Source: Medicines and Medical Devices Safety Authority (NZ) Revision Year: 2021 Publisher: Rex Medical Limited, PO Box 18-119, Glen Innes, Auckland Telephone (09) 574 6060
Pharmacotherapeutic group: Anti-inflammatory and Antirheumatic Products, Non-Steroids
ATC code: M01AE01
Ibuprofen is a non-steroidal anti-inflammatory agent. Its mode of action, like that of other nonsteroidal anti-inflammatory agents, is not completely understood, but may be related to prostaglandin synthetase inhibition. Ibuprofen has shown anti-inflammatory, analgesic and antipyretic activity in both human and animal studies. These properties provide symptomatic relief of inflammation and pain.
Ibuprofen is well absorbed after oral administration. A single dose of 200mg taken on an empty stomach by volunteers produced peak serum levels after approximately 45 minutes. When taken after food, the absorption of ibuprofen was slower, and peak serum levels appeared between 1.5 and 3 hours.
The apparent volume of distribution is 0.14 l/kg. Ibuprofen and its metabolites readily cross the placental barrier in pregnant rats and rabbits. It is not known if ibuprofen enters the CSF or is excreted in breast milk.
Approximately 99% of ibuprofen is protein bound. The high protein binding should be kept in mind when prescribing ibuprofen together with other protein bound drugs that bind to the same site on human serum albumin.
Approximately 90% of ibuprofen is metabolised to two major metabolites (A and B). These are: Metabolite A () 2-4-(2-hydroxy-2-methylpropylphenyl) propionic acid and Metabolite B () 2-4-(2-carboxypropylphenyl) propionic acid. Both metabolites are dextrorotary and do not exhibit anti-inflammatory and analgesic activity.
Patients with rheumatoid arthritis and normal volunteers were given 800mg of ibuprofen as a single dose. After 14 to 24 hours the plasma levels of ibuprofen and metabolites were less than 0.25 mcg/ml.
The major route of excretion is via the kidney, with 95% of ibuprofen being excreted in the urine within 24 hours of a single dose of 500mg. Of this 35 % was excreted as metabolite A (15% free, 20% conjugated), 51% as metabolite B (42% free, 9% conjugated) and 9% as ibuprofen (1% free, 8% conjugated).
The plasma half life of ibuprofen is between 1.9 to 2.2 hours.
Not applicable.
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