tiludronate


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tiludronate

 [ti-loo´drah-nāt]
an inhibitor of bone resorption, administered orally as the disodium salt in treatment of Paget's disease of bone.

tiludronate

(tye-loo-droe-nate) ,

Skelid

(trade name)

Classification

Therapeutic: bone resorption inhibitors
Pharmacologic: biphosphonates
Pregnancy Category: C

Indications

Management of Paget’s disease of the bone in patients with:
  • Serum alkaline phosphatase ≥2 times the upper limit of normal,
  • Symptoms,
  • Risk for complications.

Action

Inhibits resorption of bone by inhibiting osteoclast activity.

Therapeutic effects

Decreased progression of Paget’s disease.

Pharmacokinetics

Absorption: Rapidly but poorly absorbed following oral administration (6% bioavailability).
Distribution: Distributes to bone and soft tissue; subsequently is slowly released from bone.
Protein Binding: 90% protein binding.
Metabolism and Excretion: Excreted mostly in urine.
Half-life: 150 hr.

Time/action profile (blood levels)

ROUTEONSETPEAKDURATION
POunknownwithin 2 hrunknown

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Inability to stand/sit upright for at least 30 min; Severe renal impairment (CCr <30 mL/min).
Use Cautiously in: History of upper GI disorders; Invasive dental procedures, cancer, receiving chemotherapy or corticosteroids, poor oral hygeine, periodontal disease, dental disease, anemia, coagulopathy, infection, or poorly-fitting dentures (may ↑ risk of jaw osteonecrosis); Obstetric / Lactation / Pediatric: Safety not established.

Adverse Reactions/Side Effects

Central nervous system

  • anxiety
  • drowsiness
  • fatigue
  • insomnia
  • nervousness
  • syncope
  • vertigo
  • weakness

Ear, Eye, Nose, Throat

  • cataracts
  • conjunctivitis
  • glaucoma
  • pharyngitis
  • rhinitis
  • sinusitis

Respiratory

  • bronchitis

Cardiovascular

  • chest pain
  • dependent edema
  • hypertension
  • peripheral edema

Gastrointestinal

  • abdominal pain
  • anorexia
  • constipation
  • diarrhea
  • dry mouth
  • dysphagia
  • esophageal ulcer
  • esophagitis
  • flatulence
  • gastric ulcer
  • gastritis
  • nausea
  • tooth disorder
  • vomiting

Genitourinary

  • urinary tract infection

Dermatologic

  • flushing
  • increased sweating
  • pruritus
  • rash
  • skin disorder

Endocrinologic

  • hyperparathyroidism

Fluid and Electrolyte

  • hypocalcemia

Musculoskeletal

  • musculoskeletal pain (most frequent)
  • arthrosis
  • involuntary muscle contractions
  • osteonecrosis (primarily of jaw)
  • pathological fractures

Neurologic

  • paresthesia

Miscellaneous

  • infection

Interactions

Drug-Drug interaction

Absorption is decreased by concurrent administration of calcium supplements, aspirin, or aluminum- or magnesium-containing antacids.Bioavailability is ↑ by concurrent administration of indomethacin.Food ↓ absorption.

Route/Dosage

Oral (Adults) 400 mg/day taken with 8 oz of plain water only, for 3 mo.

Availability

Tablets: 400 mg

Nursing implications

Nursing assessment

  • Paget’s Disease: Assess for symptoms of Paget’s disease (bone pain, headache, decreased visual and auditory acuity, increased skull size).
  • Lab Test Considerations: Monitor alkaline phosphatase prior to and periodically during therapy. Tiluronate is indicated for patients with alkaline phosphatase 2 times the upper limit of normal.

Potential Nursing Diagnoses

Risk for injury (Indications)

Implementation

  • Oral: Administer first thing in the morning with 6–8 oz plain water 30 min prior to other medications, beverages, or food.
    • Calcium supplements, aspirin, or indomethacin should not be taken for 2 hr before or 2 hr after tiludronate; antacids should not be taken for at least 2 hr following tiludronate.

Patient/Family Teaching

  • Instruct patient on the importance of taking exactly as directed, first thing in the morning, 30 min prior to other medications, beverages, or food. Waiting longer than 30 min will improve absorption. Tiluronate should be taken with 6–8 oz plain water (mineral water, orange juice, coffee, and other beverages decrease absorption). If a dose is missed, skip dose and resume the next morning; do not double doses or take later in the day. Do not discontinue without consulting health care professional.
    • Caution patients to remain upright for 30 min following dose to facilitate passage to stomach and minimize risk of esophageal irritation.
    • Advise patient to eat a balanced diet and consult health care professional about the need for supplemental calcium and vitamin D.
    • Encourage patient to participate in regular exercise and to modify behaviors that increase the risk of osteoporosis (stop smoking, reduce alcohol consumption).
    • Advise patient to inform health care professional of tiludronate therapy prior to dental surgery.
    • Advise female patient to notify health care professional if pregnancy is planned or suspected or if she is nursing.

Evaluation/Desired Outcomes

  • Decrease in the progression of Paget’s disease.

tiludronate

/ti·lu·dro·nate/ (ti-loo´drah-nāt) an inhibitor of bone resorption, used as the disodium salt in the treatment of osteitis deformans.

tiludronate

a parathyroid agent (calcium regulator).
indication It is used to treat Paget's disease.
contraindications Factors that prohibit its use include known hypersensitivity to biphosphonates, pathological fractures, colitis, and severe renal disease with creatinine 5 mg/dL. Its use is also contraindicated in children.
adverse effects Adverse effects include dry mouth, gastritis, vomiting, flatulence, gastric ulcers, rhinitis, rales, sinusitis, upper respiratory infection, headache, somnolence, dizziness, anxiety, vertigo, nervousness, involuntary movements, hyperparathyroidism, rash, epidermal necrosis, pruritus, sweating, nephrotoxicity, decreased mineralization of nonaffected bones, and pathological fractures. Common side effects include nausea, diarrhea, and bone pain.
References in periodicals archive ?
Respecto el tratamiento con BP estudios in vitro han demostrado que el tiludronate, bisfosfonato de segunda generacion, inhibe la secrecion de enzimas que degradan la matriz cartilaginosa mediada por IL-1 [beta], de parte de condrocitos y celulas sinoviales, (Emonds-Alt et al.
Patients taking alendronate (Fosamax[R]), risedronate (Actonel[R]), ibandronate (Boniva[R]), etidronate (Didronel[R]), or tiludronate (Skelid[R]) should carefully read and follow the directions on how to take the medication.
Currently available bisphosphonates include alendronate (Fosamax), ibandronate (Boniva), risedronate (Actonel), etidronate (Didronel), pamidronate (Aredia), tiludronate (Skelid) and zoledronic acid (Reclast, Zometa).
Primary Nitrogen Indication Containing Dose Etidronate (Didronel [R]) Paget's Disease No 300-750 mg Procter & Gamble daily for Pharmaceuticals 6 months Tiludronate (Skelid [R]) Paget's Disease No 400 mg daily Sanofi-aventis U.
The bisphosphonates approved by the FDA are alendronate (Fosamax, Fosamax plus D), etidronate (Didronel), ibandronate (Boniva), pamidronate (Aredia), risedronate (Actonel, Actonel with calcium), tiludronate (Skelid), and zoledronic acid (Reclast, Zometa).
Bisphosphonate products approved by the FDA but not included in the safety review are etidronate (Didronel, by Procter & Gamble Pharmaceuticals), pamidronate (Aredia, by Novartis), and tiludronate (Skelid, by SanofiAventis US).
Bisphosphonates: The FDA has approved six bisphosphonates to prevent bone loss and fractures in postmenopausal women: alendronate (Fosamax), etidronate (Didronel), ibandronate (Boniva), risedronate (Actonel), tiludronate (Skelid), and zoleldronic acid (Reclast, Zometra).
In order of increasing potency, these are etidronate disodium, tiludronate disodium, pamidronate disodium, alendronate sodium and risedronate sodium.
Other drugs in the BIS class are taken by mouth (tablets) and include alendronate (Fosamax), risedronate (Actonel), etidronate (Didronel), tiludronate (Skelid) and a new BIS approved for once per month dosing, ibandronate (Boniva).
Variable efficacy of bone remodeling biochemical markers in the management of patients with Paget's disease of bone treated with tiludronate.
Additional biphosphonates under investigation include tiludronate, pamidronate, and zoledronate.