Zoledronic acid
RECLAST
What it isIntravenous FPPS-inhibiting bisphosphonate; osteoporosis, Paget disease, and skeletal events in malignancy.
Why this oneA single intermittent infusion removes oral-adherence and esophagitis problems while reducing vertebral and hip fractures.
What limits itAn acute-phase reaction is common after the first infusion; check renal function and calcium, and address dental risk before oncology use.
FDA-approved for
- osteoporosis/bone metastases (2001)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Postmenopausal osteoporosis (treatment) | Women | 5 mg IV once yearly | ||
| Postmenopausal osteoporosis (prevention) | Women | 5 mg IV once every 2 years | ||
| Osteoporosis in men | Men | 5 mg IV once yearly | ||
| Glucocorticoid-induced osteoporosis (treatment/prevention) | Adults | 5 mg IV once yearly | ||
| Paget's disease of bone | Adults | 5 mg IV single infusion |
Renal Contraindicated if CrCl <35 mL/min or acute renal impairment; no adjustment needed if CrCl ≥35 mL/min. Calculate CrCl before each dose.
Hepatic Not hepatically metabolized; no clinical data in hepatic impairment
Single dose must not exceed 5 mg; infusion duration ≥15 min
Instructions
- Infuse IV over ≥15 min at a constant rate; follow with a 10 mL normal saline flush
- Ensure adequate hydration before administration
- Acetaminophen after the infusion may reduce acute-phase reaction symptoms
- Osteoporosis: supplement calcium/vitamin D if intake inadequate. Paget's: 1500 mg elemental calcium + 800 IU vitamin D daily, especially the 2 weeks after dosing
- Perform a routine oral examination before initiating
- Do not allow contact with calcium or other divalent-cation solutions; use a separate infusion line
Contraindications
- Hypocalcemia
- CrCl <35 mL/min or evidence of acute renal impairment (increased risk of renal failure)
Cautions
- Hypocalcemia — correct before treatment; ensure calcium/vitamin D supplementation
- Renal impairment/acute renal failure — monitor CrCl before each dose, hydrate, avoid in dehydration
- Osteonecrosis of the jaw — oral exam before treatment
- Atypical femoral (and other) fractures — evaluate thigh/groin pain
- Severe, occasionally incapacitating bone/joint/muscle pain
- Bronchoconstriction in aspirin-sensitive patients
- Do not give to patients receiving Zometa (same active ingredient)
Adverse reactions
- Pyrexia
- Myalgia
- Arthralgia
- Headache
- Pain in extremity
- Influenza-like illness
- Nausea
- Vomiting
- Diarrhea
- Acute-phase reaction
Pregnancy Insufficient human data; discontinue when pregnancy is recognized. Animal studies show fetal skeletal harm; bisphosphonate is retained in bone for years.
Lactation No data on presence in human milk or effects on the breastfed infant.
NO BOXED WARNINGS
Principal riskAcute-phase reaction after the first infusion
Cost, est. cash$20–$1,500/dose or month
Generic entry2013
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Zoledronic acid ballicule
