Risedronate drug data and news

Risedronate drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Risedronate
Brand Names/Synonyms Actonel; Pyridine N-Oxide; Pyridostigmine Bromide; Pyridostigmine Bromine; Risedronate; Risedronate Sodium; Risedronic Acid
Indication For the treatment of Paget's disease of the bone (osteitis deformans); Postmenopausal and glucocorticoid-induced osteoporosis
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Description Not Available
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.
Risedronate News
(When available)

Self-tanning creams spark rashes, itching  May 16, 2006
...immediately. Your osteoporosis drug Actonel (risedronate) is in the same category as Fosamax (alendronate) and Boniva (ibandronate). ... - Charlotte Observer,

What’s up doc? Pros and cons of certain medications  May 15, 2006
...trade name Fosamax), pamidronate (trade name Aredia), zoledronic acid (trade name Zometa), etidronate (trade name Didrocal) and risedronate (trade name Actonel ... - Milford Daily News,

New drug combo treats osteoporosis  May 8, 2006
Alendronate (Fosamax) and risedronate (Actonel) are medications that slow down bone loss and have been shown to decrease the risk of fractures. ... - News 8 Austin,

Don't be dense -- osteoporosis can affect everyone -- even you  May 3, 2006
...reduce fracture rate. Alendronate (fosamax), and Risedronate (actonel) are available in daily or weekly therapy. Studies show that ... - Petaluma Argus-Courier,

Sally Field talks about osteoporosis  Apr 21, 2006
Other drugs recently approved for the prevention and treatment of osteoporosis are Actonel (risedronate), a bisphosphonate similar to Fosamax, and Evista ... - Food Consumer,

Medical Files : Getting over the ‘hump’  Apr 28, 2006
Bisphosphonates (alendronate, ibandronate and risedronate), calcitonin and estrogens act by preventing bone resorption, and are classified as antiresorptive ... - INQ7.net,

Dosage Forms TABLET
Drug_Category Antiresorptives; Bisphosphonates; Antihypocalcemic Agents;
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.

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, weakness
Organisms Affected Humans and other mammals
Chemical IUPAC Name (1-hydroxy-1-phosphono-2-pyridin-3-yl-ethyl)phosphonicacid
Chemical Formula C7H11NO7P2
Molecular Weight 283.112 g/mol
Smiles String C1=CC(=CN=C1)CC(O)(P(=O)(O)O)P(=O)(O)O
Melting Point Not Available
Water Solubility Not Available
State Solid
LogP/Hphobicity Not Available
Isoelectric Point Not Available
Biotransformation No evidence found for metabolization of risedronate in humans or mammals
Half Life 1.5 hours
Protein Binding [%] ~24%
RxList Link RXlist
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Drug Reference http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/act1580.shtml
http://www.drugs.com/cons/Risedronate.html
http://www.rxlist.com/cgi/generic/risedronate.htm
Drug Type Approved Drug
Accession No APRD00410
CAS Registry Number 105462-24-6
KEGG Compound ID C08233
PubChem ID SID:634947
PharmGKB ID Not Available
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2242518

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