How Do Bisphosphonate Derivatives Work?

Reviewed on 1/10/2022


Bisphosphonate derivatives are a class of drugs used to prevent the loss of bone density to treat postmenopausal osteoporosis (a condition in which bones become thin and weak and break easily), osteoporosis in men, glucocorticoid-induced osteoporosis (a type of corticosteroid medication that may cause osteoporosis), and Paget’s disease (a condition in which bones become soft and weak and may be deformed, painful, or easily broken) and to treat high levels of calcium in the blood that may be caused by certain types of cancer.

Bone tissue undergoes constant remodeling and is kept in balance (homeostasis) by osteoblasts (cells that form new bone) and osteoclasts (responsible for bone resorption) activity. Bisphosphonates inhibit the digestion of bone by encouraging osteoclasts to undergo apoptosis (cell death), thereby slowing down bone loss. Bisphosphonate derivatives help reduce the incidence of fractures (hip and vertebral and nonvertebral osteoporosis-related fractures) and are also used with cancer chemotherapy to treat bone problems that may occur with multiple myeloma (cancer that begins in the plasma cells) and other types of cancer (such as breast and lung) that have spread to the bones.

Bisphosphonate derivatives are administered orally as a tablet, a delayed-release tablet, an effervescent tablet (dissolves in water), and a solution (liquid) and intravenously (into a vein).

Bisphosphonate derivatives work in the following ways:

  • Work by slowing down the bone loss to help maintain strong bones and reduce the risk of bone fractures.
  • Increase bone density (thickness).
  • In addition, they help in lowering high blood calcium levels by reducing the amount of calcium released from bones into the blood.


Bisphosphonate derivatives are used in conditions such as:

  • Postmenopausal osteoporosis
  • Osteoporosis in men
  • Glucocorticoid-induced osteoporosis
  • Paget’s disease
  • Heterotopic ossification (growth of bone tissue in an area of the body other than the skeleton) in patients with:
    • Total hip replacement surgery (surgery to replace the hip joint with an artificial joint) 
    • Spinal cord injury
  • Hypercalcemia of malignancy (high blood calcium levels):
    • Multiple myeloma (cancer that forms in a type of white blood cells called plasma cells)
    • Bone metastases from solid tumors


Some of the common side effects include:

  • Diarrhea
  • Nausea
  • Vomiting
  • Myalgia (muscle pain)
  • Stomach upset
  • Weakness
  • Abdominal pain
  • Headache
  • Tiredness
  • Constipation
  • Loss of appetite
  • Heartburn
  • Mouth sores
  • Bloating
  • Flatulence (gas)
  • Leg cramps
  • Back pain
  • Arthralgia (pain in one or more joints)

Other rare side effects include:

  • Chest pain
  • Dizziness (feeling faint, weak, or unsteady)
  • Flu-like symptoms (such as fever, chills, muscle/joint aches)
  • Weight loss
  • Numbness or heavy feeling in the jaw
  • Difficulty breathing
  • Hypocalcemia (low blood calcium level)
  • Urinary tract infection
  • Hypertension (high blood pressure)
  • Asthenia (abnormal physical weakness or lack of energy)
  • Severe muscle spasms
  • Irregular heartbeat
  • Insomnia (trouble falling and/or staying asleep)
  • Swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.


Generic and brand names of bisphosphonate derivatives include:


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