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Pharmacological group: Other analgesics and antipyretic, anti-inflammatory drugs. ATC Code: M01AE01.
Pharmacology: Pharmacodynamics: Ibuprofen is a non-steroidal anti-inflammatory drug, belonging to the propionic group, derived from aryl carboxylic acid. Ibuprofen has the following properties: Analgesic property, Antipyretic property, Anti-inflammatory property, Property of short-term inhibition of platelet function.
Experimental data suggest that ibuprofen competitively inhibits the effect of low doses of acetylsalicylic acid on platelet aggregation when co-administered. Pharmacodynamic studies show that when single doses of ibuprofen 400 mg were taken within 8 hours before or within 30 minutes after administration of immediate-release acetylsalicylic acid (81 mg), a decrease in the effect acetylsalicylic acid on thromboxane formation or platelet aggregation occurs. Although there are uncertainties regarding the extrapolation of these data to clinical situations, the possibility that regular, long-term ibuprofen use, may reduce the cardioprotective effect of low doses of acetylsalicylic acid cannot be excluded. No clinically relevant effects are considered likely with occasional use of ibuprofen.
Pharmacokinetics: Absorption: Maximum serum concentration is reached approximately 25 minutes after oral administration.
After a single dose, the maximum serum concentrations are proportional to the dose (Cmax between 56.4 = 13.6 ug/ml for the 400 mg dose).
Concomitant food intake does not influence the rate of absorption but delays absorption by about 1 hour, resulting in a lower Cmax (about 50%).
Distribution: The administration of ibuprofen does not give rise to accumulation phenomena. It is 99 percent bound to plasma proteins.
In the synovial fluid, ibuprofen is found with stable concentrations between the second and eighth hour after intake, the synovial Cmax, being approximately equal to one third of the plasma Cmax After taking 400 mg of ibuprofen every 6 hours by breastfeeding women, the amount of ibuprofen found in their milk is less than 1 mg per 24 hours.
Metabolism: Ibuprofen has no enzyme-inducing effect. It is metabolized for 90% in the form of inactive metabolites.
Excretion: The plasma half-life is 1-2 hours. More than 90% of the dose is recovered in the urine in the form of metabolites and conjugates.
Less than 1% is excreted in the urine unchanged.
Special Groups: Elderly: No signs of accumulation or retention in specific compartments were observed in the elderly. A dose modification is therefore not warranted.
Kidney failure: Mild to moderate renal impairment does not appear to prolong plasma elimination half-life. Patients with end stage renal disease should not take ibuprofen as it is likely to increase the risk of systemic accumulation.
Liver failure: There is little evidence of altered plasma pharmacokinetics in mild hepatic impairment. Patients with severe liver disease should not take ibuprofen as it is likely to increase the risk of systemic accumulation.
Children: The pharmacokinetics of ibuprofen in children aged 12 years and over are comparable to those observed in adults.
