Aloxif

Aloxif Tablet

Aloxif is a selective estrogen receptor modulator (SERM). The biological actions of Aloxif are largely mediated through binding to estrogen receptor. This binding results in activation of certain estrogenic pathways and blockade of others. Aloxif reduces resorption of bone and decreases overall bone turnover. These effects on bone are manifested as reductions in the serum and urine levels of bone turnover markers. Clinical trials and data suggest that Aloxif lacks estrogen like effects on the uterus and breast tissues. Aloxif is rapidly absorbed after oral administration, metabolized in liver, and primarily excreted in faeces and rest in urine.

Uses

Aloxif is an estrogen agonist/antagonist used for:

  • Treatment and prevention of osteoporosis in postmenopausal women
  • Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis
  • Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer

Important Limitations: Aloxif is not used for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer

Aloxif is also used to associated treatment for these conditions: Invasive Breast Cancer, Osteoporosis, Osteoporosis caused by glucocorticoid

Aloxif

Trade Name Aloxif
Generic Raloxifene
Raloxifene Other Names Raloxifène, Raloxifene, Raloxifeno, Raloxifenum
Weight 60mg
Type Tablet
Formula C28H27NO4S
Weight Average: 473.583
Monoisotopic: 473.166079047
Protein binding

About 95% of raloxifene and its glucuronide metabolites are bound to plasma proteins. Although this is a relatively high protein binding profile, in vitro studies suggest that raloxifene and its metabolites do not significantly interact with binding of highly protein-bound drugs. FDA Label still advises patients to use raloxifene with caution co-administering with other highly protein-bound drugs.

Therapeutic Class Other preparations: Inhibiting bone resorption
Manufacturer Incepta Pharmaceuticals Ltd, Incepta Pharmaceuticals Limited
Available Country India, Bangladesh
Last Updated: June 23, 2021 at 9:10 am

Structure

Aloxif
Raloxifene Structure

Dosage

Aloxif dosage

One tablet (60 mg) once daily orally. It can be taken without regard to meal. High fat meal increases the absorption of Aloxif.

Side Effects

Aloxif is generally well tolerated. However, a few side effects like hot flushes, leg cramps, and influenza like symptoms, gastro-intestinal disturbances etc may be seen usually during first 6 months of treatment and were not different from placebo.

Precaution

Concurrent Estrogen Therapy: Concomitant use of Aloxif with systemic estrogens is not recommended.

Lipid Metabolism: Concurrent use of Aloxif and lipid-lowering agents has not been studied.

Interaction

Co-administered with cholestyramin, ampicillin and amoxicillin may reduce the absorption of Aloxif.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Excessive and chronic alcohol consumption may be associated with vitamin D deficiency.
  • Take with or without food. The absorption is unaffected by food.

Volume of Distribution

Following oral administration of single doses randing from 30 to 150 mg in postmenopausal women, the volume of distribution was about 2348 L/kg. Following oral administration of multiple doses, the value increased to 2853 L/kg. Aloxif is widely distributed in the tissues. It is not known whether raloxifene is excreted in human milk.

Half Life

The average plasma elimination half-life of raloxifene ranges from 27 to 32 hours. The prolonged half-life has been attributed to the drug's reversible systemic metabolism and significant enterohepatic cycling.

Clearance

Following intravenous administration, raloxifene was shown to be cleared at a rate approximating hepatic blood flow. The apparent oral clearance is reported to be 44.1 L/kgxhr. The clearance can range from 40 to 60L/kgxhr following chronic dosing. In healthy postmenopausal women receiving multiple oral dose, the mean clearance was 47.4 L/kgxhr. Apparent clearance can be reduced by 56% in patients with hepatic impairment.

Pregnancy & Breastfeeding use

Pregnancy Category X: Aloxif should not be used in women who are or may become pregnant.

Lactation: It is not known whether Aloxif is excreted in breast milk. Lactating mother should not use Raloxifne.

Contraindication

Hepatic & renal impairment. In active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis. Hypersensitivity to Aloxif or any other constituents of the tablet.

Special Warning

Severe Renal Impairment: Contraindicated.

Hepatic Impairment: Contraindicated.

Acute Overdose

Incidents of overdose in humans have not been reported.

Innovators Monograph

Aloxif contains Raloxifene see full prescribing information from innovator Monograph