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Australian Journal of Pharmacy : February 2005
fessional those days to get a drug moved from pre- scription-only medicine to pharmacy. I think ibuprofen was the second in the UK to do so. Q Initially, ibuprofen was indicated for rheumatoid arthritis. Did you think in 1961, when it was patented, it would then go on to be used so widely for other indications (headache, period pain, and so on)? When it was first patented in 1961, I had no idea even that it was going to be cho- sen as a product candidate. At that time we had a number of other compounds that were more potent and it was only two years later, having subjected a selection of these to extensive toxicological and bio- chemical testing, that we chose ibuprofen because we believed potentially it was the safest compound. Good tolerance, partic- ularly in the GI tract, was one of our orig- inal objectives. No, I could not foresee it would have other indications in 1961, but later in the sixties we did know it had analgesic and antipyretic actions and in the seventies set up a lot of trials in different types of pain. Q It’s been suggested that ibuprofen may also be indicated in the future for the treatment of patent ductus arteriosus (indomethacin has been used traditionally for this indication) and possibly a role in the management of multiple sclerosis and Alzheimer’s disease. Did you ever think that this would be something that it would be used for? I have read about the possible role for Alzheimer’s disease, but had not heard about the possible multiple sclerosis indi- cation. I would like to see more clinical tri- als in both these areas to prove the claims which have been made regarding the role for ibuprofen. Q What further research on ibuprofen would you like to see occur? I would like to see the research of Dr Bart Van Overmeire in Antwerp on the use of ibuprofen in patent ductus arteriosus brought to a successful conclusion and see ibuprofen replace indomethacin in this condition. I would also like to see more clinical trials in those non-pain areas where claims for ibuprofen have been made, in order to establish their validity or otherwise. Q Can you comment on the efficacy- to-safety profile of ibuprofen over the range of doses used from OTC to high dose for rheumatoid arthritis from your perspective? Ibuprofen has a wide therapeutic range from single doses of 200mg which some people find effective in minor pains up to 2,400mg per day (even more in USA) required in patients with severe rheuma- toid arthritis and similar conditions. There is no doubt that, from many trials and epidemiological studies, ibuprofen up to 1,600mg per day has a lower degree of side effects than any other NSAID. Above that dose side effects do increase until, at 2,400mg per day, they are similar to some other NSAIDs. Some say that doses of 1,200mg per day are analgesic and that anti-inflammatory action only kicks in at higher doses. My own view is that at 1,200mg per day ibuprofen is both analgesic and anti- inflammatory. Q What role have you played in the life of ibuprofen since your retirement in 1983? I left the Research Department in 1983 to give technical advice in anticipation of OTC ibuprofen, and I was very much involved in the launch of Nurofen in the UK in August 1983. I made sure that all retail pharmacists throughout the UK received the technical brochure that we had produced. This was followed by over 20 meetings throughout the UK. Follow- ing these events I visited health authori- ties in many countries to discuss their requirements for OTC ibuprofen. Boots were the only people who could do that at that time because we were the only peo- ple who had all the technical information that was required for registration. Q Do you feel that ibuprofen is safe and efficacious such that it could be self selected without the advice of a pharmacist? I was trained as a pharmacist before I became a pharmacologist (indeed I spent 3.5 years as a pharmacy apprentice) so I am very aware of and sympathetic to the pharmacy-only argument. But as long as other analgesics are available in grocery outlets I don’t think a customer should be at a disadvantage in not being able to buy ibuprofen. However, I believe pack size should be very strictly limited and anything larger must be available only through pharmacies. Q Some of my [Ric Day’s] previous research has involved work with an Australian group on the disposition of the enantiomers of ibuprofen. In your mind, what is the value of administering the S-enantiomer? We did consider the possibility of devel- oping the S-enantiomer but were told at that time that it would have to be treated as a completely new drug. Since we had so much clinical experience with ibupro- fen that supported its efficacy and safety, there was little advantage in changing, especially since it was more expensive to produce and in any event would not be free of side effects. Q [To end, a not-so-serious question] Today there are films about World War II code breakers and mathematic geniuses. Has anyone approached you to do a film version about the discovery of ibuprofen? There have been no approaches from Hollywood, if that’s what you mean and I hope they don’t as I wouldn’t be interested. However, I was happy to take part in a technical/scientific film on the discovery of ibuprofen produced by the BBC for the Open University (OU). It appeared annually for several years on BBC2 as part of the OU’s chemistry courses. ¦ THE AUSTRALIAN JOURNAL OF PHARMACY VOL 86 FEBRUARY 2005 ? 85