1.2 English names diclofenac, diclofenac sodium, Catalam, dichromate, Kriplex, Voltaren.
1.3 sodium dichloroaniline acetate; Good interest; Dichloroacetamide; Amirel; Orfin; Treatment of Cofina; Dick Luck; Sodium dihydrofenac; Non-inflammatory; Protect his forest; Bega; Diclofenac sodium; Diclofenac; Ying Taiqing; Diclofenac sodium; Take his spirit; Divenah Voltelyn; Coveland; Novotel; Tianxin lide; Yingtaiqing capsule; Blesin diclofenac; diclofenac sodium
1.4 classification of nervous system drugs >: antipyretic and analgesic drugs > others
1.5 dosage form 1. Tablets 25 mg, 50 mg, 75 mg; ;
2. Sustained release capsules:100 mg; ;
3. Injection: 75mg；;
4. Ointment:10 mg; ;
5. Latex agent: 1%,10 mg; ;
6. Suppository: 25 mg, 50 mg, 100 mg.
7. Eye drops: 0. 1%.
Pharmacological action of diclofenac sodium 1.6 The mechanism of diclofenac sodium is to selectively cut off the action link of cyclooxygenase in arachidonic acid metabolism series and block the synthesis pathway of prostaglandin E2(PGE2). Inhibit its mutagenic and pain effects. Diclofenac sodium is an anti-inflammatory and analgesic drug of phenylacetic acid, which has obvious anti-rheumatism, anti-inflammatory, analgesic and antipyretic effects. Its effect is 2 ~ 2.5 times stronger than that of indomethacin and 26 ~ 50 times stronger than that of aspirin. It is characterized by strong drug effect, light adverse reaction, small dosage and small individual difference. Diclofenac sodium has obvious anti-rheumatism, analgesic, anti-inflammatory and antipyretic effects. Can relieve joint pain, improve joint mobility, and has good tolerance. Diclofenac sodium tablets have an antiallergic coating, which enables the active substances in the tablets to be released after leaving the stomach. So it can be used for patients with stomach sensitivity. Taking diclofenac sodium 75 ~ 150 mg orally every day has similar analgesic and anti-inflammatory effects on rheumatoid arthritis, osteoarthritis and ankylosing spondylitis as aspirin, ibuprofen, indomethacin, ketoprofen and naproxen. Many studies have proved that diclofenac sodium has a strong inhibitory effect on the collapse of blood-aqueous barrier caused by mechanical, chemical and biological factors. In recent years, it has been found that diclofenac sodium can reduce corneal perception and sensitivity, showing the effect of corneal analgesia, and its detailed mechanism is still unclear.
Pharmacokinetics of diclofenac sodium 1.7 Diclofenac sodium solution can be absorbed rapidly by oral administration, rectal suppository or intramuscular injection. When enteric-coated tablets are used, especially when taken with food, absorption tends to be slow. Although diclofenac sodium was absorbed rapidly and completely by oral administration, it reached the peak of blood drug in 2 hours, but the first-pass metabolism was obvious, and only 50% of the drug entered the systemic circulation. Diclofenac sodium is also absorbed through the skin. At the therapeutic concentration, the protein binding rate is higher than 99%. It can penetrate into synovial fluid and keep it until the blood concentration drops. It can be distributed in breast milk, but the amount is too low to bring harm to breast-fed babies. The terminal plasma t 1/2 is about 1 ~ 2h. The main metabolite is sodium hydroxydiclofenac, which is excreted with urine and bile after glucuronic acid is combined with sulfuric acid. Healthy subjects were given diclofenac sodium 100mg, Cmax4485ng/ml, tmax 1.2h, t 1/2 1.33h and ke 0.56h. Intramuscular injection of 75mg, Cmax2.73μg/ml, tmax25.3min. Local application of diclofenac sodium has good intraocular permeability, and the drug retention time in aqueous humor is about three times that of flurbiprofen, which may be due to the accumulation of diclofenac by cornea.
Indications 1.8 diclofenac sodium is clinically used for rheumatoid arthritis, ankylosing spondylitis and osteoarthropathy, and is suitable for all kinds of moderate pain, such as postoperative and post-traumatic pain, acute musculoskeletal diseases, etc. And fever caused by various inflammations. It is also used for acute gout and cancer, soft tissue injury and postoperative pain. Can be used for preventing pupil contraction during cataract extraction and treating postoperative inflammation. Anti-infective treatment of non-infectious inflammation in ophthalmology, including non-infectious inflammation caused by surgical and non-surgical factors, such as uveitis, keratitis, scleritis, episcleritis, etc. Inhibit corneal neovascularization; Inhibition of inflammatory pupillary constriction in cataract surgery: prevent postoperative inflammatory reaction and cystoid macular edema, and promote the formation of filtering blebs after glaucoma filtering surgery; It is also effective for allergic conjunctivitis.
Contraindications of diclofenac sodium 1.9 1. Patients with active peptic ulcer or ulcer, bleeding, perforation and other serious digestive diseases caused by diclofenac sodium in the past;
2. Asthma, urticaria and allergic rhinitis caused by salicylic acid or other prostaglandin synthase inhibitors.
3. It is forbidden for people who are allergic to diclofenac sodium or other non-steroidal anti-inflammatory drugs (NSAIDs).
1. 10 Note 1. (1) asthma; (2) Cardiac insufficiency and hypertension. Water retention and edema can be caused by drugs; (3) Hemophilia or other hemorrhagic diseases (including coagulation disorders and abnormal platelet function). Because the bleeding time is prolonged after medication, the bleeding tendency is aggravated; (4) History of digestive tract ulcer. Adverse gastrointestinal reactions, including new ulcers, are easy to occur after taking the medicine; (5) History of rash; (6) urticaria; (7) hepatic porphyria; (8) Loss of extracellular fluid; (9) lactating women; (10) Renal insufficiency;
2. Because of the increase of renal adverse reactions after medication, and even lead to renal failure, especially in the elderly, liver and kidney function should be routinely followed up during medication.
3. Those who have potential damage to liver and kidney function and long-term drinkers should also pay close attention to the changes of liver and kidney function when taking diclofenac sodium.
4. Long-term use of diclofenac sodium should monitor liver, renal function and hemogram as preventive measures.
5. Diclofenac sodium is not suitable for simple fever.
6. It is best to take diclofenac sodium before meals. 50m *** is not suitable for children.
7. Diclofenac sodium and mydriatic agent should not be used at the same time, and glaucoma patients should stop dripping mydriatic agent 3 hours before operation.
Diclofenac sodium 1. 1 1 Adverse reactions. Gastrointestinal discomfort (such as abdominal pain, nausea, vomiting, diarrhea, etc.). ), headache, dizziness, dizziness, erythema or rash on the skin.
2. Rare: gastrointestinal bleeding, peptic ulcer, lethargy, abnormal liver function (including icteric hepatitis), edema, allergic reaction (such as urticaria, rash, bronchospasm, etc. ) or allergic reactions, including hypotension.
3. Individual cases: sensory or visual impairment (blurred vision, diplopia), tinnitus, insomnia, irritability, convulsions; Herpes, eczema, erythema multiforme, Lyle syndrome, alopecia, photosensitive reaction, etc. Acute renal insufficiency, abnormal urine (such as hematuria), interstitial nephritis, nephrotic syndrome; Thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia and aplastic anemia; Fulminant hepatitis
4. There may be slight tingling and burning sensation after local use, and it will disappear automatically after 1min without treatment.
1. 12 usage and dosage of diclofenac sodium 1. 25mg each time, three times a day, the whole tablet is taken with water.
2. Insertion of suppository: 50 mg each time, twice a day.
3. Intramuscular injection: 75mg each time, once a day 1 time, and deep injection into gluteus muscle, after several hours if necessary 1 time.
4. Children, 1 ~ 3mg/kg/ day. Swallow it whole.
5. Ophthalmic medication: (1) to prevent pupil contraction during cataract extraction, and drop eyes 4 times within 2 hours before operation, each time 1 drop; (2) To treat postoperative inflammation of cataract, apply 1 drop 24 hours after operation, four times a day, and the course of treatment is 10 ~ 14 days. (3) Before ophthalmic surgery: generally 4 times before surgery (3h, 2h, 1h, 30min); (4) After ophthalmic surgery: 1 ~ 4 times a day, each time 1 drop; (5) Other non-surgical anti-inflammatory purposes: 1 drop, 4-6 times a day.
1. 13 drug interaction 1. When diclofenac sodium is combined with lithium salt or digoxin, the plasma concentration of the latter two drugs can be increased.
2. When combined with non-steroidal anti-inflammatory drugs or glucocorticoids, it may increase adverse reactions.
3. Combined with aspirin, the blood concentration of diclofenac sodium can be reduced.
4. When combined with potassium-preserving diuretics, the serum potassium level may increase, so attention should be paid to monitoring.
5. When combined with oral anticoagulants, relevant laboratory tests should be done to ensure the curative effect and medication safety.
6. Taking diclofenac sodium within 24 hours before and after using methotrexate, it should be observed that the blood concentration of methotrexate may increase and its toxicity may increase.
1. 14 expert comments