Pharmacology of New Products
1. "Designer Estrogens" are also known as SERMS. This is an acronym for Selective Estrogen Receptor Modulators. These modified estrogens bind the estrogen receptor at different sites of the body, but they may block the receptor or activate it. The current ones include raloxifene, idoxifene, levormeloxifene, and droloxifene. They all block endomtrial stimulation so mentrual bleeding doe not occur. No pregestin is needed. They also shrink fibroids and reduce fibrocystic breast disease. All SERMS block breast stimulation and block breast cancer cell lines. SERMS lower cholesterol and build bone to varying degrees depending on the receptor binding, but none so far do these actions better than estradiol. None of the SERMS so far control hot flashes as well as estradiol. Raloxifene and estradiol both increase thrombophlebitis three-fold and should not be used in non-ambulatory patients or patients at high risk for phlebitis. There are no known adverse interactions with other drugs.
2. Cox-2 inhibitor are selective drugs that block arachidonic acid only at the joint where the Cox-2 enzyme is found. Since Cox-1 is the enzyme used for the stomach, kidney, liver metabolism and platelet, these new arthritis drugs have no effect on these organs. The new Cox-2 inhibitors are safe with coumadin. There are no known adverse interactions with other drugs.
3. Several new bisphosphonates will be coming on the market. Etidronate (Didronel), pamidronate (Aredia; available IV only), alendronate (Fosamax), tiludronate (Skelid), and risedronate (Actonel) are now available.
4. Biological Proteins for Rheunatoid Arthritis are now
available. These are not medications but are human gene product proteins generated
with new pharmcologic technology. There is no viral vector and no virus involved in
the creation of these proteins. Because these are human proteins (like insilin),
there are no side effects for internal organs. However, these proteins are part of
the immune system and there is theoretical concern about interfering with immune functions
when fighting infection. I have prescribed oral antibiotics to be used in the event
of an infection causing fever and have asked the patient to call me. In the event of
a serious infection (such as pneumonia) I am recommending the biologic agent be held until
the infection is cleared. These proteins do not interfere with any medications and
there is no report of any allergic reaction to the human proteins. The proteins
being used are:
Tumor Necrosis Factor (antibody or receptors) = Enbrel (Wyeth-Ayerst).
Similar products are being made by Amgen and Knoll.
Interleukin 10 = Tenovil (Schering-Plough)
Interleukin1 Receptor = Anakinra (Amgen). Similar products are being made by Hoechst Marion Roussel.