Sodium risedronate

Description

Risedronate sodium was launched as Actonel in the US for treatment of Paget's disease. Risedronic acid is readily obtained by condensation of 2-(3- pyridyl)acetic acid with phosphorous acid in presence of phosphorus oxychloride. Risedronate sodium is an orally active bisphosphonate of third generation, showing more potent bone antiresorptive properties than most of prior bisphosphonates like etidronate which has been used for the same indication since 1978. The biological mechanism by which Risedronate, and generally bisphosphonates, act is not quite clear presently ; recent advances have suggested that aminobisphosphonates interfere with the HMG-CoA pathway and inhibit protein prenylation, causing apoptosis of osteoclasts and macrophages. These apoptotic effects are correlated to the anti-resorptive properties of this class of compounds. In a 2 month clinical trial involving patients with Paget's desease, 30 mg risedronate daily achieved an appreciable reduction of serum alkaline phosphatase levels, an indicator of bone stabilization, in 77% of patients, compared with 11% on etidronate at 400 mg daily for 6 months. Risedronate is also in development for the treatment and prevention of various bone diseases, particularly post-menopausal and corticosteroid-induced osteoporosis.

Chemical properties

Fine White to Off-White Crystalline Powder

Originator

Procter Gamble (US)

The Uses of Sodium risedronate

Risedronic Acid is a pyridinyl biphosphonate bone resorption inhibitor.

The Uses of Sodium risedronate

antibacterial

The Uses of Sodium risedronate

Osteoporosis

What are the applications of Application

Risedronate sodium is a pyridinyl biphosphonate

Definition

ChEBI: Risedronate sodium is a 1,1-bis(phosphonic acid).

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.

storage

Store at RT