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Full Prescribing Info
Diclofenac potassium.
Each sugar-coated tablet also contains the following excipients: Core: Magnesium stearate, povidone, anhydrous colloidal silica, sodium starch glycollate, maize starch, calcium phosphate. Sugar-Coat: Microcrystalline cellulose, polyethylene glycol 8000, red iron oxide (E172) and titanium dioxide (E171) (dispersed Anstead), povidone, talc, sucrose. Polish: Polyethylene glycol 8000, sucrose.
Each tablet is also imprinted with printing ink brown for 25 mg and white for 50 mg.
Diclofenac potassium is potassium-[o-[(2,6-dichlorophenyl)-amino]-phenyl]-acetate.
In Cataflam, the sodium ion of diclofenac sodium (Voltaren) has been replaced by a potassium ion.
Cataflam is an anti-inflammatory and anti-rheumatic product, nonsteroid, acetic acid derivative and related substance.
Pharmacology: Pharmacodynamics: Mechanism of Action: Cataflam contains the potassium salt of diclofenac, a nonsteroidal compound with pronounced analgesic, anti-inflammatory and antipyretic properties. Inhibition of prostaglandin biosynthesis, which has been demonstrated in experiments, is considered to be fundamental to its mechanism of action. Prostaglandins play a major role in causing inflammation, pain and fever.
Cataflam tablets have a rapid onset of action which makes them particularly suitable for the treatment of acute painful and inflammatory conditions.
Diclofenac potassium in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached in humans.
Pharmacodynamic Effects: Cataflam has been found to exert a pronounced analgesic effect in moderate and severe pain. In the presence of inflammation eg, due to trauma or following surgical interventions, it rapidly relieves both spontaneous pain and pain on movement and diminishes inflammatory swelling and wound oedema.
Clinical studies have also revealed that in primary dysmenorrhoea the active substance is capable of relieving the pain and reducing the extent of bleeding.
In migraine attacks, Cataflam has been shown to be effective in relieving the headache and in improving the accompanying symptoms nausea and vomiting.
Pharmacokinetics: Absorption: Diclofenac is rapidly and completely absorbed from diclofenac potassium tablets. The absorption sets in immediately after administration and the same amount is absorbed as from an equivalent dose of diclofenac sodium gastroresistant tablets.
Mean peak plasma concentrations of 3.8 micromol/L are attained after 20-60 min after ingestion of 1 tablet of 50 mg. Ingestion together with food has no influence on the amount of diclofenac absorbed although onset and rate of absorption may be slightly delayed.
The amount absorbed is in linear proportion to the size of the dose.
Since about ½ of diclofenac is metabolized during its first passage through the liver (first-pass effect), the area under the concentration curve (AUC) is about ½ as large following oral or rectal administration as it is following a parenteral dose of equal size.
Pharmacokinetic behaviour does not change after repeated administration. No accumulation occurs provided the recommended dosage intervals are observed.
Distribution: 99.7% of diclofenac binds to serum proteins, mainly to albumin (99.4%). The apparent volume of distribution calculated is 0.12-0.17 L/kg.
Diclofenac enters the synovial fluid, where maximum concentrations are measured 2-4 hrs after peak plasma values have been reached. The apparent half-life for elimination from the synovial fluid is 3-6 hrs. Two (2) hrs after reaching peak plasma levels, concentrations of the active substance are already higher in the synovial fluid than in the plasma and they remain higher for up to 12 hrs.
Biotransformation: Biotransformation of diclofenac takes place partly by glucuronidation of the intact molecule, but mainly by single and multiple hydroxylation and methoxylation, resulting in several phenolic metabolites (3'-hydroxy-, 4'-hydroxy-, 5-hydroxy-, 4',5-dihydroxy- and 3'-hydroxy-4'-methoxy-diclofenac), most of which are converted to glucuronide conjugates. Two (2) of these phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.
Elimination: Total systemic clearance of diclofenac from plasma is 263±56 mL/min (mean value ± SD). The terminal half-life in plasma is 1-2 hrs. Four (4) of the metabolites, including the 2 active ones, also have short plasma half-lives of 1-3 hrs. One (1) metabolite, 3'-hydroxy-4'-methoxy-diclofenac, has a much longer plasma half-life. However, this metabolite is virtually inactive.
About 60% of the administered dose is excreted in the urine as the glucuronide conjugate of the intact molecule and as metabolites, most of which are also converted to glucuronide conjugates. Less than 1% is excreted as unchanged substance. The rest of the dose is eliminated as metabolites through the bile in the faeces.
Characteristics in Patients: No relevant age-dependent differences in the drug's absorption, metabolism or excretion have been observed.
In patients suffering from renal impairment, no accumulation of the unchanged active substance can be inferred from the single-dose kinetics when applying the usual dosage schedule. At a creatinine clearance of <10 mL/min, the calculated steady-state plasma levels of the hydroxy metabolites are about 4 times higher than in normal subjects. However, the metabolites are ultimately cleared through the bile.
In patients with chronic hepatitis or nondecompensated cirrhosis, the kinetics and metabolism of diclofenac are the same as in patients without liver disease.
Toxicology: Preclinical Safety Data: Preclinical data from acute and repeated dose toxicity studies, as well as from genotoxicity, mutagenicity and carcinogenicity studies with diclofenac revealed no specific hazard for humans at the intended therapeutic doses. There was no evidence that diclofenac had a teratogenic potential in mice, rats or rabbits.
Diclofenac had no influence on the fertility of parent animals in rats. The prenatal, perinatal and postnatal development of the offspring was not affected.
Short-term treatment in the following acute conditions: Post-traumatic pain, inflammation and swelling eg, due to sprains; postoperative pain, inflammation and swelling eg, following dental or orthopaedic surgery; painful and/or inflammatory conditions in gynaecology eg, primary dysmenorrhoea or adnexitis; migraine attacks; painful syndromes of the vertebral column; non-articular rheumatism.
As an adjuvant in severe painful  inflammatory infections of the ear, nose or throat eg, 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.
Dosage/Direction for Use
As a general recommendation, the dose should be individually adjusted and the lowest effective dose given for the shortest possible duration.
Adults: Recommended Initial Daily Dosage: 100-150 mg. In milder cases, 75-100 mg daily is usually sufficient. The total daily dose should generally be divided in 2-3 doses.
Primary Dysmenorrhoea: The daily dosage should be individually adjusted and is generally 50-150 mg. A dose of 50-100 mg should be given initially and, if necessary, increased over the course of several menstrual cycles up to a maximum of 200 mg/day. Treatment should be started on appearance of the 1st symptoms and, depending on the symptomatology, continued for a few days.
Migraine Attacks: Initial Dose: 50 mg taken at the 1st signs of an impending attack. In cases where pain relief within 2 hrs after the 1st dose is not sufficient, a further dose of 50 mg may be taken. If needed, further doses of 50 mg may be taken at intervals of 4-6 hrs, not exceeding a total dose of 200 mg/day.
Children and Adolescents <14 years: Cataflam tablets are not recommended for use in children and adolescents <14 years; other forms of diclofenac eg, oral drops or suppositories could be used in these patients.
Adolescents ≥14 years: A daily dose of 75-100 mg is usually sufficient. The total daily dose should generally be divided in 2 to 3 doses.
The maximum daily dose of 150 mg should not be exceeded.
The use of Cataflam (all forms) in migraine attacks has not been established in children and adolescents.
Administration: The tablets should be swallowed whole with liquid, preferably before meals, and must not be divided or chewed.
Symptoms: There is no typical clinical picture resulting from diclofenac overdosage. Overdosage can cause symptoms eg, vomiting, gastrointestinal haemorrhage, diarrhoea, dizziness, tinnitus or convulsions. In the event of significant poisoning, acute renal failure and liver damage are possible.
Therapeutic Measures: 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 eg, hypotension, renal failure, convulsions, gastrointestinal disorder and respiratory depression.
Special measures eg, forced diuresis, dialysis or haemoperfusion are probably of no help in eliminating NSAIDs, including diclofenac, due to the high protein-binding and extensive metabolism.
Activated charcoal may be considered after ingestion of a potentially toxic overdose, and gastric decontamination (eg, vomiting, gastric lavage) after ingestion of a potentially life-threatening overdose.
Hypersensitivity to diclofenac potassium or to any of the excipients of Cataflam. Active gastric or intestinal ulcer, bleeding or perforation. Severe hepatic, renal and cardiac failure (see Warnings and Precautions). Like other NSAIDs, Cataflam is also contraindicated in patients in whom attacks of asthma, urticaria or acute rhinitis are precipitated by acetylsalicylic acid or other NSAIDs. Last trimester of pregnancy.
Use in pregnancy: The use of diclofenac in pregnant women has not been studied. Therefore, Cataflam should not be used during the first 2 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 3rd trimester of pregnancy is contraindicated owing to the possibility of uterine inertia and/or premature closure of the ductus arteriosus. Animal studies have not shown any directly or indirectly harmful effects on pregnancy, embryonal/foetal development, parturition or postnatal development (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
Gastrointestinal bleeding, 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. They generally have more serious consequences in the elderly. If gastrointestinal bleeding or ulceration occur in patients receiving Cataflam, Cataflam should be withdrawn.
Serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported very rarely in association with the use of NSAIDs, including Cataflam (see Adverse Reactions). Patients appear to be at highest risk of these reactions early in the course of therapy, the onset of the reaction occurring in the majority of cases within the 1st month of treatment. Cataflam should be discontinued at the 1st appearance of skin rash, mucosal lesions or any other sign of hypersensitivity.
As with other NSAIDs, allergic reactions, including anaphylactic/anaphylactoid reactions, can also occur in rare cases with diclofenac without earlier exposure to the drug.
Like other NSAIDs, Cataflam may mask the signs and symptoms of infection due to its pharmacodynamic properties.
Special Precautions
General: The concomitant use of Cataflam with systemic 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 dose be used in frail elderly patients or those with a low body weight.
Cataflam tablets contain sucrose and therefore are not recommended for patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency.
Preexisting Asthma: In patients with asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (ie, nasal polyps), chronic obstructive pulmonary diseases or chronic infections of the respiratory tract (especially if linked to allergic rhinitis-like symptoms), reactions on NSAIDs like asthma exacerbations (so-called intolerance to analgesics/analgesics-asthma), Quincke’s oedema or urticaria are more frequent than in other patients. Therefore, special precaution is recommended in such patients (readiness for emergency). This is applicable as well for patients who are allergic to other substances eg, with skin reactions, pruritus or urticaria.
Gastrointestinal Effects: As with all NSAIDs, including diclofenac, close medical surveillance is imperative and particular caution should be exercised when prescribing Cataflam in patients with symptoms indicative of gastrointestinal disorders or with a history suggestive of gastric or intestinal ulceration, bleeding or perforation (see Adverse Reactions). The risk of gastrointestinal bleeding is higher with increasing NSAID doses and in patients with a history of ulcer, particularly if complicated with haemorrhage or perforation and in the elderly.
To reduce the risk of gastrointestinal toxicity in patients with a history of ulcer, particularly if complicated with haemorrhage or perforation, and in the elderly, the treatment should be initiated and maintained at the lowest effective dose.
Combination therapy with protective agents (eg, proton pump inhibitors or misoprostol) should be considered for these patients, and also for patients requiring concomitant use of medicinal products containing low-dose acetylsalicylic acid (ASA)/aspirin or other medicinal products likely to increase gastrointestinal risk.
Patients with a history of gastrointestinal toxicity, particularly the elderly, should report any unusual abdominal symptoms (especially gastrointestinal bleeding). Caution is recommended in patients receiving concomitant medications which could increase the risk of ulceration or bleeding eg, systemic corticosteroids, anticoagulants, antiplatelet agents or selective serotonin-reuptake inhibitors (see Interactions).
Close medical surveillance and caution should also be exercised in patients with ulcerative colitis or Crohn’s disease, as their condition may be exacerbated (see Adverse Reactions).
Hepatic Effects: Close medical surveillance is required when prescribing Cataflam to patients with impaired hepatic function, as their condition may be exacerbated.
As with other NSAIDs, including diclofenac, values of ≥1 liver enzymes may increase. During prolonged treatment with Cataflam, regular 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 (eg, eosinophilia, rash), Cataflam should be discontinued. Hepatitis may occur with use of diclofenac without prodromal symptoms.
Caution is called for when using Cataflam in patients with hepatic porphyria, since it may trigger an attack.
Renal Effects: As fluid retention and oedema have been reported in association with NSAID therapy, including diclofenac, particular caution is called for in patients with impaired cardiac or renal function, history of hypertension, the elderly, patients receiving concomitant treatment with diuretics or medicinal products that can significantly impact renal function, and in those patients with substantial extracellular volume depletion from any cause eg, before or after major surgery (see Contraindications). Monitoring of renal function is recommended as a precautionary measure when using Cataflam in such cases. Discontinuation of therapy is normally followed by recovery to the pre-treatment state.
Haematological Effects: Use of Cataflam is recommended only for short-term treatment. If, however, Cataflam is used for a prolonged period, monitoring of the blood count is recommended, as with other NSAIDs.
Like other NSAIDs, Cataflam may temporarily inhibit platelet aggregation. Patients with defects of haemostasis should be carefully monitored.
Effects on the Ability to Drive or Operate Machinery: Patients experiencing visual disturbances, dizziness, vertigo, somnolence or other central nervous disturbances while taking Cataflam should refrain from driving or using machines.
Impairment of Fertility:
As with other NSAIDs, the use of Cataflam may impair female fertility and is not recommended in women attempting to conceive. In women who have difficulties conceiving or who are undergoing investigation of infertility, withdrawal of Cataflam should be considered.
Use in lactation: Like other NSAIDs, diclofenac passes into the breast milk in small amounts. Therefore, Cataflam should not be administered during breast feeding in order to avoid undesirable effects in the infant.
Use In Pregnancy & Lactation
Use in pregnancy: The use of diclofenac in pregnant women has not been studied. Therefore, Cataflam should not be used during the first 2 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 3rd trimester of pregnancy is contraindicated owing to the possibility of uterine inertia and/or premature closure of the ductus arteriosus. Animal studies have not shown any directly or indirectly harmful effects on pregnancy, embryonal/foetal development, parturition or postnatal development (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
Use in lactation: Like other NSAIDs, diclofenac passes into the breast milk in small amounts. Therefore, Cataflam should not be administered during breast feeding in order to avoid undesirable effects in the infant.
Adverse Reactions
Adverse reactions are ranked under heading of frequency, the most frequent first, using the following convention: Common (≥1/100, <1/10); uncommon (≥1/1,000, <1/100); rare (≥1/10,000, <1/1,000); very rare (<1/10,000), including isolated reports.
The following adverse reactions include those reported with Cataflam sugar-coated tablets and/or other pharmaceutical forms of diclofenac, with either short-term or long-term use.
Blood and Lymphatic System Disorders: Very Rare: Thrombocytopenia, leukopenia, anaemia (including haemolytic and aplastic anaemia), agranulocytosis.
Immune System Disorders: Rare: Hypersensitivity, anaphylactic and anaphylactoid reactions (including hypotension and shock). Very Rare: Angioneurotic oedema (including face oedema).
Psychiatric Disorders: Very Rare: Disorientation, depression, insomnia, nightmare, irritability, psychotic disorder.
Nervous System Disorders: Common: Headache, dizziness. Rare: Somnolence. Very Rare: Paraesthesia, memory impairment, convulsion, anxiety, tremor, aseptic meningitis, taste disturbances, cerebrovascular accident.
Eye Disorders: Very Rare: Visual disturbance, blurred vision, diplopia.
Ear and Labyrinth Disorders: Common: Vertigo. Very Rare: Tinnitus, impaired hearing.
Cardiac Disorders: Very Rare: Palpitations, chest pain, cardiac failure, myocardial infarction.
Vascular Disorders: Very Rare: Hypertension, vasculitis.
Respiratory, Thoracic and Mediastinal Disorders: Rare: Asthma (including dyspnoea). Very Rare: Pneumonitis.
Gastrointestinal Disorders: Common: Nausea, vomiting, diarrhoea, dyspepsia, abdominal pain, flatulence, anorexia. Rare: Gastritis, gastrointestinal haemorrhage, haematemesis, haemorrhagic diarrhoea, melaena, gastrointestinal ulcer (with or without bleeding or perforation). Very Rare: Colitis (including haemorrhagic colitis and exacerbation of ulcerative colitis or Crohn’s disease), constipation, stomatitis, glossitis, oesophageal disorder, diaphragm-like intestinal strictures, pancreatitis.
Hepatobiliary Disorders: Common: Increased transaminases. Rare: Hepatitis, jaundice, liver disorder. Very Rare: Fulminant hepatitis, hepatic necrosis, hepatic failure.
Skin and Subcutaneous Tissue Disorders: Common: Rash. Rare: Urticaria. Very Rare: Bullous eruptions, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, loss of hair, photosensitivity reaction, purpura, allergic purpura, pruritus.
Renal and Urinary Disorders: Very Rare: Acute renal failure, haematuria, proteinuria, nephrotic syndrome, interstitial nephritis, renal papillary necrosis.
General Disorders and Administration Site Conditions: Rare: Oedema.
Drug Interactions
The following interactions include those observed with Cataflam sugar-coated tablets and/or other pharmaceutical forms of diclofenac.
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 [eg, β-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 (see Warnings and Precautions).
Other NSAIDs and Corticosteroids: Concomitant administration of diclofenac and other systemic NSAIDs or corticosteroids may increase the frequency of gastrointestinal undesirable effects (see Warnings and Precautions).
Anticoagulants and Antiplatelet Agents: Caution is recommended since concomitant administration could increase the risk of bleeding (see Warnings and Precautions). Although clinical investigations do not appear to indicate that diclofenac affects the action of anticoagulants, there are isolated reports of an increased risk of haemorrhage in patients receiving diclofenac and anticoagulants concomitantly. Close monitoring of such patients is therefore recommended.
Selective Serotonin Reuptake Inhibitors (SSRIs): Concomitant administration of systemic NSAIDs, including diclofenac, and SSRIs may increase the risk of gastrointestinal bleeding (see Warnings and Precautions).
Antidiabetics: Clinical studies have shown that diclofenac can be given together with oral antidiabetic agents without influencing their clinical effect. However, there have been isolated reports of both hypoglycaemic and hyperglycaemic effects necessitating changes in the dosage of the antidiabetic agents during treatment with diclofenac. For this reason, monitoring of the blood glucose level is recommended as a precautionary measure during concomitant therapy.
Methotrexate: Caution is recommended when NSAIDs, including diclofenac, are administered <24 hrs before or after treatment with methotrexate, since blood concentrations of methotrexate may rise and the toxicity of this substance be increased.
Ciclosporin: Diclofenac, like other NSAIDs, may increase the nephrotoxicity of ciclosporin due to the effect on renal prostaglandins. Therefore, it should be given at doses lower than those that would be used in patients not receiving ciclosporin.
Quinolone Antibacterials: There have been isolated reports of convulsions which may have been due to concomitant use of quinolones and NSAIDs.
Potent CYP2C9 Inhibitors: Caution is recommended when co-prescribing diclofenac with potent CYP2C9 inhibitors (eg, sulfinpyrazone and voriconazole), which could result in a significant increase in peak plasma concentrations and exposure to diclofenac due to inhibition of diclofenac metabolism.
Phenytoin: When using phenytoin concomitantly with diclofenac, monitoring of phenytoin plasma concentrations is recommended due to an expected increase in exposure to phenytoin.
Incompatibilities: Not applicable.
Caution For Usage
Cataflam tablets must be kept out of reach and sight of children.
ATC Classification
M01AB05 - diclofenac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.
Coated tab 25 mg x 100's. 50 mg x 100's.
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