Evista-generic

Neuroimage. 2005 Mar;25(1):63-75. Epub 2005 Jan 12.
Raloxifene exposure enhances brain activation during memory performance in healthy elderly males; its possible relevance to behavior.
Goekoop R, Duschek EJ, Knol DL, Barkhof F, Netelenbos C, Scheltens P, Rombouts SA.
Department of Neurology, VU University Medical Center, De Boelelaan 1117 1081 HV, Amsterdam, The Netherlands.

Raloxifene is a selective estrogen receptor modulator (SERM) that is prescribed in females only, but its use in male subjects is increasingly considered. With a growing number of patients having potential benefit from raloxifene, the need for an assessment of its effects on brain function is growing. Effects of estrogens on brain function are very subtle and difficult to detect by neuropsychological assessment. Functional imaging techniques, however, have been relatively successful in detecting such changes. This study used functional magnetic resonance imaging (fMRI) to examine effects of raloxifene treatment on memory function. Healthy elderly males (n = 28; mean age 63.6 years, SD 2.4) were scanned during performance on a face encoding paradigm. Scans were made at baseline and after 3 months of treatment with either raloxifene (n = 14) or placebo (n = 14). Treatment effects were analyzed using mixed-effects statistical analysis (FSL). Activation during task performance involved bilateral parietal and prefrontal areas, anterior cingulate gyrus, and inferior prefrontal, occipital, and mediotemporal areas bilaterally. When compared to placebo, raloxifene treatment significantly enhanced activation in these structures (Z > 3.1), except for mediotemporal areas. Task performance accuracy diminished in the placebo group (P = 0.02), but remained constant in the raloxifene group (P = 0.60). In conclusion, raloxifene treatment enhanced brain activation in areas spanning a number of different cognitive domains, suggesting an effect on cortical arousal. Such effects may translate into small effects on behavior, including effects on attention and working memory performance, executive functions, verbal skills, and episodic memory. Further neuropsychological assessment is necessary to test the validity of these predictions.

GENERIC NAME: raloxifene
BRAND NAME: Evista

DRUG CLASS AND MECHANISM: Estrogen is a hormone which among other actions, regulates the turnover (formation and destruction) of bone. Decreases in estrogen levels that are seen after menopause or after removal of the ovaries, lead to a loss of bone density and weakened bones, a condition called osteoporosis. Raloxifene decreases bone turnover and increases bone density although not to the same extent as estrogen itself. This makes bones stronger and prevents fractures in women with osteoporosis. Raloxifene is called a "selective estrogen receptor modulator" since it has effects like estrogen on some tissues but inhibits the effects of estrogen on other tissues. Raloxifene decreases low density lipoprotein (LDL or "bad") cholesterol in the blood; however, unlike estrogen, raloxifene does not increase high density lipoprotein (HDL or "good") cholesterol.

PREPARATIONS: Tablets, 60mg.

STORAGE: Tablets should be stored between 15° (59°F) and 30°C (86°F).

PRESCRIBED FOR: Raloxifene is prescribed for the prevention and treatment of osteoporosis in post-menopausal women.

DOSING: Raloxifene generally is prescribed once daily. It can be taken with or without meals. Persons with cirrhosis may need lower doses.

DRUG INTERACTIONS: Cholestyramine (Questran) reduces the absorption of raloxifene. Therefore, these two medications should be taken several hours apart. Raloxifene may slightly reduce the ability of blood to clot and thus increase the effects of medications that reduce clotting (blood thinners). Therefore, if raloxifene is given with blood thinners such as warfarin (Coumadin), the ability of blood to clot may need to be monitored more closely with frequent measurements of the prothrombin time of blood.

PREGNANCY: It is not known if raloxifene causes adverse fetal effects if taken during pregnancy although there is an increased risk of fetal abnormalities with the use of estrogens. Therefore, estrogens (and probably raloxifene) should not be taken during pregnancy.

NURSING MOTHERS: Raloxifene should not be used by nursing mothers.

SIDE EFFECTS: The most common side effects with raloxifene are hot flashes (seen in 1 of every four persons), sinusitis (1 in 10), weight gain (1 in 11), muscle pain (1 in 12), leg cramps (1 in 20), and ankle swelling (1 in 30).

Raloxifene increases the risk of blood clots, including deep vein thrombosis (DVT) and pulmonary embolism (blood clots in the lung). The greatest increase in risk occurs during the first 4 months of use. Patients taking raloxifene should avoid prolonged periods of restricted movement during travel when blood clots are more prone to occur.

Caution! Before starting to take this medicine, it is vital that you should consult your doctor! Do not use it on your own initiative, without medical advice.