Defnac™

[Diclofenac Sodium]

Indications

Intramuscular injection

Treatment of: exacerbations of inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondylarthntis, painful syndromes of the vertebral column, non-articular rheumatism;

Acute attacks of gout;

Renal colic and biliary colic;

Post-traumatic and postoperative pain; inflammation and swelling;

Severe migraine attacks. Intravenous infusion:

Treatment or prevention of postoperative pain in a hospital setting.

Contraindications

Gastric or intestinal ulcer.

Known hypersensitivity to the active substance, or sodium metabisulphite and other excipients. Like other non-steroidal anti-inflammatory drugs (NSAIDs).

Defnac is also contraindicated in patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or other drugs with prostaglandin-synthetase inhibiting activity.

Drug Interactions

(Including interactions observed with other pharmaceutical forms of Defnac) Lithium, digoxin: Defnac may raise plasma concentrations of lithium and digoxin. Diuretics: Like other NSAIDs, Defnac may decrease the activity of diuretics. Concomitant treatment with potassium-sparing diuretics may be associated with increased serum potassium levels, which should therefore be monitored. NSAIDs: Concomitant administration of systemic NSAIDs may increase the frequency of side effects.

Anticoagulants: Although clinical investigations do not appear to indicate that Defnac affects the action of anticoagulants, there are isolated reports of an increased risk of haemorrhage in patients receiving Defnac and anticoagulants concomitantly. Close monitoring of such patients is therefore recommended. Antidiabetics: Clinical studies have shown that Defnac can be given together with oral antidiabetic agents without influencing their clinical effect. However, isolated cases have been reported of both hypoglycaemic and hyperglycaemic effects necessitating changes in the dosage of hypoglycaemic agents during treatment with Defnac.

Methotrexate: Caution is called for if NSAIDs are administered less than 24 hours before or after treatment with methotrexate since blood concentration of methotrexate may rise and the toxicity of this substance be increased.

Cyclosporin: The effects of NSAIDs on renal prostanglandins may increase the nephrotoxicity of cyclosporin.

Quinolone antibacterials: There have been isolated reports of convulsions which may have been due to concomitant use of quinolones and NSAIDs.

Side Effects

(Including undesirable effects observed with other dosage forms of Defnac either in short-term or long-term use)

The following frequency estimates were used: frequent >10%, occasional >1% to 10%, rare >0.001% to 1%, isolated cases <0.001%.

Gastrointestinal tract
Occasional: epigastric pain; other gastrointestinal disorders such as nausea, vomiting, diarrhoea, abdominal cramps, dyspepsia, flatulence, anorexia.
Rare: gastrointestinal bleeding (haematemesis, melena, bloody diarrhoea), gastric or intestinal ulcer with or without bleeding or perforation.
Isolated cases: aphthous stomatitis, glossitis, oesophageal lesions, diaphragm like intestinal strictures, lower gut disorders such as non-specific haemorrhagic colitis and exacerbation of ulcerative colitis or Crohn’s disease, constipations, pancreatitis.

Central nervous system
Occasional: headache, dizziness, vertigo.
Rare: drowsiness.
Isolated cases: sensory disturbances, including paraesthesiae, memory disturbances, disorientation, insomnia, irritability, convulsions, depression, anxiety, nightmares, tremor, psychotic reactions, aseptic meningitis.

Special senses
Isolated cases: disturbances of vision (blurred vision, diplopia), impaired hearing, tinnitus, taste disturbances.

Skin
Occasional: rashes or skin eruptions.
Rare: urticaria.
Isolated cases: bullous eruptions, eczema, erythema multiforme, Stevens Johnson syndrome, Lyell’s syndrome (acute toxic epidermolysis). erythroderma (exfoliative dermatitis), loss of hair photosensitivity reactions; purpura, including allergic purpura.

Kidney
Rare: oedema.
Isolated cases: acute renal failure, urinary abnormalities such as hematuria and proteinuria. interstitial nephritis, nephrotic syndrome, papillary necrosis.

Liver
Occasional: elevation of serum aminotransferase values.
Rare: hepatitis with or without jaundice. Isolated cases: fulminant hepatitis.

Blood
Isolated cases: thrombocytopenia, leucopenia, haemolytic anaemia, aplastic anaemia, agranulocytosis.

Hypersensitivity
Rare: hypersensitivity reactions such as asthma, systemic anaphylactic / anaphylactoid reactions including hypotension.
Isolated cases: Vasculitis, pneumonitis.

Cardiovascular system
Isolated cases: palpitation, chest pain, hypertension, congestive heart failure.

Other organ systems
Occasional: intramuscular injection site reactions such as local pain and induration.
Isolated cases: local abscesses and necrosis at the intramuscular injection site.

Warning and Precautions

Gastrointestinal bleeding or ulceration / perforation can occur at any time during treatment, with or without warning symptoms or a previous history. They generally have more serious consequences in the elderly. In the rare cases where gastrointestinal bleeding or ulceration occurs in patients receiving Defnac, the drug should be withdrawn. As with other NSAIDs, allergic reactions, including anaphylactic / anaphylactoid reactions, can also occur in rare cases, without earlier exposure to the drug. The sodium metabisulphite in the ampoules can also lead to isolated hypersensitivity reactions.

Like other NSAIDs, Defnac may mask the signs and symptoms of infection due to its pharmacodynamic properties

Pregnancy / Lactation

Because of insufficient data, administration of Defnac ampoules during pregnancy and lactation is not recommended. (See product information on oral/rectal forms for use of these during pregnancy and lactation).

Precautions

Close medical surveillance is imperative in patients with symptoms indicative of gastrointestinal disorders or a history suggestive of gastric or intestinal ulcer, patients with ulcerative colitis or Crohn’s disease, and patients suffering from impaired hepatic function.

As with other NSAIDs, values of one or moreover enzymes may increase. During prolonged treatment with

Defnac (e.g. in the form of tablets or suppositories), monitoring of hepatic function is indicated as a precautionary measure. If abnormal liver function tests persist or worsen, if clinical signs or symptoms consistent with liver disease develop, or if other manifestations occur (e.g. eosinophilia, rash, etc.), Defnac should be discontinued. Hepatitis may occur without prodromal symptoms.

Caution is called for when using Defnac in patients with hepatic porphyria, since Defnac may trigger an attack.

Owing to the importance of prostaglandins in maintaining renal blood flow, particular caution is called for in patients with impaired cardiac or renal function, the elderly, patients being treated with diuretics, and patients with substantial extracellular volume depletion of any cause, e.g. before or after major surgery. Monitoring of renal function is recommended as a precautionary measure when using Defnac in such cases. Discontinuation of therapy is normally followed by a return to the pretreatment state.

During prolonged treatment with Defnac - as with other NSAIDs - monitoring of the blood count is recommended.

Dosage

Adults

Defnac ampoules should not be given for more than 2 days; if necessary, treatment can be continued with tablets or suppositories. Intramuscular Injection
The dosage is generally one ampoule of 75 mg daily, given by deep intragluteal injection into the upper outer quardrant. In severe cases (e.g. colic) the daily dose can exceptionally be increased to two injections of 75 mg, separated by an interval of a few hours (one into each buttock). Alternatively, one ampoule of 75mg can be combined with other dosage forms up to a maximum daily dosage of 150 mg.

In migraine attacks, clinical experience is limited to initial use of one ampoule of 75mg administered as soon as possible, followed by suppositories up to 100mg on the same day if required. The total dosage should not exceed 175mg on the first day.

Intravenous infusion
Defnac must not be given as an Intravenous bolus injection.

Immediately before starting an intravenous infusion Defnac must be diluted with saline 0.9% or glucose 5% infusion solution buffered with sodium bicarbonate according to the instructions given in the section "Instructions for use/handling". Two alternative dosage regimens of Defnac are recommended.

For the treatment of moderate to severe postoperative pain, 75mg should be infused continuously over a period of 30 minutes to 2 hours. If necessary, treatment may be repeated after a few hours, but the dosage should not exceed 150mg within any period of 24 hours. For the prevention of postoperative pain, a loading dose of 25-50 mg should be infused after surgery over 15 minutes to 1 hour, followed by a continous infusion of about 5mg per hour up to a maximum daily dosage of 150mg.

Children

Defnac ampoules are not recommended for use in children.

Presentations Available

Each pack of DEFNAC contains 5 ampoules (3 ml) of 75 mg.

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