guardianactual
MuscleChemistry Registered Member
The chemical designation is methanone, [6-hydroxy-2-(4-hydr oxyphenyl)benzoth ien-3-yl]-[4-[2-(1-p iperidinyl)ethoxy]ph enyl]-, hydrochloride. Raloxifene hydrochloride (HCl) has the empirical formula C28H27NO4S•HCl, which corresponds to a molecular weight of 510.05. Raloxifene HCl is an off-white to pale-yellow solid that is very slightly soluble in water.
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</br> SERMS are "designer" estrogen-related medications that activate the estrogen receptors, but have different effects on different tissues. There are two kinds of estrogen receptors, and after binding to receptors, the drug-receptor complex can have various conformations. Some of these will act like estrogen, others will inhibit the actions of estrogen.
</br>
</br> Advantages of Raloxifene: Many screening studies of related compounds have been done to search for those which act like estrogen in the desireable ways (stablize bone mass, improve lipid profile) but do not act like estrogen in undesireable ways (cause breast cancer, stimulate the endometrium). The effects on the cardiovascular system are still uncertain: when Ralox was first developed it was felt that estrogen had a beneficial action on the heart, now this is doubted and debated. Effects on bone physiology # Decreased bone formation and resorption # No significant change in bone volume # Slight increase in mineralization density
</br>
</br> Another effect of Ralox is that users had fewer asthma attacks and less severe asthma symptoms, strongly suggesting that perhaps estrogen affects airway smooth muscle function by preventing the hyperresponsiveness characteristic of asthma and other chronic lung diseases. Toxicology report that estrogen, as well as selective estrogen receptor modifiers (SERMs), completely abolished abnormal tracheal constriction in a carbachol test.Carbachol is often used to stimulate, or mimic, contractions of airway and other muscles.
</br>
</br> Estrogen has a wide range of actions in the nervous system, including neuroprotection and potentiation of nerve regeneration (Toran-Allerand, 1999; Tanzer et al., 1999; McEwen et al., 2001; Islamov et al., 2002). In spite of the beneficial actions of estrogen on the nervous system, the opportunities for its wide therapeutic application are severely limited because of its adverse side effects in reproductive organs. Therefore, a search for pharmacological substances with selective estrogenic action on the nervous system is of great practical significance.
</br>
</br> Other positive effects: The HDL cholesterol level is considered a strong inverse predictor of cardiovascular disease .Therefore, the absence of an increase in serum HDL cholesterol levels raises concern that raloxifene may not be as effective as estrogen replacement in preventing cardiovascular disease. Although the findings of animal studies are difficult to generalize to humans, recent animal data have also raised concerns that raloxifene may not prevent the progression of coronary artery disease. Because no long-term trials have been conducted, it is impossible to determine whether the small lipid effects produced by raloxifene correlate with a smaller degree of cardioprotective activity.
</br>
</br> Raloxifene vs Tamox From the above we can infer that Ralox maybe a better choice over Tamox as it lends the following positive effects on use. a)Increasing bone density b)Prevention of asthma c)Nerve regeneration and neuroprotection d)No changes in serum concentrations of high-density lipoprotein (HDL) cholesterol and triglycerides, while reducing LDL levels.
</br>
</br> I have requested Eli&Lilly Co makers of Evista if they have reports/studies of heptatoxicity of Raloxifene to compare the effects of Ralox vs Nolva on the Liver. While taking orals have a significant effect on the liver, the least heptatoxic SERM would be the better option during a PCT.
</br>
</br> Gyno formula: Raloxifene: 60mg daily. You should see improvement in approx. 4 to 6 weeks. If not increase by 20 mg for every 3 weeks, never to exceed 100mg daily. Tamoxifen: 40mg daily for once week. Then 20mg daily until gynecomastia is reversed. Both protocols above will take time. This is not a 2 week process. Reversal will require patience. But it most certainly is effective, side-effect-free and cost incredibly effective when compared to surgery.
</br> There has been a tweek to the above protocol... See below. This is the new ADVISED protocol: 60mg daily for 10 days ONLY. Then 30mg daily until gynecomastia is reversed. WHY THE CHANGE: Doses of 60 to 100mg of Raloxifene can result in bone demineralization. effected bone morphogenetic proteins include, but not limited to FGF, PGE2, M-CSF and PDGF. Recommended Supplementation during Treatment:
</br> Vitamin D and Calcium are recommended during Raloxifene treatment. 5000 IU vitamin D daily, and 500 mg of calcium daily. This was just brought to my attention by an MD specialized in this field. I apologize for distributing the old protocol, however, this goes to show that you can research something to death and still not learn everything. raloxifene remains the superior compound for gynecomastia reversal today.
</br>
</br> MEDICAL USE: Abstract OBJECTIVES: To assess the efficacy of the anti-estrogens tamoxifen and raloxifen in the medical management of persistent pubertal gynecomastia. STUDY DESIGN: Retrospective chart review of 38 consecutive patients with persistent pubertal gynecomastia who presented to a pediatric endocrinology clinic. Patients received reassurance alone or a 3- to 9-month course of an estrogen receptor modifier (tamoxifen or raloxifene).
</br>
</br> RESULTS: Mean (SD) age of treated subjects was 14.6 (1.5) years with gynecomastia duration of 28.3 (16.4) months. Mean reduction in breast nodule diameter was 2.1 cm (95% CI 1.7, 2.7, P <.0001) after treatment with tamoxifen and 2.5 cm (95% CI 1.7, 3.3, P <.0001) with raloxifene. Some improvement was seen in 86% of patients receiving tamoxifen and in 91% receiving raloxifene, but a greater proportion had a significant decrease (>50%) with raloxifene (86%) than tamoxifen (41%). No side effects were seen in any patients.
</br>
</br> CONCLUSION: Inhibition of estrogen receptor action in the breast appears to be safe and effective in reducing persistent pubertal gynecomastia, with a better response to raloxifene than to tamoxifen. Further study is required to determine that this is truly a treatment effect.
</br>
</br> SERMS are "designer" estrogen-related medications that activate the estrogen receptors, but have different effects on different tissues. There are two kinds of estrogen receptors, and after binding to receptors, the drug-receptor complex can have various conformations. Some of these will act like estrogen, others will inhibit the actions of estrogen.
</br>
</br> Advantages of Raloxifene: Many screening studies of related compounds have been done to search for those which act like estrogen in the desireable ways (stablize bone mass, improve lipid profile) but do not act like estrogen in undesireable ways (cause breast cancer, stimulate the endometrium). The effects on the cardiovascular system are still uncertain: when Ralox was first developed it was felt that estrogen had a beneficial action on the heart, now this is doubted and debated. Effects on bone physiology # Decreased bone formation and resorption # No significant change in bone volume # Slight increase in mineralization density
</br>
</br> Another effect of Ralox is that users had fewer asthma attacks and less severe asthma symptoms, strongly suggesting that perhaps estrogen affects airway smooth muscle function by preventing the hyperresponsiveness characteristic of asthma and other chronic lung diseases. Toxicology report that estrogen, as well as selective estrogen receptor modifiers (SERMs), completely abolished abnormal tracheal constriction in a carbachol test.Carbachol is often used to stimulate, or mimic, contractions of airway and other muscles.
</br>
</br> Estrogen has a wide range of actions in the nervous system, including neuroprotection and potentiation of nerve regeneration (Toran-Allerand, 1999; Tanzer et al., 1999; McEwen et al., 2001; Islamov et al., 2002). In spite of the beneficial actions of estrogen on the nervous system, the opportunities for its wide therapeutic application are severely limited because of its adverse side effects in reproductive organs. Therefore, a search for pharmacological substances with selective estrogenic action on the nervous system is of great practical significance.
</br>
</br> Other positive effects: The HDL cholesterol level is considered a strong inverse predictor of cardiovascular disease .Therefore, the absence of an increase in serum HDL cholesterol levels raises concern that raloxifene may not be as effective as estrogen replacement in preventing cardiovascular disease. Although the findings of animal studies are difficult to generalize to humans, recent animal data have also raised concerns that raloxifene may not prevent the progression of coronary artery disease. Because no long-term trials have been conducted, it is impossible to determine whether the small lipid effects produced by raloxifene correlate with a smaller degree of cardioprotective activity.
</br>
</br> Raloxifene vs Tamox From the above we can infer that Ralox maybe a better choice over Tamox as it lends the following positive effects on use. a)Increasing bone density b)Prevention of asthma c)Nerve regeneration and neuroprotection d)No changes in serum concentrations of high-density lipoprotein (HDL) cholesterol and triglycerides, while reducing LDL levels.
</br>
</br> I have requested Eli&Lilly Co makers of Evista if they have reports/studies of heptatoxicity of Raloxifene to compare the effects of Ralox vs Nolva on the Liver. While taking orals have a significant effect on the liver, the least heptatoxic SERM would be the better option during a PCT.
</br>
</br> Gyno formula: Raloxifene: 60mg daily. You should see improvement in approx. 4 to 6 weeks. If not increase by 20 mg for every 3 weeks, never to exceed 100mg daily. Tamoxifen: 40mg daily for once week. Then 20mg daily until gynecomastia is reversed. Both protocols above will take time. This is not a 2 week process. Reversal will require patience. But it most certainly is effective, side-effect-free and cost incredibly effective when compared to surgery.
</br> There has been a tweek to the above protocol... See below. This is the new ADVISED protocol: 60mg daily for 10 days ONLY. Then 30mg daily until gynecomastia is reversed. WHY THE CHANGE: Doses of 60 to 100mg of Raloxifene can result in bone demineralization. effected bone morphogenetic proteins include, but not limited to FGF, PGE2, M-CSF and PDGF. Recommended Supplementation during Treatment:
</br> Vitamin D and Calcium are recommended during Raloxifene treatment. 5000 IU vitamin D daily, and 500 mg of calcium daily. This was just brought to my attention by an MD specialized in this field. I apologize for distributing the old protocol, however, this goes to show that you can research something to death and still not learn everything. raloxifene remains the superior compound for gynecomastia reversal today.
</br>
</br> MEDICAL USE: Abstract OBJECTIVES: To assess the efficacy of the anti-estrogens tamoxifen and raloxifen in the medical management of persistent pubertal gynecomastia. STUDY DESIGN: Retrospective chart review of 38 consecutive patients with persistent pubertal gynecomastia who presented to a pediatric endocrinology clinic. Patients received reassurance alone or a 3- to 9-month course of an estrogen receptor modifier (tamoxifen or raloxifene).
</br>
</br> RESULTS: Mean (SD) age of treated subjects was 14.6 (1.5) years with gynecomastia duration of 28.3 (16.4) months. Mean reduction in breast nodule diameter was 2.1 cm (95% CI 1.7, 2.7, P <.0001) after treatment with tamoxifen and 2.5 cm (95% CI 1.7, 3.3, P <.0001) with raloxifene. Some improvement was seen in 86% of patients receiving tamoxifen and in 91% receiving raloxifene, but a greater proportion had a significant decrease (>50%) with raloxifene (86%) than tamoxifen (41%). No side effects were seen in any patients.
</br>
</br> CONCLUSION: Inhibition of estrogen receptor action in the breast appears to be safe and effective in reducing persistent pubertal gynecomastia, with a better response to raloxifene than to tamoxifen. Further study is required to determine that this is truly a treatment effect.
