LornoxicaM (Xefo)
Lornoxicam
CAS: 70374-39-9
Molecular Formula: C13H10ClN3O4S2
LornoxicaM (Xefo) - Names and Identifiers
LornoxicaM (Xefo) - Physico-chemical Properties
| Molecular Formula | C13H10ClN3O4S2 |
| Molar Mass | 371.82 |
| Density | 1.742±0.06 g/cm3(Predicted) |
| Melting Point | 225-230°C (dec.) |
| Solubility | Soluble in water (<1 mg/ml at 25 °C), methanol (sparingly), DMSO (2 mg/ml at 25 °C) |
| Appearance | powder |
| Color | faint yellow to dark yellow |
| Merck | 14,5582 |
| pKa | pKa2 4.7(at 25℃) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Sensitive | Sensitive to heat |
| Refractive Index | 1.741 |
| MDL | MFCD00866163 |
| Physical and Chemical Properties | Orange to yellow crystals, melting point 225~230 ° C (decomposition). pKa24.7. UV absorption maximum: 371nm. Partition coefficient (N-octanol/pH 7.4 buffer):1.8. Acute toxicity LD50 mice, rats, rabbits, dogs, monkeys (mg/kg): All> 10 oral. |
LornoxicaM (Xefo) - Risk and Safety
| Risk Codes | R36/37/38 - Irritating to eyes, respiratory system and skin. R28 - Very Toxic if swallowed |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37 - Wear suitable protective clothing and gloves. S28 - After contact with skin, wash immediately with plenty of soap-suds. |
| UN IDs | UN 2811 6.1 / PGII |
| WGK Germany | 3 |
| RTECS | XJ9095000 |
| HS Code | 29349990 |
| Hazard Class | IRRITANT |
| Packing Group | II |
| Toxicity | LD50 orally in mice, rats, rabbits, dogs, monkeys: >10 mg/kg (Pruss) |
LornoxicaM (Xefo) - Reference Information
| Non-steroidal anti-inflammatory analgesic | Lornoxicam is a non-steroidal anti-inflammatory analgesic, it has strong antipyretic, analgesic and anti-inflammatory effects. It relatively balanced inhibition of cyclooxygenase (COX) two isomers of the activity, thereby inhibiting the biosynthesis of prostaglandins, resulting in anti-inflammatory analgesic effect. The COX1:COX2 inhibition rate of the drug is 0.6, so it has a good analgesic effect of traditional NSAID. At the same time, the drug does not inhibit the activity of 5-lipoxygenase, so it does not inhibit the synthesis of leukotriene, and does not shunt arachidonic acid to the 5-lipoxygenase pathway, the metabolites of arachidonic acid and 5-lipoxygenase can inhibit the Impulse process of nociceptors in the spinal cord, so that Lornoxicam has similar analgesic effect to opioid peptide analgesic drugs. Lornoxicam and naproxen can significantly reduce the rest pain score, joint tenderness index and joint swelling index in patients with OA, however, Lornoxicam was superior to naproxen in improving patient pain score. In vivo animal safety studies have shown that the toxicity profile is consistent with half oxidase inhibition. The digestive tract and kidneys are the most sensitive organs to toxic effects. The results of animal tests showed that Lornoxicam for injection had no vascular irritation and muscle irritation, and did not cause allergy and hemolysis. |
| pharmacological action | Lornoxicam is a non-steroidal anti-inflammatory analgesic and a thiazide derivative, has a strong anti-inflammatory and analgesic effect, its mechanism of action includes: (1) by inhibiting the activity of cyclooxygenase (COX) and then inhibit the synthesis of prostaglandin, lornoxicam, however, does not inhibit the activity of 5-lipoxygenase and therefore does not inhibit the synthesis of Leukotrienes and does not split arachidonic acid into 5-lipoxygenase. (2) activation of opioid neuropeptide system, play a central analgesic effect. Figure 1 shows the structural formula of Lornoxicam. |
| pharmacokinetics | absorbed rapidly and completely after oral administration of 4mg, the peak plasma concentration was 2.5 μg/L in 270 hours. At doses ranging from 2 to 6mg twice daily, a dependent pharmacokinetic profile was shown. When taken simultaneously with food, the absorption of the drug slows down and decreases by about 20%. The bioavailability was 100% and the average half-life was 3-5 hours. Lornoxicam is present in plasma in the form of unchanged and hydroxylated metabolites, and its hydroxylated metabolites do not show pharmacological activity. Lornoxicam plasma protein binding was 99.0% and was not concentration dependent. Lornoxicam was completely metabolized, 1/3 cleared by kidney and 2/3 cleared by liver. There was no significant difference in pharmacokinetic parameters when the elderly were given continuously, when the liver and kidney function damage was not serious or when combined with anti acid drugs. |
| indication | commonly used in the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, gouty arthritis and sheath inflammation. At the same time, it is also suitable for acute pain after surgery, moderate to severe pain caused by trauma, neuralgia (such as acute sciatica), low back pain and advanced cancer pain. |
| usage and dosage | injection: acute moderate postoperative pain and pain associated with acute lumbar sciatica. tablets: various acute mild to moderate pain and joint pain and inflammation caused by certain types of rheumatic diseases. injection: 8mg each time, the daily dose is generally not more than 16 mg. For some patients, if necessary, the first dose can be 16 mg in the first 24 hours, after which 8mg can be added. That is, the maximum dose on the first day is 24 mg. The subsequent dose was 8mg twice daily. The daily dose should not exceed 16mg. Tablets: need to be taken with a sufficient amount of water. Acute mild or moderate pain: the daily dose is 8-16 mg, with only one use, take 8-16 mg. For repeated use, the maximum daily dose is 16mg. It is best to take it 2 times a day. Pain and inflammation of the joints caused by rheumatic diseases: the daily dose is 12-16 mg. The recommended dose is 1 tablet twice daily. Maximum Dose: not more than 16mg per day. Dosage should be adjusted in patients with mild to moderate renal insufficiency. |
| tenoxicam | tenoxicam has anti-inflammatory, analgesic and antipyretic effects, and can also inhibit platelet aggregation. It was as effective as piroxicam, Lornoxicam, indomethacin, and dichlorofenic acid in standard animal models of inflammation, but more potent than aspirin, methanoic acid, and naproxen. Like other non-steroidal anti-inflammatory drugs, it is also an inhibitor of prostaglandin synthesis. It may produce anti-inflammatory effects by scavenging reactive oxygen species or inhibiting their production, and inhibiting Leukocyte chemotaxis and phagocytosis. Oral absorption is rapid, Tmax is 2~4H, PBP is 99.4%,t1/2 is 57H. Mainly excreted with urine and bile. [use] mainly used for rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis, extra-articular lesions such as tendinitis, strain and sprain, acute gout, etc. |
| adverse reactions | adverse reactions after oral administration included dizziness, Head Pain, stomachache, Diarrhea, dyspepsia, Nausea and Vomit. adverse reactions occurring between 1% and 10% after injection: adverse reactions associated with the injection site (eg, pain, Fever, stinging tension), stomach pain, Nausea, vomit, dizziness, drowsiness, Head Pain, skin flushing. Adverse reactions with a frequency of less than 1%: flatulence, restlessness, dyspepsia, Diarrhea, increased blood pressure, palpitations, chills, sweating, dysgeusia, dry mouth, leukopenia, thrombocytopenia, urination disorder. |
| drug interaction | 1. Cimetidine can inhibit the elimination of this product and increase the steady-state plasma concentration of this product. 2. The anticoagulant effect of warfarin and the hypoglycemic effect of sulfonylureas are enhanced by plasma protein exchange. 3. This product increases the concentration of serum lithium and the AUC of methotrexate. 4. The product can resist the antihypertensive effect of angiotensin converting enzyme inhibitor and reduce the diuretic and natriuresis effect of furosemide. 5. Aspirin reduced Cmax, AUC and elimination half-life by 20%. This product makes aspirin Cmax, AUC and elimination half-life reduced by 6%~ 15%, and enhanced side effects. 6. The bioavailability of Lornoxicam was decreased by the chelate of bismuth. 7. Digoxin increases the Cmax and elimination half-life of this product, while the renal clearance of digoxin decreases. |
| note | 1. Allergic to non-steroidal anti-inflammatory drugs, Coagulation Abnormalities, acute gastrointestinal bleeding or acute gastrointestinal ulcers, moderate to severe renal impairment, cerebral hemorrhage or suspected cerebral hemorrhage, massive blood loss or dehydration, heart or liver function is severely damaged, pregnant and lactating women, less than 18 years of age disabled. 2. History of bronchial asthma or allergic reaction History, myocardial infarction, stroke history should be used with caution. 3. Continuous and long-term medication is not recommended. |
| Use | Non-steroidal anti-inflammatory analgesic. The synthesis of prostaglandins is inhibited by blocking cyclic oxygenase, but has no effect on ester oxygenase. |
| production method | 2, 5-dichlorothiophene (I) is chlorosulfonated with chlorosulfonic acid in the presence of thionyl chloride, sulfonyl chloride (II) was obtained. Subsequent acylation with methylamine in chloroform affords the sulfonamide (III). Carboxylation with carbon dioxide and butyl lithium in diethyl ether gave the carboxylic acid (IV). (Iv) first and phosphorus pentachloride, then add methanol, esterification to obtain carboxylic acid ester (V). (V) reaction with methyl iodoacetate in dimethylformamide in the presence of sodium hydride to form tertiary amine (VI). Further, under the action of sodium methoxide, a thiazine derivative (VII) is obtained by cyclization. Finally, with 2-aminopyridine, Lornoxicam was refluxed in xylene. |
Last Update：2024-04-09 02:00:10
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