Contents 1 Pinyin 2 English reference 3 Overview 4 Piroxicam Pharmacopoeia Standard 4.1 Product name 4.1.1 Chinese name 4.1.2 Chinese Pinyin 4.1.3 English name 4.2 Structural formula 4.3 Molecular formula and molecular weight 4.4 Source (name), content (potency) 4.5 Properties 4.5.1 Melting point 4.6 Identification 4.7 Inspection 4.7.1 Related substances 4.7.2 Chloride 4.7.3 Weight loss on drying 4.7.4 Residue on ignition 4.7.5 Heavy metals 4.7.6 Arsenic salt 4.8 Content determination 4.9 Category 4.10 Storage 4.11 Preparation 4.12 Version 5 Standard issued by the Ministry of Chemical Drugs 5.1 Pinyin name 5.2 English name 5.3 Standard number 5.4 Source 5.5 Properties 5.6 Identification 5.7 Inspection 5.8 Content determination 5.9 Function and use 5.10 Usage and dosage 5.11 Note 5.12 Storage 5.13 Preparation 6 Piroxicam Instructions 6.1 Drug name 6.2 English name 6.3 Alias ??of piroxicam 6.4 Classification 6.5 Dosage form 6.6 Pharmacological effects of piroxicam 6.7 Pharmacokinetics of piroxicam 6.8 Indications of piroxicam 6.9 Contraindications of piroxicam 6.10 Precautions 6.11 Adverse effects of piroxicam Response 6.12 Usage and dosage of piroxicam 6.13 Interactions between piroxicam and other drugs 6.14 Expert comments 7 Piroxicam poisoning 7.1 Clinical manifestations 7.2 Treatment 8 References This is a redirected entry that ***shares the content of piroxicam. For the convenience of reading, piroxicam below has been automatically replaced by piroxicam. You can click here to restore the original appearance, or use the note method to display 1 Pinyin
yán tòng xǐ kāng 2 English reference
< p> [Chemistry] feldene 3 OverviewYantongxikan is an antipyretic and analgesic non-steroidal anti-inflammatory drug. It is an off-white to slightly yellowish-green crystalline powder; odorless and tasteless. It works by inhibiting cyclooxygenase, reducing prostaglandin synthesis and inhibiting leukocyte chemotaxis and the release of lysosomal enzymes. Suitable for the treatment of acute and chronic rheumatoid arthritis, ankylosing spondylitis, etc. Its efficacy is better than that of indomethacin, ibuprofen and naproxen. 4 Yantongxikang Pharmacopoeia Standard 4.1 Product name 4.1.1 Chinese name
Yantongxikang 4.1.2 Chinese Pinyin
Biluoxikang
4.1.3 English name
Piroxicam 4.2 Structural formula 4.3 Molecular formula and molecular weight
C15H13N3O4S 331.35 4.4 Source (name), content (potency)
This product is 2methyl 4-hydroxyl N (2pyridyl)2H1,2benzothiazine3carboxamide1,1dioxide. Calculated as dry product, the content of C15H13N3O4S shall not be less than 98.5%. 4.5 Properties
This product is an off-white to slightly yellowish-green crystalline powder; odorless and tasteless.
This product is easily soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or ether, and almost insoluble in water; soluble in acid and slightly soluble in alkaloids.
4.5.1 Melting point
The melting point of this product (Appendix VI C of Pharmacopoeia Part 2, 2010 edition) is 198~202℃, and it decomposes when melting. 4.6 Identification
(1) Take about 30mg of this product, add 1ml of chloroform to dissolve, then add 1 drop of ferric chloride test solution, it will appear rose red.
(2) Take this product, add 0.01mol/L hydrochloric acid methanol solution to dissolve and dilute it to make a solution containing 5μg per 1ml, and measure it with UV-visible spectrophotometry (2010 edition of Pharmacopoeia Part 2 Appendix IV A) Measurement shows maximum absorption at wavelengths of 243nm and 334nm.
(3) The infrared light absorption spectrum of this product should be consistent with the control spectrum (Figure 188 of "Drug Infrared Spectrum Collection"). 4.7 Inspection 4.7.1 Related substances
Take this product, add chloroform to dissolve it and make a solution containing 20mg per 1ml, as the test solution; accurately measure the appropriate amount, add chloroform for quantification Dilute to a solution containing 0.2mg per 1ml as a control solution. According to the thin layer chromatography test (Appendix V B of the 2010 edition of Pharmacopoeia Part 2), take 10 μl of each of the above two solutions and spot them on the same silica gel GF254 thin layer plate (0.5% sodium carboxymethylcellulose and 1mol/L sodium hydroxide). Solution isovolumetric mixture is used as adhesive), use chloroform-acetone-methanol (25:25:5) as the developing agent, unfold, dry, and inspect under ultraviolet light (254nm). If the test solution shows impurity spots, they must not be deeper than the main spots shown in the control solution. 4.7.2 Chloride
Take 2g of anhydrous sodium carbonate and spread it on the bottom and around the crucible. Take 1.0g of this product and place it on anhydrous sodium carbonate. Moisten it with a small amount of water. After drying, first use a small Burn with fire to completely ashes, let cool, add an appropriate amount of water to dissolve, filter, wash the crucible and filter with water, combine the filtrate and washing liquid, add water to make it 20ml, shake well, take 1ml of the filtrate, add nitric acid dropwise to make it medium If it is neutral, add 1 drop of nitric acid, shake well, place it in a 75-85°C water bath, remove all hydrogen sulfide, let it cool, add 1% sodium carbonate solution dropwise to make it neutral, add water to make it 25ml, and check according to the law (2010 edition Pharmacopoeia Part 2 Appendix VIII A), compared with the control solution made of 5.0 ml of standard sodium chloride solution, it shall not be more concentrated (0.1%). 4.7.3 Weight loss on drying
Take this product and dry it at 105℃ to constant weight. The weight loss shall not exceed 0.5% (Appendix VIII L of Pharmacopoeia Part 2, 2010 edition). 4.7.4 Residue on ignition
Take 1.0g of this product and check it in accordance with the law (2010 edition of Pharmacopoeia, Part II, Appendix VIII N). The remaining residue should not exceed 0.1%. 4.7.5 Heavy metals
Take the residue left under the ignition residue category and inspect it according to the law (Appendix VIII H Second Method of the 2010 Pharmacopoeia Part 2). The heavy metal content should not exceed 10 parts per million. 4.7.6 Arsenic salt
Take 10 ml of the remaining solution under the above chloride inspection item, add 5 ml of hydrochloric acid and 13 ml of water, and check according to the law (Appendix VIII J, Method 1 of the 2010 Pharmacopoeia, Part 2). It should comply with the regulations. (0.0004%). 4.8 Content determination
Take about 0.2g of this product, weigh it accurately, add 20ml of glacial acetic acid to dissolve it, add 1 drop of crystal violet indicator solution, and titrate with perchloric acid titrant (0.1mol/L) to The solution appears blue-green, and the titration results are corrected with a blank test. Each 1ml of perchloric acid titrant (0.1mol/L) is equivalent to 33.14mg of C15H13N3O4S. 4.9 Category
Antipyretic and analgesic NSAIDs. 4.10 Storage
Protect from light and seal.
4.11 Preparations
(1) Yantongxikang tablets? (2) Yantongxikang ointment? (3) Yantongxikang injection? (4) Yantongxikang capsules? (5) Yantongxikang Piluoxikang gel version 4.12
"Pharmacopoeia of the People's Republic of China" 2010 Edition 5 Standard 5.1 issued by the Ministry of Chemical Drugs Pinyin name
Piluoxikang 5.2 English name
PIROXICAMUM 5.3 Standard number
C15H13N3O4S 331.35 5.4 Source
This product is 2methyl 4hydroxy N (2 pyridyl) 2H1, 2 benzothiazine 3 carboxamide 1 ,1 dioxide. Calculated as dry product, the content of C15H13N3O4S shall not be less than 98.5%. 5.5 Properties
This product is an off-white or yellowish-green crystal or crystalline powder; odorless and tasteless. This product is easily soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or ether, almost insoluble in water, soluble in acid, and slightly soluble in alkaloids. Melting point: The melting point of this product (Chinese Pharmacopoeia 1990 edition, Part II Appendix, page 15) is 198~202℃, and it decomposes when melted. 5.6 Identification
(1) Take about 30mg of this product, add 1ml of chloroform to dissolve, then add 1 drop of ferric chloride test solution, it will appear rose red.
(2) Take this product, add hydrochloric acid methanol solution (0.01mol/L) to make a solution containing 5μg per 1ml, and measure it by spectrophotometry (Chinese Pharmacopoeia 1990 edition, Part 2 Appendix, page 24) , with maximum absorption at wavelengths of 243 and 334nm.
(3) The infrared light absorption spectrum of this product should be consistent with the control spectrum (infrared spectrum set 188). 5.7 Inspection
For relevant substances, take this product and add chloroform to make a solution containing 20mg per 1ml as the test solution; accurately measure an appropriate amount and add chloroform to dilute it into a solution containing 0.2mg per 1ml. , as a control solution. According to the thin layer chromatography test (Chinese Pharmacopoeia 1990 edition, Part II Appendix, page 30), draw 10 μl of each of the above two solutions, and spot them on the same silica gel GF<[254]> thin layer plate (0.5% sodium carboxymethylcellulose and Sodium hydroxide solution (1 mol/L) isovolumetric mixture is used as adhesive), and chloroform acetone methanol (25:25:5) is used as developing agent. After development, dry it and inspect it under ultraviolet light (254nm). . If the test solution shows impurity spots, they must not be deeper than the main spots shown in the control solution. For chloride, take 2g of anhydrous sodium carbonate and spread it on the bottom and around the crucible. Take 1.0g of this product and place it on the anhydrous sodium carbonate. Moisten it with a small amount of water. After drying, burn it with a small fire to completely ashes it. Cold, add an appropriate amount of water to dissolve, filter, wash the crucible and filter with water, combine the filtrate and washing liquid, add water to make 20ml, shake well, take 1ml of the filtrate, titrate the nitric acid to make it neutral, add 1 drop of nitric acid, shake Evenly, place it in a water bath at 75-85℃, remove all hydrogen sulfide, let it cool, add 1% sodium carbonate solution dropwise to make it neutral, add water to make it 25ml, and check according to the law (Chinese Pharmacopoeia 1990 Edition, Part 2 Appendix, page 48). Compared with the control solution made from 5.0ml of standard sodium chloride solution, it must not be more concentrated (0.1%). Weight loss on drying: Take this product and dry it at 105℃ to constant weight. The weight loss shall not exceed 0.5% (Chinese Pharmacopoeia 1990 Edition, Part II Appendix, page 55). Residue on ignition: Take 1.0g of this product and check according to the law (Chinese Pharmacopoeia, 1990 edition, Part II, Appendix, page 56). The remaining residue should not exceed 0.1%. Heavy metals: Take the residue left under the ignition residue category and inspect it according to the law (Chinese Pharmacopoeia 1990 edition, Part II, Appendix, page 51, second method). The heavy metal content should not exceed 10 parts per million. Arsenic salt: Take 10 ml of the remaining solution under the above chloride inspection item, add 5 ml of hydrochloric acid and 13 ml of water, and check according to the law (Chinese Pharmacopoeia 1990 Edition, Part Two, Appendix 53, page 1), it should meet the regulations (0.0004%).
5.8 Content determination
Take about 0.2g of this product, weigh it accurately, add 20ml of glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and titrate with perchloric acid solution (0.1mol/L). Until the solution appears blue-green, and correct the titration results with a blank test. Each 1ml of perchloric acid solution (0.1mol/L) is equivalent to 33.14mg of C15H13N3O4S. 5.9 Function and use
Anti-inflammatory and analgesic. Used for rheumatoid arthritis and rheumatoid arthritis. 5.10 Usage and dosage
Take orally after meals. Rheumatism and rheumatoid arthritis: 20 mg per day. Acute gout: 40 mg per day for 4 to 6 days. Long-term use is not suitable. 5.11 Note
Patients with gastric and duodenal ulcers who have allergic reactions to this product are not allowed to use it; pregnant women and children should not use it. 5.12 Storage
Shield from light and store in airtight container. 5.13 Preparations
(1) Yantongxikang Tablets
(2) Yantongxikang Capsules Note: Formerly known as Piroxicam
Kaifeng Pharmaceutical Factory Liaoyuan Pharmaceutical No. 1 Drafted by the Henan Provincial Drug Control Institute? Reviewed by the Jilin Provincial Drug Control Institute 6 Piroxicam Instructions 6.1 Drug Name
Piroxicam 6.2 English Name
Piroxicam, DP16171 , Feldene 6.3 Alias ??of piroxicam
Piroxicam; Piroxicam; Feldide; Anerke; Shipcon; Feldene 6.4 Classification
Nervous system drugs> Solution Thermal analgesic non-steroidal anti-inflammatory drugs 6.5 dosage forms
1. Tablets: 20mg each;
2. Capsules: 10mg, 20mg;
3 .Injection: 10mg (1ml), 20mg (2ml);
4. Gel: 0.50%;
5. Suppository: 20mg. 6.6 Pharmacological effects of piroxicam
Piroxicam is a long-acting anti-inflammatory analgesic with an enol-type structure. Animal experiments have proven that it has a broad-spectrum anti-inflammatory effect, can eliminate erythema and edema, and has an inhibitory effect on the formation of tissue granuloma and adjuvant arthritis. In vitro tests show that Yantongxikan can inhibit phagocytosis and the release of lysosomal hydrolases, and can also inhibit platelet aggregation. Piroxicam does not inhibit the spasmodogenic effects of histamine, serotonin, ethylamine choline, or prostaglandins, but it is a potent inhibitor of prostaglandin synthesis. This inhibition is reversible. Yan Tong Xikang also has analgesic effect. In animal models that simulate human gout, it can not only reduce inflammation and edema, but also inhibit the increase in inflammatory leukocytes. Yantongxicam is a derivative of oxican. Yantongxikang is a new long-acting non-steroidal anti-inflammatory drug, and its mechanism of action is related to inhibiting prostaglandin synthesis. 6.7 Pharmacokinetics of Yantongxikan
It is rapidly absorbed after oral administration and can be detected in the blood after 30 minutes. The tmax is 3 to 5 hours, and the binding rate to plasma proteins is 99%. Vd0.12～0.14L/kg, t1/236～45h. 20 mg per day, reaching the plasma peak after 5 to 7 consecutive days, with Cmax of 3 to 5 μg/ml. There is no accumulation effect. Occasionally, even if the drug is discontinued for a day, the plasma concentration will not fall below the therapeutic range. Yantongxikan is metabolized slowly and extensively in the body, with enterohepatic circulation, and more than 90% is metabolized. 66% is excreted by the kidneys, 33% is excreted in the feces, and of most metabolites, only <5% remains unchanged. Impairment of renal function does not significantly alter its kinetics. Trace amounts of hydroxylated piroxicam may be found in the plasma of patients taking long-term piroxicam. The absorption of piroxicam is not affected by food, iron and antacids, and anticoagulants or aspirin do not affect the protein binding rate of piroxicam.
6.8 Indications of Yantongxikan
Acute and chronic rheumatoid arthritis, proliferative osteoarthropathy, ankylosing spondylitis, chronic strain back pain, periarthritis of the shoulder, postoperative and trauma Post-operative pain and acute gout. Pyroxicam cannot change the progression of rheumatoid arthritis, nor can it correct the hyperuricemia of gout. Not suitable for chronic gout. 6.9 Contraindications of Piroxicam
1. It is contraindicated for those allergic to Piroxicam or other non-steroidal anti-inflammatory drugs and children.
2. It is contraindicated for those with a history of gastrointestinal bleeding or ulcers.
3. It is prohibited for patients with heart and kidney dysfunction. 6.10 Precautions
1. Use with caution in patients with bleeding ulcers, patients with ulcers, patients with a history of ulcers, and patients with liver and kidney dysfunction.
2. Use with caution in patients with coagulation mechanism or platelet dysfunction.
3. Pregnant and lactating women and children should not use this product.
4. The dosage is small, 20mg per day, and the steady-state blood concentration will be reached in 4 to 4 days. It has been reported that its efficacy is better than indomethacin, ibuprofen and naproxen. Long-term use of large doses or more than 20 mg per day can cause gastric ulcers and massive bleeding. During use, you should pay attention to check blood routine and liver and kidney function. Pay attention to whether there is any change in the color of the stool. A fecal occult blood test should be performed if necessary.
5. Piroxicam may cause cross-allergic reactions with aspirin, etc.
6. Drinking alcohol at the same time or combining it with other non-steroidal anti-inflammatory drugs will increase the adverse reactions.
7. Adverse reactions are mild, including occasional dizziness, edema, stomach discomfort, diarrhea or constipation, neutropenia, aplastic anemia, etc., which generally disappear on their own after stopping the drug. 6.11 Adverse reactions of Yantongxikan
1. Gastrointestinal reactions include nausea, vomiting, stomach discomfort, abdominal pain, diarrhea, and constipation; it can also cause peptic ulcers and gastrointestinal bleeding.
2. Yantongxikang can inhibit platelet aggregation and prolong bleeding time.
3. Other adverse reactions include dizziness, headache, drowsiness and edema; epistaxis, neutropenia and liver function abnormalities are occasionally seen. A small number of patients may experience elevated blood non-protein nitrogen levels. 6.12 Usage and dosage of Yantongxikan
1. Anti-rheumatic, 20 mg once a day, taken in the morning. For acute gout, take 40 mg once a day for 4 to 6 days.
2. Intramuscular injection: 10 to 20 mg once a day.
3. Suppository: anal plug 20mg/d. 6.13 Drug interactions
1. See indomethacin.
2. Piroxicam should not be used in combination with aspirin. Aspirin can reduce the blood concentration of piroxicam by 80%.
3. The antiviral drug ritonavir can increase the blood concentration of piroxicam and increase its toxicity.
4. Taking it at the same time as dicoumarol and other anticoagulants can increase the effect of the latter, so the dose should be adjusted. 6.14 Expert comments
Yantongxikang is used to treat rheumatoid arthritis. Take 20 mg daily. It has analgesic and sleep-improving effects on the first day. It reaches the peak effect on the 6th day. After stopping the drug, the analgesia and improvement are improved. Sleep can last 48 hours. In the treatment of ankylosing spondylitis, 20 mg per day can improve the exercise ability of 80% of patients, and the effect is better than that of indomethacin. Piroxicam is easy to tolerate, the incidence of adverse reactions is lower than that of aspirin and indomethacin, and the withdrawal symptoms are also milder than those of the latter. However, if the dosage exceeds 20mg per day, the incidence of gastrointestinal symptoms and ulcers will be greatly increased. The treatment of rheumatoid arthritis by Yantongxikang cannot change the progression of the disease, nor can it correct hyperuricemia. It can only improve clinical symptoms such as pain relief and sleep improvement. 7 Piroxicam poisoning
Piroxicam (Piroxicam) is a powerful anti-inflammatory analgesic that reduces the synthesis of prostaglandins and inhibits the chemotaxis of leukocytes by inhibiting cyclooxygenase. and the release of lysosomal enzymes. Suitable for the treatment of acute and chronic rheumatoid arthritis, ankylosing spondylitis, etc. Its efficacy is better than that of indomethacin, ibuprofen and naproxen. The drug reaches peak plasma concentration 2 hours after oral administration, and its plasma half-life is 31 to 57 hours.
The protein binding rate is greater than 90%, the half-life is 45 hours, and it is mainly metabolized by the liver. 66% is excreted by the kidneys and feces in the form of hydroxylates and glucuronic acid conjugates, and the unchanged drug accounts for 5% in urine and feces. [1] 7.1 Clinical manifestations
[2]
1. Adverse reactions: dizziness, tinnitus, nausea, vomiting, abdominal pain, diarrhea, gastric perforation, upper gastrointestinal bleeding; chest tightness, Low back pain, proteinuria, hematuria and transient elevation of transaminase, etc.
2. Severe cases: disturbance of consciousness, convulsions, respiratory depression, shock and death.
3. Urticaria-like drug eruption, purpura-type drug eruption and anaphylactic shock. Thrombocytopenic purpura and granulocytopenia are occasionally seen.
4. Extrapyramidal symptoms: salivation at the corners of the mouth, facial muscle twitching, spasmodic torticollis, etc. 7.2 Treatment
The key points of treatment for Yantongxikang poisoning are [2]:
1. In addition to inducing vomiting, gastric lavage, and catharsis, patients with shock should be rescued.
2. Patients with gastric perforation should undergo surgery.
3. Those with allergies should be treated with antihistamines and glucocorticoids.
4. Extrapyramidal symptoms can be treated with scopolamine and other drugs.