No

Bisphosphonate Derivative

Treatment of Paget's disease of the bone (1) who have a level of serum alkaline phosphatase (SAP) at least twice the upper limit of normal, (2) or who are symptomatic, (3) or who are at risk for future complications of their disease

C

Hypersensitivity to biphosphonates or any component of the product

Not recommended in patients with severe renal impairment (Cl_cr <30 mL/minute). Use with caution in patients with active upper GI problems (eg, dysphagia, symptomatic esophageal diseases, gastritis, duodenitis, ulcers).

1% to 10%:

Central nervous system: Vertigo, involuntary muscle contractions, anxiety, nervousness

Dermatologic: Pruritus, increased sweating, Stevens-Johnson type syndrome (rare)

Gastrointestinal: Xerostomia, gastritis

Genitourinary: Urinary tract infection

Neuromuscular & skeletal: Weakness, pathological fracture

Respiratory: Bronchitis

Miscellaneous: Increased diaphoresis

Hypocalcemia is a potential consequence of tiludronate overdose. No specific information on overdose treatment is available; dialysis would not be beneficial. Standard medical practices may be used to manage renal insufficiency or hypocalcemia, if signs of these occur.

Decreased effect:

Calcium supplements, antacids interfere with the bioavailability (decreased 60%) when administered 1 hour before tiludronate

Aspirin decreases the bioavailability of tiludronate by up to 50% when taken 2 hours after tiludronate

Increased effect/toxicity: Indomethacin increases the bioavailability of tiludronate two- to fourfold

Do not remove tablets from the foil strips until they are to be used

Inhibition of normal and abnormal bone resorption. Inhibits osteoclasts through at least two mechanisms: disruption of the cytoskeletal ring structure, possibly by inhibition of protein-tyrosine-phosphatase, thus leading to the detachment of osteoclasts from the bone surface area and the inhibition of the osteoclast proton pump.

Onset of effect: Delayed, may require several weeks

Metabolism: Little, if any

Bioavailability: Oral: 6%; reduced by food

Peak plasma concentrations: Within 2 hours

Tiludronate should be taken with 6-8 oz of plain water and not taken within 2 hours of food

Dosing adjustment in renal impairment: Cl_cr <30 mL/minute: Not recommended

Dosing adjustment in hepatic impairment: Adjustment is not necessary

In single-dose studies, the bioavailability of tiludronate was reduced by 90% when an oral dose 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; therefore, do not take within 2 hours of food

May cause dizziness, anxiety, or nervousness

None reported

No information available to require special precautions

No effects or complications reported

In order to be effective this drug must be taken exactly as prescribed: Take 2 hours before or 2 hours after meals, aspirin, indomethacin, or calcium, magnesium, or aluminum containing medications such as antacids. Take with 6-8 oz. of water. Do not remove medication from foil strip until ready to be used. You may experience mild skin rash; abdominal pain, diarrhea, or constipation (report if persistent). Report unresolved muscle or bone pain or leg cramps; acute abdominal pain; chest pain, palpitations, or swollen extremities; disturbed vision or excessively dry eyes; ringing in the ears; persistent rash or skin disorder; unusual weakness or increased perspiration. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.

Tablet, as disodium: 240 mg [tiludronic acid 200 mg]; dosage is expressed in terms of tiludronic acid.