Osteoporosis Medications: Before the Bone Breaks
Osteoporosis is a disease that causes bones to lose mass, to deteriorate, and to become brittle. This means that bones also lose their strength, which increases the chance of breaks or fractures. Fractures caused by osteoporosis can be debilitating and reduce quality of life. They can result in pain, emotional distress, and loss of independence. For more information about osteoporosis, please see the Osteoporosis Overview.
While men can develop osteoporosis, 80 percent of osteoporosis patients in the United States are women. According to the National Institutes of Health, 10 million people already have the disease (2 million are men), and 34 million more have low bone mass, which is a major risk factor for osteoporosis. Although osteoporosis can strike at any age, it most often appears after menopause when women’s hormone levels decline. At least 1.5 million fractures occur each year because of osteoporosis, costing more than $14 billion. The most typical sites of fractures related to osteoporosis are the hip, spine, wrist, and ribs, although the disease can affect any bone in the body.
Treatment Options
A complete osteoporosis treatment program includes focusing on proper nutrition, exercise, and safety issues to prevent falls that may result in fractures. In addition, your doctor may prescribe medications to slow or stop bone loss, increase bone strength, and reduce fracture risk.
Osteoporosis medications affect the bone remodeling cycle. Bone remodeling is made up of two stages: bone resorption (bone loss) and bone formation. These stages usually occur together to maintain a healthy bone. In osteoporosis, the cycle becomes imbalanced and bone loss occurs more rapidly than bone formation, resulting in a weakened bone.
Anti-Resorptive Medications
Bisphosphonates are nonhormonal agents that bind to active sites of bone remodeling and inhibit the action of osteoclasts, thereby preventing bone resorption. Bisphosphonates reduce bone loss, increase bone density, and prevent fractures of the hip and spine.
Oral bisphosphonates, alendronate (Fosamax®), ibandronate (Boniva®), and risedronate (Actonel®), are poorly absorbed and can cause indigestion, nausea, and esophageal irritation. For this reason, they must be taken on an empty stomach first thing in the morning, with a full glass of water (6-8 ounces), and the patient must remain upright (standing or sitting) for 30 to 60 minutes after taking a dose.
Because this procedure can be inconvenient, alendronate and risidronate are available in a once-weekly tablet and ibandronate is available in a once-monthly tablet. Other less common side effects of the oral bisphosphonates include bone, joint, and muscle pain. Bisphosphonates can be safely taken for 5-10 years.
Recently, Warner Chilcott has released a delayed-release Risedronate tablet that can be taken immediately after eating, eliminating the 30 to 60 minute delay mentioned above.
Intravenous formulations of the bisphosphonates are available for patients who cannot remain upright for the required length of time and for those who cannot tolerate the GI side effects of the oral agents. Ibandronate IV is given every three months and zolendronic acid is available in a once-yearly formulation. Side effects that can occur after IV bisphosphonates include flu-like symptoms, fever, pain in muscles and joints, and headache. In 2008, generic alendronate became available for about one-tenth of the cost of the brand name bisphosphonates.
Drug |
Brand Name / Dose |
Side Effects |
Alendronate |
Fosamax (generic available) – Prevention: 35mg/week – Treatment: 70mg/week Fosamax Plus D Fosamax Oral Liquid |
Nausea and vomiting Heartburn Irritation or pain of the esophagus Difficulty swallowing Constipation or diarrhea Gas |
Risedronate |
Actonel 150 mg/month 75 mg twice monthly 35 mg/week Actonel with calcium Atelvia delayed release tablet 35 mg/week |
Nausea and vomiting Heartburn Irritation or pain of the esophagus Difficulty swallowing Constipation or diarrhea Gas |
Ibandronate |
Boniva tablet 150 mg/month Boniva injection |
Nausea and vomiting Heartburn Irritation or pain of the esophagus Difficulty swallowing Constipation or diarrhea Gas |
Zolendronic acid |
Reclast 5 mg IV yearly |
Nausea and vomiting Heartburn Irritation or pain of the esophagus Difficulty swallowing Constipation or diarrhea Gas |
Calcitonin
Calcitonin is a naturally occurring hormone that slows bone loss and increases bone density in the spine. It can be used to treat osteoporosis in women who are at least five years beyond menopause. Because calcitonin is not absorbed orally, a nasal spray containing salmon calcitonin has been developed to treat osteoporosis. It is easy to deliver and has few side effects. Calcitonin is also available as a subcutaneous injection, although this is not often used for osteoporosis.
Drug |
Brand name |
Dose |
Side effects |
How to use |
Calcitonin nasal spray |
Fortical Nasal Spray Miacalcin Nasal Spray Generic available |
200 IU daily |
Rhinitis Nasal irritation Flushing of the face and hands Nausea, vomiting, diarrhea |
One spray alternating nostrils daily |
Estrogen
Estrogen Therapy (ET) (for women who have had a hysterectomy) and Hormone Therapy (HT) (estrogen + progesterone for women with an intact uterus) are approved for prevention of osteoporosis in postmenopausal women.
ET and HT should be used in women who are recently postmenopausal and have symptoms of menopause such as hot flashes and vaginal dryness. ET and HT prevent bone resorption and prevent fractures of the spine and hip as well as other fractures. ET and HT are available in many different doses and dosage forms such as transdermal patches and vaginal rings. Even low doses of ET and HT have been shown to protect bones.
Adverse effects associated with ET and HT include increased risk of blood clots, gall bladder disease, and breast cancer. ET and HT are generally prescribed for no more than five years after menopause; however, some women may benefit from longer therapy.
Oral Estrogen Therapy Products
Oral estrogen |
Brand name |
Strengths (mg) |
Comments |
Side effects |
Conjugated Equine Estrogens (CEE) | Premarin |
0.3 0.45 0.625 0.9 1.25 2.5 |
Purified estrogens derived from pregnant mares’ urine, >11 different compounds |
Spotting Headache Breast pain Abdominal pain |
Micronized Estradiol |
Estrace
Generic: Mylan, Geneva |
0.5 1.0 1.5 2.0 |
Same as naturally occurring estrogen pre-menopause; however, undergoes significant first pass metabolism to estrone and conjugates |
Spotting Headache Breast pain Abdominal pain |
Oral Hormone Therapy Combinations
Product/Manufacturer |
Estrogen dose |
Progestin dose |
Comments |
Premphase |
Conjugated estrogens (CEE) 0.625 mg/day x 28 days |
Medroxylprogesterone (MPA) 5 mg x 14 days |
Cyclic regimen |
Prempro
Prempro 0.45 mg/ Prempro 0.3 mg/ |
CEE 0.625 mg/day x 28 days
CEE 0.45 mg CEE 0.3 mg |
MPA 2.5 mg x 28 days
MPA 1.5 mg MPA 1.5 mg |
Continuous regimen
Continuous regimen Continuous regimen |
Femhrt (Parke-Davis) |
Ethinyl estradiol 5 mcg |
Norethindrone acetate 1 mg |
Continuous therapy
Blister card of 28 tablets |
Ortho-Prefest (Ortho-McNeil) |
Estradiol 1 mg (#15) |
Estradiol 1 mg + Norgestimate 0.09 mg (#15) |
3 days estradiol alternating with 3 days estradiol + norgestimate continuous |
Activella (Pharmacia) |
Estradiol 1 mg, 0.5 mg |
Norethindrone acetate 0.5 mg, 0.1 mg |
Continuous regimen, Dialpack |
Transdermal Estrogen/Estrogen and Progestins
Drug |
Brand name |
Strengths |
Comments |
17 beta-Estradiol | Climara |
0.025 mg/day 0.05 mg/day 0.075 mg/day 0.1 mg/day |
Once weekly patch |
17 beta-Estradiol Levonorgestrel 15 mcg/day |
ClimaraPro | 0.045 mg/day | Once weekly patch |
17 beta-Estradiol |
Alora Esclim Estraderm
Vivelle Vivelle-Dot |
0.025 mg/day 0.05 mg/day 0.075 mg/day 0.1 mg/day Vivelle & Esclim also available in 0.037 mg dose |
Twice weekly patch
Twice weekly patch Postage stamp-sized patch |
Estradiol/Norethindrone |
CombiPatch (2 times/week) |
E 0.05 / 0.14 E 0.05 / 0.25 |
Continuous HRT sequential |
Estradiol | Estrasorb (Novavax) | Topical emulsion (lotion) | Apply to thighs or calves |
Estradiol gel |
EstroGel (Solvay)
Divigel 0.1% |
Metered dose estradiol 0.075 mg/day Daily packet |
Apply to one arm daily, from wrist to shoulder
Apply to thigh, do not wash for one hour |
Vaginal Estrogen Ring
Drug |
Brand name |
Strengths |
Comments |
Estradiol acetate | Femring |
0.05 mg/day 0.1 mg/day |
Systemic therapy of menopausal symptoms Prevention of osteoporosis |
Selective Estrogen Receptor Modulator (SERM)
Raloxifene is a selective estrogen receptor modulator (SERM) with estrogen-like effects on bone and antiestrogen effects on the uterus and breast. Raloxifene reduces bone resporption, increases bone density, and reduces the risk of spine fractures. It protects against estrogen-induced cancer of the uterus and breast. Like estrogen, raloxifene increases the risk of blood clots. It should only be used in women well past menopause because it may cause hot flashes.
Drug |
Brand Name |
Dose |
Indication |
Side Effects |
Raloxifene | Evista | 60 mg/day | Prevention or treatment of osteoporosis |
Hot flashes Leg cramps Deep vein thrombosis (blood clots) |
RANK-Ligand Inhibitor
In 2010 an entirely new type of anti-resorption drug was approved. Denosumab (Prolia) is a RANK-Ligand inhibitor. After menopause, decreased estrogen levels lead to increased production of RANK-ligand. RANK-Ligand is a protein that stimulates osteoclast-induced bone loss. Denosumab 60mg, a subcutaneous injection given every six months, reduces the activity of RANK-Ligand, resulting in decreased bone resorption and increased bone strength. Denosumab reduces the incidence of vertebral, nonvertebral, and hip fractures. Denosumab is indicated for post-menopausal women who have had fractures or are at high risk of fractures who have failed other osteoporosis therapy or who are intolerant of other osteoporosis therapy. Calcium and vitamin D supplements should be taken during Denosumab therapy. Side effects of Denosumab may include low calcium levels and skin rash. Denosumab can also affect the immune system. People with weakened immune systems can be at increased risk of serious infections. Patients taking denosumab should report any signs of infection to their health care provider such as fever or severe malaise.
Drug | Brand name | Dose | Indication | Side effects |
Denosumab | Prolia | 60 mg subcutaneous injection / 6 months | Indicated for post-menopausal women with increased risk of fracture who cannot take other osteoporosis medications or for whom other osteoporosis medications do not work well. | Rash Hypocalcemia Increased risk of infection |
Anabolic Medications
Anabolic drugs are a new and distinct class of medications for osteoporosis. These drugs increase the rate of bone formation. The first drug in this category is Teriparatide (Forteo), a form of parathyroid hormone. The daily 20 mg subcutaneous dose is easily measured and administered by its unique pen device. The medication is given for a maximum of two years, which is considered the “anabolic window.”
After it is discontinued, a bisphosphonate is then prescribed to retain the benefits of treatment and prevent bone resorption. Good candidates for teriparatide are persons with very low bone density (T-scores less than -3.0) who have experienced an osteoporosis-related fracture or anyone who has had fractures occur while on anti-resorptive therapy. All anti-resorptive therapy should be discontinued before starting teriparatide.
Drug | Brand name | Dose | Indication | Side effects |
Teriparatide | Forteo | 20 mg subcutaneous daily | Osteoporosis with fractures |
Leg cramps Dizziness |
For more information:
Go to the Osteoporosis health topic.