(and dosage form):
Each 3 mL ampoule contains: 75 mg Diclofenac sodium
Preservative: 0,3% m/v Sodium metabisulphite and 4% v/v Benzyl alcohol.
A 3.1 Anti-rheumatics (anti-Inflammatory agents).
Diclofenac sodium is a non-steroidal compound with analgesic, anti-inflammatory, antirheumatic and antipyretic properties.
It is an inhibitor of cyclo-oxygenase, and its potency is substantially greater than that of indomethacin, naproxen, or several other agents. In addition, diclofenac appears to reduce intracellular concentrations of free arachidonate in leukocytes, perhaps by altering the release or uptake of the fatty acid. There is a substantial first-pass effect, such that only about 50% of diclofenac is available systematically.
Diclofenac is extensively bound to plasma proteins (99%) and its half-life in plasma is 1 to 2 hours. It is metabolized in the liver by a cytochrome P450 isozyme of the CYP2C subfamily to 4-hydroxydiclofenac, the Principal metabolite, and other hydroxylated forms; after glucuronidation and sulfation, the metabolites are excreted in the urine (65%) and bile (35%).
For use as initial therapy for inflammatory and degenerative rheumatic diseases. Painful conditions due to inflammation of non-rheumatic origin and acute attacks of gout.
Patients with porphyria.
Children under the age of two years.
Patients with a history of active gastro-intestinal bleeding or peptic ulceration. Severe hepatic or renal impairment.
Contra-indicated in patients with a history of hypersensitivity reactions to aspirin or other non-steroidal anti-inflammatory drugs, and in patients sensitive to any of the ingredients in this product, including those in whom attacks of asthma, angioedema, urticaria, or rhinitis have been precipitated by aspirin or any other non-steroidal anti-inflammatory agent.
Known hypersensitivity to sodium metabisulphite.
Safety during pregnancy and lactation has not yet been established.
Serious interactions have been reported after the use of high dose methotrexate with diclofenac.
MAY NOT BE INJECTED INTRAVENOUSLY.
Regular use of non-steroidal anti-inflammatory agents during the 3rd trimester of pregnancy may result in closure of fetal ductus arteriosus in utero, and possibly in persistent pulmonary hypertension of the newborn. The onset of labour may be delayed and its duration increased.
DOSAGE AND DIRECTIONS FOR USE:
75 mg by deep intragluteal injection, once daily, or two times daily, in severe or hospitalized cases. Each injection must be given at a different site. Not to be given by intravenous injection. Each injection should be separated by an interval of a few hours. Parenteral administration should not be given for more than a few days, if necessary, treatment can be continued with oral therapy.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
There may be pain and, occasionally, tissue damage at the site of injection when diclofenac is given intramuscularly. Abscesses have also occurred, particularly in elderly diabetics. The commonest side-effects are gastro-intestinal disturbances, such as gastro-intestinal discomfort, nausea, and diarrhoea, which are usually mild and reversible, but in some patients peptic ulcer and severe gastro-intestinal bleeding may occur.
Central nervous system (CNS) related side-effects include headache, vertigo, dizziness, nervousness, tinnitus, depression, drowsiness and insomnia. Hypersensitivity reactions may occur frequently and include fever, angioedema, bronchospasm and rashes. Hepatotoxicity and aseptic meningitis, which occur less frequently, may also be hypersensitivity reactions. Elevated transaminase levels (SGOT, SGPT) may occur. Some patients may experience visual disturbances. Haematological adverse effects include anaemias, thrombocytopenia, neutropenia, eosinophilia and agranulotocytosis. Inhibition of platelet aggregation is reversible. Some non-steroidal anti-inflammatory agents have been associated with nephrotoxicity such as interstitial nephritis and nephrotic syndrome. Renal failure may be provoked by non-steroidal ant-inflammatory agents especially in patients with pre-existing renal impairment. Haematuria has also occurred. Fluid retention may occur, less frequently precipitating congestive heart failure in elderly patients. Long-term use or abuse of analgesics, including non-steroidal anti-inflammatory agents, has been associated with nephropathy.
Other adverse effects include photosensitivity.
Alveolitis, pulmonary eosinophilia, pancreatitis, hepatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis are other less frequent adverse effects. Induction or exacerbation of colitis has also been reported. Non-steroidal anti-inflammatory agents should be used with caution in patients with a history of peptic ulceration.
Non-steroidal anti-inflammatory agents should be used with caution in patients with infections, since symptoms such as fever and inflammation may be masked, and also with caution in patients with asthma or allergic disorders.
Other general precautions to be observed include administration to patients with haemorrhagic disorders, hypertension, and impaired renal, hepatic, or cardiac function. Patients undergoing therapy with some non-steroidal anti-inflammatory agents may need to be monitored for the development of blood, kidney, liver, or eye disorders. Non-steroidal anti-inflammatory agents should be used with caution in the elderly and may need to be given in reduced doses.
Some non-steroidal anti-inflammatory agents can interfere with thyroid function tests by lowering serum-thyroid hormone concentrations. Notable interactions involving non-steroidal anti-inflammatory agents include enhancement of the effects of oral anticoagulants (especially by azapropazone and phenylbutazone) and increased plasma concentrations of lithium, methotrexate, and cardiac glycosides.
The risk of nephrotoxicitymay be increased if given with ACE (angiotensin converting enzyme) inhibitors, cyclosporin, tacrolimus, or diuretics. Effects on renal function may lead to reduced excretion of some medicines. There may also be an increased risk of hyperkalaemia with ACE inhibitors and potassium-sparing diuretics. The antihypertensive effects of some antihypertensives including ACE inhibitors, beta blockers, and diuretics may be reduced. Convulsions may occur due to an interaction with quinolones. Non-steroidal anti-inflammatory agents may enhance the effects of phenytoin and sulphonylurea antidiabetics. The effects of non-steroidal anti-inflammatory agents might be enhanced by use with moclobemide. The concomitant use of more than one non-steroidal anti-inflammatory agents (including aspirin) should be avoided because of the increased risk of adverse effects. The risk of gastro-intestinal bleeding and ulceration associated with non-steroidal anti-inflammatory agents is increased when used with corticosteroids or, possibly, alcohol, bisphosphonates, or oxpentifylline.
There may be an increased risk of haemotoxicity during concomitant use of zidovudine and non-steroidal anti-inflammatory agents; blood counts 1 to 2 weeks after starting use together are recommended. Non-steroidal anti-inflammatory agents should be avoided for 8 to 12 days after mifepristone use because of a theoretical risk that these prostaglandin synthetase inhibitors may alter the efficacy of mifepristone.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
See 'Side-effects and special precautions'. Treatment is symptomatic and supportive.
Clear colourless to slight straw-coloured solution in amber glass ampoules.
Amber glass ampoules in packs of 5 and 50.
Protect ampoules from heat and light.
Store below 25°C.
Do not freeze.
KEEP OUT OF REACH OF CHILDREN
NAME AND BUSINESS ADDRESS OF APPLICANT:
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
Updated on this site: October 2004
Source: Pharmaceutical Industry
SAEPI HOME PAGE
TRADE NAME INDEX
GENERIC NAME INDEX
Information presented by Malahyde Information Systems © Copyright 1996-2004