Product name: Diclofenac

This is a prescription drug

Read directions carefully before use

Keep out of the reach of children

Immediately inform doctors or pharmacists of adverse effects when using this product

Ingredient: A 3mL vial contains:

Product description: Clear, colorless or pale yellow solution.

Packaging: Boxes containing 10, 30 or 100 vials x3mL, enclosed with directions for use

Indications:

– Treat short-term symptoms of acute arthritis, gout-induced arthritis.

– Acute backache, radicular pain.

– Pain caused by kidney stones.

– Postsurgical pain, pain from injuries.

Usage and dosage:

– Usage:

• To reduce the risk of adverse effects, use Diclofenac at the lowest daily dose to produce effects in the shortest time possible (consult “Cautions” section). The maximum dose is 150 mg.
• Administer via intramuscular injections. Change injection site for repeated injections. If there is intense pain, immediately stop the injection. Treatment lasts 2-3 days (continue treatment by oral or rectal administration if necessary).

– Dosage:

• Adult: Ventrogluteal injection: 1 vial per day, inject in 2-3 days. Can use an additional 50mg diclofenac tablet.
• Children: 2-3mg/kg/day divided into 2-4 times/day.

Contraindications

– Allergic to diclofenac, aspirin, other non-steroidal anti-inflammatory drugs and other ingredients in the drug.

– Progressive peptic ulcers.

– Patients with asthma, bronchospasm, bleeding, cardiovascular diseases, severely impaired kidneys or liver.

– Patients using anticoagulants.

– Congestive heart failure, reduced blood volume due to diuretics or impaired kidneys, glomerular filtration rate <30mL/minute (due to risks of impaired kidneys).

– Congestive heart failure from degree II to IV as defined by New York Heart Association, ischemia heart disorder, peripheral arterial diseases, cerebrovascular diseases.

– Patients with collagen diseases.

– Pregnant women in the last trimester.

– Analgesia during coronary artery surgeries due to the risk of myocardial infarction or stroke.

– Children and adolescents under 18.

Adverse effects

Common

– Whole-body: headache, restlessness.

– Digestive issues: epigastralgia, nausea, vomiting, diarrhea, stomach distension, loss of appetite, indigestion.

– Liver: Increased transaminase.

– Ears: buzzing.

Less common

– Whole-body: edema, allergy (especially bronchoconstriction in asthma), anaphylactic shock including dropping blood pressure, rhinitis, hives.

– Digestion: stomachache, GI bleeding, worsen ulcers, bloody vomit, bloody diarrhea, local irritation (when drug is placed into the rectum).

– Nervous system: Sleepiness, dozing off, depression, insomnia, anxiety, irritability.

– Skin: hives.

– Respiration: bronchospasm.

– Eyes: blurry, dark spots in vision, eye pain, double vision.

Rare

– Whole-body: edema, rash breakout, Stevens – Johnson syndrome, hair loss.

– Nervous system: aseptic meningitis.

– Blood: drop in white blood cell, platelet and neutrophil levels, increased granulocytes, anemia.

– Liver: gallbladder contractility disorders, tests show abnormal hepatic functions, hepatotoxicity (jaundice, hepatitis).

– Urination: bladder infection, bloody urine, acute kidney failure, interstitial nephritis, nephrotic syndrome.

Risk of coronary thrombosis: Clinical and epidemiological studies show that diclofenac is associated with increased risks of coronary thrombotic events (such as myocardial infarction or stroke), especially at high doses (150 mg/day) and after prolonged use (refer to “Cautions” section).

9. Drug and food interactions

– Oral anticoagulants and heparin: risk of severe bleeding

– Quinolone antibiotics: Diclofenac and other non-steroidal anti-inflammatory drugs can enhance side effects of quinolone antibiotics on the central nervous system, causing convulsion (more research required).

– Aspirin or glucocorticoid: decrease plasma concentration of diclofenac and increase risk and severity of gastrointestinal damage.

– Diflunisal: coadministration with diclofenac can increase plasma concentration of diclofenac, reducing diclofenac excretion and cause severe bleeding in the GI tract.

– Lithium: Diclofenac can increase plasma concentration of lithium to toxic levels. If coadministration is necessary, patients need to be monitored and observed for any signs of lithium poisoning. The blood concentration of lithium also needs to be monitored. Adjust lithium dosage during and after treatment with diclofenac.

– Digoxin: Diclofenac can increase plasma concentration of digoxin and prolongs its half-life. It is necessary to measure blood concentration of digoxin and digoxin dosage should be decreased during coadministration with diclofenac.

– Ticlopidin: coadministration with diclofenac increases risk of bleeding.

– Intrauterine device: it has been reported that diclofenac can cause the contraception device to be ineffective.

– Methotrexate: diclofenac increases methotrexate toxicity.

– Cyclosporin: risk of cyclosporin poisoning. The patient’s kidney functions need to be carefully monitored.

– Diuretics: Diclofenac and diuretics can increase the risk of secondary kidney failure due to decreased blood flow to the kidneys as a result of prostaglandin inhibition.

– Hypertension medication (metabolic enzyme inhibitors, betablockers, diuretics).

– Antacids can decrease gastric irritation caused by diclofenac but also can decrease diclofenac’s plasma concentration.

– Cimetidine can decrease the plasma concentration of diclofenac but does not lower its anti-inflammatory effect. Cimetidine protects the duodenum from diclofenac’s side effects.

– Probenecid can double diclofenac concentration upon coadministration. This may have a beneficial clinical outcome on arthritic patients but can cause diclofenac poisoning, especially in patients with impaired kidney functions. Uric acid excretion by the kidney is unaffected. Decrease diclofenac dosage if necessary.

10. Missed doses:

If patients miss a dose, skip said dose and continue as per the indicated dosage. Do not double the dose.

11. Storage

Store at a clean dry area under 30⁰C, avoid direct light sources.

12. Overdosage and symptoms:

Lethal dose in human is unknown, some have used up to 4g of the drug.

Acute diclofenac poisoning primarily causes more severe side effects: vomiting, GI bleeding, diarrhea, dizziness, buzzing ears or convulsion. In case of severe poisoning, acute kidney failure and liver damage may occur.

13. What to do in case of overdosing?

– In case of overdosing and adverse effects emerge, treat the symptoms. Increase diuresis, alkalize urine, perform hemodialysis. If diuresis is enhanced, closely monitor water-electrolyte balance as electrolyte disorder and hydronephrosis may occur.

14. Cautions:

Patients that need extra precautions:

• Patients with a medical history of peptic ulcers, GI bleeding or ruptured bowel.

• Use extra precaution with geriatric patients due to increased risk of adverse effects.

• Patients with impaired kidneys, livers, systemic lupus.

• Hypertensive patients or cardiac edema, conditions that cause sodium retention

• Patients with a record of hepatic diseases. Their liver functions need to be monitored during long-term treatment with diclofenac.

• Patients with a record of clotting disorders and bleeding.

• Have extra precaution with sodium retention conditions as the product supplies Na+.

• Perform eye exams for patients with visual disorders when using diclofenac.

• Risk of coronary thrombosis: Non-steroidal anti-inflammatory drugs (NSAIDs), not aspirin, administered systemically can increase the risk of coronary thrombosis events, including myocardial infarction and stroke which can be lethal. The risk may appear early in the first few weeks of treatment and can increase as drug use is prolonged. The risk of coronary thrombosis has mainly been reported at high dosage.

• Doctors need to perform periodic examination on the patients’ cardiovascular system, even when patients show no cardiovascular symptoms beforehand. Patients need to be informed of severe cardiovascular disorders and need to see the doctor immediately when symptoms are detected.

• To minimize the risk of adverse effects, inject Diclofenac at the lowest effective daily dose in the shortest time possible.

• Care should be taken when administering diclofenac to patients with known risk factors for developing cardiovascular events (such as hypertension, increased serum lipid, diabetes and tobacco addiction).

Use during pregnancy and lactation:

– Pregnant women:

• Women planning to become pregnant should not take any medication that inhibits prostaglandin synthesis, including diclofenac, because it inhibits implantation of embryos.

• Only use for pregnant women at absolute necessity and when the patient cannot use other anti-inflammatory drugs. Use the lowest dose as necessary.
• Do not use diclofenac in the last trimester (due to the risk of inhibiting uterine contractions and early closure of the ductus arteriosus, causing irreversible hypertension and renal failure in the fetus).

– Nursing women: There is little of diclofenac that enters breastmilk. No effects on breastfeeding infants have been reported. Nursing mothers can use diclofenac. Use non-steroidal anti-inflammatory drugs when necessary.

15. Effects on work (machine operators, drivers, workers at high altitude and other cases)

Patients may experience visual disturbances, dizziness, central nervous system disorders, drowsiness or fatigue when taking NSAIDs. Therefore, avoid driving or operating machinery when using the product.

16. Incompatibility: For intravenous injections, dilute diclofenac 75mg/3mL into a 5mg/mL solution with isotonic sodium chloride solution for injection and infuse at a slow rate (25 mg in 10 minutes)

17. When to consult doctors, pharmacists?

– Consult doctors if patients are simultaneously using another drug or when any abnormal symptoms occur.

“Consult doctors or pharmacists for more information”.

Expiry date: 36 months since manufacture.