Magazine article Drug Topics

Bone to Pick: Biphosphonate Structured for Better Tolerability and More

Magazine article Drug Topics

Bone to Pick: Biphosphonate Structured for Better Tolerability and More

Article excerpt

Capable only of feeling the vibrations of his magnificent music being played on a grand piano, Beethoven might have avoided his life of silence had bisphosphonates been introduced centuries earlier. It is often thought that this great composer suffered from deafness due to Paget's disease (PD)-a chronic bone disorder that, when severe, can cause enlargement of the skull and the aforementioned otic complication.

Bisphosphonates have been used to inhibit the abnormal bone resorption responsible for the excessive rate of bone remodeling and the subsequent formation of the characteristically enlarged and weakened Paget's bone structure. And lately, the emergence of such drugs from the pipeline has been gaining momentum. Just last year, Sanofi's Skelid (tiludronate) arrived on the market, and now Procter & Gamble's Actonel (risedronate) is making its entrance.

Risedronate is indicated to induce remission in patients with PD whose levels of serum alkaline phosphatase are at least two times the upper limit of normal, in patients who are symptomatic, or in those who are at high risk for future complications.

So how does this newest bisphosphonate differ from the rest? Risedronate's most obvious contrasting feature, which may conjure up bad memories of tortured medicinal chemistry classes, is its pyridinyl structure. In this particular configuration, the amino group is contained within the cyclic makeup of the compound and is therefore "shielded." So explained Robert Lindsay, M.D., professor of medicine at Columbia University, New York City, and chief of internal medicine at Helen Hayes Hospital in West Haverstraw, N.Y. And since it is believed that the amino group, openly present in other bisphosphonates, is responsible for irritation of the upper GI tract, shielding it from GI contact may certainly be advantageous.

Indeed, patients treated with a oncedaily dose of 30 mg for two months did not experience any severe upper GI adverse effects. However, Lindsay cautioned that long-term market experience with risedronate has yet to support these findings. As with any oral bisphosphonate, risedronate's labeling cautions against lying down immediately following ingestion of the drug to ensure that it is not dissolved in the esophagus. Most commonly reported adverse effects included arthralgia, diarrhea, and headache. …

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