The main component of this product is diclofenac sodium.
Traits
This product is a colorless or almost colorless clear liquid.
Indications
This product is used for pain caused by rheumatism, rheumatoid arthritis, adhesive spondylitis, non-inflammatory joint pain, vertebral arthritis, non-articular rheumatism, etc.
Specification
2ml: 50mg.
Dosage
Deep intramuscular injection, 50mg once, 2-3 times a day.
Adverse reactions
1. Common gastrointestinal reactions, such as stomach upset, burning sensation, acid reflux, anorexia, nausea, etc., can disappear after stopping the drug or treating symptomatically.
2. Long-term application may cause gastric ulcer, gastric bleeding, and gastric perforation.
3. A small number of patients have edema, oliguria, and electrolyte disturbances.
4. Occasionally nervous system reactions (incidence rate <1%), such as headache, dizziness, drowsiness, excitement, etc.
5. Swelling and pain at the injection site.
Taboo
1. Those who are allergic to aspirin or other non-steroidal anti-inflammatory drugs or have a history of asthma are contraindicated.
2. It is forbidden for pregnant women and breastfeeding women.
Precautions
1. This product is a non-causal treatment drug, and it cannot control the course of chronic arthritis.
2. Use with caution if there is a history of peptic ulcer or ulcer bleeding.
3. Use with caution in patients with liver and kidney damage or ulcers. Especially the elderly. During medication, liver and kidney functions should be checked regularly.
4. Because this product contains sodium, it should be used with caution in patients who restrict sodium intake.
5. Interference with diagnosis: This product can cause a transient increase in serum aminotransferase, a decrease in serum uric acid content, and an increase in uric acid content.
6. If gastrointestinal bleeding, liver and kidney function damage, visual disturbance, abnormal blood picture, and allergic reactions occur during medication, the medication should be discontinued.
medicine interactions
1. It can cause hyperkalemia when used with potassium-sparing diuretics.
2. Aspirin can reduce the bioavailability of this product.
3. It may increase the risk of bleeding when used together with anticoagulants such as heparin and dicoumarin and platelet aggregation inhibitors.
4. When used with furosemide, the sodium excretion and hypotensive effect of the latter is weakened.
5. When used together with verapamil and nifedipine, the blood concentration of this product will increase.
6. This product can increase the blood concentration of digoxin, and attention should be paid to adjusting the dose of digoxin when using it together.
7. When this product is used together with antihypertensive drugs, it can affect the antihypertensive effect of the latter.
8. Probenecid can reduce the excretion of this product, increase the blood concentration, thereby increasing the toxicity, so it is advisable to reduce the dose of this product when using it at the same time.
9. This product can reduce the excretion of methotrexate, increase its blood concentration, and even reach toxic levels, so this product should not be used with medium or large doses of methotrexate.
10. This product can reduce the effect of insulin and other hypoglycemic drugs, and increase blood sugar.
11. Drinking alcohol or using it together with other non-steroidal anti-inflammatory drugs increases gastrointestinal adverse reactions and may cause ulcers. Long-term use with acetaminophen can increase the toxic and side effects on the kidneys.
12. When used with aspirin or other salicylic acid drugs, the efficacy is not enhanced, but the incidence of gastrointestinal adverse reactions and bleeding tendency increases.
Overdose
Excessive doses may cause liver toxicity symptoms caused by diclofenac sodium and acetaminophen, and liver-protecting antidote acetylcysteine should be given as soon as possible.
Pharmacological action
Diclofenac sodium is a non-steroidal anti-inflammatory analgesic derived from phenylacetic acid. Its mechanism of action is to inhibit the activity of cyclooxygenase, thereby blocking the conversion of arachidonic acid to prostaglandins. At the same time, it can also promote the combination of arachidonic acid and triglycerides, reduce the concentration of free arachidonic acid in cells, and indirectly inhibit the synthesis of leukotrienes. Diclofenac sodium is one of the more powerful non-steroidal anti-inflammatory drugs. Its inhibitory effect on prostaglandin synthesis is stronger than that of aspirin and indomethacin.
Toxicological effects
Rats were given oral diclofenac sodium 2 mg/kg daily, and long-term observation did not find an increase in the incidence of tumors. In a two-year study on mice, with a daily medication of 2 mg/kg, no tumor-prone tendency was seen. Various mutation studies have not found that diclofenac sodium induces gene mutations. The rats were given 4mg/kg daily, and neither male nor female had infertility. Acute toxicity test results: rat oral LD50 is 150mg/kg; mouse oral LD50 is 390mg/kg.
Pharmacokinetics
After intramuscular injection of this product, the plasma protein binding rate is 99.5%, about 50% is metabolized in the liver, 40-65% is excreted from the kidney, and 35% is excreted from the bile and feces.
storage
Keep away from light and airtight.
Valid period
24 months
Executive standard
National Food and Drug Administration Drug Standard WS-10001-(HD-0159)-2002.
Identify
1. Take this product and add water to make a solution containing 20mg per 1ml. According to spectrophotometry (Chinese Pharmacopoeia 2000 Edition Two Appendix IVA), there is a maximum absorption at a wavelength of 276nm.
2. Take 2ml of this product (approximately equivalent to 50mg of diclofenac sodium) and evaporate it on a water bath, add 0.2g of sodium carbonate, mix well, heat to complete carbonization, let cool, add 5ml of water to boil, filter, the filtrate shows chloride The identification reaction (Chinese Pharmacopoeia 2000 edition two appendix III).
3. Take 2ml of this product, evaporate it in a water bath, and burn it to show the identification reaction of sodium salt (Appendix III of Chinese Pharmacopoeia 2000 Edition).
an examination
1. pH value: should be 7.5-9.0 (Chinese Pharmacopoeia 2000 edition two appendix VIH).
2. Related substances: Take 1-(2,6-dichlorophenyl)-2-oxindole and use ethanol to make a solution containing 0.5mg per 1ml as a reference solution. According to thin-layer chromatography (Chinese Pharmacopoeia 2000 edition two appendix VB) test. Take 10ml of this product and 3ml of the control solution and place them on the same silica gel GF254 thin-layer plate. Use benzene-chloroform-glacial acetic acid (15:15:0.1) as the developing agent. After unfolding, let it dry and inspect under UV light at 254nm. , If the test solution shows impurity spots, it should not be deeper (0.6%) compared with the spots of the reference solution.
3. Others: it should comply with the relevant regulations under the injections (Chinese Pharmacopoeia 2000 Edition, Appendix IB).
Assay
1. Precisely measure an appropriate amount of this product (approximately equivalent to 50mg of diclofenac sodium), put it in a 100ml measuring flask, add ethanol to dilute to the mark, shake well, accurately measure 2ml, place in a 100ml measuring flask, add ethanol to dilute to the mark, shake Evenly, according to the spectrophotometric method (Chinese Pharmacopoeia 2000 edition two appendix IVA), the absorbance was measured at a wavelength of 284nm; in addition, 50mg of the reference substance of diclofenac sodium dried at 105ºC to constant weight was accurately weighed, measured in the same way, calculated, Immediately.
2. This product is a sterile aqueous solution of diclofenac sodium. Containing diclofenac sodium (C14H10Cl2NNaO2) should be 93.0%-107.0% of the labeled amount.
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