Ibuprofen is a phenylpropionic acid derivative which has analgesic, antipyretic and anti-inflammatory actions. Ibuprofen is absorbed from gastrointestinal tract and peak plasma concentration occurs about 1 to 2 hours after ingestion. It is extensively bound to plasma proteins and is rapidly excreted in the urine, mainly as metabolites and their conjugates. Approximately 1% is excreted in the urine as unchanged ibuprofen and about 14% as conjugated ibuprofen.
Zofen has analgesic, antipyretic and anti-inflammatory actions and is used for the relief of fever and mild to moderate pain such as menstrual pains (dysmenorrhea) and transient musculoskeletal pain. It is also indicated for pain and mild inflammation in rheumatic conditions and may be useful in dental pain and due to sports injuries.
Unless otherwise prescribed by the physician: Adults: One or two tablets four times a day, preferably with food or milk.
The total dose in 24 hours should not exceed 12 tablets.
Zofen should be used at the lowest effective dose for shortest possible time.
Zofen should not be used in severe or active peptic ulceration.
Zofen is contraindicated: In patients with severe heart failure; For the treatment of peri-operative pain in the setting of coronary artery bypass graft surgery.
History of gastrointestinal bleeding of perforation, related to previous NSAIDs therapy; active, or history of recurrent peptic ulcer/haemorrhage.
NSAID: Risk of GI ulceration, bleeding and perforation.
Serious GI toxicity such as bleeding, ulceration and perforation can occur at any time with or without symptoms, in patients treated with NSAID therapy. Although minor upper GI problems (e.g. dyspepsia) are common, usually developing early in therapy, prescribers should remain alert for ulceration and bleeding in patients treated with NSAIDs even in the absence of previous GI tract symptoms.
Studies to date have not identified any subset of patients not at risk of developing peptic ulceration and bleeding. Patients with prior history of serious adverse events and other risk factors associated with peptic ulcer disease (e.g. alcoholism, smoking, corticosteroid therapy) are at increased risk. Elderly or debilitated patients seem to tolerate ulceration or bleeding less than other individuals and account for most spontaneous reports for fatal GI events.
Use with caution in gastric ulceration, allergic disorder particularly in asthma and hypersensitivity to salicylates (e.g. aspirin) and renal (kidney) and hepatic (liver) impairment. It is best avoided in pregnancy as its safety for such use has not been absolutely established. In rare cases, ibuprofen has been associated with serious liver injury.
Cardiovascular and Cerebrovascular Effects: NSAIDs may cause an increased risk of serious cardiovascular thrombotic event, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cadiovascular disease may be at greater risk.
Non-selective NSAIDs may be associated with a small increase in the absolute risk of cardiovascular events (e.g. myocardial infarction and stroke), especially when used at high doses for long-term treatment.
Clinical studies suggest that use of ibuprofen, particularly at a high dose (2,400 mg/day), may be associated with a small increased risk of arterial thrombotic events (for example myocardial infarction or stroke). Overall, epidemiological studies do not suggest that low dose ibuprofen (e.g. ≤1,200 mg/day) is associated with an increased risk of arterial thrombotic events, particularly myocardial infarction. All NSAIDs should be prescribed at the lowest effective dose and the duration of treatment should be periodically reviewed and kept as short as possible.
Patients with uncontrolled hypertension, congestive heart failure, established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should only be treated with ibuprofen after careful consideration and high doses (2400mg/day) should be avoided. Careful consideration should also be exercised before initiating long-term treatment of patients with risk factors for cardiovascular events (e.g. hypertension, hyperlipidemia, diabetes mellitus, smoking), particularly if high doses of ibuprofen (2400mg/day) are required.
All NSAIDs should not be used perioperatively in patients who have recently undergone coronary artery bypass graft (CABG) surgery and revascularization procedure.
Gastrointestinal Risk: NSAIDs cause an increased risk of gastrointestinal adverse events including bleeding, ulceration and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients are at greater risk for serious gastrointestinal events.
Renal Effects: Long-term administration of NSAIDs has resulted in renal papillary necrosis and other renal injury. Renal toxicity has also been seen in patients in whom renal prostaglandins have a compensatory role in the maintenance of renal perfusion. In these patients, administration of a NSAID may cause a dose-dependent reduction in prostaglandins formation and secondarily in renal blood flow, which may precipitate overt renal decompensation. Patients at greater risk of this reaction are those with impaired renal function, heart failure, liver dysfunction, those taking diuretics and ACE inhibitors, and the elderly. Discontinuation of NSAID therapy is usually followed by recovery to the pretreatment state.
Advanced Renal Disease: No information is available from controlled clinical studies regarding the use of Zofen in patients with advance renal disease. Therefore, treatment with Zofen is not recommended in these patients with advanced renal disease. If therapy must be initiated, close monitoring of the patient's renal function is advisable.
Measures such as the use of physical therapy and mild analgesics like paracetamol (when inflammation is not a major factor) should be instituted prior to initiation of therapy with NSAID. NSAIDs should only be used after proper appraisal of potential risks to patients. It should be used with lowest effective dose for only as long as needed.
This drug should not be co-administered with other NSAIDs. Prescribers should inform patients about the signs and/or symptoms of serious GI toxicity and what steps to take if they occur. In considering the use of relatively large doses (within the recommended dosage range), sufficient benefit should offset the potential increased risk of GI toxicity.
Gastrointestinal discomfort and occasional gastro-intestinal bleeding and nausea may occur. These side effects may be reduced if the medication is taken with food or milk. Other side effects may include hypersensitivity reactions such as asthma, pruritus, urticaria and and rashes; headache; vertigo; tinnitus; and in rare cases fluid retention.
Ibuprofen may reduce the antihypotensive effect of antihypertensive. It may potentiate the effect of lithium and digoxin when given concomitantly. Diuretics may increase the risk of nephrotoxicity of NSAIDs.
Acetylsalicylic acid/Aspirin: As with other products containing NSIADs, concomitant administration of ibuprofen and acetylsalicylic acid/aspirin is not generally recommended because of the potential of increased adverse effects.
Experimental data suggest that ibuprofen may competitively inhibit the effect of low dose acetylsalicylic acid/aspirin on platelet aggregation when they are dosed concomitantly. Some pharmacodynamics studies show that when single doses of ibuprofen 400 mg were taken within 8 h before or within 30 min after immediate release aspirin dosing (81 mg), a decreased effect of acetylsalicylic acid/aspirin on the formation of thromboxane or platelet aggregation occurred. Although there are uncertainties regarding extrapolation of these data to the clinical situation, the possibility that regular, long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid/aspirin cannot be excluded. No clinically relevant effect is considered to be likely for occasional ibuprofen use.
Store in a cool dry place below 30°C.
M01AE01 - ibuprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.
FC tab (orange) 200 mg x 20's, 1000's.