Diclofenac Potassium Tablets
1 NAME OF THE MEDICINAL PRODUCT
DICLOPAC 50mg film coated tablets.
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each film coated tablet contains:
Diclofenac Potassium BP: 50mg
Colour: Red Oxide of Iron & Titanium Dioxide
3 PHARMACEUTICAL FORM
For oral administration.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
DICLOPAC is indicated for the short-term treatment of all grades of pain and inflammation in the following acute conditions:
Post-traumatic pain, inflammation and swelling, e.g. due to sprains.
Acute musculo-skeletal disorders such as periarthritis (for example frozen shoulder), tendonitis, tenosynovitis, bursitis.
Postoperative pain, inflammation and swelling, e.g. following dental or orthopaedic surgery.
Painful and/or inflammatory conditions in gynaecology, e.g. primary dysmenorrhoea or anxiety and associated menorrhagia.
Painful syndromes of the vertebral column.
As an adjuvant in severe painful inflammatory infections of the ear, nose or throat, e.g. pharyngotonsillitis, otitis. In keeping with general therapeutic principles, the underlying disease should be treated with basic therapy, as appropriate. Fever alone is not an indication.
4.2 Posology and method of administration
The recommended initial daily dose is 100 to 150mg. In milder cases, 75 to 100 mg daily is usually sufficient. The total daily dose should generally be divided in 2 to 3 doses.
Known hypersensitivity to the active substance or to any of the excipients.
History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
Active or history of recurrent peptic ulcer/ haemorrhage (two or more distinct episodes of proven ulceration or bleeding).
Last trimester of pregnancy.
Severe hepatic, renal and heart failure.
Like other non-steroidal anti-inflammatory drugs (NSAIDs) it is also contraindicated in patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or other NSAIDs.
4.4 Special warnings and precautions for use
Gastrointestinal bleeding or ulceration or perforation, which can be fatal, have been reported with all NSAIDs, including diclofenac, and may occur at any time during treatment, with or without warning symptoms or a previous history of serious gastrointestinal events. The elderly have an increased frequency of adverse reactions to NSAIDs especially gastrointestinal bleeding and perforation which may be fatal. When gastrointestinal bleeding or ulceration occurs in patients receiving diclofenac, the medicinal product should be withdrawn.
Undesirable effects may be minimized by using the lowest effective dose for the shortest possible duration necessary to control symptoms.
The use of DICLOPAC with concomitant NSAIDs including cyclooxygenase-2 selective inhibitors, should be avoided due to the absence of any evidence demonstrating synergistic benefits and the potential for additive undesirable effects.
Caution is indicated in the elderly on basic medical grounds. In particular it is recommended that the lowest effective dosage be used in frail elderly patients or those with a low body weight.
4.5 Interaction with other medicinal products and other forms of interaction
The following interactions include those observed with diclofenac potassium.
Lithium: If used concomitantly, diclofenac may raise plasma concentrations of lithium. Monitoring of the serum lithium level is recommended.
Digoxin: If used concomitantly, diclofenac may raise plasma concentrations of digoxin. Monitoring of the serum digoxin level is recommended.
Diuretics and antihypertensive agents: Like other NSAIDs, concomitant use of diclofenac with diuretics or antihypertensive agents (e.g. beta-blockers, angiotensin converting enzyme (ACE) inhibitors) may cause a decrease in their antihypertensive effect. Therefore, the combination should be administered with caution and patients, especially the elderly, should have their blood pressure periodically monitored. Patients should be adequately hydrated and consideration should be given to monitoring of renal function after initiation of concomitant therapy and periodically thereafter, particularly for diuretics and ACE inhibitors due to the increased risk of nephrotoxicity. Concomitant treatment with potassium-sparing drugs may be associated with increased serum potassium levels, which should therefore be monitored frequently.
4.6 Pregnancy and lactation
The use of diclofenac in pregnant women has not been studied. Therefore, DICLOPAC should not be used during the first two trimesters of pregnancy unless the potential benefit to the mother outweighs the risk to the foetus. As with other NSAIDs, use of diclofenac during the third trimester of pregnancy is contraindicated owing to the possibility of uterine inertia and/or premature closure of the ductus arteriosus.
Like other NSAIDs, diclofenac passes into the breast milk in small amounts. Therefore it should not be administered during breast feeding in order to avoid undesirable effects in the infant.
4.7 Undesirable effects
If serious side-effects occur, Diclofenac Potassium tablets should be withdrawn.
Gastrointestinal: The most commonly-observed adverse events are gastrointestinal in nature. Peptic ulcers, perforation or GI bleeding, sometimes fatal, particularly in the elderly, may occur. Nausea, vomiting, diarrhoea, flatulence, constipation, dyspepsia, abdominal pain, melaena, haematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease have been reported following administration. Less frequently, gastritis has been observed. Pancreatitis has been reported very rarely.
Hypersensitivity: Hypersensitivity reactions have been reported following treatment with NSAIDs. These may consist of (a) non-specific allergic reactions and anaphylaxis (b) respiratory tract reactivity comprising asthma, aggravated asthma, bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of various types, pruritus, urticaria, purpura, angiodema and, more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
There is no typical clinical picture resulting from diclofenac overdosage. Overdosage can cause symptoms such as vomiting, gastrointestinal haemorrhage, diarrhoea, dizziness, tinnitus or convulsions. In the event of significant poisoning, acute renal failure and liver damage are possible.
Management of acute poisoning with NSAIDs, including diclofenac, essentially consists of supportive measures and symptomatic treatment. Supportive measures and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal disorder, and respiratory depression.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Diclofenac Potassium tablets contain the potassium salt of diclofenac, a non-steroidal compound with pronounced and clinically demonstrable analgesic, anti-inflammatory and anti-pyretic properties.
Diclofenac is a potent inhibitor of prostaglandin biosynthesis and a modulator of arachidonic acid release and uptake.
Diclofena Potassium tablets have a rapid onset of action and are therefore suitable for the treatment of acute episodes of pain and inflammation.
In migraine attacks Diclofenac Potassium tablets have been shown to be effective in relieving the headache and in improving the accompanying symptom of nausea.
Diclofenac in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached inhuman beings.
5.2 Pharmacokinetic properties
Diclofenac is rapidly and completely absorbed from sugar coated tablet. Food intake does not affect absorption. Peak plasma concentration after one 50 mg sugar-coated tablet was 3.9 µmol/l after 20-60 minutes. The plasma concentrations show a linear relationship to the size of the dose.
Diclofenac undergoes first-pass metabolism and is extensively metabolised.
Diclofenac is highly bound to plasma proteins (99.7%), chiefly albumin (99.4%).
The biotransformation of diclofenac involves partly glucuronidation of the intact molecule but mainly single and multiple hydroxylation followed by glucuronidation.
The total systemic clearance of diclofenac in plasma is 263 ± 56 ml/min (mean ± SD). The terminal half-life in plasma is 1 – 2 hours. Repeated oral administration of Diclofenac Potassium tablets for 8 days in daily doses of 50 mg t.d.s does not lead to accumulation of diclofenac in the plasma. Approx. 60% of the dose administered is excreted in the urine in the form of metabolites, and less than 1% as unchanged substance. The remainder of the dose is eliminated as metabolites through the bile in the faeces.
6 PHARMACEUTICAL PARTICULARS
6.1 Shelf life
6.2 Special precaution for storage
Do not store above 3 0°C. Keep in the original container and protect from light.
KEEP OUT OF REACH OF CHILDREN
10 blister pack of 10 tablets in 1 pack.
7 MARKETING AUTHORISATION HOLDER
Manufactured in India by
Survey No. 198/2 & 198/3, Chachrawadi Vasna,
Tal.: Sanand, Dist.: Ahmedabad 382 210, India.
MEDITRADE Nig. Limited
3, Salawu Street OIodi Apapa, Lagos, Nigeria.
GreenPeck Nigeria Limited
54, Oyewole Street, Palm-Grove Estate
8.MARKETING AUTHORISATION NUMBER(S)
Mfg. Lic. No.: G/25/1877
Artwork No.: 5459101-02