IBUPROFEN
2-(p-isobutylphenyl) propionic acid
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) which is commonly used for relieving muscular and skeletal pain.
Chemical properties
Ibuprofen is a white powder belonging to the propionic acid derivatives, with a melting point of 74 - 77° C. It is only slightly soluble in water but readily soluble in organic solvents such as ethanol. It is a chiral compound; racemic Ibuprofen is usually used, although only one form is active medicinally.
Ibuprofen acts so as to inhibit the action of the enzyme cyclooxygenase, which catalyses the transformation of fatty acids to prostaglandins. Thus the synthesis of prostaglandin is inhibited and this is the cause for the analgesic and anti-inflammatory action of the drug. Because it is nonsteroidal, it is widely used as it does not upset the hormonal balance in the body.
Uses
Its anti-inflammatory, analgesic (pain relieving) and antipyretic (fever reducing) actions, are comparable to those of aspirin and it is commonly taken in tablet form for the relief of mild to moderate pain such as headache, toothache, and migraine as well as symptoms of fever. Ibuprofen is available for over-the-counter sale.
Many companies now market it under the trade names: Advil; Nuprin; Motrin-IB; and others.
Ibuprofen Tablets are very useful for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis, to reduce joint swelling and improves the action of joints. It is also commonly used to relieve postoperative pain and morning stiffness and has also been shown to slow down pulmonary decline in cystic fibrosis sufferers.
Adverse Effects
Ibuprofen is rapidly metabolized and eliminated in the urine. The excretion of ibuprofen is virtually complete 24 hours after the last dose. It has been associated with a significant reduction in gastrointestinal upsets when compared with aspirin. However, there is still a risk of gastric irritation at higher doses, and may cause bleeding and peptic ulcers in rare cases. Also, it may interfere with blood clotting and a side effect may be an increased risk of nosebleeds. It has been suggested that Ibuprofen may cause damage to the kidneys by decreasing the flow of blood to the kidneys and slowing down their ability to remove other drugs from the blood and also alter the way in which the kidneys regulate sodium and water balance.
There are contributing factors which increase the risk of renal toxicity (e.g. diabetes, dehydration). Ibuprofen is safe to be taken during pregnancy, but should be avoided during the last three months. It is also allowed in small doses for nursing mothers.
Children can also take Ibuprofen in small doses (5 mg/kg). However, the elderly should take the drug with care as there are positively increased risks of gastric problems and renal complications. Overall though, it would seem that the risks associated with Ibuprofen are significantly less than those with aspirin and so it is a very useful and widely used drug.