Dosing & Uses
Dosage Forms & Strengths
tablet
- 5mg
- 30mg
- 35mg
- 150mg
tablet, delayed release
- 35mg
Postmenopausal Osteoporosis
Treatment and prevention
5 mg PO once daily or 35 mg PO once weekly or 150 mg PO once monthly
35 mg once-weekly dosing copackaged with calcium carbonate 1250 mg for remaining 6 days of week
Glucocorticoid-Induced Osteoporosis
5 mg/day PO
Paget Disease
30 mg/day PO for 2 months
Monitor serum alkaline phosphatase
Osteoporosis in Men
35 mg PO once weekly
Osteogenesis Imperfecta (Orphan)
Orphan indication sponsor
- Warner Chilcott Pharmaceuticals; 100 Enterprise Drive; Rockaway, NJ 07866
Dosing Modifications
Renal impairment
- CrCl >30 mL/min: No dose adjustment necessary
- CrCl <30 mL/min: Not recommended
Hepatic impairment
- Safety and efficacy not established
- No dose adjustment suggested; drug does not undergo hepatic metabolism
Administration
Immediate release
- Take at least 30 minutes with 6-8 oz water before first food or drink of day
- Swallow with plain water only, not coffee or juice
- Stand or sit upright; do not lie down for 30 minutes after taking to avoid esophageal irritation
Delayed release
- Administer in morning immediately after breakfast; compared with immediate-release risedronate, Atelvia resulted in significantly higher incidence of abdominal pain when administered before breakfast under fasting conditions
- To facilitate delivery to stomach, swallow whole while in upright position and with ≥4 oz plain water
- Tablets should not be chewed, cut, or crushed
- Do not lie down for 30 minutes after taking medication
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>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
Warnings
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
Esophageal cancer risk (July 21, 2011, FDA safety communication)
- Conflicting findings exist from studies evaluating the risk of esophageal cancer with oral bisphosphonates
- Esophagitis and other esophageal events have been reported, particularly in patients who do not follow specific directions for use of oral bisphosphonates (eg, sitting up or standing after administration, taking with full glass of water)
- Ongoing review of data from published studies to evaluate whether use of oral bisphosphonates is associated with increased risk of cancer of esophagus is currently being conducted by FDA
- FDA has not concluded that taking oral bisphosphonates increases risk of esophageal cancer
- Data are insufficient to recommend endoscopic screening of asymptomatic patients
- FDA will continue to evaluate all available data supporting safety and effectiveness of bisphosphonates and will update public when more information becomes available
- Instruct patients to contact their healthcare provider if they develop symptoms of esophagitis (eg, swallowing difficulties, chest pain, new or worsening heartburn, trouble or pain when swallowing)
Pregnancy & Lactation
Pregnancy
Available data on use in pregnant women are insufficient to inform a drug- associated risk of adverse maternal or fetal outcomes; discontinue therapy when pregnancy recognized
Animal data
In animal reproduction studies, daily oral administration to pregnant rats during organogenesis decreased neonatal survival and body weight at doses approximately 5-26 times, respectively, the highest recommended human daily dose of 30 mg (based on body surface area, mg/m2)
A low incidence of cleft palate was observed in fetuses of dams treated at doses approximately equal to 30 mg human daily dose; delayed skeletal ossification was observed in fetuses of dams treated at approximately 2.5 to 5 times the 30 mg human daily dose
Periparturient mortality due to maternal hypocalcemia occurred in dams and neonates upon daily oral administration of risedronate to pregnant rats during mating and/or gestation starting at doses equivalent to the 30 mg daily human dose
-
Effects of bisphosphonates on bones
- Bisphosphonates are incorporated into bone matrix, from which they are gradually released over a period of years; the amount of bisphosphonate incorporated into adult bone and available for release into systemic circulation is directly related to dose and duration of bisphosphonate use
- Based on mechanism of action of bisphosphonates, there is potential risk of fetal harm, predominantly skeletal, if a woman becomes pregnant after completing a course of bisphosphonate therapy; the impact of variables such as time between cessation of bisphosphonate therapy to conception, the particular bisphosphonate used, and the route of administration (intravenous versus oral) on this risk has not been studied
Females and males of reproductive potential
- There are no data available in humans; female and male fertility may be impaired based on animal studies demonstrating adverse effects on fertility parameters
Lactation
There are no data on presence in human milk, effects on breastfed infant, or on milk production; a small degree of lacteal transfer occurred in nursing rats
Concentration of the drug in animal milk does not necessarily predict the concentration of drug in human milk; however, when a drug is present in animal milk, it is likely that the drug will be present in human milk
Developmental and health benefits of breast-feeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breast-fed child from drug or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
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)
Administration
Instructions
Immediate release
- Take at least 30 minutes with 6-8 oz water before first food or drink of day
- Swallow with plain water only, not coffee or juice
- Stand or sit upright; do not lie down for 30 minutes after taking to avoid esophageal irritation
Delayed release
- Administer in morning immediately after breakfast; compared with immediate-release risedronate, Atelvia resulted in significantly higher incidence of abdominal pain when administered before breakfast under fasting conditions
- To facilitate delivery to stomach, swallow whole while in upright position and with ≥4 oz plain water
- Tablets should not be chewed, cut, or crushed
- Do not lie down for 30 minutes after taking medication
Images
Patient Handout
Formulary
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