Dosing & Uses
Dosage Forms & Strengths
tablet
- 200mg
Paget's Disease
400 mg PO qDay for 3 months
Renal Impairment
ClCr< 30 mL/min: Not recommended
Not removed by dialysis
Administration
Take with 6-8 oz plain water
2 hours before or after food
Other Indications & Uses
Off-label: Osteoporosis
Safety & efficacy not established
Paget's disease
400 mg PO qDay for 3 months
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (15)
- aluminum hydroxide
aluminum hydroxide decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- calcium acetate
calcium acetate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- calcium carbonate
calcium carbonate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- calcium chloride
calcium chloride decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- calcium citrate
calcium citrate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- calcium gluconate
calcium gluconate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- deferasirox
deferasirox, tiludronate. Other (see comment). Use Caution/Monitor. Comment: Combination may increase GI bleeding, ulceration and irritation. Use with caution.
- magnesium supplement
magnesium supplement will decrease the level or effect of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Formation of a chelate reduces absorption of the drug through intestinal tract; administer magnesium 2hr before or 2hr after the bisphosphonate derivative
- selenium
selenium will decrease the level or effect of tiludronate by cation binding in GI tract. Modify Therapy/Monitor Closely. Avoid administering polyvalent cations 2 hr before or after tiludronate.
- sodium bicarbonate
sodium bicarbonate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- sodium citrate/citric acid
sodium citrate/citric acid decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- sodium sulfate/?magnesium sulfate/potassium chloride
sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of tiludronate by Other (see comment). Use Caution/Monitor. Comment: Coadministration with medications that cause fluid and electrolyte abnormalities may increase the risk of adverse events of seizure, arrhythmias, and renal impairment.
- sodium sulfate/potassium sulfate/magnesium sulfate
sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of tiludronate by Other (see comment). Use Caution/Monitor. Comment: Coadministration with medications that cause fluid and electrolyte abnormalities may increase the risk of adverse events of seizure, arrhythmias, and renal impairment.
- trimagnesium citrate anhydrous
trimagnesium citrate anhydrous decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.
- voclosporin
voclosporin, tiludronate. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Coadministration with drugs associated with nephrotoxicity may increase the risk for acute and/or chronic nephrotoxicity.
Minor (6)
- aspirin
aspirin decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- aspirin rectal
aspirin rectal decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate decreases levels of tiludronate by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- foscarnet
foscarnet increases effects of tiludronate by pharmacodynamic synergism. Minor/Significance Unknown. Risk of severe hypocalcemia.
- indomethacin
indomethacin increases levels of tiludronate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- teriparatide
teriparatide, tiludronate. Other (see comment). Minor/Significance Unknown. Comment: No advantage to bone density with combined treatment.
Adverse Effects
1-10%
Dizziness (4%)
Edema (2.7%)
Insomnia
Flushing
Hypertension
Chest pain
Frequency Not Defined
Back pain
Musculoskeletal pain
Diarrhea
Dyspepsia
Flushing
Headache
Nausea
Rhinitis
Sinusitis
URI
Warnings
Contraindications
Hypersensitivity
Inability to stand or sit upright for at least 30 minutes
Abnormalities of the esophagus which delay emptying such as stricture or achalasia
Hypocalcemia
Cautions
Risk of esophageal adverse effects, including esophagitis, esophageal ulceration/erosion, or esophageal bleeding with strictures or perforation
Following therapy, allow 3 months interval to assess response
Not recommended in severe renal failure (CrCl <30 mL/min)
Take with plain water only-NOT coffee, juice or mineral water; sit or stand upright for at least 30 minutes after administration
Risk of osteonecrosis of jaw
Food reduces bioavailability
Risk of severe bone, joint &/or muscle pain
Avoid concurrent multivalent cation-containing medicines or food
Esophageal cancer risk (July 21, 2011 FDA safety communication)
- Conflicting findings exist from studies evaluating the risk of esophageal cancer with oral bisphosphonates
- Esophagitis and other esophageal events have been reported, particularly in patients who do not follow the specific directions for use of oral bisphosphonates (eg, sit up or stand after administration, take with full glass of water)
- An ongoing review of data from published studies to evaluate whether use of oral bisphosphonate drugs is associated with an increased risk of cancer of the esophagus is currently being conducted by the FDA
- The FDA has not concluded that taking an oral bisphosphonate drug increases the risk of esophageal cancer
- There are insufficient data to recommend endoscopic screening of asymptomatic patients
- FDA will continue to evaluate all available data supporting the safety and effectiveness of bisphosphonate drugs and will update the public when more information becomes available
- Instruct patients to contact their healthcare provider if they develop symptoms of esophagitis (eg, swallowing difficulties, chest pain, new or worsening heartburn, trouble or pain when swallowing)
Pregnancy & Lactation
Pregnancy Category: C
Lactation: not known if crosses in to breast milk, use caution
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Bisphosphanate that inhibits bone resorption via actions on osteoclast activity, leading to an indirect increase in bone formation
Pharmacokinetics
Half-Life: 50 (single dosing) -150 hr (repeated dosing)
Onset: 2 days -1 month
Peak Effect: 3 month
Duration: 3-6 months after completion (multiple doses)
Peak plasma time: 2 hr
Bioavailability: 6%; food reduces bioavailability by up to 90%
Protein bound: 90%
Metabolism: None
Excretion: Urine
