What is Raloxifene HCl 60mg?
Raloxifene is used by women to prevent and treat bone loss (osteoporosis) after menopause. It slows down bone loss and helps to keep bones strong, making them less likely to break. Raloxifene may also lower the chance of getting a certain type of breast cancer (invasive breast cancer) after menopause.
What is the prototype of raloxifene hydrochloride?
Raloxifene, the prototype of the selective estrogen receptor modulators, has been associated with an increased risk of venous thromboembolism.
What is Raloxifene HCl used for?
Raloxifene is used to help prevent and treat thinning of the bones (osteoporosis) only in postmenopausal women. It works like an estrogen to stop the bone loss that can develop in women after menopause, but it does not increase the bone density as much as daily 0.625 mg doses of conjugated estrogens.
What is the MOA of raloxifene?
The mechanism of action of raloxifene occurs through binding to estrogen receptors. This binding results in activation of estrogenic pathways (estrogen-agonistic effect) and blockade (estrogen-antagonistic effect) in tissues that express estrogen receptors.
How long is it safe to take raloxifene?
Abstract. Background: Due to the chronic nature of osteoporosis and the risk of invasive breast cancer, raloxifene 60 mg/day (raloxifene) is intended to be used for long-term treatment (treatment >3 years).
What is a serious adverse effect that may occur with use of raloxifene?
Seek immediate medical attention if any of these unlikely but serious side effects occur: leg swelling/pain, trouble breathing, chest pain, sudden vision changes, severe headache, weakness on one side of the body, confusion. A very serious allergic reaction to this drug is rare.
Is raloxifene an agonist or antagonist?
Raloxifene, a selective estrogen receptor (ER) modulator, is a mixed estrogen agonist/antagonist that has been shown to prevent osteoporosis and breast cancer in women.
Who should not use raloxifene?
38 Do not take EVISTA if you: 39 • have or have had blood clots in your legs, lungs, or eyes. Taking EVISTA may increas 40 the risk of getting blood clots. e 41 • are pregnant or could become pregnant. EVISTA could harm your unborn child.
What is the side effects of raloxifene?
Raloxifene may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
- hot flashes (more common in the first 6 months of raloxifene therapy)
- leg cramps.
- swelling of the hands, feet, ankles, or lower legs.
- flu-like syndrome.
- joint pain.
- sweating.
- difficulty falling asleep or staying asleep.
Where is raloxifene an agonist?
Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER). It has estrogenic effects in bone and antiestrogenic effects in the breasts and uterus. Raloxifene was approved for medical use in the United States in 1997.
Who should not take raloxifene?
Is raloxifene an immunosuppressant?
Decreased levels of mRNA for both tumor necrosis factor alpha and RANKL in spleen cells from raloxifene-treated arthritic mice indicated an immunosuppressive action of this SERM.
What is the structure of raloxifene hydrochloride?
Raloxifene hydrochloride is a hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride. It has a role as a bone density conservation agent, an estrogen antagonist and an estrogen receptor modulator. It contains a raloxifene (1+).
How is raloxifene metabolized in the body?
Raloxifene is metabolized in the liver and undergoes enterohepatic recycling. It is metabolized exclusively by glucuronidation and is not metabolized by the cytochrome P450 system. Less than 1% of radiolabeled material in plasma comprises unconjugated raloxifene. The metabolites of raloxifene include several glucuronides.
What is the volume of distribution of raloxifene in the US?
The volume of distribution of raloxifene with a single 30 to 150 mg oral dose is approximately 2348 L/kg, which corresponds to ~170,000 L for a 72 kg person. Both raloxifene and its glucuronide metabolites show high plasma protein binding (>95%), including to both albumin and α 1 acid glycoprotein, but not to sex hormone-binding globulin.
What is the history of raloxifene in the US?
History. Raloxifene was approved in the United States for the prevention of postmenopausal osteoporosis in 1997, the treatment of postmenopausal osteoporosis in 1999, and to prevent or reduce the risk of breast cancer in certain postmenopausal women in 2007. It received orphan designation in 2005.