Tiludronate

A bisphosphonate drug used in the treatment of bone disorders

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Tiludronate

Drug Information
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Tiludronate is a bisphosphonate drug used primarily in the treatment of Paget's disease of bone and other bone disorders. It functions by inhibiting bone resorption, which is the process by which osteoclasts break down bone tissue and release minerals, resulting in a transfer of calcium from bone fluid to the blood.

Mechanism of Action

Tiludronate belongs to the class of drugs known as bisphosphonates, which are analogs of pyrophosphate. These compounds bind to hydroxyapatite found in bone, inhibiting the action of osteoclasts. By doing so, tiludronate reduces bone turnover and stabilizes the bone matrix.

Pharmacokinetics

Tiludronate is administered orally, and its bioavailability is approximately 6%. It is highly protein-bound in the plasma, with about 90% of the drug bound to proteins. The drug is not metabolized and is excreted unchanged in the urine. The elimination half-life of tiludronate is approximately 150 hours, which allows for once-daily dosing.

Clinical Uses

Tiludronate is primarily used in the treatment of Paget's disease of bone, a condition characterized by abnormal and excessive bone remodeling. It may also be used off-label for other conditions involving bone loss, such as osteoporosis, although other bisphosphonates are more commonly used for this purpose.

Side Effects

Common side effects of tiludronate include gastrointestinal disturbances such as nausea, diarrhea, and abdominal pain. Less commonly, patients may experience musculoskeletal pain, headache, and skin rash. As with other bisphosphonates, there is a risk of osteonecrosis of the jaw, particularly in patients undergoing invasive dental procedures.

Contraindications

Tiludronate is contraindicated in patients with hypersensitivity to bisphosphonates, severe renal impairment, and in those with esophageal abnormalities that delay esophageal emptying. Caution is advised in patients with active upper gastrointestinal problems.

Interactions

Tiludronate may interact with calcium supplements, antacids, and other medications containing divalent cations, as these can interfere with its absorption. It is recommended to take tiludronate at least two hours before or after such products.

Also see

• Bisphosphonate
• Paget's disease of bone
• Osteoporosis
• Osteonecrosis of the jaw