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Tenoxicam

CAS# 59804-37-4

Tenoxicam

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Tenoxicam

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Chemical Properties of Tenoxicam

Cas No. 59804-37-4 SDF Download SDF
PubChem ID 54677971 Appearance Powder
Formula C13H11N3O4S2 M.Wt 337.37832
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (148.21 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-ylthieno[2,3-e]thiazine-3-carboxamide
SMILES CN1C(=C(O)Nc2ccccn2)/C(=O)c3sccc3[S]1(=O)=O
Standard InChIKey WZWYJBNHTWCXIM-RAXLEYEMSA-N
Standard InChI InChI=1S/C13H11N3O4S2/c1-16-10(13(18)15-9-4-2-3-6-14-9)11(17)12-8(5-7-21-12)22(16,19)20/h2-7,18H,1H3,(H,14,15)/b13-10-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Tenoxicam

DescriptionTenoxicam, an antiinflammatory agent with analgesic and antipyretic properties. Target: COX Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID). Tenoxicam-treated patients had significant decrease in nitrite levels (p = 0.036) and XO activity (p = 0.01), but their SOD, GSH-Px enzyme activities, and MDA levels were unchanged from baseline. Tenoxicam may have antioxidant effects, and it may reduce nitrite levels, indicating an alteration of NO pathways [1]. Tenoxicam was administered intraperitoneally immediately after BCAO. Histological analyses show that ischemia produced significant striatal as well as hippocampal lesions which were reversed by the Tenoxicam treatment. Tenoxicam also significantly reduced, to control levels, the increased myeloperoxidase activity in hippocampus homogenates observed after ischemia [2].

References:
[1]. Ozgocmen, S., et al., In vivo effect of celecoxib and tenoxicam on oxidant/ anti-oxidant status of patients with knee osteoarthritis. Ann Clin Lab Sci, 2005. 35(2): p. 137-43. [2]. Galvao, R.I., et al., Tenoxicam exerts a neuroprotective action after cerebral ischemia in rats. Neurochem Res, 2005. 30(1): p. 39-46.

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Preparing Stock Solutions of Tenoxicam

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.964 mL 14.8202 mL 29.6403 mL 59.2806 mL 74.1008 mL
5 mM 0.5928 mL 2.964 mL 5.9281 mL 11.8561 mL 14.8202 mL
10 mM 0.2964 mL 1.482 mL 2.964 mL 5.9281 mL 7.4101 mL
50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.1856 mL 1.482 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.5928 mL 0.741 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Tenoxicam

[Comparison of the effectivity of oral and intra-articular administration of tenoxicam in patients with knee osteoarthritis].[Pubmed:26363688]

Rev Bras Anestesiol. 2015 Sep-Oct;65(5):333-7.

BACKGROUND AND OBJECTIVES: Tenoxicam is widely used in osteoarthritis treatment and we aimed to compare the effectivity of oral and intra-articular administration of Tenoxicam in osteoarthritis treatment. METHODS: This study was performed between 2011 and 2012 by retrospectively analyzing and comparing the findings of 60 patients who were clinically and radiologically diagnosed with knee degenerative osteoarthritis in Bunyan state hospital pain policlinic. 60 patients included in the study were divided into two groups. The first group (Tenoxicam IA, n=30) included patient findings of those subjected to intra-articular injection of 20mg Tenoxicam to the knee once a week for three weeks and the second group (oral Tenoxicam, n=30) included patients who were administered 20mg oral Tenoxicam once a day for three weeks. All patients were clinically evaluated pre-treatment and in the 1st week, 1st month and 3rd month post-treatment according to specified criteria. RESULTS AND CONCLUSIONS: 22 of 60 patients included in the study were male and 38 were female. In both groups significant improvements were detected in all of the observed parameters: visual analog scale, Western Ontario McMaster Osteoarthritis Index (pain, physical activity, knee stiffness) and Lequesne index scores and in the evaluations performed in 1st week, 1st month and 3rd month with respect to pre-treatment values. Besides, a better compliance to treatment and gastrointestinal system tolerability in Tenoxicam IA group was also observed. Intra-articular Tenoxicam administration could be thought as an alternative treatment method in patients with knee osteoarthritis who cannot use oral Tenoxicam especially due to systemic gastrointestinal system side effects and those who have difficulties in adapting to treatment.

Comparison of the Effects of Daily Single-Dose Use of Flurbiprofen, Diclofenac Sodium, and Tenoxicam on Postoperative Pain, Swelling, and Trismus: A Randomized Double-Blind Study.[Pubmed:27311846]

J Oral Maxillofac Surg. 2016 Oct;74(10):1946.e1-6.

PURPOSE: The aim of the present study was to compare the effects of daily single-dose use of flurbiprofen, diclofenac sodium, and Tenoxicam on pain, swelling, and trismus that occur after surgical extraction of impacted wisdom teeth using local anesthesia. MATERIALS AND METHODS: The present study included 3 groups with 30 patients in each group. Those volunteering to participate in this double-blind randomized study (n = 90) were selected from a patient population with an indication for extraction of impacted wisdom teeth. Group 1 patients received 200 mg flurbiprofen, group 2 patients received 100 mg diclofenac sodium, and group 3 patients received 20 mg Tenoxicam. All doses were once a day, starting preoperatively. Pain was evaluated postoperatively at 1, 2, 3, 6, 8, and 24 hours and at 2 and 7 days using a visual analog scale (VAS). For comparison with the preoperative measurements, the patients were invited to postoperative follow-up visits 2 and 7 days after extraction to evaluate for swelling and trismus. The statistical analysis was performed using descriptive statistics in SAS, version 9.4 (SAS Institute, Cary, NC), software. Statistical analysis of the pain, swelling, and trismus data was performed using the Kruskal-Wallis, Dunn, and Wilcoxon-Mann-Whitney U tests. The statistical level of significance was accepted at P = .05 and power of 0.80. RESULTS: Clinically, Tenoxicam showed better analgesic and anti-inflammatory efficacy compared with diclofenac sodium and, in particular, flurbiprofen. Although the VAS scores in the evaluation of pain showed statistically significant differences at 2 days, no statistically significant difference was found for swelling and trismus. CONCLUSIONS: Our study evaluated the analgesic and anti-inflammatory effects with a daily single dose of flurbiprofen, diclofenac sodium, and Tenoxicam. Daily 20 mg Tenoxicam can be accepted as an adequate and safe option for patients after a surgical procedure.

Comparison of intra-articular bupivacaine-morphine with bupivacaine-tenoxicam combinations on post-operative analgesia in patients with arthroscopic meniscectomy: a prospective, randomised study.[Pubmed:26374114]

Int Orthop. 2016 Mar;40(3):601-5.

AIM: There are many alternatives for post-operative pain relief in patients who have had general anaesthesia. The aim of this study was to evaluate the efficacy of intra-articular bupivacaine + morphine and bupivacaine + Tenoxicam applications in post-operative pain control in patients undergoing knee arthroscopy with general anaesthesia. METHOD: This was a prospective study. Standard anaesthesia procedures were applied to each patient, and the 240 patients chosen at random were then divided into two groups. Each group received a different combination of drugs for this double-blind study. The first group (group A: 120 patients) received 0.5% bupivacaine 100 mg + Tenoxicam 20 mg (22 ml); the second group (group B) received 0.5% bupivacaine 100 mg + morphine 2 mg (22 ml); both groups received their drugs at the end of the intra-articular operation before tourniquet deflation. Before the operation, patients were asked about their post-operative pain at particular periods over the following 24 hours using the visual analogue scale (VAS) and the numeric rating scale (NRS). An additional analgaesic requirement and possible side effects were also recorded. RESULTS: Group A patients needed analgaesics sooner after operation than patients in group B. In Group B, VAS and NRS values were statistically higher compared with group A at the 12th hour. There were also fewer side effects seen in group A versus group B. CONCLUSION: Effective and reliable results were obtained in post-operative pain control in bupivacaine added to the morphine or Tenoxicam groups following arthroscopic meniscectomy. In the Tenoxicam group, patients reported less pain, fewer side effects and less need for analgesics at 12 hours after the operation. LEVEL OF EVIDENCE: level 1, therapeutic, randomised, multicentric study.

Development of a nanogel formulation for transdermal delivery of tenoxicam: a pharmacokinetic-pharmacodynamic modeling approach for quantitative prediction of skin absorption.[Pubmed:27910712]

Drug Dev Ind Pharm. 2017 Apr;43(4):531-544.

This study investigates potentials of solid lipid nanoparticles (SLN)-based gel for transdermal delivery of Tenoxicam (TNX) and describes a pharmacokinetic-pharmacodynamic (PK-PD) modeling approach for predicting concentration-time profile in skin. A 2(3) factorial design was adopted to study the effect of formulation factors on SLN properties and determine the optimal formulation. SLN-gel tolerability was investigated using rabbit skin irritation test. Its anti-inflammatory activity was assessed by carrageenan-induced rat paw edema test. A published Hill model for in vitro inhibition of COX-2 enzyme was fitted to edema inhibition data. Concentration in skin was represented as a linear spline function and coefficients were estimated using non-linear regression. Uncertainty in predicted concentrations was assessed using Monte Carlo simulations. The optimized SLN was spherical vesicles (58.1 +/- 3.1 nm) with adequate entrapment efficiency (69.6 +/- 2.6%). The SLN-gel formulation was well-tolerated. It increased TNX activity and skin level by 40 +/- 13.5, and 227 +/- 116%, respectively. Average Cmax and AUC0-24 predicted by the model were 2- and 3.6-folds higher than the corresponding values computed using in vitro permeability data. SLN-gel is a safe and efficient carrier for TNX across skin in the treatment of inflammatory disorders. PK-PD modeling is a promising approach for indirect quantitation of skin deposition from PD activity data.

Description

Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.

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