zoledronic acid (Rx)

Brand and Other Names:Reclast, Zometa
  • Print

Dosing & Uses

AdultPediatric

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

Next:

Interactions

Interaction Checker

and zoledronic acid

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            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.

              Previous
              Next:

              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

              Previous
              Next:

              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

              Previous
              Next:

              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.

              Previous
              Next:

              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%)

              Previous
              Next:

              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)

              Previous
              Next:

              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 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.

              Previous
              Next:

              Patient Handout

              A Patient Handout is not currently available for this monograph.
              Previous
              Next:

              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

              To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

              Adding plans allows you to:

              • View the formulary and any restrictions for each plan.
              • Manage and view all your plans together – even plans in different states.
              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
              Additional Offers
              Email to Patient

              From:

              To:

              The recipient will receive more details and instructions to access this offer.

              By clicking send, you acknowledge that you have permission to email the recipient with this information.

              Email Forms to Patient

              From:

              To:

              The recipient will receive more details and instructions to access this offer.

              By clicking send, you acknowledge that you have permission to email the recipient with this information.

              Previous
              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.