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Tiludronate Disodium

Pronunciation: TYE-loo-DROE-nate dye-SOE-dee-um
Class: Bisphosphonate

Trade Names

- Tablets 200 mg (equiv. to 240 mg of tiludronate disodium)


Inhibits normal and abnormal bone resorption.



Rapidly absorbed. Tiludronate bioavailability is 6%; bioavailability is reduced by 90% when administered with or 2 h after breakfast. In clinical studies, efficacy was seen when dosed at least 2 h before or after meals. Tiludronate C max is 3 mg/L; T max occurs with 2 h of dose.


Tiludronate is approximately 90% bound to proteins.


Tiludronate is not metabolized in human liver microsomes and hepatocytes.


The primary route of elimination is in urine. Approximately 60% of a dose is excreted in urine. Tiludronate half-life is 150 h in pagetic patients.

Special Populations

Renal Function Impairment

Tiludronate is not recommended for patients with severe renal failure (CrCl less than 30 mL/min) because of a lack of clinical experience. After administration of a single oral dose equivalent to tiludronic acid 400 mg to patients with CrCl 11 to 18 mL/min, the plasma elimination half-life was approximately 205 h.

Hepatic Function Impairment

Because tiludronate undergoes little or no metabolism, no studies were conducted in subjects with hepatic insufficiency.


Plasma concentrations of tiludronic acid were higher in elderly pagetic patients; however, this difference was not clinically significant.


Tiludronate pharmacokinetics have not been investigated in subjects younger than 18 y of age.


There were no clinically significant differences in plasma concentrations after repeated administration of tiludronate to male and female pagetic patients.


Pharmacokinetic differences due to race have not been studied.

Indications and Usage

Treatment of Paget disease of bone.

Unlabeled Uses

Osteoporosis with spinal cord injury.


Known hypersensitivity to any component of this product; inability to stand or sit upright for at least 30 min.

Dosage and Administration


PO 400 mg every day for 3 mo.

General Advice

  • Should be taken with 6 to 8 oz of plain water. Beverages other than plain water (including mineral water), food, and some medications are likely to reduce the absorption of tiludronate.
  • Should not be taken within 2 h of food. Calcium or mineral supplements, aspirin, and indomethacin should not be taken within 2 h before or 2 h after tiludronate.
  • Aluminum- or magnesium-containing antacids should be taken at least 2 h after taking tiludronate.
  • Following therapy, allow an interval of 3 mo to assess response.
  • Maintain adequate vitamin D and calcium intake.


Store between 59° and 86°F. Do not remove from foil strip until ready for administration.

Drug Interactions

Aluminum salts (eg, aluminum hydroxide), magnesium salts (eg, magnesium hydroxide)

The bioavailability of tiludronate is decreased 60% by some aluminum- or magnesium-containing antacids when administered 1 h before tiludronate. If needed, aluminum and/or magnesium salts should be taken at least 2 h after tiludronate.


Aspirin may decrease bioavailability of tiludronate by up to 50% when taken 2 h after tiludronate. Separate the administration times by at least 2 h.

Calcium (eg, calcium carbonate)

The bioavailability of tiludronate is decreased 80% by calcium when calcium and tiludronate are administered at the same time. Do not administer calcium salts within 2 h before or after tiludronate.


In single-dose studies, tiludronate bioavailability was reduced by 90% when an oral dose equivalent to 400 mg of tiludronic acid was taken with or 2 h after a standard breakfast compared with the same dose given after an overnight fast and 4 h before a standard breakfast. Tiludronate should not be taken within 2 h of food.


Increases tiludronate bioavailability 2- to 4-fold. Do not administer tiludronate within 2 h of indomethacin.

Adverse Reactions


Hypertension, syncope (1% or more).


Headache (7%); dizziness, paresthesia (4%); anorexia, anxiety, asthenia, fatigue, insomnia, involuntary muscle contractions, nervousness, somnolence (1% or more).


Rash, skin disorder (3%); increased sweating, pruritus (1% or more); Stevens-Johnson syndrome (rare).


Cataract, conjunctivitis, glaucoma (3%).


Diarrhea, nausea (9%); dyspepsia (5%); vomiting (4%); flatulence, tooth disorder (3%); abdominal pain, constipation, dry mouth, gastritis (1% or more).


Back pain (8%); arthralgia, arthrosis (3%).


Rhinitis, sinusitis, upper respiratory tract infection (5%); coughing, pharyngitis (3%); bronchitis (1% or more).


Pain (21%); influenza-like symptoms (4%); chest pain, dependent edema, hyperparathyroidism, infection, peripheral edema, vitamin D deficiency (3%); flushing, fracture pathological, urinary tract infection (1% or more).



Category C .




Safety and efficacy not established.

Renal Function

Not recommended in patients with CrCl less than 30 mL/min.

GI effects

Bisphosphonates may cause local irritation of the upper GI mucosa. Use with caution in patients with active upper GI problems (eg, Barrett esophagus, duodenitis, dysphagia, gastritis, ulcer).

Musculoskeletal pain

Severe and incapacitating bone, joint, and/or muscle pain have been reported.


Osteonecrosis, primarily of the jaw, has been reported in patients receiving bisphosphonates.



Acute renal failure, death, hypocalcemia.

Patient Information

  • Instruct patient to take drug with 6 to 8 oz of plain water. Advise patient to not use any other beverage (eg, mineral water).
  • Advise patient not to lie down for at least 30 min after taking tiludronate.
  • Instruct patient to avoid eating 2 h before and 2 h after taking medication since absorption of drug is reduced by food.
  • Instruct patient to maintain adequate intake of vitamin D and calcium.
  • Advise patient to take calcium or mineral supplements 2 h before or 2 h after tiludronate.
  • Advise patient to take aluminum- or magnesium-containing antacids at least 2 h after tiludronate.
  • Advise patients taking aspirin or indomethacin to take these 2 h before or 2 h after tiludronate.
  • Advise patient to not remove medication from foil strip until just before administration.

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