2 English reference piroxicam [Xiangya Medical Dictionary]
Summary Piroxicam is a non-steroidal anti-inflammatory drug with antipyretic and analgesic effects, which is white to yellow-green crystalline powder. Odorless and tasteless. It can reduce prostaglandin synthesis, inhibit leukocyte chemotaxis and lysosomal enzyme release by inhibiting cyclooxygenase. Is suitable for treating acute and chronic rheumatic arthritis and ankylosing spondylitis. Its curative effect is better than that of indomethacin, ibuprofen and naproxen.
4 Pharmacopoeia standard of piroxicam 4. 1 product name 4. 1. 1 Chinese name piroxicam
4. 1.2 Chinese Pinyin Biluo Xikang
4. 1.3 English name piroxicam
4.2 structural formula 4.3 molecular formula and molecular weight C 15H 13N3O4S? 33 1.35
4.4 Source (name) and content (potency) This product is 2 methyl 4 hydroxy N(2 pyridyl) 2H 1, 2 benzothiazine 3 formamide 1, 1 dioxide. The content of C 15H 13N3O4S shall not be less than 98.5% in terms of dry products.
4.5 Properties This product is white to yellow-green crystalline powder; Odorless and tasteless.
This product is soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or ether, and almost insoluble in water; Soluble in acid, slightly soluble in alkali.
4.5. 1 melting point The melting point of this product (Appendix VI C of Pharmacopoeia II, 20 10) is 198 ~ 202℃, and it decomposes at the same time when it melts.
4.6 Identification (1) Take about 30mg of this product, add 1ml chloroform to dissolve it, and add 1 drop of ferric chloride test solution, which is rosy.
(2) Take this product, add 0.0 1mol/L hydrochloric acid methanol solution to dissolve and dilute it, make a solution containing 5μg per 1ml, and determine it by UV-Vis spectrophotometry (Appendix Ⅳ a of Pharmacopoeia Part II, 20 10 edition), with maximum absorption at wavelengths of 243nm and 334nm.
(3) The infrared absorption spectrum of this product should be the same as that of the reference substance (drug infrared spectrogram 188).
4.7 Check 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 an appropriate amount, add chloroform, and dilute quantitatively into a solution containing 0.2mg per 1ml as a control solution. According to the test of thin-layer chromatography (appendix ⅴ b of Pharmacopoeia Part II, 20 10), the above two solutions 10μl were absorbed on the same silica gel GF254nm thin-layer plate (with the mixed solution of 0.5% sodium carboxymethyl cellulose and 1mol/L sodium hydroxide solution as the adhesive). If the test solution shows impurity spots, it must not be deeper than the main spots shown in the control solution.
4.7.2 Take 2g of anhydrous sodium carbonate chloride, spread it on the bottom and around the crucible, take 1.0g of this product, put it on anhydrous sodium carbonate, moisten it with a little water, dry it, first burn it with a small fire until it is completely ashed, let it cool, add a proper amount of water to dissolve it, filter it, wash the crucible with water and filter it, combine the filtrate and lotion, add water to make it 20ml, shake it evenly, and take the filtrate. Add 1 drop nitric acid, shake well, put it in a water bath at 75 ~ 85℃, remove hydrogen sulfide, let it cool, add 1% sodium carbonate solution dropwise to neutrality, add water to make the volume to 25ml, check according to the law (Appendix VIII A of Pharmacopoeia II, 20 10), and make the volume to 5.0ml standard sodium chloride solution.
4.7.3 loss on drying takes this product and dries it to constant weight at 105℃, and the weight loss shall not exceed 0.5% (Appendix VIII L of Pharmacopoeia II, 20 10).
4.7.4 Take this product 1.0g as residue on ignition, and check it according to law (Appendix VIII N of Pharmacopoeia II, 20 10), and the residue shall not exceed 0. 1%.
4.7.5 Take the residue left under the heavy metal residue on ignition and check it according to law (the second method in Appendix VIII H of Pharmacopoeia 20 10), and the content of heavy metals shall not exceed 10 parts per million.
4.7.6 Arsenic salt should take 65,438+00 ml of the residual solution under the above chloride inspection, add 5ml of hydrochloric acid and 65,438+03 ml of water, and be inspected according to law (the first method in Appendix VIII J of Pharmacopoeia II, 2065,438+00 edition), which should meet the requirements (0.0004%).
4.8 Content determination Take about 0.2g of this product, weigh it accurately, add 20ml glacial acetic acid to dissolve it, add 1 drop crystal violet indicator, titrate the solution with perchloric acid (0. 1mol/L) until it turns blue-green, and correct the titration result with blank test. Every 1ml perchloric acid titration solution (0. 1mol/L) is equivalent to 33. 14mg of c15h13N3O4 S.
Class 4.9 Non-steroidal anti-inflammatory drugs for antipyretic and analgesic purposes.
4. 10 storage and shading, sealed preservation.
4. 1 1 preparation (1) piroxicam tablets? (2) Piroxicam Ointment? (3) Piroxicam injection? (4) Piroxicam capsules? (5) Piroxicam gel
4. 12 Edition People's Republic of China (PRC) Pharmacopoeia 20 10 Edition
5 Standards promulgated by the Ministry of Chemical Industry 5. 1 Pinyin name Piluoxikang
5.2 English name PIROXICAMUM
5.3 standard number c15h13N3O4S331.35.
5.4 The source of this product is 2 methyl 4 hydroxy N(2 pyridyl) 2H 1, 2 benzothiazine 3 formamide 1, 1 dioxide. The content of C 15H 13N3O4S shall not be less than 98.5% in terms of dry products.
5.5 Properties This product is white or yellow-green crystal or crystalline powder; Odorless and tasteless. This product is soluble in chloroform, slightly soluble in acetone, slightly soluble in ethanol or ether, almost insoluble in water, soluble in acid and slightly soluble in alkali. Melting point This product (China Pharmacopoeia 1990 Edition, Appendix 15) has a melting point of 198 ~ 202℃, which is decomposed at the same time when it is melted.
5.6 Identification (1) Take about 30mg of this product, add 1ml chloroform to dissolve it, and add 1 drop of ferric chloride test solution, which is rosy.
(2) Take this product, add methanol solution of hydrochloric acid (0.0 1mol/L) to make a solution containing 5μg per 1ml, and determine it by spectrophotometry (China Pharmacopoeia 1990, Appendix 24), with the maximum absorption at wavelengths of 243 and 334nm.
(3) The infrared absorption spectrum of this product should be consistent with the reference spectrum (infrared spectrum setting 188).
5.7 Check the related substances, take this product, add chloroform to make a solution containing 20mg per 1ml as the test solution; Accurately measure an appropriate amount, add chloroform and dilute it into a solution containing 0.2mg per 1ml as a control solution. According to the test of thin-layer chromatography (China Pharmacopoeia 1990 Edition, Appendix 30), absorb the above two solutions 10μl and spot them on the same silica gel GF.
5.8 Content determination takes about 0. Take 2g of this product, accurately weigh it, add 20ml glacial acetic acid to dissolve it, add 1 drop crystal violet indicator, titrate with perchloric acid solution (0. 1mol/L) until the solution turns blue-green, and correct the titration result with blank test. Every 1ml perchloric acid solution (0. 1mol/L) is equivalent to 33. 14mg of C 15H 13N3O4S.
5.9 Functions and uses of anti-inflammatory and analgesic drugs. Can be used for treating rheumatoid arthritis and rheumatoid arthritis.
5. 10 Usage and dosage: acute gout 20mg, acute gout 40mg after meals for 4 ~ 6 days, not suitable for long-term use.
5. 1 1 Pay attention to the allergic reaction of this product, and it is forbidden for patients with gastric and duodenal ulcers; Not suitable for pregnant women and children.
5. 12 Keep it in a light-proof seal.
5. 13 preparation (1) piroxicam tablets
(2) Piroxicam Capsule Note: A drug called Tongyan Xikang was used.
Liaoyuan No.1 Factory of Kaifeng Pharmaceutical Factory drafted the audit of Henan Institute for Drug Control and Jilin Institute for Drug Control.
6 Instructions for Piroxicam 6. 1 Drug Name Piroxicam
6.2 English name of piroxicam, DP 16 17 1, Feldene.
6.3 The alias of piroxicam is Tong Yan Xi Kang; Pyroxethiazine; Feiding; Anerke; Shipcon feldne
6.4 classification of nervous system drugs >: antipyretic and analgesic nonsteroidal anti-inflammatory drugs
6.5 dosage form 1. Tablets: 20mg each;
2. Capsule: 10mg, 20mg；;
3. Injection: 1 0mg (1ml), 20mg (2ml);
4. Gel: 0.50%;
5. Bolt: 20 mg.
6.6 pharmacological effects of piroxicam piroxicam is a long-acting anti-inflammatory and analgesic drug with enol structure. Animal experiments have proved that it has broad-spectrum anti-inflammatory effect, can eliminate erythema and edema, and has inhibitory effect on the formation of tissue granuloma and adjuvant arthritis. In vitro, piroxicam can inhibit phagocytosis, release of lysosomal hydrolase and platelet aggregation. Piroxicam does not inhibit the spasticity of histamine, serotonin, ethambutol or prostaglandin, but it is a powerful inhibitor of prostaglandin synthesis, and this inhibition is reversible. Piroxicam also has analgesic effect. In the animal model simulating human gout, it can not only reduce inflammation and edema, but also inhibit inflammatory leukocytosis. Piroxicam is a derivative of Oxicam. Piroxicam is a new long-acting non-steroidal anti-inflammatory drug, and its mechanism is related to the inhibition of prostaglandin synthesis.
6.7 After oral administration, the pharmacokinetics of piroxicam is rapidly absorbed and can be detected in blood after 30 minutes. The binding rate of TMAX to plasma protein was 99%. Vd0. 12~0. 14L/kg, t 1/236~45h, 20mg daily, reaching the plasma peak for 5 ~ 7 consecutive days, with a Cmax of 3 ~ 5 μ g/ml. It won't accumulate. Once the drug is stopped for one day, the plasma concentration will not drop below the therapeutic range. Piroxicam is metabolized slowly and widely in the body, with intestinal and liver circulation, and more than 90% of it is metabolized. 66% is excreted by kidney, 33% by feces, and most metabolites, only < 5% are prototypes. Renal function damage will not significantly change its dynamic process. A small amount of hydroxylated piroxicam may be found in the plasma of patients who take piroxicam for a long time. The absorption of piroxicam is not affected by food, iron and antacids, and anticoagulant or aspirin does not affect the protein binding rate of piroxicam.
6.8 Indications of piroxicam: acute and chronic rheumatoid arthritis, proliferative osteoarthropathy, ankylosing spondylitis, chronic strain low back pain, scapulohumeral periarthritis, postoperative and post-traumatic pain and acute gout. Piroxicam can not change the progression of rheumatoid arthritis, nor can it correct hyperuricemia of gout. Not suitable for chronic gout.
Contraindications of piroxicam 1. Children who are allergic to piroxicam or other non-steroidal anti-inflammatory drugs are prohibited.
2. Those with a history of gastrointestinal bleeding or ulcer are prohibited.
3. People with cardiac and renal insufficiency are prohibited.
6. 10 Precautions 1. Use with caution in patients with hemorrhagic ulcer, ulcer, patients with ulcer history and patients with hepatic and renal insufficiency.
2. Coagulation mechanism or platelet dysfunction should be used with caution.
3. Pregnant women and lactating women and children should not use it.
4. the dosage is small, 20mg per day, and the steady-state blood concentration will be reached in 4 ~ 4 days. It is reported that its curative effect is better than that of indomethacin, ibuprofen and naproxen. Long-term use of large doses or more than 20mg per day can lead to gastric ulcer and massive bleeding. Blood routine and liver and kidney function should be checked when taking it. Pay attention to the change of stool color. When necessary, a fecal occult blood test should be carried out.
5. Piroxicam can have cross-allergic reaction with aspirin.
6. Drinking alcohol at the same time or combining with other non-steroidal anti-inflammatory drugs will increase adverse reactions.
7. Adverse reactions are mild, with occasional dizziness, edema, stomach discomfort, diarrhea or constipation, granulocytopenia, aplastic anemia, etc. Generally, it can disappear by itself after stopping the drug.
6. 1 1 piroxicam 1 Adverse reactions. Gastrointestinal reactions include nausea, vomiting, stomach upset, abdominal pain, diarrhea and constipation; It can also cause peptic ulcer and gastrointestinal bleeding.
2. Piroxicam can inhibit platelet aggregation and prolong bleeding time.
3. Other adverse reactions include dizziness, headache, lethargy and edema; Occasionally nosebleeds, granulocytopenia, abnormal liver function. A few patients may have elevated blood non-protein nitrogen levels.
6. Usage and dosage of 1 2 piroxicam1 Anti-rheumatism, daily 1 time, 20mg each time, taken in the morning. Acute gout, 1 time/day, 40mg, 4 ~ 6 days.
2. intramuscular injection: daily 1 time, 10 ~ 20 mg.
3. Suppository: 20mg/d anal suppository.
6. 13 drug interaction 1. See indomethacin.
2. Piroxicam should not be combined with aspirin. Aspirin can reduce the plasma concentration of piroxicam by 80%.
3. The antiviral drug ritonavir can increase the plasma concentration of piroxicam and increase its toxicity.
4. The combination of dicoumarin and other anticoagulants can increase the effect of the latter, so the dosage should be adjusted.
6. 14 Expert comments: Piroxicam is used to treat rheumatoid arthritis. Taking 20mg every day 1 day can relieve pain and improve sleep, reaching the peak on the sixth day. After drug withdrawal, the pain and sleep improvement can last for 48 hours. Treatment of ankylosing spondylitis, 20mg per day, 80% patients' exercise ability has been improved, and the effect is better than indomethacin. Piroxicam is easily tolerated, the incidence of adverse reactions is lower than that of aspirin and indomethacin, and the withdrawal symptoms are lighter than that of the latter. However, if the daily dosage exceeds 20mg, the incidence of gastrointestinal symptoms and ulcers will greatly increase. Piroxicam can not change the progression of rheumatoid arthritis, nor can it correct hyperuricemia. It can only improve clinical symptoms such as pain relief and sleep improvement.
7 piroxicam poisoning piroxicam (yantongxikang) is a powerful anti-inflammatory and analgesic drug, which plays a role by inhibiting cyclooxygenase to reduce prostaglandin synthesis, leukocyte chemotaxis and lysosomal enzyme release. Is suitable for treating acute and chronic rheumatic arthritis and ankylosing spondylitis. Its curative effect is better than that of indomethacin, ibuprofen and naproxen. The plasma concentration reached its peak 2 hours after oral administration, and the plasma half-life was 3 1 ~ 57 hours. The protein binding rate is more than 90% and the half-life is 45 hours. It is mainly metabolized by the liver, of which 66% is excreted by the kidney and feces in the form of hydroxylate and glucuronic acid, and the original drug accounts for 5% in urine and feces. [ 1]
7. 1 clinical manifestations [2]
Adverse reactions: dizziness, tinnitus, nausea, vomiting, abdominal pain, diarrhea, gastric perforation, upper gastrointestinal bleeding; Chest tightness, low back pain, proteinuria, hematuria and transient transaminase elevation.
2. Severe cases: disturbance of consciousness, convulsion, respiratory depression, shock and death.
3. Urticaria-like drug eruption, purpura-like drug eruption and anaphylactic shock. Occasionally thrombocytopenic purpura, granulocytopenia, etc.
4. Extrapyramidal symptoms: salivation, hemifacial spasm, spastic torticollis, etc.
7.2 treatment of piroxicam poisoning treatment points for [2]:
1. Besides inducing vomiting, gastric lavage and catharsis, people in shock should be rescued.
2. Patients with gastric perforation should undergo surgery.
3. Allergic patients are treated with antihistamines and glucocorticoids.
4. Extrapyramidal symptoms can be treated with scopolamine.