Zoledronic acid (Zometa)

Generic Name: Zoledronic acid

Zometa contains zoledronic acid, a bisphosphonic acid which is an inhibitor of osteoclastic bone resorption. Zoledronic acid is designated chemically as (1-Hydroxy-2-imidazol-1-yl-phosphonoethyl) phosphonic acid monohydrate and its structural formula is:

Zoledronic acid is a white crystalline powder. Its molecular formula is C5H10N2O7P2•H2O and its molar mass is 290.1g/mol. Zoledronic acid is highly soluble in 0.1N sodium hydroxide solution, sparingly soluble in water and 0.1N hydrochloric acid, and practically insoluble in organic solvents. The pH of a 0.7% solution of zoledronic acid in water is approximately 2.0. Zometa is available in 100 mL bottles as a sterile liquid ready-to-use solution for intravenous infusion and in 5 mL vials as a sterile liquid concentrate solution for intravenous infusion.

  • Each 100 mL ready-to-use bottle contains 4.264 mg zoledronic acid monohydrate, corresponding to 4 mg zoledronic acid on an anhydrous basis, 5100 mg of mannitol, USP, water for injection, and 24 mg of sodium citrate, USP.
  • Each 5 mL concentrate vial contains 4.264 mg zoledronic acid monohydrate, corresponding to 4 mg zoledronic acid on an anhydrous basis, 220 mg of mannitol, USP, water for injection, and 24 mg of sodium citrate, USP.

Inactive Ingredients: mannitol, USP, as bulking agent, water for injection, and sodium citrate, USP, as buffering agent.

No health feed found.

The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

Zoledronic acid is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer, as well as for treating osteoporosis. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.

It can be given at home rather than in hospital. Such use has shown safety and quality-of-life benefits in people with breast cancer and bone metastases.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

More common

  • Agitation
  • black, tarry stools
  • blurred vision
  • chest pain
  • chills
  • coma
  • confusion
  • convulsions
  • cough
  • depression
  • difficult or labored breathing
  • dizziness
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • fever
  • irregular heartbeat
  • irritability
  • lack or loss of strength
  • lethargy
  • lower back or side pain
  • muscle pain or cramps
  • muscle trembling or twitching
  • nausea or vomiting
  • numbness and tingling around the mouth, fingertips, or feet
  • painful or difficult urination
  • pale skin
  • rapid weight gain
  • seizures
  • shaking of the hands, arms, feet, legs, or face
  • skin rash, cracks in the skin at the corners of the mouth, or soreness or redness around the fingernails and toenails
  • sore throat
  • sores, ulcers, or white spots on the lips or mouth
  • stupor
  • sudden sweating
  • swollen glands
  • tightness in the chest
  • trouble breathing with exercise
  • unusual bleeding or bruising
  • unusual tiredness or weakness

Less common

  • Feeling of constant movement of self or surroundings
  • muscle cramps in the hands, arms, feet, legs, or face
  • muscle spasms
  • neck pain
  • pounding in the ears
  • rapid breathing
  • sensation of spinning
  • slow or fast heartbeat
  • sunken eyes
  • tingling of the hands or feet
  • tremor

Incidence not known

  • Blurred vision or other change in vision
  • decreased frequency or amount of urine
  • decreased vision
  • eye pain
  • eye tenderness
  • heavy jaw feeling
  • increased blood pressure
  • increased tearing
  • increased thirst
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • loosening of a tooth
  • pain, swelling, or numbness in the mouth or jaw
  • redness of the eye
  • sensitivity of the eye to light
  • severe eye pain
  • swelling of the face, hands, fingers, lower legs, or ankles
  • weight gain

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Abdominal or stomach pain
  • back pain
  • bad, unusual, or unpleasant (after) taste
  • bladder pain
  • blistering, crusting, irritation, itching, or reddening of the skin
  • bloody or cloudy urine
  • bone pain
  • burning, crawling, itching, numbness, prickling, “pins and needles”, or tingling feelings
  • change in taste
  • constipation
  • cracked lips
  • cracked, dry, or scaly skin
  • diarrhea
  • difficulty with swallowing
  • discouragement
  • dry mouth
  • ear congestion
  • feeling sad or empty
  • frequent urge to urinate
  • hair loss or thinning hair
  • headache
  • hyperventilation
  • joint pain or swollen joints
  • loss of appetite
  • loss of interest or pleasure
  • loss of voice
  • muscle stiffness or difficulty with moving
  • nasal congestion or runny nose
  • pain, swelling, or redness in the joints
  • partial loss of feeling
  • seeing, hearing, or feeling things that are not there
  • sleepiness or unusual drowsiness
  • swelling or inflammation of the mouth
  • thirst
  • trouble concentrating
  • trouble sleeping
  • unusually cold, shivering
  • vomiting
  • weight loss

Less common

  • Acid or sour stomach
  • belching
  • heartburn
  • indigestion
  • red streaks on the skin
  • stomach discomfort or upset
  • swelling, tenderness, or pain at the injection site
  • unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness
  • wrinkled skin

Rare

  • Burning, dry, or itching eyes
  • discharge or excessive tearing
  • redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
  • throbbing pain

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Adult

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

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Anemia or
  • Bleeding problems or
  • Cancer, history of or
  • Dental or tooth problems or
  • Dental procedures or
  • Poor oral hygiene, or
  • Surgery (eg, dental surgery)—May increase risk for severe jaw problems.
  • Asthma, aspirin-sensitive or
  • Heart disease or
  • Kidney disease or
  • Mineral imbalance (eg, high or low calcium, magnesium, phosphorus, or potassium in the blood)—Use with caution. May make these conditions worse.
  • Bowel resection or
  • Parathyroid disease (eg, hypoparathyroidism) or
  • Parathyroid surgery or
  • Stomach absorption problems or
  • Thyroid surgery—These conditions may increase your risk of having hypocalcemia (low levels of calcium in the blood).
  • Dehydration (not enough water or fluid in your body)—May increase risk of severe kidney problems.
  • Hypocalcemia (low calcium in the blood) or
  • Kidney disease, severe (eg, kidney failure)—Should not be used in patients with these conditions.

Your doctor may also give you vitamins containing Vitamin D and calcium. Tell your doctor if you are unable to take these supplements.

Drink extra fluids so you will pass more urine while you are using this medicine. This will keep your kidneys working well and help prevent kidney problems. However, it is very important to not drink too much liquid. Talk to your doctor about the right amount of liquids for you.

This medicine comes with a Medication Guide. It is very important that you read and understand this information. Be sure to ask your doctor about anything you do not understand.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Zoledronic acid injection is not indicated for use in children.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of zoledronic acid injection in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution in patients receiving zoledronic acid injection.

Pregnancy

Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breastfeeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

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