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Purity: ≥98%
Piroxicam (formerly BAXO; CP16171; CP-16171; Feldene; Pyroxycam; Roxicam), an approved non-steroidal anti-inflammatory drug (NSAID), is a potent and non-selective COX inhibitor with potential anti-inflammatory activity. It was approved for the treatment of rheumatoid and osteoarthritis.
ln Vitro |
CP-16171, piroxicam, is a non-steroidal anti-inflammatory medication that inhibits COX. Its IC50 values for human monocyte COX-1 and COX-2 are 47 and 25 μM, respectively[1]. Piroxicam (CP-16171) (167, 333, 500 μM) reduces the T24 and 5637 cell populations. When coupled with 0.05 μM carboplatin, piroxicam (CP-16171) (500 μM) dramatically lowers the viability of T24 and 5637 cells as well. Additionally, the combination prevents booth cells from expressing Ki-67[3].
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ln Vivo |
In 12 out of 18 dogs, piroxicam (CP-16171) (0.3 mg/kg qd 24-h po) lowers the volume of the tumor. This action is caused by apoptosis induction and a decrease in the concentration of basic fibroblast growth factor in the urine[2].
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Animal Protocol |
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ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Well absorbed following oral administration. Piroxicam and its biotransformation products are excreted in urine and feces, with about twice as much appearing in the urine as in the feces. Approximately 5% of a piroxicam dose is excreted unchanged. However, a substantial portion of piroxicam elimination occurs by hepatic metabolism. Piroxicam is excreted into human milk. 0.14 L/kg Metabolism / Metabolites Renal Piroxicam has known human metabolites that include 5'-Hydroxypiroxicam. Biological Half-Life 30 to 86 hours |
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Toxicity/Toxicokinetics |
Hepatotoxicity
Elevated serum aminotransferase levels have been reported in 3% to 18% of patients taking piroxicam, but symptomatic liver disease with jaundice is rare (estimated at 1 to 5 cases per 100,000 prescriptions). The latency to onset of symptoms of clinically apparent liver injury due to piroxicam is variable from a few days to several months, but is generally within the first 1 to 6 weeks of treatment. The pattern of injury is predominantly cholestatic, although cases presenting with mixed or hepatocellular patterns have been reported (Case 1). Eosinophilia, rash and fever can occur, but are not always present and are usually not prominent. Autoantibodies are rarely found. The injury is usually self-limited and recovery occurs within 1 to 2 months. Rare cases of acute liver failure have been reported. Likelihood score: B (rare but likely cause of clinically apparent liver injury). Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Low amounts of piroxicam in milk and failure to detect piroxicam or its metabolites in the urine of 2 older infants indicates that it would not be expected to cause adverse effects in older breastfed infants. Because there is no published experience with piroxicam during breastfeeding in the newborn period, shorter-acting agents may be preferred while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants No adverse effects were found in the breastfed infant of a patient receiving 20 mg of piroxicam daily for 4 months starting the 9th month postpartum. Four infants 3 to 4.5 months of age remained healthy during long-term therapy of their mothers with piroxicam 20 mg daily. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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Additional Infomation |
Piroxicam is a monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide with the exocyclic nitrogen of 2-aminopyridine. A non-steroidal anti-inflammatory drug of the oxicam class, it is used to relieve pain and works by preventing the production of endogenous prostaglandins involved in the mediation of pain, stiffness, tenderness and swelling. It has a role as an analgesic, a cyclooxygenase 1 inhibitor, a non-steroidal anti-inflammatory drug, an EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor and an antirheumatic drug. It is a benzothiazine, a member of pyridines and a monocarboxylic acid amide.
A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily. Piroxicam is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of piroxicam is as a Cyclooxygenase Inhibitor. Piroxicam is a commonly used nonsteroidal antiinflammatory drug (NSAID) that is available by prescription only and is used in therapy of chronic arthritis. Piroxicam can cause mild serum aminotransferase elevations and, in rare instances, leads to clinically apparent acute liver injury that can be severe and even fatal. Piroxicam is a nonsteroidal oxicam derivative with anti-inflammatory, antipyretic and analgesic properties. As a non-selective, nonsteroidal anti-inflammatory drug (NSAID), piroxicam binds and chelates both isoforms of cyclooxygenases (COX1 and COX2), thereby stalling phospholipase A2 activity and conversion of arachidonic acid into prostaglandin precursors at the rate limiting cyclooxygenase enzyme step. This results in inhibition of prostaglandin biosynthesis. As a second, independent effect, piroxicam inhibits the activation of neutrophils thereby contributing to its overall anti-inflammatory effects. A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily. See also: Piroxicam Olamine (is active moiety of); Piroxicam betadex (has subclass). Drug Indication For treatment of osteoarthritis and rheumatoid arthritis. FDA Label Mechanism of Action The antiinflammatory effect of Piroxicam may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis. The prostaglandins are produced by an enzyme called Cox-1. Piroxicam blocks the Cox-1 enzyme, resulting into the disruption of production of prostaglandins. Piroxicam also inhibits the migration of leukocytes into sites of inflammation and prevents the formation of thromboxane A2, an aggregating agent, by the platelets. Pharmacodynamics Piroxicam is in a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Piroxicam works by reducing hormones that cause inflammation and pain in the body. Piroxicam is used to reduce the pain, inflammation, and stiffness caused by rheumatoid arthritis and osteoarthritis. |
Molecular Formula |
C15H13N3O4S
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Molecular Weight |
331.35
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Exact Mass |
331.062
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CAS # |
36322-90-4
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Related CAS # |
Piroxicam-d3;942047-64-5;Piroxicam-d4
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PubChem CID |
54676228
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Appearance |
Light yellow to yellow solid powder
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Density |
1.5±0.1 g/cm3
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Boiling Point |
568.5±60.0 °C at 760 mmHg
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Melting Point |
198-200°C
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Flash Point |
297.6±32.9 °C
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Vapour Pressure |
0.0±1.6 mmHg at 25°C
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Index of Refraction |
1.692
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LogP |
2.23
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
2
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Heavy Atom Count |
23
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Complexity |
611
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Defined Atom Stereocenter Count |
0
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InChi Key |
QYSPLQLAKJAUJT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H13N3O4S/c1-18-13(15(20)17-12-8-4-5-9-16-12)14(19)10-6-2-3-7-11(10)23(18,21)22/h2-9,19H,1H3,(H,16,17,20)
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Chemical Name |
4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-yl-1λ6,2-benzothiazine-3-carboxamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0180 mL | 15.0898 mL | 30.1796 mL | |
5 mM | 0.6036 mL | 3.0180 mL | 6.0359 mL | |
10 mM | 0.3018 mL | 1.5090 mL | 3.0180 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05104931 | Completed | Drug: Nanoformed Piroxicam IR Tablet Drug: Felden (piroxicam) Tablets Drug: Brexidol (piroxicam) Tablets |
Pain | Nanoform Finland Plc | December 2, 2020 | Phase 1 |
NCT04062591 | Completed | Drug: Piroxicam group Drug: Placebo |
Postoperative Pain | Ain Shams University | August 16, 2019 | Early Phase 1 |
NCT03612323 | Unknown † | Drug: Intra-ligamentary Piroxicam Drug: Intra-ligamentary Articaine |
Pulpitis - Irreversible | Cairo University | November 2018 | Early Phase 1 |
NCT03153657 | Completed | Drug: Piroxicam-Beta-Cyclodextrin Drug: Placebo |
Tooth Sensitivity Toothache |
Universidade Federal de Sergipe | December 13, 2016 | Phase 3 |
NCT02253446 | Completed | Drug: Piroxicam Drug: Diclofenac Sodium |
Primary Dysmenorrhea | Pamukkale University | May 2013 | Phase 4 |