|
Product
Anti-asthmatic Products (Aerocort Inhaler)
|
Ralista(Raloxifene Hydrochloride)
|
|
| |
 |
Ralista
Raloxifene Hydrochloride
Composition
Each film-coated tablet contains
Raloxifene Hydrochloride ............. 60 mg
Description
• Raloxifene hydrochloride is a selective estrogen receptor modulator (SERM) that belongs to the benzothiophene class of compounds.
Pharmacology
Pharmacodynamics
◊ Decreases in estrogen levels after oophorectomy or menopause lead to increases in bone resorption and accelerated bone loss.
◊ Bone is initially lost rapidly because the compensatory increase in bone formation is inadequate to offset resorptive losses.
◊ In addition to loss of estrogen, this imbalance between resorption and formation may be due to age-related impairment of osteoblasts .
|
Pharmacokinetics
Absorption
◊ Raloxifene is absorbed rapidly after oral administration.
◊ Approximately 60% of an oral dose is absorbed .
◊ Administration of raloxifene HCl with a standardized, high-fat meal increases the absorption of raloxifene .
◊ Raloxifene can be administered without regard to meals.
Distribution
◊ Raloxifene is highly (95%) bound to plasma proteins.
◊ Raloxifene binds to both albumin and (alpha) 1-acid glycoprotein, but not to sex-steroid binding globulin.
Metabolism
◊ Raloxifene undergoes extensive first-pass metabolism to the glucuronide conjugates: raloxifene-4`-glucuronide, raloxifene-6-glucuronide, and raloxifene-6, 4`-diglucuronide.
Indications
◊ Raloxifene hydrochloride is indicated for the treatment and prevention of osteoporosis in postmenopausal women.
◊ For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate.
Dosage & administration
The recommended dosage is one 60-mg
Raloxifene hydrochloride tablet daily, which
may be administered any time of day without regard to meals.
Contraindications
◊ Raloxifene hydrochloride is contraindicated in lactating women or women who are or may become pregnant.
◊ It may cause fetal harm when administered to a pregnant woman.
◊ Raloxifene hydrochloride is also contraindicated in women with active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism, retinal vein thrombosis.
» » » » In women known to be hypersensitive to raloxifene or other constituents of the tablets.
Warnings and precautions
Drug Interactions
◊ Warfarin - If Raloxifene hydrochloride is given concurrently with warfarin or other coumarin derivatives.
◊ Prothrombin time should be monitored more closely when starting or stopping therapy with Raloxifene hydrochloride.
◊ In the osteoporosis treatment trial, there were no clinically relevant effects of warfarin co-administration on plasma concentrations of raloxifene .
Hepatic Impairment
◊ Raloxifene was studied, as a single dose, in Child-Pugh Class A patients with cirrhosis and total serum bilirubin ranging from 0.6 to 2.0 mg/dL.
◊ Plasma raloxifene concentrations were approximately 2.5 times higher than in controls and correlated with bilirubin concentrations.
◊ Safety and efficacy have not been evaluated further in patients with hepatic insufficiency.
Pregnancy
Pregnancy Category X — Raloxifene hydrochloride should not be used in women who are or may become pregnant.
Lactation
Raloxifene hydrochloride should not be used by lactating women. It is not known whether raloxifene is excreted in human milk.
Pediatric use
Raloxifene hydrochloride should not be used in pediatric patients.
Use in elderly
◊ Safety and efficacy in older and younger postmenopausal women in the osteoporosis treatment trial appears to be comparable.
Use in Men
◊ Safety and efficacy have not been evaluated in men.
Side effects
◊ The adverse events seen with raloxifene are:
Hot flashes, leg cramps, infection, headache, fever, nausea, diarrhoea, gastro intestinal disorders, weight gain, arthritis, sinusitis, rhinitis, rash.
◊ Very rarely Retinal vein occlusion.
Overdosage
◊ Incidents of overdose in humans have not been reported.
◊ There is no specific antidote for raloxifene.
Presentation
Raloxifene hydrochloride - Blister pack of 10 tablets
|
|
