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Drug classification

HISTORY

Osteoporosis develops when bone mineral density (BMD) and bone mass decreases or when the quality or structure of bone changes, leading to a decrease in bone strength that can increase the risk of fractures. Fractures occur most often in bones of the hip, vertebrae, and wrist.

Factors that may increase the risk for osteoporosis include: Sex: Chances of developing osteoporosis are greater in females. Age: Bone loss happens quicker and new bone growth is slower. Body size: Slender, thin-boned women and men are at greater risk. Race: White and Asian women are at highest risk. Family history: Hereditary factors may increase risk. Diet: A diet low in calcium and vitamin D may increase risk for osteoporosis and fracture.

Diagnosis: DEXA Scan (DXA) measures the BMD at sites that are prone to fracture (e.g., hip, spine). Bone density measurement by DXA at the hip and spine is generally considered the most reliable way to diagnose osteoporosis and predict risk of fracture.

ACTION

Bisphosphonates: Nonhormonal drugs that decrease bone resorption by binding to active sites of bone remodeling and inhibit osteoclasts. Slow down bone loss, which may decrease risk of fractures.

Selective estrogen receptor modulator (SERM): Decreases bone resorption, increasing BMD and decreasing the incidence of fractures.

Conjugated estrogens and selective estrogen receptor modulator: Increases BMD in postmenopausal women.

Parathyroid hormone analogs: Increase BMD by stimulating bone formation.

RANK ligand (RANKL) inhibitor: Inhibits osteoclast formation, function, and survival, reducing bone resorption. Increases BMD and reduces the incidence of new vertebral and hip fractures.

Sclerostin inhibitor: Binds to and inhibits sclerostin, increasing bone formation and decreasing bone resorption.

BISPHOSPHONATES

NameAvailabilityDosageClass Side Effects
Alendronate (Binosto, Fosamax)
  • T: 5 mg, 10 mg, 35 mg, 70 mg

  • S: 70 mg/75 mL

  • Prevention: 5 mg/day or 35 mg/wk

  • Treatment: 10 mg/day or 70 mg/wk

Hypocalcemia, may cause jaw osteonecrosis (rarely); GI (e.g., heartburn, esophageal irritation, esophagitis, abdominal pain, diarrhea); severe bone, joint, or muscle pain. IV: acute-phase reaction (e.g., low-grade fever, myalgia, arthralgia) within 1–3 days of the infusion
Ibandronate (Boniva)
  • T: 150 mg

  • 1: 1 mg/mL

  • Prevention and treatment: 150 mg/mo

  • IV Injection: Treatment: 3 mg/3 mos

Risedronate (Actonel)
  • T: 5 mg, 35 mg, 150 mg

  • T (DR): 35 mg

Prevention and treatment: 5 mg/day, 35 mg/wk, or 150 mg/mo
Zoledronic acid (Reclast)I: 5 g/100 mL
  • Prevention: IV: 5 mg every 2 yrs

  • Treatment: IV: 5 mg every yr

SERM

NameAvailabilityDosageSide Effects
Raloxifene (Evista)T: 60 mgPrevention and treatment: 60 mg/dayLeg cramps, hot flashes, increased risk of thromboembolic events

PARATHYROID HORMONE

NameAvailabilityDosageClass Side Effects
  • I: 2,000 mcg/mL prefilled pen delivers 80 mcg/dose

  • I: 250 mcg/mL syringe delivers 20 mcg/dose

  • Treatment: 80 mcg subcutaneously once daily

  • Treatment: 20 mcg subcutaneously once daily

Muscle cramps, injection site reactions, tachycardia, hypotension, increased serum uric acid concentration, hypercalciuria, dizziness, nausea, headache, hypercalcemia

CONJUGATED ESTROGENS AND SELECTIVE ESTROGEN RECEPTOR MODULATOR

NameAvailabilityDosageSide Effects
Conjugated estrogens and bazedoxifene (Duavee)T: 0.45 mg/20 mgPrevention: 1 tablet once dailyMuscle spasms; nausea; dyspepsia; and abdominal, neck, or oropharyngeal pain, increased risk of DVT/ thromboembolism with long term use

MONOCLONAL ANTIBODY RANKL INHIBITOR

NameAvailabilityDosageSide Effects
Denosumab (Prolia)I: 60 mg/mLSQ: 60 mg once every 6 mosDermatitis, rash, eczema, hypocalcemia. May cause jaw osteonecrosis (rarely).
DR, Delayed-release; I, injection; S, solution (oral); T, tablet.

SCLEROSTIN INHIBITOR

NameAvailabilityDosageSide Effects
Romosozumab (Evenity)I: 105 mg/1.17 mL syringeSQ: 210 mg (2 injections) once every mo for up to 12 dosesArthralgia, headache, increased risk of jaw osteonecrosis, atypical femoral fractures, serious cardiovascular events (e.g., MI, stroke)
SQ, subcutaneous.