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American Journal of Veterinary Research May 2013To determine the pharmacokinetics of meloxicam after IV and PO administration to 6 healthy sheep. (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
To determine the pharmacokinetics of meloxicam after IV and PO administration to 6 healthy sheep.
ANIMALS
6 healthy adult Dorset cross sheep (5 males and 1 female).
PROCEDURES
Meloxicam (0.5 mg/kg, IV, or 1.0 mg/kg, PO) was administered in a randomized crossover design with a 10-day washout period. Blood samples were collected at predetermined times over 96 hours. Serum drug concentrations were determined by high-pressure liquid chromatography with mass spectrometry. Computer software was used to estimate values of pharmacokinetic parameters through noncompartmental methods.
RESULTS
Following IV administration (n = 5), the geometric mean (range) elimination half-life was 14.0 hours (10.5 to 17.0 hours), volume of distribution was 0.204 L/kg (0.171 to 0.272 L/kg), and clearance was 0.17 mL/min/kg (0.12 to 0.27 mL/min/kg). Following oral administration (n = 6), maximum serum concentration was 1.72 μg/mL (1.45 to 1.93 μg/mL), time to maximum serum concentration was 19.0 hours (12.0 to 24.0 hours), clearance per bioavailability was 0.22 mL/min/kg (0.16 to 0.30 mL/min/kg), and terminal half-life was 15.4 hours (13.2 to 17.7 hours). Bioavailability of orally administered meloxicam was calculated as 72% (40% to 125%; n = 5). No adverse effects were evident following meloxicam administration via either route.
CONCLUSIONS AND CLINICAL RELEVANCE
Meloxicam administered PO at 1.0 mg/kg has good bioavailability with slow elimination kinetics in sheep. These data suggested that meloxicam may be clinically useful, provided the safety and analgesic efficacy of meloxicam as well as feed-related influences on its pharmacokinetics are established in ruminants.
Topics: Administration, Oral; Animals; Area Under Curve; Biological Availability; Female; Half-Life; Injections, Intravenous; Male; Meloxicam; Sheep; Thiazines; Thiazoles
PubMed: 23627392
DOI: 10.2460/ajvr.74.5.779 -
Molecules (Basel, Switzerland) Mar 2018The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with...
The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in "nose-to-brain" relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The "nose-to-blood" results predicted the nasal applicability of MEL and MELP in pain management. The "nose-to-brain" pathway requires further study.
Topics: Administration, Intranasal; Animals; Drug Delivery Systems; Male; Meloxicam; Nasal Absorption; Rats; Rats, Sprague-Dawley; Thiazines; Thiazoles
PubMed: 29597330
DOI: 10.3390/molecules23040784 -
The Canadian Veterinary Journal = La... Feb 2017The objectives of this study were to describe the routine use of analgesics by Ontario veterinarians for common surgeries in dogs and cats, and to compare routine use of...
The objectives of this study were to describe the routine use of analgesics by Ontario veterinarians for common surgeries in dogs and cats, and to compare routine use of analgesics between species and surgeries, using Chi-square analyses. In total, 239 veterinarians responded to the questionnaires; a response rate of 13.1%. Fifty-two percent to 79% of veterinarians used meloxicam for both species and all surgeries. Approximately 9% of veterinarians did not use analgesics for dog ovariohysterectomy and castration, while 16% to 22% did not use analgesics for these surgeries in cats. Veterinarians used and dispensed analgesics to dogs more often than to cats ( < 0.05). Many (60% or more) veterinarians administered analgesics pre-emptively to both dogs and cats for all surgeries. Continuing education for veterinarians needs to focus on understanding of pre-emptive analgesia, preventive analgesia, and the importance of dispensing analgesic drugs after surgery for all surgeries.
Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Castration; Cats; Dogs; Female; Hysterectomy; Male; Meloxicam; Ontario; Ovariectomy; Pain; Pain, Postoperative; Surveys and Questionnaires; Thiazines; Thiazoles; Veterinarians
PubMed: 28216684
DOI: No ID Found -
Brazilian Dental Journal 2017The effects of the non-steroidal anti-inflammatory drugs (NSAIDs) on bone quantity and quality were investigated for years. However, there is lack of information on the...
The effects of the non-steroidal anti-inflammatory drugs (NSAIDs) on bone quantity and quality were investigated for years. However, there is lack of information on the impact of NSAIDs on the quality of tooth-supporting alveolar bone in absence of periodontal inflammation. Thus, the aim of this study was to evaluate histometrically the influence of a selective COX-2 NSAID (Meloxicam) on the inter-radicular bone mineral density in rats. Forty-nine adult male Wistar rats were randomly divided into four experimental groups: Subcutaneous injection of 0.9% sterile saline for 15 days (G1; n=12) and 45 days (G2; n=11); and subcutaneous injection of Meloxicam for 15 days (G3; n=13) and 45 days (G4; n=13). Mineral density was histometrically determined in the inter-radicular area of the 1st mandibular molars and data analysis performed by two-way ANOVA (a=5%). Results showed no interaction between time and treatment (p>0.05) and that meloxicam did not affect the alveolar bone density. In contrast, it was found that inter-radicular alveolar bone density increased with time (91.88±3.08% and 92.86±2.38% for groups 15 and 45 days, respectively) (p<0.05). Within the limits of this study, daily administration of a selective COX-2 inhibitor (Meloxicam) did not affect the quality of the inter-radicular alveolar bone in absence of periodontal infection.
Topics: Animals; Bone Density; Cyclooxygenase 2 Inhibitors; Male; Meloxicam; Rats; Rats, Wistar; Thiazines; Thiazoles; Tooth
PubMed: 28492740
DOI: 10.1590/0103-6440201701081 -
Medicine Sep 2021Meloxicam is commonly administrated to control postoperative pain in orthopedic surgery, while its efficacy in total knee arthroplasty (TKA) is not clear. Therefore,... (Randomized Controlled Trial)
Randomized Controlled Trial
Evaluation of analgesic effect, joint function recovery and safety of meloxicam in knee osteoarthritis patients who receive total knee arthroplasty: A randomized, controlled, double-blind study.
Meloxicam is commonly administrated to control postoperative pain in orthopedic surgery, while its efficacy in total knee arthroplasty (TKA) is not clear. Therefore, this study aimed to explore the postoperative analgesic effect and tolerance of meloxicam in knee osteoarthritis (OA) patients undergoing TKA.Totally, 128 knee OA patients scheduled for TKA were enrolled in this randomized, controlled, double-blind study, then randomized into meloxicam group (N = 65) and control group (N = 63) as 1:1 ratio. Patients took meloxicam or placebo from 4 hours (h) to 72 h after TKA. Patients were followed up at 6 h, 12 h, day (D)1, D2, D3, D7, month (M)1, and M3.Pain visual analog scale score at rest was decreased in meloxicam group at 12 h, D1 and D3 compared to control group; pain visual analog scale score at flexion was reduced in meloxicam group at 6 h, 12 h, D1, D2, and D3 compared to control group. Additional and total consumption of patient-controlled analgesia were both attenuated in meloxicam group compared to control group. Furthermore, patient satisfaction score was higher on D1, D2, D3 in meloxicam group compared to control group. However, no difference of hospital for special surgery knee score score at M1 or M3 was found between the 2 groups. Moreover, the occurrence of adverse events was similar between the 2 groups.Meloxicam displays good effect on controlling postoperative pain and improving patient satisfaction, while does not affect long-term knee function recovery or safety profile in knee OA patients undergoing TKA.
Topics: Aged; Anti-Inflammatory Agents, Non-Steroidal; Arthroplasty, Replacement, Knee; Chi-Square Distribution; Double-Blind Method; Female; Humans; Male; Meloxicam; Middle Aged; Osteoarthritis, Knee; Pain Management; Pain Measurement; Recovery of Function
PubMed: 34477120
DOI: 10.1097/MD.0000000000026873 -
Nature Communications Dec 2021Nonsteroidal anti-inflammatory drugs (NSAIDs), including salicylic acid (SA), target mammalian cyclooxygenases. In plants, SA is a defense hormone that regulates...
Nonsteroidal anti-inflammatory drugs (NSAIDs), including salicylic acid (SA), target mammalian cyclooxygenases. In plants, SA is a defense hormone that regulates NON-EXPRESSOR OF PATHOGENESIS RELATED GENES 1 (NPR1), the master transcriptional regulator of immunity-related genes. We identify that the oxicam-type NSAIDs tenoxicam (TNX), meloxicam, and piroxicam, but not other types of NSAIDs, exhibit an inhibitory effect on immunity to bacteria and SA-dependent plant immune response. TNX treatment decreases NPR1 levels, independently from the proposed SA receptors NPR3 and NPR4. Instead, TNX induces oxidation of cytosolic redox status, which is also affected by SA and regulates NPR1 homeostasis. A cysteine labeling assay reveals that cysteine residues in NPR1 can be oxidized in vitro, leading to disulfide-bridged oligomerization of NPR1, but not in vivo regardless of SA or TNX treatment. Therefore, this study indicates that oxicam inhibits NPR1-mediated SA signaling without affecting the redox status of NPR1.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Arabidopsis; Arabidopsis Proteins; Gene Expression Regulation, Plant; Meloxicam; Piroxicam; Salicylic Acid
PubMed: 34911942
DOI: 10.1038/s41467-021-27489-w -
International Braz J Urol : Official... 2013We aimed to compare the effect and feasibility of a combined therapy with tamsulosin hydrochloride plus meloxicam, and tamsulosin hydrochloride alone in patients with... (Randomized Controlled Trial)
Randomized Controlled Trial
The effect of combined therapy with tamsulosin hydrochloride and meloxicam in patients with benign prostatic hyperplasia symptoms and impact on nocturia and sleep quality.
PURPOSE
We aimed to compare the effect and feasibility of a combined therapy with tamsulosin hydrochloride plus meloxicam, and tamsulosin hydrochloride alone in patients with benign prostate hyperplasia symptoms and impact on nocturia and sleep quality.
MATERIALS AND METHODS
Four hundred male patients were included in this study between 2008 and 2011. Patients were randomly divided into two groups: one received tamsulosin hydrochloride 0.4 mg (Group 1, 200 patients) and the other tamsulosin hydrochloride 0.4 mg plus meloxicam 15 mg (Group 2, 200 patients) prospectively. Patients were evaluated for benign prostate hyperplasia (BPH) symptoms according to the American Urological Association clinical guidelines and sleep quality according to Pittsburgh Sleep Quality Index (PSQI). Patients were reevaluated after three months of treatment. The International Prostatic Symptom Score (IPSS), IPSS-Quality of Life (IPSS-QoL), maximal urinary flow rates (Qmax), average urinary flow rates (AFR), post void residual urine volumes (PVR), nocturia and Pittsburgh Sleep Quality Score (PSQS) were recorded at baseline and after three months.
RESULTS
Mean age was 63.3 ± 6.6 and 61.4 ± 7.5 years in groups 1 and 2, respectively (p = 0.245). There were no statistically significant differences between both groups. Also, baseline prostate specific antigen (PSA), prostate volume, creatinine, International Prostatic Symptom Score (IPSS), IPSS-Quality of Life (IPSS-QoL), maximal urinary flow rates (Qmax), average urinary flow rates (AFR), post void residual urine volumes (PVR), nocturia and Pittsburgh Sleep Quality Score (PSQS) were similar in both groups. In addition, the total IPSS, IPSS-QoL, PVR, nocturia, and PSQS were significantly lower in Group 2 compared with Group 1 after treatment (p < 0.05). Qmax and AFR were higher significantly in Group 2 compared with Group 1 after treatment (p < 0.05).
CONCLUSIONS
Cyclooxygenase (COX)-2 inhibitors in combination with an alpha blocker may decrease benign prostatic hyperplasia symptoms and increase sleep quality without serious side effects.
Topics: Adrenergic alpha-1 Receptor Antagonists; Aged; Cyclooxygenase 2 Inhibitors; Drug Therapy, Combination; Feasibility Studies; Humans; Male; Meloxicam; Middle Aged; Nocturia; Prostatic Hyperplasia; Quality of Life; Reference Values; Sleep; Statistics, Nonparametric; Sulfonamides; Tamsulosin; Thiazines; Thiazoles; Treatment Outcome; Urination
PubMed: 24267123
DOI: 10.1590/S1677-5538.IBJU.2013.05.07 -
Veterinary and Comparative Oncology Mar 2023Organoid cultures could constitute a valuable in vitro model to explore new treatments for canine (c) medullary thyroid carcinoma (MTC). The study's objectives were to...
Organoid cultures could constitute a valuable in vitro model to explore new treatments for canine (c) medullary thyroid carcinoma (MTC). The study's objectives were to establish and characterize 3D organoid cultures of cMTC using histology and immunohistochemistry (IHC) and to evaluate the effect of antitumor drugs on organoids' viability. Five cMTC tissue samples were used to develop organoid cultures of which one organoid line, named cMTC N°2, could be passaged for an extended period. This cMTC N°2 organoid line was further compared to the primary tumour regarding morphology and IHC expression of thyroid transcription factor-1 (TTF-1), thyroglobulin, calcitonin, synaptophysin, vimentin, Ki-67, cyclooxygenase-2 (COX-2), P-glycoprotein and vascular endothelial growth factor (VEGF). Quality control of the cMTC N°2 organoid line was achieved by a single nucleotide polymorphism (SNP) array of the organoids, primary tumour and healthy blood cells of the same dog. The effect of carboplatin, meloxicam and toceranib phosphate (TOC) on cMTC N°2 organoids' viability was evaluated. The cMTC N°2 organoid line was cultured for 94 days and showed similar histological features with the primary tumour. Immunolabelling for TTF-1, thyroglobulin, calcitonin and VEGF was similar between the primary tumour and cMTC N°2 organoids. Compared to the primary tumour, organoids showed higher immunolabelling for vimentin and Ki-67, and lower immunolabelling for synaptophysin, COX-2 and P-glycoprotein. The SNP genotype was similar for each chromosome between healthy blood cells, primary tumour and cMTC N°2 organoids. Carboplatin, meloxicam and TOC had no effect on cMTC N°2 organoid cell viability within achievable in vivo concentration range. In conclusion, the cMTC N°2 organoid line is a promising first milestone towards an established in vitro organoid model to explore pathophysiology and new treatment modalities in cMTC.
Topics: Dogs; Animals; Calcitonin; Thyroglobulin; Synaptophysin; Vascular Endothelial Growth Factor A; Vimentin; Carboplatin; Cyclooxygenase 2; Ki-67 Antigen; Meloxicam; Dog Diseases; Thyroid Neoplasms; Organoids; ATP Binding Cassette Transporter, Subfamily B
PubMed: 36583463
DOI: 10.1111/vco.12872 -
Inflammation Research : Official... Aug 2010The objective of this study was to determine the ability of meloxicam prophylaxis and therapy to blunt the effect of complete Freund's adjuvant (CFA) induced...
OBJECTIVE AND DESIGN
The objective of this study was to determine the ability of meloxicam prophylaxis and therapy to blunt the effect of complete Freund's adjuvant (CFA) induced monoarthritis.
MATERIALS AND METHODS
First the validity of this animal model was established by examining joint changes at multiple levels after injecting CFA into the tibio-tarsal joint. Next, meloxicam (5 mg/kg) or vehicle was administered on days 0-7 (prophylactic) and on days 7-16 (therapeutic) in separate groups of animals.
RESULTS
The CFA-injected joint demonstrated hallmark histological and structural changes such as pannus formation, bone remodeling, cartilage erosion and immune cell infiltration. Both prophylactic and therapeutic treatment with meloxicam effectively reduced swelling (ankle circumference), oedema and extravasation of Evans blue dye in the affected joint. Moreover, meloxicam reduced loss in range of motion and also reduced mechanical stimulus evoked pain scores. Notably, these effects persisted after discontinuing drug treatment.
CONCLUSION
The present study provides a unique comparison of prophylactic versus therapeutic effects of meloxicam in the CFA-induced model of monoarthritis.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Experimental; Cyclooxygenase Inhibitors; Freund's Adjuvant; Humans; Inflammation; Male; Meloxicam; Rats; Rats, Sprague-Dawley; Tarsus, Animal; Thiazines; Thiazoles
PubMed: 20349327
DOI: 10.1007/s00011-010-0179-3 -
Journal of Dairy Science Feb 2021Both the economic loss and welfare implications of lameness affect the dairy industry. Currently no analgesic drugs are approved to alleviate lameness-associated pain in...
Both the economic loss and welfare implications of lameness affect the dairy industry. Currently no analgesic drugs are approved to alleviate lameness-associated pain in lactating dairy cattle in the United States. In this randomized controlled trial, 48 lactating Holsteins were enrolled to evaluate the effect of oral meloxicam and i.v. flunixin meglumine on induced lameness. Cows were allocated to 1 of 4 treatment groups (n = 12 per group): lameness and flunixin meglumine (LAME + FLU); lameness and meloxicam (LAME + MEL); lameness and placebo (LAME + PLBO); or sham induction and placebo (SHAM + PLBO). Six hours before treatment, arthritis-synovitis was induced in the distal interphalangeal joint with 20 mg of amphotericin B, whereas SHAM cows were given an intra-articular injection of an equal volume (4 mL) of isotonic saline. Cows in LAME + FLU received 2.2 mg/kg flunixin meglumine i.v. and whey protein placebo orally; LAME + MEL were administered 1 mg/kg meloxicam orally and 2 mL/45 kg sterile saline placebo i.v.; LAME + PLBO were administered 2 mL/45 kg sterile saline placebo i.v. and whey protein placebo orally; and SHAM + PLBO received 2 mL/45 kg sterile saline placebo i.v. and whey protein placebo orally. The initial treatment of MEL, FLU, or PLBO was identified as time 0 h and followed by a second dose 24 h later with data collection for 120 h. The methods used to assess analgesic efficacy were electronic pressure mat, visual lameness assessment, visual analog score, plasma cortisol concentration, plasma substance P concentration, mechanical nociception threshold, and infrared thermography imaging. Linear mixed effect modeling was the primary method of statistical analysis. Visual lameness scoring indicated a lower proportion of the FLU + LAME group was lame at the T2 h and T8 h time points in comparison to the positive controls, whereas MEL therapy resulted in a lower proportion of lame cows at the T8 h time point. Cortisol area under the effect curve was lower following FLU therapy compared with LAME + PBLO for the 0-2 h (LSM difference = 35.1 ng·h/mL, 95% CI: 6.8, 63.3 ng·h/mL), 2-8 h (LSM difference = 120.6 ng·h/mL, 95% CI: 77.2, 164.0 ng·h/mL), and 0-24 h (LSM difference = 226.0 ng·h/mL, 95% CI: 103.3, 348.8 ng·h/mL) time intervals. Following MEL therapy, cortisol area under the effect curve was lower than LAME + PLBO for both the 2 to 8 h (LSM difference = 93.6 ng·h/mL, 95% CI: 50.2, 137.0 ng·h/mL) and 0 to 24 h time intervals (LSM difference = 187.6 ng·h/mL, 95% CI: 64.9, 310.4 ng·h/mL). Analysis of data from other assessment modalities failed to discern biologically relevant differences between treatment groups. We conclude that meaningful differences were evident for visual lameness assessment and cortisol from MEL and FLU treatment versus the positive control. Further clinical research is needed toward development of a model that will create reproducible events that are more pronounced in severity and duration of lameness which can be validated as a substitute for naturally occurring lameness cases.
Topics: Administration, Oral; Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Cattle; Cattle Diseases; Clonixin; Dairying; Female; Injections, Intravenous; Lactation; Lameness, Animal; Meloxicam; Pain
PubMed: 33309349
DOI: 10.3168/jds.2020-18563