risedronate (Rx)

>10%

Arthralgia (7-33%)

Diarrhea (5-20%)

Headache (3-18%)

Nausea (4-13%)

Constipation (3-13%)

Rash (8-12%)

Abdominal pain (2-12%)

Hypertension (11%)

Dyspepsia (4-11%)

1-10%

Flulike syndrome (10%)

Depression (7%)

Chest pain (5-7%)

Dizziness (3-7%)

Pharyngitis (6%)

Rhinitis (6%)

Prostatic hyperplasia (5%)

Hypocalcemia (<5%)

Dyspnea (4%)

Gastritis (3%)

Nephrolithiasis (3%)

Hypophosphatemia (<3%)

Arrhythmia (2%)

<1%

Diaphyseal femur

Dysphagia

Esophageal cancer

Esophageal ulcer

Femur fracture

Gastric and duodenal ulcer

Osteonecrosis

Postmarketing Reports

Hypersensitivity reactions including angioedema, generalized rash and bullous skin reactions, some severe

Gastrointestinal: Esophagitis, flatulence, bloating, esophageal or gastric ulcers

Musculoskeletal pain: Bone, joint, or muscle pain, described as severe or incapacitating, have been reported rarely

Eye inflammation: Iritis, uveitis

Jaw osteonecrosis

Stevens-Johnson syndrome

Toxic epidermal necrolysis

Pulmonary: Asthma exacerbations

Contraindications

Hypersensitivity; angioedema, generalized rash, bullous skin reactions, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported

Hypocalcemia

Hypercalcemia from any cause including, but not limited to, hyperparathyroidism, hypercalcemia of malignancy, or sarcoidosis

Inability to stand or sit upright for at least 30 minutes

Esophagus abnormalities (eg, stricture, achalasia) that delay esophageal emptying

Cautions

Ensure adequate intake of calcium and vitamin D; correct hypocalcemia, if present, before initiating therapy

Avoid concomitant polyvalent cation-containing medications

May cause upper GI disorders (eg, dysphagia, esophagitis, esophageal or gastric ulcer); instruct patients to follow dosing instructions; discontinue use if new or worsening symptoms occur

Severe irritation of upper GI mucosa; discontinue if new or worsening symptoms occur in patients with active upper GI disease

Osteonecrosis of the jaw, can occur spontaneously and is generally associated with tooth extraction and/or local infection with delayed healing; known risk factors include invasive dental procedures (e.g., tooth extraction, dental implants, boney surgery), diagnosis of cancer, concomitant therapies (e.g., chemotherapy, corticosteroids, angiogenesis inhibitors), poor oral hygiene, and co-morbid disorders; risk of osteonecrosis of jaw may increase with duration of exposure to bisphosphonates

Food decreases bioavailability

Not recommended in severe renal impairment (CrCl <30 mL/min)

Risk of severe joint, muscle, or bone pain

Possible increased risk of atypical subtrochanteric and diaphyseal femur fractures; consider periodic reevaluation of need for continued bisphosphonate therapy, particularly if treatment lasts >5 years; patients with new thigh or groin pain should be evaluated to rule out a femoral fracture

Consider appropriate hormone replacement therapy if necessary

Administration of calcium has been associated with a slight increase in risk of kidney stones; in patients with a history of kidney stones or hypercalciuria, metabolic assessment to seek treatable causes of these conditions is warranted; if administration of calcium tablets necessary, monitor urinary calcium excretion periodically; patients with achlorhydria may have decreased absorption of calcium; taking calcium with food enhances absorption; concomitant use of calcium-containing antacids should be monitored to avoid excessive intake of calcium

Mechanism of Action

Bisphosphonate; binds to hydroxyapatite crystals in bone and inhibits osteoclast-mediated bone resorption

Absorption

Bioavailability: 0.54-0.75%

Peak plasma time: 1-3 hr

Distribution

Protein bound: 24%

Vd: 13.8 L/kg

Metabolism

Not metabolized

Elimination

Half-life: Initial, 1.5 hr; terminal, 480 hr

Renal clearance: 105 mL/min

Total body clearance: 122 mL/min

Excretion: Urine (up to 85%), feces (unabsorbed drug)

Instructions