What are Bisphosphonates?

ID-100201750Bisphosphonates (BPNs) are analogues of pyrophosphate. Bisphosphonates are produced from pyrophosphate by replacing the oxygen atom with carbon atom of the P-O-P skeleton of pyrophosphate.

Bisphosphonates are newer group of drugs used for various medical conditions where there is bone resorption, such as osteoporosis, Paget’s disease etc. These newer group of drugs have attracted considerable attention in recent years, because of their ability to prevent osteoporosis (where there is increased risk of fracture due to weak bones), a common problem of old age, especially among post-menopausal women.

Currently bisphosphonates are the most effective group of drugs for osteoporosis management and preventing fractures of old age due to weak bones, due to osteoporosis and other bone resorptive diseases.

What are different types of bisphosphonates?

Chronologically (according to date of development the drug), as well as according to potency bisphosphonates are grouped into three generations (1st, 2nd and 3rd generation).

First generation bisphosphonates (relative potency in bracket):

  • Etidronate                   (1)
  • Tiludronate                  (10)

Second generation bisphosphonates:

  • Pamidronate                (100)
  • Alendronate                (100-500)
  • Ibandronate                 (500-1000)

Third generation bisphosphonates:

  • Risedronate                 (1000)
  • Zoledronate                 (5000)

As one can see from the above info, the first generation bisphosphonates are least potent and no more in use currently. The second and third generation bisphosphonates are highly potent and they are commonly used currently.

The highly potent second and third generation bisphosphonates are developed by changing the side chain in the basic bisphosphonates molecular structure. Replacing the side chain with amino or nitrogenous ring makes bisphosphonates more potent with additional mechanism of action.

Read Mechanism of Action of Bisphosphonates here.

Read different therapeutic uses of bisphosphonates here.

 

“Image courtesy of stockimages / FreeDigitalPhotos.net”.

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