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Risedronate: profile and news
Self-tanning creams spark rashes, itching May 16, 2006 What’s up doc? Pros and cons of certain medications May 15, 2006 New drug combo treats osteoporosis May 8, 2006 Don't be dense -- osteoporosis can affect everyone -- even you May 3, 2006 Sally Field talks about osteoporosis Apr 21, 2006 Medical Files : Getting over the ‘hump’ Apr 28, 2006 Other information Indication For the treatment of Paget's disease of the bone (osteitis deformans); Postmenopausal and glucocorticoid-induced osteoporosis 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 isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. Drug Category Antiresorptives; Bisphosphonates; Antihypocalcemic Agents; Brand Names/Synonyms Actonel; Pyridine N-Oxide; Pyridostigmine Bromide; Pyridostigmine Bromine; Risedronate; Risedronate Sodium; Risedronic Acid Dosage Forms TABLET Absorption Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract Interactions -->Interactions for Risedronate: No specific drug-drug interaction studies were performed. Risedronate is not metabolized and does not induce or inhibit hepatic microsomal drug-metabolizing enzymes (Cytochrome P450). Calcium Supplements/Antacids Co-administration of ACTONEL and calcium, antacids, or oral medications containing divalent cations will interfere with the absorption of ACTONEL. Hormone Replacement Therapy One study of about 500 early postmenopausal women has been conducted to date in which treatment with ACTONEL (5 mg/day) plus estrogen replacement therapy was compared to estrogen replacement therapy alone. Exposure to study drugs was approximately 12 to 18 months and the primary endpoint was change in BMD. If considered appropriate, ACTONEL may be used concomitantly with hormone replacement therapy. Aspirin/Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) Of over 5700 patients enrolled in the ACTONEL Phase 3 osteoporosis studies, aspirin use was reported by 31% of patients, 24% of whom were regular users (3 or more days per week). Forty-eight percent of patients reported NSAID use, 21% of whom were regular users. Among regular aspirin or NSAID users, the incidence of upper gastrointestinal adverse experiences in ACTONEL-treated patients (24.5%) was similar to that in placebo-treated patients (24.8%). H2 Blockers and Proton Pump Inhibitors (PPIs) Of over 5700 patients enrolled in the ACTONEL Phase 3 osteoporosis studies, 21% used H2 blockers and/or PPIs. Among these patients, the incidence of upper gastrointestinal adverse experiences in the ACTONEL-treated patients was similar to that in placebo-treated patients. Drug/Laboratory Test Interactions Bisphosphonates are known to interfere with the use of bone-imaging agents. Specific studies with ACTONEL have not been performed. Chemical IUPAC Name (1-hydroxy-1-phosphono-2-pyridin-3-yl-ethyl)phosphonicacid Chemical Formula C7H11NO7P2 Half Life 1.5 hours Drug Type Approved Drug # Accession No APRD00410 CAS Registry Number 105462-24-6 |
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