What Is Diclofenac?

Diclofenac is a non-steroidal anti-inflammatory drug. It has anti-inflammatory, analgesic and antipyretic effects. For rheumatoid arthritis, adhesive spondylitis, non-inflammatory arthralgia, arthritis, non-articular rheumatism, pain caused by non-articular inflammation, various neuralgia, cancer pain, post-traumatic pain and various inflammations Caused by fever and so on. For some animals, it is toxic, such as vultures.

Chinese name: Meclofenamic acid
English name: Diclofenac
nickname: 2-[(2,6-dichlorophenyl) amino] phenylacetic acid
Chemical formula: C14H11Cl2NO2

Molecular weight: 296.15
CAS Registry Number: 644-62-2
Melting point: 156-158
Application: Cancer pain medicine
Ingredients: Diclofenac sodium 50mg

Introduction of Diclofenac Compounds

Diclofenac Basic Information

Chinese name: diclofenac

Chinese alias: 2- (2,6-dichloroaniline) phenylacetic acid; sodium dichloroaniline acetate; Diazepam; diclofenac; Amirel; Olfen; oxafina; dicloxacin; dihydrofen Sodium; Non-inflammatory; Hutalin; Jiabei; Sodium diclofenac; Sodium diclofen; Indocyanine; Sodium diclofenac; Futalin; Differner; Futalin; Kaifulan; Norfodine Tianxin Lide Yingtaiqing Capsule

English name: diclofenac

English alias: 2- (2-((2,6-dichlorophenyl) amino) phenyl) acetic acid; Diclofenac acid; 2-[[2,6-Dichlorophenyl] amino] benzeneacetic acid; Blesin; Diclofe; Diclofenac

CAS number: 15307-86-5

Molecular formula: C ₁₄ H ₁₁ Cl ₂ NO ₂

Molecular weight: 296.14900

Exact mass: 295.01700

PSA: 49.33000

LogP: 4.43710

Physical and Chemical Properties of Diclofenac

Appearance and properties: white to light yellow crystalline powder

Density: 1.431 g / cm ³

Melting point: 156-158ºC

Diclofenac

Boiling point: 412ºC at 760 mmHg

Flash point: 203ºC

Refractive index: 1.66

Vapor pressure: 1.07E-09mmHg at 25 ° C

Diclofenac Safety Information

Packing level: III

Hazard category: 6.1 (b)

Customs code: 2942000000 ^[1]

Diclofenac Drug Description

Diclofenac dosage form

1. Tablets 25mg, 50mg, 75mg;

2. Sustained-release capsule: 100mg;

3. Injection: 75mg;

4. Ointment: 10mg;

5. Latex: 1%, 10mg;

6. Suppositories: 25mg, 50mg, 100mg;

7. Eye drops: 0.1%.

Diclofenac pharmacological action

The mechanism of diclofenac is to selectively cut off the action of cyclooxygenase in the arachidonic acid metabolism series and block the pathway of prostaglandin E2 (PGE2). Suppresses its mutagenic and pain-causing effects. Diclofenac is a phenylacetic acid anti-inflammatory analgesic and has significant anti-rheumatic, anti-inflammatory, analgesic and antipyretic effects. Its effect is 2 to 2.5 times stronger than indomethacin, and 26 to 50 times stronger than aspirin. It is characterized by strong efficacy, light adverse reactions, small doses, and small individual differences. Diclofenac has significant antirheumatic, analgesic, anti-inflammatory and antipyretic effects. Can well relieve joint pain and improve its activity, and is well tolerated. Diclofenac tablets have an anti-allergy coating that allows the active substance in the tablet to be released after it leaves the stomach, so it can be used in patients with sensitive stomachs. Diclofenac is administered orally 75 to 150 mg per day, and its analgesic and anti-inflammatory effect on rheumatoid arthritis, osteoarthritis and articular spondylitis is similar to aspirin, ibuprofen, indomethacin, ketoprofen, naproxen and the like. Many studies have proven that diclofenac has a strong inhibitory effect on the breakdown of the blood-aqueous aqueous barrier caused by mechanical, chemical, and biological stimuli. In recent years, studies have found that diclofenac can reduce the perception and sensitivity of the cornea, showing the effect of corneal analgesia, and the detailed mechanism is not clear ^[2] .

Diclofenac pharmacokinetics

Diclofenac oral solution, rectal suppositories, or intramuscular injection of diclofenac can be quickly absorbed. When using enteric tablets, especially when taken with food, absorption tends to be slow. Although oral diclofenac was absorbed quickly and completely, and reached the peak blood level in 2 hours, the first pass metabolism was obvious, and only 50% of the drugs entered the systemic circulation. Diclofenac is also absorbed transdermally. At the therapeutic concentration, the protein binding rate was higher than 99%. It can penetrate into the synovial fluid and can be kept until the blood concentration decreases. Can be distributed into breast milk, but in low amounts so as not to cause harm to the nursing infant. The terminal plasma t1 / 2 is about 1 to 2 hours. The main metabolite is diclofenac. The metabolite glucuronic acid and sulfuric acid are excreted with urine and bile. Healthy subjects took diclofenac 100 mg orally, C _max 4485ng / ml, t _max 1.2h, t _1/2 1.33h, and Ke 0.56 per hour. 75 mg intramuscularly, C _max 2.73 g / ml, t _max 25.3 min. Diclofenac has good intraocular permeability in local eye drops, and the drug retention time in aqueous humor is longer, about three times that of flurbiprofen. The reason may be that the cornea has a certain accumulation of diclofenac ^[3] .

Diclofenac indication

It is clinically used for rheumatism and rheumatoid arthritis, ankylosing spondylitis, osteoarthropathy, and is suitable for all kinds of moderate pain, such as post-operative and post-traumatic pain, acute muscle-skeletal disease; and fever caused by various inflammations Wait. It is also used for acute gout and cancer, soft tissue damage, and pain after surgery. It is used to prevent intraocular pupil shrinkage and treat postoperative inflammation during cataract extraction. 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, episcleral inflammation; inhibition of corneal neovascularization; inhibition of inflammation during cataract surgery Spontaneous pupillary reaction; prevention of postoperative inflammatory response and macular cystoid edema formation, and can promote the formation of filter blebs after glaucoma filtering surgery; also has a therapeutic effect on allergic conjunctivitis.

Diclofenac contraindications

1. People with active peptic ulcer, or those who have had severe digestive tract lesions such as ulcers, bleeding and perforation caused by diclofenac in the past;

2. Asthma attacks, urticaria, and allergic rhinitis induced by salicylic acid or other prostaglandin synthase inhibitors.

3. Prohibited for those allergic to diclofenac or other non-steroidal anti-inflammatory drugs (NSAIDs).

Enteric-coated tablets are used to treat :

Inflammatory and degenerative rheumatism, such as rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, osteoarthropathy and spinal arthritis.

drug

Non-articular rheumatism.

Acute onset of gout.

trauma and postoperative inflammatory pain and swelling, gynecological pain or inflammation.

Adjuvant treatment of severe painful infections of ears, nose and throat.

Latex is used for local treatment of the following diseases :

Traumatic inflammation of tendons, ligaments, muscles and joints, such as sprains, strains and contusions.

Limited soft tissue inflammation, such as tenosynovitis and bursitis.

Limited rheumatic diseases, such as osteoarthropathy of the limbs and spine, and lesions around the joints.

Diclofenac Usage and Dosage

1. 25mg each time, 3 times a day, send the whole tablet with water.

2. Anal insertion of suppository: 50mg each time, 2 times a day

Diclofenac .

3. Intramuscular injection: 75mg each time, once a day, deep gluteal muscle injection, and another injection after a few hours if necessary.

4. Children, 1 to 3 mg / kg daily. Swallow the entire tablet.

5. Ophthalmic medication: (1) prevent pupil shrinkage during cataract extraction, 4 eye drops within 2 hours before surgery, 1 drop each time; (2) treatment of inflammation after cataract removal, eye drops started 24 hours after surgery, each time 1 Drops, 4 times a day, continuous treatment for 10 to 14 days. (3) Before ophthalmic surgery: generally 4 times before surgery (before 3h, 2h, 1h, 30min); (4) After ophthalmic surgery: 1 to 4 times a day, 1 drop each time; (5) Other non-surgical Anti-inflammatory: 4 to 6 times a day, 1 drop each time.

Diclofenac precautions

(1) Common adverse reactions are gastrointestinal reactions such as diarrhea, nausea and abdominal pain. Others still have heartburn, anorexia, flatulence, vomiting, constipation, stomatitis, and gastric ulcers, so it should not be used as the first choice. In addition, it can cause headache, dizziness, rash, edema, urticaria, pruritus, tinnitus, palpitations, fatigue, paresthesia, insomnia, depression, nocturia, and taste disorders.

(2) There may be cross-sensitivity with aspirin and other non-steroidal anti-inflammatory drugs, so it is not suitable for patients with bronchospasm, allergic rhinitis or urticaria caused by the above drugs.

(3) Not suitable for pregnant women, lactating women and children.

(4) Not suitable for use with aspirin.

(5) The effect of warfarin can be enhanced. Therefore, the dose of warfarin should be reduced when combined.

Diclofenac is contraindicated for caution

(1) Cross-allergy: same as ibuprofen.

(2) Diclofenac can pass through the placenta. Animal tests are toxic to fetal rats but not teratogenic. It is generally recommended that it should be avoided during pregnancy.

(3) Patients with liver or kidney dysfunction or history of ulcer should be used with caution, especially the elderly. Liver and kidney function should be routinely followed up during medication.

(4) Diclofenac should be used with caution in patients with limited sodium intake due to its sodium content.

(5) The contraindication for drug administration is basically the same as that of ibuprofen. In addition, those with anal inflammation should not use rectal administration.

Purpura. People with allergic asthma or history of asthma should not use this product, liver and kidney dysfunction and pregnant women with caution. Avoid use in pregnant women for the first three months.

Patients with gastrointestinal dysfunction, history of gastrointestinal ulcers, ulcerative colitis, clonal disease and severe liver dysfunction should be closely monitored; if peptic ulcer or gastrointestinal bleeding occurs during medication, the drug should be promptly discontinued. The latex is only suitable for non-damaged skin surface, and it is forbidden to use on skin damage or open wounds. Peptic ulcers and those who are known to be allergic to potassium diclofenac, acetylsalicylic acid or other prostaglandin synthase inhibitors are contraindicated. Patients with a history of gastrointestinal ulcers and liver damage should be used with caution. Used with caution in patients with heart / renal impairment symptoms / history, elderly patients, taking diuretics, and extracellular fluid loss for any reason. Patients with a history of vertigo or other central nervous system diseases should not drive or operate machinery while taking this product.

Diclofenac adverse reactions

(1) It can cause headache and gastrointestinal reactions such as abdominal pain, constipation, diarrhea, burning sensation, nausea, and indigestion. Allergic rashes are uncommon.

(2) Rarely, there is a decline in renal function, which can lead to retention of water and sodium, which is manifested by decreased urine output, facial edema, and sudden weight gain. Rarely can cause arrhythmia, tinnitus and so on.

(3) This product may cause bone marrow suppression or make it worse.

Can cause gastrointestinal reactions: nausea, vomiting, loss of appetite, bloating, diarrhea. Dizziness, headache, rash, gastrointestinal ulcers, muscle necrosis, and allergic reactions.

Occasionally, epigastric pain, nausea, vomiting, diarrhea, headache, dizziness, skin erythema or rash, rare gastrointestinal bleeding, peptic ulcer, drowsiness, urticaria, abnormal liver function and allergic reactions. Individual patients may also experience sensory or visual disturbances, tinnitus, insomnia, herpes, eczema, photosensitivity, acute renal insufficiency, and fulminant hepatitis.

Occasionally nausea, vomiting, and other gastrointestinal discomfort, headache, dizziness, dizziness, rash, and elevated serum transaminase. Rare gastrointestinal ulcers, bleeding, hepatitis and allergic reactions. Individual cases of pancreatitis, sacral bowel stenosis, aseptic meningitis, pneumonia, Steven-Johnson syndrome, Lyell's syndrome, erythroderma, cardiovascular abnormalities, visual or sensory disorders, erythema polymorpha, purpura, blood The system is abnormal.

Diclofenac drug interactions

1. When diclofenac is combined with lithium salt or digoxin, the blood concentration of the latter two can be increased.

2. Systemic combination with non-steroidal anti-inflammatory drugs or glucocorticoids may increase adverse reactions.

3. Combined with aspirin, can reduce the blood concentration of diclofenac.

4. When combined with potassium-preserving diuretics, serum potassium levels may be raised, and monitoring should be taken care of.

5. When combined with oral anticoagulants, relevant laboratory inspections should be done to ensure efficacy and drug safety.

6. Take diclofenac within 24 hours before and after using methotrexate. Care should be taken to observe that the blood concentration of methotrexate may be increased and the toxicity may be increased.

3 times / d. Children: Take 2 to 3 mg / kg daily in divided doses. Anal suppository: 50-100mg / time. Intramuscular injection: 75mg / time, 1 time / d, in severe cases, 2 times / d, deep gluteal muscle should be injected ^[3] .

Ecological hazards of diclofenac

Diclofenac, an anti-inflammatory drug commonly used in the livestock industry, has triggered a natural disaster in the ecosystem.

In 2004, researchers led by Washington State University's late microbiologist J. Lindsay Oaks found that diclofenac, an anti-inflammatory drug widely used in livestock, kills the Indian subcontinent. The culprit of this vulture. Oaks happened to be interested in falconry training in the Middle East and heard about the lethal effects of diclofenac. He had an idea and decided to test the drug on Indian vultures, which had shrunk by 95% in the previous decade.

The vultures mysteriously died of kidney failure and gout, and researchers have been searching for traces of heavy metals, pesticides and diseases without success. They did not consider the side effects of veterinary medicine, as there has never been a precedent for veterinary medicine causing wild animal deaths. If Oaks' discovery was a few years later, it might not help.

Prior to 1990, the intellectual property of diclofenac belonged to Novartis Pharmaceuticals. After the patent expired, Indian pharmacies took over the production of diclofenac, a cheap and effective drug that quickly swept the country and sold millions of copies to farmers. In many parts of South Asia, livestock is sacred, and diclofenac can ease the suffering of older livestock.

Because the animals are sacred, the dead carcasses cannot be eaten or cremated. Instead, they want to "expose the dead" for vultures to peck. In 2004, a survey of dead bodies found that one-tenth of them were contaminated with diclofenac, and researchers calculated that vultures had a one-percent chance of dying each time they ate diclofenac-containing meat. The decrease in vultures has led to an increase in the number of wild dogs, and the increasing number of wild dogs has also increased the hidden danger of rabies in humans. Not only that, the growth of wild dog populations in villages, towns, and the wild has led to the leopards living in deep forests switching to hunting wild dogs, which has increased the chance of leopard injuries. At the same time, the degradation of the carrion by the wild dog is less efficient than that of the vulture (its strong acidic property inhibits the growth of bacteria), thereby further exacerbating the deterioration of the natural environment.

In 2006, veterinary use of diclofenac was banned in Nepal, Pakistan and India. It took a decade for the United States to ban DDT.

Diclofenac Expert Reviews

Diclofenac has good anti-rheumatic, analgesic, anti-inflammatory, and antipyretic effects. It can relieve joint pain, improve its activity, and has good tolerance. Its effect is stronger than aspirin and comparable to indomethacin. According to domestic reports, 318 cases of diclofenac enteric-coated tablets have been verified in nearly 10 hospitals, with a marked effect of 44.3% and a total effective rate of 88.67%. During clinical verification, 107 patients were treated for liver and kidney function and blood before and after diclofenac Routine inspection and control, found no adverse effects. Diclofenac sodium has no accumulation effect when taken for a long time, the individual difference is small, and the side effects are small. Its dosage is one of the smallest varieties among current antipyretic and analgesics. Ophthalmology is often used for anti-inflammatory treatment of non-infectious inflammation, such as uvea, keratitis, scleritis, episcleritis, etc. ^[3] .