Alendronate Sodium API

CAS No. 121268-17-5
Drug Description

A drug used to treat certain bone conditions, such as osteoporosis and Paget disease of the bone. It is also being studied in the treatment of hypercalcemia (high levels of calcium in the blood) and bone pain caused by cancer. Alendronate sodium slows the breakdown of bone and prevents the loss of calcium. It is a type of bisphosphonate.

Alendronate sodium is a bisphosphonate that acts as a specific inhibitor of osteoclast-mediated bone resorption. Bisphosphonates are synthetic analogs of pyrophosphate that bind to the hydroxyapatite found in bone.

Alendronate sodium is chemically described as (4-amino-1-hydroxybutylidene) bisphosphonic acid monosodium salt trihydrate.

The empirical formula of alendronate sodium is C4H12NNaO7P2•3H2O and its formula weight is 325.12. 

Alendronate sodium is a white, crystalline, nonhygroscopic powder. It is soluble in water, very slightly soluble in alcohol, and practically insoluble in chloroform.

Uses

Treatment of osteoporosis in postmenopausal women; prevention of osteoporosis in postmenopausal women at risk of developing osteoporosis; increase bone mass in men; treatment of glucocorticoid-induced osteoporosis in men and women; treatment of Paget disease of the bone.

Prescribed for the prevention and treatment of osteoporosis, the brittle bone disease, in postmenopausal women. It is also used to increase bone mass in men with osteoporosis, and is prescribed for both men and women who have developed a form of osteoporosis sometimes caused by steroid medications such as prednisone. This drug can also be used to relieve Paget’s disease of bone, a painful condition that weakens and deforms the bones.

Mechanism of Action

Animal studies have indicated the following mode of action. At the cellular level, alendronate shows preferential localization to sites of bone resorption, specifically under osteoclasts. The osteoclasts adhere normally to the bone surface but lack the ruffled border that is indicative of active resorption. Alendronate does not interfere with osteoclast recruitment or attachment, but it does inhibit osteoclast activity. Studies in mice on the localization of radioactive [3H]alendronate in bone showed about 10-fold higher uptake on osteoclast surfaces than on osteoblast surfaces. Bones examined 6 and 49 days after [3H]alendronate administration in rats and mice, respectively, showed that normal bone was formed on top of the alendronate, which was incorporated inside the matrix. While incorporated in bone matrix, alendronate is not pharmacologically active. Thus, alendronate must be continuously administered to suppress osteoclasts on newly formed resorption surfaces. Histomorphometry in baboons and rats showed that alendronate treatment reduces bone turnover (i.e., the number of sites at which bone is remodeled). In addition, bone formation exceeds bone resorption at these remodeling sites, leading to progressive gains in bone mass.

Alendronate Sodium API – Taj Ando Pharmaceuticals, South Africa | A drug used to treat certain bone conditions, such as osteoporosis and Paget disease of the bone. It is also being studied in the treatment of hypercalcemia (high levels of calcium in the blood) and bone pain caused by cancer. Alendronate sodium slows the breakdown of bone and prevents the loss of calcium. It is a type of bisphosphonate.