115436-72-1

Description

Risedronate sodium is a nitrogen-containing bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism. Risedronate sodium is used for the treatment of postmenopausal osteoporosis to reduce the risk of vertebral fractures, treatment of established postmenopausal osteoporosis to reduce the risk of hip fractures, treatment of osteoporosis in men at high risk of fractures, and treatment of Paget’s disease. It is marketed as Actonel (tablet) and Atelvia (delayed-release tablet).

Chemical Properties

Fine White to Off-White Crystalline Powder

Originator

Procter Gamble (US)

Uses

antibacterial

Brand name

Actonel (Procter & Gamble).

Hazard

Human systemic effects.

Biological Activity

Orally active biphosphonate that inhibits farnesyl diphosphate (FPP) synthase. Exhibits antiproliferative and proapoptotic activity in numerous tumor cell lines and inhibits osteoclast-mediated bone reabsorption in vivo .

Biochem/physiol Actions

Risedronate sodium is a bisphosphonate bone resorption inhibitor. It has an affinity for hydroxyapatite crystals in bone and acts as an antiresorptive agent and is an inhibitor of farnesyl diphosphate (FPP) synthase, which results in downstream inhibition of osteoclast activity and reduced bone resorption and turnover. Risedronate sodium has been used to treat postmenopausal osteoporosis and Paget′s disease.

Clinical Use

Bisphosphonate: Treatment and prevention of osteoporosis (including corticosteroid induced) Paget’s disease

Drug interactions

Potentially hazardous interactions with other drugs Calcium-containing substances: avoid for 2 hours before and after administration.

Metabolism

The mean bioavailability of risedronate is 0.63% in the fasting state, and there is no evidence of systemic metabolism of risedronate sodium. About half of the absorbed portion is excreted in the urine within 24 hours; the remainder is sequestered to bone for a prolonged period. Unabsorbed drug is eliminated unchanged in the faeces.