Information about UNI BRUFEN
Film Coated Tablet (200 mg, 400 mg, 600 mg)
Oral Suspension (100 mg/5 mL, 200 mg/5 mL)
The Composition:
Each Film Coated Tablet Contains:
200 mg, 400 mg or 600 mg Ibuprofen.
Each 5ml Contains:
Ibuprofen 100 or 200 mg.
Pharmacology:
Ibuprofen is a non-steroidal anti-inflammatory agent that possesses analgesic and antipyretic activities. Its mode of action, like that of other non-steroidal anti-inflammatory agents, is not completely understood, but may be related to prostaglandin synthetize inhibition.
Ibuprofen has shown anti-inflammatory, analgesic and antipyretic activity in both animal and human studies. These properties provide symptomatic relief of inflammation and pain in rheumatoid arthritis, osteoarthritis and allied conditions.
Pharmacokinetics:
Absorption: Ibuprofen is well absorbed after oral administration. Single dose of 200 mg taken on an empty stomach by volunteers produced peak serum levels after approximately 45 minutes. When taken after food, absorption was slower, peak levels appearing at 1.5 to 3 hours.
Distribution: Apparent volume of distribution is 0.14 L/kg. Ibuprofen and its metabolites readily cross the placental barrier in pregnant rabbits and rats. It is not known if ibuprofen enters the CSF or is excreted in milk.
Protein binding: 99% of ibuprofen is protein bound. The high protein binding of ibuprofen should be borne in mind when prescribing ibuprofen together with other protein bound drugs which bind to the same site on human serum albumin.
Metabolism: About 90% of ibuprofen is metabolized to two major metabolites .Both metabolites are dextrorotatory and are devoid of anti-inflammatory and analgesic activity.
Excretion: The kidney is the major route of excretion. 95% of ibuprofen was excreted in the urine within 24 hours of a single dose of 500 mg.
Half-life: Plasma half-life of ibuprofen is in the range 1.9 to 2.2 hours.
Indications:
• Rheumatoid arthritis.
• Osteoarthritis.
• Juvenile rheumatoid arthritis.
• Primary dysmenorrhea.
• Pyrexia.
• Ibuprofen is also indicated for the relief of acute and/or chronic pain states in which there is an inflammatory component.
Contraindications:
• Known hypersensitivity to ibuprofen or any of the inactive ingredients.
• Hypersensitivity (e.g. asthma, rhinitis or urticaria) to aspirin or other nonsteroidal anti-inflammatory drugs.
• History of gastrointestinal bleeding or perforation, related to previous NSAID therapy.
• History of, ulcerative colitis, Crohn’s disease, recurrent peptic ulceration or gastrointestinal hemorrhage (defined as two or more distinct episodes of proven ulceration or bleeding).
• Severe heart failure.
• Severe liver failure.
• Severe renal failure (glomerular filtration below 30ml/min).
• Conditions involving an increased tendency or active bleeding.
• During the third trimester of pregnancy.
Possible Side Effects:
The most common (greater than 1%) adverse effects reported include: nausea, epigastric pain, heartburn, diarrhea, abdominal distress, nausea and vomiting, dyspepsia, abdominal cramps or pain, constipation, gastrointestinal hemorrhage, hematemesis, flatulence, tinnitus, hearing impaired, edema, fluid retention generally responds promptly to discontinuation of the drug, dizziness, headache. nervousness, decreased appetite, fatigue.
Hypersensitivity reactions have also been reported following treatment with NSAIDs. These may include:
• Non-specific allergic reaction and anaphylaxis.
• Resiratory tract reactivity comprising asthma, bronchospasm or dyspnoea.
• Assorted skin disorders, including rashes, pruritus, urticaria, purpurea, angioedema and more rarely, exfoliative and bullous dermatoses.
• Warnings and Precutions:
• *Hypertension:
- NSAIDs may lead to onset of new hypertension or worsening of pre-existing hypertension and patients taking anti-hypertensive with NSAIDs may have an impaired anti-hypertensive response .Caution is advised when prescribing NSAIDs to patients with hypertension and monitoring blood pressure when initiating therapy and regularly thereafter on long term treatment.
• *Heart Failure:
- Fluid retention and edema have been observed in some patients taking NSAIDs; therefore, caution is advised in patients with fluid retention or heart failure.
• *Respiratory Disorders:
- Caution is required if ibuprofen is administered to patients suffering from ,or with a previous history of ,bronchial asthma, chronic rhinitis or allergic diseases since ibuprofen has been reported to cause bronchospasm ,urticaria or angiooedema in such patients.
• *Impaired Liver Function or History of Liver Disease:
- Patients with impaired liver function or history of liver disease who are on long-term ibuprofen therapy should have hepatic function monitored at regular intervals. Ibuprofen has been reported to have a minor and transient effect on liver enzymes. Severe hepatic reactions including jaundice and cases of fatal hepatitis, though rare, have been reported with ibuprofen as with other NSAIDs. If abnormal liver tests persist or worsen, or if clinical signs and symptoms consistent with liver disease develop, or if systemic manifestations occur (e.g. eosinophilia, rash, etc.), ibuprofen should be discontinued.
• *Impaired Renal Function:
- Caution should be used when initiating treatment with ibuprofen in patients with considerable dehydration. There is a risk of renal impairment especially in dehydrated children and adolescents. In patients with renal, cardiac or hepatic impairment, those taking diuretics and ACE inhibitors, and the elderly, caution is required since the use of NSAIDs may result in deterioration of renal function. The long-term concomitant intake of various analgesics further increases the risk. For patients with renal, hepatic or cardiac impairment, use the lowest effective dose, for the shortest possible duration and monitor renal function especially in long-term treated patients.
• *Hematological Effects:
- Anemia is sometimes seen in patients receiving NSAIDs, including ibuprofen. Patients on long-term treatment with NSAIDs, including ibuprofen, should have their hemoglobin or hematocrit checked if they exhibit any signs or symptoms of anemia.
- NSAIDs inhibit platelet aggregation and have been shown to prolong bleeding time in some patients. Unlike aspirin, their effect on platelet function is quantitatively less, of shorter duration, and reversible.
• *Skin Reactions:
- NSAIDs, including ibuprofen, can cause serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), which can be fatal. The drug should be discontinued at the first appearance of skin rash or any other sign of hypersensitivity.
• *Ophthalmological Effects:
- Blurred and/or diminished vision, scotoma, and/or changes in color vision have been reported. When such complications occur the drug should be discontinued.
• *Aseptic Meningitis:
- Aseptic meningitis with fever and coma has been observed on rare occasions in patients on ibuprofen therapy.
• *Anaphylactoid Reactions:
- As with other NSAIDs, anaphylactoid reactions may occur in patients without known exposure to ibuprofen. This symptom complex typically occurs in asthmatic patients who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs. Emergency help should be sought in cases where an anaphylactoid reaction occurs.
• *Pre-existing asthma:
- Patients with asthma may have aspirin-sensitive asthma. The use of aspirin in patients with aspirin-sensitive asthma has been associated with severe bronchospasm, which can be fatal. Since cross reactivity, including bronchospasm between aspirin and NSAIDs has been reported in such aspirin-sensitive patients, ibuprofen should not be administered to patients with this form of aspirin sensitivity and should be used with caution in patients with preexisting asthma.
• *As with other NSAIDs, ibuprofen may mask the signs of infection.
Drug Interactions:
• *IBUPROFEN SHOULD NOT BE USED IN COMBINATION WITH:
- Aspirin (above 75mg daily): This may increase the risk of adverse reactions.
- Other NSAIDs: These may increase the risk of adverse reactions.
• *IBUPROFEN SHOULD BE USED WITH CAUTION IN COMBINATION WITH:
- ACE inhibitors: NSAIDs may diminish the antihypertensive effect of ACE inhibitors.
- Aspirin (as anti-aggregant): As with other NSAIDs, concomitant administration of ibuprofen and aspirin is not generally recommended because of the potential for increased adverse effects.
- Selective serotonin-reuptake inhibitors: may increase the risk of gastrointestinal bleeding.
- Corticosteroids: may increase the risk of adverse reactions, especially of the gastrointestinal tract.
- Cyclosporine: NSAIDs may increase the plasma concentration of cyclosporine and the risk of cyclosporine nephrotoxicity.
- Zidovudine: There is an evidence of an increased risk of haemarthroses and haematoma in HIV positive haemophiliacs receiving concurrent treatment with zidovudine and ibuprofen.
- Diuretics: Ibuprofen can reduce the natriuretic effect of furosemide and thiazides in some patients.
- Anticoagulants (coumarin type): Bleeding has been reported when ibuprofen and other NSAIDs have been administered to patients on coumarin-type anticoagulants. The effects of warfarin and NSAIDs on GI bleeding are synergistic. - Lithium: There is evidence for potential increase in plasma levels of lithium.
- Methotrexate: NSAIDs may enhance the toxicity of methotrexate.
- H-2 Antagonists: Co-administration of cimetidine or ranitidine with ibuprofen had no
Pregnancy:
During the first and second trimester of pregnancy, ibuprofen should not be given unless clearly necessary. If ibuprofen is used by a woman attempting to conceive, or during the first or second trimester of pregnancy, the dose should be kept as low and duration of treatment as short as possible.
Ibuprofen is contraindicated during the last trimester of pregnancy.
Lactation:
Ibuprofen is not recommended for use in nursing mothers.
Female Fertility:
The use of ibuprofen 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 ibuprofen should be considered.
Effects on ability to drive and to use machines:
Patients who experience dizziness, drowsiness, vertigo, or visual disturbances while taking ibuprofen, should avoid driving or using machinery. Single administration or short-term use of ibuprofen does not usually warrant the adoption of special precautions.
Dosage and Administration:
For Film Coated Tablet:
It should be swallowed preferably with a drink of water. Taken with or after food.
After assessing the risk/benefit ratio in each individual patient, the lowest effective dose for the shortest duration should be used.
*ADULTS:
The recommended initial dosage of ibuprofen is 1200mg-1800 mg daily in divided doses. Some patients can be maintained on 600-1200 mg daily. In severe or acute conditions, it can be advantageous to increase the dosage until the acute phase is brought under control, providing that the total daily dosage does not exceed 2400 mg in divided doses.
*Primary Dysmenorrhea:
The initial dose is 400-800 mg at the first sign of pain or menstrual bleeding, then 400 mg 4-6 hourly with a maximum total daily dose of 1600 mg.
*Children:
The daily dosage of ibuprofen is 20 mg per kg of body weight in divided doses. In juvenile rheumatoid arthritis up to 40 mg/kg of body, weight in divided doses may be taken. In children, weighing less than 30 kg the total dose given in 24 hours should not exceed 500 mg.
*Maintenance Dose:
In all indications, the dose should be adjusted for each patient and the smallest dose that results in acceptable control of the symptoms employed. In general, patients with rheumatoid arthritis and osteoarthritis tend to require higher doses than patients with other conditions.
*Elderly: In elderly patients, receiving 600-1200 mg daily ibuprofen appeared to be well tolerated. However, since elderly patients may have a degree of impaired liver or renal function the adult dosage should be used with caution.
*Impaired Hepatic or Renal Function:
Ibuprofen should be used with caution in patients with impaired liver or renal function.
For Oral Suspension Syrup:
Directions for use:
Shake well before using.
The dose could be repeated every 6 – 8 hours, if needed. But not more than 4 times a day.
Pediatric Patients:
Fever Reduction: In children, 6 months up to 2 years of age, the dosage should be adjusted on the basis of the initial temperature level. The recommended dose is 5 mg/kg if the baseline temperature is less than 39ºC, or 10 mg/kg if the baseline temperature is 39ºC or greater. The duration of fever reduction is generally 6 to 8 hours. The recommended maximum daily dose is 40 mg/kg.
Analgesia: For mild to moderate pain in children 6 months up to 2 years of age, the recommended dosage is 10 mg/kg, every 6 to 8 hours. The recommended maximum daily dose is 40 mg/kg. Doses should be given so as not to disturb the child's sleep pattern.
Juvenile Arthritis: The recommended dose is 30 to 40 mg/kg/day divided into three to four doses. Patients with milder disease may be adequately treated with 20 mg/kg/day. In patients with juvenile arthritis, doses above 50 mg/kg/day are not recommended because they have not been studied and doses exceeding the upper recommended dose of 40 mg/kg/day may increase the risk of causing serious adverse events. The therapeutic response may require from a few days to several weeks to be achieved. Once a clinical effect is obtained, the dosage should be lowered to the smallest dose of Ibuprofen Oral Suspension needed to maintain adequate control of symptoms. Pediatric patients receiving doses above 30 mg/kg/day or if abnormal liver function tests have occurred with previous NSAID treatments should be carefully followed for signs and symptoms of early liver dysfunction.
Overdosage:
*Symptoms:
Headache, nausea, abdominal pain and vomiting, gastrointestinal bleeding. Rarely: diarrhea, disorientation, excitation, drowsiness, dizziness, tinnitus, fainting, depression of the CNS and the respiratory system, coma, occasionally convulsions and rarely, loss of consciousness. In cases of significant poisoning, acute renal failure and liver damage are possible.
*Management:
There is no specific antidote to ibuprofen.
The treatment is symptomatic and supportive and include the maintenance of a clear airway and monitoring of cardiac and vital signs until stable. Activated charcoal should be considered if the patient is presented within 1 hour of ingestion of a potentially toxic amount. The patient should be observed for at least four hours after ingestion of a potentially toxic amount. Hepatic and renal function should be controlled. Frequent or prolonged convulsions should be treated with intravenous diazepam. Give bronchodilators for asthma.
Storage:
For Film Coated Tablets: Store below 30°C.
For Oral Suspension Syrup: Store below 30°C, Away from Light
Presentation:
• Film Coated Tablets:
For Strength 200 mg: Carton Pack of 24 Film Coated Tablets
For Strength 400 mg: Carton Pack of 24 Film Coated Tablets.
For Strength 600 mg: Carton Pack of 10 Film Coated Tablets.
• For Oral Suspension Syrup:
Carton Pack Contains Glass Bottle (Amber) of 100 mL