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).
References
[1] https://www.medicines.org.uk
[2] http://www.rxlist.com
[3] http://www.healthline.com
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)
Uses
Risedronic Acid is a pyridinyl biphosphonate bone resorption inhibitor.
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.
