Raloxifene belongs to a pharmacological class known as selective estrogen receptor modulators (SERMs). It is a US FDA-approved second-generation selective estrogen receptor modulator. Raloxifene is a drug used to treat osteoporosis in postmenopausal women. It lowers the likelihood of invasive breast cancer in postmenopausal women. Raloxifene, like estrogen hormone, prevents bone loss in women following menopause. It increases bone density and mass by reducing bone resorption.
BRAND NAME:
Evista – It contains Raloxifene hydrochloride as a dug composition and is available in Evista Raloxifene hydrochloride 60mg oral tablets.
MECHANISM OF ACTION:
Raloxifene’s mechanism of action occurs through binding to estrogen receptors as it belongs to the selective estrogen receptor modulator class. This binding results in the activation of estrogen agonistic effect and blockade in tissues that express estrogen receptors. These are of two types, the alpha estrogen receptor(activating effect) and the beta estrogen receptor(inhibiting effect). These receptors modify the cellular and tissue responses to estrogens.
It has an estrogen antagonistic effect in the uterus and breast, in contrast with tamoxifen, which has an estrogen agonistic effect over the uterus. In postmenopausal osteoporosis, drastically the bone density decreases. Raloxifene can inhibit accelerated bone resorption both short and long-term, increasing bone mineral density and enhancing bone strength.
PHARMACOKINETICS:
Absorption: Raloxifene is readily absorbed from the gastrointestinal tract. Raloxifene has a bioavailability of approximately two percent and is absorbed at 60%.
Distribution: The apparent distribution of raloxifene protein-bound is more than 95%.
Metabolism: The metabolism of raloxifene occurs in the liver.
Excretion: More than 93% of the drug is excreted through feces and 0.2% through urine.
PHARMACODYNAMICS:
Raloxifene is a selective estrogen receptor modulator medication that has oestrogenic effects on bone and lipid metabolism while also exerting anti-estrogenic effects on the uterine endometrium and breast tissues. Raloxifene stimulates bone-depositing osteoblasts and inhibits bone-resorbing osteoclasts, resulting in increased bone density. Raloxifene has oestrogenic effects on bones, decreasing bone resorption and improving bone mineral density in postmenopausal women.
DOSAGE AND ADMINISTRATION:
Raloxifene hydrochloride is available in oral tablets with strength 60mg tablets.
- For the treatment of postmenopausal osteoporosis, the recommended dose is 60mg daily. And also suggested to take calcium and Vitamin D supplements daily.
- For prevention and risk reduction of invasive breast cancer in postmenopausal women the recommended dose is 60mg.
CONTRAINDICATIONS:
Raloxifene is contraindicated in patients having a history of malignancy, thrombophilia, antiphospholipid syndrome, venous thrombosis, pulmonary embolism, and renal vein thrombosis.
DRUG INTERACTIONS:
Raloxifene when interacted with some drugs causes serious adverse effects and also decreases the function of the drug. Below are the drugs that raloxifene should not take along with them, if it is required, then should discuss it with the doctor.
- Ospemifene
- Famciclovir
- Levothyroxine
- Warfarin
- Amoxicillin
- Ampicillin
- Digoxin
- Diazepam
- Diazoxide
- lidocaine
FOOD INTERACTIONS:
Avoid excessive consumption of alcohol.
ADVERSE EFFECTS:
- Arthralgia
- Hot flashes
- Muscle spams
- Sinusitis
- Venous thrombosis
- Bronchitis
- Vaginal bleeding
- Breast pain
- Pharyngitis
- Flu symptoms
TOXICITY:
Taking an overdose of raloxifene can cause toxic effects.
- Seizures
- Ataxia
- Flushing
- Tremor
- Diarrhea
- Vomitings
