VIVIAN-50 (Diclofenac Tablets BP)
Diclofenac sodium is a non-steroidal agent with analgesic, antipyretic and anti-inflammatory properties. It is an inhibitor of prostaglandin synthetase (cyclooxygenase).
Diclofenac is rapidly and completely absorbed. The oral bioavailability is 50% due to the effect of first pass metabolism. More than 99% of Diclofenac is reversibly bound to human plasma albumin. Diclofenac diffuses into synovial fluid, where maximum concentrations are measured 2-4 hours after peak plasma. Diclofenac is rapidly metabolized and almost completely, mainly in the liver. The major routes of metabolism are hydroxylation and glucuronidation. Excretion is both urinary and fecal incontinence. Less than 1% of the active substance is excreted unchanged in the urine. Approximately 60% of the amount administered is excreted as metabolites in the urine, the remainder is excreted in the feces. The half-life in plasma of unchanged Diclofenac is around 1 to 2 hours.
Diclofenac sodium is used for pain and inflammation in rheumatic disease (including juvenile idiopathic arthritis) and other musculoskeletal disorders; acute gout, postoperative pain.
Hypersensitivity to the Diclofenac sodium or any of the excipients.
Special precautions and warnings
Gastrointestinal: bleeding, ulceration or gastrointestinal perforations, sometimes fatal, have been reported with all NSAIDs, including Diclofenac Diclofenac should also be used with caution in Crohn’s disease or ulcerative colitis, as these conditions may be exacerbated.
Cardiovascular and cerebrovascular effects: it should be used with caution in patients with a history of cardiac failure, left ventricular dysfunction, hypertension, in patients with oedema for any other reason and in patients with other risk factors for cardiovascular events. Diclofenac is associated with an increased risk of thrombotic events (e.g., myocardial infarction and stroke).
Asthmatic subjects: patients with asthma associated with chronic rhinitis, chronic sinusitis with and/or nasal polyposis, have a risk of allergic reaction when taking aspirin and/or non-steroidal anti-inflammatory drugs, higher than the rest of the population.
Elderly: the elderly have an increased risk of adverse reactions to NSAIDs especially gastrointestinal bleeding and perforation which may be fatal.
Renal impairment: NSAIDs should be avoided if possible or used with caution in patients with renal impairment; the lowest effective dose should be used for the shortest possible duration, and renal function should be monitored. Sodium and water retention may occur and renal function may deteriorate, possibly leading to renal failure.
Hepatic impairment: NSAIDs should be used with caution in patients with hepatic impairment; there is an increased risk of gastrointestinal bleeding and fluid retention. NSAIDs should be avoided in severe renal failure.
Pregnancy: Avoiding the NSAIDs during pregnancy or avoiding them unless the potential benefit outweighs the risk. NSAIDs should be avoided during the third trimester because use is associated with a risk of closure of fetal ductus arteriosus in utero and possibly persistent pulmonary hypertension of the newborn. In addition, the onset of labour may be delayed and its duration may be increased.
Breast feeding: it should be used with caution during breast-feeding.
Dosage and directions for use
Adults: 75-150mg daily in 2-3 divided doses
Children (6months to 18 years): Juvenile idiopathic arthritis 1-3mg/kg/day in divided doses.
Gastrointestinal disturbances including discomfort, nausea, diarrhoea and occasionally bleeding and ulceration occur. Other side effects include hypersensitivity reactions (particularly rashes, angioedema, and bronchospasm), asthma, headache, dizziness, nervousness, depression, drowsiness, insomnia, vertigo, tinnitus, photosensitivity and haematuria.
Blood disorders have also occurred.
Fluid retention may occur (rarely precipitating congestive heart failure); blood pressure may be raised.
Renal failure may be provoked by NSAIDs, especially in patients with pre-existing renal impairment.
Hepatic damage, alveolitis, pulmonary eosinophilia, pancreatitis, visual disturbances and toxic epidermal necrolysis are other rare side effects. Induction of or exacerbation of colitis or Crohn’s disease has been reported
Lithium: increase in serum lithium concentrations and toxicity
Cyclosporine, tacrolimus: Risk of additive nephrotoxic effects, especially in elderly patients.
Diuretics, angiotensin converting enzyme (ACE) inhibitors, angiotensin II receptor antagonist: increased risk of renal impairment when NSAIDs given with diuretics, ACE inhibitors or angiotensin II receptor antagonists.
Adrenergic neuron blockers, aliskiren, alpha-blockers, Beta-blockers, calcium-channel blockers, clonidine, dazoxide, methyldopa, moxonidine, nitrates: NSAIDs antagonize hypertensive effects of these drugs.
Cardiac glycosides: NSAIDs possibly increase plasma concentration of cardiac glycosides, also possible exacerbation of heart failure and reduction of renal function.
Analgesics: increased risk of toxicity. Avoid concomitant use with other NSAIDs.
Anticoagulants: Increased risk of haemorrhage when Diclofenac is given with anticoagulants (avoid concomitant use, including low-dose heparin); NSAIDs possibly enhance anticoagulant effect of coumarins and phenindione.
Antidepressants, corticosteroids, pentoxifylline: increased risk of bleeding when used with NSAIDs
Methotrexate: increased hematological toxicity of methotrexate (decreased renal clearance by anti-inflammatory drugs)
Symptoms include headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, rarely diarrhoea, disorientation, excitation, coma, drowsiness, tinnitus, fainting, occasionally, convulsions. In rare cases of significant poisoning acute renal failure and liver damage are possible. Patients should be treated symptomatically as required. Within one hour of ingestion of a potentially toxic amount, activated charcoal should be considered.