Osteoporosis Medications

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What Is Osteoporosis?

Osteoporosis is a disease characterized by low bone mass and loss of bone tissue that leads to weak and fragile bones.

What Causes Osteoporosis?

Osteoporosis occurs when the body fails to form enough new bone, when too much old bone is reabsorbed by the body, or both. Women are at a greater risk than men, especially women who are elderly, thin, or small. Other risk factors include the following:

What Are the Risks of Osteoporosis?

Bone pain similar to that of arthritis may occur in the early course of the disease. Later, sharp pain may suddenly occur and become worse with activity or weight bearing. Fractures may occur, particularly in your spine, although you may not have fallen. These are called spontaneous fractures. These fractures compress the vertebrae in the spine and are the cause for loss of height. Fractures at other sites, especially the hips, wrists, or ribs, occur more easily from falling down.

Medical Treatment Guidelines for Osteoporosis

Weight-bearing exercise, such as walking or jogging, riding stationary bicycles, using rowing machines, or lifting weights, helps promote bone strength. A diet rich in calcium and vitamin D is important for bone development, as well as for some of the medications for prevention or treatment to work to their fullest capacity. Vitamin D is also gained from short exposure to sunlight each day (5 minutes without sunscreen, or 1 hour with sunscreen). Unfortunately, vitamin D and calcium supplements, by themselves, are not able to prevent most cases of osteoporosis.

In addition to exercise and diet, various drugs, vitamins, and minerals are used to prevent and treat osteoporosis. Avoiding excessive alcohol ingestion and quitting smoking are also very important.

Dietary phytoestrogens found in soy products and legumes are not potent enough to justify their use as a treatment for osteoporosis, but they may be useful in delaying or preventing osteoporosis as part of a healthy lifestyle that includes a calcium-rich diet and exercise.

Calcium and Vitamin D Supplements

Calcium is widely available without a prescription. Some examples of calcium-containing tablets or capsules include Os-Cal, Citracal, and Cal-Citrate. Some antacids (for example, TUMS) contain calcium carbonate and are often used as a calcium supplement. New forms of calcium include Viactiv, a chewable candy-like supplement containing calcium carbonate, vitamin D, and vitamin K.

  • How calcium and vitamin D work: Adequate calcium and vitamin D are essential for reducing bone loss. Also, in order for other prevention and treatment medications to be effective, adequate calcium and vitamin D levels are essential.
  • Who should not use these medications: Persons with any of the following conditions should not use calcium or vitamin D supplements:
  • Use: These supplements should be used as follows:
    • Calcium: Daily oral intake of 1000-1200 mg of calcium is recommended to decrease osteoporosis risk. This can be accomplished by a diet rich in calcium and calcium supplements. Adults typically do not meet daily calcium dietary requirements and may require calcium supplements in order to do so. Your doctor may recommend up to 1500 mg per day if you already have osteoporosis or are at high risk for it. For maximum absorption of calcium from the stomach, the daily requirement should be divided into 2-3 doses per day that do not exceed 600 mg per dose.
    • Vitamin D: Daily intake of 600-800 units of vitamin D is needed to increase bone mass for treatment. Diet, sun exposure, or vitamin D supplements can provide the necessary requirement. Prevention of osteoporosis can be achieved with lower doses of 200-400 units per day. Many multivitamins or calcium supplements also contain vitamin D.
  • Drug or food interactions: Ask your doctor or pharmacist if certain foods affect your particular calcium supplement. Some calcium supplements are better absorbed from the stomach after a meal, while others are not. Some food (for example, spinach, rhubarb, whole-grain bran cereals) may bind with calcium and decrease calcium absorption. Calcium may bind to some oral medications, making them unable to be absorbed by the stomach. This is usually easy to avoid by not taking calcium within 1-2 hours before or 2-4 hours after taking medications such as sucralfate (Carafate), tetracycline (Sumycin), ciprofloxacin (Cipro), and moxifloxacin (Avelox). Thiazide diuretics, such as hydrochlorothiazide (HydroDIURIL), may increase calcium levels and cause toxicity.
  • Side effects: Calcium may cause constipation, nausea, or vomiting. Individuals who have had kidney stones should have the calcium level in their urine checked to see if the increased calcium ingestion will contribute to kidney stones. Vitamin D doses recommended by your doctor should not be exceeded. Taking high-dose vitamin D for a long time can lead to toxicity and cause symptoms such as weakness, headache, drowsiness, muscle pain, bone pain, and elevated liver enzyme levels.

Estrogen Therapy for Osteoporosis

Estrogen is available in oral tablets or capsules or as a transdermal (skin) patch. Estrogen is used as part of hormone replacement therapy (HRT) after menopause. Following a hysterectomy (removal of the uterus), estrogen alone is used. For women with a uterus, progestin is added to estrogen to decrease the risk of endometrial (the inside lining of the uterus) cancer. Women with a personal or family history of breast cancer should not take estrogens.

Other effective preventive and treatment options for osteoporosis exist, and more are being developed to avoid increasing hormone-related risks. The duration of HRT therapy women take following menopause is currently being questioned because of the increased risk of cancer, stroke, and heart attack. Examples of oral estrogens include conjugated estrogen (Premarin) and estradiol (Estrace). Examples of oral combination products of estrogen with progestin include Premphase, Prempro, Activella, and Ortho-Prefest. Examples of skin patches include estradiol (Alora, Climara, Esclim, Estraderm, Vivelle) and combination patches containing estradiol and progestin (Climara Pro, CombiPatch).

  • How estrogen works: This substance slows bone loss and prevents osteoporosis when taken after menopause.
  • Who should not use these medications: Persons with the following conditions should not use estrogen:
  • Use: The following are general guidelines:
    • The dose of estrogen used, whether alone or with a progestin, should be the lowest effective dose taken for the shortest time consistent with treatment goals.
    • Oral tablets are typically taken daily; for those requiring progestin, it may be given in a combination product or at various times in the monthly cycle.
    • Skin patches are applied to the abdomen, hip, or upper buttock. The replacement schedule for patches depends on which patch is used. Some are replaced weekly (Climara); others are replaced twice a week (Vivelle).
  • Drug or food interactions: Estrogens may decrease the effectiveness of anticoagulants such as warfarin (Coumadin). Contact your doctor or pharmacists before taking other prescription drugs, over-the-counter drugs, or herbal products.
  • Side effects: The Women's Health Initiative (WHI) study reported increased risks of heart attack, stroke, invasive breast cancer, pulmonary emboli (blood clots in the lungs), and deep vein thromboses (blood clots in the legs) in postmenopausal women (50-79 years) during 5 years of treatment with conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo (sugar pills). Estrogens may cause breast tenderness, weight gain, fluid retention, gall bladder disease, and vaginal bleeding, along with increasing the risk of breast or endometrial cancers. They also increase the risk of blood clots and may increase the risk of complications from clots, such as stroke, heart attack, or thrombophlebitis. Call your doctor immediately if you experience any of the following side effects:
    • Itching, hives, swelling in face or hands, breathing troubles, or other allergic reactions
    • Breast lumps
    • Tenderness in the upper right stomach, nausea, vomiting, fever, or pain
    • Vision changes
    • Severe headache
    • Coughing up blood
    • Chest or lower leg pain

Selective Estrogen Receptor Modulators

Raloxifene (Evista) is a selective estrogen receptor modulator (SERM). Unlike estrogen, raloxifene is not associated with an increased risk of uterine cancer and reduces invasive breast cancer.

  • How SERMs work: SERMs have been specifically tailored to provide particular estrogen effects. Raloxifene is a SERM that preserves bone density but is not associated with estrogen risk factors such as uterine or breast cancer.
  • Who should not use these medications: Persons with the following conditions should not use SERMS:
    • Allergy to SERMs
    • Pregnancy
    • Breastfeeding
    • Active or past history of venous thrombosis (blood clots in veins)
  • Use: SERMS are taken orally as a tablet every day for prevention or treatment of osteoporosis.
  • Drug or food interactions: Cholestyramine (Questran, Cholybar) decreases raloxifene blood concentrations. The time of administration of each drug should be as far apart as possible.
  • Side effects: These drugs may cause hot flushes and blood clots at a risk comparable to that of estrogen. Raloxifene should be discontinued 3 days before surgery and throughout the recovery period following surgery. Call your doctor immediately if you experience any of the following side effects:
    • Chest pain
    • Trouble breathing
    • Coughing up blood
    • Pain, swelling, or redness in your leg, particularly if below the knee
    • Severe headache
    • Blurred vision or vision changes

Bisphosphonates for Osteoporosis

Alendronate (Fosamax), ibandronate (Boniva), risedronate (Actonel), and zoledronic acid (Reclast) are used for both prevention and treatment of osteoporosis.

  • How bisphosphonates work: These drugs slow bone loss by increasing bone formation and decreasing bone turnover. Calcium and vitamin D are required for bisphosphonates to work most effectively. Bisphosphonates are also effective in treating osteoporosis in men and people with corticosteroid-induced osteoporosis.
  • Who should not use these medications: Persons with the following conditions should not use bisphosphonates:
    • Allergy to bisphosphonates
    • Hypocalcemia
    • Abnormalities of the esophagus
    • Inability to stand or sit upright for 30 minutes after taking a bisphosphonate
    • Decreased kidney function
    • Increased risk of aspiration (contents from stomach or throat go into lungs)
  • Use: Various dosage regimens are used. Bisphosphonates may be taken daily for prevention or treatment, or a larger dose may be given once each week and now once a month with Boniva. It is important to take oral bisphosphonates only with a full glass of water and to stand or sit upright for 30-60 minutes after swallowing the drug. Do not take at the same time with your other medication. After 30 minutes, you can take your other medications that may be scheduled for the same time. Zoledronic acid (Reclast) is given as a once yearly IV infusion for those who cannot tolerate oral bisphosphates.
  • Drug or food interactions: Food, caffeine, milk, orange juice, and antacids reduce the absorption of bisphosphonates from the stomach, potentially decreasing efficacy. Use with caution with other drugs that cause stomach or esophagus irritation, such as aspirin or aspirin products (salsalate or mesalamine [Asacol, Pentasa, Rowasa]).
  • Side effects: Your doctor will monitor your blood to make sure you have adequate calcium and vitamin D levels. Gastrointestinal side effects, such as abdominal pain, constipation or diarrhea, gas, esophagus ulcer, or stomach bloating, may occur. Esophageal ulcers or swelling may be severe enough to cause bleeding and has resulted in hospitalization, even death. Standing or sitting upright for 30 minutes after taking oral bisphosphonates helps prevent the drug causing esophageal irritation. Call your doctor immediately if you experience any of the following side effects:
    • Allergy symptoms, such as itching, hives, swelling of mouth or hands, tightness in chest, or trouble breathing
    • Unusual or severe stomach or throat pain


    • Coughing up or vomiting blood

Calcitonins for Osteoporosis

Calcitonin (Miacalcin Nasal Spray) is useful for treating bone pain after a fracture due to osteoporosis. Newer drugs are typically used for osteoporosis treatment.

  • How calcitonin works: This hormone responds to elevated calcium levels in the blood by increasing calcium stores in bone and elimination of calcium by the kidneys. They are typically used for only a short time (several weeks to months). Calcium and vitamin D supplements are vital to ensure calcitonin efficacy. The drug may be genetically engineered from human calcitonin or derived from salmon.
  • Who should not use these medications: Individuals with allergy to salmon calcitonin should not use it.
  • Use: Calcitonins may be administered by injection given every other day or daily. It can also be taken as a nasal spray each day.
  • Drug or food interactions: Calcitonin may decrease lithium blood concentrations.
  • Side effects: Resistance to salmon calcitonin may occur. Calcitonins may cause nausea, vomiting, altered blood sugar levels, increased urinary frequency, runny nose (with nasal spray), and flushing of hands or face. Call your doctor immediately if you experience any of the following side effects:
    • Chest tightness
    • Trouble breathing
    • Itching or hives
    • Swelling of face or hands
    • Tingling in mouth or throat
    • Heavy or ongoing nose bleeds (with nasal spray)
    • Lightheadedness or fainting

Parathyroid Hormone Derivatives for Osteoporosis

Teriparatide (Forteo) is a genetically engineered parathyroid hormone (PTH).

  • How parathyroid hormone derivatives work: PTH regulates calcium in the blood and stimulates bone formation.
  • Who should not use these medications: Persons with allergy to PTH derivatives should not take them, nor should those with an increased risk of osteosarcoma, such as people with Paget's disease, unexplained alkaline phosphatase elevations, open epiphyses (a part of long bones), or prior skeletal radiation.
  • Use: PTH derivatives are given as a subcutaneous (beneath the skin) injection each day. Because of the potential for fainting after administering the drug, the initial doses should be given while sitting or lying down.
  • Drug or food interactions: No drug or food interactions have been identified at this time.
  • Side effects: Since PTH derivatives increase calcium levels in the blood, your doctor will monitor your blood levels. They may also increase uric acid levels in the blood and cause low blood pressure following administration. A sudden drop in blood pressure may aggravate existing heart disease. Nausea, vomiting, constipation, and unusual tiredness or weakness are possible. Contact your doctor if these side effects persist.

Investigational Drugs for Osteoporosis

  • Etidronate (Didronel): This is another bisphosphonate approved by the FDA for treatment in Paget's disease.
  • Lasofoxifene: This is a SERM that decreases bone loss. It has favorable effects on blood cholesterol level and may prevent the growth of certain breast cancer cells.
  • Basedoxifene: This is another SERM currently undergoing clinical trials.
  • Strontium (Protos): This is an oral drug in development in Europe, Australia, and Japan. It decreases breakdown of bone and increases bone formation.

For More Information on Osteoporosis

National Osteoporosis Foundation

North American Menopause Society

International Osteoporosis Foundation

National Osteoporosis Foundation, Medications To Prevent & Treat Osteoporosis

The National Women's Health Information Center, Osteoporosis

breastcancer.org, Bone Strength, Osteoporosis, Medications

Osteoporosis Pictures

The image on the left shows decreased bone density in osteoporosis. The image on the right shows normal bone density.
The image on the left shows decreased bone density in osteoporosis. The image on the right shows normal bone density.. Click to view larger image.

Arrow indicates vertebral fractures
Arrow indicates vertebral fractures Click to view larger image.

A. Normal spine, B. Moderately osteoporotic spine, C. Severely osteoporotic spine.
A. Normal spine, B. Moderately osteoporotic spine, C. Severely osteoporotic spine. Click to view larger image.

Hormone replacement therapy causes calcium to be retained in bone cells. Calcium increases bone strength.
Hormone replacement therapy causes calcium to be retained in bone cells. Calcium increases bone strength. Click to view larger image.

Reviewed on 12/4/2017

Medically reviewed by John A. Daller, MD; American Board of Surgery with subspecialty certification in surgical critical care

REFERENCE:

"Overview of the management of osteoporosis in postmenopausal women"

UpToDate.com

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