Name: | risedronate |
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Name (isomeric): | DB00884 |
Drug Type: | small molecule |
Synonyms: |
Risedronic acid; NE-58095; Risedronate sodium
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Brand: | Benet, Actonel 150, Actonel |
Brand name mixture: | Actonel with Calcium (Procter & Gamble)(risedronate sodium + calcium carbonate), Actonal Plus Calcium (Warner Chilcott)(risedronate sodium hemi-pentahydrate + calcium carbonate) |
Category: | Antihypocalcemic Agents, Bisphosphonates, Calcium Channel Blockers, Bone Density Conservation Agents, Antiresorptives |
CAS number: | 105462-24-6 |
Indication: | For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis |
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Pharmacology: | Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women. |
Mechanism of Action: |
The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isopr...
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Absorption: | Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract |
Protein binding: | ~24% |
Biotransformation: | No evidence found for metabolization of risedronate in humans or mammals |
Route of elimination: | Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats. |
Half Life: | 1.5 hours |
Clearance: | 122 mL/min 73 mL/min [osteopenic postmenopausal women] |
Toxicity: | Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness. |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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