Dosing & Uses
Dosage Forms & Strengths
IV injectable solution
- 4mg/5mL (5mL)
- 5mg/100mL
Hypercalcemia of Malignancy
Zometa: No more than 4 mg IV (infused over >15 minutes) once; may be repeated in 7 days
Monitor serum calcium, and wait at least 7 days before considering retreatment
Multiple Myeloma; Bone Metastases From Solid Tumors
Zometa: 4 mg IV (infused over >15 minutes) every 3-4 weeks
Osteoporosis
Reduction in incidence of fractures (hip, vertebral, and nonvertebral osteoporosis-related fractures)
Prevention in postmenopausal women
- Reclast: 5 mg IV over >5 minutes every 2 years
Treatment in men and postmenopausal women
- Reclast: 5 mg IV over >15 minutes every year
Glucocorticoid-Induced Osteoporosis
Treatment and prevention
Reclast: 5 mg IV over >15 minutes every year; supplemented with elemental calcium and vitamin D
Paget Disease
Reclast: 5 mg IV over >15 minutes once; supplemented with elemental calcium and vitamin D
Dosage Modifications
Renal impairment (Zometa)
- CrCl >60 mL/min: 4 mg
- CrCl 50-60 mL/min: 3.5 mg
- CrCl 40-49 mL/min: 3.3 mg
- CrCl 30-39 mL/min: 3 mg
- CrCl <30 mL/min: Not recommended
Renal impairment (Reclast)
- CrCl >35 mL/min: No adjustment needed
- CrCl <35 mL/min: Contraindicated
Hepatic impairment
- Safety and efficacy not established
Complex Regional Pain Syndrome (Orphan)
Orphan designation for treatment of complex regional pain syndrome (CRPS)
Sponsors
- Axsome Therapeutics, Inc.; 45 Rockefeller Plaza, Suite 2000; New York, NY 10111
- Thar Pharmaceuticals; 150 Gamma Drive; Pittsburgh, PA 15238
Glioma (Orphan)
Orphan designation for treatment of glioma
Sponsor
- Laboratorio Italiano Biochimico Farmaceutico Lisapharma SpA; Via Licinio 11; Erba (CO), Italy
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- human parathyroid hormone, recombinant
zoledronic acid decreases effects of human parathyroid hormone, recombinant by Other (see comment). Contraindicated. Comment: Coadministration of bisphosphonates with rhPTH leads to reduction in rhPTH's calcium sparing effect, which can interfere with the normalization of serum calcium.
Serious - Use Alternative (0)
Monitor Closely (13)
- aluminum hydroxide
aluminum hydroxide decreases levels of zoledronic acid 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 zoledronic acid 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 zoledronic acid 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 zoledronic acid 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 zoledronic acid 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 zoledronic acid by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 30 minutes.
- dichlorphenamide
dichlorphenamide and zoledronic acid both decrease serum potassium. Use Caution/Monitor.
- peramivir
zoledronic acid increases levels of peramivir by decreasing renal clearance. Use Caution/Monitor. Caution when peramivir coadministered with nephrotoxic drugs.
- sodium bicarbonate
sodium bicarbonate decreases levels of zoledronic acid 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 zoledronic acid 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 zoledronic acid 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 zoledronic acid 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.
- voclosporin
voclosporin, zoledronic acid. 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 (17)
- amikacin
amikacin, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- aspirin
aspirin decreases levels of zoledronic acid by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- aspirin rectal
aspirin rectal decreases levels of zoledronic acid 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 zoledronic acid by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- bumetanide
bumetanide, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- entecavir
zoledronic acid, entecavir. Either increases effects of the other by decreasing renal clearance. Minor/Significance Unknown. Coadministration with drugs that reduce renal function or compete for active tubular secretion may increase serum concentrations of either entecavir or the coadministered drug.
- ethacrynic acid
ethacrynic acid, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- foscarnet
foscarnet increases effects of zoledronic acid by pharmacodynamic synergism. Minor/Significance Unknown. Risk of severe hypocalcemia.
- furosemide
furosemide, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- gentamicin
gentamicin, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- indomethacin
indomethacin increases levels of zoledronic acid by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- neomycin PO
neomycin PO, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- paromomycin
paromomycin, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- streptomycin
streptomycin, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- teriparatide
teriparatide, zoledronic acid. Other (see comment). Minor/Significance Unknown. Comment: No advantage to bone density with combined treatment.
- tobramycin
tobramycin, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
- torsemide
torsemide, zoledronic acid. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive hypocalcemia.
Adverse Effects
>10%
Bone pain (55%)
Nausea (29-46%)
Fever (32-44%)
Fatigue (39%)
Anemia (22-33%)
Vomiting (14-32%)
Constipation (27-31%)
Dyspnea (22-27%)
Diarrhea (17-24%)
Anorexia (9-22%)
Arthralgia (5-21%)
Headache (5-19%)
Dizziness (18%)
Insomnia (15-16%)
Urinary tract infection (UTI; 12-14%)
Anxiety (11-14%)
Hypophosphatemia (5-14%)
Hypokalemia (12%)
Hypotension (11%)
Hypomagnesemia (11%)
Rash (11%)
Frequency Not Defined
Ocular inflammation (eg, uveitis, scleritis, episcleritis, conjunctivitis, iritis, orbital inflammation)
Postmarketing Reports
Ocular: Uveitis, scleritis, episcleritis, conjunctivitis, iritis, blurred vision, orbital inflammation (including orbital edema)
CNS: Taste disturbance, hyperesthesia, tremor
GI: Dry mouth
Skin: Increased sweating
Musculoskeletal: Muscle cramps, osteonecrosis of jaw, pain, atypical subtrochanteric and diaphyseal femoral fractures
Osteonecrosis of other bones including femur, hip, knee, ankle, wrist and humerus
Cardiovascular: Hypertension, bradycardia, hypotension (associated with syncope or circulatory collapse, primarily in patients with underlying risk factors)
Acute-phase reaction (≤3 days after administration) with symptoms including pyrexia, fatigue, bone pain or arthralgias, myalgias, chills, flulike illness, arthritis with subsequent joint swelling
Hypersensitivity: Bronchoconstriction or bronchospasm, interstitial lung disease, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis
Renal: Hematuria, proteinuria
General disorders and administration site: Weight increase, flulike illness (pyrexia, asthenia, fatigue or malaise) persisting for >30 days
Laboratory abnormalities: Hyperkalemia, hypernatremia
Acqured Fanconi syndrome
Warnings
Contraindications
Pregnancy
All indications: Hypersensitivity, including rare cases of urticaria, angioedema, and anaphylactic reaction or shock
Nononcologic uses: Hypocalcemia, severe renal impairment (CrCl <35 mL/min or evidence of acute renal impairment)
Cautions
Assess renal function before and after treatment; if renal function is decreased after treatment, withhold additional treatment until it returns to within 10% of baseline
Before each Reclast dose, calculate CrCl on basis of actual body weight, using Cockcroft-Gault formula
Other risks for renal impairment include coadministration of zoledronic acid with nephrotoxic or diuretic medications, severe dehydration before or after zoledronic acid administration, and advanced age
Previous renal insufficiency (serum creatinine >3 mg/dL [265 mmol/L]), hepatic insufficiency, musculoskeletal pain
Infuse over ≥15 minutes; faster infusion increases renal toxicity
May cause significant risk of hypocalcemia (seizures, tetany, and numbness); hypocalcemia must be corrected before initiation of therapy; adequately supplement patients with calcium and vitamin D; monitor serum calcium closely with concomitant administration of other drugs known to cause hypocalcemia to avoid severe or life-threatening hypocalcemia
Use with caution in aspirin-sensitive asthma; may cause bronchoconstriction
Increased risk of osteonecrosis of jaw (advise patients against dental work); reported predominantly in cancer patients treated with IV bisphosphonates, including zoledronic acid; many patients were also receiving chemotherapy and corticosteroids which may be risk factors; risk may increase with duration of exposure to bisphosphonates; perform preventive dental exams before initiating therapy; avoid invasive dental procedures; monitor diabetic patients carefully
Cases of osteonecrosis (primarily involving the jaw but also of other anatomical sites including hip, femur and external auditory canal) reported predominantly in cancer patients
Risk of osteonecrosis of the jaw may increase with duration of exposure to bisphosphonates
Possible increased risk for atypical subtrochanteric and diaphyseal femur fractures; consider periodic reevaluation of need for continued bisphosphonate therapy, particularly if treatment lasts >5 years
If patients are receiving Zometa, they should not receive Reclast
Severe bone, joint, and muscle pain may occur; withhold future doses of zoledronic acid if severe symptoms occur
Rehydrate patients with hypercalcemia of malignancy prior to administration of zoledronic acid injection and monitor electrolytes during treatment
Women of childbearing age should be advised of potential hazard to fetus and avoid becoming pregnant
Femur Fractures reported; patients with thigh or groin pain should be evaluated to rule out a femoral fracture
Severe bone, joint, and muscle pain may occur; withhold future doses of reclast if severe symptoms occur
Pregnancy & Lactation
Pregnancy
There are no available data in pregnant women to inform the drug-associated risk
Bisphosphonates are incorporated into bone matrix and are gradually released over periods of weeks to years; there may be a risk of fetal harm (e.g., skeletal and other abnormalities) if a woman becomes pregnant after completing a course of bisphosphonate therapy; advise pregnant women and females of reproductive potential of the potential risk to a fetus
Verify pregnancy status of females of reproductive potential prior to initiation of therapy
Therapy can cause fetal harm when administered to a pregnant woman; drug binds to bone long term and may be released over weeks to years; advise females of reproductive potential to use effective contraception during and after therapy
Based on animal studies, therapy may impair fertility in females of reproductive potential
Animal data
- Based on findings from animal studies and its mechanism of action, drug can cause fetal harm when administered to a pregnant woman; in animal reproduction studies, administration of drug to pregnant rats during organogenesis resulted in fetal malformations and embryo-fetal lethality at maternal exposures that were greater than or equal to 2.4 times the human clinical exposure based on AUC
Lactation
Not known whether drug is present in human milk, or whether it affects milk production, or breastfed child; drug binds to bone long term and may be released over weeks to years
Consider developmental and health benefits of breast-feeding along with the mother’s clinical need for therapy and any potential adverse effects on breast-fed child from drug or from underlying maternal condition
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
Bisphosphonate; inhibits bone resorption via actions on osteoclast activity, leading to indirect increase in bone density
Absorption
Onset: Hypercalcemia of malignancy, 4-7 days; osteolytic bone metastases, 1 week
Duration: 32 days
Distribution
Protein bound: 28-53%
Metabolism
Not metabolized
Elimination
Half-life: 146 hr (terminal)
Renal clearance: 66 mL/min
Total body clearance: 5.6 L/hr
Excretion: Urine (39% as unchanged drug) within 24 hr, feces (<3%)
Administration
IV Incompatibilities
Calcium-containing solutions
IV Preparation
Zometa: Reconstitute powder with 5 mL SWI; once powder is fully dissolved, dilute further in 100 mL NS or D5W before administering
Infusion of solution must be completed within 24 hours of initial reconstitution
IV Administration
Zometa: Infuse over ≥15 minutes, in line separate from other medications
Reclast: Infuse over ≥15 minutes, using ready-to-use infusion solution
Ensure appropriate hydration, especially in patients on diuretics
Storage
Zometa: Before dilution, store vials at 25°C (77°F); after final dilution, use solution immediately or store at 2-8°C (36-46°F)
Reclast: Store at 25°C (77°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  | |
| zoledronic acid intravenous - | 4 mg/5 mL vial |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
zoledronic acid intravenous
ZOLEDRONIC ACID - INJECTION
(ZOLE-eh-dron-ick)
COMMON BRAND NAME(S): Zometa
USES: This medication is used to treat high blood calcium levels (hypercalcemia) that may occur with cancer. Zoledronic acid is also used with cancer chemotherapy to treat bone problems that may occur with multiple myeloma and other types of cancer (such as breast, lung) that have spread to the bones. Zoledronic acid belongs to a class of drugs known as bisphosphonates. It lowers high blood calcium levels by reducing the amount of calcium released from your bones into your blood. It also works by slowing the breakdown of your bones by cancer to prevent bone fractures.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start receiving zoledronic acid and each time you get a treatment. If you have any questions, ask your doctor or pharmacist.This medication is given by injection into a vein as directed by your doctor, usually over at least 15 minutes. The dosage is based on your medical condition (including your kidney function) and response to treatment.If you are giving this medication to yourself at home, learn all preparation and usage instructions from your health care professional. Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Learn how to store and discard medical supplies safely.Avoid mixing zoledronic acid with IV fluids that have calcium in them (such as Ringer's solution, Hartmann's solution, parenteral nutrition-TPN/PPN). Talk to your pharmacist for more details.For the treatment of high blood calcium levels, fluids are usually given through a vein before you receive this medication. To decrease the chance of kidney problems, drink plenty of fluids during treatment unless otherwise directed by your doctor. It takes at least 7 days after a dose to get the full benefit of this drug. The dose may need to be repeated depending on your blood calcium levels.For the treatment of multiple myeloma and bone problems caused by the spread of cancer, this medication is usually given every 3 to 4 weeks or as directed by your doctor. You may also be instructed to take calcium and vitamin D supplements each day.
SIDE EFFECTS: Dizziness, headache, tiredness, or flu-like symptoms (such as fever, chills, muscle/joint aches) may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: increased or severe bone/joint/muscle pain, new or unusual hip/thigh/groin pain, jaw/ear pain, eye/vision problems, numbness/tingling, muscle spasms, irregular heartbeat.Get medical help right away if you have any serious side effects, including: signs of kidney problems (such as change in the amount of urine), seizures.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before using zoledronic acid, tell your doctor or pharmacist if you are allergic to it; or to other bisphosphonates (such as alendronate, risedronate); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, dehydration, aspirin-sensitive asthma.Some people using zoledronic acid may have serious jawbone problems. Your doctor should check your mouth before you start this medication. Tell your dentist that you are using this medication before you have any dental work done. To help prevent jawbone problems, have regular dental exams and learn how to keep your teeth and gums healthy. If you have jaw pain, tell your doctor and dentist right away.Before having any surgery (especially dental procedures), tell your doctor and dentist about this medication and all other products you use (including prescription drugs, nonprescription drugs, and herbal products).This drug may make you dizzy. Alcohol or marijuana (cannabis) can make you more dizzy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).This medication may cause severe kidney problems, especially in the elderly. Consult your doctor or pharmacist for more information. To help prevent harm to your kidneys, drink plenty of fluids unless otherwise directed by your doctor. (See also How to Use section.)Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using zoledronic acid. Zoledronic acid may harm an unborn baby. Ask about reliable forms of birth control while using this medication and after stopping treatment. This medication may stay in your body for many years. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is unknown if this drug passes into breast milk. Because it may harm a nursing infant, breast-feeding while using this drug and after stopping treatment is not recommended. This medication may stay in your body for many years. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.While using this medication, you should not be treated with other bisphosphonates, including other brands of zoledronic acid used to prevent or treat bone loss (osteoporosis).Some products that may interact with this drug include: calcium-containing IV fluids, "water pills" (diuretics such as bumetanide, furosemide).Also tell your doctor or pharmacist of drugs that may be harmful to your kidneys such as: aminoglycoside antibiotics (including gentamicin, tobramycin), amphotericin B, nonsteroidal anti-inflammatory drugs (NSAIDs such as ibuprofen), tacrolimus.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: change in the amount of urine, muscle spasms, muscle weakness, mental/mood changes, irregular heartbeat, seizures.
NOTES: Laboratory and/or medical tests (such as calcium and other blood mineral levels, kidney function tests) will be performed before you start treatment, periodically to monitor your progress, or to check for side effects. Consult your doctor for more details.
MISSED DOSE: It is important to get each dose of this medication as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule. Do not double the dose to catch up.
STORAGE: Consult the product instructions and your pharmacist for storage details. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised April 2022. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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