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QuickView for Tiludronate (compound)


DrugBank
Identification
Name: tiludronate
Name (isomeric): DB01133
Drug Type: small molecule
Synonyms:
Tiludronate disodium; Acide tiludronique [INN-French]; Acidum tiludronicum [INN-Latin]; Tiludronic Acid Disodium Salt; Acido tiludronico [INN-Spanish]; Tiludronic acid
Brand: Skelid
Category: Antihypocalcemic Agents, Osteoporosis Prophylactic, Bone Density Conservation Agents
CAS number: 89987-06-4
Pharmacology
Indication: For treatment of Paget's disease of bone (osteitis deformans).
Pharmacology:
Tiludronate is a first generation (non-nitrogenous) bisphosphonate in the same family as etidronate and clodronate. Tiludronate affects calcium metabolism and inhibits bone resorption and soft tissue calcification. Of the tiludronate that is resorbed (from oral preparation) or infused (for intravenous drugs), about 50% is excreted unchanged by the ...
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Mechanism of Action:
The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. In vitro studies indicate that tiludronate acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable redu...
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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.
Protein binding: Approximately 90% bound to human serum protein (mainly albumin) at plasma concentrations between 1 and 10 mg/L.
Biotransformation: In vitro, tiludronic acid is not metabolized in human liver microsomes and hepatocytes. There is no evidence that tiludronate is metabolized in humans.
Route of elimination: The principal route of elimination of tiludronic acid is in the urine.
Half Life: 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.
Clearance: renal cl=10 mL/min [IV administration of 20-mg dose]
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.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
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.
Drug interaction:
Magnesium oxideThe divalent cation of oral Magnesium oxide may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours.
Magnesium SulfateThe divalent cation of oral Magnesium sulfate may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours.
Calcium ChlorideCalcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 2 hours before or after tiludronate/clodronate/etidronate.
Calcium AcetateThe divalent cation of oral Calcium Acetate may significantly decrease the absorption of Tiludronate by forming a nonabsorbable chelate. Oral dosing should be separated by at least 2 hours.

Targets