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Pronunciation:

(tye LOO droe nate)

U.S. Brand Names:

Skelid®

Synonyms:

Tiludronate Disodium

Generic Available:

Use:

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

Pregnancy Risk Factor:

Pregnancy Implications:

Teratogenic and nonteratogenic embryo/fetal effects have been reported in animal studies. There are no adequate and well-controlled studies in pregnant women. Bisphosphonates are incorporated into the bone matrix and gradually released over time. Theoretically, there may be a risk of fetal harm when pregnancy follows the completion of therapy. Based on limited case reports with pamidronate, serum calcium levels in the newborn may be altered if administered during pregnancy.

Lactation:

Excretion in breast milk unknown/use caution

Contraindications:

Hypersensitivity to bisphosphonates or any component of the formulation

Warnings/Precautions:

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

Adverse Reactions:

The following events occurred >2% and at a frequency > placebo:

1% to 10%:

Cardiovascular: Chest pain (3%), edema (3%)

Central nervous system: Dizziness (4%), paresthesia (4%)

Dermatologic: Rash (3%), skin disorder (3%)

Gastrointestinal: Nausea (9%), diarrhea (9%), heartburn (5%), vomiting (4%), flatulence (3%)

Neuromuscular & skeletal: Arthrosis (3%)

Ocular: Cataract (3%), conjunctivitis (3%), glaucoma (3%)

Respiratory: Rhinitis (5%), sinusitis (5%), cough (3%), pharyngitis (3%)

<1% (Limited to important or life-threatening): Stevens-Johnson syndrome

Postmarketing and/or case reports: Osteonecrosis

Overdosage/Toxicology:

Hypocalcemia is a potential consequence of overdose. Treatment is supportive.

Drug Interactions:

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

Ethanol/Nutrition/Herb Interactions:

Food: 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.

Stability:

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

Mechanism of Action:

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.

Pharmacodynamics/Kinetics:

Onset of action: Delayed, may require several weeks

Absorption: Rapid

Distribution: Widely to bone and soft tissue

Protein binding: 90%, primarily to albumin

Metabolism: Little, if any

Bioavailability: 6%; reduced by food

Half-life elimination: Healthy volunteers: 50 hours; Pagetic patients: 150 hours

Time to peak, plasma: ~2 hours

Excretion: Urine (60% as unchanged drug) within 13 days

Dosage:

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

Adults: Oral: 400 mg (2 tablets of tiludronic acid) daily for a period of 3 months; allow an interval of 3 months to assess response

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

Dosing adjustment in hepatic impairment: Adjustment is not necessary

Administration:

Administer as a single oral dose, take with 6-8 oz of plain water. Beverages other than plain water (including mineral water), food, and some medications (see Drug Interactions) are likely to reduce the absorption of tiludronate. Do not take within 2 hours of food. Take calcium or mineral supplements at least 2 hours before or after tiludronate. Take aluminum- or magnesium-containing antacids at least 2 hours after taking tiludronate. Do not take tiludronate within 2 hours of indomethacin.

Dietary Considerations:

Do not take within 2 hours of food.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Do not remove medication from foil strip until ready to be used. Take as directed, on an empty stomach with a full glass of water. Do not take within 2 hours of food, aspirin, indomethacin, or calcium-, magnesium-, or aluminum-containing medications. Stay in sitting or standing position for 30 minutes following administration. Consult prescriber to determine possibility of lifestyle changes (eg, decreased smoking, decreased alcohol intake, dietary supplements of calcium, or increased dietary vitamin D). May cause mild skin rash; or 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; or unusual weakness or increased perspiration. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

May cause dizziness, anxiety, or nervousness

Mental Health: Effects on Psychiatric Treatment:

None reported

Dosage Forms:

Tablet, tiludronic acid: 200 mg [equivalent to 240 mg tiludronate disodium]

International Brand Names:

Skelid® (ES)

References

French AE, Kaplan N, Lishner M, et al, "Taking Bisphosphonates During Pregnancy,"Can Fam Physician, 2003, 49:1281-2.

Ruggiero SL, Mehrotra B, Rosenberg TJ, et al, "Osteonecrosis of the Jaws Associated With the Use of Bisphosphonates: A Review of 63 Cases,"J Oral Maxillofac Surg, 2004, 62(5):527-34.

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