × (72 ± 5% of control, both P < 0.05). The inhibitions by acetaminophen and meloxicam combined were similar to those by acetaminophen or meloxicam. aPTT was prolonged by meloxicam starting at 4 ×. No changes were observed in PT or any of Rotem measurements by acetaminophen and/or meloxicam. Acetaminophen and meloxicam compromised platelet aggregation and aPTT. Further effort is warranted to characterize the effects of acetaminophen and meloxicam on bleeding in vivo.
Topics: Acetaminophen; Arachidonic Acid; Blood Cells; Blood Coagulation; Blood Specimen Collection; Cells, Cultured; Collagen; Dose-Response Relationship, Drug; Humans; Meloxicam; Partial Thromboplastin Time; Platelet Aggregation; Prothrombin Time; Thiazines; Thiazoles; Thrombelastography
PubMed: 25004022
DOI: 10.1097/MBC.0000000000000162 -
Journal of Veterinary Pharmacology and... Mar 2022The pharmacokinetics and bioavailability of meloxicam were investigated after single intravascular (IV), intramuscular (IM), and oral dose of 1 mg/kg in rainbow trout...
The pharmacokinetics and bioavailability of meloxicam were investigated after single intravascular (IV), intramuscular (IM), and oral dose of 1 mg/kg in rainbow trout broodstock at 11 ± 1.2°C. A total of 36 healthy rainbow trout (Oncorhynchus mykiss) broodstock weighing 1.40 ± 0.26 kg was used for the investigation. Plasma concentrations of meloxicam were measured with high-performance liquid chromatography-ultraviolet detection, and pharmacokinetic parameters were calculated by non-compartmental analysis. The elimination half-life for IV, IM, and oral routes was 3.63, 4.55, and 2.95 h, respectively. The IV route for meloxicam showed the total clearance of 0.05 L/h/kg and volume of distribution at a steady state of 0.20 L/kg. The peak plasma concentration was 2.97 μg/ml for the IM route and 0.84 μg/ml for the oral route. The bioavailability was 78.45% for the IM route and 21.48% for the oral route. Meloxicam following IM and oral administration displayed short t . The short t could be an advantage for the short-term use in acute conditions. The IM route with the good bioavailability can be preferred for the treatment of various conditions. However, developing new oral formulations with the good bioavailability for meloxicam is necessary to minimize stress and trauma through minimal handling in rainbow trout broodstock.
Topics: Administration, Oral; Animals; Biological Availability; Half-Life; Injections, Intramuscular; Meloxicam; Oncorhynchus mykiss
PubMed: 34778976
DOI: 10.1111/jvp.13031 -
Drug Design, Development and Therapy 2021This study aimed to formulate an orally disintegrating tablet (ODT) containing both baclofen and meloxicam together for treating osteoarthritis. (Comparative Study)
Comparative Study
Formulation and Evaluation of Baclofen-Meloxicam Orally Disintegrating Tablets (ODTs) Using Co-Processed Excipients and Improvement of ODTs Performance Using Six Sigma Method.
PURPOSE
This study aimed to formulate an orally disintegrating tablet (ODT) containing both baclofen and meloxicam together for treating osteoarthritis.
METHODS
Direct compression method was used to prepare ODTs using three types of co-processed excipients (Prosolv ODT G2, F-melt, and Pharmaburst500). ODTs were evaluated according to weight variation, thickness, friability, hardness, drug content, wetting time, in-vitro disintegration time, in-vitro dissolution test, and palatability. To enhance the in-vitro dissolution of meloxicam and palatability of ODT, a six sigma methodology was used, and an improvement phase was established where ODTs were prepared using lyophilization and levigation techniques. Finally, a pharmacokinetic study of the improved ODT was accomplished in comparison to the conventional oral tablet.
RESULTS
Pharmaburst-based formula (F4) showed the shortest wetting time and, consequently, the shortest disintegration time and the highest percentage of drug dissolved within 3 min compared to the other formulae. All the improved ODTs had a bitterness taste score vary from (0) palatable and (+1) tasteless. The current sigma level was 3.628 σ and 3.33 σ for palatability and solubility of ODT, respectively, which indicated the process was successfully improved compared with the previous sigma level of 2.342 σ of both processes. Pharmacokinetic study of the improved ODTs showed a significant decrease of T to 120 and 30 min instead of 180 and 120 min for meloxicam and baclofen, respectively.
CONCLUSION
ODTs were successfully improved using the six sigma methodology, the pharmacokinetic parameters of both drugs were enhanced due to rapid absorption through the oral mucosa.
Topics: Administration, Oral; Adult; Baclofen; Drug Compounding; Drug Liberation; Excipients; Female; Freeze Drying; Humans; Male; Meloxicam; Muscle Relaxants, Central; Solubility; Tablets; Taste; Total Quality Management
PubMed: 34690500
DOI: 10.2147/DDDT.S327193 -
Journal of Avian Medicine and Surgery Aug 2022Backyard poultry are commonly treated in veterinary hospitals; however, there is limited information regarding appropriate dosing of medications and withdrawal times for...
Backyard poultry are commonly treated in veterinary hospitals; however, there is limited information regarding appropriate dosing of medications and withdrawal times for eggs. Six healthy adult bantam Cochin hens were given a single oral dose of meloxicam (1 mg/kg). Meloxicam plasma concentrations and egg residues were analyzed by high-performance liquid chromatography. Noncompartmental analysis was used to calculate pharmacokinetic parameters. The apparent terminal half-life, maximum concentration, and time to maximum concentration were 5.94 ± 0.92 hours, 7.03 ± 2.68 µg/mL, and 2.83 ± 1.33 hours, respectively. Meloxicam was detected in egg whites for 4.8 ± 1.5 days and egg yolks for 9.8 ± 2.4 days. Results were compared with previous studies in white leghorn and Columbian Wyandotte hens. Bantam Cochin hens demonstrated a significantly longer mean apparent terminal half-life, greater area under the curve, smaller elimination rate constant, and longer egg residue times compared with white leghorn hens. However, the pharmacokinetic results from the bantam Cochin hens did not significantly differ from those reported for the Columbian Wyandotte hens. Until pharmacodynamic studies can be performed, dosing of oral meloxicam in bantam Cochins should follow recommendations for Columbian Wyandotte hens to reduce the likelihood of adverse effects. These results better inform appropriate dosing of meloxicam in domestic hens, as well as recommended withdrawal times for egg consumption.
Topics: Administration, Oral; Animals; Chickens; Drug Residues; Egg Yolk; Female; Meloxicam; Ovum
PubMed: 35972866
DOI: 10.1647/21-00023 -
Turkish Journal of Medical Sciences Apr 2017Platelet-rich plasma (PRP) application has gained widespread interest for musculoskeletal injuries. Nonsteroidal antiinflammatory drugs are frequently used in sports...
BACKGROUND/AIM
Platelet-rich plasma (PRP) application has gained widespread interest for musculoskeletal injuries. Nonsteroidal antiinflammatory drugs are frequently used in sports medicine before and/or after PRP application. Our study seeks to determine whether serum levels of platelet-derived growth factor-AB (PDGF-AB) and vascular endothelial growth factor (VEGF) levels of PRP would be affected by nonsteroidal antiinflammatory drugs.
MATERIALS AND METHODS
Two different final concentrations of diclofenac (0.5 μg mL and 2.5 μg mL), meloxicam (0.8 μg mL and 2.0 μg mL), and acetylsalicylic acid (final concentration 450 μm) were obtained in separate tubes with PRPs prepared from 20 healthy male volunteers. Medicine-free PRP was the control group. Growth factors were measured using ELISA.
RESULTS
PDGF-AB and VEGF serum levels did not change with diclofenac, meloxicam, or acetylsalicylic acid addition. PDGF-AB and VEGF serum levels correlated with each other.
CONCLUSION
Diclofenac, meloxicam, and acetylsalicylic acid did not affect PDGF-AB and VEGF serum levels.
Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Humans; Male; Meloxicam; Platelet-Derived Growth Factor; Platelet-Rich Plasma; Vascular Endothelial Growth Factor A; Young Adult
PubMed: 28425247
DOI: 10.3906/sag-1602-60 -
Archives of Pharmacal Research Dec 2021Meloxicam, a non-steroidal anti-inflammatory drug, is used for the treatment of rheumatoid arthritis and osteoarthritis. Cytochrome P450 (CYP) 2C9 and CYP3A4 are major...
Meloxicam, a non-steroidal anti-inflammatory drug, is used for the treatment of rheumatoid arthritis and osteoarthritis. Cytochrome P450 (CYP) 2C9 and CYP3A4 are major and minor enzymes involved in the metabolism of meloxicam. Impaired enzyme activity of CYP2C9 variants increases the plasma exposures of meloxicam and the risk of adverse events. The objective of our study is to develop and validate the physiologically based pharmacokinetic (PBPK) model of meloxicam related to CYP2C9 genetic polymorphism using the PK-Sim software. In vitro k of CYP2C9 was optimized in different CYP2C9 genotypes. The demographic and pharmacokinetic dataset for the development of the PBPK model was extracted from two previous clinical pharmacokinetic studies. Thirty-one clinical datasets, representing different dose regimens and demographic characteristics, were utilized to validate the PBPK model. The shapes of simulated plasma concentration-time profiles in each CYP2C9 genotype were visually similar to observed profiles. The predicted exposures (AUC) of meloxicam in CYP2C9*1/*3, CYP2C9*1/*13, and CYP2C9*3/*3 genotypes were increased by 1.77-, 2.91-, and 8.35-fold compared to CYP2C9*1/*1 genotype, respectively. In all datasets for the development and validations, fold errors between predicted and observed pharmacokinetic parameters were within the two-fold error criteria. As a result, the PBPK model was appropriately established and properly described the pharmacokinetics of meloxicam in different CYP2C9 genotypes. This study is expected to contribute to reducing the risk of adverse events of meloxicam through optimization of meloxicam dosing in different CYP2C9 genotypes.
Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; Cytochrome P-450 CYP2C9; Female; Genotype; Humans; Male; Meloxicam; Models, Biological; Young Adult
PubMed: 34807366
DOI: 10.1007/s12272-021-01361-3 -
Journal of Controlled Release :... Feb 2022For effective resolution of regional subacute inflammation and prevention of biofouling formation, we have developed a polymeric implant that can release meloxicam, a...
For effective resolution of regional subacute inflammation and prevention of biofouling formation, we have developed a polymeric implant that can release meloxicam, a selective cyclooxygenase (COX)-2 inhibitor, in a sustained manner. Meloxicam-loaded polymer matrices were produced by hot-melt extrusion, with commercially available biocompatible polymers, poly(ε-caprolactone) (PCL), poly(lactide-co-glycolide) (PLGA), and poly(ethylene vinyl acetate) (EVA). PLGA and EVA had a limited control over the drug release rate partly due to the acidic microenvironment and hydrophobicity, respectively. PCL allowed for sustained release of meloxicam over two weeks and was used as a carrier of meloxicam. Solid-state and image analyses indicated that the PCL matrices encapsulated meloxicam in crystalline clusters, which dissolved in aqueous medium and generated pores for subsequent drug release. The subcutaneously implanted meloxicam-loaded PCL matrices in rats showed pharmacokinetic profiles consistent with their in vitro release kinetics, where higher drug loading led to faster drug release. This study finds that the choice of polymer platform is crucial to continuous release of meloxicam and the drug release rate can be controlled by the amount of drug loaded in the polymer matrices.
Topics: Animals; Delayed-Action Preparations; Drug Carriers; Drug Liberation; Meloxicam; Polymers; Rats
PubMed: 34990702
DOI: 10.1016/j.jconrel.2021.12.038