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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01133
rdf:type
n3:Drug
n3:description
Tiludronate is a bisphosphonate characterized by a (4-chlorophenylthio) group on the carbon atom of the basic P-C-P structure common to all bisphosphonates.
n3:generalReferences
# Murakami H, Takahashi N, Sasaki T, Udagawa N, Tanaka S, Nakamura I, Zhang D, Barbier A, Suda T: A possible mechanism of the specific action of bisphosphonates on osteoclasts: tiludronate preferentially affects polarized osteoclasts having ruffled borders. Bone. 1995 Aug;17(2):137-44. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8554921 # Rogers MJ: New insights into the molecular mechanisms of action of bisphosphonates. Curr Pharm Des. 2003;9(32):2643-58. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14529538 # Sansom LN, Necciari J, Thiercelin JF: Human pharmacokinetics of tiludronate. Bone. 1995 Nov;17(5 Suppl):479S-483S. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8573422
n3:group
approved
n3:halfLife
Half-life in healthy subjects is 50 hours following administration of a 400 mg single oral dose. Half-life in pagetic patients is about 150 hours following administration of 400 mg tiludronate a day for 12 days. In patients with renal insufficiency (creatinine clearance between 11 and 18 mL per minute [mL/min]), half-life is 205 hours from plasma after administration of a single, oral dose equivalent to 400 mg tiludronate.
n3:indication
For treatment of Paget's disease of bone (osteitis deformans).
owl:sameAs
n11:DB01133 n15:DB01133
dcterms:title
Tiludronate
adms:identifier
n17:Tiludronate n18:DB01133 n19:C08141 n20:54905 n21:60937 n22:46505302 n23:0024-1800-16 n24:PA451688
n3:mechanismOfAction
The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. <i>In vitro</i> studies indicate that tiludronate acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable reduction in the enzymatic and transport processes that lead to resorption of the mineralized matrix. Bone resorption occurs following recruitment, activation, and polarization of osteoclasts. Tiludronate appears to inhibit osteoclasts by at least two mechanisms: disruption of the cytoskeletal ring structure, possibly by inhibition of protein-tyrosine-phosphatase, thus leading to detachment of osteoclasts from the bone surface and the inhibition of the osteoclastic proton pump.
n3:packager
n9:271B4634-363D-11E5-9242-09173F13E4C5
n3:patent
n8:4876248 n8:1327009
n3:routeOfElimination
The principal route of elimination of tiludronic acid is in the urine.
n3:synonym
Tiludronate Tiludronic acid Acido tiludronico Acidum tiludronicum Acide tiludronique
n3:toxicity
Based on the known action of tiludronate, hypocalcemia is a potential consequence of overdose. In one patient with hypercalcemia of malignancy, intravenous administration of high doses (800 mg/day total dose, 6 mg/kg/day for 2 days) was associated with acute renal failure and death.
n3:foodInteraction
Do not take aluminum or magnesium-containing antacids within 2 hours of taking tiludronate. Take on an empty stomach (at least 2 hours before or after meals) with a full glass of plain water. Other beverages may reduce drug absorption.
n3:proteinBinding
Approximately 90% bound to human serum protein (mainly albumin) at plasma concentrations between 1 and 10 mg/L.
n3:salt
n3:synthesisReference
William Rocco, Sharon M. Laughlin, "Stable pharmaceutical compositions containing tiludronate hydrates and process for producing the pharmaceutical compositions." U.S. Patent US5656288, issued April, 1995.
n13:hasConcept
n14:M0163475
foaf:page
n6:tiludronate.htm n25:tiludronate.html
n3:IUPAC-Name
n4:271B463A-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4640-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B463F-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B463C-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B463D-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B463E-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4638-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4639-363D-11E5-9242-09173F13E4C5 n4:271B464F-363D-11E5-9242-09173F13E4C5 n4:271B4636-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4637-363D-11E5-9242-09173F13E4C5
n26:hasATCCode
n27:M05BA05
n3:H-Bond-Acceptor-Count
n4:271B4646-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4647-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4641-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4642-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4644-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4643-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4645-363D-11E5-9242-09173F13E4C5
n3:absorption
The mean oral bioavailability in healthy male subjects is 6% after an oral dose equivalent to 400 mg tiludronic acid administered after an overnight fast and 4 hours before a standard breakfast. In single-dose studies, bioavailability was reduced by 90% when an oral dose equivalent to 400 mg tiludronic acid was administered with, or 2 hours after, a standard breakfast compared to the same dose administered after an overnight fast and 4 hours before a standard breakfast.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
89987-06-4
n3:category
n3:clearance
* renal cl=10 mL/min [IV administration of 20-mg dose]
n3:containedIn
n12:271B4635-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B464B-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B464D-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B464E-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B464A-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4649-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B464C-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B463B-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4648-363D-11E5-9242-09173F13E4C5