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Osteoporosis

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
70 mg + 2800 IU Vitamin D3/week

Fosamax Oral Liquid
70 mg/week
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
35 mg/week + calcium 500 mg/day

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
3 mg IV every 3 months
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/
1.5 mg

Prempro 0.3 mg/
1.5 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
0.025 mg, 0.05 mg, 0.1 mg
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, where you can:

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Last Reviewed: Jun 30, 2011

Debra K Gardner, PhamD Debra K Gardner, PhamD
Former Assistant Clinical Professor of Pharmacy College Business Office
Internal Resource Pool-Allied at OSU Medical Center
Wexner Medical Center
The Ohio State University