Bisphosphonates: Uses, common brands, and safety info

Bisphosphonates are a class of medications that slow down and prevent bone loss. Used to increase bone strength and reduce the risk of bone fractures, bisphosphonate medications help treat osteoporosis, Paget’s disease, and other conditions that may lead to a loss of bone mineral density. 

Continue reading to learn more about bisphosphonates, their uses, and their side effects. 

Other bisphosphonates

• Zometa (zoledronic acid)

• Aclasta (zoledronic acid)

• Actonel with Calcium (risedronate/calcium carbonate)

• Skelid (tiludronate)

• Didronel (etidronate)

• Aredia (pamidronate)

What are bisphosphonates?

Bisphosphonates are medications that strengthen bones by slowing or preventing bone turnover and bone loss. Bone loss is a normal part of the aging process, but women can experience an increased risk of bone disease after menopause. Estrogen levels decrease in postmenopausal women, which can lead to decreased bone mass. A loss of bone mass can lead to an increased risk of hip fractures and vertebral fractures. 

Bisphosphonate treatment reduces the risk of fractures in people with conditions that cause bone loss, such as osteoporosis. Bisphosphonates are recommended for the management of osteoporosis because they help slow the bone remodeling process and prevent bones from losing calcium and other minerals. 

How do bisphosphonates work?

Your bones are constantly rebuilding themselves in a process known as bone remodeling. During this process of bone turnover, old bone tissue is broken down and replaced with new bone tissue. As old bone tissue is broken down, calcium is released from the bone into the bloodstream. 

Osteoclasts are the bone cells that are responsible for removing old bone tissue and osteoblasts are the bone cells that help form the new bone tissue. In conditions like osteoporosis, osteoclasts may be more active causing bone tissue to be broken down faster than it can be rebuilt. Bisphosphonates slow down the process of bone remodeling and help maintain the strength of bones. 

Like other antiresorptive agents, bisphosphonates inhibit the action of the osteoclasts and decrease bone resorption. As bisphosphonates bind to sites on the bone’s surface, osteoclasts cannot carry out their function of removing old bone cells. This mechanism of action helps slow the thinning of bones and prevents bone fractures. 

What are bisphosphonates used for?

Bisphosphonates are primarily used for the treatment of osteoporosis but may also be used for the following conditions:

• Osteopenia

• Paget’s disease

• Breast cancer with bone metastases

• Heterotopic ossification from spinal cord injury or hip replacement surgery

• Hypercalcemia

• Osteolytic bone lesions

• Osteogenesis imperfecta

Bone density can be measured in a test known as a DEXA scan. This scan is a type of x-ray that assesses bone loss by measuring bone mineral density. A DEXA scan measures how many grams of calcium and other bone minerals a segment of bone contains. The scan typically measures bone mineral density in the spine, hip, or forearm. The higher the mineral content, the denser your bones are. With a high bone mineral density, the bones are less likely to break. If you have a low bone mineral density for your age, you may be a candidate for treatment with a bisphosphonate. 

Who can take bisphosphonates?

Adults

Adults can take various forms of bisphosphonates. Most bisphosphonates are available in tablet form. For example, Fosamax is supplied as an effervescent tablet. Some formulations of bisphosphonates are given once weekly while others may be taken daily. Reclast is only available as an injection, which is administered yearly. Vitamin D and calcium supplementation are usually recommended in those treated with bisphosphonates for bone loss. 

Bisphosphonates are often taken first thing in the morning on an empty stomach. Tablets should be swallowed whole, and the medication should be taken with six to eight ounces of water. You should remain sitting upright for at least 30 minutes after taking a bisphosphonate or until you have consumed food. 

Bisphosphonates are generally taken for a period of three to five years of treatment. Bone density tests can determine if bisphosphonates are needed for bone loss and if they have effectively prevented further loss. 

Children

Children with osteogenesis imperfecta or other diseases that lead to bone loss may be prescribed bisphosphonates. However, bisphosphonates have not been FDA-approved for use in children. Bisphosphonates like Fosamax, Reclast, or Aredia may sometimes be prescribed off-label in children. The dosage may be based on the child’s weight. 

Bisphosphonates should be taken first thing in the morning on an empty stomach. Tablets should be swallowed whole, and medication should be taken with six to eight ounces of water. Children should remain sitting upright for at least 30 minutes after taking a bisphosphonate or until eating. Liquid bisphosphonates should be followed with at least two ounces of water.  

Seniors

Seniors can take bisphosphonates without any dose adjustments required. 

Are bisphosphonates safe?

In general, bisphosphonates are deemed safe by the FDA and have few side effects when taken as prescribed. However, there are a few groups of people that should not take bisphosphonates. Individuals with altered kidney function should not take bisphosphonates, including those on peritoneal dialysis or hemodialysis. 

Bisphosphonate recalls

There are no current bisphosphonate recalls as of May 2021.

Bisphosphonate restrictions

Individuals prescribed bisphosphonates must tolerate sitting upright or standing for at least 30 minutes after taking the medication. If you have active stomach problems, esophageal problems, or esophagitis, bisphosphonates may increase the risk of worsened symptoms from these conditions. For those that cannot tolerate oral bisphosphonates, intravenous bisphosphonates, such as Reclast, may be an option.

Can you take bisphosphonates while pregnant or breastfeeding?

Bisphosphonates may cross the placenta during pregnancy and lead to adverse effects on both the unborn baby and mother. Because of this, the risks and benefits of taking a bisphosphonate during pregnancy should be evaluated by a healthcare provider. 

Bisphosphonates may cross into breast milk in small amounts. Although bisphosphonates are likely to be poorly absorbed by a nursing infant, a healthcare provider should be consulted before taking a bisphosphonate while breastfeeding. 

Are bisphosphonates controlled substances?

No, bisphosphonates are not controlled substances. 

Common bisphosphonate side effects

The most common side effects of bisphosphonates include:

• Muscle pain

• Bone pain

• Joint pain

• Nausea

• Headache

• Flatulence

• Heartburn

• Flu-like symptoms

• Irritation of the esophagus

More severe but rare side effects of bisphosphonates include:

• Allergic reactions

• Severe bone pain

• Chest pain

• Muscle spasms

• Muscle twitching 

• Tingling or numbness around the mouth, fingers, or toes

• Pain or difficulty with swallowing

• Unusual pain in the groin, thigh, or hip

• Pain, swelling, numbness, or a heavy feeling in the jaw

• Loose teeth or tooth problems

• Blistering, peeling, red skin rash

Bisphosphonates have two side effects that, while rare, are quite serious. The first is a risk for a rare type of fracture in the femur of the thigh bone. This type of femoral fracture has been reported with bisphosphonate use. 

Another possible serious side effect of using bisphosphonates is osteonecrosis of the jaw (ONJ). It can develop spontaneously, especially after a dental extraction or other dental procedure. Injury to the bone during dental surgery could lead to loss of bone in the jaw, which can lead to symptoms of pain and swelling in the jaw. The risk of developing osteonecrosis of the jaw may be higher with high doses of bisphosphonates or infusions of bisphosphonates, such as Reclast, rather than other oral bisphosphonates. Other risk factors for developing ONJ include older age, female gender, chemotherapy, and steroid treatment.  

This list of side effects is not comprehensive. Speaking with a healthcare professional is the best way to get a complete list of side effects and determine whether bisphosphonate use is suitable for you.

Tell your doctor if you have a history of any of the following before taking a bisphosphonate:

• Any medication allergies

• Problems in the esophagus

• Low calcium levels (hypocalcemia)

• Kidney disease or other kidney problems

• Trouble swallowing food or medications

• Inability to stand or sit upright for 30 minutes

• Pregnancy or plans to become pregnant

• Use of parathyroid hormone (Forteo)

• Vitamin D deficiency

• Stomach ulcers

You should also tell your doctor about any and all medications you may be taking, including over-the-counter medications, prescription medications, and herbal supplements. Some medications may interact with bisphosphonates. For example, supplements that contain aluminum or magnesium can alter the absorption of bisphosphonates and should not be taken within 30 minutes after taking a bisphosphonate. 

How much do bisphosphonates cost?

Bisphosphonates are generally affordable medications that are available in brand-name and generic formulas. Almost all Medicare and insurance plans will cover bisphosphonates. Costs will vary depending on your insurance plan. Without insurance, the price can vary widely depending on the medication and quantity of tablets prescribed. However, using a prescription discount card from SingleCare may help reduce the cost of bisphosphonates.