IBUMOL®
Composition:
Each uncoated tablet contains:
Paracetamol BP............325 mg
Ibuprofen BP.................400 mg
DESCRIPTION
Ibumol is an anti-inflammatory analgesic combination. Ibuprofen is a potent anti-inflammatory with analgesic and antipyretic action. Its analgesic and antipyretic effects are further reinforced by Paracetamol.
CLINICAL PHARMACOLOGY
Mechanism of action:
Ibuprofen is a non steroidal anti-inflammatory agent used in painful inflammatory conditions. This acts by biosynthesis and release of prostaglandins in the cells. It inhibits the enzymes prostaglandin synthetase.
Paracetamol is an analgesic and antipyretic agent. It is a weak anti-inflammatory agent as it is a weak inhibitor of cyclo-oxygenase in presence of high concentrations of peroxides that are found in inflammatory lesions. Paracetamol does not inhibit neutrophil activation as other NSAIDs.
The antipyretic activity is due to the direct action on the hypothalmic heat regulating centres that results in increase dissipation of body heat. The two drugs combined have an additive effect in relief of pain and inflammation. Ibuprofen acts peripherally and Paracetamol acts centrally, thus reinforcing analgesic activity in the combination.
Pharmacokinetics:
Absorption:
Ibuprofen is absorbed from the GI tract and peak plasma concentrations occur about 1-2 hours after ingestion. It is 90-99% bound to plasma proteins and has a half life of 2 hours.
Paracetamol is well absorbed from the GI tract with peak plasma concentration occurring 10-60 minutes after ingestion. The plasma elimination half-life ranges from 1 to 3 hours for Paracetamol.
Distribution:
Ibuprofen has high plasma protein binding which results in a relatively low volume of distribution, about 0.1 litre/kg. Only very small amounts of Ibuprofen are excreted in breast milk. It is not known whether the drug crosses the placenta.
Paracetamol is distributed into most body tissues. It crosses the placenta and is present in breast milk. It is metabolized primarily in the liver.
Elimination:
Ibuprofen is eliminated rapidly in urine. 1% is excreted unchanged and 14.5% as conjugated Ibuprofen.
Paracetamol is excreted in the urine mainly as glucoronide and sulfate conjugates. Less than 5% is excreted as conjugated Paracetamol.
INDICATIONS
Pain and inflammation associated with musculoskeletal and joint disorders.
CONTRAINDICATIONS
Not to be used in patients with active peptic ulcer history of hypersensitivity to either component recent GI bleeding & in neonates.
PRECAUTIONS
Bronchospasm may be precipitated in patients suffering from or with a previous history of bronchial asthma.
Ibuprofen should not be given to patients in whom aspirin and other non-steroidal anti-inflammatory drugs induce the symptoms of asthma, rhinitis or urticaria.
WARNINGS
Overdose may be injurious to liver.
PREGNANCY AND LACTATION:
Ibuprofen:
Pregnancy Category C: Adequate and well -controlled studies in humans have not been done. Studies in animals have not shown that these agents cause adverse effects on fetal development.
Second and third trimesters: Although studies in humans have not been done with NSAIDs other than indomethacin, use of NSAIDs during the second half of pregnancy is not recommended because of possible adverse effects on the fetus, such as premature closure of the ductus arteriosus, which may lead to persistent pulmonary hypertension in the newborn.
Studies in full-term pregnant rats have shown Ibuprofen have a strong constrictive effect on the fetal ductus arteriosus.
Animal studies have also shown that administration of NSAIDS during late pregnancy may cause prolonged gestation, dystocia and delayed parturition, possibly because of decreased uterine contractility resulting from inhibition of uterine prostaglandins. Decreases in pup survival rates also have been reported.
Breast Feeding: Studies in humans have failed to detect Ibuprofen in breast milk using methodology capable of detecting the medication in a concentration of 1 mcg/mL.
The maternal dosage was 400 mg four times a day.
Paediatrics: Appropriate studies performed to date have not demonstrated paediatrics-specific problems that would limit the usefulness of Ibuprofen in children 6 months of age or older. Safety and efficacy in infants younger than 6 months of age have not been established.
Geriatrics: Whether geriatric patients are at increased risk of serious gastrointestinal toxicity during NSAID therapy has not been established. However, NSAID-induced gastrointestinal ulceration and/or bleeding may be more likely to cause serious consequences, including fatalities, in geriatric patients than in younger adults. In addition, elderly patients are more likely to have agerelated renal function impairment, which may increase the risk of NSAID- induced hepatic or renal toxicity and may also require dosage reduction to prevent accumulation of the medication. Some clinicians
recommend that geriatric patients, especially those 70 years of age or older, be given one half of the usual adult dose initially. Also, careful monitoring of the patient is recommended.
Paracetamol:
Fertility: Chronic toxicity studies in animals have shown that high doses of Paracetamol cause testicular atrophy and inhibition of spermatogenesis; the relevance of this finding to use in humans is not known.
Pregnancy: Problems in humans have not been documented. Although controlled studies have not been done, it has been shown that acetaminophen crosses the placenta.
Breast-feeding: Problems in humans have not been documented. Although peak concentrations of 10 to 15 mcg per mL (66.2 to 99.3 micromoles/L) have been measured in breast milk 1 to 2 hours following maternal ingestion of a single 650-mg dose, neither Paracetamol nor its metabolites were detected in the urine of the nursing infants. The half-life in breast milk is 1.35 to 3.5 hours.
Paediatrics: Studies performed to date have not demonstrated paediatrics specific problems that would limit the usefulness of Paracetamol in children.
Geriatrics: Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of Paracetamol in the elderly.
ADVERSE REACTIONS
Dyspepsia, heart burn, GI bleeding, rash, asthmatic attacks, thrombocytopenia, drug induced ulcer, drowsiness, hepatic necrosis, renal papillary necrosis, vision disturbances & disorientation; rarely nausea & vomiting can occur.
Potentially Fatal: Hematemesis, agranulocytosis, severe allergic reaction.
DRUG INTERACTIONS:
Ibuprofen:
• Coumarin-Type Anticoagulants: Several short-term controlled studies failed to show that Ibuprofen significantly affected prothrombin times or a variety of other clotting factors when administered to individuals on coumarin-type anticoagulants. However, because bleeding has been reported when Ibuprofen and other nonsteroidal anti-inflammatory agents have been administered to patients on coumarin-type anticoagulants, the physician should be cautious when administering Ibuprofen to patients on anticoagulants.
• Aspirin: Animal studies show that aspirin given with nonsteroidal anti-inflammatory agents, including Ibuprofen, yields a net decrease in anti-inflammatory activity with lowered blood levels of the non-aspirin drug. Single dose bioavailability studies in normal volunteers have failed to show an effect of aspirin on Ibuprofen blood levels. Correlative clinical studies have not been performed.
• Methotrexate: Ibuprofen, as well as other nonsteroidal anti-inflammatory drugs, probably reduces the tubular secretion of methotrexate based on in vitro studies in rabbit kidney slices. This may indicate that Ibuprofen could enhance the toxicity of methotrexate. Caution should be used if Ibuprofen is administered concomitantly with methotrexate.
• H₂ Antagonists: In studies with human volunteers, coadministration of cimetidine or ranitidine with Ibuprofen had no substantive effect on Ibuprofen serum concentrations,
• Furosemide: Clinical studies, as well as random observations, have shown that Ibuprofen can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition of renal prostaglandin synthesis. During concomitant therapy with Ibuprofen, the patient should be observed closely for signs of renal failure as well as to assure diuretic efficacy.
• Lithium: Ibuprofen produced an elevation of plasma lithium levels and a reduction in renal lithium clearance in a study of eleven normal volunteers. The mean minimum lithium concentration increased 15% and the renal clearance of lithium was decreased by 19% during this period of concomitant drug administration.
This effect has been attributed to inhibition of renal prostaglandin synthesis by Ibuprofen. Thus, when Ibuprofen and lithium are administered concurrently, subjects should be observed carefully for signs of lithium toxicity.
Paracetamol:
None reported.
DOSAGE
1 tablet three times a day or as directed by physician.
Presentation: Available in blister pack of 4 & 10 tablets.
PRECAUTIONS FOR STORAGE
Store at temperature below 30°C.
Protect from light.
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