Risedronate sodium CAS No. 115436-72-1
Category: Pyridinyl bisphosphonate
Product Description
Risedronate sodium is a bisphosphonate medication primarily used to treat and prevent osteoporosis in postmenopausal women and men, as well as glucocorticoid-induced osteoporosis and Paget’s disease of bone. It works by inhibiting osteoclast-mediated bone resorption, thereby increasing bone mineral density and reducing fracture risk. Available in various tablet forms (5 mg, 30 mg, 35 mg, 150 mg) and delayed-release tablets (35 mg), risedronate sodium must be taken on an empty stomach with a full glass of plain water, and patients should remain upright for at least 30 minutes afterward to avoid esophageal irritation. Common side effects include gastrointestinal upset, while rare but serious side effects can involve esophagitis, osteonecrosis of the jaw, atypical femur fractures, and hypocalcemia. It is contraindicated in individuals with hypersensitivity to bisphosphonates, severe kidney impairment (CrCl <30 mL/min), and those unable to sit or stand upright for 30 minutes. Drug interactions may occur with calcium, iron, antacids, PPIs, NSAIDs, and loop diuretics. Patients should ensure adequate calcium and vitamin D intake and undergo dental exams before starting therapy, especially due to the risk of osteonecrosis of the jaw. Long-term use may require periodic reassessment to manage potential risks.
Product Use & Characteristics
Chemical & Physical Properties
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Molecular Formula: C₇H₁₀NNaO₇P₂ (hemipentahydrate form)
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Molecular Weight: 305.09 g/mol
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IUPAC Name: Sodium; hydroxy-(1-hydroxy-1-phosphono-2-pyridin-3-ylethyl)phosphinate
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CAS Number: 115436-72-1
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Physical Appearance: Fine, white to off-white crystalline powder, soluble in water, insoluble in organic solvents
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Bioavailability: Very low (~0.6–0.7%) due to poor gastrointestinal absorption
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Pharmacokinetics: No metabolic transformation; eliminated via kidneys and feces; half-life ~1.5 hours for plasma but retained in bone long-term
Mechanism of Action
Risedronate sodium is a nitrogen-containing bisphosphonate that binds strongly to hydroxyapatite in bone, inhibiting osteoclast-mediated bone resorption. It induces apoptosis in osteoclasts by disrupting key cellular pathways, leading to decreased bone breakdown and increased bone density.
Clinical Uses
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Indications:
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Treatment and prevention of postmenopausal osteoporosis
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Treatment of osteoporosis in men
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Treatment of glucocorticoid-induced osteoporosis
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Management of Paget’s disease of bone
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Efficacy: Reduces vertebral fractures by ~41–49%, hip fractures by ~46% in high-risk women over 3 years
Dosage Forms & Regimens
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Oral Tablets: 5 mg daily, 35 mg weekly, 75 mg twice monthly, or 150 mg once monthly
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Delayed-Release Tablets: 35 mg weekly, taken right after breakfast
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Paget’s Disease: 30 mg daily for 2 months
Administration Guidelines
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Original Tablets: Taken in the morning on an empty stomach with 6–8 oz plain water; remain upright for ≥30 minutes; no food, drink, or other meds during that time
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Delayed-Release Form: Take after breakfast with ≥4 oz water; same upright rule applies
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Important Note: Avoid calcium, iron, antacids, or dairy within 2 hours of dosing to prevent absorption interference
Contraindications & Precautions
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Contraindications:
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Hypersensitivity to bisphosphonates
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Severe kidney impairment (CrCl <30 mL/min)
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Inability to sit/stand upright for ≥30 minutes
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Hypocalcemia (must be corrected before starting treatment)
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Pregnancy (Category C) – Not recommended unless benefits outweigh risks
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Monitor: Dental health (risk of osteonecrosis of the jaw), calcium levels, renal function
Side Effects & Risks
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Common Side Effects:
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Gastrointestinal discomfort (heartburn, nausea, diarrhea, abdominal pain)
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Musculoskeletal pain (bone, muscle, or joint pain)
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Headache
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Flu-like symptoms
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Serious Side Effects (Rare):
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Esophagitis
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Osteonecrosis of the jaw (ONJ)
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Atypical femur fractures
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Hypocalcemia
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Eye inflammation
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Severe allergic reactions (anaphylaxis)
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Important Notes
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Supplemental Calcium and Vitamin D: Recommended if dietary intake is inadequate
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Dental Exams: Recommended before starting bisphosphonates due to ONJ risk
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Long-Term Use: (>3–5 years) may require periodic reassessment due to potential risks
Brand Names
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Actonel
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Atelvia (delayed-release)
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Generics
Drug Interactions
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Reduced Absorption: Calcium, iron, antacids, PPIs (take at a different time of day)
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Increased GI Irritation: NSAIDs
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Increased Risk of Hypocalcemia: Loop diuretics
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