More information can be found at
http://www.ibuprofen-foundation.com

Introduction

Ibuprofen, is a long-established, non-prescription, peripherally-acting antipyretic analgesic anti inflammatory drug. As such it is a common ingredient in over-the-counter analgesics and cold and flu remedies.

Structure

Discovery

The patent to the propionic acid derivatives of which ibuprofen is a member was filed at the UK Patents Office in 1962 following many years of research by a team at the Boots Company, lead by Dr Stewart Adams. In 1956, when this research started, only two pain relieving anti-inflammatory drugs were available, aspirin and phenylbutazone. The objective of the research was to develop a drug which had a superior profile both in terms of potency and toxicity to these two drugs. The discovery of ibuprofen achieved both of these objectives.

Synthesis

A number of routes are available for the manufacture of ibuprofen and for many years the Boots Company used the following method.

More recently, manufacture of the methyl ester of ibuprofen has been via the catalyzed carboxylation of the appropriate olefin as described below:

Chemical characteristics of ibuprofen

Formula C₁₃ H18 O₂

Molecular weight 206.28

Melting point 75-77ºC

almost insoluble in water

Mode of action

Ibuprofen, like all non-steroidal anti-inflammatory agents acts via the inhibition of the enzyme cyclooxygenase which in turn reduces the level of prostaglandins in the body.
Prostaglandins are involved in pain sensation, inflammation and fever and ibuprofen is effective in reducing all three of these effects. Unlike aspirin, ibuprofen has a relatively weak antithrombotic effect, being a weak inhibitor of platelet aggregation. Good evidence exists to suggest that it is safer on the stomach than aspirin, having a safety profile similar to that of paracetamol. Unlike aspirin, it has never been implicated in Reye's Syndrome. It is also more potent than aspirin or paracetamol, 400mg being roughly equivalent in effect to 1000mg of aspirin or paracetamol.

Use of ibuprofen

While uses may vary in different countries, ibuprofen is generally indicated for the relief of mild to moderate pain, for the reduction in fever and for reduction of inflammation. A range of specific indications exist, in the UK for instance it is licensed for use in headaches, colds and flu, rheumatic pain, muscular pain, backache, feverishness, migraine, period pain, dental pain and neuralgia. It seems to be particularly appropriate for period pain, a number of studies have suggested its superiority over the other common pain killing ingredients.

General Contraindications

Warnings and contraindications on ibuprofen may differ in different countries. Always read the label and leaflet appropriate to the product in your country

The product should not be taken if the patient has previously had an allergic reaction to aspirin or has had urticaria, rhinitis or asthma associated with NSAIDs or aspirin: or if the patient is allergic to ibuprofen or has a history of active peptic ulcer. People should contact their doctor before taking ibuprofen if they suffer from asthma, heart, liver or kidney disease, if they are pregnant or breast feeding, if they are elderly or if they have had stomach pains or heartburn after taking aspirin or if they have a bleeding disorder.

Drug interactions

Warnings of drug interactions warnings on ibuprofen may differ in different countries. Always read the label and leaflet appropriate to the product in your country.

Children

Warnings on ibuprofen usage in children may differ in different countries. Always read the label and leaflet appropriate to the product in your country.

Ibuprofen is not associated with Reye's Syndrome and so can be taken by children; special liquid children's formulas are available in some countries.

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Further information is available from the following website http://www.ibuprofen-foundation.com